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Method for preparing rotigotine nose micelle temperature-sensitive gel

A rotigotine nasal and temperature-sensitive gel technology, which is applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc., to achieve high drug bioavailability, improved solubility, and easy availability of raw materials Effect

Active Publication Date: 2020-03-27
ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Based on this, the present invention has developed rotigotine nasal micellar thermosensitive gel, and there is no relevant report on rotigotine micellar thermosensitive gel at present

Method used

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  • Method for preparing rotigotine nose micelle temperature-sensitive gel
  • Method for preparing rotigotine nose micelle temperature-sensitive gel
  • Method for preparing rotigotine nose micelle temperature-sensitive gel

Examples

Experimental program
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Effect test

Embodiment 1

[0026] A preparation method of rotigotine micellar thermosensitive gel, comprising the following steps:

[0027] (1) Weigh 6 mg of rotigotine and 30 mg of mPEG-PLA, add 1 mL of acetone to dissolve, add the solution dropwise to 5 mL of rapidly stirred pure water, and continue stirring for 4 hours until the residual solvent is evaporated, and the obtained rotigotine Tigotine polymer micelles. The particle size of the polymer micelles was measured to be (95.84±8.75) nm, and the encapsulation efficiency was (89.08±0.09)%.

[0028] (2) Add poloxamer 407 with a weight fraction of 21.84% and poloxamer 188 with a weight fraction of 2.17% to the rotigotine polymer micelles, mix well, store at 4°C for 24h, fully swell and exhaust the air bubbles , to prepare rotigotine nasal micellar thermosensitive gel, then add 0.001g of benzalkonium bromide, add 6 μL of 30% tris to adjust the pH value to 4.760, test tube inversion method to measure the gelation of this embodiment The temperature wa...

Embodiment 2

[0030] A preparation method of rotigotine micellar thermosensitive gel, comprising the following steps:

[0031] (1) Weigh 15 mg of rotigotine and 50 mg of mPEG-PLGA, add 2 mL of dichloromethane to dissolve, add the solution dropwise to 10 mL of rapidly stirred pure water, and continue stirring for 4 h until the residual solvent is evaporated, Derotigotine polymer micelles. The particle size of the polymer micelles was measured to be (88.62±1.47) nm, and the encapsulation efficiency was (93.5±0.79)%.

[0032] (2) Add poloxamer 407 with a weight fraction of 22.69% and poloxamer 188 with a weight fraction of 2.58% to the rotigotine polymer micelles, mix well, store at 4°C for 24 hours, fully swell to exhaust air bubbles To prepare rotigotine nasal micellar thermosensitive gel, add 0.001 g of benzalkonium bromide, and add 6 μL of 30% tris to adjust the pH value to 5.186.

[0033] The rotigotine micellar thermosensitive gel obtained in this example can complete the rapid sol-gel...

Embodiment 3

[0041] A preparation method of rotigotine micellar thermosensitive gel, comprising the following steps:

[0042] (1) Weigh 10 mg of rotigotine and 50 mg of mPEG-PDLLA, add 1 mL of absolute ethanol to dissolve, add the solution dropwise to 5 mL of rapidly stirring pure water, and continue stirring for 4 h until the residual solvent is evaporated, Derotigotine polymer micelles. The particle size of the polymer micelles was measured to be (83.26±1.21) nm, and the encapsulation efficiency was (94.36±0.52)%.

[0043] (2) Add poloxamer 407 with a weight fraction of 23.06% and poloxamer 188 with a weight fraction of 3.27% to the rotigotine polymer micelles, mix well, store at 4°C for 24 hours, fully swell and exhaust the air bubbles , to prepare rotigotine nasal micellar thermosensitive gel, then add 0.001g of benzalkonium bromide, add 6 μL of 30% tris to adjust the pH value to 5.417, test tube inversion method to measure the gelation of this embodiment The temperature was 31.3°C. ...

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Abstract

The invention relates to the technical field of medicine preparations and in particular relates to a method for preparing a rotigotine nose micelle temperature-sensitive gel. The method comprises thefollowing steps: dissolving rotigotine and a polymer carrier material into an organic solvent to form an organic phase, slowly dropwise adding the organic phase into pure water, and performing stirring so as to obtain rotigotine polymer micelle; and adding a temperature-sensitive gel matrix into the rotigotine polymer micelle, performing uniform mixing, and completely removing bubbles, so as to obtain the rotigotine nose micelle temperature-sensitive gel. By adopting the method, defects that rotigotine is low in bioavailability and high in fat dissolubility in oral taking can be overcome, advantages of the two components, namely the polymer micelle and the temperature-sensitive gel, are combined, and a rotigotine nose micelle temperature-sensitive gel composite system is developed. By adopting the polymer micelle, the dissolution performance of the rotigotine in water is effectively improved, the prepared rotigotine nose micelle temperature-sensitive gel is at a solution state at a lowtemperature and can be rapidly converted into a gel at a nose cavity temperature, a preparation can be well adhered to the nose cavity, the bioavailability of medicines is high, and the brain targeting performance is good.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a preparation method of rotigotine nasal micellar thermosensitive gel. Background technique [0002] Rotigotine is a new type of non-ergot selective dopamine receptor agonist, which plays an anti-parkinsonian effect by stimulating dopamine receptors in the body and mimicking the neurotransmitter dopamine. However, the first-pass effect of rotigotine is very obvious, and the bioavailability is extremely low (<1%-5%), so it is not suitable for oral administration. Currently, only rotigotine transdermal patch has been marketed The patch has a good therapeutic effect and reduces the occurrence of motor complications. However, clinical application shows that most of them will produce local side effects such as erythema and itching, which reduces the compliance of patients. In 2008, crystallization occurred in the patch, which reduced the amount of drug avail...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/107A61K31/381A61K47/10A61K47/34A61P25/16
CPCA61K9/06A61K9/1075A61K9/0043A61K31/381A61K47/10A61K47/34A61P25/16
Inventor 桂双英杨转转王方园舒子璇刘梦丽
Owner ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE