PREPARATION AND EVALUATION OF STARCH LACTOSE (1:1) AND SUCROSE LACTOSE (1:2) GRANULES AS DIRECTLY COMPRESSIBLE VEHICLES.

AIM: To prepare and evaluate starch lactose (1:1) and sucrose lactose (1:2) granules as
directly compressible vehicles.

REQUIREMENTS:
Materials: Apparatus: starch, acacia, sucrose, water , lactose. mortar and pestle, measuring cylinder, 10# mesh, sieve shaker, funnel.

PRINCIPLE:
Tablets can be prepared by various methods in which direct compression is one such method. The drug is blended with a directly compressible vehicle, which determines the characteristics of the tablet. Direct compression is economic compare to wet granulation since it requires fewer unit operations. This means less equipment, lower power consumption, less space, less time and less labor leading to reduced production cost of tablets. More suitable for moisture and heat sensitive APIs, since it eliminates wetting and drying steps and increases the stability of active ingredients by reducing detrimental effects. The tablets prepared by direct compression disintegrate into API particles instead of granules that directly come into contact with dissolution fluid and exhibits comparatively faster dissolution. The high compaction pressure involved in the production of tablets by slugging or roller compaction can be avoided by adopting direct compression. The directly compressible vehicle should have good flow property. The prepared directly compressible vehicles are evaluated for its flow property, by angle of repose method and compressibility index.

EXPERIMENTAL WORK: PREPARATION OF GRANULES:

Accurately weigh required amounts of lactose and starch / sucrose were taken into a mortar and mixed thoroughly by adding 8% W/V solution of acacia. It is then made into dough mass and passed through 10# mesh to get granules which were dried in an oven at 50c. The dried granules were again passed through 10# mesh.

s.no

ingredients

Starch

lactose Sucrose

lactose purpose

granules(1:1) 1 2 3 4 Lactose Starch sucrose Acacia (8%w/v) 2.5 g 2.5 g --Q.S

granules(1:2) 3.33 g --1.67 g Q.S Binder Diluent disintegrant

EVALUATION OF GRANULES:
The flow properties and characteristics of granules were found by measuring 1. Angle of repose 2. Bulk density 3. True density 4. Compressibility index 5. Hausners ratio 6. Size distribution curve.

1.Angle of repose:
When bulk granular materials are poured onto a horizontal surface, a conical pile will form. The internal angle between the surface of the pile and the horizontal surface is known as the angle of repose

= tan1 ( h / r )

Where, h= height of the heap. r= radius of base of the heap.

Procedure:
Fix a funnel to the burette stand and close the funnel tip with thumb and fill the granules. Then allow the granules to form a heap on the horizontal paper surface. Then measure height, radius of heap.

Limits:
< 25 25 - 35 35 - 45 Flow property very good good poor

2. Bulk density
The bulk density of a powder is the ratio of the mass of an untapped powder sample and its volume including the contribution of the interparticulate void volume. Hence, the bulk density

depends on both the density of powder particles and the spatial arrangement of particles in the powder bed. The bulk density is expressed in grams per milliliter (g/mL) although the international unit is kilogram per cubic meter (1 g/mL = 1000 kg/m3) because the measurements are made using cylinders. It may also be expressed in grams per cubic centimeter (g/cm3).

Bulk density =

3. True density
The true density is an increased bulk density attained after mechanically tapping a container containing the powder sample. The true density is obtained by mechanically tapping a graduated measuring cylinder or vessel containing the powder sample. After observing the initial powder volume or mass, the measuring cylinder or vessel is mechanically tapped for 100 times, and volume or mass readings are taken until little further volume or mass change is observed.

true density =

Compressibility index:
The granules were filled into a measuring cylinder and initial volume was noted. The cylinder is tapped on a stable horizontal surface for 100 times uniformly and the final volume was noted.

I = (V0 -Vf/Vf )100

Where V0 = initial volume of granules V = volume of granules after 100 tappings.

Limits:
I <15% 15 - 25 >25% Flow property good moderate poor

Hausners Ratio: It is the ratio of initial volume of granules to volume of granules after tapings

Particle size distribution curve:

Powder is said to be polydispersed. The distribution of different size particles in a powder is called its particle size distribution. A series of standard sieves were placed one above the other in the increasing order of the sieve number. A definite mass of sample was placed on top sieve and whole set up is shaken mechanically for a definite period. Powder remained on each sieve was collected separately and weighed. A graph was plotted by taking mean particle size on X - axis and percentage weight retained (frequency) on Y- axis. Mean particle size is calculated as x= xifi /Fi

RESULTS:

1. ANGLE OF REPOSE:

2.BULK DENSITY:

3. TRUE DENSITY

4. COMPRESSIBILITY INDEX:

5. HAUSNERS RATIO:

6.PARTICLE SIZE DISTRIBUTION:

S.NO. SEIVE NO. PORE SIZE(m) MEAN SIZE(xi) STARCH-LACTOSE Wt %wt SUCROSE-LACTOSE Wt %wt

retained retained xifi

retained retained xifi

1 2 3 4 5

10 10/25 25/60 60/80 80/120

2000 2000/710 710/250 250/180 180/125

2000 1355 480 215 152.5 xifi= xifi=

x for starch-lactose =

x for sucrose-lactose =

REPORT:
S.NO. 1 2 3 PROPERTIES Angle of repose Compressibility index Particle size distribution STARCHLACTOSE SUCROSE-LACTOSE