{"title":"羟丙基甲基纤维素与麦芽糖糊精湿法制备对乙酰氨基酚的研究","authors":"Ortega Leticia, G. Martin, D. Rodríguez","doi":"10.11648/J.JDDMC.20190502.12","DOIUrl":null,"url":null,"abstract":"The purpose of this work is to improve one of the important physicochemical properties of an active pharmaceutical ingredient (API), as is the water solubility of paracetamol. To improve the physicochemical properties of this API, two pharmaceutical excipients such as the HPMC and maltodextrin were used, which help to improve the solubility, and this helps to the manufacturing process of a pharmaceutical product. Different granule formulations were manufactured by applying a matrix design of experiment where the wet granulation process was performed, combining Paracetamol with the excipients to obtain a uniform particle size and subsequently evaluate the properties of interest. The solubility was evaluated using a method (Mexican pharmacopoeia - FEUM) based on UV / VIS method, performing the calibration curve only for the API to evaluate the granule and calculate the percentage of solubility of these. Favorable results were obtained for two of the seven granule formulations manufactured, the mixture of granule F and G: 25 g of paracetamol, 1.5; 1.75 g of HPMC and 23.5 g; 23.25 of the maltodextrin has a solubility of 104.17% and 101.48% of the G, which shows that the process by wet granulation can improve its solubility. This type of co-processed granule also fulfills the function of masking the bitter taste of paracetamol in one oral pharmaceutical form, as in the case of a syrup and it could be an advantage in the market. The flavor was evaluated by a panel of 20 people and the taste of the syrups that were prepared with the granule with better solubility was compared with the syrups containing only the API dissolved. It is shown that the granules F have improvement in the solubility of paracetamol and can mask the unpleasant (bitter) taste of the active ingredient.","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"19 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2019-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development of Co-processed Paracetamol with Hydroxypropyl Methylcellulose (HPMC) and Maltodextrin by Wet Granulation Process\",\"authors\":\"Ortega Leticia, G. Martin, D. Rodríguez\",\"doi\":\"10.11648/J.JDDMC.20190502.12\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The purpose of this work is to improve one of the important physicochemical properties of an active pharmaceutical ingredient (API), as is the water solubility of paracetamol. 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Favorable results were obtained for two of the seven granule formulations manufactured, the mixture of granule F and G: 25 g of paracetamol, 1.5; 1.75 g of HPMC and 23.5 g; 23.25 of the maltodextrin has a solubility of 104.17% and 101.48% of the G, which shows that the process by wet granulation can improve its solubility. This type of co-processed granule also fulfills the function of masking the bitter taste of paracetamol in one oral pharmaceutical form, as in the case of a syrup and it could be an advantage in the market. The flavor was evaluated by a panel of 20 people and the taste of the syrups that were prepared with the granule with better solubility was compared with the syrups containing only the API dissolved. 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引用次数: 0
摘要
这项工作的目的是改善活性药物成分(API)的一个重要的物理化学性质,即扑热息痛的水溶性。为了改善该原料药的理化性质,使用了两种药用辅料,如HPMC和麦芽糖糊精,这有助于提高溶解度,这有助于制药产品的制造过程。不同的颗粒配方是通过应用实验的基质设计,其中湿制粒过程进行,结合扑热息痛与辅料,以获得一个统一的粒度,随后评估感兴趣的性质。采用基于紫外/可见法的方法(墨西哥药典- FEUM)评价溶解度,仅对API进行校准曲线评价颗粒并计算其溶解度百分比。制备的七种颗粒剂中有两种效果良好,F和G颗粒剂的混合物:25g扑热息痛,1.5;1.75 g HPMC和23.5 g;23.25的麦芽糖糊精对G的溶解度为104.17%,对G的溶解度为101.48%,说明湿造粒工艺可以提高其溶解度。这种类型的协同加工颗粒还可以在一种口服药物形式中掩盖扑热息痛的苦味,就像糖浆一样,这可能是市场上的一个优势。由20人组成的小组对风味进行了评估,并用溶解度更好的颗粒制备的糖浆的味道与仅溶解API的糖浆进行了比较。研究表明,颗粒F改善了扑热息痛的溶解度,可以掩盖活性成分的不愉快(苦)味。
Development of Co-processed Paracetamol with Hydroxypropyl Methylcellulose (HPMC) and Maltodextrin by Wet Granulation Process
The purpose of this work is to improve one of the important physicochemical properties of an active pharmaceutical ingredient (API), as is the water solubility of paracetamol. To improve the physicochemical properties of this API, two pharmaceutical excipients such as the HPMC and maltodextrin were used, which help to improve the solubility, and this helps to the manufacturing process of a pharmaceutical product. Different granule formulations were manufactured by applying a matrix design of experiment where the wet granulation process was performed, combining Paracetamol with the excipients to obtain a uniform particle size and subsequently evaluate the properties of interest. The solubility was evaluated using a method (Mexican pharmacopoeia - FEUM) based on UV / VIS method, performing the calibration curve only for the API to evaluate the granule and calculate the percentage of solubility of these. Favorable results were obtained for two of the seven granule formulations manufactured, the mixture of granule F and G: 25 g of paracetamol, 1.5; 1.75 g of HPMC and 23.5 g; 23.25 of the maltodextrin has a solubility of 104.17% and 101.48% of the G, which shows that the process by wet granulation can improve its solubility. This type of co-processed granule also fulfills the function of masking the bitter taste of paracetamol in one oral pharmaceutical form, as in the case of a syrup and it could be an advantage in the market. The flavor was evaluated by a panel of 20 people and the taste of the syrups that were prepared with the granule with better solubility was compared with the syrups containing only the API dissolved. It is shown that the granules F have improvement in the solubility of paracetamol and can mask the unpleasant (bitter) taste of the active ingredient.