Compositions of rotigotine, derivatives thereof, or pharmaceutically acceptable salts of rotigotine or its derivative

A composition and medicinal salt technology, which is applied in the direction of drug combination, pharmaceutical formula, medical preparations of non-active ingredients, etc., can solve the problems of patients' pain, sudden release, drug overdose, etc.

Active Publication Date: 2013-12-18
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the disclosed rotigotine microspheres of CN1762495A can achieve long-acting slow-release effect, there is a burst release problem
Therefore, in the treatment of patients with Parkinson's disease in the developing stage with rotigotine microspheres, the drug loading amount of the active ingredient should not be too low, otherwise, in order to achieve the sa

Method used

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  • Compositions of rotigotine, derivatives thereof, or pharmaceutically acceptable salts of rotigotine or its derivative
  • Compositions of rotigotine, derivatives thereof, or pharmaceutically acceptable salts of rotigotine or its derivative
  • Compositions of rotigotine, derivatives thereof, or pharmaceutically acceptable salts of rotigotine or its derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0137] Example 1 Preparation of microspheres with a single PLGA (theoretical drug loading 20%)

[0138] Weigh 0.3104g of rotigotine and PLGA75254A1.2083g, add 7.5ml of dichloromethane and stir to dissolve, add to 750ml of 0.5% PVA aqueous solution with stirring (1200-2000rpm) and emulsify for 2 minutes, Reduce the stirring speed to evaporate the solvent for 5 hours, filter the obtained solution through a 1200-mesh sieve to collect the microspheres, wash the microspheres on the 1200-mesh sieve with purified water for 3 to 5 times, freeze-dry, and sieve through a 100-mesh sieve to obtain the final of microspheres.

Embodiment 2

[0139] Example 2 Preparation of microspheres with a single PLGA (theoretical drug loading 25%)

[0140] Weigh 0.3752 g of rotigotine and 1.1291 g of PLGA75254A, and prepare according to the method of Example 1 to obtain rotigotine microspheres.

Embodiment 3

[0141] Example 3 Preparation of microspheres from a single PLGA (theoretical drug loading 30%)

[0142] Weigh 0.4522 g of rotigotine and 1.0511 g of PLGA75254A, and prepare according to the method in Example 1 to obtain rotigotine microspheres.

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Abstract

The disclosure provides a composition comprising rotigotine or a pharmaceutically acceptable salt thereof; at least one poly(lactide-co-glycolide) (PLGA); and at least one fatty acid, wherein the at least one fatty acid is at least 0.5% in weight relative to the total weight of the composition. The composition as disclosed herein has significantly reduced burse release effect. The disclosure also provides a method of treating Parkinson's disease comprising administering an effective amount of the composition as disclosed to a subject in need thereof.

Description

[0001] This application takes the priority of the Chinese patent application with application number CN201010576447.5 (application date November 25, 2010). technical field [0002] The present invention relates to a composition of rotigotine, its derivatives, or a medicinal salt of rotigotine or its derivatives. Background technique [0003] Rotigotine is not suitable for oral administration due to its low oral bioavailability (about 1%-5%) due to the hepatic first-pass effect. At present, the rotigotine transdermal patch developed by Schwarz Pharma AG has a trade name of It is the first transdermal patch for the treatment of Parkinson's disease, and the transdermal patch has been launched in Germany, the UK, Australia and other countries. However, crystallization of rotigotine may occur during use of this product. In order to solve this problem, cold chain storage and distribution (temperature 2-8°C) is adopted, and each prescription should not exceed 1 month to avoid cr...

Claims

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Application Information

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IPC IPC(8): A61K31/381A61K9/50A61K9/14A61P25/16
CPCA61K9/1617A61K9/1647A61K31/381A61P25/16A61K9/50A61K9/14A61K47/34
Inventor 王爱萍李又欣刘万卉孙考祥李军孙丽芳
Owner SHANDONG LUYE PHARMA CO LTD
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