Basu Sanat Kumar, Rajendran Adhiyaman
Division of Pharmaceutics, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
Chem Pharm Bull (Tokyo). 2008 Aug;56(8):1077-84. doi: 10.1248/cpb.56.1077.
Nateglinide loaded alginate-chitosan beads were prepared by ionic gelation method for controlling the drug release by using various combinations of chitosan and Ca2+ as cation and alginate as anion. IR spectrometry, scanning electron microscopy, differential scanning calorimetry and X-ray powder diffractometry were used to investigate the physicochemical characteristics of the drug in the bead formulations. The calcium content in beads was determined by atomic absorption spectroscopy. The swelling ability of the beads in different media (pH 1.2, 4.5, 6.8) has been found to be dependent on the presence of polyelectrolyte complex of the beads and the pH of the media. The ability to release the Nateglinide was examined as a function of chitosan and calcium chloride content in the gelation medium. It is evident that the rate of drug release and its kinetics could be controlled by changing the chitosan and the calcium chloride concentrations. Calcium alginate beads released more than 95% of drug with in 8 h; whereas coated beads sustained the drug release and released only 75-80% of drug. The drug release mechanism analyzed indicates that the release follows either "anomalous transport" or "case-II transport".
采用离子凝胶法制备了载有那格列奈的海藻酸钠-壳聚糖微球,通过使用壳聚糖和Ca2+作为阳离子以及海藻酸钠作为阴离子的各种组合来控制药物释放。采用红外光谱、扫描电子显微镜、差示扫描量热法和X射线粉末衍射法研究了微球制剂中药物的物理化学特性。通过原子吸收光谱法测定微球中的钙含量。已发现微球在不同介质(pH 1.2、4.5、6.8)中的溶胀能力取决于微球的聚电解质复合物的存在以及介质的pH值。研究了那格列奈的释放能力与凝胶介质中壳聚糖和氯化钙含量的关系。显然,通过改变壳聚糖和氯化钙的浓度可以控制药物释放速率及其动力学。海藻酸钙微球在8小时内释放了超过95%的药物;而包衣微球则持续释放药物,仅释放了75-80%的药物。分析的药物释放机制表明,释放遵循“异常转运”或“Ⅱ型转运”。