RECENT APPROACHES OF SOLID DISPERSION: A NEW CONCEPT TOWARD ORAL BIOAVAILABILITY .
Â Solid dispersion (SD) has been a major advanced technology in overcoming dissolution and bioavailability problem of poorly soluble compounds. Formulation of SD in water-soluble carrier has becoming more researched over the past four decades for solubility and relative bioavailability enhancement. By reduction of the size of the drug particle to the minimum level which will enhance drug wettability and ultimately bioavailability will be definitely improved. This review article elaborates recent advanced technology and characterization of SDs and also discusses the problems and their solution for the development of better formulations.
2. Lipinski CA, Lombardo F., Dominyl BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev. 2001;46:3-26.
3. Pudipeddi M, Serajuddin AT. Trends in solubility of polymorphs. J Pharm Sci 2005;94:929-39.
4. Craig DQ. The mechanisms of drug release from solid dispersions in water-soluble polymers. Int J Pharm 2002;231:131-44.
5. Sekiguchi K, Obi N. Studies on absorption of eutectic mixture. I. A comparison of the behavior of eutectic mixture of sulfathiazole and that of ordinary sulfathiazole in man. Chem Pharm Bull 1961;9:866-72.
6. Okonogia S, Oguchib T, Yonemochi E, Puttipipatkhachorn S, Yamamoto K. Improved dissolution of of loxacin via solid dispersion. Int J Pharm 1997;156:175-80.
7. Vasconcelos T, Sarmento B, Costa P. SDs as strategy to improve oral bioavailability of poor water soluble drug. Drug Discovery Today 2007;12:1068-75.
8. Kohri N, Yamayoshi Y, Xin H, Iseki K, Sato N, Todo S, et al. Improving the oral bioavailability of albendazole in rabbits by the solid dispersion technique. J Pharm Pharmacol 1999;51:159-64.
9. Linn M, Collnot EM, Djuric D, Hempel K, Fabian E. SoluplusÂ® as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo. Eur J Pharm Sci 2012;45:336-43.
10. Damian F, Blaton N, Naesens L, Balzarini J, Kinget R, Augustijns P, et al. 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.
11. Jagdale S, Patil S, Kuchekar B, Chabukswar A. Preparation and characterization of metformin hydrochloride - Compritol 888 ATO solid dispersion. J Young Pharm 2011;3:197-204.
12. Ali W, Williams AC, Rawlinson CF. Stochiometrically governed molecular interactions in drug: Poloxamer solid dispersions. Int J Pharm 2010;391:162-8.
13. Mooter GV, Weuts I, Ridder T De, Blaton N. Evaluation of inutec SP1 as a new carrier in the formulation of solid dispersions for poorly soluble drugs. Int J Pharm 2006;316:1-6.
14. Goddeeris C, Willems T, Houthoofd K, Martens JA, Mooter GV. Dissolution enhancement of the anti-HIV drug UC 781 by formulation in a ternary solid dispersion with TPGS 1000 and Eudragit E100. Eur J Pharm Biopharm 2008;70:861-8.
15. de Waard H, Hinrichs WL, Visser MR, Bologna C, Frijlink HW. Unexpected differences in dissolution behavior of tablets prepared from solid dispersions with a surfactant physically mixed or incorporated. Int J Pharm 2008;349:66-73.
16. Huang J, Wigent RJ, Schwartz JB. Nifedipine molecular dispersion in microparticles of ammonio methacrylate copolymer and ethylcellulose binary blends for controlled drug delivery: Effect of matrix composition. Drug Dev Ind Pharm 2006;32:1185-97.
17. Cui F, Yang M, Jiang Y, Cun D, Lin W, Fan Y, et al. Design of sustained-release nitrendipine microspheres having solid dispersion structure by quasi-emulsion solvent diffusion method. J Controll Release 2003;91:375-84.
18. Leuner C, Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm 2000;50:47-60.
19. Van den Mooter G. The use of amorphous solid dispersions: A formulation strategy to overcome poor solubility and dissolution rate. Drug Discovery Today Technol 2011;9:79-85.
20. Baird JA, Taylor LS. Evaluation of amorphous solid dispersion properties using thermal analysis techniques. Adv Drug Delivery Rev 2012;64:396-421.
21. Yoshioka M, Hancock BC, Zografi G. Crystallization of indomethacin from the amorphous state below and above its glass transition temperature. J Pharm Sci 1994;83:1700-5.
22. Vasanthavada M, Tong WK(twin), Joshi Y, Kislalioglu MS. Phase behavior of amorphous molecular dispersions II: Role of hydrogen bonding in solid solubility and phase separation kinetics. Pharm Res 2005;22:440-8.
23. Mura P, Moyano JR, GonzÃ¡lez-RodrÃguez ML, Rabasco-AlvarÃ©z AM, Cirri M, Maestrelli F, et al. 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.
24. Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci 1971;60:1281-302.
25. KolaÅ¡inac N, Kachrimanis K, HomÅ¡ek L, GrujiÄ‡ B, ÄuriÄ‡ Z, IbriÄ‡ S. Solubility enhancement of desloratadine by solid dispersion in poloxamers. Int J Pharm 2012;436:161-70.
26. Verhoeven E, De Beer TR, Schacht E, Van den Mooter G, Remon JP, Vervaet C, et al. Influence of polyethylene glycol/polyethylene oxide on the release characteristics of sustained-release ethylcellulose mini-matrices produced by hot-melt extrusion: In vitro and in vivo evaluations. Eur J Pharm Biopharm 2009;72:463-70.
27. Ye X, Patil H, Feng X, Tiwari RV, Lu J, Gryczke A, et al. Conjugation of hot-melt extrusion with high-pressure homogenization: A Novel method of continuously preparing nanocrystal solid dispersions. AAPS PharmSciTech 2016;17:78-88.
28. Desai S, Disouza J, Musle K, Avinash H. Solubility enhancement of Ritonavir by hotmelt extrusion. Int J Pharm Pharm Sci 2016;8:309-12.
29. Vasconcelos T, Sarmento B, Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today 2007;12:1068-75.
30. Seo A, Holm P, Kristensen HG, Schaefer T. The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer. Int J Pharm 2003;259:161-71.
31. Vilhelmsen T, Eliasen H, Schaefer T. Effect of a melt agglomeration process on agglomerates containing solid dispersions. Int J Pharm 2005;303:132-42.
32. Takafumi H, Fumie K, Ikuo F. Solid dispersion preparation. European Patent EP No. 1847260 A3; 2007.
33. Zhang X, Lu Y. Centrifugal spinning: An alternative approach to fabricate Nanofibers at high speed and low cost. J Polym Rev 2014;54:677-701.
34. Jiang H, Ge Y, Fu K, Lu Y, Chen C, Zhu J, et al. Centrifugally-spun tin-containing carbon nanofibers as anode material for lithium-ion batteries. J Mater Sci 2015;50:1094-102.
35. Paaver U, HeinÃ¤mÃ¤ki J, LaidmÃ¤e I, Lust A, Kozlova J, Sillaste E, et al. Electrospun nanofibers as a potential controlled-release solid dispersion system for poorly water-soluble drugs. Int J Pharm 2015;479:252-60.
36. Won DH, Kim MS, Lee S, Park JS, Hwang SJ. Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process. Int J Pharm 2005;301:199-208.
37. Gang Y, Zhao Y, Feng N, Zhang Y, Liu Y, Dang B. Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids. Asian J Pharm Sci 2015;10:194-202.
38. Shaofeng W, Ma Y, Luo J, He X, Yue P, Guan Z, et al. Hydroxypropylcellulose as matrix carrier for novel cage-like microparticles prepared by spray-freeze-drying technology. Carbohydr Polym 2017;157:953-61.
39. Badens E, Majerik V, Horvath G, Szokonya L, Bosc N, Teillaud E, et al. Comparison of solid dispersions produced by supercritical antisolvent and spray-freezing technologies. Int J Pharm 2009;377:25-34.
40. Wei-Juan X, Xie HJ, Cao QR, Shi LL, Cao Y, Zhu XY, et al. Dissolution and oral bioavailability of valsartan solid dispersions prepared by a freeze-drying technique using hydrophilic polymer. J Drug Delivery 2016;23:41-8.
41. Kaur P, Singh SK, Garg V, Gulati M, Vaidya Y. Optimization of spray drying process for formulation of solid dispersion containing polypeptide-k powder through quality by design approach. Powder Technol 2015;284:1-11.
42. Ramesh K, Shekar BC, Khadgapathi P. Formulation and evaluation of travertine by spray drying method. Int J Pharm Pharm Sci 2015;7:98-103.
43. Li J, Miao X, Chen T, Ouyang D, Zheng Y. Preparation and characterization of pelletized solid dispersion of resveratrol with mesoporous silica microparticles to improve dissolution by fluid-bed coating techniques. Am J Pharm Sci 2016;11:528-35.
44. Dennis AB, Farr SJ, Kellaway IW, Taylor G, Davidson R. In vivo evaluation of rapid release and sustained release gelucire capsule formulations. Int J Pharm 1990;65:85-100.
45. Dordunoo SK, Ford JL, Rubinstein MH. Preformulation studies on solid dispersions containing triamterene or temazepam in polyethylene glycols or gelucire 44/14 for liquid filling of hard gelatin capsules. Drug Dev Ind Pharm 1991;17:1685-713.
46. Porter CJ, Charman SA, Williams RD, Bkalova MV, Charman WN. Evaluation of emulsifiable glasses for the oral administration of cyclosporin in beagle dogs. Int J Pharm 1996;141:227-37.
47. Shah B, Kakumanu VK, Bansal AK. Analytical techniques for quantification of amorphous/crystalline phases in pharmaceutical solids. J Pharm Sci 2006;95:1641-65.
48. Berndl G, Degenhardt M, Maegerlein M, Dispersyn G. Itraconazole Compositions with Improved Bioavailability. U.S. Patent No. US9149431 B2; 2015.
49. Guinot S, Leveiller F. The use of MTDSC to assess the amorphous phase content of a micronized drug substance. Int J Pharm 1999;192:63-75.
50. Miyazaki T, Aso Y, Yoshioka S, Kawanishi T. Differences in
crystallization rate of nitrendipine enantiomers in amorphous solid dispersions with HPMC and HPMCP. Int J Pharm 2011;407:111-8.
51. Hifumi H, Ewing AV, Kazarian SG. ATR-FTIR spectroscopic imaging to study the drying and dissolution of pharmaceutical polymer-based films. Int J Pharm 2016;515:57-68.
52. Frizon F, Jd OE, Donaduzzi CM, Mitsui ML, Marchetti JM, Dissolution rate enhancement of loratadine in polyvinylpyrrolidone K-30 solid dispersions by solvent methods. Powder Technol 2013;235:532-9.
53. Paudel A, Geppi M, Mooter GV. Structural and dynamic properties of amorphous solid dispersions: The role of solid-state nuclear magnetic resonance spectroscopy and relaxometry. J Pharm Sci 2014;103:2635-62.
54. Choi JS, Park JS. Design of PVP/VA S-630 based tadalafil solid dispersion to enhance the dissolution rate. Eur J Pharm Sci 2017;97:269-76.
55. Wang W, Kang Q, Liu N, Zhang Q, Zhang Y, Li H, et al. Enhanced dissolution rate and oral bioavailability of Ginkgo biloba extract by preparing solid dispersion via hot-melt extrusion. Fitoterapia 2015;102:189-97.
56. Srinarong P, Faber JH, Visser MR, Hinrichs WL, Frijlink HW. Strongly enhanced dissolution rate of fenofibrate solid dispersion tablets by incorporation of superdisintegrants. Eur J Pharm Biopharm 2009;73:154-61.
57. Marano S, Barker SA, Raimi-Abraham BT, Missaghi S, Rajabi-Siahboomi A, Craig DQM, et al. Development of micro-fibrous solid dispersions of poorly water-soluble drugs in sucrose using temperature-controlled centrifugal spinning. Eur J Pharm Biopharm 2016;103:84-94.
58. Yu M, Sun L, Li W, Lan Z, Li B, Tan L, et al. Investigation of structure and dissolution properties of a solid dispersion of lansoprazole in polyvinylpyrrolidone. J Mol Struct 2011;1005:70-7.
59. Li J, Lee IW, Shin GH, Chen X, Park HJ. Curcumin-eudragitÂ® E PO solid dispersion: A simple and potent method to solve the problems of curcumin. Eur J Pharm Biopharm 2015;94:322-32.
60. Leung SS, Parumasivam T, Gao FG, Carrigy NB, Vehring R, Finlay WH, et al. Production of inhalation phage powders using spray freeze drying and spray drying techniques for treatment of respiratory infections. J Pharm Res 2016;33:1486-96.
61. Marano S, Barker SA, Raimi-Abraham BT, Missaghi S, Rajabi-Siahboomi A, Aliev AE, et al. Microfibrous solid dispersions of poorly water-soluble drugs produced via centrifugal spinning: Unexpected dissolution behavior on recrystallization. Mol Pharm 2017;14:1666-80.
62. Hacene YC, Singh A, Mooter GV. Drug loaded and ethylcellulose coated mesoporous silica for controlled drug release prepared using a pilot scale fluid bed system. Int J Pharm 2016;506:138-47.
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