SOLID DISPERSION TABLETS IN IMPROVING ORAL BIOAVAILABILITY OF POORLY SOLUBLE DRUGS

Authors

  • PRASENJIT SARKAR Division of Pharmaceutics, Department of Pharmaceutical Technology, NSHM Knowledge Campus, Kolkata-Group of Institutions, 124 BL Saha Road, Kolkata 700053, West Bengal
  • SAUMYAJYOTI DAS Division of Pharmaceutics, Department of Pharmaceutical Technology, NSHM Knowledge Campus, Kolkata-Group of Institutions, 124 BL Saha Road, Kolkata 700053, West Bengal
  • SUTAPA BISWAS MAJEE Division of Pharmaceutics, Department of Pharmaceutical Technology, NSHM Knowledge Campus, Kolkata-Group of Institutions, 124 BL Saha Road, Kolkata 700053, West Bengal

DOI:

https://doi.org/10.22159/ijcpr.2022v14i2.1961

Keywords:

Carrier, Controlled release, Fast release, Fickian transport, First-order kinetics, Higuchi model, Solid dispersion, Superdisintegrant, Sustained-release, Tablet

Abstract

Recent advances in the field of conversion of solid dispersions of poorly water-soluble drugs in a wide range of hydrophilic or water-soluble carriers into solid dispersion tablets have shown great promise in improving solubility, dissolution rate and oral bioavailability of such drugs. Moreover, proper choice of tablet excipients during tableting of optimised solid dispersions can produce either fast/rapid or sustained drug release profile. Release kinetics have been found to follow either first-order kinetics or Higuchi model and release profiles in most of the cases have been found to be superior to that of conventional tablets or capsules. The present review aims to sum up the various studies on solid dispersion tablets and establish the novelty of this unique approach in the overall improvement of oral bioavailability of poorly water-soluble drugs in a simple and cost-effective manner.

Downloads

Download data is not yet available.

References

Sapkal S, Babhulkar M, Rathi A, Mehetre G, Narkhede M. An overview on the mechanisms of solubility and dissolution rate enhancement in solid dispersion. Int J Pharm Tech Res. 2013;5(1):31-9.

Vemula VR, Lagishetty V, Lingala S. Solubility enhancement techniques. Int J Pharm Sci Rev Res. 2010;5(1):41-51.

Kesarwani P, Rastogi S, Bhalla V, Arora V. Solubility enhancement of poorly water-soluble drugs: a review. Int J Pharm Sci Res. 2014;5(8):3123-7.

Gulia R, Singh S, Sharma N, Arora S. Hydrotropic solid dispersions: A robust application to undertake solubility challenges. Plant Arch. 2020;20(1):3279-84.

Sharma N, Jain N, Sudhakar CK. Jain S. Formulation and evaluation of gastro retentive floating tablets containing cefpodoxime proxetil solid dispersions. Int J Curr Pharm Res. 2012;4(4):82-7.

Katore GS, Bidkar SJ, Dama GY. Formulation and evaluation of solid ciprofloxacin dispersion controlled release floating capsules for solubility improvement. IJPBR 2017;5(3):7-16. doi: 10.30750/ijpbr.5.3.2.

Rahman Z, Zidan AS, Khan MA. Risperidone solid dispersion for orally disintegrating tablet: its formulation design and non-destructive methods of evaluation. Int J Pharm. 2010;400(1-2):49-58. doi: 10.1016/j.ijpharm.2010.08.025, PMID 20801200.

Paul AD, Vinay J, Rajyalakshmi KG, Prasad PV. Formulation design for poorly water-soluble drug by using solid dispersion of telmisartan for solubility and dissolution rate enhancement. Glob J Pharm Sci. 2019;7(4):1-11.

Sakure K, Kumari L, Badwaik H. Development and evaluation of solid dispersion based rapid disintegrating tablets of poorly water-soluble anti-diabetic drug. J Drug Deliv Sci Technol. 2020;60:2-29. doi: 10.1016/j.jddst.2020.101942.

Chae JS, Chae BR, Shin DJ, Goo YT, Lee ES, Yoon HY, Kim CH, Choi YW. Tablet formulation of a polymeric solid dispersion containing amorphous alkalinized telmisartan. AAPS PharmSciTech. 2018;19(7):2990-9. doi: 10.1208/s12249-018-1124-y, PMID 30043191.

Alshehri S, Imam SS, Hussain A, Altamimi MA, Alruwaili NK, Alotaibi F, Alanazi A, Shakeel F. 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):1625-43. doi: 10.1080/10717544.2020.1846638, PMID 33207947.

Das PS, Verma S, Saha P. Fast dissolving tablet using solid dispersion technique: a review. Int J Curr Pharm Sci. 2017;9(6):1-4. doi: 10.22159/ijcpr.2017v9i6.23435.

Varma MM, PSK. Formulation and evaluation of gliclazide tablets containing PVP-K30 and hydroxypropyl-β-cyclodextrin solid dispersion. PCI-Approved-IJPSN 2012;5(2):1706-19. doi: 10.37285/ijpsn.2012.5.2.6.

Fujii M, Okada H, Shibata Y, Teramachi H, Kondoh M, Watanabe Y. Preparation, characterization, and tableting of a solid dispersion of indomethacin with crospovidone. Int J Pharm. 2005;293(1-2):145-53. doi: 10.1016/j.ijpharm.2004.12.018, PMID 15778052.

Sammour OA, Hammad MA, Megrab NA, Zidan AS. Formulation and optimization of mouth dissolve tablets containing rofecoxib solid dispersion. AAPS PharmSciTech. 2006;7(2):E55. doi: 10.1208/pt070255, PMID 16796372.

Raj AR, Das AC, Sreerekha S, Harindran J. Formulation and evaluation of verapamil solid dispersion tablets for solubility enhancement. J Pharm Sci. 2016;7(1):39-54.

Muhammad Sarfraz R, Bashir S, Mahmood A, Ahsan H, Riaz H, Raza H, Rashid Z, Atif Raza S, Asad Abrar M, Abbas K, Yasmeen T. Application of various polymers and polymers based techniques used to improve solubility of poorly water soluble drugs: a review. Acta Pol Pharm. 2017;74(2):347-56. PMID 29624239.

Maheshwari RK, Indurkhya A. Novel application of mixed hydrotropic solubilization technique in the formulation and evaluation of hydrotropic solid dispersion of aceclofenac. Asian J Pharm. 2010;4(3):235-8. doi: 10.4103/0973-8398.72124.

Ha ES, Baek IH, Cho W, Hwang SJ, Kim MS. Preparation and evaluation of solid dispersion of atorvastatin calcium with Soluplus® by spray drying technique. Chem Pharm Bull (Tokyo). 2014;62(6):545-51. doi: 10.1248/cpb.c14-00030, PMID 24881660.

Suthar RM, Chotai NP, Patel HK, Patel SR, Shah DD, Jadeja MB. In vitro dissolution enhancement of ondansetron by solid dispersion insuperdisintegrants. Dis SoL Technol. 2013;2013:34-8.

Mohanachandran PS, Sindhumol PG, Kiran TS. Superdisintegrants: an overview. Int J Pharm Sci Rev Res. 2011;6(1):105-9.

Kanikkannan N. Technologies to improve the solubility, dissolution and bioavailability of poorly soluble drugs. JAPLR. 2018;7(1):44-50. doi: 10.15406/japlr.2018.07.00198.

Savjani KT, Gajjar AK, Savjani JK. Drug solubility: importance and enhancement techniques. ISRN Pharm. 2012;2012:195727. doi: 10.5402/2012/195727, PMID 22830056.

Manna S, Kollabathula J. Formulation and evaluation of ibuprofen controlled release matrix tablets using its solid dispersion. Int J Appl Pharm. 2019;11(2):71-6. doi: 10.22159/ijap.2019v11i2.30503.

Das A, Nayak AK, Mohanty B, Panda S. Solubility and dissolution enhancement of etoricoxib by solid dispersion technique using sugar carriers. ISRN Pharm. 2011;2011:819765. doi: 10.5402/2011/819765, PMID 22389861.

Saharan VA, Kukka V, Kataria M, Gera M, Choudhury PK. Dissolution enhancement of drugs. Part II: Effect of carriers. Int J Health Res. 2009;2(3):207-23. doi: 10.4314/ijhr.v2i3.47904.

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(1):43-51. doi: 10.4314/tjpr.v8i1.14711.

Altamimi MA, Elzayat EM, Qamar W, Alshehri SM, Sherif AY, Haq N, Shakeel F. Evaluation of the bioavailability of hydrocortisone when prepared as solid dispersion. Saudi Pharm J. 2019;27(5):629-36. doi: 10.1016/j.jsps.2019.03.004, PMID 31297016.

Alshehri S, Shakeel F, Elzayat E, Almeanazel O, Altamimi M, Shazly G, Kazi M, Almutairy B, Alsulays B, Alshetaili A, Alalaiwe A, Repka M. Rat palatability, pharmacodynamics effect and bioavailability of mefenamic acid formulations utilizing hot-melt extrusion technology. Drug Dev Ind Pharm. 2019;45(10):1610-6. doi: 10.1080/03639045.2019.1645161, PMID 31311329.

McFall H, Sarabu S, Shankar V, Bandari S, Murthy SN, Kolter K, Langley N, Kim DW, Repka MA. Formulation of aripiprazole-loaded pH-modulated solid dispersions via hot-melt extrusion technology: in vitro and in vivo studies. Int J Pharm. 2019;554:302-11. doi: 10.1016/j.ijpharm.2018.11.005, PMID 30395959.

Alshehri SM, Shakeel F, Ibrahim MA, Elzayat EM, Altamimi M, Mohsin K, Almeanazel OT, Alkholief M, Alshetaili A, Alsulays B, Alanazi FK, Alsarra IA. Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques. Saudi Pharm J. 2019;27(2):264-73. doi: 10.1016/j.jsps.2018.11.008, PMID 30766439.

Puhan KK, Raja S, Choudhary NK. Solid dispersion extended-release system: a review. Int J Pharm Sci Res. 2021;12(10):5281-91.

Sekiguchi K, Obi N. Studies on the absorption of eutectic mixture. I. A comparison of the behavior of the eutectic mixture of sulfathiazole and that of ordinary sulfathiazole in man. Chem Pharm Bull. 1961;9(11):866-72. doi: 10.1248/cpb.9.866.

Sekiguchi K, Obi N, Ueda Y. Studies on the absorption of eutectic mixture. ii. absorption of fused conglomerates of chloramphenicol and urea in rabbits. Chem Pharm Bull (Tokyo). 1964;12:134-44. doi: 10.1248/cpb.12.134, PMID 14126741.

Lee YS, Song JG, Lee SH, Han HK. Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH-independent polymers: preparation and in vitro/in vivo characterization. Drug Deliv. 2017;24(1):1731-9. doi: 10.1080/10717544.2017.1399304, PMID 29124978.

Kaur J, Aggarwal G, Singh G, Rana AC. Improvement of drug solubility using solid dispersion. Int J Pharm Pharm Sci. 2012;4(2):47-53.

Sareen S, Mathew G, Joseph L. Improvement in solubility of poor water-soluble drugs by solid dispersion. Int J Pharm Investig. 2012;2(1):12-7. doi: 10.4103/2230-973X.96921, PMID 23071955.

Vasconcelos TF, Sarmento B, Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water-soluble drugs. Drug Discov Today. 2007;12(23-24):1068-75. doi: 10.1016/j.drudis.2007.09.005.

Surendran SA, Iyer SR. Fast dissolving tablet using solid dispersion technique: an overview. Indo Am J Pharm Res. 2015;5(2):668-79.

Coltescu A, Butnariu M, Sarac I. The importance of solubility for new drug molecules. Biomed Pharmacol J. 2020;13(2):577-83. doi: 10.13005/bpj/1920.

Christopher D, Vimalson S, Parimalakrishnan N, Jeganathan S. Techniques to enhance the solubility of hydrophobic drugs: an overview. Asian J Pharm. 2016;10(2):S67-75.

Vaneetha G, Martha S, Potnuri N. Design and solubility enhancement of empagliflozin immediate release tablets by using solid dispersion method. Int J Pharm Pharm Res. 2017;10(2):163-79.

Giri TK, Kumar K, Alexander A, Ajazuddin BH, Badwaik H, Tripathi DK. A novel and alternative approach to controlled release drug delivery system based on solid dispersion technique. Bull Fac Pharm Cairo Univ. 2012;50(2):147-59. doi: 10.1016/j.bfopcu.2012.07.002.

Chaulang G, Patil K, Ghodke D, Khan S, Yeole P. Preparation and characterization of solid dispersion tablet of furosemide with crospovidone. Res J Pharm Technol. 2008;1(4):386-9.

Kumar Katual M, Singh G, L Harikumar S. Solubility enhancement of poorly aqueous soluble novel drug using natural gum as carriers. Panacea J Med Sci. 2020;9(3):104-16. doi: 10.18231/j.pjms.2019.024.

Linn M, Collnot EM, Djuric D, Hempel K, Fabian E, Kolter K, Lehr CM. Soluplus® as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo. Eur J Pharm Sci. 2012;45(3):336-43. doi: 10.1016/j.ejps.2011.11.025, PMID 22172603.

Perge L, Robitzer M, Guillemot C, Devoisselle JM, Quignard F, Legrand P. New solid lipid microparticles for controlled ibuprofen release: formulation and characterization study. Int J Pharm. 2012;422(1-2):59-67. doi: 10.1016/j.ijpharm.2011.10.027, PMID 22027394.

Bikiaris DN. Solid dispersions, Part I: Recent evolutions and future opportunities in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs. Expert Opin Drug Deliv. 2011;8(11):1501-19. doi: 10.1517/17425247.2011.618181, PMID 21919807.

Iqbal B, Ali A, Ali J, Baboota S, Gupta S, Dang S, Shadab M, Sahni JK. Recent advances and patents in solid dispersion technology. Recent Pat Drug Deliv Formul. 2011;5(3):244-64. doi: 10.2174/187221111797200551, PMID 21834778.

Mali RK, Pawar HA, Mali KK, Dias RJ. Fast disintegrating tablets of olmesartanmedoxomil using solid dispersion technique. Asian J Pharm. 2017;11(1):S425-33.

Chouhan M, Gupta D, Choukse R, Maheshwari RK. Formulation and evaluation fast dissolving tablets of lovastatin using solid dispersion method. J Drug Deliv Ther. 2019;9(2A):29-31.

Desai J, Alexander K, Riga A. Characterization of polymeric dispersions of dimenhydrinate in ethylcellulose for controlled release. Int J Pharm. 2006;308(1-2):115-23. doi: 10.1016/j.ijpharm.2005.10.034, PMID 16326055.

Iqbal Z, Babar A, Ashraf M. Controlled-release naproxen using micronized ethylcellulose by wet-granulation and solid-dispersion method. Drug Dev Ind Pharm. 2002;28(2):129-34. doi: 10.1081/ddc-120002445, PMID 11926356.

Qushawy M, Nasr A, Swidan S, Mortagi Y. Development and characterization of glimepiride novel solid nanodispersion for improving its oral bioavailability. Sci Pharm. 2020;88(4):1-17. doi: 10.3390/scipharm88040052.

Patil SA, Kuchekar BS, Chabukswar AR, Jagdale SC. Formulation and evaluation of extended-release solid dispersion of metformin hydrochloride. J Young Pharm. 2010;2(2):121-9. doi: 10.4103/0975-1483.63147, PMID 21264113.

Rathinaraj BS, Rajveer CH, Choudhury PK, Sheshrao GB, Shinde GV. Studies on dissolution behavior of sustained-release solid dispersions of nimodipine. Int J Pharm Sci Rev Res. 2010;3(1):77-82.

Srinivas M, Singh A. Enhancement of solubility and dissolution rate of BCS class-II fluvoxamine tablets using solvent evaporation solid dispersion technique. J Pharm Res Int. 2021;33(31B):44-53. doi: 10.9734/jpri/2021/v33i31B31689.

Jain S, Jain S, Mishra A, Gopal G, Kumar MR. Formulation and characterization of fast disintegrating tablets containing cefdinir solid dispersion. Int J Pharm Life Sci. 2012;3(12):2190-9.

Kumar S, Nagpal M, Nagpal K, Dhingra GA. Sustained release solid dispersions of pentoxifylline: formulation and optimization. JPTRM. 2014;2(1):13-28. doi: 10.15415/jptrm.2014.21002.

Momoh MA, Ugwu CE, Jackson TC, Udodiri NC. Sustained release formulation of metformin-solid dispersion based on gelucire 50/13- PEG4000: an in vitro study. IJDD 2017;9(3). doi: 10.5138/09750215.2162.

Shah M, Patel D. Design and evaluation of fast dissolving tablet containing tadalafil solid dispersion. Crit Rev. 2020;7(2):579-82.

Raj AR, Harindran DJ. Formulation and evaluation of carvedilol solid dispersion tablets for solubility enhancement. Eur J Biomed Pharm Sci. 2017;4(2):337-48.

Valleri M, Mura P, Maestrelli F, Cirri M, Ballerini R. Development and evaluation of glyburide fast dissolving tablets using solid dispersion technique. Drug Dev Ind Pharm. 2004;30(5):525-34. doi: 10.1081/ddc-120037483, PMID 15244088.

Patel DM, Patel SP, Patel CN. Formulation and evaluation of fast dissolving tablet containing domperidone ternary solid dispersion. Int J Pharm Investig. 2014;4(4):174-82. doi: 10.4103/2230-973X.143116, PMID 25426438.

Suthar RM, Chotai NP, Shah DD. Formulation and evaluation of fast dissolving tablets of ondansetron by solid dispersion in superdisintegrants. Indian J Pharm Educ Res. 2013;47(3):49-55. doi: 10.5530/ijper.47.3.8.

Elmubarak EH, Osman ZA, Abdelrahman M. Formulation and evaluation of solid dispersion tablets of furosemide using polyvinylpyrrolidone K-30. Int J Curr Pharm Sci 2021;13(2):43-50. doi: 10.22159/ijcpr.2021v13i2.41554.

Mohammadi H, Kumar VH. Formulation and evaluation of solid dispersion incorporated fast disintegrating tablets of tenoxicam using design of experiment. IJPSDR. 2019;11(1):35-44. doi: 10.25004/IJPSDR.2019.110106.

Desu PK, Rao PV, Prasanthi T, Lakshmi GS, Sankar KS, Muneer S. Formulation and evaluation of immediate-release tablets of nevirapine solid dispersions. Arc J Pharm Sci. 2018;4(3):13-20.

Vasanthan M, Narayanasamy D. Development of fast dissolving tablets of nisoldipine by solid dispersion technology using poloxamer 407 and poloxamer 188. J Young Pharm. 2016;8(4):341-9. doi: 10.5530/jyp.2016.4.9.

Sambasivarao A. Formulation and evaluation of immediate-release tablets of glimepiride by using solid dispersion technique using Gelucires. World J Pharm Pharm Sci. 2016;5(5):1659-78.

Suryadevara V, Lankapalli SR, Sunkara S, Sakhamuri V, Danda H. Dissolution rate enhancement of irbesartan and development of fast-dissolving tablets. Egypt Pharm J. 2016;15(3):150-7. doi: 10.4103/1687-4315.197583.

Iyer SR, Sivakumar R, Siva P, Sajeeth CI. Formulation and evaluation of fast dissolving tablets of risperidone solid dispersion. Int J Pharm Chembiol Sci. 2013;3(2):388-97.

Tamboli JA, Mohite SK. Immediate release solid dispersion tablet of azilsartan: formulation strategy to enhance oral bioavailability. Int J Appl Pharm. 2020;12(4):126-34. doi: 10.22159/ijap.2020v12i4.37695.

Suryawanshi S, Sonawane J, Shaikh S, Shaikh H. Design preparation and formulation of piroxicam solid dispersion. Asian J Pharm Technol. 2021;11(1):27-35. doi: 10.5958/2231-5713.2021.00005.2.

Annepogu H, Ahad HA, Nayakanti D. Determining the best poloxamer carrier for thiocolchicoside solid dispersions. Turk J Pharm Sci. 2020;17(4):372-80. doi: 10.4274/tjps.galenos.2019.78800, PMID 32939132.

Cho JH, Kim YI, Kim DW, Yousaf AM, Kim JO, Woo JS, Yong CS, Choi HG. Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged-release tablet. Eur J Pharm Sci. 2014;54:1-7. doi: 10.1016/j.ejps.2013.12.016, PMID 24388864.

Tran HTT, Park JB, Hong KH, Choi HG, Han HK, Lee J, Oh KT, Lee BJ. Preparation and characterization of pH-independent sustained release tablet containing solid dispersion granules of a poorly water-soluble drug. Int J Pharm. 2011;415(1-2):83-8. doi: 10.1016/j.ijpharm.2011.05.052, PMID 21641985.

Tran PHL, Tran TTD, Piao ZZ, Vo TV, Park JB, Lim J, Oh KT, Rhee YS, Lee BJ. Physical properties and in vivo bioavailability in human volunteers of isradipine using controlled release matrix tablet containing self-emulsifying solid dispersion. Int J Pharm. 2013;450(1-2):79-86. doi: 10.1016/j.ijpharm.2013.04.022, PMID 23612354.

Tanaka N, Imai K, Okimoto K, Ueda S, Tokunaga Y, Ohike A, Ibuki R, Higaki K, Kimura T. Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine. J Control Release. 2005;108(2-3):386-95. doi: 10.1016/j.jconrel.2005.08.024, PMID 16253377.

Zhao Y, Xin T, Ye T, Yang X, Pan W. Solid dispersion in the development of a nimodipine delayed-release tablet formulation. Asian J Pharm Sci. 2014;9(1):35-41. doi: 10.1016/j.ajps.2013.11.006.

Tahseen F, Gangurde AB. Formulation development and in vitro evaluation of sustained-release tablets of carvedilol solid dispersion. Int J Pharm Res Allied Sci. 2014;3(4):52-61.

Liu H, Du K, Li D, Du Y, Xi J, Xu Y, Shen Y, Jiang T, Webster TJ. A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology. Int J Nanomedicine. 2018;13:8379-93. doi: 10.2147/IJN.S181002, PMID 30587966.

Latha MM, Sundar VD, Kumar SN, Dhana M. Design and evaluation of sustained-release tablets containing solid dispersion of ziprasidone hydrochloride. Int J Pharm Tech Res. 2014;6(3):959-68.

Published

15-03-2022

How to Cite

SARKAR, P., S. DAS, and S. B. MAJEE. “SOLID DISPERSION TABLETS IN IMPROVING ORAL BIOAVAILABILITY OF POORLY SOLUBLE DRUGS”. International Journal of Current Pharmaceutical Research, vol. 14, no. 2, Mar. 2022, pp. 15-20, doi:10.22159/ijcpr.2022v14i2.1961.

Issue

Section

Review Article(s)