Design, optimization, preparation and evaluation of dispersion granules of valsartan and formulation into tablets

Current Drug Delivery

Volumn 6, Issue 1, 2009, Pages 28-37

  Shrivastava, Agnivesh R ^a   Ursekar, Bhalchandra ^a   Kapadia, Chhanda J ^a  

^a BOMBAY COLLEGE OF PHARMACY   (India)

Author keywords

Dispersion granules; Dissolution; Flow properties; Optimization; Solid dispersion; Valsartan

Indexed keywords

ADSORBENT; AEROPERL 300; AEROSIL; EXCIPIENT; GELUCIRE; MICROCRYSTALLINE CELLULOSE; UNCLASSIFIED DRUG; VALSARTAN;

ADSORPTION KINETICS; ARTICLE; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG DESIGN; DRUG GRANULE; DRUG SCREENING; DRUG SOLUBILITY; DRUG SYNTHESIS; INFRARED SPECTROSCOPY; PRIORITY JOURNAL; SCANNING ELECTRON MICROSCOPY; TABLET COMPRESSION; TABLET FORMULATION; X RAY POWDER DIFFRACTION;

CALORIMETRY, DIFFERENTIAL SCANNING; CHEMISTRY, PHARMACEUTICAL; DRUG STABILITY; MODELS, STATISTICAL; SOLUBILITY; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; TABLETS; TECHNOLOGY, PHARMACEUTICAL; TETRAZOLES; VALINE; X-RAY DIFFRACTION;

EID: 61849159945     PISSN: 15672018     EISSN: None     Source Type: Journal    
DOI: 10.2174/156720109787048258     Document Type: Article

References (34)

1. Criscione, L.; Gasparo, M. D.; Buehlmayer, P.; Whitebread, S.; Ramjoue, H.P.; Wood J.M. Pharmacological profile of valsartan: a potent, orally active, nonpeptide antagonist of the angiotensin II AT1-receptor subtype. Br. J. Pharmacol., 1993, 110, 761-71.
2. Dina, R.; Jafari, M. Angiotensin-II receptor antagonists: an overview. Am. J. Health Syst. Pharm., 2000, 57, 1231-41.
3. Lobenberg, R.; Amidon, G. L. Modern bioavailability, bioequivalence and biopharmaceutics classification system: new scientific approaches to international regulatory standards. Eur. J. Pharm. Biopharm., 2000, 50, 3-12.
4. Brunella, C.; Clelia, D. M.; Maria, I., A. Improvement of solubility and stability of valsartan by hydroxypropyl-beta-cyclodextrin. J. Incl. Phenom. Macrocycl. Chem., 2006, 54, 289-94.
5. Loftsson, T.; Brewster, M.E.; Masson, M. Role of cyclodextrins in improving oral drug delivery. Am. J. Drug Deliv., 2004, 2, 261-75.
6. Gohel, M.C.; Patel, L.D. Processing of nimesulide-PEG 400-PG-PVP solid dispersions: preparation, characterization and in vitro dissolution. Drug. Dev. Ind. Pharm., 2005, 29, 299-310.
7. Carlota, O.; Rangel,Y.; Adalberto, P.; Leoberto, C.T. Micellar solubilization of drugs. J. Pharm. Pharmaceut. Sci., 2005, 8, 147-63.
8. Gupta, U.; Agashe, H.B.; Asthana, A.; Jain, N. K. Dendrimers: novel polymeric nanoarchitectures for solubility enhancement. Biomacromolecules, 2006, 7, 649-58.
9. Hong, J.Y.; Kim, J.K.; Song, Y.K.; Park, J.S.; Kim, C.K. A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption. J. Control. Release, 2006, 110, 332-8.
10. Chauhan, B.; Shimpi, S.; Paradkar, A. Preparation and characterization of etoricoxib solid dispersions using lipid carriers by spray drying technique. AAPS PharmSciTech., 2005, 6, E405-E412.
11. Troy, P.; Jason, M. V.; True, L. R.; Xiaoxia, C.; Kirk, A. O.; Prapasri, S.; Jiahui, H.; Jason, T. M.; Keith, P. J.; Williams III, R.O. Cryogenic liquids, nanoparticles, and microencapsulation. Int. J. Pharm., 2006, 324, 43-50.
12. Banerjee, R.; Chakraborty, H.; Sarkar, M. Host-Guest complexation of oxicam NSAIDs with β-cyclodextrin. Biopolymers, 2004, 75, 355-65.
13. Bastin, R. J.; Bowker, M. J.; Slater, B. J. Salt selection and optimization procedures for pharmaceutical new chemical entities. Org. Process Res. Dev., 2000, 4, 427-35.
14. Chiou, W.L.; Riegelman, S. Pharmaceutical applications of solid dispersion systems. J. Pharm. Sci., 1971, 60, 1281-302.
15. Ford, J.L. The current status of solid dispersions. Pharm. Acta Helv., 1986, 61, 69-88.
16. Ambike, A.A.; Mahadik, K.R.; Paradkar, A. Stability study of amorphous valdecoxib. Int. J. Pharm., 2004, 282, 151-62.
17. Doshi, D.H.; Ravis, W.R.; Betageri, G.V. Carbamazepine and polyethylene glycol solid dispersion preparation, in vitro dissolution, and characterization. Drug. Dev. Ind. Pharm., 1967, 23, 1167-76.
18. Takeuchi, H.; Nagira, S.; Yamamoto, H.; Kawashima, Y. Solid dispersion particles of tolbutamide prepared with fine silica particles by the spray-drying method. Powder Technol., 2004, 141, 187-95.
19. Damian. F.; Blaton, N.; Naesens, L.; Balzarini, J.; Kinget, R.; Augustijns, P.; Vanden M.G. Physicochemical characterization of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14. Eur. J. Pharm. Sci., 2000, 10, 311-22.
20. Fattah, A.A.M.; Bhargava, H.N. Preparation and in vitro evaluation of solid dispersions of halofantrine. Int. J. Pharm., 2002, 235, 17-33.
21. Gupta, M.K.; Goldman, D.; Bogner, R.H.; Tseng, Y.C. Enhanced drug dissolution and bulk properties of solid dispersions granulated with a surface adsorbent. Pharm. Dev. Technol., 2001, 6, 563-72.
22. Gupta, M.K.; Bogner, R.H.; Goldman, D.; Tseng, Y.C. Mechanism for further enhancement in drug dissolution from solid-dispersion granules upon storage. Pharm. Dev. Technol., 2002, 7, 103-12.
23. Hu, J.; Rogers, T.L.; Brown, J.; Young, T.; Johnston, K.P.; Williams, R.O. III. Improvement of dissolution rates of poorly water soluble APIs using novel spray freezing into liquid technology. Pharm. Res., 2002, 19, 1278-84.
24. Fini, A.; Rodriguez, C.; Cavallari, C.; Albertini, B.; Passerini, N. Ultrasound-compacted and spray-congealed indomethacin/polyethyleneglycol systems. Int. J. Pharm., 2002, 247, 11-22.
25. Brietenbach, J.; Berndl, G.; Neumann, J.; Rosenberg, J.; Simon, D.; Zeidler, J. Solid dispersion by integrated melt extrusion system. Proc. Control. Release Soc., 1998, 25, 804-5.
26. Sethia, S.; Squillante, E. Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods. Int. J. Pharm., 2004, 272, 1-10.
27. Passerini, N.; Perissutti, B.; Moneghini, M.; Voinovich, D.; Albertini, B.; Cavallari, C.; Rodriguez, L. Characterization of cabamazepine-Gelucire 50/13 microparticles prepared by a spraycongealing process using ultrasounds. J. Pharm. Sci., 2002, 91, 699-707.
28. Serajuddin, A.T.M. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J. Pharm. Sci., 1999, 88, 1058-66.
29. Gupta, M.K.; Tseng, Y.C.; Goldman, D.; Bogner, R.H. Hydrogen bonding with adsorbent during storage governs drug dissolution from solid-dispersion granules. Pharm. Res., 2002, 19, 1663-72.
30. th ed., Marcel Dekker; New York, 2002, Vol. 121, pp. 607-26.
31. Akhgari, A.; Afrasiabi, G. H.; Sadeghi, F.; Azimaie, M. Statistical optimization of indomethacin pellets coated with pH-dependent methacrylic polymers for possible colonic drug delivery. Int. J. Pharm., 2005, 305, 22-30.
32. McKenna, A.; McCafferty, D.F. Effect of particle size on the compaction mechanism and tensile strength of tablets. J. Pharm. Pharmacol., 1982, 34, 347-51.
33. Chuang, I. S.; Maciel, G. E. Probing hydrogen bonding and the local environment of silanols on silica surfaces via nuclear spin cross polarization dynamics. J. Am. Chem. Soc., 1996, 118, 401-6.
34. Chuang, I. S.; Maciel, G. E. A detailed model of local structure and silanol hydrogen bonding of silica gel surfaces. J. Phys. Chem. B., 1997, 101, 3052-64.