Development of Controlled Release Spheriods using Natural Polysaccharide as Release Modifier

Figures & data

FIG. 1 SEM of Tamarindus indica polysaccharide (magnification 220×).

TABLE 1 Physical characteristics of tamarind seed polysaccharide

Yield (% w/w)	Viscosity of 1% solution (cP)	Swelling index (ml)
78.07 (0.009)	74.69 (0.308)	18.7 (1.021)

Values in parentheses are SEM; n = 3.

TABLE 2 Results of optimization of spheronization process

MCC-drug-polysaccharide ratio	Amount of water (ml/g)	Spheronization speed (rpm)	Spheroid description
65:30.5	0.9	300	Dumbbell shape
		400	Spheroids with wide size range
		500	Spheroids with wide size range
		1000	Dumbbell shape
		2000	Rod shape
60:30:10	0.9	300	Dumbbell shape
		400	Spheroids with narrow size range
		500	Spheroids with narrow size range
		1000	Dumbbell shape
		2000	Rod shape
55:30:15	0.9	300	Dumbbell shape
		400	Dumbbell shape
		500	Dumbbell shape
		1000	Rod shape
		2000	Rod shape
50:30:20	0.9	300	Dumbbell shape
		400	Dumbbell shape
		500	Dumbbell shape
		1000	Rod shape
		2000	Rod shape
45:30:25	0.9	300	Formation of elastic mass; no extrudes
		400
		500
		1000
		2000

Microcrystalline cellulose (MCC) was used as spheronization enhancer.

TABLE 4 Characteristics of spheroids

Yield (%)	Average particle size^† (mm)	Bulk density (g/cc)	Friability (%)	Angle of repose^† (degrees)
74.42 (0.06)	0.69	0.88 (0.003)	0.77 (0.003)	23.76 (0.032)

Values in parentheses are SEM; n = 3.

^†Average particle size was determined using sieve analysis.

^‡Angle of repose was determined using funnel method.

FIG. 2 SEM of the formulated spheroid (magnification 55×).

TABLE 3 Results of optimization of spheronization time

MCC-drug-polysaccharide ratio	Amount of water (ml/g)	Spheronization speed (rpm)	Spheronization time (min)	Spheroid description
60:30:10	0.9	400	10	Spheroids not formed
			15	Spheroids not formed
			20	Spheroids formed
			25	Spheroids formed
			30	Spheroids formed

FIG. 3 In vitro release profile of diclofenac sodium from spheroids of tamarind seed polysaccharide.

FIG. 4 Higuchi's plot for the release data of diclofenac sodium from spheroids of tamarind seed polysaccharide.

FIG. 5 Peppas' plot for the release data of diclofenac sodium from spheroids of tamarind seed polysaccharide.

TABLE 5 Pharmacokinetic parameters for the spheroids and marketed formulation of diclofenac sodium

Parameter	For spheroids	For marketed formulation
Tmax	2.00	1.00
Cmax	580.90	192.12
AUCtotal	2562.66	659.56
t1/2	3.66	2.20

FIG. 6 Plasma concentration-time profile of diclofenac sodium from prepared spheroids and marketed sustained release tablet.