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    • 1. 发明申请
    • METHOD FOR PROLONGING ACTIVITY OF AUTODEGRADABLE ENZYMES AND COMPOSITIONS THEREOF
    • 用于增强可自由可扩链酶活性的方法及其组合物
    • US20100104551A1
    • 2010-04-29
    • US12603988
    • 2009-10-22
    • Dharmendra M. JaniKai KwokGregory L. McIntireBruce A. PfefferAfshin ShafieeRuiwen ShiSrini VenkateshHongna WangYan HuangStephen R. Davio
    • Dharmendra M. JaniKai KwokGregory L. McIntireBruce A. PfefferAfshin ShafieeRuiwen ShiSrini VenkateshHongna WangYan HuangStephen R. Davio
    • A61K38/48A61P27/02
    • C12N9/50A61K31/198C12N9/6435C12N9/96C12Y304/21007
    • A composition of a long-acting enzyme comprises the enzyme in a formulation comprising a buffer and an additive selected from the group consisting of tranexamic acid, ε-aminocaproic acid, and analogs of L-lysine other than tranexamic acid and ε-aminocaproic acid, combinations thereof, and mixtures thereof. The composition can further comprise another additive selected from the group consisting of L-lysine, L-arginine, L-ornithine (or its pharmaceutically acceptable salts; e.g., L-ornithine hydrochloride), γ-aminobutyric acid, 5-aminovaleric acid, 7-aminoheptanoic acid, glycylglycine, triglycine, N-α-acetyl-L-arginine, betaine, sarcosine, gelatin, HSA, streptokinase, tPA, uPA, non-ionic surfactants, glycerin, D-sorbitol, combinations thereof, and mixtures thereof. A method for prolonging the activity of an autodegradable enzyme comprises storing the enzyme after manufacture at a low pH, and reconstituting the acidified enzyme before use with a solution containing at least one of such additives. The method is useful to provide enzyme for wide use, which otherwise would lose activity upon long storage. In one embodiment the method is applicable to provide enzyme for inducing controlled posterior vitreous detachment.
    • 长效酶的组合物包含在包含缓冲液和添加剂的制剂中的酶,所述缓冲剂和添加剂选自氨甲环酸,氨基己酸和除了氨甲环酸以外的L-赖氨酸和β-氨基己酸 酸,其组合,及其混合物。 所述组合物可以进一步包含选自L-赖氨酸,L-精氨酸,L-鸟氨酸(或其药学上可接受的盐,例如L-鸟氨酸盐酸盐),γ-氨基丁酸,5-氨基戊酸,7 氨基庚酸,甘氨酰甘氨酸,三甘氨酸,N-α-乙酰基-L-精氨酸,甜菜碱,肌氨酸,明胶,HSA,链激酶,tPA,uPA​​,非离子表面活性剂,甘油,D-山梨糖醇,其组合及其混合物。 用于延长自动降解酶的活性的方法包括在低pH下制备后储存酶,并且在使用前将酸化酶与含有至少一种这样的添加剂的溶液重新组合。 该方法对于提供广泛使用的酶是有用的,否则将在长期储存时失去活性。 在一个实施方案中,该方法适用于提供用于诱导受控的后玻璃体脱离的酶。