【摘要】：通過單因素試驗篩選鹽酸普拉克索緩釋片處方,采用Box-Behnken效應(yīng)面法優(yōu)化處方并制備鹽酸普拉克索緩釋片。單因素試驗考察羥丙基甲基纖維素(HPMC)不同型號、不同用量及與不溶性緩釋材料組合使用對鹽酸普拉克索緩釋片體外釋放度的影響。確定以HPMC K100M、Eudragit RSPO、Eudragit L100為主要考察因素,以不同時間的累積釋放度為評價指標。Box-Behnken效應(yīng)面法優(yōu)化處方得出三者的最優(yōu)范圍,以其中優(yōu)選處方HPMC K100M 101.5 mg、Eudragit RSPO 98mg和Eudragit L100 13.7 mg和其他輔料制備鹽酸普拉克索緩釋片并考察釋放度。通過相似因子計算,優(yōu)選處方的體外累積釋放度預(yù)測值和實測值相似度均大于80。對體外釋藥數(shù)據(jù)進行方程擬合,探討其釋藥機制,Eudragit RSPO促進鹽酸普拉克索的釋放,Eudragit L100阻滯鹽酸普拉克索的釋放,二者互為拮抗作用。結(jié)果表明,該處方制備的普拉克索緩釋片p H依賴性小,體外釋放行為穩(wěn)定,實現(xiàn)了該緩釋片的處方優(yōu)化。
[Abstract]:The formulation of Praxol hydrochloride sustained-release tablets was selected by single factor test. The formulation was optimized by Box-Behnken effect surface method and Praxol hydrochloride sustained release tablets were prepared. The effects of different types of hydroxypropyl methylcellulose (HPMC), different dosage and combination with insoluble sustained-release materials on the in vitro release of Praxol hydrochloride sustained-release tablets were investigated by single factor test. Taking HPMC K100m Eudragit RSPO,Eudragit L100 as the main investigation factor and the cumulative release of different time as the evaluation index, the optimal range of the three prescriptions was obtained by Box-Behnken effect surface method, in which the optimal prescription HPMC K100M 101.5 mg, was selected. Praxol hydrochloride sustained release tablets were prepared by Eudragit RSPO 98mg and Eudragit L 100 13.7 mg and other excipients. Through the calculation of similarity factor, the prediction value of cumulative release in vitro and the similarity of measured value of optimal prescription were higher than 80. The in vitro drug release data were fitted to investigate the mechanism of drug release:, Eudragit RSPO promoted the release of Praxol hydrochloride, and Eudragit L100 blocked the release of Praxol hydrochloride, which was antagonistic to each other. The results showed that the Praxol sustained-release tablets prepared by this prescription had less pH dependence and stable release behavior in vitro, and the formulation of the tablets was optimized.
【作者單位】： 中國藥科大學(xué)中藥學(xué)院;江蘇神龍藥業(yè)有限公司;
【基金】：江蘇省“創(chuàng)新團隊計劃”(科技類)資助項目~~
【分類號】：R944

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本文編號：2366184