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.
Highlights
Paracetamol (Figure 1a) is an analgesic and antipyretic drug widely used by the Mexican population for the control of mild or moderate pain
It is known that the pharmacological effect depends on the physicochemical characteristics of the active principle and one of the most important is the solubility; in the FEUM (Pharmacopoeia of the United Mexican States) specifies that Paracetamol is soluble in alcohol and methanol; soluble in acetone, hot water and in 1 N sodium hydroxide solution; almost insoluble in chloroform and diethyl ether [1]
Based on the literature and these results it is verified that the parameters established for each excipient used and the active pharmaceutical ingredient (API) (Paracetamol) meet the identity test established by FEUM [12]
Summary
Paracetamol (Figure 1a) is an analgesic and antipyretic drug widely used by the Mexican population for the control of mild or moderate pain. It is known that the pharmacological effect depends on the physicochemical characteristics of the active principle and one of the most important is the solubility; in the FEUM (Pharmacopoeia of the United Mexican States) specifies that Paracetamol is soluble in alcohol and methanol; soluble in acetone, hot water and in 1 N sodium hydroxide solution; almost insoluble in chloroform and diethyl ether [1]. The characteristics of the solute conditioning the solubility are the size and shape of the particle, the amorphous or crystalline state, the polymorphism, the density, the melting. Ortega Leticia et al.: Development of Co-processed Paracetamol with Hydroxypropyl Methylcellulose (HPMC) and Maltodextrin by Wet Granulation Process temperature (melting point) and the porosity rate among other properties of the solid phase. The solubility is conditioned by the solvent and its wetting capacity, in particular the surface tension between the water and the solute (paracetamol) is relevant [2]
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