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首页> 外文会议>Proceedings of international symposium on crystal engineering and drug delivery system 2009 >Recent Advances of Penetration of Biological Macromolecular Drugs in Transdermal Drug Delivery System
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Recent Advances of Penetration of Biological Macromolecular Drugs in Transdermal Drug Delivery System

机译：生物大分子药物在透皮给药系统中的渗透研究进展

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The research of biological macromolecular drugs in transdermal drug delivery system (including transdermal and mucous administration) always is a crucial and difficult field in pharmaceutics research, because this drug generally displays characteristics including high molecular weight, high hydrophilic properties, poor stability, short biological half-life, enzymatic degradation in the gastrointestinal tract and the hepatic first-pass metabolism effect for oral administration. Therefore, The main route in clinical therapy is conducted by injection or implantation, which cause great agony and inconvenient to patients. Dermal or mucous surface drug delivery can not only avoide the destroying of gastrointestinal environment to drug molecules and the first-pass metabolism effect, efficiently solving the problem that biological macromolecular drugs easily lost activity leading to low bioavailabilities and short biological half-life, and sustained a long-term steady rate of drug delivery and plasma concentration, as well as reduce systemic side effects; but also avoid the disadvantage of biological macromolecular drugs by injection or implantation, and provide patients with an easier and more convenient route for drug administration. However, there also are some limitations in transdermal and mucous drug delivery, such as requiring the drugs with Molecular weight lower than 500, melting point less than 300℃, and a certain distribution coefficient. It is difficult for aqueous macromolecules to permeate skin or mucous membrane due to its low permeability, high hydrophilicity and physiological structure barrier. A key problem that biological macromolecular drugs permeate skin or mucous membrane is to overcome the barrier function of skin or mucous membrane and improve drug permeability. Therefore, more and more studies have been carried out to increase drug permeability through the stratum corneum or mucous membrane, to achieve therapeutic levels.
机译：透皮给药系统（包括透皮和粘液给药）中生物大分子药物的研究一直是药物学研究的关键和困难领域，因为该药物通常表现出高分子量，高亲水性，稳定性差，生物学半衰期短等特点。寿命，胃肠道酶促降解以及口服肝的首过代谢作用。因此，临床治疗的主要途径是通过注射或植入进行，这给患者带来极大的痛苦和不便。皮肤或粘液表面的药物传递不仅可以避免胃肠道环境对药物分子的破坏和首过代谢作用，还可以有效解决生物大分子药物容易失去活性，导致生物利用度低，生物半衰期短，持续的问题。长期稳定的药物输送速度和血浆浓度，以及减少全身性副作用；但也避免了注射或植入生物大分子药物的弊端，为患者提供了更简便，更方便的给药途径。但是，在透皮和粘液递送方面也存在一些局限性，例如要求分子量小于500，熔点小于300℃且具有一定分配系数的药物。水性大分子由于其低渗透性，高亲水性和生理结构屏障而难以渗透皮肤或粘膜。生物大分子药物渗透皮肤或粘膜的关键问题是克服皮肤或粘膜的屏障功能并提高药物渗透性。因此，已经进行了越来越多的研究来增加药物穿过角质层或粘膜的渗透性，从而达到治疗水平。

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