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Pharmaceutical compositions comprising timolol

Pending Publication Date: 2021-04-29
NOVALIQ GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention is about a new way to make eye drop medications that use a special type of liquid called semifluorinated alkane. These liquids have the advantage of evaporating quickly after being applied to the eye, which helps to get the medicine out of the eye and into the rest of the body. This is different from other types of eye drop medications that can leave behind a layer of oil that can cause problems. The invention is useful for treating and preventing diseases that affect the eye, and can be applied directly to the eye.

Problems solved by technology

In certain cases, however, the development of a more complex formulation such as a suspension may be considered.
For example, if a drug substance is very poorly soluble in aqueous or other biocompatible solvent systems, or if it is hydrolytically labile, a simple solution may not be feasible or represent the best choice.

Method used

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  • Pharmaceutical compositions comprising timolol
  • Pharmaceutical compositions comprising timolol
  • Pharmaceutical compositions comprising timolol

Examples

Experimental program
Comparison scheme
Effect test

example 1

on of Timolol Suspensions

[0180]109.34 mg of timolol maleate, CAS number 26921-17-5 (LKT Labs; purity 99.5%) were introduced to a 25 mL vessel, filled with stainless steel balls, diameter 2 mm. Afterwards, 8 mL of 1-perfluorohexyl-octane (F6H8) were added, the vessel was closed and the milling was performed with a planetary ball mill (PM 100, Retsch GmbH Germany) for 3 hours at 150 rpm with an interval of 10 minutes (with change of direction). After the milling, the thereby formed suspension was transferred into a glass vial, shaken on a Vortex shaker for a minimum of 30 seconds, and sealed. Considering that 1.3668 mg timolol maleate correspond to 1.0 mg timolol free base, a 1.0% (w / v) Timolol suspension (10 mg / mL) in F6H8 was obtained.

[0181]Following the same procedure as described above, a 15 mg / ml timolol suspension was prepared.

[0182]A suspension with the concentration 5 mg / mL was diluted out of the 10 mg / mL stock suspension by diluting the suspension with F6H8.

[0183]The 10 mg / mL...

example 2

nt of Intraocular Pressure (IOP) in an Animal Study

[0188]An animal study utilizing 8 normotensive dogs was carried out in order to assess the pharmacodynamics of a composition comprising Timolol and a semifluorinated alkane with regard to its capability to lower the IOP (intraocular pressure) in comparison with a commercial solution of Timolol which is administered in form of an aqueous solution. The study setup and design was as follows.

[0189]The dogs were selected for participation in the study based on overall health, body weight, results of ophthalmic examinations, response to IOP challenge, and the following criteria:[0190]healthy, normal ocular surface;[0191]no invasive ocular procedures for at least one month prior to the study; particularly procedures involving the cornea or ocular anterior segment in general;[0192]no topical or systemic corticosteroid treatment for at least one month;[0193]washout from prior topical ocular study medication commensurate with the typical wash...

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Abstract

The present invention relates to pharmaceutical composition comprising the beta 1(β1)-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, ocular hypertension and / or a symptom associated therewith.

Description

BACKGROUND[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 composition of the present invention may be useful for topical administration, especially ophthalmic topical administration.[0002]Pharmaceutical compositions in liquid form represent one of the preferred types of drug formulations. Certain routes of topical administration, such as ophthalmic administration, typically require the liquid form in order to provide for an efficient 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 the active pharmaceutical ingredient. In certain cases, however, the development of a more complex formulation such as a suspension may be considered. For example, if a drug substance is very poorly soluble in aqueous or other...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61P27/06A61K9/00A61K9/08
CPCA61K31/5377A61K9/08A61K9/0048A61P27/06A61K9/10A61K47/06A61P27/02
Inventor LÖSCHER, FRANKKRÖSSER, SONJASTREHL, DIANAHAUPTMEIER, BERNHARDEICKHOFF, KIRSTEN
Owner NOVALIQ GMBH
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