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

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...

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 same therapeutic effect as the high drug loading amount, when administering the drug to the patient, inject The amount of microspheres with low drug loading is too large, which will cause pain to the patient

However, if the drug loading is too large, the drug will be released suddenly when the drug is administered to the patient, which may easily cause drug overdose

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