Dexmethylphenidate skeleton pattern transdermal patch containing vitiligo inhibitor and preparing method and application thereof

A technology of dexmethylphenidate and transdermal patch is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, nervous system diseases, etc., and can solve the problem of low bioavailability of oral dexmethylphenidate, The environment and human health are unfavorable, and the pharmacological activity of L-body is low, so as to achieve good pharmacological activity and curative effect, avoid the phenomenon of sudden release, and inhibit the formation of vitiligo on the skin.

Inactive Publication Date: 2016-03-16
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patents CN102160857A and US20000618626 disclose methylphenidate patches, which are superior in the stability of the drug in the patch and skin permeability, but the pharmacological activity of the L-isomer in methylphenidate is low, which affects the overall curative effect. , can cause permanent white spots on the skin
In addition, the polyisobutylene in the CN102160857A prescription needs to be used in combination with more harmful solvents such as toluene and gasoline, which is harmful to the environment and human health
Chinese patent CN101683342A discloses a freeze-dried powder preparation of dexmethylphenidate and its preparation process. The obtained preparation has good stability and rapid onset of action, but children have poor compliance with injection administration, high safety risks, and cannot achieve long-lasting Efficacy
Patent CN101933913A discloses a double-release preparation of dexmethylphenidate hydrochloride and its preparation method. Compared with common preparations, it reduces the number of daily doses, but the bioavailability of oral dexmethylphenidate is low and the side effects are more obvious

Method used

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  • Dexmethylphenidate skeleton pattern transdermal patch containing vitiligo inhibitor and preparing method and application thereof
  • Dexmethylphenidate skeleton pattern transdermal patch containing vitiligo inhibitor and preparing method and application thereof
  • Dexmethylphenidate skeleton pattern transdermal patch containing vitiligo inhibitor and preparing method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] 【Prescription】(Based on 1000 stickers)

[0046] Dexmethylphenidate Hydrochloride 25g, Dioxidized Peptide 4g, Glycolic Acid 8g, Aminomethyl Propanol 8g, Ethanol 125g, DURO-TAK387-2052 Polyacrylate Pressure Sensitive Adhesive 120g, Ethyl Lauryl 4g, dl-a- Tocopherol 0.5g.

[0047]

[0048] The pressure-sensitive adhesive is a solvent-based pressure-sensitive adhesive, with a weight solid content of 47.5%. After drying, the solvent is removed from the solvent. The total weight is 120g, and it is 57g after drying;

[0049] Preparation:

[0050] Dissolve the dexmethylphenidate hydrochloride, ethyl lauryl alcohol, dl-a-tocopherol of prescription quantity in ethanol, the weight consumption of ethanol is 5 times of dexmethylphenidate hydrochloride; Stir 20 minutes with the speed of 500rpm, obtain clarification Transparent liquid; add dioxidized peptide and glycolic acid to the above liquid, stir at a speed of 1000rpm for 25 minutes to obtain a suspension; add polyacrylate p...

Embodiment 2

[0054] 【Prescription】(Based on 1000 stickers)

[0055] Dexmethylphenidate 18g, tretinoin 10g, ethyl acetate 126g, DURO-TAK87-2287 polyacrylate pressure-sensitive adhesive 180g, isosorbide dimethyl ether 35g, L-ascorbyl palmitate 0.35g.

[0056]

[0057] The pressure-sensitive adhesive is a solvent-based pressure-sensitive adhesive with a solid content of 50.5% by weight. After drying, the solvent is removed from the solvent. The total weight is 180g, and it is 90.9g after drying;

[0058] Preparation:

[0059] Dexmethylphenidate, isosorbide dimethyl ether, L-ascorbyl palmitate of recipe quantity are dissolved in ethyl acetate, and the weight consumption of ethyl acetate is 7 times of dexmethylphenidate; Stir with the speed of 1200rpm 15 Minutes, a clear and transparent liquid was obtained; vitamin A acid was added to the above liquid, and stirred at a speed of 3000rpm for 30 minutes to obtain a clear solution; polyacrylate pressure-sensitive adhesive was added to the suspe...

Embodiment 3

[0063] 【Prescription】(Based on 1000 stickers)

[0064] Dexmethylphenidate 65g, tetrahydromethylpyrimidine carboxylic acid 26g, ethyl acetate 390g, DURO-TAK87-2510 polyacrylate pressure-sensitive adhesive 450g, DowCorningBIO-PSA4202 pressure-sensitive adhesive 100g, 1,2-propylene glycol 50g, 2, 4.7 g of 6-di-tert-butyl-4-methylphenol.

[0065]

[0066] The DURO-TAK87-2510 polyacrylate pressure-sensitive adhesive is a solvent-based pressure-sensitive adhesive, with a weight solid content of 40.5%. After drying, the solvent is removed from the solvent. The total weight and dosage is 450g, and the drying is 182.25g;

[0067] DowCorningBIO-PSA7-4202 pressure-sensitive adhesive is a solvent-based pressure-sensitive adhesive, with a solid content of 60% by weight. After drying, the solvent is removed from the solvent. The total weight and dosage is 100g, and 60g after drying;

[0068] Preparation:

[0069] Dissolve the prescribed amount of dexmethylphenidate, 1,2-propylene glyco...

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PUM

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Abstract

The invention discloses a dexmethylphenidate skeleton pattern transdermal patch containing a vitiligo inhibitor and a preparing method thereof. The transdermal patch comprises a skeleton pattern adhesive layer, wherein the skeleton pattern adhesive layer comprises dexmethylphenidate or hydrochloride thereof, the vitiligo inhibitor and an adhesive, the vitiligo inhibitor contains one or more of titanium dioxide, tartaric acid, tretinoin, trichloroacetic acid, zinc oxide, hydroxyl dimethoxy phenylmalonate diethyl hexyl ester and ectoin, and the weight ratio of the vitiligo inhibitor is 5-15%. By the adoption of the transdermal patch, curative effect is guaranteed, and perpetual skin vitiligos are prevented from being generated; the efficacy of the preparation is improved, children clinical medication risks are reduced, and the safety of the preparation is fully guaranteed. The transdermal patch is simple in composition, the technology is simple and easy to apply, cost is low, and production is highly efficient.

Description

technical field [0001] The present invention relates to dexmethylphenidate skeleton type transdermal patch, preparation method and application thereof Background technique [0002] Attention deficit hyperactivity disorder (ADHD) is a common behavioral disorder in childhood, mainly manifested as obvious attentional disorientation and short attention span, hyperactivity, impulsive behavior accompanied by learning difficulties and conduct disorders. The incidence rate of children is higher, and the reported ADHD rate in my country is 1.3% to 13.4%. It not only affects children's life at school and at home, but also easily causes learning difficulties and behavioral problems, some of which persist for life. Some or even all of the symptoms of inattention and impulsivity may remain after adulthood, and there may be more social function problems, such as difficulty in work, poor interpersonal communication, low self-evaluation, impulsivity, irritability, etc.; obvious mental prob...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/4458A61K47/32A61K47/34A61P25/14A61K33/24A61K31/191A61K31/194A61K31/19A61K31/203A61K31/216A61K31/505
CPCA61K9/7084A61K31/19A61K31/191A61K31/194A61K31/203A61K31/216A61K31/4458A61K31/505A61K33/24A61K47/32A61K47/34A61K2300/00
Inventor 罗华菲林国钡张成豪武余波王浩侯惠民
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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