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Analgesic and antiphlogistic medicines and micro-needle transdermal administration method for same

A technology for analgesics and drugs, applied in the field of microneedle transdermal drug delivery methods and systems for drugs and their compositions, can solve problems such as drug dependence, and achieve the effect of improving pain

Inactive Publication Date: 2012-04-11
上海泰因生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the heavy use of pain relievers such as opioids often leads to side effects such as drug dependence

Method used

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  • Analgesic and antiphlogistic medicines and micro-needle transdermal administration method for same
  • Analgesic and antiphlogistic medicines and micro-needle transdermal administration method for same

Examples

Experimental program
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Effect test

Embodiment 1

[0031] The transdermal administration of aconitin was performed using solid titanium metal microneedle array system. They were in 2cm 2 Different amounts of aconitin were smeared on the microneedle sequence, and acted on the skin of guinea pigs for 5min or 15min. The results showed that the bioavailability of aconitin could reach 75%, and the variability was at an acceptable level (30%); the concentration of aconitin in the blood reaches the peak after 40min; after transdermal and intravenous administration, the elimination kinetics of aconitin are very similar, indicating that there is no storage in the skin; the aconitin on the microneedles Only 7% of the dose of aconitin remained on the skin surface, indicating that the transdermal administration of aconitin by using the microneedle array system is a safe and effective means.

Embodiment 2

[0033] Feasibility of solid microneedles for transdermal administration of urine, using high concentration dextrin as a base to add urine, making biodegradable microneedles, and administering hormonin to mice. Select 3 Three kinds of different doses of gaurine, respectively: 0.5, 1.0, 2.5 I U / kg. Results The bioavailability of these three doses were: 98.7%, 93.8%, 92.3%. In vitro release studies showed that almost all The homogenate was released within 1 hour, and the time for 50% release was (15.4±1.1) min. In addition, the homogenate was stored in this microneedle under the conditions of -80, 20, and 40°C for 1 The remaining amounts after one month are 98.2%, 98.9%, and 99.0%, respectively, that is, they can exist relatively stably at 40°C.

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Abstract

The invention provides analgesic and antiphlogistic medicines and a micro-needle transdermal administration method for the same. Analgesic and antiphlogistic traditional Chinese medicines with aconitum alkaloid as a representative have the characteristics of long action and non-frequent administration; a micro-needle administration system enables slow release and sustained release of aconitum alkaloid to be realized. A plasma concentration in a range of 0.5 to 500 ng / ml is achieved in 0.5 to 14 h after administration. The invention provides a micro-needle transdermal administration method and system for analgesic and antiphlogistic medicines capable of enhancing pain or inflammation, with aconitum alkaloid included. According to the invention, usage amount of aconitum alkaloid is sufficient to enable a plasma concentration of about 0.5 to 400 ng / ml to be achieved and maintained; administration through skin pricking enables painless administration to be realized, and the medicines themselves do not cause direct irritation or damage to skin surface.

Description

technical field [0001] The present invention mainly relates to a microneedle administration method and system of a drug capable of improving pain and inflammation and a composition thereof. More specifically, the present invention relates to a microneedle transdermal drug delivery method and system for drugs and compositions thereof that can improve pain and inflammation, including alkaloid compounds extracted from plants of the genus Aconitum. Background of the invention [0002] Everyone experiences pain of various kinds throughout their lives. Pain and inflammation accompany most diseases and physical injuries. Research and search for analgesic and anti-inflammatory drugs with maximum efficacy and minimum side effects (such as drug dependence) have always been the pursuit of people in this field. At present, many analgesics such as codeine and tramadol have been used to control mild to moderate pain. Additionally, some opioids such as morphine, methadone, hydromorphone...

Claims

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Application Information

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IPC IPC(8): A61K31/439A61P29/00A61M37/00
Inventor 齐念民穆玉彬李巍巍郑琛
Owner 上海泰因生物技术有限公司
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