Stable aqueous compositions of prostaglandin agonist prodrugs and methods of use thereof
A prostaglandin and composition technology, applied in the direction of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of inactive esters, inactive therapeutically active compounds, etc.
Inactive Publication Date: 2016-05-18
ALLERGAN INC
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Problems solved by technology
Usually, but not necessarily, the ester is inactive or less active than the therapeutically active compound to which it is converted
Method used
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[0070] Compounds 2 and 3 were used to evaluate the aqueous stability of the compositions of the invention. Four formulations were prepared for each compound as shown in the table below.
[0071] Table 1
[0072]
[0073] Table 2
[0074]
[0075] The formulations were analyzed by HPLC using the following measurement parameters.
[0076] Column: BioWidePoreC18 (SUPELCO), 4.6mmx25cm, 5μm
[0077] Mobile phase A: 0.1% (V / V) trifluoroacetic acid (TFA) in deionized water, 0.8 micron filtered
[0078] Mobile phase B: 100% acetonitrile, 0.8 micron filtered
[0079] Column temperature: ambient temperature
[0080] Injection volume: 30μL
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The present invention is based on obtaining significantly increased aqueous stability of the composition (thus shelf life) found. Accordingly, the compositions and methods of the present invention provide the aqueous stability required for commercially available topical medical treatments for a number of visual disorders.
Description
[0001] related application [0002] This application claims the benefit of US Provisional Application Serial No. 61 / 267,897, filed December 9, 2009, the disclosure of which is incorporated herein by reference in its entirety. technical field [0003] The present invention relates generally to prostaglandin agonist prodrug compositions, and more particularly, to stable aqueous compositions of prostaglandin agonist prodrugs and methods of use thereof. Background technique [0004] Ocular hypotensive agents are used in the treatment of a large variety of ocular hypertensive conditions, such as post-lasertrabeculectomy hypertensive episodes, glaucoma, and as a preoperative adjunct. [0005] Glaucoma is an eye disease characterized by elevated intraocular pressure. Based on its etiology, glaucoma can be classified as primary or secondary glaucoma. For example, primary glaucoma (congenital glaucoma) in adults can be open angle or acute, or chronic angle closure glaucoma. Second...
Claims
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IPC IPC(8): A61K9/08A61K31/4025A61K31/4436A61K47/12A61P27/06
CPCA61K9/0048A61K31/4025A61K31/4436A61K47/12A61P27/00A61P27/02A61P27/06A61P27/10A61K31/559A61K47/02A61K47/10A61K47/26
Inventor R·M·伯克W·B·艾姆
Owner ALLERGAN INC