Evaluation of physicochemical properties and dissolution studies on quality control of low water solubility drugs (raw materials and pharmaceutical formulations)

• Published in: Revista colombiana de ciencias químico-farmacéuticas Vol. 49; no. 2
• Main Authors: Da Silva Ferreira, Matheus, De Carvalho Teles Júnior, Gilmar Antônio, Ramos Carvalho Júnior, Carlos Magno, De Souza Dias, Fernanda, Dias dos Santos Júnior, Wilson Saback, Oliveira da Guarda Souza, Marluce, De Freitas Santos Júnior, Aníbal
• Format: Journal Article
• Language: English; Portuguese
• Published: Bogota Universidad Nacional de Colombia 01-08-2020
• Subjects: Crystal structure; Dissolution; Drug delivery systems; Drugs; Equivalence; Morphology; Pharmaceuticals; Quality control; Raw materials; Scanning electron microscopy; Solubility; Tablets; Thermogravimetry; X-ray diffraction
• ISSN: 0034-7418; 1909-6356
• DOI: 10.15446/rcciquifa.v49n2.89486

The purpose of this study was to evaluate physicochemical properties and dissolution studies of furosemide (FUR), hydrochlorothiazide (HCTZ) and nifedipine (NIF), low water solubility drugs, in raw materials and pharmaceutical formulations. Surface and physicochemical characterization techniques -scanning electronic microscopy (SEM), thermogravimetry (TG), X-ray diffraction (XRD) and infrared (IR) spectrometry- as well as physical and physicochemical tests on tablets and capsules were applied as supporting information on drug quality control. Simple, rapid, and efficient UV-Vis methods were developed and validated for the determination of FUR, HCTZ and NIF samples. SEM exhibited considerable differences in the crystal morphological structures. Among the drugs studied, except for furosemide, more than one polymorph was present in the samples. Drug release profiles were satisfactory for all products. FUR and HCTZ tablets exhibited similar dissolution profiles, with very rapid release to the pharmaceutical specialties (reference, similar and generic). For HCTZ tablets, the similar drug (f2= 48.74) is not equivalent to the reference drug. NIF capsules (reference and compounded) showed a release ≥80% of stated on product labels, in 10 minutes. The results obtained in this study suggest that the quality parameters and drug dissolution profiles may have been influenced by the morphology and size of the crystals, excipients, and technological processes.