Formulation and Evaluation of Floating Microspheres of Ranolazine for the Treatment of Chronic Angina
DOI:
https://doi.org/10.37285/ijpsn.2013.6.3.5Abstract
Ranolazine is indicated for the treatment of chronic angina alone or in combination with other cardiovascular agents. The objective of present investigation was to formulate floating microspheres of ranolazine to increase gastric residence time, increased bioavailability and reduce dose frequency of drug therapy. Novel o/w emulsion solvent diffusion technique was used for preparation of microspheres of ranolazine by using various polymers such as HPMC (hydroxyl propyl methyl cellulose), ethyl cellulose and Eudragit L 100. Entrapment efficiency of drug was up to 80.16%. Eudragit L100 based microspheres were found to be hollow cavity, spherical and porous nature from the results of scanning electron microscopy. Micromeritic profile of these microspheres was found satisfactory. From the results of FTIR spectroscopy it was revealed that there was no drug--polymer interaction. Eudragit L100 based microspheres shows good in vitro buoyancy and sustained release profile for longer period of time (> 14 hours), suggesting the viability of floating microspheres of ranolazine for improved pharmacokinetics for treatment of chronic angina.
Downloads
Metrics
Keywords:
Ethyl cellulose, Ranolazine, Microspheres, Eudragit L100, HPMCDownloads
Published
How to Cite
Issue
Section
References
Chien YE (1993). New approaches in oral controlled release drug delivery system. Drug Dev Ind Pharm. 9: 486-488.
Curatolo WJ and Lo J (1995). Gastric retention system for controlled drug release. US Patent 5: 443,843.
Ichikawa M, Watanabe S and Miyake YA (1991). New multiple– unit oral floating dosage system, I: preparation and in vitro evaluation of floating and sustained–release characteristics. J Pharm Sci. 80: 1062-6.
Kumar SA, Narayanrao RD and Saurabh W (2005). Floating microspheres of cimetidine: Formulation characterization and in vitro evaluation. Acta Pharm 55: 277–285.
Lachman L, Liberman AH and Kanig LJ (1991).Text book of the theory and practice of industrial pharmacy, 3rd Edn. Mumbai, Varghese Publication House pp.317-324.
Lee JH, Park TG and Choi HK (1999). Development of oral drug delivery system using floating microspheres. J Microencapsul 16: 715-729.
Ramachandran S, Shaheedha S.M, Thirumurugan G and Dhanaraju MD (2010). Floating controlled drug delivery system of famotidine loaded hollow microspheres (microballoons) in the stomach. Current Drug Del. 7: 93-97.
Sanjay SP, Ray S and Thakur RS (2006). Formualtion and Evaluation of Floating Drug Delivery System containing Clarithromycin for Helicobacter Pylori. Acta Poloniae Pharmaceutica - Drug Research 63(1): 53-61.
Sheth PR and Tossounian J (1984). The hydrodynamicaly balanced system: A novel drug delivery system for oral use. Drug Dev Ind Pharm 10: 313-339.
Shweta A, Javed A, Alka A, Roop KK and Sanjula B (2005). Floating Drug Delivery Systems: A Review. AAPS PharmSciTech 6(3): 372-390.
Woo BH, Jiang G, Jo YW and DeLuca PP (2001). Preparation and characterization of a composite PLGA and poly (acryloyl hydroxymethyl starch) microsphere system for protein delivery. Pharm Res. 18: 1600‐1606.
Yasunori S, Yoshiaki K, Hirofumi T and Hiromitsu Y (2004). In vitro evaluation of floating and drug releasing behaviors of hollow microspheres (microballoons) prepared by the emulsion solvent diffusion method. Eur J Pharmaceutics and Biopharmaceutics 57: 235–243.