Preparation of double-encapsulated microcapsules for mitigating drug loss and extending release.

Preparation of double-encapsulated microcapsules for mitigating drug loss and extending release.
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用于减轻药物损失和延长释放的双囊微胶囊的制备。

DOI:
10.1080/02652040010019460
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发表时间:
2001
影响因子:
3.9
通讯作者:
H. Chen
H. Chen
中科院分区:
医学4区
文献类型:
--
作者:
Y. Tsai;C. C. Jong;H. Chen

文献摘要

被引文献

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采用无溶剂加成、相分离法制备双囊微胶囊,形成芯材,采用O/W乳状液非溶剂加成法制备双囊微胶囊,提高载药量,调节释药速率。使用的药物是茶碱,它是水溶性的。以二氯甲烷为溶剂,正己烷为非溶剂。本研究考察了不同的芯材和微囊EC/TH比例对药物损失、颗粒大小、表面形态和释放速率的影响。双囊化微囊的药物损失率比单用O/W乳状液无溶剂添加法制备的微囊低12.8%。在第二次包埋过程中,随着EC聚合物浓度的增加,双包埋微胶囊的粒径逐渐减小。它们的表面粗糙度也与第二次包埋过程中使用的聚合物溶液的浓度成正比。溶出度研究表明,双囊化微囊的T20为2~35.4h,O/W乳液型无溶剂法微囊的T20为2.7~7.7h,当EC不超过临界值时,聚合物溶液中EC的含量越大,微囊中药物的释放速度越慢。
The double-encapsulated microcapsules were prepared by the non-solvent addition, phase-separation method to form core material and, encapsulated with the O/W emulsion non-solvent addition method to increase drug loading and regulate drug release rate. The drug used was theophylline, which is water-soluble. Dichloromethane and n-hexane were used as the solvent and non-solvent, respectively. This study investigated how various core material and microcapsule EC/TH ratios affect the drug loss, particle size, surface morphology and release rate. The drug loss of the double-encapsuLated microcapsules was 12.8% less than that of microcapsules prepared by the O/W emulsion non-solvent addition method alone. The particle size of these double-encapsulated microcapsules decreased as the concentration of EC polymer was increased in the second encapsulation process. The roughness of their surface was also in proportion to the concentration of polymer solution used in the second encapsulation process. The dissolution study showed that the T20 of the double-encapsulated microcapsules ranged from 2-35.4 h, while that of the O/W emulsion non-solvent addition method microcapsules was from 2.7-7.7 h. The greater the level of EC in the polymer solution, the slower the release rate of the drug from the microcapsules when the EC was not over the critical amount.