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NON-POROUS MICROSPHERES ADAPTED FOR PARENTERAL ADMINISTRATION, METHOD FOR PREPARING SAME AND SUSPENSION BASED ON SAID MICROSPHERES

机译:适用于腹腔镜管理的非多孔微球,基于所述微球的相同和悬浮物的制备方法

摘要

FIELD: medicine. SUBSTANCE: proposed solid non-porous sustained-effect microspheres have diameter 5-300 mcm and contain at least one pharmaceutically active substance enclosed into spherical envelope formed by at least one pharmaceutically inert carrier substance. Latter is naturally present in recipient's organism, remains stable in solid state up to at least 60 C, and is dissolved by recipient physiological medium at slower pace than pharmaceutically active principle. Proposed method for preparing said microspheres comprises following steps of: melting down pharmaceutically inert carrier substance, dispersing pharmaceutically active principle into melt in inert atmosphere, pulverizing dispersion thus-obtained in form of mist in freezing chamber under pressure in inert atmosphere at temperatures ranging from -15 C up to -50 C, separating resultant microspheres into fractions according to their sizes. Proposed suspension intended for administration by parenteral injection comprises effective amount of said microspheres distributed in pharmaceutically acceptable liquid vehicle, said pharmaceutically active principle being insoluble in said liquid vehicle. EFFECT: novel microspheres make it possible to retard and prolong curative effect of active agents which are too fast dissolved in physiological medium agents acting upon central or vegetative nervous system, such as vasodilative and antihistaminic agents, hormones, contraceptives. 16 cl, 13 dwg
机译:领域:医学。物质:提出的固体无孔持续作用微球直径为5-300 mcm,并包含至少一种药物活性物质,该药物活性物质封闭在由至少一种药物惰性载体物质形成的球形包膜中。后期自然存在于接受者的生物体中,在至少60°C的温度下仍保持固态稳定,并且被接受者的生理介质溶解的速度比药物活性成分慢。提议的制备所述微球的方法包括以下步骤:在惰性气氛中将药学上惰性的载体物质熔化,将药物活性成分分散到熔体中,在惰性气氛中在压力下在冷冻室中以雾状将如此获得的分散体粉碎成雾状,温度范围为- 15 C至-50 C,根据其大小将生成的微球分为多个部分。拟通过肠胃外注射给药的建议的混悬剂包括有效量的分布在药学上可接受的液体媒介物中的所述微球,所述药学活性成分不溶于所述液体媒介物中。效果:新的微球可以延缓和延长太快溶解在作用于中枢或植物神经系统的生理介质中的活性剂的作用,例如血管扩张和抗组胺药,激素,避孕药。 16厘升,13载重吨

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