Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems

Indian Journal of Pharmaceutical Sciences

Volumn 75, Issue 3, 2013, Pages 291-301

  Koh, P ^a   Chuah, J ^a   Talekar, Meghna ^b   Gorajana, A ^b   Garg, S ^b  

^a INTERNATIONAL MEDICAL UNIVERSITY   (Malaysia)

^b UNIVERSITY OF AUCKLAND   (New Zealand)

Author keywords

dissolution enhancement; efavirenz; polyethylene glycol; PVP K30; Solid dispersion; Tween 80

Indexed keywords

EFAVIRENZ; MACROGOL 8000; POLYSORBATE 80; POVIDONE;

ARTICLE; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; INFRARED SPECTROSCOPY; PHYSICAL CHEMISTRY; SCANNING ELECTRON MICROSCOPY; X RAY DIFFRACTION; X RAY POWDER DIFFRACTION;

EID: 84883696949     PISSN: 0250474X     EISSN: 19983743     Source Type: Journal    
DOI: 10.4103/0250-474X.117434     Document Type: Article

References (37)

1. Rinaki E, Valsami G, Macheras P. Quantitative biopharmaceutics classification system: The central role of dose/solubility ratio. Pharm Res 2003;20:1917-25. (Pubitemid 38005521)
2. Iqbal Z, Babar A, Ashraf M. Controlled-release naproxen using micronized ethyl cellulose by wet-granulation and solid-dispersion method. Drug Dev Ind Pharm 2002;28:129-34. (Pubitemid 34218776)
3. Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci 1971;60:1281-302.
4. Law D, Wang W, Schmitt EA, Qiu Y, Krill SL, Fort JJ. Properties of rapidly dissolving eutectic mixtures of poly (ethylene glycol) and fenofibrate: The eutectic microstructure. J Pharm Sci 2003;92:505-15. (Pubitemid 36258965)
5. Biswal S, Sahoo J, Murthy PN. Characterisation of gliclazide-PEG 8000 solid dispersions. Trop J Pharm Res 2009;8:417-24.
6. Serajuddin AT. Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs. J Pharm Sci 1999;88:1058-66.
7. Dhirendra K, Lewis S, Udupa N, Atin K. Solid dispersions: A review. Pak J Pharm Sci 2009;22:234-46.
8. Chaulang G, Patel P, Hardikar S, Kelkar M, Bhosale A, Bhise S. Formulation and evaluation of solid dispersions of furosemide in sodium starch glycolate. Trop J Pharm Res 2009;8:43-51.
9. Dhanaraju MD, Enose Arno A, Sundarseelan, Prasanna PM, Krishnan RK. A study of solid dispersion of griseofulvin with polyethylene glycol 6000: Polysorbate 80 mixture. Indian Drugs 2001;38: 633-637. (Pubitemid 34070712)
10. Franco M, Trapani G, Latrofa A, Tullio C, Provenzano Mr, Serra M, et al. Dissolution properties and anticonvulsant activity of phenytoin-polyethylene glycol 6000 and polyvinylpyrrolidone K-30 solid dispersions. Int J Pharm 2001;225:63-73. (Pubitemid 32728200)
11. Jain SK, Shukla M, Shrivastava V. Development and in vitro evaluation of ibuprofen mouth dissolving tablets using solid dispersion technique. Chem Pharm Bull 2010;58:1037-42.
12. Najmuddin M, Khan T, Mohsin AA, Shelar S, Patel V. Enhancement of dissolution rate of ketoconazole by solid dispersion technique. Int J Pharm Pharm Sci 2010;2:132-6.
13. Csajka C, Marzolini C, Fattinger K, Dacosterd LA, Fellay J, Telenti A, et al. Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection. Clin Pharmacol Ther 2003;73:20-30. (Pubitemid 36158483)
14. Chiappetta DA, Hocht C, Taira C, Sosnik A. Efavirenz-loaded polymeric micelles for pediatric anti-HIV pharmacotherapy with significantly higher oral bioavailaibility. Nanomedicine 2010;5:11-23.
15. Craig DQ. Polyethylene glycols and drug release. Drug Dev Ind Pharm 1990;16:2501-26.
16. Van Den Mooter G, Augustijns P, Blaton N, Kinget R. Physico-chemical characterization of solid dispersions of temazepam with polyethylene glycol 6000 and PVP K30. Int J Pharm 1998;164:67-80. (Pubitemid 28160099)
17. Okonogi S, Puttipipatkhachorn S. Dissolution improvement of high drug-loaded solid dispersion. AAPS Pharm Sci Tech 2006;7:E148-53.
18. Khan CA, Rhodes CT. The concept of dissolution efficiency. J Pharm Pharmacol 1975;27:48-9.
19. Shah J, Vasanti S, Anroop B, Vyas H. Enhancement of dissolution rate of valdecoxib by solid dispersions technique with PVP K 30 and PEG 4000: Preparation and in vitro evaluation. J Incl Phenom Macrocycl Chem 2009;63:69-75.
20. Indrajit S, Banerjee S, Ramchandran AV, Geckeler KE, Murthy CN. Synthesis of cyclodextrin and sugar-based oligomers for the efavirenz drug delivery. Macromol Symp 2010;287:51-9.
21. Khattab IS, Nada A, Zaghloul AA. Physicochemical characterization of gliclazidemacrogol solid dispersion and tablets based on optimized dispersion. Drug Dev Ind Pharm 2010;36:893-902.
22. Patel RP, Patel DJ, Bhimani DB, Patel JK. Physicochemical characterization and dissolution study of solid dispersions of furosemide with polyethylene glycol 6000 and polyvinylpyrrolidone k30. Dissolut Technol 2008;15:17-25.
23. Patel RP, Patel MM. Physicochemical characterization and dissolution study of solid dispersions of lovastatin with polyethylene glycol 4000 and polyvinylpyrrolidone K30. Pharm Dev Tech 2007;12:21-33. (Pubitemid 46902607)
24. 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. (Pubitemid 38293005)
25. Mura P, Moyano JR, González-Rodríguez ML, Rabasco-Alvaréz AM, Cirri M, Maestrelli F. Characterization and dissolution properties of ketoprofen in binary and ternary solid dispersions with polyethylene glycol and surfactants. Drug Dev Ind Pharm 2005;31:425-34. (Pubitemid 41289155)
26. Ford JL. The current status of solid dispersions. Pharm Acta Helv 1986;61:69-88. (Pubitemid 16134014)
27. Akbuga J, Gursoy A, Kendi E. The preparation and stability of fast release furosemide-PVP solid dispersion. Drug Dev Ind Pharm 1988;14:1439-64.
28. Park YJ, Ryu DS, Li DX, Quan QZ, Oh DH, Kim JO, et al. Physicochemical characterization of tacrolimus-loaded solid dispersion with sodium carboxylmethyl cellulose and sodium lauryl sulfate. Arch Pharm Res 2009;32:893-8.
29. Joe JH, Lee WM, Park YJ, Joe KH, Oh DH, SeoYG, et al. Effect of the solid-dispersion method on the solubility and crystalline property of tacrolimus. Int J Pharm 2010;395:161-6.
30. Rama Rao N, Chowdary KP. Improvement of dissolution rate and bioavailability of piroxicam with pregelatinized starch. Indian J Pharm Sci 2001;63:36-40. (Pubitemid 33700290)
31. Rawat S, Jain SK. Solubility enhancement of celecoxib using β-cyclodextrin inclusion complexes. Eur J Pharm Biopharm 2004;57:263-7. (Pubitemid 38283702)
32. Morris KR, Knipp GT, Serajuddin AT. Structural properties of polyethylene glycol-polysorbate 80 mixture, a solid dispersion vehicle. J Pharm Sci 1992;81:1185-8. (Pubitemid 23018125)
33. Taylor LS, Zografi G. Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions. Pharm Res 1997;14:1691-8. (Pubitemid 28062912)
34. Martínez Ohárriz MC, Rodríguez-Espinosa C, Martín C, Goñi MM, Trosilarduya MC, Sánchez M. Solid dispersions of diflunisal-PVP: Polymorphic and amorphous states of the drug. Drug Dev Ind Pharm 2002;28:717-25. (Pubitemid 34809572)
35. El-Hinnawi MA, Najib NM. Ibuprofen-polyvinylpyrrolidone dispersions. Proton nuclear magnetic resonance and infrared studies. Int J Pharm 1987;37:175-7. (Pubitemid 17084964)
36. Zheng Y, Eli W, Li G. FTIR study of tween80/1-butyl-3-methylimidazolium hexafluorophosphate/toluene microemulsions. Colloid Polym Sci 2009;287:871-6.
37. Talari R, Varshosaz J, Mostafavi SA, Nokhodchi A. Dissolution enhancement of gliclazide using pH change approach in presence of twelve stabilizers with various physico-chemical properties. J Pharm Pharm Sci 2009;12:250-65