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Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

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Abstract

Colloidal solid dispersion is an innovative breakthrough in the pharmaceutical industry that overcomes the solubility-related issue of poorly soluble drugs by using an amorphous approach and also the stability-related issue by means of a complex formation phenomenon using different carrier materials. In the present study, a newly developed adsorption method is introduced to incorporate a high-energy sulfathiazole–polyvinylpyrrolidone (Plasdone® K-29/32) solid dispersion on porous silicon dioxide (Syloid® 244FP). Different ternary systems of sulfathiazole–Plasdone® K-29/32–Syloid® 244FP were prepared (1:1:2, 1:1:3, and 1:2:2) and categorized depending on the mechanism by which Syloid® 244FP was incorporated. Modulated differential scanning calorimetry (MDSC), X-ray diffraction, Fourier transform infrared spectroscopy, and in vitro dissolution studies were conducted to characterize the ternary systems. The X-ray diffraction and MDSC data showed a lack of crystallinity in all internal and external ternary systems, suggesting a loss of the crystallinity of sulfathiazole compared to the physical mixtures. USP apparatus II was used to measure the in vitro dissolution rate of the prepared systems at 75 rpm in different media. The dissolution rate of the optimum ratio (1:2:2) containing an internal ternary solid dispersion system was found to be three times higher than that of the external and physical systems. Thus, the porous silicon dioxide incorporated into the conventional binary solid dispersion acted as a carrier to disperse the complex and increase the dissolution rate.

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REFERENCES

  1. Arnum P. Solubilizing the insoluble. Pharm Technol. 2010;34(11):50–6.

    Google Scholar 

  2. Dare J. Particle size in relation to formulation. Australas J Pharm. 1964;45:S58–65.

    CAS  Google Scholar 

  3. Kai T, Akiyama Y, Nomura S, Sato M. Oral absorption improvement of poorly soluble drug using solid dispersion technique. Chem Pharm Bull. 1996;44:568–71.

    Article  PubMed  CAS  Google Scholar 

  4. Serajuddin A. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J Pharm Sci. 1999;88:1058–66.

    Article  PubMed  CAS  Google Scholar 

  5. Chiou W, Riegelman S. Pharmaceutical application of solid dispersion systems. J Pharm Sci. 1971;60:1281–302.

    Article  PubMed  CAS  Google Scholar 

  6. Noyes A, Whitney W. The rate of solution of solid substances in their own solutions. J Am Chem Soc. 1897;19:930–4.

    Article  Google Scholar 

  7. 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.

    Article  CAS  Google Scholar 

  8. Vasconcelos T, Sarmento B, Costa P. Solid dispersion as the strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today. 2010;12:1068–75.

    Article  Google Scholar 

  9. Leuner C, Dressman J. Improving drug solubility using solid dispersion. Eur J Pharm Biopharm. 2000;50:47–60.

    Article  PubMed  CAS  Google Scholar 

  10. Gupta M, Goldman D, Bogner R, Tseng Y. Enhanced drug dissolution and bulk properties of solid dispersions granulated with a surface adsorbent. Pharm Dev Technol. 2001;6:563–72.

    Article  PubMed  CAS  Google Scholar 

  11. Prabhu S, Brocks D, Betageri G. Enhancement of dissolution of ethopropazine using solid dispersions prepared with phospholipid and/or polyethylene glycol. Drug Dev Ind Pharm. 2001;27:413–8.

    Article  PubMed  CAS  Google Scholar 

  12. Hirasawa N, Ishise S, Miyata H, Danjo K. An attempt to stabilize nilvadipine solid dispersion by the use of ternary systems. Drug Dev Ind Pharm. 2003;29:997–1004.

    Article  PubMed  CAS  Google Scholar 

  13. Okonogi S, Puttipipatkhachorn S. Dissolution improvement of high drug-loaded solid dispersion. AAPS PharmSciTech. 2006;7:E1–6.

    Article  Google Scholar 

  14. Chutimaworapan S, Ritthidej G, Yonemochi E, Oguchi T, Yamamoto K. Effect of water-soluble carriers on dissolution characteristics of nifedipine solid dispersions. Drug Dev Ind Pharm. 2000;26(11):1141–50.

    Article  PubMed  CAS  Google Scholar 

  15. Lalitha Y, Lakshmi P. Enhancement of dissolution of nifedipine by surface solid dispersion technique. Int J Pharm Pharm Sci. 2011;3 Suppl 3:41–6.

    CAS  Google Scholar 

  16. Elbary A, Salem H, Maher M. In vitro and in vivo evaluation of glibenclamide using surface solid dispersion (SSD) approach. Br J Pharmacol Toxicol. 2011;2(1):51–62.

    Google Scholar 

  17. Wang L, Cui F, Sunada H. Preparation and evaluation of solid dispersions of nitrendipine prepared with fine silica particles using the melt-mixing method. Chem Pharm Bull. 2006;54:37–43.

    Article  PubMed  Google Scholar 

  18. Kim K, Frank M, Henderson N. Application of differential scanning calorimetry to the study of solid drug dispersions. J Pharm Sci. 1985;74(3):283–9.

    Article  PubMed  CAS  Google Scholar 

  19. Takeuchi H, Nagira S, Yamamoto H, Kawashima Y. Solid dispersion particles of amorphous indomethacin with fine porous silica particles prepared by using spray-drying method. Int J Pharm. 2005;293:155–64.

    Article  PubMed  CAS  Google Scholar 

  20. Takeuchi H, Nagira S, Yamamoto H, Kawashima Y. Solid dispersion particles of tolbutamide prepared with fine silica particles by the spray-drying method. Powder Technol. 2004;141:187–95.

    Article  CAS  Google Scholar 

  21. Simonell A, Mehta S, Higuchi W. Inhibition of sulfathiazole crystal growth by polyvinylpyrrolidone. J Pharm Sci. 1970;59:633–44.

    Article  Google Scholar 

  22. Simonelli A, Mehta S, Higuchi W. Dissolution rate of high energy polyvinylpyrrolidone (PVP)–sulfathiazole coprecipitates. J Pharm Sci. 1969;58:538–49.

    Article  PubMed  CAS  Google Scholar 

  23. 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.

    Article  PubMed  CAS  Google Scholar 

  24. Bakara M, Nagya Z, Rielly C, Dann S. Investigation of the riddle of sulfathiazole polymorphism. Int J Pharm. 2011;414:86–103.

    Article  Google Scholar 

  25. Tantishaiyakul V, Kaewnopparat N, Ingkatawornwong S. Properties of solid dispersions of piroxicam in polyvinylpyrrolidone K-30. Int J Pharm. 1996;143:59–66.

    Article  CAS  Google Scholar 

  26. Karavas E, Ktistis G, Xenakis A, Georgarakis E. Miscibility behavior and formation mechanism of stabilized felodipine–polyvinylpyrrolidone amorphous solid dispersions. Drug Dev Ind Pharm. 2005;31(6):473–89.

    Article  PubMed  CAS  Google Scholar 

  27. Drooge D, Hinrichs W, Visser M, Frijlink H. Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale, using differential scanning calorimetry and gravimetric water vapour sorption techniques. Int J Pharm. 2006;310:220–9.

    Article  PubMed  Google Scholar 

  28. Feng T, Pinal R, Carvjal MT. Process induced disorder in crystalline materials: differentiating defective crystals from the amorphous form of griseofulvin. J Pharm Sci. 2008;88:1058–66.

    Google Scholar 

  29. Bahl D, Bogner RH. Amorphization alone does not account for the enhancement of solubility of drug co-ground with silicate: the case of indomethacin. AAPS PharmSciTech. 2008;9(1):146–53.

    Article  PubMed  CAS  Google Scholar 

  30. Benchaabane H, Ozer Y, Ozalp M, Kilic E, Polat M, Korkmaz M. Gamma radiation studies on sulfathiazole (powder and model-ophthalmic solution). FABAD J Pharm Sci. 2003;28(2):93–106.

    CAS  Google Scholar 

  31. 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.

    Article  Google Scholar 

  32. Boldyrev V, Shakhtshneider T, Burleva L, Severtsev V. Preparation of the disperse system of sulfathiazole–polyvinylpyrrolidone by mechanical activation. Drug Dev Ind Pharm. 1994;20(6):1103–14.

    Article  CAS  Google Scholar 

  33. Hirasawa N, Ishise S, Miyata H, Danjo K. Physicochemical characterization and drug release studies of nilvadipine solid dispersions using water-insoluble polymer as a carrier. Drug Dev Ind Pharm. 2003;29(3):339–44.

    Article  PubMed  CAS  Google Scholar 

  34. 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.

    Article  PubMed  CAS  Google Scholar 

  35. Zhu L, Wong L, Yu L. Surface-enhanced crystallization of amorphous nifedipine. Mol Pharm. 2008;5(6):921–6.

    Article  PubMed  CAS  Google Scholar 

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Authors and Affiliations

  1. Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, 75 Dekalb Avenue, HS Building 605, Brooklyn, New York, 11201, USA

    Vaibhav I. Patel & Rutesh H. Dave

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  1. Vaibhav I. Patel
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  2. Rutesh H. Dave
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Correspondence to Rutesh H. Dave.

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Patel, V.I., Dave, R.H. Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile. AAPS PharmSciTech 14, 620–628 (2013). https://doi.org/10.1208/s12249-013-9947-z

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  • DOI: https://doi.org/10.1208/s12249-013-9947-z

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