Transdermal patch containing rotigotine, and preparation method thereof

The technology of a transdermal patch and a softener is applied to the transdermal patch containing rotigotine and the field of preparation thereof, and can solve the problem of low skin penetration rate, low penetration rate, inability to achieve therapeutic effect and stability and other problems, to achieve the effects of easy availability of materials, improved initial viscosity, and improved transdermal release performance.

Active Publication Date: 2018-08-28
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a kind of composition that is used for preparing the transdermal patch containing rotigotine, in order to solve the low skin penetration rate of rotigotine in the low penetration rate of acrylic pressure-sensitive adhesive at present , can not achieve the therapeutic effect and the technical problems of poor stability

Method used

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  • Transdermal patch containing rotigotine, and preparation method thereof
  • Transdermal patch containing rotigotine, and preparation method thereof
  • Transdermal patch containing rotigotine, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 is used to prepare the preparation of the transdermal patch composition containing rotigotine

[0043] Take a suitable glass container, add the prescribed amount of rotigotine and DL-α-tocopherol in Table 1 to an appropriate amount of absolute ethanol solution, and stir until the mixture is completely dissolved. Take the polyisobutylene B100, B10, and low-molecular-weight polybutene in the prescription amount in Table 1 and stir and mix evenly to form a polyisobutylene pressure-sensitive adhesive. Add colloidal silicon dioxide and light liquid paraffin to the above-mentioned pressure-sensitive adhesive, and stir and mix until uniform ; Then add the drug solution, stir while adding, until a uniform dispersion system is obtained, and prepare by vacuum degassing to obtain compositions 1-1 and 1-2.

[0044] Using a laboratory small-scale coating machine (England, Elcometer), the obtained compositions 1-1 and 1-2 are coated on the release film, and the specific coa...

Embodiment 2

[0053] The comparative test of embodiment 2 different softening agents

[0054] Screen the types of softeners in order to improve their permeability behavior by changing the softeners, and investigate three different softeners: light liquid paraffin, liquid paraffin, and glycerin. The components and amounts used are shown in Table 3. Preparation method The method described in Example 1 was used.

[0055] Table 3. Components and dosages used

[0056]

[0057]

[0058] Wherein, the above-mentioned polyisobutylene pressure-sensitive adhesive adopts polyisobutylene (Polyisobutylene (oppanol B100, viscosity average molecular weight 1,000,000)) that is 30.7 parts by weight, polyisobutylene (Polyisobutylene (oppanol B10, viscosity average molecular weight 30,000)) that is 30.7 parts by weight, Mix evenly with low molecular weight polybutene (HV-300, viscosity average molecular weight 1,260) of 5 parts by weight to form a polyisobutylene pressure-sensitive adhesive. The polyiso...

Embodiment 3

[0072] Example 3 is used to prepare the preparation of the transdermal patch composition containing rotigotine

[0073] Composition 1:

[0074] Take a suitable glass container, add the prescribed amount of rotigotine, ascorbyl palmitate and all-racem-a-tocopherol in Table 7 to an appropriate amount of absolute ethanol solution, and stir until the mixture is completely dissolved.

[0075] Take the polyisobutylene pressure-sensitive adhesive of the prescription amount in Table 1, add liquid paraffin, stir and mix until uniform; then add the drug solution into it, stir while adding, until a uniform dispersion system is obtained, and vacuum degassing. Use laboratory small-scale coating machine (England, Elcometer) to coat the colloid system obtained on the release film. The specific coating thickness should ensure that the drug content per unit area in the patch after drying is constant, that is, every 10cm 2 The patch contains rotigotine 4.5mg. Form a uniform thin layer, dry a...

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Abstract

The invention discloses a transdermal patch composition containing rotigotine, and more specifically discloses a transdermal patch containing rotigotine, and a preparation method thereof. The transdermal patch composition contains effective doses of rotigotine and a self-adhesive matrix; the self-adhesive matrix comprises a polyisobutylene pressure-sensitive adhesive and a colloid softener. According to the preparation method, the polyisobutylene pressure-sensitive adhesive is adopted, the C-H skeleton of the polyisobutylene pressure-sensitive adhesive is long and straight, only the terminal groups contain unsaturated bonds, double bond content is low, and reaction sites are few, so that the transdermal patch containing rotigotine is extremely stable, is excellent in weatherability, heat resistance, and aging resistance, is low in cost; the materials are easily available; the operationality is high; the colloid softener is added, so that the stability of the transdermal patch containing rotigotine is improved, and precipitation of drug active components out from the transdermal patch containing rotigotine is prevented; and in addition, an adhesiveness conditioning agent is added, so that the permeability of the transdermal patch containing rotigotine is excellent.

Description

technical field [0001] The invention belongs to the technical field of preparing medicines for treating symptoms of Parkinson's disease, in particular to a transdermal patch containing rotigotine and a preparation method thereof. Background technique [0002] Parkinson's disease is a disease that strikes mainly in middle-aged and older people, and it affects both men and women equally. The highest incidence of Parkinson's disease occurs in people over the age group of 70 years, 1.5-2.5% of these people have Parkinson's disease. The average age at onset is 58-62 years old, and most patients who develop Parkinson's disease are between 50-79 years old. In the United States alone, approximately 800,000 people are living with Parkinson's disease. The lack of movement early in Parkinson's disease can be traced to the degeneration of cells that release dopamine in the substantia nigra. This neuronal degeneration produces defects in the dopamine pathway that connects the substant...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/381A61K47/32A61P25/16
CPCA61K9/7053A61K31/381A61K47/32
Inventor 蒲晓蕾卢迪张运杨旸田莉莉
Owner BEIJING TIDE PHARMA
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