Topical mecamylamine formulations for ocular administration and uses thereof

A mecamylamine, topical application technology, applied in the direction of medical preparations of non-active ingredients, drug delivery, amine active ingredients, etc., can solve the problems of not being commercially available, difficult to model nicotine, and not surprising

Inactive Publication Date: 2009-02-25
COMENTIS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Even in vivo models of nicotine are difficult to perform precisely and may lead to opposite results (Maurice (2002) Survey of Ophthalmology 47(Supp.1):S41-S52)
It is therefore not at all surprising that methods of topical treatment of conditions associated with proliferative retinopathy affecting the tissues at the back of the eye have not been commercially available to date.

Method used

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  • Topical mecamylamine formulations for ocular administration and uses thereof
  • Topical mecamylamine formulations for ocular administration and uses thereof
  • Topical mecamylamine formulations for ocular administration and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0276] Embodiment 1: mecamylamine parenteral preparation

[0277]

[0278] A parenteral formulation of mecamylamine hydrochloride was prepared by substantially dissolving 1 g of mecamylamine hydrochloride USP (white powder) and 33.33 mL of 0.9% sterile NaCl in a volumetric flask. The mixture was manually stirred at room temperature until the mecamylamine powder was completely dissolved to give a clear solution. The pH of the solution was adjusted to 7.4 using NaOH and HCl.

Embodiment 2

[0279] Example 2: Ocular Bioavailability After Intravenous Administration

[0280] This study was designed to model the ocular bioavailability of mecamylamine when administered systemically. The rabbit eye is the preferred model for in vivo modeling of ophthalmic drugs, however, rabbits are not the subject of choice for modeling oral bioavailability. However, systemic administration does mimic orally administered mecamylamine to a reasonable approximation due to mecamylamine's rapid absorption and high oral bioavailability. Therefore, intravenous injection was used to model the ocular bioavailability of systemically administered mecamylamine in order to determine the disposition of mecamylamine from blood to plasma, vitreous, and posterior ocular tissues (retina / choroid).

[0281] The study included 2 groups (N = 6 each, 12 rabbits in total) of male NZW (New Zealand White) rabbits weighing approximately 2.5-3 kg and obtained from Kralek Farms (Turlock, CA). A solution of mec...

Embodiment 3

[0285] Example 3: Preparation of Topical Ophthalmic Solution Formulations

[0286]

[0287] Dissolve mecamylamine hydrochloride USP in 100 mL of DI water. Then 0.9 g weight of sodium chloride was added while stirring to make an isotonic solution (0.9% NaCl w / v). The solution was then filtered through a 0.2 micron membrane filter and packaged under sterile conditions.

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PUM

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Abstract

Provided are methods, pharmaceutical formulations and kits thereof for the treatment and/or prevention of conditions mediated by neovascularization, abnormal angiogenesis, vascular permeability, or combinations thereof, of posterior and/or anterior tissues and fluids of the eye, including conditions associated with proliferative retinopathies, for example, diabetic retinopathy, age-related maculopathy, retinopathy of prematurity, retinopathy associated with macular edema, or retinopathy associated with sickle cell disease, using the topical administration of mecamylamine or a pharmaceutically acceptable salt thereof to the eye. Methods of preparing the pharmaceutical formulations are also provided.

Description

[0001] Cross References to Related Applications [0002] This application claims U.S. Provisional Application No. US60 / 859,582, filed November 17, 2006, U.S. Provisional Application No. US60 / 838,605, filed August 17, 2006, and U.S. Provisional Application No. US60 / 751,808, filed December 19, 2005 rights and interests, the contents disclosed in these documents are fully incorporated herein by reference. Background of the invention [0003] Age-related macular degeneration (AMD) is the leading cause of irreversible vision loss in older adults in North America and Europe (see Arch Ophthalmol. (2004), 1122:564-72; Olejnik et al., (2005) Adv.Drug.Dev.Rev 57:1991-1993; Kulkarni et al., (2005) Adv.Drug.Dev.Rev.57:1994-2009; Gryziewicz (2005) Adv.Drug.Dev.Rev.57:2092-2098). There are two forms of AMD: non-neovascular (also called dry or non-exudative) and neovascular (also called wet or exudative). Although less common, the neovascular form accounts for the vast majority of blindnes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/13A61K47/36
Inventor 张晓明M·肯加塔兰J·P·库克H·塔克鲁里
Owner COMENTIS
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