Solid state interaction of raloxifene HCl with different hydrophilic carriers during co-grinding and its effect on dissolution rate

Drug Development and Industrial Pharmacy

Volumn 35, Issue 4, 2009, Pages 455-470

  Garg, Anuj ^a   Singh, S ^a   Rao, V U ^b   Bindu, K ^b   Balasubramaniam, J ^b  

^a BANARAS HINDU UNIVERSITY   (India)

^b ISP Hong Kong Limited   (India)

Author keywords

Solid state characterization

Indexed keywords

ALGINIC ACID; HYDROXYPROPYLCELLULOSE; HYDROXYPROPYLMETHYLCELLULOSE; PHARMACOAT; POLYSORBATE 20; POVIDONE; RALOXIFENE; UNCLASSIFIED DRUG; CELLULOSE; DRUG CARRIER; DRUG DERIVATIVE; EXCIPIENT; GLUCURONIC ACID; HEXURONIC ACID; METHYLCELLULOSE; SELECTIVE ESTROGEN RECEPTOR MODULATOR;

ARTICLE; CONTROLLED STUDY; DRUG RELEASE; DRUG SOLUBILITY; MOLECULAR INTERACTION; PARTICLE SIZE; SOLID STATE; CHEMISTRY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG FORMULATION; DRUG INCOMPATIBILITY; DRUG STORAGE; INFRARED SPECTROSCOPY; SCANNING ELECTRON MICROSCOPY; SOLUBILITY; X RAY DIFFRACTION;

ALGINATES; CALORIMETRY, DIFFERENTIAL SCANNING; CELLULOSE; CHEMISTRY, PHARMACEUTICAL; DRUG CARRIERS; DRUG COMPOUNDING; DRUG INCOMPATIBILITY; DRUG STORAGE; EXCIPIENTS; GLUCURONIC ACID; HEXURONIC ACIDS; METHYLCELLULOSE; MICROSCOPY, ELECTRON, SCANNING; PARTICLE SIZE; POVIDONE; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATORS; SOLUBILITY; SPECTROSCOPY, FOURIER TRANSFORM INFRARED; X-RAY DIFFRACTION;

EID: 65749099276     PISSN: 03639045     EISSN: 15205762     Source Type: Journal    
DOI: 10.1080/03639040802438365     Document Type: Article

References (45)

1. Ahuja, N., Katare, O. P., & Singh, B. (2007). Studies on dissolution enhancement and mathematical modeling of drug release of poorly water-soluble drug using water soluble carriers. Eur. J. Pharm. Biopharm., 65, 26-38.
2. Akbuga, J., Gursoy, A., & Kendi, E. (1988). The preparation and stability of fast release furosemide-PVP solid dispersion. Drug Dev. Ind. Pharm., 14, 1439-1464. (Pubitemid 18189534)
3. Amidon, G. L., Lennernas, H., Shah, V. P., & Crison, J. R. A. (1995). A theoretical basis for a biopharmaceutical drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res., 12, 413-420.
4. Attama, A. A., & Mpamaugo, V. E. (2006). Pharmacodynamics of piroxicam from self emulsifying lipospheres formulated with homolipids extracted from Capra hircus. Drug Deliv., 13, 133-137.
5. Betageri, G. V., & Makarla, K. R. (1995). Enhancement of dissolution of glyburide by solid dispersion and lyophilization techniques. Int. J. Pharm., 126, 155-160.
6. Chaumeil, J. C. (1998). Micronization: A method of improving the bioavailability of poorly soluble drugs. Methods Find. Exp. Clin. Pharmacol., 20, 211-215.
7. Chee, S. N., Johansen, A. L., Gu, L., Karlsen, J., & Heng, P. W. S. (2005). Microwave drying of granules containing a moisture-sensitive drug: A promising alternative to fluid bed and hot air oven drying. Chem. Pharm. Bull., 53, 770-775.
8. Delmas, P. D., Bjarnason, N. H., Mitlak, B., Ravoux, A. C., Shah, A., Huster, W., Draper, M., & Christiansen, C. (1997). Effects of Raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. N. Engl. J. Med., 337, 1641-1647.
9. De Villiers, M. M., & Tiedt, L. R. (1996). An analysis of fine grinding and aggregation of poorly soluble drug powders in a vibrating ball mill. Pharmazie, 51, 564-567.
10. Etman, M. A., & Nada, A. H. (1999). Evaluation of simple and ball-mill ground mixtures of two NSAIDs with hydrophilic carriers. Alex. J. Pharm. Sci., 13, 135-140.
11. Florence, A. T., & Salole, E. G. (1976). Changes in crystallinity and solubility on comminution of digoxin and observations on spironolactone and oestradiol. J. Pharm. Pharmacol., 28(8), 637-642.
12. Ford, J. L. (1986). The current status of solid dispersions. Pharm. Acta Helv., 61, 69-88.
13. Friedrich, H., Nada, A., & Bodmeier, R. (2005). Solid state and dissolution rate characterization of co-ground mixtures of nifedipine and hydrophilic carriers. Drug Dev. Ind. Pharm., 31, 719-728.
14. Hancock, B. C., & Parks, M. (2000). What is true solubility advantage for amorphous pharmaceuticals? Pharm. Res., 17(4), 397-403.
15. Hancock, B. C., & Zografi, G. (1997). Characteristic and significance of the amorphous state in pharmaceutical systems. J. Pharm. Sci., 86, 1-12.
16. Hixson, A. W. & Crowell, J. H. (1931). Dependence of reaction velocity upon surface and agitation. Ind. Eng. Chem., 23, 923-993.
17. Khan, K. A. (1975). The concept of dissolution efficiency. J. Pharm. Pharmacol., 27, 48-49.
18. Kubo, H., Osawa, T., Takashima, K., & Mizobe, M. (1996). Enhancement of oral bioavailability and pharmacological effect of 1-(3,4-dimethoxyphenyl)- 2, 3-bis (methoxycarbonyl)-4-hydroxy-6,7,8-trimethoxynaphthalene (TA-7552), a new hypocholesterolemic agent, by micronization in co-ground mixture with D-mannitol. Biol. Pharm. Bull., 19(5), 741-747.
19. Lipinski, C. (2002). Poor aqueous solubility - An industry wide problem in drug discovery. Am. Pharm. Rev., 5, 82-85.
20. Liversidge, G. G. (1997). Formulation of oral gastrointestinal diagnostic X-ray contrast agents and oral gastrointestinal therapeutic agents. US Patent No. 5628981.
21. Liversidge, G. G., & Cundy, K. C. (1995). Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs. Int. J. Pharm., 125, 91-97.
22. Liversidge, G. G., Engers, D. A., Roberts, M. E., Ruddy, S. B., Wong, S., & Xu, S. (2000). Methods of making nanocrystalline formulations of human immunodeficiency virus (hiv) protease inhibitors using cellulosic surface stabilizers. US Patent No. 6068858.
23. Mitlak, B. H., & Cohen, F. J. (1997). In search of optimal long term female hormone replacement: The potential of selective estrogen receptor modulators. Horm. Res., 48, 155-163.
24. Mura, P., Cirri, M., Faucci, M. T., Ginès-Dorado, J. M., & Bettinetti, G. P. (2002). Investigation of the effects of grinding and co-grinding on physicochemical properties of glisentide. J. Pharm. Biomed. Anal., 30(2), 227-237.
25. Mura, P., Faucci, M. T., & Parrini, P. L. (2001). Effects of grinding with microcrystalline cellulose and cyclodextrins on ketoprofen physicochemical properties. Drug Dev. Ind. Pharm., 27(2), 119-128.
26. Mura, P., Zerrouk, N., Meennini, N., Maestrelli, F., & Chemtob, C. (2003). Development and characterization of naproxen-chitosan solid systems with improved drug dissolution properties. Eur. J. Pharm. Sci., 19, 67-75.
27. Nada, A. H. (1997). Evaluation of ball-mill ground mixtures of hydrophilic carriers and phenytoin. Alex. J. Pharm. Sci., 11, 29-33.
28. Nozawa, Y., Mizumoto, T., & Higashide, F. (1985). Roll mixing of formulation. Pharm. Acta Helv., 60, 175-177.
29. Nozawa, Y., Mizumoto, T., & Higashide, F. (1986). Improving dissolution rate of practically insoluble drug kitasamycin by forcibly roll mixing with additives. Pharm. Ind., 8, 967-969.
30. Otsuka, M., & Kaneniwa, N. (1984). Effects of grinding on the physicochemical properties of cephalexin. Chem. Pharm. Bull., 32, 1071-1079.
31. Parrott, E. L. (1987). Milling. In L. Lachman, H. A. Lieberman, & J. L. Kanig (Eds.), The theory and practice of industrial pharmacy (pp. 21-46). Bombay: Varghese Publishing House.
32. Rogers, T. L., Hu, J., Yu, Z., Johnston, K. P., & Williams III, R. O. (2002). A novel particle engineering technology: Spray freezing into liquid. Int. J. Pharm., 242, 93-100.
33. Sankalia, M. G., Mashru, R. C., Sankalia, J. M., & Sutariya, V. B. (2005). Papain entrapment in alginate beads for stability improvement and site-specific delivery: Physicochemical characterization and factorial optimization using neural network modeling. AAPS PharmSciTech., 6(2), E209-222.
34. Scott, T. J., & Roger, D. M. (2002). Environmental fate and chemistry of raloxifene hydrochloride. Environ. Toxicol. Chem., 21(4), 729-736.
35. Sugimoto, M., Okagaki, T., Narisawa, S., Koide, Y., & Nakajima, K. (1998). Improvement of dissolution characteristics and bioavailability of poorly water-soluble drugs by novel co-grinding method using water-soluble polymer. Int. J. Pharm., 160, 11-19.
36. Suzuki, H., Ogawa, M., Hironaka, K., Ito, K., & Sunada, H. (2001). A nifedipine co-ground mixture with sodium deoxycholate. I. Colloidal particle formation and solid state analysis. Drug Dev. Ind. Pharm., 27(9), 943-949.
37. Valizadeh, H., Nokhodchi, A., Qarakhani, N., Zakeri-Milani, P., Azarmi, S., Hassanzadeh, D., & Lobenberg, R. (2004). Physicochemical characterization of solid dispersions of indomethacin with PEG 6000, Myrj 52, lactose, sorbitol, dextrin, and Eudragit® E100. Drug Dev. Ind. Pharm., 30, 303-317.
38. Van Nijlen, T., Brennan, K., Van den Mooter, G., Blaton, N., Kinget, R., & Augustijns, P. (2003). Improvement of the dissolution rate of artemisinin by means of supercritical fluid technology and solid dispersion. Int. J. Pharm., 254(2), 173-181.
39. Veiga, F., Fernandes, C., & Maincent, P. (2001). Influence of the preparation method on the physicochemical properties of tolbutamide/cyclodextrin binary systems. Drug Dev. Ind. Pharm., 27, 523-532.
40. Vippangunta, S. R., Maul, K. A., Tallavajhala, S., & Grant, D. J. W. (2002). Solid state characterization of nifedipine solid dispersion. Int. J. Pharm., 236, 111-126.
41. Wempe, M. F., Wacher, V. J., Ruble, K. M., Ramsey, M. G., Edgar, K. J., Buchanan, N. L., & Buchanan, C. M. (2008). Pharmacokinetics of raloxifene in male Wistar-Hannover rats: Influence of complexation with hydroxybutenyl- beta-cyclodextrin. Int. J. Pharm., 346, 25-37.
42. Williams, A. C., Timmins, P., Lu, M., & Forbes, R. T. (2005). Disorder and dissolution enhancement: Deposition of ibuprofen on to insoluble polymers. Eur. J. Pharm. Sci., 26, 288-294.
43. Yamada, T., Saito, N., Anraku, M., Imai, T., & Otagiri, M. (2000). Physicochemical characterization of a new crystal form and improvements in the pharmaceutical properties of the poorly water-soluble antiosteoporosis drug 3,9-bis (N,N-dimethylcarbamoy-loxy)- 5H-benzofuro[3,2-c]quinoline-6- one (KCA-098) by solid dispersion with hydroxypropylcellulose. Pharm. Dev. Technol., 5(4), 443-454.
44. Yamamoto, K., Nakano, M., Arita, T., Takayama, Y., & Nakai, Y. (1976). Dissolution behavior and bioavailability of phenytoin from a ground mixture with microcrystalline cellulose. J. Pharm. Sci., 65(10), 1484-1488.
45. Zingone, G., & Rubessa, F. (1994). Release of carbamazepine from solid dispersions with polyvinylpyrrolidone/vinylacetate copolymer (Pvp/Va). STP Pharm. Sci., 4, 122-127.