ЧОВХАН Масуд А. (US),ХАН Уэсли Вехсин (US),ШНЕЙДЕР Л. Уэйн (US)
申请号：
RU2011130552/15
公开号：
RU2011130552A
申请日:
2009.12.08
申请国别(地区):
RU
年份:
2013
代理人:
摘要：
1. A local ophthalmic composition, wherein said composition includes: an active agent having lipophilicity, measured using a partition coefficient, Log D of more than 1.4, solubility at a physiological pH of less than 0.1%, and pKa between 7, 0 and 8.0, while the effective concentration of the active agent in the composition is more than 0.1%； an ibuffer salt having pKa outside the range between the pH of the finished form and a physiological pH of 7.4； however, the buffer salt does not form a salt crystal, which is less soluble than the solubility of the free base； while the composition is a solution without a surfactant； the composition is a solution having a pH range between 4.0 and 7.0.2. The ophthalmic composition according to claim 1, wherein the active agent is tandospiron or its salt, provided that the active agent is not the citrate salt of tandospiron. The ophthalmic composition according to claim 2, in which the crystalline form of tandospiron is selected from the group consisting of the free base of tandospiron and the hydrochloride salt of tandospiron. The ophthalmic composition according to claim 1, wherein the concentration of the active agent is from 0.1% to 10%. The ophthalmic composition according to claim 1, wherein said concentration of the active agent is from 0.1% to 10%. The ophthalmic composition according to claim 1, wherein the composition has a pH range between 4.7 and 5.5.7. The ophthalmic composition according to claim 1, in which the pH of the composition is approximately 5.1.8. The ophthalmic composition according to claim 1, wherein the composition does not cause a burning sensation in places1. Местная офтальмологическая композиция, при этом указанная композиция включает в себя:активный агент, обладающий липофильностью, измеренный с помощью коэффициента распределения, Log D более чем 1,4, растворимость при физиологическом pH менее чем 0,1%, и pKa между 7,0 и 8,0, при этом эффективная концентрация активного агента в композиции составля
