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钙浓度、硬化剂和干燥条件对果胶酸钙凝胶珠中口服蛋白质释放特性的影响。

Effect of calcium concentration, hardening agent and drying condition on release characteristics of oral proteins from calcium pectinate gel beads.

作者信息

Sriamornsak P

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.

出版信息

Eur J Pharm Sci. 1999 Jul;8(3):221-7. doi: 10.1016/s0928-0987(99)00010-x.

Abstract

Pectin has been investigated for its ability to produce solid calcium pectinate gel (CPG) beads containing bovine serum albumin (BSA). Several factors can influence the properties and release characteristics of the CPG beads. In this study, the effect of calcium concentration, hardening agent and drying condition on the encapsulation and release characteristics of BSA from the matrix gel beads made of calcium pectinate were studied. BSA release studies under conditions mimicking mouth to colon transit have shown that calcium pectinate protects the drug from being released completely in the physiological environment of the upper gastrointestinal tract, and is susceptible to the enzymatic action with consequent drug release. In addition, the release of BSA from CPG beads was strongly affected by calcium concentration and drying condition. However, the release was not particularly affected by the presence of hardening agent at the concentration of 1% or lower. Since the release of BSA as a model protein drug could be controlled by the regulation of the preparation conditions of CPG beads, the CPG beads may be used for a potential oral controlled release system for protein drugs.

摘要

人们已对果胶生产含牛血清白蛋白(BSA)的固体果胶酸钙凝胶(CPG)珠粒的能力进行了研究。有几个因素会影响CPG珠粒的性质和释放特性。在本研究中,研究了钙浓度、硬化剂和干燥条件对由果胶酸钙制成的基质凝胶珠粒中BSA的包封和释放特性的影响。在模拟口腔到结肠转运的条件下进行的BSA释放研究表明,果胶酸钙可保护药物在上消化道的生理环境中不会完全释放,并易受酶作用从而导致药物释放。此外,CPG珠粒中BSA的释放受钙浓度和干燥条件的强烈影响。然而,在浓度为1%或更低时,硬化剂的存在对释放没有特别影响。由于作为模型蛋白药物的BSA的释放可通过调节CPG珠粒的制备条件来控制,因此CPG珠粒可用于潜在的蛋白药物口服控释系统。

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