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LIPOSOME-TYPE MIXED TOPICAL ANESTHETIC USED FOR APPLYING TO WOUND AND PRODUCING METHOD THEREOF

机译:用于伤口的脂质体型混合麻醉剂及其生产方法

摘要

PURPOSE: A liposome-type mixed topical anesthetic used for applying to the wound and a producing method thereof are provided, thereby the produced anesthetic can rapidly penetrate into the corneous tissue of the skin and sustains efficacy for a long time. CONSTITUTION: The liposome-type mixed topical anesthetic contains 0.5 to 10 wt.% of topical anesthetic and 20 to 50 wt.% of mixed lipid mixed of phospholipid and cholesterol, in which the topical anesthetic is selected from the group consisting of lidocaine, tetracaine, ropivacaine, cocaine and pontocaine; phospholipid is selected from the group consisting of phosphatidylcholine, dioleoylphosphatidyl, palmitoylphosphatidyl, phosphatidylethanolamine, phosphatidylserine and phosphatidylglycerol. The liposome-type mixed topical anesthetic is produced by dissolving 0.5 to 10 wt.% of topical anesthetic and 20 to 50 wt.% of mixed lipid in organic solvents, evaporating the organic solvent in a rotation evaporator to form a thin layer lipid film, hydrating the film in a buffer solution having pH 7.0 to 8.2, and repeating freezing and melting to produce the liposome-type mixed topical anesthetic, in which organic solvent is chloroform, methanol, ethanol, and diethylether.
机译:用途:提供了一种用于伤口的脂质体型混合局部麻醉剂及其生产方法,从而使所生产的麻醉剂能够快速渗透到皮肤的角质组织中并长期保持疗效。组成:脂质体型混合局部麻醉药含有0.5至10 wt。%的局部麻醉药和20至50 wt。%的混合磷脂和胆固醇的脂质,其中局部麻醉药选自利多卡因,丁卡因罗哌卡因,可卡因和pontocaine;磷脂选自磷脂酰胆碱,二油酰基磷脂酰,棕榈酰磷脂酰,磷脂酰乙醇胺,磷脂酰丝氨酸和磷脂酰甘油。脂质体型混合局部麻醉剂是通过将0.5至10重量%的局部麻醉剂和20至50重量%的混合脂质溶解在有机溶剂中,然后在旋转蒸发仪中蒸发有机溶剂以形成薄层脂质膜来制备的,将膜在pH 7.0至8.2的缓冲溶液中水合,并重复冷冻和熔化以产生脂质体型混合局部麻醉剂,其中有机溶剂为氯仿,甲醇,乙醇和二乙醚。

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