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通过乳液溶剂扩散法制备的中空微球(微球囊)浮力测定的物理化学性质。

Physicochemical properties to determine the buoyancy of hollow microspheres (microballoons) prepared by the emulsion solvent diffusion method.

作者信息

Sato Yasunori, Kawashima Yoshiaki, Takeuchi Hirofumi, Yamamoto Hiromitsu

机构信息

Teikoku Hormone Mfg. Co., Ltd., Kanagawa, Japan.

出版信息

Eur J Pharm Biopharm. 2003 May;55(3):297-304. doi: 10.1016/s0939-6411(03)00003-1.

Abstract

Hollow microspheres (microballoons) floatable on JPXIII No.1 solution were developed as a dosage form capable of floating in the stomach. Hollow microspheres were prepared by the emulsion solvent diffusion method using enteric acrylic polymers with drug in a mixture of dichloromethane and ethanol. It was found that preparation temperature determined the formation of cavity inside the microsphere and the surface smoothness, determining the floatability and the drug release rate of the microballoon. The correlation between the buoyancy of microballoons and their physical properties, e.g. apparent density and roundness of microballoons were elucidated. The drug loading efficiency of microballoons with various types of drug was investigated and correlated to the distribution coefficient of drug between dichloromethane and water. The optimum loading amount of riboflavin in the microballoon was found to impart ideal floatable properties to the microballoons. On the other hand, little entrapment was observed for aspirin due to the low distribution coefficient; however, entrapment improved to some extent upon reduction of the pH of the process.

摘要

研制出了可漂浮于JPXIII No.1溶液上的中空微球(微囊),作为一种能够在胃中漂浮的剂型。采用乳液溶剂扩散法,以肠溶丙烯酸聚合物为原料,在二氯甲烷和乙醇的混合物中加入药物制备中空微球。结果发现,制备温度决定了微球内部空洞的形成以及表面光滑度,进而决定了微囊的漂浮性和药物释放速率。阐明了微囊的浮力与其物理性质(如微囊的表观密度和圆度)之间的相关性。研究了不同类型药物微囊的载药效率,并将其与药物在二氯甲烷和水之间的分配系数相关联。发现微囊中核黄素的最佳负载量能赋予微囊理想的漂浮性能。另一方面,由于阿司匹林的分配系数较低,观察到其包封率较低;然而,在降低制备过程的pH值后,包封率有所提高。

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