Research Of VIN-SMEDDS Soft Capsule

According to a research of world health organization, cerebrovacular disease hasbecome the second leading cause of death worldwide and there is a pressing demandof effective drug therapies. Vinpocetine (VIN) is a synthetic ethyl ester of the alkaloidapovincamine, which is a kind of indole alkaloid isolated from the leaves of vincaminor. As vinpocetine showscerebral blood-flow enhancing and neuroprotectiveeffects, it has widely used to treat brain vascular abnormalities involved diseases. Theonly oral dosage form of VIN that has been marketed is normal tablet. But as VIN isalmost insoluble in water, its bioavailability is very low for only about7%.In order to improve the oral absorption of VIN, this paper optimized theformulation of VIN-SMEDDS at first. After the construction of pseudo-ternary phase,the formulation of SMEDDS was optimized using central composite design/responsesurface methodology with particle size as the evaluating indexes. The finalformulation of VIN-SMEDDS contains GTCC as oil phase (30%), Cremophor EL35(50%) as Surfactant, and Transcutol P (20%) as cosurfactant, and the drug load is1%.After diluted by purified water, the optimized VIN-SMEDDS formed intomicroemulsion with particle size under50nm, and the time of self-microemusifyingwas less than1min. By using dissolution experiment, the plasticizer, antioxidant,acidity regulator and disintegrating agent added in soft capsule was screened bymeans of dissolution rate. The amount of plasticizer was determined to be40%of thegelatin mass and the addition of an appropriate amount of glycine and citric canrestrain the cross-linking of gelatin. Three batches of VIN-SMEDDS soft capsuleswere prepared by pressing method. The investigation of VIN-SMEDDS soft capsuleshowed that content uniformity, mass uniformityand disintegration time accorded The Chinese Pharmacopoeia. The results of in vitro dissolution experiments showed thatthe cumulative dissolution amount of VIN-SMEDDS soft capsule in purified waterand artificial gastric juice was more than90%in30minutes. These results indicatedthat the VIN-SMEDDS soft capsule prepared in the paper reached the designrequirements.