Abstract
Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.
Highlights
The poor dissolution rate of water-insoluble drugs confronts a major obstacle in the development of pharmaceutical dosage forms
Application of the mathematical model for designing the liquisolid systems The formulation design of liquisolid systems was done in accordance with new mathematical model described by Spireas et al In this study, PEG 400, microcrystalline cellulose (Avicel® PH 102MCC), and Aerosil® 200 were used as a liquid vehicle, carrier and coating materials respectively
The solubility of furosemide in different media is presented in table 2
Summary
The poor dissolution rate of water-insoluble drugs confronts a major obstacle in the development of pharmaceutical dosage forms. The drugs which are poorly water soluble will be released at a slow rate owing to their limited solubility within gastrointestinal tract [1]. The various properties of drug-like solubility, particle size, polymorphism, salt form, complexation, wettability affect drug dissolution and its rate and can be targeted to enhance dissolution of poorly water-soluble drugs [3]. Some commonly used physical modifications to enhance the dissolution of API includes: (a) Reducing particle size to increase surface area, increasing dissolution rate of drug, (b) solubilization in surfactant systems, (c) formation of water-soluble complexes, (d) drug derivatization such as a strong electrolyte salt form that usually has higher dissolution rate, and (e) manipulation of solid state of drug substance to improve drug dissolution, i.e., by decreasing crystallinity of drug substance through formation of solid solutions [4]. Liquisolid compacts promote dissolution rate of water-insoluble drugs to a greater extent and enhances the drug flow property [5]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
