Development of co-processed Paracetamol with ...
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Development of co-processed Paracetamol with Hydroxypropylmethyl cellulose (HPMC) and Maltodextrin by wet granulation process Leticia ORTEGA * 1 , Martín GOMEZ * 2 & Daniela RODRIGUEZ * 3 * Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana - Xochimilco lortegaa@correo.xoc.uam.mx 1 [email protected] 2 , [email protected] 3 INTRODUCTION RESULT The purpose of this work is to improve some of the important physicochemical properties to an active pharmaceutical ingredient (API) as the solubility in water of Paracetamol. To upgrade the physicochemical properties of API, two pharmaceutical excipients, HPMC and Maltodextrin were used, which help to improve the solubility and this also help the manufacturing process of a Pharmaceutical product. METHODOLOGY Different granules were manufactured applying a design of experiments matrix where the wet granulation was used, combining Paracetamol with the excipients to obtain a uniform particle size and subsequently assess the properties of interest. The solubility was evaluated using a method (Mexican Pharmacopoeia - FEUM) based on UV / VIS, the calibration curve is constructed only for the API in order to evaluate the granules and calculate the percentage of solubility of these. Table 1. Percentage of every excipient for the granulations preparation Scheme 2: Stages of the humid granulation process and paracetamol compression Favourable results were obtained for two of the seven manufactured granules, the granules F and G containing 25 g of Paracetamol, 1.5;1.75 g of HPMC, and 23.5 g; 23.25 of Maltodextrin has a solubility of 104.17% and 101. 48% respectively, demonstrating that the process by wet granulation is able to improve its solubility. This type of coprocessed granules also fulfills the function to mask the bitter taste of Paracetamol in an oral pharmaceutical form, as in the case of a syrup. The flavour was assessed by a panel with 20 people, the taste of the syrups that were made with the granules with better solubility was compared with the syrups containing only the API. Table 2. Paracetamol solubility from granulations in percentage, evaluated by UV-Vis method CONCLUSIONS It was improve some of the important rheological and solubility in water properties of Paracetamol. The granules F with better solubility was compared with the syrups containing only the API and it is shown that has improvements in the solubility of Paracetamol and can mask the unpleasant (bitter) taste of the active ingredient. Financial support and /or acknowledgments § Laboratory of excipients No. 112 in the Universidad Autónoma Metropolitana Campus Xochimilco. § Collaboration of Makymat S.A. of C. V.
Transcript of Development of co-processed Paracetamol with ...
Developmentofco-processedParacetamolwithHydroxypropylmethylcellulose(HPMC)andMaltodextrinbywetgranulationprocess
Leticia ORTEGA * 1, Martín GOMEZ * 2 & Daniela RODRIGUEZ * 3 * Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana - Xochimilco [email protected] [email protected], [email protected]
INTRODUCTION RESULT
The purpose of this work is to improve some of the importantphysicochemicalpropertiestoanactivepharmaceuticalingredient(API) as the solubility in water of Paracetamol. To upgrade thephysicochemicalpropertiesofAPI,twopharmaceuticalexcipients,HPMC and Maltodextrin were used, which help to improve thesolubility and this also help the manufacturing process of aPharmaceuticalproduct.
METHODOLOGY
Different granules were manufactured applying a design ofexperiments matrix where the wet granulation was used,combining Paracetamol with the excipients to obtain a uniformparticle size and subsequently assess the properties of interest.The solubility was evaluated using a method (MexicanPharmacopoeia-FEUM)basedonUV/VIS,thecalibrationcurveisconstructedonlyfortheAPIinorderto evaluatethegranulesandcalculatethepercentageofsolubilityofthese.
Table 1. Percentage of every excipient for the granulations preparation
Scheme 2: Stages of the humid granulation process and paracetamol compression
Favourable results were obtained for two of the sevenmanufacturedgranules,thegranulesFandGcontaining25gof Paracetamol, 1.5;1.75 g of HPMC, and 23.5 g; 23.25of Maltodextrin has a solubility of 104.17% and 101. 48%respectively, demonstrating that the process by wetgranulation is able to improve its solubility. This type ofcoprocessed granules also fulfills the function to mask thebittertasteofParacetamolinanoralpharmaceuticalform,asin the caseof a syrup. The flavourwas assessedby a panelwith20people,thetasteofthesyrupsthatweremadewiththe granules with better solubility was compared with thesyrupscontainingonlytheAPI.
Table 2. Paracetamol solubility from granulations in percentage, evaluated by UV-Vis method
CONCLUSIONS
Itwasimprovesomeoftheimportant rheologicalandsolubilityinwaterpropertiesofParacetamol.The granules F with better solubility was comparedwiththesyrupscontainingonlytheAPIanditisshownthathasimprovementsinthesolubilityofParacetamolandcanmasktheunpleasant(bitter)tasteoftheactiveingredient.
Financial support and /or acknowledgments
§ Laboratory of excipients No. 112 in the UniversidadAutónomaMetropolitanaCampusXochimilco.
§ CollaborationofMakymatS.A.ofC.V.
