Study Of Granisetron Transdermal Patch

Granisetron is a potent and highly selective 5-HT3 receptor antagonist of peripheral and centralnervous system.It has good effect on preventing and treating the nausea and vomiting induced by chemotherapy,radiotherapy and surgery. Tablets, capsules and injections are used in clinical at present.However, oral administration has disadvantages aciociated with first pass effect and low bioavailability about 60% and it is also difficult to use as a means of drug delivery to a patient who is already suffering severe nauses and vomiting. Similarly intravenous administrantion has a Poor patient compliance.Transdermal drug delivery system can ensure essentially constant drug input, Reduce or eliminate the liver first pass effect,reduce the side effect and improve compliance of the patients. SANCUSO,the transdermal patch which is developed by PROSTRAKAN company comes into market in 2008. Its patented technologies include the use of hydroxyl containing acrylic pressure sensitive adhesive technology (DURO-TAK (?) 87-2287).Based on the analysis of the foreign patent and our own technology advantages,we design a novel formulation of granisetron transdermal patch:granisetron is used as a raw material, carboxyl contained acrylic pressure sensitive adhesive DURO-TAK(?)87-2677 is selected as the matrix.It has strong anti-aging,good skin adaptability,high drug loading and sustained release of drugs.It increases the release of granisetron and its percutaneous permeation rate by adding pH adjusting agent aiming for decreasing the interaction between the pressure-sensitive adhesive and drug. Propylene glycol/IPM combinations are used to improve the granisetron transdermal absorption.Besides, vacuum packaging are used to increase the stability of granisetron in PSA.The permeation rate of the trasdermal patch of granisetron we prepare is similar with the patent WO 2004/069141 of PROSTRAKAN company.Optimal prescription is used on human skin, it is evaluated that the 24 hours permeation flux can reach 3mg with area of 52cm2,which is comparable with the SANCUSO public data which described the daily dose is 3mg.The patch has a good stability when vacuum sealed packaged by Aluminum foil.