Pharmaceutical composition comprising timolol

A composition, a technology of a drug, applied in the field of topical application in the eye, raising intraocular pressure, treating glaucoma, high intraocular pressure and/or symptoms related thereto, capable of solving not representing the best choice, poor solubility, infeasible And other issues

Pending Publication Date: 2020-10-30
NOVALIQ GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, if the drug substance is very poorly soluble in aqueous or other biocompatible solvent systems, or if it is hydrolytically unstable, then a simple solution may not be feasible or represent the best choice

Method used

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  • Pharmaceutical composition comprising timolol
  • Pharmaceutical composition comprising timolol
  • Pharmaceutical composition comprising timolol

Examples

Experimental program
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Effect test

example 1

[0187] The following examples serve to illustrate the invention; however, these should not be construed as limiting the scope of the invention. Example 1: Preparation of Timolol Suspension

[0188] 109,34 mg of timolol maleate CAS number 26921-17-5 (LKT Labs; 99.5% purity) was introduced into a 25 mL vessel fitted with a 2 mm diameter stainless steel ball. Then, 8 mL of 1-perfluorohexyl-octane (F6H8) was added, the vessel was closed and ground for 3 hours at 150 rpm with a planetary ball mill (PM 100, Retsch GmbH, Germany) at 10 minute intervals (variation method). After trituration, the suspension thus formed was transferred to a glass vial, shaken on a Vortex shaker for a minimum of 30 seconds, and sealed. Considering that 1.3668 mg timolol maleate corresponds to 1.0 mg timolol free base, a 1.0% (w / v) suspension of timolol in F6H8 (10 mg / mL) was obtained.

[0189] Following the same procedure as above, a 15 mg / ml timolol suspension was prepared.

[0190] Dilute the suspen...

example 2

[0201] Example 2: Measurement of Intraocular Pressure (IOP) in Animal Studies

[0202] To evaluate the pharmacodynamics of the ability of a composition comprising timolol and a semifluorinated alkane to reduce IOP (intraocular pressure) compared to a commercially available solution of timolol administered in aqueous solution, a blood Animal studies of normal dogs. The study setup and design are as follows.

[0203] Dogs were selected for participation in the study based on general health, body weight, ophthalmic examination results, response to IOP challenge, and the following criteria:

[0204] - healthy, normal ocular surface;

[0205] - No invasive eye surgery for at least one month prior to the study; especially surgery generally involving the cornea or anterior segment;

[0206] - No topical or systemic corticosteroid therapy for at least one month;

[0207] - Clearance of drug from previous topical ocular studies comparable to the typical washout period (at least one...

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Abstract

The present invention relates to pharmaceutical composition comprising the [beta]1([beta]1)-receptor blocker timolol and a liquid vehicle comprising a semifluorinated alkane. The pharmaceutical composition of the present invention may be useful for topical administration, for example ophthalmic topical administration and for use in the treatment of glaucoma, increased intraocular pressure, ocularhypertension and / or a symptom associated therewith.

Description

Background technique [0001] The present invention relates to a pharmaceutical composition comprising a) timolol and / or a pharmaceutically acceptable salt thereof and b) a liquid vehicle comprising a semifluorinated alkane. The pharmaceutical compositions of the present invention are useful for topical administration, especially ophthalmic topical administration. [0002] Pharmaceutical compositions in liquid form represent one of the preferred types of pharmaceutical preparations. Certain routes of topical administration, such as ophthalmic administration, often require liquid forms to provide effective delivery of the active ingredient and a patient-friendly mode of use. [0003] The simplest type of liquid formulation is a solution, such as an aqueous solution of an active pharmaceutical ingredient. However, in some cases, the development of more complex formulations, such as suspensions, may be considered. For example, if the drug substance is very poorly soluble in aque...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/10A61K31/5377A61P27/06
CPCA61K9/0048A61K9/10A61K31/5377A61P27/06A61K47/06A61P27/02A61K9/08
Inventor F·洛舍尔S·克鲁瑟D·斯特雷尔B·豪普特梅尔K·艾克霍夫
Owner NOVALIQ GMBH
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