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[贝诺酯片的处方及生物利用度研究]

[Studies on formulation and bioavailability of benorilate tablets].

作者信息

Chen J, Tu X D

机构信息

Department of Pharmaceutics, China Pharmaceutical University, Nanjing.

出版信息

Yao Xue Xue Bao. 1994;29(9):707-12.

PMID:7900541
Abstract

A new formulation tablet B was developed and compared with tablet A with the purpose of improving the bioavailability of benorilate by reducing its particle size. The dissolution rate in vitro was determined by paddle method and using surfactant solution medium. The plasma concentrations of hydrolyzates which are salicylic acid and paracetamol from benorilate in vivo were measured by HPLC. The dissolution rates of ground and unground drug are 0.0337 min-1 and 0.0152 min-1 (P < 0.001) respectively. Compared with tablet A, the cumulative dissolution percentage of B is higher. The mean dissolution time of B and A are 15.77 min and 42.25 min (P < 0.001) respectively. The study in vivo showed that the Cmax, Tp and AUC of salicylic acid for these two formulations have no significant difference (P > 0.1). The relative bioavailability of B to A is 125.59%. Their in vivo process fits one-compartment model and first order elimination.

摘要

开发了一种新的制剂片剂B,并与片剂A进行比较,目的是通过减小贝诺酯的粒径来提高其生物利用度。体外溶出速率采用桨法并使用表面活性剂溶液介质进行测定。体内贝诺酯水解产物水杨酸和对乙酰氨基酚的血浆浓度通过高效液相色谱法测定。研磨药物和未研磨药物的溶出速率分别为0.0337 min⁻¹和0.0152 min⁻¹(P < 0.001)。与片剂A相比,B的累积溶出百分比更高。B和A的平均溶出时间分别为15.77分钟和42.25分钟(P < 0.001)。体内研究表明,这两种制剂的水杨酸的Cmax、Tp和AUC没有显著差异(P > 0.1)。B相对于A的相对生物利用度为125.59%。它们的体内过程符合一室模型和一级消除。

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