发明名称 |
THE PROCESS FOR MANUFACTURING FORMULATION OF TOPICAL BETA BLOCKERS WITH IMPROVED EFFICACY |
摘要 |
Beta blockers are used as topical ophthalmic preparation for reducing Intra Ocular Pressure. B-blocker used for this purpose include timolol, levobunolo l, carteolol, metipranalol. They reduce the aqueous production and thereby redu ce I.O.P. They are commonly used as drops. Efficacy of topical B-blockers is dependent on concentration of drug in formulation. However, increasing the concentration of drug beyond approved dosage forms does not increase the efficacy significantly e.g. Timolol 0.5% has identical pressure lowering capacity as 1% Timolol. The attempts to improve pressure reduction efficienc y of B-blockers has not met with success so far. The sustained release formulation of Timolol (Timolol XE) has resulted in amount of drug to achiev e same therapeutic effect. However, none of the formulation has improved efficacy of drug for reducing I.O.P. The present invention relates to the process of manufacturing such formulation of B-blocker which improves its I.O.P lowering effect. The formulation so prepared is non-irritating and wel l tolerated. The process of manufacturing new formulation with improved effica cy involves use of carboprolol and preservative. The timolol 0.5% gel formulate d using process was evaluated in normal as well as glaucomatous eyes. The reduction in I.O.P. is found to be approx. 15% more than found with drops in normal individuals. Similar findings are also observed in glaucomatous eyes.
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申请公布号 |
CA2354765(A1) |
申请公布日期 |
2000.06.22 |
申请号 |
CA19992354765 |
申请日期 |
1999.03.04 |
申请人 |
KHAMAR, BAKULESH MAFATLAL |
发明人 |
KHAMAR, BAKULESH MAFATLAL |
分类号 |
A61K31/13;A61K9/00;A61K31/138;A61K31/216;A61K31/4704;A61K31/5355;A61K31/78;A61K47/00;(IPC1-7):A61K31/13 |
主分类号 |
A61K31/13 |
代理机构 |
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代理人 |
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地址 |
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