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Ophthalmic compositions comprising polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymers

A technology of polyvinyl acetate and polyethylene glycol grafting, which can be used in drug combinations, medical preparations containing active ingredients, and medical preparations with non-active ingredients, etc., and can solve problems such as poor solubility

Inactive Publication Date: 2014-10-22
ALLERGAN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some therapeutically active agents may have poor solubility in aqueous solutions, which may limit topical ophthalmic use
For some therapeutically active agents, nonionic surfactants can be used to increase solubility, but further enhancement may be required

Method used

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  • Ophthalmic compositions comprising polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymers
  • Ophthalmic compositions comprising polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymers
  • Ophthalmic compositions comprising polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymers

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080]Table 1 summarizes the solubility of bimatoprost in vehicles with 5 different solubilizers within a certain stability range. Bimatoprost was more soluble in PCA-PVA-PEG containing vehicles than other solubilizers at room temperature (RT) and higher temperatures.

[0081] Table 1 : Solubility of bimatoprost in 5 different formulation vehicles at different temperatures. PCA-PVA-PEG showed the highest solubilization of bimatoprost at room temperature and higher temperature.

[0082]

[0083] * Measured only at week 1; ** Measured at week 8

Embodiment 2

[0085] Data Supporting Improved Efficacy of BAK

[0086] A preservative titration study was performed to compare the efficacy of BAK in formulations using different solubilizers. In general, it is seen that the preservative efficacy of BAK is significantly reduced in the presence of surfactants. Therefore, higher levels of BAK may be required to meet the standards for preservatives in ophthalmic products as defined in USP and European Pharmacopoeia Chapter 5.1.3. It appears that when using PCA-PVA-PEG as a solubilizer, the preservative criteria are met at lower BAK levels compared to all other surfactants summarized in Table 2. In fact, formulations containing PCA-PVA-PEG met PhEurA criteria with as low as 50 ppm BAK, which was similar to formulations without solubilizers.

[0087] Table 2: Summary of preservative titration to failure results for formulations containing different solubilizers

[0088]

[0089] 1 APET criteria are as defined in USP and European Pharm...

Embodiment 3

[0090] Embodiment 3: the purposes in PCA-PVA-PEG self-corrosion system

[0091] Formulations containing PCA-PVA-PEG exhibited antibacterial activity even without the use of any preservatives. The formulations evaluated are listed in Table 3 along with the APET test results. The formulation containing 1% PCA-PVA-PEG and phosphate-citrate buffer (Formulation 1) was found to meet the USP criteria for all organisms. Phosphate buffer exchange to borate buffer and removal of EDTA brought formulations (Formulations 3-5) to PhEurB standards for all organisms at PCA-PVA-PEG concentrations of 0.5%-1%.

[0092] Table 3: Effect of PCA-PVA-PEG Levels and Borate Buffer in APET Assay

[0093]

[0094]

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PUM

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Abstract

Compositions and methods related to ophthalmic use of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymers and therapeutic uses are described herein.

Description

[0001] Related applications [0002] This application claims the benefit of US Provisional Application Serial No. 61 / 576,453, filed December 16, 2011, which is hereby incorporated by reference in its entirety. Background of the invention [0003] Topically applied formulations, such as those applied to the cornea, conjunctiva, eyelid margin, etc., are commonly used in ophthalmology for the treatment of acute and chronic conditions because they are potentially safer than systemically delivered formulations. However, some therapeutically active agents may have poor solubility in aqueous solutions, which may limit topical ophthalmic use. For some therapeutically active agents, solubility can be enhanced using nonionic surfactants, but further enhancement may be required. Summary of the invention [0004] Some embodiments include topical ophthalmic compositions comprising polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCA-PVA-PEG). [0005] Some em...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/498A61K31/5575A61P27/06A61K47/32
CPCA61K9/0048A61K47/02A61K47/186A61K38/13A61K31/496A61K31/573A61K31/5377A61K31/4985A61K31/568A61K31/407A61K31/4178A61K47/32A61K31/5575A61K9/08A61K31/498A61K31/417A61K47/34A61P27/02A61P27/06A61K2300/00
Inventor A·V·戈雷R·S·格雷厄姆C·P·普亚拉M·古尔梅吉安K·普林R·斯瑞库马
Owner ALLERGAN INC
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