Development of Co-processed Paracetamol with Hydroxypropyl Methylcellulose (HPMC) and Maltodextrin by Wet Granulation Process
Journal of Drug Design and Medicinal Chemistry
Volume 5, Issue 2, June 2019, Pages: 26-32
Received: Jul. 5, 2019;
Accepted: Jul. 22, 2019;
Published: Aug. 7, 2019
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Ortega Leticia, Department of Biological Systems, Metropolitan Autonomous University–Campus Xochimilco (UAM-X), Mexico City, Mexico
Gómez Martín, Department of Biological Systems, Metropolitan Autonomous University–Campus Xochimilco (UAM-X), Mexico City, Mexico
Daniela Rodríguez, Department of Biological Systems, Metropolitan Autonomous University–Campus Xochimilco (UAM-X), Mexico City, Mexico
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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.
Paracetamol, HPMC, Maltodextrin, Granulation
To cite this article
Development of Co-processed Paracetamol with Hydroxypropyl Methylcellulose (HPMC) and Maltodextrin by Wet Granulation Process, Journal of Drug Design and Medicinal Chemistry.
Vol. 5, No. 2,
2019, pp. 26-32.
Copyright © 2019 Authors retain the copyright of this article.
This article is an open access article distributed under the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/
) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
FEUM, F. d. (2018). Paracetamol (12th ed., Vol. 1). of Mexico: Secretary of Health.
Isabel González Álvarez, M. Á. (2015). Biopharmaceutical methodologies in the development of medicines (08-06-15 ed.). Miguel Hernández University of Elche.
Herazo, EA (2012). Physicochemical study of the solubility of acetaminophen in polyethylene glycol 400 + water mixtures. Thesis, Bogotá.
Domínguez-Gil, AM (2011). Royal National Academy of Pharmacy; Advances in pharmaceutical technology. Retrieved March 29, 2018 from http://www.analesranf.com/index.php/mono/article/view/532/550.
Varona S, Fernández J, Rossmann M and Braeuer A (2013). Solubility of Paracetamol and Polyvinylpyrrolidone in Mixtures of Carbon Dioxide, Ethanol, and Acetone at Elevated Pressures. American Chemical Society. 58, 1054-1061.
Ruether F and Sadowski G (2009). Modeling the Solubility of Pharmaceuticals in Pure Solvents and Solvent Mixtures for Drug Process Design. Wiley InterScience. DOI 10.1002 / jps.21725.
Espada García JI, Fernandes Tavares DF, Fraguas Sánchez AI, Aparicio Blanco J, Martín Sabroso C, Torres Suárez AI (2015). Masking of flavors in solid oral dosage forms. Annals of the Royal Academy of Pharmacy (1697-4298), 116-128.
IPEC, TI (2006). The Join IPEC- PQG Good Manufacturing Practices Guide for pharmaceutical excipients.
Acofarma (nd) Tokens of technical information. Maltodextrin Retrieved March 29, 2018 from http://www.acofarma.com/admin/uploads/descarga/6596-65aa65d75536417fb925977904912902b92d2316/main/files/Maltodextrina.pdf.
López, OM (2006). Influence of the use of additives on the performance of the spray drying process of aqueous extract of Calendula officinalis L. Cuban Journal of Medicinal Plants.
Acofarma (nd) Hydroxypropyl Methyl Cellulose. Retrieved August 31, 2017 from http://www.acofarma.com/admin/uploads/descarga/4373-47a1ee7b1d50cddacc89770a35df329dd1da0fdc/main/files/Hidroxipropil_metil_celulosa.pdf.
Villafuerte, L. (2011). The excipients and their functionality in solid pharmaceutical products. Scielo, 42 (1), 18-36.
Chiappetta DA, Rodríguez Llimós AC, Witte NL, Széliga ME, Niselman V and Bregni C (2004). Enmascaramiento de Sabor de Paracetamol Utilizando Microencapsulación. Acta Farm. Bonaerense 23 (3): 292-6.
Minakshi Marwaha, DS (2010). Coprocessing of Excipients: A Review on Excipient Development For Improved Tabletting Performance. International Journal of Applied Pharmaceutics, 2 (3), 41-47.
Afrasiabi Garekani H, Sadeghi F and Ghazi A (2003). Increasing the Aqueous Solubility of Acetaminophen in the Presence of Polyvinylpyrrolidone and Investigation of the Mechanisms Involved, Drug Development and Industrial Pharmacy, 29: 2, 173-179, DOI: 10.1081/DDC-120016725.