本文選題：經(jīng)皮給藥系統(tǒng) + 經(jīng)皮吸收��； 參考：《中國藥房》2017年31期

【摘要】：目的:為加強(qiáng)經(jīng)皮給藥制劑的開發(fā)與應(yīng)用提供參考。方法:以"微針""駐極體""離子導(dǎo)入""經(jīng)皮給藥系統(tǒng)""促滲""Microneedle""Electret""Inotophoresis""Transdermal drug delivery system"等為關(guān)鍵詞,組合查詢2001年1月-2017年2月在PubMed、ScienceDirect、中國知網(wǎng)、萬方、維普等數(shù)據(jù)庫中的相關(guān)文獻(xiàn),對促進(jìn)藥物經(jīng)皮吸收的物理技術(shù)的研究進(jìn)行綜述。結(jié)果與結(jié)論:共檢索到相關(guān)文獻(xiàn)584篇,其中有效文獻(xiàn)65篇。常用的單一物理技術(shù)促滲方法有微針、駐極體、離子、超聲、電致孔、激光、磁場導(dǎo)入、熱穿孔。其中,微針經(jīng)皮給藥適用于大分子藥物(如皮膚滲透率較低的多肽、蛋白質(zhì)和疫苗等);微針的針體長度、形狀以及硬度、針壁厚度、載藥量、滯留時間和體內(nèi)降解問題是今后重點(diǎn)的研究對象。駐極體對離子型藥物和非離子型藥物都有良好的透皮促滲作用,但對離子型藥物效果更佳;國內(nèi)對于駐極體促滲的實驗研究少,目前其臨床應(yīng)用無相關(guān)報道。離子導(dǎo)入、電致孔促滲在中藥中的運(yùn)用較熱門,適用于電離性能較好的小分子藥物(如胰島素),但依賴帶電裝置及能量的特點(diǎn)導(dǎo)致推廣受限。離子導(dǎo)入適用于慢性疾病如癌癥和糖尿病的治療;今后研究重點(diǎn)在于明確導(dǎo)入體內(nèi)發(fā)揮作用的主要成分及其作用機(jī)制。超聲導(dǎo)入主要適用于水溶性好的藥物(如多肽和蛋白質(zhì));加強(qiáng)系統(tǒng)的安全性研究以及空化作用的機(jī)制研究、改善裝置設(shè)計缺陷是今后研究的重點(diǎn)。利用激光破壞表皮的屏障作用促進(jìn)藥物經(jīng)皮吸收,在醫(yī)藥領(lǐng)域應(yīng)用前景良好。目前磁場導(dǎo)入與熱穿孔技術(shù)促滲的國內(nèi)外相關(guān)文獻(xiàn)報道較少,今后的重點(diǎn)是加強(qiáng)這兩者的機(jī)制、優(yōu)化裝置性能研究以及解決安全性問題。兩種或多種物理技術(shù)的聯(lián)用盡管能大大提高藥物經(jīng)皮透過率,但制作的復(fù)雜性和高成本是亟需突破的難題。
[Abstract]:Objective: to provide reference for the development and application of transdermal drug delivery. Methods: using "microneedle" "electret" "ion introduction" "percutaneous drug delivery system" "Microneedle", "Electret", "Inotophoresis" "Transdermal drug delivery system" as the keywords, the relevant documents in the database of PubMedine Science Direct, China knowledge Network, Wanfang, Weip, etc., from January 2001 to February 2017, were investigated. This paper reviews the research on physical techniques to promote drug percutaneous absorption. Results & conclusion: a total of 584 related literatures were retrieved, of which 65 were valid. The commonly used single physical techniques are microneedle, electret, ion, ultrasonic, electroporation, laser, magnetic field introduction, hot perforation. Among them, microneedle transdermal administration is suitable for macromolecular drugs (such as peptides, proteins and vaccines with low skin permeability, etc.); needle length, shape, hardness, thickness of needle wall, drug load, etc. Retention time and degradation in vivo are the key research objects in the future. Electret has good transdermal permeation effect on ionic drugs and Nonionic drugs, but it has better effect on ionic drugs. There are few experimental studies on electret permeation in China, and there are no related reports on its clinical application at present. The application of ion introduction and electroporation in traditional Chinese medicine is more popular. It is suitable for small molecular drugs with good ionization performance (such as insulin), but its popularization is limited due to its dependence on charged devices and energy. Iontophoresis is suitable for the treatment of chronic diseases such as cancer and diabetes. Ultrasonic introduction is mainly suitable for water-soluble drugs (such as peptides and proteins). It is the focus of the future research to strengthen the safety study of the system and the mechanism of cavitation mechanism, and to improve the design defects of the device. Using laser to destroy the barrier of epidermis to promote drug transdermal absorption has a good prospect in the field of medicine. At present, there are few reports about magnetic field introduction and hot perforation technology in domestic and foreign literature. In the future, the emphasis is to strengthen the mechanism of the two, optimize the performance of the device and solve the safety problems. Although the combination of two or more physical technologies can greatly improve the transdermal transmittance of drugs, the complexity and high cost of preparation are the difficult problems that need to be overcome.
【作者單位】： 廣東藥科大學(xué)藥學(xué)院/廣東省藥物新劑型重點(diǎn)實驗室;
【基金】：廣州市重點(diǎn)實驗室專項項目(No.2014SY000005)
【分類號】：R943

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