Solid dispersion: application and limitations: Solid dispersion Application and  limitations

Ebtissam Ameer Mohammed; Mohanad Alfahad; Mohannad E Qazzaz

doi:10.22270/jddt.v14i2.6410

Authors

Ebtissam Ameer Mohammed noCollege of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq https://orcid.org/0009-0004-2080-7925
Mohanad Alfahad College of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq https://orcid.org/0000-0003-0722-3066
Mohannad E Qazzaz College of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq https://orcid.org/0000-0001-7816-5321

Abstract

Solubility and dissolution rate are essential factors in the bioavailability of a drug. The drug must be well-soluble in water to have good bioavailability. Solid dispersion is among the most widely used and effective methods for increasing solubility and releasing inadequately water-soluble medications. Solid dispersion requires the choice of a suitable carrier for the right active pharmaceutical ingredients and the proper techniques for preparing solid dispersions. The reliable dispersion system is designed in various ways to achieve the goal and avoid the accompanying obstacles.

Keywords: solid dispersion, solubility, solvent evaporation, lyophilization, generation, methods

Keywords:

solid dispersion; solubility;, solvent evaporation;, lyophilization;, generation;, methods;

DOI

https://doi.org/10.22270/jddt.v14i2.6410

Author Biographies

Ebtissam Ameer Mohammed, noCollege of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq

College of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq

Mohanad Alfahad, College of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq

Department of Pharmaceutics, College of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq

Mohannad E Qazzaz, College of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq

Department of Pharmacognosy and Medicinal Plants, College of Pharmacy, University of Mosul, Mosul, Nineveh province, Iraq

References

Sheetal Z Godse MS, Patil, Swapnil M Kothavade RBS. Techniques for solubility enhancement of Hydrophobic drugs : A Review. J Adv Pharm Educ Res. 2013;3(4):403-414.

Administration USF and D. The Biopharmaceutics Classification System (BCS) Guidance. US Food Drug Adm Drug Eval Res. Published online 2019.

Pitani L. Solubility Enhancement of Model Compounds. Published online 2017.

Jagtap S, Magdum C, Jadge D, Jagtap R. Solubility enhancement technique: a review. J Pharm Sci Res. 2018;10(9):2205-2211.

Dahan A, Miller JM, Amidon GL. Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs. AAPS J. 2009;11:740-746. https://doi.org/10.1208/s12248-009-9144-x PMid:19876745 PMCid:PMC2782078

Kuchekar AB, Gawade A, Boldhane S. Hydrotropic Solubilization: An Emerging Approach. J Drug Deliv Ther. 2021;11(1-s):200-206. doi:10.22270/jddt.v11i1-s.4724 https://doi.org/10.22270/jddt.v11i1-s.4724

Noyes AA, Whitney WR. The rate of solution of solid substances in their own solutions. J Am Chem Soc. 1897;19(12):930-934. https://doi.org/10.1021/ja02086a003

Nernst W. Theorie der Reaktionsgeschwindigkeit in heterogenen Systemen. Zeitschrift für Phys Chemie. 1904;47(1):52-55. https://doi.org/10.1515/zpch-1904-4704

Vasconcelos T, Marques S, das Neves J, Sarmento B. Amorphous solid dispersions: Rational selection of a manufacturing process. Adv Drug Deliv Rev. 2016;100:85-101. https://doi.org/10.1016/j.addr.2016.01.012 PMid:26826438

Seo JH, Park JB, Choi WK, et al. Improved oral absorption of cilostazol via sulfonate salt formation with mesylate and besylate. Drug Des Devel Ther. 2015;9:3961. https://doi.org/10.2147/DDDT.S87687 PMid:26251575 PMCid:PMC4524531

R Serrano D, H Gallagher K, Marie Healy A. Emerging nanonisation technologies: tailoring crystalline versus amorphous nanomaterials. Curr Top Med Chem. 2015;15(22):2327-2340. https://doi.org/10.2174/1568026615666150605122917 PMid:26043733

Kumar Sarangi M. "Solid Dispersion - a Novel Approach for Enhancement of Bioavailability of Poorly Soluble Drugs in Oral Drug Delivery System." Glob J Pharm Pharm Sci. 2017;3(2). https://doi.org/10.19080/GJPPS.2017.03.555608

Bhowmik D, G.Harish, S.Duraivel, Kumar BP, Raghuvanshi V, Kumar KPS. Solid Dispersion - A Approach To Enhance The Dissolution Rate of Poorly Water Soluble Drugs. Pharma Innov J. 2013;1(12):24-38. https://www.thepharmajournal.com/archives/?year=2013&vol=1&issue=12&ArticleId=104

Wu CY, Benet LZ. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res. 2005;22:11-23. https://doi.org/10.1007/s11095-004-9004-4 PMid:15771225

Gulia R, Singh S, Sharma N, Arora S. Hydrotropic solid dispersions: A robust application to undertake solubility challenges. Plant Arch. 2020;20:3279-3284.

Kapadiya N, Singhvi I, Mehta K, Karwani G, Dhrubo JS. Hydrotropy: A promising tool for solubility enhancement: A review. Int J Drug Dev Res. 2011;3(2):26-33.

Arunachalam A, Karthikeyan M, Kishore K, Pottabathula HP, Sethuraman S, Hutoshkumar SA. Solid Dispersions. Curr Pharma Res. 2010;1(1). https://doi.org/10.33786/JCPR.2010.v01i01.016

Singh S, Baghel RS, Yadav L. A review on solid dispersion. Int J Pharm life Sci. 2011;2(9).

Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci. 1971;60(9):1281-1302. https://doi.org/10.1002/jps.2600600902 PMid:4935981

Zhou D, Grant DJW, Zhang GGZ, Law D, Schmitt EA. A calorimetric investigation of thermodynamic andmolecular mobility contributions to the physical stability of two pharmaceutical glasses. J Pharm Sci. 2007;96(1):71-83. https://doi.org/10.1002/jps.20633 PMid:17031846

Taylor LS, Zografi G. Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions. Pharm Res. 1997;14:1691-1698. https://doi.org/10.1023/A:1012167410376 PMid:9453055

Pokharkar VB, Mandpe LP, Padamwar MN, Ambike AA, Mahadik KR, Paradkar A. Development, characterization and stabilization of amorphous form of a low Tg drug. Powder Technol. 2006;167(1):20-25. https://doi.org/10.1016/j.powtec.2006.05.012

Alshehri S, Imam SS, Hussain A, et al. Potential of solid dispersions to enhance solubility, bioavailability, and therapeutic efficacy of poorly water-soluble drugs: newer formulation techniques, current marketed scenario and patents. Drug Deliv. 2020;27(1):1625-1643. https://doi.org/10.1080/10717544.2020.1846638 PMid:33207947 PMCid:PMC7737680

Zhang X, Sun N, Wu B, Lu Y, Guan T, Wu W. Physical characterization of lansoprazole/PVP solid dispersion prepared by fluid-bed coating technique. Powder Technol. 2008;182(3):480-485. https://doi.org/10.1016/j.powtec.2007.07.011

Meng F, Gala U, Chauhan H. Classification of solid dispersions: correlation to (i) stability and solubility (ii) preparation and characterization techniques. Drug Dev Ind Pharm. 2015;41(9):1401-1415. https://doi.org/10.3109/03639045.2015.1018274 PMid:25853292

Vo CLN, Park C, Lee BJ. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm. 2013;85(3):799-813. https://doi.org/10.1016/j.ejpb.2013.09.007 PMid:24056053

Zhang X, Xing H, Zhao Y, Ma Z. Pharmaceutical dispersion techniques for dissolution and bioavailability enhancement of poorly water-soluble drugs. Pharmaceutics. 2018;10(3). https://doi.org/10.3390/pharmaceutics10030074 PMid:29937483 PMCid:PMC6161168

Van Duong T, Van den Mooter G. The role of the carrier in the formulation of pharmaceutical solid dispersions. Part II: amorphous carriers. Expert Opin Drug Deliv. 2016;13(12):1681-1694. https://doi.org/10.1080/17425247.2016.1198769 PMid:27267583

Vasconcelos T, Sarmento B, Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today. 2007;12(23-24):1068-1075. https://doi.org/10.1016/j.drudis.2007.09.005 PMid:18061887

Kaushik R, Budhwar V, Kaushik D. An Overview on Recent Patents and Technologies on Solid Dispersion. Recent Pat Drug Deliv Formul. 2020;14(1):63-74. https://doi.org/10.2174/1872211314666200117094406 PMid:31951172 PMCid:PMC7569281

Swain RP, Subudhi BB. Effect of semicrystalline polymers on self-emulsifying solid dispersions of nateglinide: in vitro and in vivo evaluation. Drug Dev Ind Pharm. 2018;44(1):56-65. https://doi.org/10.1080/03639045.2017.1371739 PMid:28845687

Marsac PJ, Shamblin SL, Taylor LS. Theoretical and practical approaches for prediction of drug-polymer miscibility and solubility. Pharm Res. 2006;23:2417-2426. https://doi.org/10.1007/s11095-006-9063-9 PMid:16933098

Matsumoto T, Zografi G. Physical properties of solid molecular dispersions of indomethacin with poly (vinylpyrrolidone) and poly (vinylpyrrolidone-co-vinyl-acetate) in relation to indomethacin crystallization. Pharm Res. 1999;16:1722-1728. https://doi.org/10.1023/A:1018906132279 PMid:10571278

Sun N, Zhang X, Lu Y, Wu W. In vitro evaluation and pharmacokinetics in dogs of solid dispersion pellets containing Silybum marianum extract prepared by fluid-bed coating. Planta Med. 2008;74(02):126-132. https://doi.org/10.1055/s-2008-1034294 PMid:18240100

Vasconcelos T, Sarmento B, Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today. 2007;12(23-24):1068-1075. https://doi.org/10.1016/j.drudis.2007.09.005 PMid:18061887

Vo CLN, Park C, Lee BJ. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm. 2013;85(3 PART B):799-813. https://doi.org/10.1016/j.ejpb.2013.09.007 PMid:24056053

Sekiguchi K, Obi N, Ueda Y. Studies on Absorption of Eutectic Mixture. II. Absorption of fused Conglomerates of Chloramphenicol and Urea in Rabbits. Chem Pharm Bull. 1964;12(2):134-144. https://doi.org/10.1248/cpb.12.134 PMid:14126741

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(11):866-872. https://doi.org/10.1248/cpb.9.866

Kaur N, Gupta RC. To quantify the luteolin content from the aerial parts of Heteropogon contortus (L.) Beauv.(spear grass) through High-performance thin-layer chromatography. Asian J Pharm Clin Res. 2018;11(1):191-194. https://doi.org/10.22159/ajpcr.2018.v11i1.22116

Vo CL, Park C, Lee B. European Journal of Pharmaceutics and Biopharmaceutics Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm. 2013;85:799-813. https://doi.org/10.1016/j.ejpb.2013.09.007 PMid:24056053

Saharan V, Kukkar V, Kataria M, Gera M, Choudhury PK. Dissolution enhancement of drugs. Part I: technologies and effect of carriers. Int J Heal Res. 2009;2(2). https://doi.org/10.4314/ijhr.v2i2.55401

Hülsmann S, Backensfeld T, Keitel S, Bodmeier R. Melt extrusion-an alternative method for enhancing the dissolution rate of 17β-estradiol hemihydrate. Eur J Pharm Biopharm. 2000;49(3):237-242. https://doi.org/10.1016/S0939-6411(00)00077-1 PMid:10799815

Jatwani S, Rana AC, Singh G, Aggarwal G. An overview on solubility enhancement techniques for poorly soluble drugs and solid dispersion as an eminent strategic approach. Int J Pharm Sci Res. 2012;3(4):942. https://doi.org/10.1002/chin.201313244

Shuai S, Yue S, Huang Q, et al. Preparation, characterization and in vitro/vivo evaluation of tectorigenin solid dispersion with improved dissolution and bioavailability. Eur J Drug Metab Pharmacokinet. 2016;41:413-422. https://doi.org/10.1007/s13318-015-0265-6 PMid:25669445

Daravath B, Tadikonda RR, Vemula SK. Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen. Drug Dev Ind Pharm. 2015;41(8):1254-1262. https://doi.org/10.3109/03639045.2014.940963 PMid:25039470

Dhapte V, Mehta P. Advances in hydrotropic solutions: An updated review. St Petersbg Polytech Univ J Phys Math. 2015;1(4):424-435. https://doi.org/10.1016/j.spjpm.2015.12.006

Mustapha O, Kim KS, Shafique S, et al. Comparison of three different types of cilostazol-loaded solid dispersion: Physicochemical characterization and pharmacokinetics in rats. Colloids Surfaces B Biointerfaces. 2017;154:89-95. https://doi.org/10.1016/j.colsurfb.2017.03.017 PMid:28324691

Al-Hamidi H, Obeidat WM, Nokhodchi A. The dissolution enhancement of piroxicam in its physical mixtures and solid dispersion formulations using gluconolactone and glucosamine hydrochloride as potential carriers. Pharm Dev Technol. 2015;20(1):74-83. https://doi.org/10.3109/10837450.2013.871029 PMid:24392858

Kim SJ, Lee HK, Na YG, et al. A novel composition of ticagrelor by solid dispersion technique for increasing solubility and intestinal permeability. Int J Pharm. 2019;555:11-18. https://doi.org/10.1016/j.ijpharm.2018.11.038 PMid:30448313

Zhang W, Zhang C ning, He Y, et al. Factors affecting the dissolution of indomethacin solid dispersions. Aaps Pharmscitech. 2017;18:3258-3273. https://doi.org/10.1208/s12249-017-0813-2 PMid:28584898

Crucitti VC, Migneco LM, Piozzi A, et al. Intermolecular interaction and solid state characterization of abietic acid/chitosan solid dispersions possessing antimicrobial and antioxidant properties. Eur J Pharm Biopharm. 2018;125:114-123. https://doi.org/10.1016/j.ejpb.2018.01.012 PMid:29366926

Frizon F, de Oliveira Eloy J, Donaduzzi CM, Mitsui ML, Marchetti JM. Dissolution rate enhancement of loratadine in polyvinylpyrrolidone K-30 solid dispersions by solvent methods. Powder Technol. 2013;235:532-539. https://doi.org/10.1016/j.powtec.2012.10.019

Khuspe PR, Kokate K, Mandhare T, Otari K, Katiyar P. THE COMPREHENSIVE REVIEW ON SOLID DISPERSION TECHNOLOGY. Published online 2017.

Madgulkar A, Bandivadekar M, Shid T, Rao S. Sugars as solid dispersion carrier to improve solubility and dissolution of the BCS class II drug: clotrimazole. Drug Dev Ind Pharm. 2016;42(1):28-38. https://doi.org/10.3109/03639045.2015.1024683 PMid:25874729

de los Santos CJJ, Pérez-Martínez JI, Gómez-Pantoja ME, Moyano JR. Enhancement of albendazole dissolution properties using solid dispersions with Gelucire 50/13 and PEG 15000. J Drug Deliv Sci Technol. 2017;42:261-272. https://doi.org/10.1016/j.jddst.2017.03.030

Xu H, Liu L, Li X, Ma J, Liu R, Wang S. Extended tacrolimus release via the combination of lipid-based solid dispersion and HPMC hydrogel matrix tablets. Asian J Pharm Sci. 2019;14(4):445-454. https://doi.org/10.1016/j.ajps.2018.08.001 PMid:32104473 PMCid:PMC7032121

Karolewicz B, Gajda M, Pluta J, Górniak A. Dissolution study and thermal analysis of fenofibrate-Pluronic F127 solid dispersions. J Therm Anal Calorim. 2016;125:751-757. https://doi.org/10.1007/s10973-015-5013-2

Shen Y, Lu F, Hou J, Shen Y, Guo S. Incorporation of paclitaxel solid dispersions with poloxamer188 or polyethylene glycol to tune drug release from poly (ϵ-caprolactone) films. Drug Dev Ind Pharm. 2013;39(8):1187-1196. https://doi.org/10.3109/03639045.2012.704042 PMid:22803692

Chamsai B, Limmatvapirat S, Sungthongjeen S, Sriamornsak P. Enhancement of solubility and oral bioavailability of manidipine by formation of ternary solid dispersion with d-α-tocopherol polyethylene glycol 1000 succinate and copovidone. Drug Dev Ind Pharm. 2017;43(12):2064-2075. https://doi.org/10.1080/03639045.2017.1371731 PMid:28836855

Krishnamoorthy V, Prasad VPR. Physicochemical characterization and in vitro dissolution behavior of olanzapine-mannitol solid dispersions. Brazilian J Pharm Sci. 2012;48:243-255. https://doi.org/10.1590/S1984-82502012000200008

Prasad R, Radhakrishnan P, Singh SK, Verma PRP. Furosemide-Soluplus® Solid Dispersion: Development and Characterization. Recent Pat Drug Deliv Formul. 2017;11(3):211-220. https://doi.org/10.2174/1872211311666171129120020 PMid:29189186

Betageri G V, Makarla KR. Enhancement of dissolution of glyburide by solid dispersion and lyophilization techniques. Int J Pharm. 1995;126(1-2):155-160. https://doi.org/10.1016/0378-5173(95)04114-1

Altamimi MA, Neau SH. Investigation of the in vitro performance difference of drug-Soluplus® and drug-PEG 6000 dispersions when prepared using spray drying or lyophilization. Saudi Pharm J. 2017;25(3):419-439. https://doi.org/10.1016/j.jsps.2016.09.013 PMid:28344498 PMCid:PMC5357108

Jacobsen AC, Elvang PA, Bauer-Brandl A, Brandl M. A dynamic in vitro permeation study on solid mono-and diacyl-phospholipid dispersions of celecoxib. Eur J Pharm Sci. 2019;127:199-207. https://doi.org/10.1016/j.ejps.2018.11.003 PMid:30408522

Suzuki H, Yakushiji K, Matsunaga S, et al. Amorphous solid dispersion of meloxicam enhanced oral absorption in rats with impaired gastric motility. J Pharm Sci. 2018;107(1):446-452. https://doi.org/10.1016/j.xphs.2017.05.023 PMid:28551427

Ngo AN, Thomas D, Murowchick J, Ayon NJ, Jaiswal A, Youan BBC. Engineering fast dissolving sodium acetate mediated crystalline solid dispersion of docetaxel. Int J Pharm. 2018;545(1-2):329-341. https://doi.org/10.1016/j.ijpharm.2018.04.045 PMid:29689368

Phillips EM, Stella VJ. Rapid expansion from supercritical solutions: application to pharmaceutical processes. Int J Pharm. 1993;94(1-3):1-10. https://doi.org/10.1016/0378-5173(93)90002-W

Nikolai P, Rabiyat B, Aslan A, Ilmutdin A. Supercritical CO 2: Properties and technological applications-a review. J Therm Sci. 2019;28:394-430. https://doi.org/10.1007/s11630-019-1118-4

Rantakylä M. Particle Production by Supercritical Antisolvent Processing Techniques. Helsinki University of Technology; 2004.

Manna L, Banchero M, Sola D, Ferri A, Ronchetti S, Sicardi S. Impregnation of PVP microparticles with ketoprofen in the presence of supercritical CO2. J Supercrit Fluids. 2007;42(3):378-384. https://doi.org/10.1016/j.supflu.2006.12.002

Martin TM, Bandi N, Shulz R, Roberts CB, Kompella UB. Preparation of budesonide and budesonide-PLA microparticles using supercritical fluid precipitation technology. AAPS PharmSciTech. 2002;3:16-26. https://doi.org/10.1208/pt030318 PMid:12916933 PMCid:PMC2784047

Dohrn R, Bertakis E, Behrend O, Voutsas E, Tassios D. Melting point depression by using supercritical CO2 for a novel melt dispersion micronization process. J Mol Liq. 2007;131:53-59. https://doi.org/10.1016/j.molliq.2006.08.026

Adeli E. The use of supercritical anti-solvent (SAS) technique for preparation of Irbesartan-Pluronic® F-127 nanoparticles to improve the drug dissolution. Powder Technol. 2016;298:65-72. https://doi.org/10.1016/j.powtec.2016.05.004

Zhang J, Huang Y, Liu D, Gao Y, Qian S. Preparation of apigenin nanocrystals using supercritical antisolvent process for dissolution and bioavailability enhancement. Eur J Pharm Sci. 2013;48(4-5):740-747. https://doi.org/10.1016/j.ejps.2012.12.026 PMid:23305994

Moneghini M, Kikic I, Voinovich D, Perissutti B, Filipović-Grčić J. Processing of carbamazepine-PEG 4000 solid dispersions with supercritical carbon dioxide: preparation, characterisation, and in vitro dissolution. Int J Pharm. 2001;222(1):129-138. https://doi.org/10.1016/S0378-5173(01)00711-6 PMid:11404039

Tabbakhian M, Hasanzadeh F, Tavakoli N, Jamshidian Z. Dissolution enhancement of glibenclamide by solid dispersion: solvent evaporation versus a supercritical fluid-based solvent-antisolvent technique. Res Pharm Sci. 2014;9(5):337.

Teja SB, Patil SP, Shete G, Patel S, Bansal AK. Drug-excipient behavior in polymeric amorphous solid dispersions. J Excipients Food Chem. 2016;4(3).

Craig DQM. The mechanisms of drug release from solid dispersions in water-soluble polymers. Int J Pharm. 2002;231(2):131-144. https://doi.org/10.1016/S0378-5173(01)00891-2 PMid:11755266

Kumar R, Singh A, Salwan R, Bhanot R, Rahar S, Dhawan RK. An informative review on solid dispersion. GSC Biol Pharm Sci. 2023;22(1):114-121. https://doi.org/10.4103/jpbs.jpbs_432_22 PMid:37654356 PMCid:PMC10466630

Shah B, Kakumanu VK, Bansal AK. Analytical techniques for quantification of amorphous/crystalline phases in pharmaceutical solids. J Pharm Sci. 2006;95(8):1641-1665. https://doi.org/10.1002/jps.20644 PMid:16802362

Patel A, Jain RK, Jain V, Khangar PK. Formulation and Evaluation of Sustained Release Solid Dispersed Nifedipine Microcapsules. Asian J Dental Health Sci [Internet]. 2022 Nov. 22 [cited 2024 Feb. 8];2(3):12-8. https://doi.org/10.22270/ajdhs.v2i3.21

Berndl G, Degenhardt M, Mägerlein M, Dispersyn G. Itraconazole compositions with improved bioavailability. Published online October 6, 2015.

Kerc J, Srcic S. Thermal analysis of glassy pharmaceuticals. Thermochim Acta. 1995;248:81-95. https://doi.org/10.1016/0040-6031(94)01949-H

Kumar B. Solid dispersion-a review. PharmaTutor. 2017;5(2):24-29

Solid dispersion: application and limitations