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对含有扑热息痛和咖啡因的颗粒剂物理性质的评估。

Assessment of physical properties of granules with paracetamol and caffeine.

作者信息

Szumilo Michal, Belniak Piotr, Swiader Katarzyna, Holody Ewelina, Poleszak Ewa

机构信息

Chair and Department of Applied Pharmacy, Medical University of Lublin, Chodzki 1 Str., 20-093 Lublin, Poland.

出版信息

Saudi Pharm J. 2017 Sep;25(6):900-905. doi: 10.1016/j.jsps.2017.02.009. Epub 2017 Feb 16.

Abstract

Caffeine increases the analgesic properties of acetaminophen and therefore it is reasonable to use both substances together in one drug form in stronger pain. Currently, there are no commercially available pharmaceutical combination products containing acetaminophen and caffeine, which is present as granules. The aim of the study was to obtain twelve different granules with these therapeutic substances and determine the effect of various excipients on the quality of the drug form. All the granules were made by wet granulation. Two types of binders were used: polyethylene glycol 6000 (PEG) and polyvinylpyrrolidone K30 (PVP) as well as different types of fillers. The physical properties of granules were assessed in accordance to the requirements of the European Pharmacopoeia 8th ed. The highest apparent density was found in preparations containing calcium hydrophosphate (0.609 g/mL) and the lowest - containing mannitol (0.353 g/mL) as a filler. The Hausner ratio of most prepared granules ranged from 1.05 to 1.11, while the compressibility index ranged from 4.59 to 10.48%. The evaluation of properties of individual granules helped to indicate formulation with good features, which perhaps will be a good alternative to currently available painkillers with caffeine and acetaminophen.

摘要

咖啡因可增强对乙酰氨基酚的镇痛特性,因此在疼痛较剧烈时,将这两种物质制成单一剂型共同使用是合理的。目前,尚无市售的含有呈颗粒状的对乙酰氨基酚和咖啡因的复方制剂。本研究的目的是制备含这些治疗物质的12种不同颗粒,并确定各种辅料对剂型质量的影响。所有颗粒均采用湿法制粒。使用了两种粘合剂:聚乙二醇6000(PEG)和聚乙烯吡咯烷酮K30(PVP)以及不同类型的填充剂。根据欧洲药典第8版的要求对颗粒的物理性质进行了评估。含磷酸氢钙作为填充剂的制剂表观密度最高(0.609 g/mL),而含甘露醇作为填充剂的制剂表观密度最低(0.353 g/mL)。大多数制备颗粒的豪斯纳比在1.05至1.11之间,而压缩指数在4.59至10.48%之间。对单个颗粒性质的评估有助于确定具有良好特性的制剂,这可能是目前含咖啡因和对乙酰氨基酚的止痛药的良好替代品。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e1f/5605841/5c31e047ced4/gr1.jpg

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