盐酸维拉帕米缓释片体外溶出及生物利用度的研究

Dissolution Test in Vitro and Bioavailability Study on Sustained-Release Verapamil Hydrochloride Tablets

对盐酸维拉帕米缓释片(VR·HCl-SRT)的体外溶出速率进行了研究,HPLC法测定了8名健康受试者口服单剂量及多剂量时的稳态血药浓度,并以Knoll公司Isoptin-SRT及市售普通片为对照,实验数据按单室模型采用AST 360型计算机和非线性最小二乘法模型嵌合程序进行迭代处理,求得药动学参数。结果表明:VR·HCl-SRT达峰时间较Isoptin-SRT短,而维持体内有效血浓时间长,相对生物利用度为112.9%,体内外显著相关。理论值与实测值基本相符。

This paper deals with the preparation and evaluation of sustained-release verapamil hydrochloride (VR·HCl-SRT) tablet by measuring in vitro/in vivo test. The plasma levels of VR·HCl in eight volunteers following the single and multiple oral doses of three dosage forms were determined using HPLC method. The pharmacokinetic paramaters were fitted by nonlinear leastsquare method with a computer on the basic of two-compartment model. The results showed that the VR·HCl-SR tablets released drug with a first-order kinetic and a significant correlation was found between in vitro dissolution and in vivo absorption. The pharmacokinetic-pharmacodynamic data suggested a good relationship between the drug concentration in plasma and therapeutic effects.