Screening de formas polimórficas e desenvolvimento de comprimidos de betametasona e maleato de dexclorfeniramina

Abstract

Solid-state drugs, including betamethasone and dexchlorpheniramine maleate, may present a phenomenon called polymorphism, capable of altering important physico- chemical and pharmaceutical properties. Not all Active Pharmaceutical Inputs (APIs) entered the market have been identified and characterized as polymorphic forms. Many drugs were also produced without studies that ensure chemical and physical compatibility between their active and pharmaceutical excipients. The objective of this study was to screen for possible polymorphic forms of the drugs betamethasone and dexchlorpheniramine maleate, as well as to develop a compatibility study between these APIs and pharmaceutical excipients used in solid forms to obtain and characterize tablets optimized through this process. Compatibility studies with APIs and excipients used in solid dosage forms were performed using thermoanalytical techniques, FTIR and XRD. The crystals of the APIs used to search for polymorphic forms were obtained by the technique of slow evaporation of the solvent from a saturated solution, the samples obtained were characterized by Differential Scanning Calorimetry, X -Ray Diffraction, Fourier Transform Infrared Spectroscopy, Scanning Electron Microscopy and Optical Microscopy. The development of the compatibility study made it possible to obtain a formulation suitable for the direct compression production of dexchlorpheniramine maleate and betamethasone tablets, containing as pharmaceutical excipients, microcrystalline cellulose 102, croscamelose sodium, colloidal silicon dioxide and talc. The batch of tablets obtained had a mean weight of 196.03 mg, average hardness of 37.65 N, friability of 0.30% and mean disintegration time of 15.01 seconds. Screening of possible polymorphic forms indicated evidence of polymorphism in the two APIs.