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Effect of Adjuvants on the Release Pattern of Suppositories Containing Paracetamol

机译:佐剂对扑热息痛栓剂释放规律的影响

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  ABSTRACT There is a vast interest in the scientific community and drug industry to exploit various mucosal routes of delivering drugs, which are poorly absorbed after oral administration. Human rectum remains to be a relatively unexplored route of drug delivery despite its potential as a non- invasive route of drug administration. The presence of dense network of blood vessels has made the rectum an excellent route of drug delivery for both systemic and local effect. The present investigation was aimed to evaluating the possibility of using different surfactant i.e. Span 60 and 80, Tween 60 and 80 on the release rate of formulation for the development of rectal drug delivery system of paracetamol, an NSAIDs, to minimize the gastric irritation of the drug upon oral administration. Suppositories were formulated by fusion method & evaluated for their physicochemical characterization followed by in vitro evaluation through spectrophotometrically. Suppositories containing PEG 4000 with Tween 80 showed a better permeation of drug with faster dissolution rate in vitro than other formulations. The formulations were designed to overcome the risk of upper gastrointestinal complications such as stomach bleeding, and may cause kidney or liver damage. Suppositories are dosage forms for use in the unavoidable circumstances such as comatose, nauseous or vomiting.
机译:摘要在科学界和制药行业中,人们非常感兴趣地利用各种粘膜途径来递送药物,这些途径在口服后难以吸收。尽管人类直肠具有作为药物非侵入性给药途径的潜力,但它仍然是相对未开发的药物给药途径。密集的血管网络的存在使直肠成为全身和局部药物输送的极佳途径。本研究旨在评估使用不同的表面活性剂(即Span 60和80,Tween 60和80)对制剂的释放速率的可能性,以开发对乙酰氨基酚(一种NSAIDs)的直肠药物输送系统,以最大程度地降低其对胃的刺激性。口服给药。通过融合法配制栓剂并对其理化性质进行评估,然后通过分光光度法进行体外评估。与其他制剂相比,含有PEG 4000和Tween 80的栓剂在体外具有更快的溶出速率,具有更好的药物渗透性。该制剂旨在克服上消化道并发症(如胃出血)的风险,并可能引起肾脏或肝脏损害。栓剂是在不可避免的情况下使用的剂型,例如昏迷,恶心或呕吐。

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