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Aconite and glycyrrhiza composition transdermal patch

A technology of licorice composition and transdermal patch, which is applied in the field of medicine, can solve the problems of being unsuitable for patients who have difficulties in taking it orally, affecting the normal life of patients, and consuming time and effort to prepare it, so as to reduce cardiotoxicity and other adverse reactions, Avoid the first-pass effect and improve the effect of specificity

Active Publication Date: 2014-07-16
云南白药集团无锡药业有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] But the above-mentioned decoction is time-consuming and labor-intensive, and is not suitable for patients who have difficulty in oral administration; the toxicity of aconite in the formula is high, and oral administration is likely to cause serious adverse reactions, affecting the normal life of patients; oral administration, poor treatment specificity, And the efficacy of the drug is often greatly reduced due to the "first-pass effect" of the liver, resulting in poor efficacy

Method used

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  • Aconite and glycyrrhiza composition transdermal patch
  • Aconite and glycyrrhiza composition transdermal patch
  • Aconite and glycyrrhiza composition transdermal patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～ Embodiment 3

[0047] Embodiment 1~Example 3 Adhesive type screening

[0048] According to the bioavailability ratio of common external preparations and oral preparations 1.2 conversion, the above-mentioned administration area (6.5×10cm 2 ), the content of active ingredient extract of aconite and active ingredient extract of licorice in the prepared patch should be greater than 5wt%, so the maximum drug-loading concentration of the active ingredient extract of aconite and active ingredient extract of licorice in the adhesive matrix should be greater than 5wt%. .

[0049] According to the above patch preparation method, the aconite extract and licorice extract were added to different adhesives to directly prepare sample patches with different drug contents (contents were 1wt%, 2.5wt%, 5wt%, 10wt%, 15wt%, 20wt%) %), observe the prescription compatibility of the patch with the naked eye and a microscope (if the drug content exceeds the maximum drug loading capacity of the adhesive matrix, ther...

Embodiment 4～ Embodiment 12

[0059] Embodiment 4~Example 12 transdermal absorption enhancer type screening

[0060] Using Duro-Tak87-9301 as adhesive, add the following penetration enhancers: propylene glycol (PG), oleic acid (OA), isopropyl myristate (IPM), azone (Azone), N-methylpyrrolidone (NMP ), diethylene glycol monoethyl ether (Transcutol P), menthol (MT), menthol heptyl ester (M-OCT), menthol decyl ester (M-DOD), made into 9 transdermal patches ( Examples 4 to 12), the components of the patch and their contents are shown in Table 2; the transdermal permeation performance of each patch was investigated by in vitro percutaneous penetration test, two kinds of aconitine and licorice isoflavane A The time-drug cumulative permeation curve of the active ingredient is as follows: image 3 with Figure 4 shown. Depend on image 3 , Figure 4 It can be seen that the patch with NMP as the transdermal absorption enhancer has the best skin permeability (p<0.01), therefore, NMP is preferred as the transder...

Embodiment 13～ Embodiment 15

[0061] Embodiment 13~Example 15 Transdermal absorption accelerator NMP content optimization

[0062] Using NMP as a transdermal absorption accelerator, three kinds of transdermal patches (Example 13-Example 15) with different NMP contents were prepared. The components and contents of the drug storage layer of the patch are shown in Table 2; The permeation test was used to investigate the percutaneous penetration performance of each patch (Example 8, Example 13-Example 15). The time-drug cumulative penetration curves of the two active ingredients of aconitine and licorice isoflavane A are as follows: Figure 5 with Image 6 shown. Depend on Figure 5 , Image 6 It can be seen that when the content of NMP reaches 5wt%, its permeability-enhancing activity is close to saturation, therefore, the preferred concentration of NMP is 5wt%.

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Abstract

The invention provides an aconite and glycyrrhiza composition transdermal patch. The transdermal patch consists of a backing layer, a medicine storage layer and an anti-sticking layer. The medicine storage layer comprises 4-15wt% of aconite effective constituent extract, 4-15wt% of glycyrrhiza effective constituent extract, 60-90wt% of adhesive and 1-15wt% of skin penetration enhancer. A preparation method of the aconite and glycyrrhiza composition transdermal patch comprises the following steps of: completely and uniformly mixing the aconite effective constituent extract, the glycyrrhiza effective constituent extract, the adhesive and the skin penetration enhancer, coating a mixture on the anti-sticking layer, drying for 10 to 30 minutes at a temperature of 50-70 DEG C, and then covering the backing layer on the medicine storage layer, and punching to obtain a finished product. The transdermal patch provided by the invention is remarkable in analgesic effect, good in skin permeability, strong in treating specificity, low in toxic and side effects and convenient to use, and is applied to treating symptoms caused by rheumatic arthritis, rheumatoid arthritis and the like, such as pain, swelling and ankylosis, so that the aconite and glycyrrhiza composition transdermal patch has an extensive market application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a traditional Chinese medicine compound transdermal patch with active ingredient extracts of aconite and licorice. Background technique [0002] Rheumatic and rheumatoid arthritis is a common disease among middle-aged and elderly people, and its incidence rate is as high as 80% among people over 55 years old. In 1999, the World Health Organization listed such diseases together with cancer and cardiovascular diseases as the three major killers threatening human health. [0003] Gancao Fuzi Decoction comes from "Quanshengzhimifang" written by Wang Kuang in the Song Dynasty. Modern pharmacological studies have shown that aconitum alkaloids can significantly inhibit pain, and flavonoids in licorice can reduce the cardiotoxicity caused by aconite alkaloids to a certain extent. These studies have proved that the compound Rationality of drug compatibility. [0004] But ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K36/714A61K9/70A61P19/02A61P29/00
Inventor 穆利伟陆晔辉刘跃
Owner 云南白药集团无锡药业有限公司
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