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Percutaneous sustained-release patch for resisting schizophrenia

A technology of schizophrenia and slow-release patches, which is applied to nervous system diseases, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., can solve problems such as poor compliance, achieve blood drug concentration stability, Good penetration promoting effect and good dissolution effect

Active Publication Date: 2019-12-20
ZHEJIANG ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to overcome the shortcomings of the existing aripiprazole preparations, especially the poor compliance of patients with long-term use of aripiprazole, the present invention provides a transdermal slow-release patch of aripiprazole

Method used

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  • Percutaneous sustained-release patch for resisting schizophrenia
  • Percutaneous sustained-release patch for resisting schizophrenia
  • Percutaneous sustained-release patch for resisting schizophrenia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Prescription (100g feeding):

[0041]

[0042] Add the prescribed amount of aripiprazole to ethyl oleate, Span-20 and menthol to dissolve, add 1,2-propylene glycol under high-speed homogeneous stirring, then add polyacrylate and polyisobutylene respectively, and stir evenly. Finally, hydroxypropyl-β-cyclodextrin and anhydrous sodium sulfite were added and stirred evenly, and the bubbles were removed by ultrasonic waves and left to stand until the bubbles completely disappeared to obtain a pressure-sensitive adhesive reservoir layer. Coat the pressure-sensitive adhesive reservoir layer on the release layer, dry at 80°C for 45 minutes, and cut the backing layer covering the surface of the pressure-sensitive adhesive reservoir layer into 50cm 2 Patch, prepared aripiprazole transdermal slow-release patch.

[0043] The aripiprazole sustained-release transdermal patch has passed the human isolated skin penetration test in a Valia-Chien osmotic cell, and the receiving solu...

Embodiment 2

[0045] Prescription (total 100g):

[0046]

[0047] Add the prescribed amount of aripiprazole to linoleic acid monoglyceride, Span 20 and laurocaprazine to dissolve, add 1,2-propanediol under high-speed homogeneous stirring, and then add polyacrylate and polyisobutylene respectively, Stir evenly, and finally add chitosan and dibutylphenol, stir evenly, remove bubbles by ultrasonic waves and let the bubbles disappear completely, so as to obtain a pressure-sensitive adhesive storage layer. Coat the pressure-sensitive adhesive reservoir layer on the release layer, dry at 80°C for 45 minutes, and cut the backing layer covering the surface of the pressure-sensitive adhesive reservoir layer into 50cm 2 Patch, prepared aripiprazole transdermal slow-release patch.

[0048] The aripiprazole sustained-release transdermal patch has passed the human isolated skin penetration test in a Valia-Chien osmotic cell, and the receiving solution is 40% polyethylene glycol normal saline. Such ...

Embodiment 3

[0050] Prescription (total 100g):

[0051]

[0052] Add the prescribed amount of aripiprazole into monoglyceride, lauric caprylic acid monoglyceride, diethylene glycol monoethyl ether to dissolve, add 1,2-propanediol under high-speed homogeneous stirring, and then add polyacrylate, poly Isoprene, stirred evenly, finally added hydroxypropyl-β-cyclodextrin, anhydrous sodium sulfite, stirred evenly, ultrasonically removed the bubbles and left to stand still, the bubbles completely disappeared, and the pressure-sensitive adhesive reservoir layer was obtained. Coat the pressure-sensitive adhesive reservoir layer on the release layer, dry at 80°C for 45 minutes, and cut the backing layer covering the surface of the pressure-sensitive adhesive reservoir layer into 50cm 2 Patch, prepared aripiprazole transdermal slow-release patch.

[0053] The aripiprazole sustained-release transdermal patch has passed the human isolated skin penetration test in a Valia-Chien osmotic cell, and th...

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Abstract

The invention discloses a percutaneous sustained-release patch for resisting schizophrenia, and belongs to the field of pharmaceutical preparations. The percutaneous sustained-release patch is composed of a backing layer, a pressure-sensitive adhesive storage layer and an anti-sticking layer. The pressure-sensitive adhesive storage layer comprises 1 to 12 percent of aripiprazole, 10 to 35 percentof a penetration enhancer, 60 to 80 percent of a viscous polymer and 0.5 to 2 percent of a drug stabilizer. According to the percutaneous sustained-release patch, medicines can permeate the skin to reach higher blood concentration within 24 hours, the blood medicine concentration can be kept stable within 5-6 days, and the patch is expected to be clinically used for achieving the effects of long acting, convenience in use and good medication compliance of a patient. The pressure-sensitive adhesive storage layer of the percutaneous sustained-release patch comprises the medicines, the penetration enhancer, the viscous polymer and the drug stabilizer. The viscous polymer is a mixture of at least two lipophilic viscous polymers and at least one hydrophilic viscous polymer; and the penetrationenhancer is a mixed penetration enhancer containing penetration enhancers with an emulsifying effect.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an anti-schizophrenia transdermal sustained-release patch and a preparation method thereof. Background technique [0002] Schizophrenia affects 1% of the world's population, and occurs mostly in young adults. Schizophrenia affects a person's ability to think, control emotions, and make decisions. Those who are positive for schizophrenia experience symptoms such as hallucinations and delusions, while those who are negative for schizophrenia are socially withdrawn and lack emotional change. Its onset is mainly centered on self-disorder, which leads to a decrease in the sense of existence of the patient's conscious subject, leading to confusion in consciousness control, deviations in the understanding of things, and finally causing patients to have serious consequences due to hallucinations. Clinically, aripiprazole has obvious curative effects on positive and negative s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/40A61K47/36A61K47/32A61K47/44A61K31/496A61P25/28A61P25/24A61P25/22
CPCA61K9/7023A61K47/40A61K47/36A61K47/32A61K47/44A61K31/496A61P25/28A61P25/24A61P25/22Y02A50/30
Inventor 叶金翠张琪江昌照高文彦郑高利曹晓春
Owner ZHEJIANG ACAD OF MEDICAL SCI
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