Lipase-catalyzed regioselective preparation of fatty acid esters of hydrocortisone
摘要:
A series of fatty acid derivatives of hydrocortisone has been prepared by an enzymatic methodology. Nine 21-monoacyl products and one 3,11,17-triacetyl derivative, nine of them novel compounds, were obtained in a highly regioselective way through lipase-catalyzed esterification, transesterification and alcoholysis reactions. The influence of various reaction parameters Such as acylating agent: substrate ratio, enzyme: substrate ratio. solvent, temperature and nature of acylating agent and alcohol was evaluated. Among the tested lipases. Candida antarctica lipase appeared to be the most appropriate and showed a high efficient behavior especially in a one-pot transesterification. The advantages presented by this methodology, such as mild reaction conditions and low environmental impact, make the biocatalysis a convenient way to prepare acyl derivatives of hydrocortisone. These lipophilic compounds are potential products in the pharmaceutical industry. (C) 2009 Elsevier Inc. All rights reserved.
Use of tocopherol ascorbic adic phosphates for hemorrhoidal diseases
申请人:Senju Pharmaceutical Co., Ltd.
公开号:EP0661053A1
公开(公告)日:1995-07-05
A therapeutic agent for hemorrhoidal diseases, comprising, as an active ingredient, a diester phosphate compound of the formula (I)
wherein R₁ and R₂ are the same or different and each is a hydrogen atom or a methyl, or a pharmacologically acceptable salt thereof, and a method for treating hemorrhoidal diseases, comprising administering a pharmaceutically effective amount of said diester phosphate compound or a pharmacologically acceptable salt thereof.
An ophthalmic composition which contains a component A consisting of at least one member selected from the group consisting of polyoxyalkylene block copolymers and their derivatives, and a component B consisting of at least one member selected from the group consisting of caproic acid and its derivatives.
一种眼科组合物,其中包含至少一种由聚氧亚烷基嵌段共聚物及其衍生物组成的成分 A 和至少一种由己酸及其衍生物组成的成分 B。
Antifungal compositions comprising Sertaconazole and either Hydrocortisone or an antibacterial agent
申请人:FERRER INTERNACIONAL, S.A.
公开号:EP1698336A1
公开(公告)日:2006-09-06
Pharmaceutical compositions useful for treating dermal diseases caused by fungi and yeasts with inflammation and/or associated with a bacterial infection. Such compositions contain a therapeutically effective amount of Sertaconazole, or a pharmaceutically acceptable salt, solvate, isomer thereof or mixtures thereof; and a therapeutically effective amount of at least one compound selected from the group consisting of Hydrocortisone, a pharmaceutically acceptable ester of Hydrocortisone, an antibacterial agent or mixtures thereof.
ANTIFUNGAL COMPOSITIONS COMPRISING SERTACONAZOL AND HYDROCORTISONE AND/OR AN ANTIBACTERIAL QUINOLONE COMPOUND
申请人:FERRER INTERNACIONAL, S.A.
公开号:EP1858510A1
公开(公告)日:2007-11-28
Antifungal Compositions
申请人:Palacin Celia
公开号:US20080166398A1
公开(公告)日:2008-07-10
Pharmaceutical compositions useful for treating dermal diseases caused by fungi and yeasts with inflammation and/or associated with a bacterial infection. Such compositions contain a therapeutically effective amount of sertaconazole, or a pharmaceutically acceptable salt, solvate, isomer thereof or mixtures thereof; and a therapeutically effective amount of at least one compound selected from the group consisting of hydrocortisone, a pharmaceutically acceptable ester of hydrocortisone, an antibacterial quinolone compound, and mixtures thereof.