Swelling-controlled release system for the vaginal delivery of miconazole.
Swelling-controlled release system for the vaginal delivery of miconazole.
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DOI：
10.1016/s0939-6411(00)00124-7
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发表时间：
2000-11
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影响因子：
--
通讯作者：
T. Mandal
中科院分区：
文献类型：
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作者：
T. Mandal
硝酸咪康唑是一种杀真菌剂，对阴道炎的局部治疗有效。本项目的目的是开发一种咪康唑的溶胀控释给药系统。将15%w/w聚（乙烯醇）的水溶液与特定量的咪康唑粉末混合。所得混合物通过冻融交联。在四个水平上研究了冻融循环次数的影响。通过混合不同浓度的两种不同PEG来研究PEG存在的影响。对于经历四个循环的批次，在48小时结束时的溶胀显著更高（32%）。含有PEG 1000的批次在前15分钟内的溶胀约为9%。然而，在同一时间段内，含有浓度低得多的PEG 1450的批次的溶胀在10%至19%之间。药物释放曲线长达108小时是独立的冻融循环次数。在不存在PEG的情况下，在108 h结束时释放的咪康唑累积百分比（2、4、6、8个循环）为30 - 35%。与含PEG 1450的批次相比，含PEG 1000的批次的药物释放较低，与浓度无关。扩散指数（n）值的比较表明从水凝胶释放的Fickian扩散机制占优势。
Miconazole nitrate, a fungicidal, is effective for the local treatment of vaginitis. The objective of this project was to develop a swelling-controlled release delivery system for miconazole. An aqueous solution of 15% w/w poly(vinyl alcohol) was mixed with a specific amount of miconazole powder. The resultant mixture was cross-linked by freeze–thawing. The effect of the number of freeze–thawing cycles was studied at four levels. The effect of the presence of PEG was studied by mixing different concentrations of two different PEG. The swelling at the end of 48 h was significantly higher (32%) for the batch that underwent four cycles. The swelling within the first 15 min for the batches containing PEG1000 was approximately 9%. However, the swelling for the batches containing PEG1450, at much lower concentration, within the same period was between 10 and 19%. The drug release profiles up to 108 h were independent of the number of freeze–thawing cycles. The cumulative percent miconazole released, in the absence of PEG, (two, four, six, eight cycles) at the end of 108 h was between 30 and 35%. The drug release was lower for the batches containing PEG1000, irrespective of the concentrations, compared with the batches containing PEG1450. A comparison of the value of diffusional exponent (n) indicates the predominance of a Fickian diffusion mechanism of release from the hydrogels.