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http://doi.org/10.5281/zenodo.1050439
polymers prolongs the residence time when contact improves glycemic control by improving insulin
with mucous membrane due to its high degree of sensitivity and decreasing intestinal absorption of
swelling property with aqueous medium , results gel glucose.
formation. The rate and extent of drug release is
controlled by concentration of polymer and the Melting point: 223-226 0 C
release pattern in a sustained manner. The main Structure:
drawback is, in clinical use drug loading efficiency of
biodegradable microspheres is complex and is
difficult to control the drug release.
(b) Synthetic polymeric microspheres:
The interest of synthetic polymeric microspheres are
widely used in clinical application, moreover that
also used as bulking agent, fillers, embolic particles,
drug delivery vehicles etc and proved to be safe and
biocompatible. But the main disadvantage of these
kind, are tend to migrate away from injection site and
lead to potential risk, embolism and further organ
damage. Polyethylene, polystyrene and expandable
microspheres are the most common types of polymer Fig1 : Metformin Hydrochloride structure
microspheres. [13,14]
Chemical name: 1-carbamimidamido-N,N-
MATERIALS AND METHODS: dimethylmethanimidamide.
Table 1: Materials used for the study
INGREDIENTS SUPPLIER Pharmacokinetics:
After oral administration Metformin Hydrochloride is
Metformin Yarrow chem. Products freely soluble. Half-life of Metformin Hydrochloride
hydrochloride Mumbai. salt is 4-6 hours. The oral bioavailability of the drug
Hydroxy propyl is 50-60 % under fasting conditions.
Ozone International
methyl cellulose
Mumbai. Formulation of Sustained Release Microspheres
K100M
Procedure: The following steps involved in
Sodium Carboxy Ozone International preparation of Metoprolol microspheres.
methyl cellulose Mumbai. 1. Preparation of Polymer Solution by dissolving in
S.D. Fine chemicals distilled water.
Sodium bicarbonate 2. Dissolve Drug (Metformin Hydrochloride) in
Ltd, Mumbai.
S.D. Fine chemicals above Solution.
Calcium chloride 3. Sonicate the Drug-Polymer Solution for proper
Ltd, Mumbai.
mixing.
Loba Chemie Pvt 4. Above solution was added drop wise by a 26G
Sodium alginate
.Ltd.Mumbai. hypodermic needle into 50ml of 5% w/v CaCl2
solution.
DRUG PROFILE [24,25] 5. Formed Metoprolol Microspheres were stirred in
Empirical formula: The Empirical formula of the cross linking agent for 1hr at 100rpm.
Metformin HCl is C4H11N5 HCl. 6. Wash the Microspheres with de-ionized water and
Molecular weight: 165.63. dried at 80oC for 2 hour.
7. Transfer prepared Microspheres to desiccators to
Description: maintain the constant Humidity conditions.
A biguande hypoglycemic agent used in the treatment All Formulations were prepared by Ionic Gelation
of non-insulin dependent diabetes mellitus not method using different polymers. [7,15,16]
responding to dietary modification. Metformin
Sodium Carboxy
Metformin HCl HPMC-K100 Sodium
Formulations methyl
(mg) M(mg) bicarbonate(mg)
cellulose(mg)
Evaluation Tests:
Particle Size
Percentage Yield:
Inference: From the above table the percentage yield of prepared Microspheres was found to be more for the
formulation F- 4 (72 %)
Inference: From the above fig the dissolution profile for the formulation F-4 was found to be have the more
cumulative % drug release.
Inference: From the above graphs the R2 value is (0.977) and for zero order plot R2 value is ( 0.957) which
indicating that the order of release was first order.
Higuchis Plot
Inference: As per the above plot Fig No. 17 and Fig No. 18. The R2 value for Higuchi (0.974) and for Korsemeyer -
Peppas plot (0.964), showing that the mechanism of drug release from the formulation was found to be Diffusion
controlled release.
H.Berkel, R.F. Holcomle , m.Middle, blcooks and 17. Ghodake. P , Patil Sangamesh A, Belhekar Anaga
R.Kannam , Non-steroidal anti-inflammatory drug A, Halligudi Shivraj B, Aminabhavi Tejraj M.
and colorectal cancer , epidermal Rev; (1996) ; 18: preparation and evaluation of floating microspheres
205-217. with Metformin Hydrochloride. Journal of pharmacy
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