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二磷酸伯氨喹脂质体的表征、体外和体内研究

Characterization, in vitro and in vivo studies on primaquine diphosphate liposomes.

作者信息

Arica B, Ozer A Y, Ercan M T, Hincal A A

机构信息

Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Ankara, Turkey.

出版信息

J Microencapsul. 1995 Sep-Oct;12(5):469-85. doi: 10.3109/02652049509006778.

Abstract

In this study, several Primaquine diphosphate (PQ) liposomal formulations containing phospholipid, charge inducer and with or without cholesterol in molar ratios of 7:1:(2) and 10:1:(4) were investigated. Gel state (DPPC:CHEMS:CHOL and PL-100H:CHEMS:CHOL) and liquid-crystalline state (PL-100:CHEMS:CHOL and PL-90G:CHEMS:CHOL) liposomes were prepared. The film method followed by sonication and extrusion through polycarbonate membrane was used. Particle size distribution, percentage of entrapped active substance, content of phospholipid and bilayer type and composition were determined. Lamellarity was determined by 31P-NMR technique. In vitro release of PQ was investigated at 37 degrees C, 35 rpm and in Tris (pH: 7.4) buffer. In vitro release and its fit to kinetic models were investigated. Liposomes were labelled by 99mTc and injected intravenously to Swiss Albino mice.

摘要

在本研究中,对几种含有磷脂、电荷诱导剂且胆固醇摩尔比为7:1:(2)和10:1:(4)的二磷酸伯氨喹(PQ)脂质体制剂进行了研究。制备了凝胶态(二棕榈酰磷脂酰胆碱:胆固醇硫酸酯钠:胆固醇和PL - 100H:胆固醇硫酸酯钠:胆固醇)和液晶态(PL - 100:胆固醇硫酸酯钠:胆固醇和PL - 90G:胆固醇硫酸酯钠:胆固醇)脂质体。采用薄膜法,随后进行超声处理并通过聚碳酸酯膜挤出。测定了粒径分布、包封活性物质的百分比、磷脂含量以及双层类型和组成。通过31P - NMR技术测定了片层结构。在37℃、35转/分钟的条件下,在Tris(pH:7.4)缓冲液中研究了PQ的体外释放。研究了体外释放及其与动力学模型的拟合情况。脂质体用99mTc标记并静脉注射给瑞士白化小鼠。

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