氨茶碱控释片体内外试验相关性的研究

本文研究了两种类型的氨茶碱控释片体内外试验的相关性。体外溶出试验表明骨架控释片和膜包衣控释片的溶出均属于表观一级释放过程,释放速度常数分别为0.1529h~(-1)和0.1510h~(-1)。体内试验表明,以单室模型拟合测得的血药浓度,其吸收速度常数分别为1.84h~(-1)和0.97h~(-1),二者有显著性差异,但其它动力学参数无显著性差异。体内外相关性研究表明,膜包衣控释片存在有一定相关性,而骨架片未见类似相关性。

CORRELATION BETWEEN THE ABSORPTION IN VIVO AND THE RELEASE IN VITRO OF TWO CONTROLLED-RELEASE TABLETS OF AMINOPHYLLINE

The correlation between the absorption in vivo and the release in vitro of two controlled-release tablets of Arainophylline was studied.The resultsof release test showed that the release-machanism for both tablets,a filmcoating-type controlled-release tablet(B)and a matrix-type controlled-release tablet(A),may be described by apparent first-order process atthe same dissolution condition.The apparent release rate constants werefound to be 0.1529 h~(-1) for A and 0.1150 h~(-1) for B.The absorption testswere performed in six heathy-male volunteers,who took orally A and Bat a single-dose 400 mg in a crossover design.The drug behaviour of B inthe GI was significantly different from that of A.The Ka(apparent ab-sorption rate constants)were 1.84 h~(-1) and 0.97 h~(-1) for A and B respec-tively(p<0.10).The correlation between the fraction of dose released invitro(X)and the fraction of dose absorbed in vivo(Y)for B was givenby the regression equation y=1.20X 3.25(r=0.985)during the first fourhours and by y=080X 69.07(r=0.962)during the subsequent four hours in all the tests.There existed no similar relation for A.