Cyclodextrin-containing drug preparation, drug transdermal patch and preparation method for drug transdermal patch

A technology of pharmaceutical preparations and transdermal patches, which is applied in the field of medicine to achieve the effects of reducing irritation, reducing adverse reactions, and improving bioavailability

Pending Publication Date: 2020-12-04
江苏一全药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the existing transdermal patches are still difficult to achieve long-lasting (up to 5-7 days) effective release, and new absorption enhancers may bring new risks to the human body

Method used

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  • Cyclodextrin-containing drug preparation, drug transdermal patch and preparation method for drug transdermal patch
  • Cyclodextrin-containing drug preparation, drug transdermal patch and preparation method for drug transdermal patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment A1

[0088] (1) Prepare packaged medicine

[0089] Weigh 0.28g of escitalopram, 0.3g of β-cyclodextrin and 0.2g of 2,6-dimethyl-β-cyclodextrin, add water at 60°C with electric stirring at constant temperature to make the hydroxypropyl β-cyclodextrin When the dextrin reaches saturation, continue to stir for 30 minutes, then pour it into an evaporating dish, evaporate to dryness in a water bath at 90°C, place it in a desiccator, and grind it finely to obtain the escitalopram cyclodextrin coating, with an average particle size of 254nm.

[0090] (2) Ingredients

[0091] Encapsulated drug: prepared in this embodiment;

[0092] Unpacked drug: escitalopram, 0.1g;

[0093] Transdermal absorption enhancer: isopropyl myristate, 0.57g;

[0094] Drug-loaded matrix: a total of 6.19g, of which 4.33g is 2852 pressure-sensitive adhesive (containing carboxyl group), 1.23g is 2287 pressure-sensitive adhesive (containing hydroxyl group), and 4098 pressure-sensitive adhesive (no functional group) ...

Embodiment A2

[0100] (1) Prepare packaged medicine

[0101] Weigh 0.25g of escitalopram, 0.33g of β-cyclodextrin and 0.17g of 6-hydroxypropyl-β-cyclodextrin, add water at 60°C with electric stirring at constant temperature to make hydroxypropyl-β-cyclodextrin When it reaches saturation, continue to stir for 30 minutes, then pour it into an evaporating dish, evaporate to dryness in a water bath at 90°C, place it in a desiccator, and grind it finely to obtain the escitalopram cyclodextrin coating, with an average particle size of 312nm.

[0102] (2) Ingredients

[0103] Encapsulated drug: prepared in this embodiment;

[0104] Unpacked drug: escitalopram, 0.1g;

[0105] Transdermal absorption enhancer: isopropyl myristate, 0.42g;

[0106] Drug-loaded matrix: a total of 6.38g, of which 5.1g is 235A pressure-sensitive adhesive (containing carboxyl group), 0.64g is 2516 pressure-sensitive adhesive (containing hydroxyl group), and 4098 pressure-sensitive adhesive (no functional group) 0.64g; ...

Embodiment A3

[0112] Weigh 0.22g of escitalopram, 0.18g of β-cyclodextrin and 0.15g of carboxymethyl-β-cyclodextrin, add water and stir at a constant temperature of 60°C to make the hydroxypropyl β-cyclodextrin reach saturation , continue to stir for 30 minutes, then pour it into an evaporating dish, evaporate to dryness in a water bath at 90°C, place it in a desiccator for drying, and grind it finely to obtain the escitalopram cyclodextrin coating, with an average particle size of 348nm.

[0113] (2) Ingredients

[0114] Encapsulated drug: prepared in this embodiment;

[0115] Unpacked drug: escitalopram, 0.1g;

[0116] Transdermal absorption enhancer: Span 20, 0.7g;

[0117] Drug-loaded matrix: 5.2g in total, of which 3.12g is 2852 pressure-sensitive adhesive (containing carboxyl group), 2.08g is 2516 pressure-sensitive adhesive (containing hydroxyl group);

[0118] Solvent: n-butanol, 0.5 g.

[0119] (3) preparation of drug transdermal patch

[0120] Mix and dissolve the unwrapped d...

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Abstract

The invention relates to the field of medicine, in particular to a drug preparation, a drug transdermal patch containing the drug preparation and a preparation method for the drug transdermal patch The drug preparation comprises a coated drug and an uncoated drug; the coated drug includes a drug A and an inclusion material coating the drug A; the inclusion material contains cyclodextrin and / or a derivative thereof; the uncoated drug is a drug B; and the drug A and the drug B are same or different. The drug preparation and the drug transdermal patch of the invention can stably release an effective dose of the drug lastingly (up to 7 days), and have relatively high controllability so as to meet the medication requirements of patients of different degrees.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a pharmaceutical preparation, a drug transdermal patch containing the pharmaceutical preparation and a preparation method thereof. Background technique [0002] External treatment is a commonly used method in clinical practice. In the early days, it was mostly in the form of Chinese herbal plasters, which were used to apply acupoints or local injuries to achieve therapeutic effects. This treatment method is simple and easy to operate, and has a high degree of patient acceptance. [0003] In addition, for Western medicines that are traditionally taken orally or injected, transdermal patches have appeared in recent years to replace oral or injected. On the other hand, it can increase patient acceptance. However, it is still difficult for the drug to release an effective dose through the stratum corneum of the skin, and the penetration dose, stability and duration have not been ideal. In t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/69A61K31/5517A61P25/20A61P25/22A61P25/08A61P25/24
CPCA61K9/7061A61K47/6951A61K47/6949A61K31/5517A61P25/20A61P25/22A61P25/08A61P25/24
Inventor 全丹毅
Owner 江苏一全药业有限公司
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