Jh. Guo et Km. Cooklock, BIOADHESIVE POLYMER BUCCAL PATCHES FOR BUPRENORPHINE CONTROLLED DELIVERY - SOLUBILITY CONSIDERATION, Drug development and industrial pharmacy, 21(17), 1995, pp. 2013-2019
By using a two-roll milling method, a new bioadhesive polymer patch fo
rmulation for buprenorphine controlled delivery and consisting of poly
isobutylene, polyisoprene, and Carbopol(R) 934P was prepared. Since so
lubility of drug in the polymer patches is the first factor which shou
ld be considered before to modify the feasibility of delivering drug t
hrough the buccal mucosa, the effects of alpha-cyclodextrin, beta-cycl
odextrin, sodium taurocholate, and sodium glycodeoxycholate on the sol
ubility of buprenorphine were investigated, and beta-cyclodextrin was
found the strongest solubility enhancer of them. The drug release prof
iles were significantly affected by the drug loading and the existence
of beta-cyclodextrin. Increasing the drug loading and solubility enha
ncer would increase the drug release from the buccal polymer patches.
The pH value change in the microenviroment of polymer patches during t
he hydration of Carbopol(R) 934P could even release 20% of drug from t
he polymer patches which didn't contain any solubility enhancer.