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采用 MTR 技术增强阿苯达唑丸的溶出度。

Enhancement of the dissolution of albendazole from pellets using MTR technique.

机构信息

Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia ; Department of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Al-Azhar University, Assiut, Egypt.

出版信息

Saudi Pharm J. 2013 Apr;21(2):215-23. doi: 10.1016/j.jsps.2012.03.001. Epub 2012 Mar 19.

Abstract

Albendazole (ABZ), a broad-spectrum anthelmintic agent, is poorly absorbed after oral administration due to its low aqueous solubility. The aim of this study was to improve albendazole dissolution rate by formulating avicel pellets loaded with 10% w/w drug using extrusion/spheronization technique. In addition the wet masses were characterized by mix torque rheometry (MTR) prior to pelletization process. Different additives (i.e., lactose, Tween 80 and low molecular weight chitosan) were formulated with avicel to enhance the dissolution rate of ABZ from the produced pellets. Moreover, mix torque rheometer was used to quantitatively determine the suitable moisture content in the pastes before the extrusion process. The produced pellets were characterized for their ABZ content, particle size, particle shape, dissolution profile and thermal behaviors. The maximum consistencies (the peak torques) of the wet granules were obtained using 0.667-1.333 ml/g of water or water containing surfactant. Also, the produced pellets have size range from 1036 to 1246 μm. The calculated drug RDR30 for 10%, 30% and 50% lactose concentrations were 1.08, 1.08 and 2.03, respectively, while that calculated for 10%, 30% and 50% w/w chitosan concentrations were 1.71, 3.62 and 3.62, respectively. The results revealed also that increasing the weight ratio of lactose and chitosan was accompanied by a significant reduction of the peak torque magnitude and this was accompanied by an enhanced ABZ dissolution rate.

摘要

阿苯达唑(ABZ)是一种广谱驱虫药,由于其水溶性低,口服后吸收不良。本研究旨在通过挤出/滚圆技术,用载药量为 10%w/w 的 AVICEL 微丸来提高 ABZ 的溶出速率。此外,在微丸化之前,通过混合转矩流变仪(MTR)对湿物料进行了特性研究。用 AVICEL 与不同添加剂(即乳糖、吐温 80 和低分子量壳聚糖)一起配制,以提高从所制得的微丸中 ABZ 的溶出速率。此外,混合转矩流变仪用于在挤出过程之前定量确定糊剂中的合适水分含量。对所制得的微丸进行了 ABZ 含量、粒径、颗粒形状、溶出度和热行为的特性研究。使用 0.667-1.333ml/g 的水或含有表面活性剂的水,湿颗粒的最大稠度(峰值扭矩)可获得最大稠度。此外,所制得的微丸的粒径范围为 1036-1246μm。对于 10%、30%和 50%乳糖浓度,计算得到的药物 RDR30 分别为 1.08、1.08 和 2.03,而对于 10%、30%和 50%w/w 壳聚糖浓度,计算得到的药物 RDR30 分别为 1.71、3.62 和 3.62。结果还表明,乳糖和壳聚糖的重量比增加伴随着峰值扭矩幅度的显著降低,这伴随着 ABZ 溶出速率的提高。

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Enhancement of the dissolution of albendazole from pellets using MTR technique.采用 MTR 技术增强阿苯达唑丸的溶出度。
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