Development of Colon Targeting Drug Delivery System Using Plant Polysaccharide

WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES
Priya et al. World Journal of Pharmacy and Pharmaceutical Sciences

SJIF Impact Factor 6.041
Volume 5, Issue 8, 992-1024 Research Article ISSN 2278 – 4357
DEVELOPMENT OF COLON TARGETING DRUG DELIVERY

SYSTEM USING PLANT POLYSACCHARIDE
Bhanu Priya1*, Shubham Verma2 and Nitin Sharma3
1
IIMT College of Pharmacy, Greater Noida, India.
2
Oxford College of Pharmacy, Ghaziabad, India.
3
Meerut Institute of Engineering & Technology, Meerut.
ABSTRACT
Article Received on
28 May 2016, An attempt has been made to formulate colon targeted tablet dosage
Revised on 17 June 2016,
Accepted on 07 July 2016
form of metronidazole as model drug using natural polysaccharide
DOI: 10.20959/wjpps20168-7342 extracted from Abelmoschus moschatus (Mushkadana, family-
Malvaceae). In preliminary study, extracted polysaccharide was
*Corresponding Author characterized in terms of physicochemical properties. Swelling study at
Bhanu Priya different pH confirmed, utility of plant polysaccharide as a colon
IIMT College of targeting carrier. Core tablets were prepared by changing the
Pharmacy, Greater Noida,
concentration of polysaccharide (10 to 30 mg) and using wet and dry
India.
granulation method. Optimized core tablets were coated by
compression coating with 350 mg polysaccharide (Abelmoschus moschatus). The amount of
metronidazole released from tablets at different time intervals was estimated by UV-
Spectroscopy method. In-vitro dissolution studies revealed that natural polysaccharide based
colon targeted tablet was successfully following the release pattern specific to colon delivery.
It was observed that release of drug was become rapid by decreasing the concentration of
extracted polysaccharide. The result of the studies shows that compression coated
formulation of metronidazole tablets with 350 mg of Abelmoschus moschatus polysaccharide
as coating material is most likely to provide targeting of drug for local action in the colon
owing to its minimal release of the drug in the first 5 hr.
KEYWORDS: Colon, Abelmoschus moschatus, Metronidazole, Natural Polymer, Anti

Amoebic.
www.wjpps.com Vol 5, Issue 8, 2016. 992

INTRODUCTION
An ideal targeted drug delivery system is the one which delivers the drug at a predetermined
rate locally or systemically for a specified period of time. Oral route has been the most
preferred and suitable route for the delivery of drug. Oral route of drug management has
gained consideration in the pharmaceutical field, because of more adaptability in the
designing of dosage form as compared to other dosage form for other routes. Drug delivery
by oral route depends on different variables such as patient, type of delivery system, disease
being treated, duration of therapy and drug properties of the majority of oral controlled drug
delivery system. Oral drug delivery for colon targeting is the most preferred route by a
majority of patients due to its ease of administration.
By definition, colonic delivery refers to targeted delivery of drugs into the lower GI tract,
which occurs primarily in the large intestine (i.e. colon). Targeted drug delivery to the colon
would therefore ensure direct treatment at the disease site, lower dosing and fewer systemic
side effects. In addition to local therapy, the colon can also be utilized as a portal for the entry
of drugs into the systemic circulation. Colon drug delivery is beneficial not only for oral
delivery of peptide and protein drugs but also delivery of those compounds whose molecular
weight is very low and used to treat the colon diseases.[1]
ANATOMY OF COLON
The gastro intestine is divided into three parts- stomach, small intestine, and large intestine.
The large intestine in human is about 1.5 m long. The colon is upper part (five feet) of large
intestine situated mainly in the abdomen. The large intestine extending from the ileocecal
junction to the anus is divided in to three main parts- colon, rectum and anal canal. The colon
is cylindrical tube which is lined by moist, soft pink lining called mucosa and the pathway is
called the lumen. The cecum forms the first part of the colon and leads to the right colon (just
under the liver) followed by the descending colon, sigmoid colon, rectum and anal cana.[2]
Figure 1: Structure of human intestine

Table 1: Anatomical Properties of Gastrointestinal Tract.

Region of gastrointestinal tract Length (cm)
Duodenum 20- 30
Small intestine Jejunum 150- 250
Ileum 200-350
Cecum 6- 9
Ascending colon 20- 25
Descending colon 10- 15
Large intestine Transverse Colon 40- 45
Sigmoid colon 35- 40
Rectum 12
Anal canal 3
pH of colon pH of stomach and small intestine is given below.[3]
Table 2: pH of Stomach and Small Intestine.
Region pH
1- 1.5 (Fasted)
Stomach
2- 3 (fed)
Small intestine
5.0-7.5
Jejunum
6.0-7.3
Illeum
Large intestine
6.4-7.0
Colon
Advantages of colon targeting

1. Direct treatment at the disease site, lower dosing and fewer systemic side effects.
2. Drug absorption may be delay by using colon targeting.
3. Colon targeting specific formulation allow oral administration of protein and peptides
drugs that could be used to prolong the drug delivery.
4. In the treatment of colon diseases.
5. To reduce incidence of adverse effects.
Limitations and challenges in colon targeted drug delivery.[4]

 Multiple manufacturing steps.
 Delivery of colon specific drug delivery system requires well established dissolution
testing method.
 Drug should be in solution form before it arrives in the colon or alternatively.
 Metabolic degradation of drug and colonic performances are also effected by resident
microflora.

 The tight junction and lower surface area in colon can also restrict the drug transport
across the mucosa and into the systemic circulation.
 Before the designing of colon delivery system, the stability of the drug should be known.
The drug may potentially bind in non specific way to dietary residues, mucus or feacal
matter and intestinal secretion.
MATERIALS AND METHOD

Albemoschus moschatus (AM) was procured from the local market of Greater Noida, India. It
was authenticated by the Department of Botany, Banaras Hindu University, Varanasi, India.
Metronidazole drug was obtained from Zee Laboratories, Himachal Pradesh, India.
Isolation of Polysaccharide
The stems of the plant AM were collected and washed with distilled water to remove the dirt
particles and crushed. The crushed stems were soaked in double distilled water at room
temperature and kept overnight to settle down undissolved material. The supernatant was
separated by decantation. Supernatant was concentrated to its 1/3rd volume under vacuum by
using rotatory evaporator (Yamato) and was cooled. The concentrated liquid was precipitated
with acetone using 1:3 mucilage: acetone ratio. Green precipitates were obtained after
repeated washing, which were then dried at 50-60°C. The dried material was powdered and
kept in desiccator till further use. After extraction of polysaccharide by above procedure the
percentage yield of the polysaccharide was found to be 8%.w/w.
Preliminary Chemical Tests for Characterization of Isolated Albemoschus moschatus

Polysaccharide
Preparation of test solution of Albemoschus moschatus (AM).
Pinches of the above dried precipitate were dissolved in distilled waterhence forth referred as
test solution.
TEST FOR CARBOHYDRATE

a) Molish’s Test:
The Molish’s reagent was prepared by dissolving 10 g of alpha naphthol in 100 ml of 95%
alcohol. A few ml of test solution was placed in test tube, and it was mixed with 2 drops of
Molish’s reagent. To this solution, 1mL of concentrated sulphuric acid was added from the
side of the inclined test tube, so that the acid formed a layer beneath the aqueous solution

without mixing with it. Development of red brown ring at the junction of two layers of the
liquids indicates the presence of carbohydrates.
b) Fehling’s Solution Test

The two solutions (Fehling‘s solution A + Fehling‘s solution B) were mixed in equal volumes
immediately before use. A little of test solution was taken in the above test tube and then this
mixture was warmed. Red precipitates of cuprous oxide formation confirmed the presence of
carbohydrates.
TEST FOR STEROLS

a) Salkowaski Reaction
Few mg of dried precipitates were taken in 2 mL of chloroform and 2 mL of conc. sulphuric
acid was added from the side of test tube. The test sample was shaken for few minutes. The
presence of red colour in the chloroform layer will indicate the presence of sterols.
b) Libermann-Burchard Reaction
Few mg of dried precipitates were dissolve in chloroform and few drops of acetic anhydride
were added to it. Then few drops of conc. sulphuric acid were added from the side of the test
tube. If the transient colour develops from red to blue and finally green, then indicates the
presence of sterol.
TEST FOR ALKALOIDS

Few mg of dried precipitates were taken separately in 5 mL of 1.5% v/v hydrochloric acid
and filtered. These filtrates were then used for testing alkaloids with following reagents.
a) Dragendroff’s reagent
In the presence of dragendroff’s reagent (potassium bismuth iodide solution) the above
filtrates give raddish brown precipitate then it indicates the presence of alkaloids.
b) Mayer’s Reagent
In the presence of alkaloids it gives cream colour precipitate with mayer’s reagent (potassium
iodide solution).

c) Wagner’s reagent
1.27 g of iodine and 2 g of potassium iodide were dissolved in 5 mL of water and the solution
was diluted to 100 mL with water. When few drops of this reagent were added to the test
filtrate, If a brown flocculent precipitate was formed indicating the presence of alkaloids.
d) Hanger’s Reagent
A saturated aqueous solution of picric acid was employed for this test. When the test filtrate
was treated with this reagent. If it gives orange yellow precipitate then it will indicate the
presence of alkaloids.
TEST FOR SAPONINS (Foam Test)

A few mg of the dried precipitate was taken in a test tube and shaken vigorously with a small
amount of sodium bicarbonate and water. If stable, characteristic honeycomb like froth is
obtained, then saponins are presents.
TEST FOR TANNINS

The dried precipitate was taken separately in water, warmed and filtered. Tests were carried
out with the filtrate using following reagents.
a) Ferric chloride reagent

A 5% w/v solution of ferric chloride in 90% alcohol was prepared. Few drops of this solution
were added to the filtrate. The presence of Dark green or deep blue colour will indicate the
presence of tannins.
b) Lead acetate test

A 10% w/v solution of basic lead acetate in distilled water was added to the test filtrate if the
formation of precipitate then it indicates the presence of tannins.
c) Bromine water test

Bromine solution was added to the test filtrate. Decolourization of bromine water indicates
the presence of tannins.
PROTEIN TEST
a) Xanthoproteic test
A few mg of dried precipitate was taken with 2mL of water and 0.5 mL of concentrated nitric
acid was added to it. If the yellow colour produced it will indicate the presence of proteins.

b) Million’s Test (Mercuric Nitrate Solution)

Million’s reagent was prepared by dissolving 3 mL of mercury in 27 mL of fuming nitric acid
keeping the mixture well cooled; this solution was then diluted with equal quantity of
distilled water. Aqueous solution of the dried precipitate was taken and 2 mLor 3 mL of
million’s was added. In the presence of proteins it will gives white precipitate, which slowly
turns to pink.
c) Warming test
Test solution was heated in a boiling water bath, proteins get coagulated.
TEST FOR AMINO ACIDS

a) Ninhydrin Test
The Ninhydrin reagent is 0.1% w/v solution of ninhydrine in n-butanol. A little of this
reagent was added to the extract. A violet or purple colour is developed if the amino acids
are present.
TEST FOR GLYCOSIDES

About 2mL of dried precipitate were taken and subjected to following tests.
a) Killer - killani Test

glacial acetic acid (1 mL) containing traces of ferric chloride and 1mL of concentrated
sulphuric acid was added to the dried precipitate and observed for formation of reddish
brown colour at the junction of two layers formation of the bluish green colour at the upper
layer,will indicates the presence of glycoside.
b) Borntrager’s Test
One mL of benzene and 0.5mL of dilute ammonia solution were added to the extracted dried
precipitate and observed it will produce the reddish pink colour in the presence of glycosides.
c) Legal Test
The above test solution was made alkaline with few drops of 10% w/v of sodium hydroxide
solution and then freshly prepared sodium nitroprusside solution was added to the solution
and observed for the formation of blue colour.

d) Baljet Test
To the concentrated extracts sodium picrate reagent were added and observed for the
formation of orange and yellow colour.
TEST FOR PHENOLIC COMPOUNDS

a) Ferric Chloride Solution
The test sample was taken and warmed add 2mL of ferric chloride solution and observed for
the formation of green and blue colour in the presence of phenolic compounds.
b) Lead Acetate Solution

The test sample was taken and add the 2mL of lead acetate solution if precipitate were
observed then phenolic compounds are present.
c) Gelatine Solution
A few mL of Gelatine Solution was added to the test solution and observed the formation of
precipitate or turbidity will indicate the presence of phenolic compounds.
TEST FOR LIPIDS AND OIL

a) Rub a small quantity of dried precipitate on a paper in the presence of lipids or oil it will
produced a permanent translucent stain.
b) To 2 mL of test solution, 2-3 drops of N/50 iodine solution was added and the colour of
the particles was noted.
TEST FOR STARCH

a) Iodine test
Mix 3 mL test solution and few drops of dilute iodine solution. In the presence of starch blue
colour appear, it disappear on boiling and reappear on cooling.
b) Tannic acid test for starch

The test sample was mixed with 20% tannic acid; if it gives precipitate then indicates the
presence of starch.
TEST FOR MUCILAGE

a) Ruthenium red test: The dried precipitate was mounted on a slide with ruthenium red
solution and covered with a cover slip. After a few seconds, it was irrigated with lead acetate
and the excess stain was sucked off with a blotting paper. Lead acetate solution was added to

prevent undue swelling of the test solution. The pink colour of the particles shows the
presence of mucilage.
b) The test sample was heated for some time and then cooled. Formation of gelatinous mass
indicates presence of mucilage.
PREFORMULATION STUDIES
Preformulation study is an important step for determination of physical and chemical
properties of the drug before incorporating it in formulation development. The nature of the
drug highly affects the processing parameters like method of preparation, selection of
solvents, compatibility and pharmacokinetic response of the formulation. Preformulation
studies are indispensable protocol for development of safe, effective and stable dosage form.
Thus, in order to ensure optimum condition for clinically beneficial delivery system,
preformulation studies were carried out. A thorough understanding of these properties,
ultimately provide a rational for formulation design. Drug identification test and drug
excipients compatibility studies were done in this phase to provide a useful support in
development of dosage form.[5,6]
Performulation Study of Drug

Preformulation is defined as the application of pharmaceutical principles to the
physicochemical parameters of drug substance and other excipients characterized with the
aim of designing optimum drug delivery system.
Drug Identification Tests

The selected drug Metronidazole was identified by various methods like physical
characterization, melting point determination, UV-spectrophotometric study, and infrared
(IR) spectroscopy.
Physical Characterization
Metronidazole was physically characterized on the basis of appearance, colour, odour and
taste. All these organoleptic parameters were recorded and compared with standard data.
Melting Point Apparatus

Capillary melting point apparatus was used to determine melting point of the drug. The
temperature at which a solid melts becomes a liquid is the melting point. The melting point of
a drug can be determined by introducing a tiny amount of drug into a small capillary tube

(one side fused by heat), attaching this to the stem of a thermometer centered in a heating
bath, bath was heated slowly, and temperatures was observed at which melting begins and is
completed. The melting point was recorded in triplicate and compared with literature value.
UV- Spectrophotometer Study

UV spectrophotometric study was carried out in order to determine the λmax of metronidazole
in phosphate buffer solution of pH 6.8 as per IP 1996. A standard stock solution of
metronidazolewas prepared by dissolving 100 mg of drug in a 100 ml volumetric flask and
the volume was made upto 100 ml by using phosphate buffer solution of pH 6.8 to get the
concentration 1000 µg/ml of standardmetronidazole. From the standard stock solution, 1 ml
was pipette out into 10 ml volumetric flask and the volume was made upto 10 ml with
phosphate buffer solution of pH 6.8 to get the concentration. Maximum wavelength (λmax)
was obtained by scanning the resulting solution (10 µg/ml) in the wavelength region between
200 nm to 400 nm by using UV-VIS spectrophotometer (UV1700 Pharma Spec, Shimadzu,
Japan).
Same procedure was repeated with pH 1.2 and maximum wavelength (λmax) was obtained by
scanning the resulting solution (10 µg/ml) in the wavelength region between 200 nm to 400
nm by using UV-VIS spectrophotometer.
Infrared (IR) Spectroscopy

IR spectroscopy was done using Shimadzu Fourier Transform Infrared (FTIR)
spectrophotometer. Perfectly dried metronidazole (5mg) was mixed with powder, which have
no absorption in IR region such as potassium bromide (KBr). Pellet of this mixture was then
prepared by using KBr press at 15 tons and IR spectrum was taken by at frequency of 4000-
-1
400 cm . Obtained IR spectrum was compared with reported spectra to match the
characteristic peaks.
Drug Excipients Compatibility Screening

Drug (Metronidazole), polysaccharide of Albemoschus moschatus and all excipient were
taken in ratio similar to that to be used in formulation. The prepared physical mixture was
placed in a petri-dish and kept for 15th days at room temperature. Compatibility of this
mixture was examined after 15th days via observation for physical changes. Physical mixture
was also subjected to FTIR spectroscopy to find out any interaction at molecular level.

Calibration Curve
Calibration curve of metronidazole was prepared by using U.V. (UV 1700 PharmaSpec,
Shimadzu, Japan).
Selection of Media
pH values was selected on the basis of pH value in stomach and intestine (Colon) for
preparation of calibration curves. The media selected was USP phosphate buffer, pH 1.2 and
pH 6.8.
Preparation of Buffers and Reagents

a) Sodium hydroxide solution, 0.2 M: 8 gm of sodium hydroxide was dissolved in distilled
water and diluted to1000 mL with distilled water.
b) Potassium dihydrogen phosphate solution, 0.2 M: Potassium dihydrogen phosphate
(27.218 g) was dissolved in distilled water and diluted to 1000 mL.
c) Hydrochloric acid solution, 0.1 N: Concentrated hydrochloric acid (8.5 mL) acid was
diluted with distilled water and volume was made up to 1000 mL with distilled water. pH
(1.2) was adjusted with dilute hydrochloric acid.
Preparation of Calibration Curve of Metronidazole at pH 1.2

A standard stock solution of metronidazole was prepared by dissolving 100 mg of drug in a
100 mL volumetric flask and the volume was made upto 100 ml by using pH 1.2 to get the
concentration 1000 μg/mL of standard metronidazole. From the standard stock solution, 1 mL
was pipette out into 10 mL volumetric flask and the volume was made upto 10 mLwith pH1.2
buffer solution to get the concentration 100 μg/mL.
From the above prepared stock solution, ten dilutions were made by using buffer solution
pH 1.2 which has ultimate concentrations of 1, 2,3,4,5,6,7,8,9, and 10 µg/mL. The
absorbance was measured at λmax 277 nm by using UV-VIS spectrophotometer (UV1700
PharmaSpec, Shimadzu, Japan).
Preparation of Calibration Curve of Metronidazole at pH 6.8

A standard stock solution of metronidazole was prepared by dissolving 100 mg of drug in a
100 mL volumetric flask and the volume was made upto 100 mLby using phosphate buffer
pH 6.8 to get the concentration 1000 μg/mL of standard metronidazole. From the standard

stock solution, 1 mL was pipette out into 10 ml volumetric flask and the volume was made
upto 10 ml with phosphate buffer pH 6.8 to get the concentration 100 μg/ml.
From the above prepared stock solution, ten dilutions were made by using pH 6.8 which has
ultimate concentrations of 1, 2,3,4,5,6,7,8,9, and 10 µg/mL. The absorbance was measured at
λmax 319 nm by using UV-VIS spectrophotometer (UV1700 PharmaSpec, Shimadzu, Japan).
Preparation of Rat Cecal Content Medium

Albino rat weighing 150-200 gm and kept in fasting condition over night. Forty- five minutes
before the commencement of drug release studies, seven rats were killed. The abdomen were
opened, the cecae were traced, ligated at both the ends, dissected, and immediately
transferred into pH 6.8 buffer. The cecal bages were opened, their contents were individually
pooled and suspended in the buffer.[7]
RESULT AND DISCUSSIONS

Chemical Characterization of Isolated Polysaccharide
Chemical characterization of isolated polysaccharide was done as per the reported models test
and obtained results are given in Table 3. There was only carbohydrate tests (ruthenium red
test, and molish’s test) found to be positive that indicated polysaccharide contain mucilage
and reducing sugar.
Table 3: Chemical Characterization of Isolated Polysaccharide.

Albemoschus
Test for Positive if Present moschatus
polysaccharide
Carbohydrate:
Molish’s test Reddish brown layer +ve
Fehling solution A & B Brick red +ve
Benedict’s test Red precipitate +ve
Steroids and terpenoids:
Salwoski reaction Red colour layer -ve
Libernann- Burchared reaction Green colour -ve
Alkaloid:
Dragendroff test Orange brown colour -ve
Mayer’s test Cream-colored precipitate -ve
Wagner test Reddish-brown precipitate -ve
Saponins:
Froth formation test Froth is formed -ve

Tannins:
Potassium dichromate test Red precipitate -ve
Bromine water Discolourisation -ve
Protien:
Biuret test Violet or pink colour -ve
Xanthoprotien test White precipitate -ve
Warming test Protein coagulates -ve
Amino acid:
Ninhydrin test Violet purple colour -ve
Glycoside:
Killer killani test Reddish brown ring ve
Baljet test Orange colour -ve
Legal test Pink to red colour -ve
Phenolic compound:
Ferric chloride test Green or brown colour -ve
Lead acetate test Precipitate formation -ve
Acetic acid solution Red colour solution -ve
Starch:
N/50 iodine solution Blue colour -ve
Mucilage test
Ruthenium test Pink colour +ve
Organoleptic Evaluation of Polysaccharide

Organoleptic evaluation of the extracted polysaccharidewas done and obtained results are
given in Table 4. The surface morphology of polysaccharide was found to be slightly rough,
determined by scanning electron microscopy.
Table 4: Organoleptic Properties of Polysaccharide.

Colour Odour Taste Texture Shape
Brown Odourless Characteristic Rough Irregular
Solubility Profile of Polysaccharide

The solubility profile is given in Table 5. From the solubility data it was found that
polysaccharide forms viscous solution in hot and cold water and insoluble in organic
solvents.
Table 5: Solubility Profile of polysaccharide

Solvents Solubility
Cold water Form viscous solution
Hot water Form viscous solution
Ethanol Insoluble
Alcohol Insoluble
Acetone Insoluble
Phosphate buffer(6.8pH) Form viscous solution

pH of Polysaccharide Solution
pH of polysaccharide was investigated to check the acceptability with the biological mucosa.
pH study showed that the polysaccharide have pH within physiological range so they are non
– irritating to the biological mucosa. The result of are summarized in Table 6.
Loss on Drying
Loss on drying was done to identify the amount of volatile content or moisture which was
entrapped within the particles. The result polysaccharide AM was represented in
Table 6.
Swelling Index
Swelling index of polysaccharide was examined to find out the water holding capacity of the
polysaccharide. Swelling index of AM was found 323.1±233. The result polysaccharide AM
was represented in Table 6.
Table 6: pH, Swelling Index and Loss on Drying of AM Polysaccharide.

pH of 1% Swelling Loss on drying
polysaccharide
w/v solution index (%) (%w/v)
AM 7.86±0.03 323.1 ± 2.33 13±0.70
*Average of three readings ±S.D.
Determination of swelling index of extracted polysaccharide Albemoschus moschatus

(AM) in different pH media
The swelling behaviour of extracted polysaccharide was examined in different pH media such
as 1.2, 5.8, 7.8, and 8. The swelling behaviour of polysaccharide was found to be 82.1±0.1
and 72.1±0.015 in pH8 and 7.8 respectively. Henceits indicate this polysaccharide shows
higher swelling behaviour in alkaline medium and may be used as colon delivery of drug.
Table 7: Determination of swelling index of extracted polysaccharide (Albemoschus

moschatus) in different pH.
pH Swelling index (%)
8 82.1±0.1
7.8 72.1±0.15
5.8 53.2±0.18
1.2 30.1±0.20

Figure 2: swelling index of Polysaccharide at different pH.
Ash Value
Ash value was determined to identify the quality and purity of both the extracted
polysaccharide. Ash value of both the polysaccharide was calculated by three ways and
shown in Table 8.
Table 8: Ash Value of AM Polysaccharide.

Total Acid soluble Water soluble ash
Polysaccharide
ash (%) ash (%) (%)
AM 4±0.35 1±0.15 6±0.02
*Average of three readings ±S.D.
Scanning Electron Microscopy (SEM)

From the SEM photograph (Fig 3), itis clear that polysaccharide(AM) possess rough surface
and may be used for various pharmaceutical operations.
Figure 3: Scanning electron microscopy of extracted polysaccharide of Abelmoschus

moschatus(AM).

Micromeritics properties
The result of the AM were found as represented in Table 9.
Table 9: Physical Characterization of Polysaccharide.
Parameters Value
Bulk density(g/mL) 0.510±0.03
Tapped density(g/mL) 0.717±0.21
Carr’s index (%) 29.87±0.346
Hausner’s ratio 1.405±0.12
Angle of repose 28.52±0.09
Physical Characterization of Drug

Metronidazole was evaluated for its physical properties and it was observed that
metronidazole was a pale‐yellow crystal and odourless that was slightly soluble in water and
alcohol. Metronodazole is an antiprotozoal, anti parasitic agent, very effective in the
treatment of amoebiasis, trichomoniasis, giardiasis and many other parasitic diseases. The
physical properties were found similar to that reported in. (IP 2007).This proves the identity
of metronidazole.
Melting Point Determination

The melting point of drug was determined in triplicate and their mean values with standard
deviation. The melting point of metronidazole was found to be 156 ±2ºC, which corresponds
to the literature value of 158ºC to 160ºC that proves the identity and purity of drug.
UV- Spectrophotometer Study

Scannedλmax value of metronidazole in phosphate buffer (pH 6.8)
U-V Spectroscopy study was carried out in order to determine the λmax of metronidazole in
pH 6.8 phosphate buffer. Scanned λmax for metronidazole was shown in Figure 4.

Figure: 4 Scannedλmax value of metronidazole in phosphate buffer (pH 6.8).
Table 10: Scanned λmax and the absorbance value of sample of metronidazole prepared
in 6.8 phosphate buffer.
S.No. Strength Scanned λmax Absorbance
1 10 µg/mL 319 0.084
The scanned λmax found to be 319 nm and absorbance value for 10 to be 0.084.
Scanned λmax value of metronidazole in phosphate buffer (pH 1.2)

The absorbance and concentration data of metronidazole in pH 1.2 were given in
Table 11.
These absorbance were plotted on Y-axis against concentration on X-axis, and slope of the
standard curves was obtained, shown in Figure 5.
Figure 5: Scannedλmax value of metronidazole in buffer solution pH 1.2.

Table 11: Scanned λmax and the absorbance value of sample of metronidazole prepared
in 1.2 pH phosphate buffers.
S.No. Strength Scanned λmax Absorbance
1 10 µg/mL 277 2.660
FTIR Spectroscopy of Drug

FTIR spectra of Metronidazole are given in Figure 6 and the interpretation in shown in
Table 12.
Figure 6: FTIR Spectra of Metronidazole.
Table 12: Interperation of FTIR of Metronidazole.
Functional group Reported frequency (cm-1) Observed frequency (cm-1)

OH stretching 3330 3409.91
C=C ,C=CH stretching 3105 3099.39
NO2,N-O stretching 1538 -1375 1537.16
C-OH, C-O stretching 1078 1074.28
C-NO2,C-N stretching 700 763.76
Drug Excipient Compatibility Studies

Drug excipient compatibility studies were carried out by FTIR spectroscopy method.
Preformulation studies were carried out to study the compatibility of pure drug metronidazole
with the extracted polysaccharide Albemoschus moschatus. The individual IR spectra and of

the combination of the drug and excipients are shown in figure 7, 8 and 9 that indicates no
interaction between drug and polymer when compared with infrared spectrum of pure drug.
Figure 7: FTIR Spectra of polysaccharide (Albemoschus moschatus)
From the above IR spectrum of AM polysaccharide(Fig 7) it was interpreted that AM

polysaccharide have characteristic peak at 3382.91 cm-1 for O-H stretching, 2927.74 cm-1 for
methyl C-H stretching, 1596.38 cm-1 for O-H bending and 1384.79 cm-1 for C-O-C
absorption band.
Figure 8: FTIR Spectra of mixture of drug and polysaccharide(Albemoschus moschatus)

Figure 9: FTIR Spectra of physical mixture ofdrug, polysaccharide(AM) and excipients.
Standard Curve of metronidazole in buffer solution pH 1.2

Table 13: Standard curve data of metronidazolein buffer at 1.2 pH
S. No. Concentration (µg/ml) Absorbance(nm)
0 0 0.000
1 1 0.056
2 2 0.117
3 3 0.191
4 4 0.251
5 5 0.307
6 6 0.368
. 7 7 0.415
8 8 0.472
9 9 0.513
10 10 0.606
Figure 10: Standard curve of metronidazole in pH 1.2.

2.2.5.6 Standarad curve of metronidazole in phosphate buffer of pH 6.8

The absorbance and concentration data of metronidazole in phosphate buffer of pH 6.8 were
given in Table 14. These absorbances were plotted on Y-axis against concentration on X-
axis, shown in Figure 11.
Table 14: Standard curve data of metronidazole in phosphate buffer at pH 6.8.
Figure 11: Standard curve of metronidazole at 6.8 pH phosphate buffer.

Formulation Development
Preparation of metronidazole tablets were carried out by wet granulation and dry granulation
method by using natural polysaccharide(AM).Twelve different batches of metronidazole
were prepared using natural polysaccharide as binder in core tablets and coating material. The
present investigation is aimed using the inexpensive, naturally and abundantly available
polysaccharide(Albemoschus moschatus) for colon targeted delivery of metronidazole.
Preparation of metronidazole tablets by wet granulation method

The most widely used and most general method of tablet preparation is wet granulation
method. Tablets formulation were blended and granulated with 10% starch paste (corn)and
albemoschus moschatus and mix the microcrystalline cellulose. The wet mass was passed
through a mesh (20µm) sieve and the granules were dried at 50˚C for 2-3 hour.
The dried granules were sieved (22µm), lubricated with magnesium sterarate and talc, and
compressed on a tablet punching machine by using 10 mm round slightly concave punches.
Preparation of metronidazole tablets by dry granulation method

In dry granulation method all powder ingredients are mix and sieved (22µm), blended and
mix talc, magnesium stearate and compressed using 10 mm round concave punches.
Preparation of compression coated tablets

The core tablets (average weight 398 mg) of metronidazole were prepared by wet
granulationand dry granulation method.The coating of core tablets was done by using 350 mg
of Albemoshus moschatus (polysaccharide) in six batches i.e. from F1 to F6.For compression
coating, 175 mg of coat weight was placed in the die cavity followed by carefully placing the
core tablet in center and addition of the reminder 175 mg of coat weight. The coating material
was compressed around the core tablet by using 12 mm of round concave punch by on 16-
station tablet punching machine. Quantity of polysaccharide (AM) was replaced by MCC in
coating material from batch F7 to F12prepared by wet granulation and drygranulation method.
Composition of metronidazole (200 mg) core tablet formulations prepared by wet granulation
and dry granulation methods (total wt 398 mg).

Table 15: Composition of prepared tablet with coating material.

Ingredients (mg)
Technique and Starch Coating material
AM Corn Magnesium Talc
Formulation Paste MCC Polysaccharide
(polysaccharide) starch Stearate 1%
(10%) AM MCC
Wet
granulation
F1 30 100! 10 50 4 4 350 0
F2 20 100 20 50 4 4 350 0
F3 10 100 30 50 4 4 350 0
Dry granulation
F4 30 _ 10 150 4 4 350 0
F5 20 _ 20 150 4 4 350 0
F6 10 _ 30 150 4 4 350 0
Wet granulation
F7 10 100 30 50 4 4 325 25
F8 10 100 30 50 4 4 300 50
F9 10 100 30 50 4 4 275 75
Dry granulation
F10 10 _ 30 150 4 4 325 25
F11 10 _ 30 150 4 4 300 50
F12 10 _ 30 150 4 4 275 75
RESULTS AND DISCUSSION

The colon specific tablets of metronidazole were prepared, evaluated and the best formulation
was selected for their use in colon targeted drug delivery. In the present work total 12
formulations were prepared. These formulations were subjected to evaluation studies.
Evaluation of all these formulation batches showed promising results and confirmed the
utility of extracted polysaccharide as pharmaceutical excipient for colonic drug delivery.
Evaluation of Granules
Granules were prepared bywet granulation and dry granuulation method by using extracted
polysaccharide as binder in core tablet. Prepared granules were evaluated for bulk density,
tapped density, compressibility index (carr’s index), angle of repose and hausner’s ratio and
results are presented in Table 16.
Bulk density and Tapped density

The result of bulk density and tapped density are found to be0.36±0.00 to0.63 ±0.00 and
0.47±0.00 to 0.83±0.00 respectively. It was observed that density data of granules prepared
by wet granulation was less than the data of granules prepared by dry granulation method.
The data of density characterstic of prepared granules is given in Table no 16.

Angle of repose
Although all prepared batches were showing good floability but angle of repose of batch F3
and F6 were below 30º which shows excellent flow properties in comparison to other batches.
The angle of repose for the formulation blends was carried out after lubrication and result
were reported in Table no. 16 Which ranges between 28.33 to 33.66. It concluded that, all
the formulation blends have good flow property.
Compressibility index
The data of compressibility was found in between 15.47±0.46 to21.88±0.57.Generally
compressibility index values up to 15% result in good to excellent flow properties. The
compressibility index of optimize batch F3 and F6 had lower than other F1, F2, F4 and F5
because of F3 and F6 exhibit lower concentration of polysaccharide than other batches then
others having comparatively poor flow properties. Data of compressibility index is reported
in Table no. 16.
Hausner’s ratio: Batch F1, F2, F4, F5 had higher hausner’s ratio than other batches because
of higher concentration of polysaccharide hence, it may be concluded that these
batchespossess comparatively poor flow properties. The data of Hausner’s ratioof prepared
granules is givenin Table 16.
Table 16: Precompression results for all batches prepared by wet and dry granulation
method.
Formulation Bulk Tapped Angle of Carr’s Haursner’s

Code density density repose Index Ratio
F1 0.42±0.00 0.51±0.00 33.66±0.57 21.88±0.57 1.27±0.00
F2 0.42±0.00 0.55±0.00 33.33±0.57 20.71±0.51 1.24±0.00
F3 0.36±0.00 0.47±0.00 28.33±0.57 15.47±0.46 1.10±0.00
F4 0.64±0.00 0.77±0.00 32.66±0.57 23.66±0.57 1.32±0.00
F5 0.63±0.00 0.92±0.00 33.66±0.57 20.77±0.68 1.22±0.00
F6 0.51±0.00 0.55±0.00 27.31±0.57 16.33±0.57 1.06±0.00
Evaluation of Uncoated Core Tablets

The in-process quality control parameters like average diameter, thickness, weight variation,
hardness, friability and disintegration were evaluated and obtained data is summerized in
Table 17. The average length, width, and thickness of core tablets were found within limit.

Weight Variation
According to the USP limit of weight variation the formulated tablets fall within limit of ± 5.
All the formulations show748 ±0.01 to748± 0.03 % of weight variation (Table no.17).
Hardness
The hardness of different trial batches was determined with Monsanto hardness tester and
results showed that all the formulations possessed good hardness.The hardness of all the
tablets were maintained within 7.2±0.00 to 7.5±0.05 (Table no 17).
Friability: According to the IP limit friability of the formulated batches showed be less than
1% w/w. The results of friability test indicates that all formulations showed 0.042% to
0.048% friability which was within the range of IP limit (Table no 17).
Disintegration Time
According to IP limit of disintegration time, the formulated tablets showed disintegration
within 15 minutes (Table no. 17).
Thickness
The thickness of all formulation ranged between 3.64±0.00 to 36.64±0.01 mm (Table no 17).
Drug content
The percentage drug content of both tablet prepared by different granulation methods was
found to be within limits.A percentage drug content value of metronidazole was foundin the
range from 97.22±0.00 to 98.56±0.00 (Table no 17).
Table 17: Tablet parameters of tablets prepared by different granulation method.

Weight Disintegration Drug
Hardness Friability Thickness
variation Time content
F1 7.5±0.05 0.048±0.00 3.64±0.01 748±0.01 7.06±0.05 98.56±0.00
F2 7.5±0.01 0.047±0.00 3.64±0.00 748±0.03 7.03±0.05 98.23±0.00
F3 7.3±0.05 0.047±0.00 3.64±0.00 748±0.01 7.01±0.01 98.23±0.01
F4 7.5±0.01 0.042±0.00 3.64±0.00 758+0.02 7.01±0.01 97.31±0.00
F5 7.4±0.05 0.046±0.00 3.64±0.01 748±0.03 7.06±0.05 97.23±0.01
F6 7.2±0.00 0.048±0.00 3.64±0.01 748±0.02 7.02±0.01 98.46±0.01
In Vitro Drug Release of compression coated tablets

Cumulative percentage drug release of compression coated tablets were estimated for the all
12 batches at different time intervals. Data of percentage drug release are given in Table 18

and 19.The present study was aimed at developing oral colon targeting formulation for
metronidazole using Albemoschus moschatus as binder in core tablets and as a tablet coating
material. Metronidazole tablets were prepared by wet and dry granulation method. The tablets
were subjected to in-vitro drug release studies in pH1.2 (2h), pH 6.8 phosphate buffer (3 h),
and simulated colonic fluid contain rat cacecal medium at the end of 24 hours.
In order to determine the effect of granulation method and concentration of extracted

polysaccharide over drug release first six formulations (F1 to F6) was subjected to release
study. Obtained data are summarized in Table 18 and illustrated in Figure 12 and 13. It was
observed polysaccharide concentration in prepared tablets play crucial role to release the drug
in both types of tablets prepared by changing the granulation method. Obtained data revealed
that percentage drug release of metronidazole was increased by decreasing the concentration
of extracted polysaccharide as binder. In the tabletsprepared by wet granulation method, the
least drug release was found in batch F1 with highest concentration of polysaccharide
(70.16%) whereas, batch F3 possess highest drug release with lowest concentration of
extracted polysaccharide in tablet as binder. Reason may be attributed that increased
concentration of polysaccharide in the tablets may alter the permeation of drug through
highly branched network of polysaccharide. Hydration of polysaccharide cause conversion in
to a thick gel network which retard the drug release from polymer matrix.
Table 18: In-vitro drug release of metronidazole tablets of prepared by different

granulation method.
Time(hr) F1 F2 F3 F4 F5 F6
0 0 0 0 0 0 0
1 1.3±0.00 3.72±0.02 4.15±0.00 3.33±0.00 4.33±0.00 5.87±0.00
2 3.16±0.00 4.67±0.05 5.80±0.00 4.80±0.05 5.80±0.01 6.87±0.05
3 6.53±0.01 7.30±0.05 8.01±0.05 6.56±0.00 7.38±0.00 9.32±0.00
4 7.58±0.00 8.36±0.01 11.63±0.00 7.56±0.00 20.07±0.06 22.44±0.00
5 8.45±0.01 10.44±0.01 13.47±0.01 10.58±0.01 24.81±0.05 28.13±0.01
6 24.38±0.00 20.70±0.00 25.06±0.00 11.85±0.02 31.47±0.00 35.44±0.01
7 26.38±0.00 19.26±0.11 27.17±0.00 20.89±0.05 40.63±0.01 45.61±0.05
8 33.87±0.01 22.41±0.05 36.52±0.05 25.48±0.07 41.69±0.00 49.68±0.01
9 39.51±0.01 39.54±0.07 41.68±0.00 30.16±0.00 44.79±0.01 50.15±0.01
10 42.15±0.00 45.72±0.03 52.52±0.01 41.07±0.00 49.07±0.03 52.69±0.01
11 44.85±0.01 48.72±0.00 54.44±0.05 46.39±0.00 51.06±0.00 58.12±0.01
12 46.25±0.00 53.71±0.01 60.81±0.06 51.46±0.01 52.77±0.00 60.69±0.01
16 52.75±0.02 58.72±0.05 65.64±0.00 56.18±0.00 54.23±0.00 63.12±0.00
20 54.95±0.01 60.31±0.00 69.54±0.01 60.18±0.00 63.96±0.01 65.18±0.05
24 70.16±0.07 72.81±0.05 73.54±0.01 73.30±0.01 75.30±0.00 76.13±0.00

Figure 12:Comparative cumulative drug releases prepared by wet granulation method
Figure 13: comparative cumulative drug releases prepared by dry granulation method.
Similarly, in order to investigate the effect of concentration of extracted polysaccharide as

coating material six more batches (F7-F12) were prepared by replacing the polysaccharide
concentration with microcrystalline cellulose (MCC). Although, the core tablets content was
same in (F7-F9) and (F10-12). Data of percentage release of drug from the tablets prepared
by changing the coating material are summerized in Table 19 and illustrated in Figure 14
and 15. Obtained data indicates that concentration of extracted polysaccharide again play an
crucial role during drug release. It was observed that the whole drug was come out within 7h
in both cases (F9 and F12) with least content of polysaccharide and higest content of MCC as
coating material. Drug release pattern was found proportional to the concentration of
extracted polysaccharide as coating material. Reason may be attributed that higher amount of
polysaccharide make highest viscous polymeric network cause to alter the drug from it.

Table 19: In-vitro release of tablets prepared by changing the content of polysaccharide
as coating material.
Time(hr) F7 F8 F9 F10 F11 F12
0 0 0 0 0 0 0
1 5.93±0.01 6.72±0.00 9.12±0.01 7.88±0.01 10.01±0.00 9.52±0.01
2 6.18±0.00 7.52±0.05 10.34±0.11 8.80±0.00 12.31±0.00 11.21±0.00
3 7.63±0.05 14.14±0.05 20.16±0.05 22.09±0.05 32.33±0.00 23.09±0.00
4 12.53±0.00 20.17±0.01 31.33±0.03 31.04±0.03 40.11±0.05 39.12±0.00
5 17.85±0.00 28.75±0.11 52.47±0.01 31.71±0.01 42.18±0.01 53.06±0.00
6 23.58±0.00 30.87±0.11 62.11±0.05 39.81±0.00 56.99±0.01 67.15±0.01
7 25.28±0.00 49.96±0.11 71.12±0.00 49.68±0.01 61.01±0.05 72.25±0.00
8 36.58±0.00 57.47±0.00 - 52.08±0.05 63.11±0.01 -
9 42.32±0.00 70.47±0.01 - 62.39±0.05 72.11±0.05 -
10 57.06±0.01 - - 70.13±0.01 - -
11 58.19±0.01 - - 72.02±0.01 - -
12 74.54±0.01 - - 75.06±0.00 - -
Figure 14: Cumulative drug releases prepared by wet granulation method and
polysaccharide concentration as coating material.
Figure 15: Cumulative drug releases prepared by dry granulation method and
polysaccharide concentration as coating material.

Drug Release Kinetics

The correlation coefficients for the different drug release kinetic models are shown in Table 20
Models with the highest correlation coefficient were judged to be the most appropriate model for the
dissolution data. The results of in vitro drug release studies were treated with zero order, first order
kinetics, Higuchi and Korsemeyer‐Peppas model. The dissolution data of the various batches of
tablets were fitted into the various kinetic models and their regression values used to assess the best
fit. The higher the R2 value (i.e. the more linear the graph), the better the fit of the dissolution profile
to that kinetic model. From the results obtained from the study, higher R2 values were obtained for the
Higuchi model than the other kinetic models. This happened especially in the batches that passed the
dissolution test (i.e. batches 1 to 12). Higuchi describes drug release as a diffusion process based on
the Fick’s law, square root time dependent (Kalam et al. 2007). This model can be used to describe
the drug dissolution from several types of modified release in pharmaceutical dosage forms.
(Suvakanta et al. 2010). The dissolution data was fitted into the Korsmeyer-Peppas model to
determine the exact mechanism of drug release. This model is generally used to analyze the release of
polymeric dosage form, where the release mechanism is not well known or when more than one type
of release phenomenon could be involved (Kalam et al. 2007). The graphs of log cumulative percent
release against log time was plotted and the release rate constant, k, and the release exponent, n,
determined.
Table 20: Drug release kinetics model of different batches.

Formulation/model and parameter
S. No Formulation Zero order First order Korsemeyer -
2 Higuchi (r2)
Code (r ) (r2) Peppas (r2)/n
1 F1 0.8953 0.9461 0.9581 0.9241/0.0217
2 F2 0.9429 0.9755 0.9546 0.9696/0.0197
3 F3 0.918 0.9776 0.9722 0.9673/0.0234
4 F4 0.9595 0.9114 0.9642 0.9842/0.0206
5 F5 0.8484 0.9843 0.9414 0.9536/0.0207
6 F6 0.8116 0.9114 0.9582 0.9582/0.0218
7 F7 0.9766 0.9773 0.9316 0.9615/0.025
8 F8 0.9634 0.9657 0.9185 0.9578/0.0354
9 F9 0.9572 0.9878 0.8305 0.9236/0.0495
10 F10 0.8343 0.9456 0.954 0.9067/0.0518
11 F11 0.8055 0.9289 0.9209 0.9155/0.0373
12 F12 0.959 0.9653 0.8531 0.9336/0.0518
Table 21: Release mechanism with variation of n* values

‘n’ Mechanism
<0.5 Fickian diffusion
0.5 < n < 1 Non Fickian diffusion or anomalous release
>1 Case II Transport

All formulation shows high linearity (r2=0.9289 to 0.9878) in case of first order release
profile this shows that all formulation follow first order release kinetic. This is indicates that
the amount of drug release is dependent on the amount of drug loaded. (Concentration
dependent).
In our experiments, the in‐vitro release profiles of drug from all the formulations could be
best expressed by Higuchi’s equation, as the plots showed high linearity (r2= 0.8305 to
0.9722 ). To confirm the diffusion mechanism, the data were fitted into Korsemeyer‐Peppas
model.
All formulations F1 to F12 showed high linearity (r2= 0.9067 to 0.9842), with slope (n)
values ranging from 0.0197 to 0.0518. This indicates that F1 to F12 shows purely fickian
diffusion. This means drug release mechanism involving swelling of the tablets. It might be
concluded that the drug release is controlled by one mechanism i.e. diffusion mechanism.
Figure 16: Log cumulative % drug retain vs. Time.
Figure 17: Cumulative % drug releases vs. Time (hr).

Figure 18: Cumulative % drug release vs. √T.
Figure19: Log cumulative % drug retain vs.log Time.
Evaluation of Stability Study

Coated colon targeted tablet of metronidazole (F3) was subjected to stability study at room
temperature and relative humidity (250C ± 20C/ 60% ± 5%) and evaluated for physical
appearance, drug content, average weight. The formulation showed no significant change in
the physical appearance at room temperature (250C ± 20C/ 60% ± 5%).
Table 21: Room Temperature stability study data.

Tests Specification After 15 days After 30 days
Brown round Brown round Brown round
Description
biconvex coated tablets biconvex coated tablets biconvex coated tablets
Odour Odourless Odourless Odourless
Weight (Avg.) 748mg±0.01 mg 748 ±0.05mg 748±0.01 mg
Drug content 98.59±0.00% 98.37±0.01% 98.61±0.00%

SUMMARY AND CONCLUSION

In present study, oral colon targeting drug delivery system was developed by using natural
polysaccharide extracted froml plant Abelmoschus moschatus(AM). Chemical
characterization of the polysaccharide showed that AMwere of mucilaginous in nature as
ruthenium red test result was found to be positive. Micromeritics study showed that AM
powder has good flow property as data ofcarr’s index, hausner’s ratio and angle of repose
was found within the prescribed limit.
Organoleptic evaluation of the polysaccharide dried powder showed that powder possess
rough surface as observed in SEM photographs. From the swelling study as function of pH it
can be conclude that AM polysaccharide powder has more capability to use as colon targeting
excipient since,swelling behavior of polysaccharide was found to be more in alkaline
medium.
The result of the study show that compression coated formulation of metronidazole tablets
with 350 mg of Albemoschus moschatus (polysaccharide) coat is most likely to provide
targeting of drug for local action in the colon owing to its minimal release of the drug in the
first 5 hr. The comparison between corresponding concentrations different ratio of the same
polysaccharide was found it was more effective at low concentration.
Stability study was conducted on tablets of Batch F3 stored at 25°C ± 2°C/60% RH ± 5% RH

(Room temperature). After one month no significant changes were observed in any of the
studied parameters during the study period, thus it could be concluded that formulation was
stable at room temperature.
Thus a stable and effective colon targeting tablet (metronidazole) containing natural
polysaccharide was successfully developed.
ACKNOWLEDGEMENT
Authors are highly thankful to Department of Pharmacy, IIMT College of Pharmacy, Greater
Noida and Oxford College of Pharmacy, Ghaziabad, India for providing necessary facilities.
Conflict of Interest: There is no conflict of Interest.

REFERENCES
1. Vinaykumar KV, Sivakumar T., et al. Colon Targeting Drug Delivery system, A review
on recent approaches. Int Journal of Pharm Biomed Sci., 2011; 2(1): 1-19.
2. Patel A, Bhatt N, et al. Colon Targeted Drug Delivery System A Revie. Int Journal of
Pharmaceutical Science and Bioscientific Research., 2011; 1: 1-49.
3. Malik K, Goswami L, et al. A review on Colon Targeting Drug Delivery System, Novel
Approaches, Anatomy and Evaluation. The Pharma Innovation., 2012; 9: 1-12.
4. Sonasaniya B, Patel M R, .Patel K R, Patel N M. A Review on colon targeted drug
delivery system. International Journal of Universal Pharmacy and Bio Sciences., 2013;
2(1): 20-34.
5. Sanket DG, Priyanka RP, Girish KJ, Nishant NU, Upendra N. Formulation development
and evaluation of colon targeted tablets of secnidazole for the treatment of amoebiasis.
Int J Pharm Sci Rev Res., 2010; 5(3): 64-71.
6. Chetan SC, Pushpendra SS, Naruka, Rajendrapal SR, Viral KB. Formulation and
evaluation of prednisolone tablet for colon targeted drug delivery sytem. J Chem Pharm
Res., 2010; 2(4): 993-8.
7. Sinha V R, Mittal B R, Kumria Rachna. In vivo evaluation of time and site of
disintegration of polysaccharide tablet prepared for colon-specific drug delivery.
International journal of Pharmaceutics., 2005; 289: 79-85.

Development of Colon Targeting Drug Delivery System Using Plant Polysaccharide

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WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

Priya et al. World Journal of Pharmacy and Pharmaceutical Sciences

Volume 5, Issue 8, 992-1024 Research Article ISSN 2278 – 4357

DEVELOPMENT OF COLON TARGETING DRUG DELIVERY

Bhanu Priya1*, Shubham Verma2 and Nitin Sharma3

KEYWORDS: Colon, Abelmoschus moschatus, Metronidazole, Natural Polymer, Anti

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Figure 1: Structure of human intestine

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Table 1: Anatomical Properties of Gastrointestinal Tract.

Table 2: pH of Stomach and Small Intestine.

Advantages of colon targeting

Limitations and challenges in colon targeted drug delivery.[4]

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MATERIALS AND METHOD

Preliminary Chemical Tests for Characterization of Isolated Albemoschus moschatus

TEST FOR CARBOHYDRATE

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b) Fehling’s Solution Test

TEST FOR STEROLS

TEST FOR ALKALOIDS

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TEST FOR SAPONINS (Foam Test)

TEST FOR TANNINS

a) Ferric chloride reagent

b) Lead acetate test

c) Bromine water test

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b) Million’s Test (Mercuric Nitrate Solution)

TEST FOR AMINO ACIDS

TEST FOR GLYCOSIDES

a) Killer - killani Test

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TEST FOR PHENOLIC COMPOUNDS

b) Lead Acetate Solution

TEST FOR LIPIDS AND OIL

TEST FOR STARCH

b) Tannic acid test for starch

TEST FOR MUCILAGE

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Performulation Study of Drug

Drug Identification Tests

Melting Point Apparatus

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UV- Spectrophotometer Study

Infrared (IR) Spectroscopy

Drug Excipients Compatibility Screening

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Preparation of Buffers and Reagents

Preparation of Calibration Curve of Metronidazole at pH 1.2

Preparation of Calibration Curve of Metronidazole at pH 6.8

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Preparation of Rat Cecal Content Medium

RESULT AND DISCUSSIONS

Table 3: Chemical Characterization of Isolated Polysaccharide.

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Organoleptic Evaluation of Polysaccharide

Table 4: Organoleptic Properties of Polysaccharide.

Solubility Profile of Polysaccharide

Table 5: Solubility Profile of polysaccharide

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Table 6: pH, Swelling Index and Loss on Drying of AM Polysaccharide.