Transdermal pharmaceutical preparations

A technology for pharmaceutical preparations and pharmaceutical activity, applied in the field of transdermal pharmaceutical preparations, can solve problems such as microbial contamination, reduction of preparation stability and storage period, etc.

Inactive Publication Date: 2012-07-11
EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAG (EGIS PHARMA PLC)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although absorption from such formulations is adequate in most cases, these formulations are prone to physico-chemical changes during storage, including breakdown of the active ingredient, degradation of the colloidal structure of the formulation, and often microbial contamination
This process reduces formulation stability and shelf life

Method used

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  • Transdermal pharmaceutical preparations
  • Transdermal pharmaceutical preparations
  • Transdermal pharmaceutical preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Transdermal gel for systemic effects

[0075]

[0076] The amount of active ingredient is selected according to the desired formulation strength or according to the volume of reconstitution and the unit dose.

Embodiment 2

[0078] Transdermal semisolid formulations for topical application

[0079]

[0080] The amount of active ingredient is selected according to the desired formulation strength or according to the volume of reconstitution and the unit dose.

Embodiment 3

[0082] Preparation

[0083] Compositions according to example 1 or 2 and compositions of similar qualitative composition were prepared as follows.

[0084] 3.1. Preparation of active ingredient suspension

[0085] The optionally micronized active ingredient is mixed with silicone oil. The mixture is then homogenized with a suitable laboratory mixer, such as a laboratory-scale mixer, using an Ultra-Turrax mixing device (4000 min -1 , 5min).

[0086] 3.2. Preparation of gel matrix

[0087]Add hydroxypropyl cellulose to water in small portions at a temperature of 25°C and stir until completely dissolved. Carbopol 980NF was then added to the solution and stirred until dissolved. The solution was then neutralized with a 10% by weight potassium hydroxide solution. Stir continuously until a smooth gel state is obtained.

[0088] 3.3. Preparation of drug-containing gel

[0089] Add the active ingredient suspension in small portions to the gel base prepared according to 3.2 and...

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Abstract

The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.

Description

technical field [0001] The present invention relates to semi-solid transdermal pharmaceutical formulations containing coated particles of active ingredients dispersed in a gel base or cream base and a process for their preparation. More particularly, the present invention relates to formulations for transdermal application in which the active ingredient is coated with volatile silicones (siloxanes) and the suspension thus obtained is dispersed in a gel or cream vehicle in the substance matrix. The physical, chemical and microbiological stability of the transdermal preparation according to the present invention is excellent, and its preparation can be carried out by simple operation and selection of an appropriate volatile silicone component for coating the active ingredient, and has been able to produce Transdermal formulations for topical, local or systemic application. Background technique [0002] Silicone (also known as siloxane, silane or poly Silicone) has a particu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/24A61K9/50A61K47/34
CPCA61K9/5031A61K47/24A61K47/38A61K47/32A61K9/0014A61P1/16A61P11/00A61P15/00A61P17/00A61P19/00A61P25/00A61P25/16A61P25/18A61P25/26A61P29/00A61P3/00A61P31/04A61P31/10A61P31/12A61P37/02A61P9/00A61K47/34
Inventor E·米库拉希克P·法泽卡斯
Owner EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAG (EGIS PHARMA PLC)
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