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Implants of rotigotine and its derivatives or pharmaceutically acceptable salts thereof

A technology of implants and medicinal salts, applied in the field of its derivatives, drug implants, and rotigotine, can solve the problems of increased use and difficulty for patients, and achieve reduced release stagnation, stable release, and reduced individual differences Effect

Active Publication Date: 2019-08-23
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, crystallization of rotigotine occurred during the use of this product. In order to solve this problem, cold chain storage and distribution (temperature 2-8°C) was adopted, and each prescription should not exceed 1 month to avoid crystallization. However, this obviously increases the difficulty for patients to use

Method used

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  • Implants of rotigotine and its derivatives or pharmaceutically acceptable salts thereof
  • Implants of rotigotine and its derivatives or pharmaceutically acceptable salts thereof
  • Implants of rotigotine and its derivatives or pharmaceutically acceptable salts thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1 PLGA (75 / 25, 0.20, 13000) to prepare implants (theoretical drug loading 30%)

[0050] Weigh 1.800 g of rotigotine and 4.199 g of PLGA (75 / 25, 0.20, 13000), place them in a grinding tank, freeze them at a low temperature, and use a grinder at 25 Hz·s -1 The frequency of crushing. Put it into the mini-CTW micro-conical twin-screw mixer that has been heated to 80°C in advance, stir and circulate for 10 minutes, and the obtained mixture is placed in the mold rod mold (1 mm size) at the screw speed of 0-100rpm. Extruded on the conveyor belt, the traction speed of the conveyor belt is consistent with the extrusion speed of the sample. When the sample is conveyed to the end of the conveyor belt, the sample is collected, and the length of the sample is cut to obtain the implant.

Embodiment 2

[0051] Example 2 PLGA (75 / 25, 0.40, 50000) to prepare implants (theoretical drug loading 30%)

[0052] Weigh 1.801 g of rotigotine and 4.201 g of PLGA (75 / 25, 0.40, 50000) and prepare according to the method of Example 1 to obtain the rotigotine implant.

Embodiment 3

[0053] Example 3 PLGA (75 / 25, 0.50, 70000) to prepare implants (theoretical drug loading 30%)

[0054] Weigh 1.801 g of rotigotine and 4.202 g of PLGA (75 / 25, 0.50, 70000), and prepare according to the method of Example 1 to obtain the rotigotine implant.

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Abstract

The invention provides an implant of rotigotine, derivatives thereof or rotigotine and derivative pharmaceutical salts thereof. The implant comprises rotigotine, derivatives thereof or rotigotine, derivative pharmaceutical salts thereof and at least two poly lactide-co-glycolides (PLGA), a polymerization ratio of lactide to glycolide is 95:5-5:95, and at least one water-soluble pharmaceutical excipient can be added. The implant prepared is suitable for long-time administration for patients, more stable in release during drug release and free of stagnation at the early stage of drug release.

Description

technical field [0001] The present invention relates to a drug implant of rotigotine, its derivatives, or the medicinal salt composition of rotigotine, its derivatives. Background technique [0002] Parkinson's disease (PD), also known as Parkinson's paralysis, is one of the most common neurodegenerative diseases. life safety. Levodopa used to be the gold standard for the treatment of PD, but long-term use can easily lead to motor complications. Studies have shown that this may be related to the long-term non-physiological pulse-like stimulation of striatal dopamine receptors[1], thus proposing the PD A new concept of treatment - continuous dopaminergic stimulation (continuous dopaminergic stimulation, CDS). CDS is mainly achieved by continuous administration of levodopa or dopamine receptor agonists. [0003] Rotigotine is a new type of non-ergot selective D3 / D2 / D1 dopamine receptor agonist for the adjuvant treatment of early secondary Parkinson's disease and advanced Pa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/381A61K47/34A61K47/26A61K47/38A61P25/16
Inventor 王爱萍刘艳香刘万卉王涛张晓喜王文艳孙考祥
Owner SHANDONG LUYE PHARMA CO LTD