Solid Dispersions: Technique to Enhance Solubility of Poorly Water Soluble Drug
Main Article Content
Abstract
Solid dispersions are one of the most promising strategies to enhance solubility of poorly water soluble drugs because they are easier to produce and more applicable. They show many advantages such as reducing particle size of drug, improving wettability and dissolvability, and converting crystalline structure of drug to amorphous form. The solid dispersions can also be classified into three generations based on composition of formulation i.e. first generation (using crystalline carriers: urea, mannitol), second generation (using amorphous carriers: polyvinylpyrrolidone, polyethylene glycol, hydroxypropyl methylcellulose) and third generation (using surfactant or amphiphilic polymer carriers: Gelucire®, Poloxamer®, Soluplus®). There are three different methods to prepare solid dispersions such as melting or fusion method, solvent evaporation method and melting-solvent method. Nowadays, solid dispersions have been developed in manufacturing process to solve the drawback of the initial process such as hot melt extrusion, MeltrexTM, spray dry, freeze dry. Thus, the review article presents an overview of definition of solid dispersion, advantages and disadvantages, classification according to generation and type of carrier including preparation and evaluation of solid dispersions.
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References
Adeli E. A comparative evaluation between utilizing SAS supercritical fl uid technique and solvent evaporation method in preparation of azithromycin solid dispersions for dissolution rate enhancement. J Supercrit Fluids 2014;87:9-21.
Bley H, Fussnegger B, Bodmeir R. Characterization and stability of solid dispersions base on PEG/polymer blens. Int J Pharm 2010; 390:165-173.
Chauhan B, Shimpi S, Paradkar A. Preparation and evaluation of glibenclamide-polyglycolized glycerides solid dispersions with silicon dioxide by spray-drying technique. Eur J Pharm Sci 2005;26:219–30.
Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci 1971;60(9):1281-1302.
Damian F, Blaton N, Naesens L, 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;10:311–322.
Devi DR, Sandhya P, Vedha Hari BN. Poloxamer: A novel functional molecule for drug delivery and genetherapy. J Pharm sci & Res 2013;5(8):159-165.
Dhirendra K, Lewis S, Udupa N, et al. Solid Dispersions: A Review. Pak J Pharm Sci 2009; 22 (2): 234-246.
Djuris J, Nikolakakis I, Ibric S, et al. Preparation of carbamazepine–Soluplus solid dispersions by hot-melt extrusion, and prediction of drug–polymer miscibility by thermodynamic model fi tting. Eur J Pharm Biopharm 2013; 84:228-237.
El-badry M, Hassan MA, Ibrahim MA, et al. Performance of poloxamer 407 ashydrophilic carrieron the binary mixtures with nimesulide. Farmacia 2013;61(6): 1137- 1150.
El-badry M, Fetih G, Fath M. Improvement of solubility and dissolution rate of indomethacin by solid dispersions in Gelucire 50/13 and PEG 4000. Saudi Pharm J 2009;17:217–25.
Eloy JO, Marchetti JM. Solid dispersions containing ursolic acid in poloxamer 407 and PEG 6000: A comparative study of fusion and solvent methods. Powder Technol 2014; 253:98-106.
Fini A, Moyano J, Ginés J, et al. Diclofenac salts II. Solid dispersions in PEG6000 and Gelucire 50/13. Eur J Pharm Biopharm 2005;60:99–111.
Frizon F, Eloy JO, Donaduzzi CM, et al. Dissolution rate enhancement of loratadine in polyvinylpyrrolidone K-30 solid dispersions by solvent methods. Powder Technol 2013;235:532-539.
Fukushima K, Terasaka S, Haraya K, et al. Pharmaceutical approach to HIV inhibitor atazanavir for bioavailability enhancement based on solid dispersion system. Biol Pharm Bull 2007;30:733–8.
Fule R, Amin P. Development and evaluation of lafutidine solid dispersion via hot melt extrusion: Investigating drug-polymer miscibility with advanced characterisation. AJPS 2014;9:92-106.
Ghareeb MM, Abdulrasool AA, Hussein AA, et al. Kneading technique for preparation of binary solid dispersion of meloxicam with poloxamer 188. AAPS PharmSciTech 2009;10(4):1206-1215.
Hardung H, Djuric, D, Ali S. Combining HME and solubilization: soluplus – the solid solution. Drug Deliv Technol 2010;10:20–27.
Huang Y, Dai W-G. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharm Sin B 2014; 4(1) 18-25.
Hughey JR, Keen JM, Miller DA, et al. The use of inorganic salts to improve the dissolution characteristics of tablets containing Soluplus-based solid dispersions. Eur J Pharm Sci 2013; 48:758-766.
Javeer SD, Patole R, Amin P. Enhanced solubility and dissolution of simvastatin by HPMC-base solid dispersions prepared by hot melt extrusion and spray-drying method. J Pharm Investig 2013;43:471- 480.
Kawabata Y, Wada K, Nakatani M, et al. Formulation design for poorly water-soluble drugs based on biopharmaceutics classifi cation system: Basic approaches and practical applications. Int J Pharm 2011; 420:1-10.
Kolašinac N, Kachrimanis K, Homˇsek I, et al. Solubility enhancement of desloratadine by solid dispersion in poloxamers. Int J Pharm 2012;436:161-170.
Le-Ngoc Vo C, Park C, Lee B-J. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm 2013; 85:799-813.
Leuner C and Dressman J. Improving drug solubility for oral delivery using solid dispersion. Eur J Pharm Biopharm 2000;50:47-60.
Levy G. Effect of particle size on dissolution and gastrointestinal absorption rates of pharmaceuticals. Am J Pharm Sci 1963; 135:78-92.
Lipinski CA. Avoiding investment in doomed drugs, is poor solubility an industry wide problem?. Curr Drug Discov 2001; 4:17-19.
Loh GOK, Tan YTF, Peh KK. Hydrophilic polymer solubilization on norfl oxacin solubility in preparation of solid dispersion. Powder Technol 2014;256:462-469.
Newa M, Bhandari KH, Oh DH, et al. Enhanced dissolution of ibuprofen using solid dispersion with poloxamer 407. Arch Pharm Res 2008;31(11):1497-1507.
Okonogi S, Oguchi T, Yonemochi E, et al. Improved dissolution of ofl oxacin via solid dispersion. Int J Pharm 1997;156: 175-180.
Patel BP, Patel DM, Patel JK, et al. A review on techniques which are useful for solubility enhancement of poorly water soluble drugs. IJRMP 2012;1(1):56-70.
Reynolds TD, Gehrke SH, Hussain AS, et al. Polymer erosion and drug release characterization of hydroxypropylmethylcellulose matrices. J Pharm Sci 1998; 87: 1115-1123.
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; 9:866–872.
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.
Sharma A, Jain CP. Preparation and characterization of solid dispersions of valsartan with poloxamer 188. Der Pharmacia Lettre 2010;2(2): 54-63
Shamma RN, Basha M. Soluplus®: A novel polymeric solubilizer for optimization of Carvedilol solid dispersions: Formulation design and effect of method of preparation. Powder Technol 2013;237:406-414.
Taylor LS, Zografi G.Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions. Pharm Res 1997;14(12): 1691-1698.
Vippagunta S, Maul K, Tallavayhala S, et al. Solid-state characterization of nifedipine solid dispersions. Int J Pharm 2002;236 :111–23.
Xu W, Ling P, Zhang T. Polymeric micelles, a promising drug delivery system to enhance bioavailability of poorly watersoluble drugs. J Drug Deliv 2013; http://dx.doi.org/10.1155/2013/34015.
Yun F, Kang A, Shan J, et al. Preparation of osthole-polymer solid dispersions by hot-melt extrusion for dissolution and bioavailability enhancement. Int J Pharm 2014;465:436-443.
Yuvaraja K, Khanam J. Enhancement of carvedilol solubility by solid dispersion technique using cyclodextrins, water soluble polymers and hydroxyl acid. J Pharm Biomed Anal 2014;96:10-20.