Characterization and physical stability of spray dried solid dispersions of probucol and PVP-K30

Pharmaceutical Development and Technology

Volumn 13, Issue 5, 2008, Pages 375-386

  Thybo, Pia ^a   Pedersen, Betty L ^b   Hovgaard, Lars ^b   Holm, Rene ^c   Müllertz, Anette ^d  

^a Pharmaceutical Development   (Denmark)

^b NOVO NORDISK A S   (Denmark)

^c H LUNDBECK A S   (Denmark)

^d UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

Amorphous; Flow through dissolution; Probucol; Solid dispersion; Spray drying; Stability

Indexed keywords

POLYMER; POVIDONE; POVIDONE K30; PROBUCOL; UNCLASSIFIED DRUG;

AMORPHOUS STATE; ARTICLE; BRUNAUER EMMETT TELLER METHOD; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DRUG SOLUBILITY; IN VITRO STUDY; LASER DIFFRACTION; PARAMETER; PARTICLE SIZE; PHYSICAL CHEMISTRY; PREFORMULATION; PRIORITY JOURNAL; SCANNING ELECTRON MICROSCOPE; SOLID DISPERSION; SOLID STATE; SPECIFIC SURFACE AREA; SPRAY DRYING; STORAGE; TECHNIQUE; WETTABILITY; X RAY POWDER DIFFRACTION;

ANTICHOLESTEREMIC AGENTS; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; DRUG STABILITY; DRUG STORAGE; EXCIPIENTS; HUMIDITY; PARTICLE SIZE; POVIDONE; POWDERS; PROBUCOL; SOLUBILITY; WETTABILITY;

EID: 51949116318     PISSN: 10837450     EISSN: 10979867     Source Type: Journal    
DOI: 10.1080/10837450802244843     Document Type: Article

References (28)

1. Craig DQM, Royall PG, Kett VL, Hopton ML. The relevance of the amorphous state to pharmaceutical dosage forms: glassy drugs and freeze dried systems. Int. J. Pharm. 1999;179(2):179-207.
2. Hancock BC, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J. Pharm. Sci. 1997;86(1):1-12.
3. Yoshioka M, Hancock BC, Zografi G. Inhibition of indomethacin crystallization in poly(vinylpyrrolidone) coprecipitates. J. Pharm. Sci. 1995;84(8):983-986.
4. Ambike AA, Mahadik KR, Paradkar A. Stability study of amorphous valdecoxib. Int. J. Pharm. 2004;282(1-2):151-162.
5. Chokshi RJ, Zia H, Sandhu HK, Shah NH, Malick WA. Improving the dissolution rate of poorly water soluble drug by solid dispersion and solid solution - pros and cons. Drug Deliv. 2007;14(1):33-45.
6. Jung JY, Yoo SD, Lee SH, Kim KH, Yoon DS, Lee KH. Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique. Int. J. Pharm. 1999;187(2):209-218.
7. CDER/FDA. Guidance for industry. Dissolution testing of immediate release solid oral dosage forms. 1997; August: 1-11.
8. FIP guidelines for dissolution testing of solid oral products. Dissolution Technol. 1997;4(4):1371-1382.
9. Perng CY, Kearney AS, Palepu NR, Smith BR, Azzarano LM. Assessment of oral bioavailability enhancing approaches for SB-247083 using flow-through cell dissolution testing as one of the screens. Int. J. Pharm. 2003;250(1):147-156.
10. Sunesen VH, Pedersen BL, Kristensen HG, Mullertz A. In vivo in vitro correlations for a poorly soluble drug, danazol, using the flow-through dissolution method with biorelevant dissolution media. Eur. J. Pharm. Sci. 2005;24(4):305-313.
11. Bhattachar SN, Wesley JA, Fioritto A, Martin PJ, Babu SR. Dissolution testing of a poorly soluble compound using the flow-through cell dissolution apparatus. Int. J. Pharm. 2002;236(1-2):135-143.
12. Giunchedi P, Conte U, Chetoni P, Saettone MF. Pectin microspheres as ophthalmic carriers for piroxicam: evaluation in vitro and in vivo in albino rabbits. Eur. J. Pharm. Sci. 1999;9(1):1-7.
13. Emara LH, Badr RM, Abd Elbary A. Improving the dissolution and bioavailability of nifedipine using solid dispersions and solubilizers. Drug Dev. Ind. Pharm. 2002;28(7):795-807.
14. Broman E, Khoo C, Taylor LS. A comparison of alternative polymer excipients and processing methods for making solid dispersions of a poorly water soluble drug. Int. J. Pharm. 2001;222(1):139-151.
15. Pongpeerapat A, Higashi K, Tozuka Y, Moribe K, Yamamoto K. Molecular interaction among probucol/PVP/SDS multicomponent system investigated by solid-state NMR. Pharm. Res. 2006;23(11):2566-2574.
16. Yagi N, Terashima Y, Kenmotsu H, Sekikawa H, Takada M. Dissolution behavior of probucol from solid dispersion systems of probucol- polyvinylpyrrolidone. Chem. Pharm. Bull. 1996;44(1):241-244.
17. Gerber JJ, Caira MR, Lötter AP. Structures of two conformational polymorphs of the cholesterol-lowering drug probucol. J. Crystallogr. Spectrosc. Res. 1993;23(11):863-869.
18. Lehto VP, Tenho M, Vaha-Heikkila K, Harjunen P, Paallysaho M, Valissaari J, Niemela P, Jarvinen K. The comparison of seven different methods to quantify the amorphous content of spray dried lactose. Powder Technol. 2006;167(2):85-93.
19. Crison JR, Weiner ND, Amidon GL. Dissolution media for in vitro testing of water-insoluble drugs: Effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate. J. Pharm. Sci. 1997;86(3):384-388.
20. McPherson A. Crystallization of Biological Macromolecules. New York: CSHL Press: 1999.
21. Noory C, Tran N, Ouderkirk L, Shah V. Steps for development of a dissolution test for sparingly water-soluble drug products. Dissolution Technol. 2000;7(1):16-19.
22. Brown CK, Chokshi HP, Nickerson B, Reed RA, Rohrs BR, Shah PA. Dissolution testing of poorly soluble compounds. Pharm. Technol. 2004;Dec:56-65.
23. Langenbucher F, Benz D, Kurth W, Moller H, Otz M. Standardized flow-cell method as an alternative to existing pharmacopoeial dissolution testing. Pharm. Ind. 1989;51(11):1276-1281.
24. Leuner C, Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm. 2000;50(1):47-60.
25. Craig DQM. The mechanisms of drug release from solid dispersions in water-soluble polymers. Int. J. Pharm. 2002;231(2):131-144.
26. Karavas E, Ktistis G, Xenakis A, Georgarakis E. Miscibility behavior and formation mechanism of stabilized felodipine-polyvinylpyrrolidone amorphous solid dispersions. Drug Dev. Ind. Pharm. 2005;31(6):473-489.
27. Karavas E, Georgarakis E, Sigalas MP, Avgoustakis K, Bikiaris D. Investigation of the release mechanism of a sparingly water-soluble drug from solid dispersions in hydrophilic carriers based on physical state of drug, particle size distribution and drug-polymer interactions. Eur. J. Pharm. Biopharm. 2007;66(3):334-347.
28. Thybo P, Kristensen J, Hovgaard L. Characterization and physical stability of tolfenamic Acid-PVP K30 solid dispersions. Pharm. Dev. Technol. 2007;12(1):43-53.