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Risperidone percutaneous absorption paster

A risperidone and patch technology, applied in the field of pharmacy, can solve the problems of unfavorable long-term treatment of schizophrenia, higher price than oral dosage forms, unfavorable diabetic patients, etc., and achieves prolonging the action time of the drug, convenient storage and transportation, and production. low cost effect

Inactive Publication Date: 2009-02-18
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, RISPERDAL CONSTA has many shortcomings: the route of administration is deep intramuscular injection, and PLGA degradation product lactic acid will cause pain at the injection site and increase blood sugar concentration, which is very unfavorable for diabetic patients
Although PLGA is a biodegradable material, it may initially form lumps and may cause allergic reactions
The use of RISPERDAL CONSTA is not only cumbersome but also has strict requirements, storage conditions are harsh, and the price is more expensive than oral dosage forms. For most patients with schizophrenia, long-term administration of RISPERDAL CONSTA is unbearable
None of this is good for the long-term treatment of schizophrenia

Method used

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  • Risperidone percutaneous absorption paster
  • Risperidone percutaneous absorption paster
  • Risperidone percutaneous absorption paster

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Polyacrylate pressure-sensitive adhesive 500mg, drug risperidone 50mg, lauryl alcohol 23mg (or 35mg, 48mg), dissolved in ethyl acetate, spread on 100cm 2 On the protective film, dry at 60°C for 30 minutes to remove ethyl acetate, and cover the backing layer after cooling. The dried matrix layer contains 87.3% (or 85.5%, 83.6%) of polyacrylate, 8.7% (or 8.5%, 8.4%) of risperidone, and 4% (or 6%, 8%) of dodecanol. The determination of permeability and risperidone was performed as in the comparative example. image 3 For the cumulative drug penetration-time curve of this example, the penetration rates of the patches with dodecyl alcohol content of 4%, 6% or 8% are 3.37±0.17 μg cm -2 h -1 , 4.28±0.31μg cm -2 h -1 , 3.41±0.30μg cm -2 h -1 .

Embodiment 2

[0040] Polyacrylate pressure sensitive adhesive 500mg, drug risperidone 50mg, lauryl nitrogen Ketone 11.5mg (or 23mg, 35mg, 48mg, 62mg), dissolved in ethyl acetate, spread on 100cm 2 On the backing layer, dry at 60°C for 30 minutes to remove ethyl acetate, and cover with a protective film after cooling. The matrix layer after drying contains polyacrylate 89% (or 87.3%, 85.5%, 83.6%, 82%), risperidone 9% (or 8.7%, 8.5%, 8.4%, 8%), lauryl nitrogen Ketones 2% (or 4%, 6%, 8%, 10%). The determination of permeation rate and risperidone was performed as in the comparative example. Figure 4 Be the drug cumulative penetration-time curve of this embodiment, lauryl nitrogen The penetration rate of patches with ketone content of 2%, 4%, 6%, 8% or 10% was 2.31±0.17 μg cm -2 h -1 , 3.09±0.15μg cm -2 h -1 , 4.27±0.25μg cm -2 h -1 , 3.43±0.11μg cm -2 h -1 , 6.97±0.98μg cm -2 h -1 .

Embodiment 3

[0042] Polyacrylate pressure sensitive adhesive 500mg, drug risperidone 50mg, lauryl nitrogen Ketone 36mg, propylene glycol 24mg (or 37mg, 51mg, 65mg), dissolved in ethyl acetate, spread on 100cm 2 On the protective film, dry at 60°C for 30 minutes to remove ethyl acetate, and cover the backing layer after cooling. The matrix layer after drying contains polyacrylate 82% (or 80%, 78%, 76.8%), risperidone 8% (or 8%, 8%, 7.7%), lauryl nitrogen Ketone 6% (or 6%, 6%, 5.5%), propylene glycol 4% (or 6%, 8%, 10%). The determination of permeability and risperidone was performed as in the comparative example. Figure 5 It is the drug cumulative penetration-time curve of this embodiment, as can be seen from the figure containing 6% lauryl nitrogen The penetration rates of ketone and propylene glycol 4%, 6%, 8% or 10% patches were 4.29±0.17μg·cm -2 h -1 , 5.15±0.01μg cm -2 h -1 , 5.52±0.33μg cm -2 h -1 , 5.24±0.15μg cm -2 h -1 .

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Abstract

The invention discloses a risperidone transdermal absorbing patch, which consists of a back lining layer, a protective film and a substrate layer which is arranged between the back lining layer and the protective film and contains medicines. The compositions of the substrate layer containing the medicines by weight percent are 65 to 95 percent of polyacrylate pressure sensitive adhesive, 4 to 15 percent of risperidone and 1 to 20 percent of transdermal enhancer. The patch delivers the risperidone by means of transdermal impregnation, can prolong the acting time of the medicine, maintains stable blood drug level, reduces the side effect of the medicine, is convenient to use, and can be taken as a medicine for treating various mental sickness such as schizophrenia, mania or dementia and so on.

Description

technical field [0001] The invention belongs to the field of pharmacy, in particular to a transdermal absorption patch of drug risperidone. Background technique [0002] Risperidone is a selective monoaminergic antagonist with unique properties. It is a new generation of antipsychotic drugs and is mainly used for the treatment of schizophrenia, mania and dementia. It is related to the serotonergic 5-HT 2 receptors and dopaminergic D 2 The receptor has a high affinity, so it can be used for the treatment of mental disorders, including acute and chronic schizophrenia and other positive symptoms (such as hallucinations, delusions, disordered thinking, hostility, suspicion) and negative symptoms ( (e.g., unresponsiveness, apathy, hypophasia, social difficulties), may also reduce affective symptoms (e.g., depression, guilt, anxiety) and associated behavioral disturbances associated with schizophrenia. Risperidone is the most commonly prescribed antipsychotic today. [0003] F...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/519A61P25/18
Inventor 梁文权陈晓瑾胡公允金一
Owner ZHEJIANG UNIV
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