Dissolution improvement of four poorly water soluble drugs by cogrinding with commonly used excipients

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 68, Issue 2, 2008, Pages 330-337

  Vogt, Markus ^a,b   Kunath, Klaus ^b   Dressman, Jennifer B ^a  

^a GOETHE UNIVERSITY   (Germany)

^b MERCK KGAA   (Germany)

Author keywords

Albendazole; Cogrinding; Danazol; Dissolution rate enhancement; Felodipine; Jet milling; Particle size reduction; Poorly soluble drugs; Solubility; Supersaturation

Indexed keywords

5 [1 (3,4 DIMETHOXYBENZOYL) 1,2,3,4 TETRAHYDRO 6 QUINOLYL] 3,6 DIHYDRO 6 METHYL 2H 1,3,4 THIADIAZIN 2 ONE; ALBENDAZOLE; DANAZOL; DODECYL SULFATE SODIUM; EXCIPIENT; FELODIPINE; HYDROXYPROPYLMETHYLCELLULOSE; LACTOSE; POVIDONE; STARCH;

ARTICLE; DIFFERENTIAL SCANNING CALORIMETRY; DRUG SOLUBILITY; SOLID STATE; X RAY DIFFRACTION;

CHROMATOGRAPHY, HIGH PRESSURE LIQUID; EXCIPIENTS; PARTICLE SIZE; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; WATER; X-RAY DIFFRACTION;

EID: 37849045222     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2007.05.009     Document Type: Article

References (30)

1. Lipinski C.A., Lombardo F., Dominy B.W., and Feeney P.J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 23 (1997) 3-25
2. Testa B., and Caldwell J. Prodrugs revisited: The "ad hoc" approach as a complement to ligand design. Med. Res. Rev. 16 (1996) 233-241
3. Hancock B.C., and Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J. Pharm. Sci. 86 (1997) 1-12
4. Grau M.J., Kayser O., and Müller R.H. Nanosuspensions of poorly soluble drugs - reproducibility of small scale production. Int. J. Pharm. 196 (2000) 155-157
5. Liversidge G.G., and Cundy K.C. Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: absolute oral bioavailability of nanocrystalline danazol in beagle dogs. Int. J. Pharm. 125 (1995) 91-97
6. Munoz A., Guichard J.P., and Reginault P. Micronised fenofibrate. Atherosclerosis 110 Suppl. (1994) S45-S48
7. Adkins J.C., and Faulds D. Micronised fenofibrate: a review of its pharmacodynamic properties and clinical efficacy in the management of dyslipidemia. Drugs 54 (1997) 615-633
8. Hargrove J.T., Maxson W.S., and Wentz A.C. Absorption of oral progesterone is influenced by vehicle and particle size. Am. J. Obstet. Gynecol. 161 (1989) 948-951
9. Englund D.E., and Johansson E.D. Oral versus vaginal absorption in oestradiol in postmenopausal women. Effects of different particle size. Ups. J. Med. Sci. 86 (1981) 297-307
10. Jounela A., Pentikainen P., and Sothmann A. Effect of particle size on the bioavailability of digoxin. Eur. J. Clin. Pharmacol. 8 (1975) 365-370
11. Atkinson R.M., Bedford C., Child K.J., and Tomich E.G. Effect of particle size on blood griseofulvin levels in man. Nature 193 (1962) 588-589
12. Kraml M., Dubuc J., and Gaudry R. Gastrointestinal absorption of griseofulvin: 2. influence of particle size in man. Antibiot. Chemother. 12 (1962) 239-242
13. Shakhtshneider T.P., Vasiltchenko M.A., Politov A.A., and Boldyrev V.V. The mechanochemical preparation of solid disperse systems of ibuprofen-polyethylene glycol. Int. J. Pharm. 130 (1996) 25-32
14. Sugimoto M., Okagaki T., Narisawa S., Koida Y., and Nakajima K. Improvement of dissolution characteristics and bioavailability of poorly water-soluble drugs by novel cogrinding method using water soluble-polymer. Int. J. Pharm. 160 (1998) 11-19
15. Taylor L.S., and Zografi G. Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersion. Pharm. Res. 14 (1997) 1691-1698
16. Doherty C., and York P. Accelerated stability of an X-ray amorphous furosemide-poly(vinylpyrrolidone) solid dispersion. Drug Dev. Ind. Pharm. 15 (1989) 1969-1987
17. Otsuka M., Ofusa T., and Matsuda Y. Dissolution improvement of water-insoluble glybuzole by co-grinding and co-melting with surfactants and their physicochemical properties. Colloids Surf. B: Biointerfaces 10 (1998) 217-226
18. Kubo H., Osawa T., Takashima K., and Mizobe M. 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 (1996) 741-747
19. 2+ sensitizing agent. Cardiovasc. Drug Rev. 14 (1996) 334-350
20. Barth H.G. Modern Methods of Particle Size Analysis (1984), John Wiley & Sons, New York
21. Moroi Y., Nishikido N., Uehara H., and Matuura R. An interrelationship between heat of micelle formation and critical micelle concentration. J. Colloid Interface Sci. 50 (1975) 254-264
22. Johnson I., Olofsson G., and Jönsson B. Micelle formation of ionic amphiphiles. Thermochemical test of a thermodynamic model. J. Chem. Soc., Faraday Trans. I 83 (1987) 3331-3344
23. Van Os N.M., Haak J.R., and Rupert L.A.M. Physico-Chemical Properties of Selected Anionic, Cationic and Non-ionic Surfactants (1993), Elsevier, Amsterdam
24. Schamp K., Schreder S.-A., and Dressman J. Development of an in vitro/in vivo correlation for lipid formulations of EMD 50733 [sic], a poorly soluble, lipophilic drug substance. Eur. J. Pharm. Biopharm. 26 (2006) 227-234
25. Sekikawa H., Nakano M., and Arita T. Inhibitory effect of polyvinylpyrrolidone on the crystallization of drugs. Chem. Pharm. Bull. 26 (1978) 118-126
26. Simonelli A.P., Mehta S.C., and Higuchi W.I. Inhibition of sulfathiazole crystal growth by polyvinylpyrrolidone. J. Pharm. Sci. 59 (1970) 633-638
27. Ziller K.H., and Rupprecht H. Control of crystal growth in drug suspensions. Drug Dev. Ind. Pharm. 14 (1988) 2341-2370
28. Ibrahim H.G., Pisano E., and Bruno A. Polymorphism of phenylbutazone: properties and compressional behavior of crystals. J. Pharm. Sci. 66 (1977) 669-673
29. Bakatselou V., Oppenheim R.C., and Dressman J.B. Solubilization and wetting effects of bile salts on the dissolution of steroids. Pharm. Res. 8 (1991) 1461-1469
30. Anderberg E.K., Bisrat M., and Nyström C. Physicochemical aspects of drug release, VII: the effect of surfactant concentration and drug particle size on solubility and dissolution rate of felodipine, a sparingly soluble drug. Int. J. Pharm. Sci. 47 (1988) 67-77