Rotundine transdermal patch and preparation method thereof

A technology of transdermal patch and penetration enhancer, which is applied in the field of medicine to achieve the effect of improving action time and bioavailability, small molecular weight, non-irritating and toxic

Active Publication Date: 2014-12-10
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When the effect of using a specific drug penetration enhancer alone is not ideal, the combined application of different varieties of volatile oil or volatile oil with chemical penetration enhancers such as azone may have a better penetration enhancement effect than single use

Method used

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  • Rotundine transdermal patch and preparation method thereof
  • Rotundine transdermal patch and preparation method thereof
  • Rotundine transdermal patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Prepare the rotundine transdermal patch, which is composed of a backing layer, a drug-containing adhesive layer and a protective layer, and its preparation method is:

[0030] (1) Preparation of medicinal solution 1: Accurately weigh 0.35g of rotundine, weigh 0.06g of succinic acid, add 1ml of 10%H 2 SO 4 and 3ml of 80% ethanol sonicated to completely dissolve into a colorless and transparent solution;

[0031] (2) Preparation of drug solution 2: add 0.9g Eudragit E100 to drug solution 1, stir to dissolve it into a colorless and transparent solution, then add 0.6ml glycerin and 0.6ml acrylate emulsion pressure-sensitive adhesive, stir well, then add 200μl cloves For volatile oil, stir and sonicate to make it evenly mixed without bubbles;

[0032] (3) Patch preparation: pour the prepared drug solution 2 on the 50cm area where the backing layer is laid 2 In the mould, it is paved by salivating process, air-dried at 40°C for 1.5h, then taken out and dried at 25°C for 12...

Embodiment 2～11

[0034] Prepare rotundine transdermal patch, which is made up of backing layer, drug-containing adhesive layer and protective layer, its preparation method is the same as the preparation process described in embodiment 1, only the added clove volatile oil (warming medicine, called for short cloves) Oil, hereinafter the same) were successively changed to star anise oil (inner-warming medicine) optimized by test sieve; notopterygium oil (pungent and warm-relieving medicine); Borneol (aromatic rejuvenating medicine), and several mixed penetration enhancers (mixing ratio 1:1) Piper Cubeb Oil + Azone, White Cardamom Oil + Asarum Oil, Clove Oil + Notopterygium Oil, Amomum Oil + White Cardamom oil was respectively prepared into rotundine patches containing different volatile oil penetration enhancers, which were sequentially compiled into Examples 2-11.

Embodiment 12

[0036] Prepare the rotundine transdermal patch, which is composed of a backing layer, a drug-containing adhesive layer and a protective layer, and its preparation method is:

[0037] (1) Preparation of medicinal solution 1: Accurately weigh 0.35g of rotundine and 0.06g of adipic acid, dissolve in 2ml of absolute ethanol by ultrasonic, add 0.6g of E100 and stir to dissolve;

[0038] (2) Preparation of medicinal solution 2: add 0.3ml diethyl phthalate, 0.6g polyisobutylene 6T and polyisobutylene B50, 0.6ml propylene glycol, 100μl asarum volatile oil and 100μl azone to the medicinal solution 1, mix evenly have to.

[0039] (3) Patch preparation: Take the drug solution 2 and spread a film on the backing by salivation process, dry at 25°C for 12 hours, take it out and cover it with a protective layer, cut it, and seal it.

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Abstract

The invention discloses a rotundine transdermal patch and a preparation method thereof. The transdermal patch is formed by a lining layer, a drug-containing sticking layer and a protective layer which are sequentially laminated, wherein the drug-containing sticking layer is prepared from 7-14 parts of rotundine or rotundine sulphate, 1-10 parts of percutaneous penetration enhancer, 40-70 parts of pressure-sensitive adhesive, 10-30 parts of moisturizer, 10-25 parts of plasticizer and 1-3 parts of crosslinking agent. The rotundine transdermal patch disclosed by the invention is higher in rotundine accumulation infiltration capacity and can maintain effective blood concentration for a longer time, and experiments adopting a writhing method and a hot plate method show that the rotundine transdermal patch disclosed by the invention has a good analgesic effect. Blood concentration is still kept at 0.433mg / L 48 hours after administration, stable blood concentration is kept in vivo, and no peak phenomenon is caused; and pharmacology experiments prove that the rotundine transdermal patch disclosed by the invention has an obvious and long-lasting analgesic effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a rotundine transdermal patch with continuous analgesic effect. At the same time, the invention also relates to a preparation method of the transdermal patch. Background technique [0002] Rotundine (Cranialin, L-tetrahydropalmatine, Rotundine, L-Tetrahydropalmatine) is 2,3,9,10-tetramethoxy-5,8,13,13a-tetrahydro-6H-diphenyl And[a,g]quinazine is an alkaloid extracted from plants of the genus Stephaniaceae. Rotundine has analgesic, sedative, hypnotic and stable effects, and its analgesic effect is weaker than pethidine, stronger than general antipyretic and analgesic drugs, and its biggest feature is that it is non-addictive. At therapeutic doses, it has no respiratory depressant effect and does not cause gastrointestinal smooth muscle spasm. It is better for chronic persistent pain and visceral dull pain, but less effective for acute sharp pain (such as postoperat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K31/4375A61P29/00
Inventor 马云淑杨芬崔利利黄金娥张贵华程欣
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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