Ophtalmic ointment composition comprising a drug, an ointment base and a solubilizing/dispersing agent

A kind of technology of ophthalmic composition and ointment base, applied in the field of ointment, can solve problems such as being unsuitable for application

Inactive Publication Date: 2013-05-22
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this ointment is not suitable for application to the eye

Method used

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  • Ophtalmic ointment composition comprising a drug, an ointment base and a solubilizing/dispersing agent
  • Ophtalmic ointment composition comprising a drug, an ointment base and a solubilizing/dispersing agent
  • Ophtalmic ointment composition comprising a drug, an ointment base and a solubilizing/dispersing agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0146] A typical preservative-free ointment of the present invention is as follows:

[0147] Element

Example 1 1)

CGP 41251 2)

1.00

lanolin

5.52

White Vaseline

60.52

liquid paraffin

26.96

PEG400 3)

6.00

total

100

[0148] 1) Amount expressed in weight / weight percent (% w / w)

[0149] 2) The staurosporine derivative of formula (I), wherein R is benzoyl

[0150] 3) H-(OCH 2 -CH 2 ) n OH poly(ethylene glycol) wherein the index n has a value from about 8.5 to about 9 (average relative molecular weight of about 400).

[0151] Prepare as follows:

[0152] The staurosporine derivative is dissolved in poly(ethylene glycol) under heating and sonication, and the solution is thoroughly mixed with a molten ointment base containing lanolin, white petrolatum, and liquid paraffin. The resulting liquid composition is then stirred until room temperature is reached.

Embodiment 2 to 7

[0153] Embodiment 2 to 7 (ointment containing preservative)

[0154]

[0155] * Phenylethyl alcohol can be conveniently replaced, for example, by 0.01% benzalkonium chloride or cetrimonium bromide.

[0156] Preparation method

[0157] 1. Weigh the liquid paraffin in a media bottle. Remove air bubbles from the liquid paraffin by connecting to a vacuum for 30 minutes or until all air bubbles are removed.

[0158] 2. Melt white petrolatum and lanolin on a stirrer at about 70°C.

[0159] 3. Gently mix the liquid paraffin, white petrolatum, and lanolin at about 70°C for 15 minutes or until the ingredients are well mixed to form Part 1 .

[0160] 4. Dissolve PKC 412 in PEG400 or PEG 4000 by sonicating PKC 412 in a 45°C water bath. It takes about 4 hours to completely dissolve PKC 412. This is part 2.

[0161] 5. Add alpha-tocopherol and phenylethyl alcohol or benzalkonium chloride or cetrimonium bromide to PEG with PKC 412 (part 2). This is part 3.

[0162] 6. Add diss...

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Abstract

This invention relates to a semisolid ophthalmic composition, in particular an ointment, comprising (1) an ophthalmic drug, e. g. a staurosporine derivative, (2) an ointment base and (3) an agent for dispersing and / or dissolving said drug in the ointment base, selected from a poly(ethylene-glycol), a polyethoxylated castor oil, an alcohol having 12 to 20 carbon atoms and a mixture of two or more of said components.

Description

[0001] This application is a divisional application of Chinese Patent Application No. 03817208.9 with a filing date of July 22, 2003 and a priority date of July 23, 2002. technical field [0002] The present invention relates to semi-solid ophthalmic compositions containing ophthalmic drugs, in particular to corresponding ointments. Background technique [0003] Semi-solid ophthalmic compositions, and especially ointments, are a pharmaceutical form suitable for topical application, eg, to the skin or eye. However, it is often difficult to incorporate into ointments an amount of drug sufficient to effectively treat a condition or disease. Fortunately, ointment formulations are infrequently applied topically to the eye because of the poor tolerance of ocular tissue to one or more of the ingredients in ointments. For example, EP-A-0474126 describes a drug comprising a drug, namely ascomycin, in an oily ointment base and a lower alkylene carbonate or alkanedicarboxylate for dis...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/34A61K47/44A61K47/10A61K31/436A61K31/553A61P27/02A61P9/00A61P9/10A61P3/10A61P29/00A61P27/14A61K9/00A61K31/196A61K31/355A61K31/404A61K31/502A61K31/7076A61K47/06A61K47/18A61K47/22A61P37/08A61P43/00
CPCA61K9/0048A61K31/502A61K31/436A61K9/06A61K31/33A61K47/44A61K47/06A61K31/553A61K47/10A61K31/404A61K31/355A61K47/22A61K31/196A61K31/195A61P27/02A61P27/14A61P29/00A61P3/10A61P37/08A61P43/00A61P9/00A61P9/10A61K2300/00
Inventor J·奥库努鲁M·巴比奥勒索尼耶J-C·比泽克G·L·基斯C·肖赫M·P-H·翁
Owner NOVARTIS AG
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