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Strategies for formulation development of andrographolide

机译：Andrographolide配方发育的策略

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Andrographolide (AN), a diterpenoid lactone, is one of the prime phytoconstituents of Andrographis paniculata. AN possesses various therapeutic benefits such as hepatoprotective, analgesic, anti-inflammatory, anti-tumor, anti-hyperglycemic, anti-oxidant activities. However, AN has not reached its milestone therapeutic potential as clinical studies have suggested that a conventional dosage form of AN showed low oral bioavailability (2.67%). The factors attributed to low bioavailability included specific site absorption, hydrolysis in weak alkaline environments, first pass metabolism, P-gp excretion in the terminal intestine, biliary excretion and poor aqueous solubility (3.29 mg mL(-1)). A successful AN therapy warrants an apt delivery system that will enhance its bioavailability. Current approaches for developing an improved delivery system for AN are mainly focused on overcoming solubility and toxicity issues. The path to identify new molecules with better therapeutic efficacy will continue to be an integral part of health care systems but here the authors have emphasized on 'better delivery of drugs', which is going to further refine therapy. The different formulation approaches investigated so far have shown much promise experimentally in improving the bioavailability of AN. However, a product for human use is still far away. Since its isolation and characterisation in 1911 several developments related to AN have occurred. This review is the first comprehensive account of the pharmaceutical aspects of AN with special emphasis on its delivery that have occurred over the last century.
机译：andrographolide（An），​​二萜内酯，是Andrographis Paniculata的原始植物植物中的一种。 AN具有各种治疗益处，如肝脏保护，镇痛，抗炎，抗肿瘤，抗高血糖，抗氧化活性。然而，随着临床研究表明，临床研究表明，常规剂型显示出低口服生物利用度（2.67％），尚未达到其里程碑治疗潜力。归因于低生物利用度的因素包括特异性位点吸收，弱碱性环境中的水解，首先通过代谢，末端肠道中的P-GP排泄，胆汁排泄和差的水溶性（3.29mg ml（-1））。成功的治疗权证保证了一个可提高其生物利用度的APT交付系统。用于开发改进的交付系统的目前的方法主要集中在克服溶解度和毒性问题上。识别具有更好治疗效力的新分子的路径将继续成为医疗保健系统的一个组成部分，但这里的作者强调了“更好地交付药物”，这将进一步细化治疗。到目前为止调查的不同的配方方法在实验上提高了提高的生物利用度。然而，用于人类使用的产品仍然很远。自1911年在1911年的隔离和表征中发生了几个与已发生相关的发展。该审查是第一个特别强调其在上世纪发生的交付的第一个全面叙述。

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  • 来源
    《RSC Advances》 |2016年第73期|共19页
  • 作者

    Pawar Atmaram; Rajalakshmi S.; Mehta Piyush; Shaikh Karimunnisa; Bothiraja Chellampillai;

  • 作者单位

    Bharati Vidyapeeth Deemed Univ Dept Pharmaceut Poona Coll Pharm Pune 411038 Maharashtra India;

    Padmashree Dr DY Patil Coll Pharm Dept Pharmaceut Pune 411044 Maharashtra India;

    Bharati Vidyapeeth Deemed Univ Dept Pharmaceut Poona Coll Pharm Pune 411038 Maharashtra India;

    Modern Coll Pharm Dept Pharmaceut Pune 411044 Maharashtra India;

    Bharati Vidyapeeth Deemed Univ Dept Pharmaceut Poona Coll Pharm Pune 411038 Maharashtra India;

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  • 正文语种 eng
  • 中图分类 化学;
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