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Enhanced bimatoprost ophthalmic solution

A bimatoprost and ophthalmic technology, applied in the field of pharmaceutical compositions of bimatoprost

Active Publication Date: 2011-06-15
ALLERGAN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although no other bimatoprost is currently marketed for the treatment of glaucoma, there are several commercially available prostaglandin analogs that contain BAK as a preservative

Method used

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  • Enhanced bimatoprost ophthalmic solution
  • Enhanced bimatoprost ophthalmic solution
  • Enhanced bimatoprost ophthalmic solution

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Preparations are prepared by conventional methods well known in the art, these preparations contain 0.268% disodium hydrogen phosphate heptahydrate, 0.014% citric acid, 0.83% sodium chloride, adjust the pH to 7.3 in qs (quality safety) water, and The amounts of prostaglandin, BAK and EDTA are listed in Table 1 below.

[0043] Table 1

[0044] preparation

[0045] 5.0.03% bimatoprost-0.4% TPGS (no preservatives)

Embodiment 2

[0047]An in vivo study was performed to determine the effect of benzalkonium chloride (BAK) and d-alpha tocopherol 1000 succinate (TPGS) on the ocular absorption of bimatoprost. In this in vivo experiment, one drop of 28 μL eye drops was added to each eye of eighteen female rabbits, and aqueous humor samples were collected 60 minutes after administration (n = 3 animals, 6 eyes per formulation). Two rabbits (4 eyes) were untreated as untreated bioassay controls. Bimatoprost and its parent carboxylic acid extracted from aqueous humor and in vitro samples were analyzed by liquid chromatography tandem mass spectrometry (LC-MS / MS), with a quantitative range of 0.25-60 ng / mL.

[0048] Due to the extensive metabolism of bimatoprost in rabbit eyes, its parent acid was used as a surrogate to determine the ocular absorption of bimatoprost. Figure 1 and Table 2 below summarize the acid concentrations in the aqueous humor of rabbits following a single dose of 6 different bimatoprost form...

Embodiment 3

[0056] Preparations are prepared by conventional methods well known in the art, these preparations contain 0.268% disodium hydrogen phosphate heptahydrate, 0.014% citric acid, 0.83% sodium chloride, adjust the pH to 7.3 in qs (quality safety) water, and The amounts of prostaglandin, BAK and EDTA are listed in Table 3 below.

[0057] table 3

[0058] preparation

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PUM

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Abstract

A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein.

Description

technical field [0001] The present invention relates to pharmaceutical compositions comprising bimatoprost. Background technique [0002] Related Technical Notes [0003] Bimatoprost, shown below, is a commercially available prostamide used in the treatment of glaucoma and ocular hypertension. [0004] [0005] chemical formula I [0006] Benzalkonium chloride (BAK) is a preservative used in many commercial ophthalmic products to prevent microbial contamination in multiple-use products. Commercially available eye drops (Bimatoprost, Allergan, Irc., Irvine, CA) contained 0.03% bimatoprost and 0.005% BAK. Although no other bimatoprost is currently marketed for the treatment of glaucoma, there are several commercial prostaglandin analogs that contain BAK as a preservative. These prostaglandin analogs include latanoprost (Xalatan), travoprost (Travatan), and isopropyl unoprostone (Rescula), which require considerable amounts of BAK, 150 to 200 ppm, to reach the U.S. And ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5575A61K9/00A61K47/18A61P27/06
CPCA61K31/165A61K9/0048A61K31/14A61K31/557A61K31/5575A61P27/02A61P27/06A61P27/14A61K9/08A61K47/18A01N33/12A61K47/02A61K47/12
Inventor 张金明J·N·张R·M·希夫曼R·S·乔丹J-E·张-林
Owner ALLERGAN INC
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