摘要
溶出度按Weibull's分布处理得Td=5.76 h,T_(50)=3.9 h,零级溶出速度常数K_t=9.9450,平均体外溶解时间MDT=5.391 h。测定8名健康受试者,单剂量口服,得C_(max)=76.2±16.7 ng/ml,T_(amx)=8.0 h,t_(1/2)=9.75 h,MRT=19.41 h,MAT=5.34 h,与Knoll公司SR片相比,F_(rel)=101.71%;与市售普通片相比,F_(rel)=96.16%。多剂量口服,得C_(max)=121.47±34.5 ng/ml,T_(max)=7.14 h。按Loo-Riegelman方程处理表明体内外显著相关。理论值与实测值基本相符。
This paper deals with the evaluation of osmotic pump of verapamil hydrochloridetablet(C) by measuring/n vitro/in vivo test. The results showed that the dissolution behaviors were of zero-order kinetic and release constant in vitro(Kr) of C was 9.9450. The plasma levels of Ver·HCl in eight volunteers following single and multiple oral doses of these dosage forms were determined using HPLC method. The pharmacokinetic parameters were fitted by nonlinear least square method with a computer on the basis of two-compartment model. The pharmacokinetic parameters of C_(max), T_(max), t_(1/2), K_a, K_(10) and K_(21) were calculated. The bioavailability of tablet C relative to B and A was 101.7%, 96. 16% respectively. A significant correlation was found between/n vitro dissolution and m vivo absorption.
出处
《药学学报》
CAS
CSCD
北大核心
1993年第9期714-720,共7页
Acta Pharmaceutica Sinica
关键词
盐酸
维拉帕米
溶出度
生物利用度
Verapamil hydrochloride
Oral osmotic pump
HPLC
Dissolution rate
Pharmacokinetics
