Enhancement of solubility and dissolution of cilostazol by solid dispersion technique

详细信息    查看全文

• 作者：Jun-Hyung Park ; Hoo-Kyun Choi
• 关键词：Cilostazol ; Solid dispersion ; Spray drying ; Solubility ; Dissolution
• 刊名：Archives of Pharmacal Research
• 出版年：2015
• 出版时间：July 2015
• 年：2015
• 卷：38
• 期：7
• 页码：1336-1344
• 全文大小：1,011 KB
• 参考文献：Amidon, G.L., H. Lennernas, V.P. Shah, and J.R. Crison. 1995. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharmaceutical Research 12: 413-20.PubMed View Article
  Chiou, W.L., and S. Riegelman. 1971. Pharmaceutical applications of solid dispersion systems. Journal of Pharmaceutical Sciences 60: 1281-302.PubMed View Article
  Chow, A.H.L., C.K. Hsia, J.D. Gordon, J.W.M. Young, and E.I. Vargha-Butler. 1995. Assessment of wettability and its relationship to the intrinsic dissolution rate of doped phenytoin crystals. International Journal of Pharmaceutics 126: 21-8.View Article
  Davis, S.S. 1986. Transit of pharmaceutical dosage forms through the small intestine. Gut 27: 886.PubMed Central PubMed View Article
  Dindyal, S., and C. Kyriakides. 2009. A review of cilostazol, a phosphodiesterase inhibitor, and its role in preventing both coronary and peripheral arterial restenosis following endovascular therapy. Recent Patents on Cardiovascular Drug Discovery 4: 6-4.PubMed View Article
  Ghebremeskel, A.N., C. Vemavarapu, and M. Lodaya. 2007. Use of surfactants as plasticizers in preparing solid dispersions of poorly soluble API: Selection of polymer-surfactant combinations using solubility parameters and testing the processability. International Journal of Pharmaceutics 328: 119-29.PubMed View Article
  Hamming, J.J. 1959. Intermittent claudication at an early age, due to an anomalous course of the popliteal artery. Angiology 10: 369.PubMed View Article
  Hasegawa, A., M. Taguchi, R. Suzuki, T. Miyata, H. Nakagawa, and I. Sugimoto. 1988. Supersaturation mechanism of drugs from solid dispersions with enteric coating agents. Chemical & Pharmaceutical Bulletin 36: 4941-950.View Article
  Jinno, J., N. Kamada, M. Miyake, K. Yamada, T. Mukai, M. Odomi, H. Toguchi, G.G. Liversidge, K. Higaki, and T. Kimura. 2006. Effect of particle size reduction on dissolution and oral absorption of a poorly water-soluble drug, cilostazol, in beagle dogs. Journal of Controlled Release 111: 56-4.PubMed View Article
  Joe, J.H., W.M. Lee, Y.-J. Park, K.H. Joe, D.H. Oh, Y.G. Seo, J.S. Woo, C.S. Yong, and H.-G. Choi. 2010. Effect of the solid-dispersion method on the solubility and crystalline property of tacrolimus. International Journal of Pharmaceutics 395: 161-66.PubMed View Article
  Kim, M.-S., S. Lee, J.-S. Park, J.-S. Woo, and S.-J. Hwang. 2007. Micronization of cilostazol using supercritical antisolvent (SAS) process: Effect of process parameters. Powder Technology 177: 64-0.View Article
  Kimura, Y., T. Tani, T. Kanbe, and K. Watanabe. 1985. Effect of cilostazol on platelet aggregation and experimental thrombosis. Arzneimittel-Forschung 35: 1144-149.PubMed
  Konno, H., T. Handa, D.E. Alonzo, and L.S. Taylor. 2008. Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine. European Journal of Pharmaceutics and Biopharmaceutics 70: 493-99.PubMed View Article
  Leuner, C., and J. Dressman. 2000. Improving drug solubility for oral delivery using solid dispersions. European Journal of Pharmaceutics and Biopharmaceutics 50: 47-0.PubMed View Article
  Marques, M. 2004. Dissolution media simulating fasted and fed states. Dissolution Technologies 11: 16.View Article
  Moustafine, R.I., T.V. Kabanova, V.A. Kemenova, and G. Van Den Mooter. 2005. Characteristics of interpolyelectrolyte complexes of Eudragit E100 with Eudragit L100. Journal of Controlled Release 103: 191-98.PubMed View Article
  Park, Y.-J., D.-H. Oh, Y.-D. Yan, Y.-G. Seo, S.-N. Lee, H.-G. Choi, and C.-S. Yong. 2010. Surface-attached solid dispersion. Journal of Pharmaceutical Investigation 40: 103-12.View Article
  Patel, S.G., and S.J. Rajput. 2009. Enhancement of oral bioavailability of cilostazol by forming its inclusion complexes. AAPS PharmSciTech 10: 660-69.PubMed Central PubMed View Article
  Pouton, C.W. 2006. Formulation of poorly water-soluble drugs for oral administration: Physicochemical and physiological issues and the lipid formulation classification system. European Journal of Pharmaceutical Sciences 29: 278-87.PubMed View Article
  Quadir, A., and K. Kolter. 2006. A comparative study of current superdisintegrants. Pharmaceutical Technology 30: s38–s42.
  Sekiguchi, K., and N. Obi. 1961. Studies on absorption of eutectic mixture. I. A comparison of the behavior of eutectic mixture of sulfathiazole and that of ordinary sulfathiazole in man. Chemical & Pharmaceutical Bulletin 9: 866-72.View Article
  Serajuddin, A.T.M., P.-C. Sheen, and M.A. Augustine. 1990. Improved dissolution of a poorly water-soluble drug from solid dispersions in polyethylene glycol: Polysorbate 80 mixtures. Journal of Pharmaceutical Sciences 79: 463-64.PubMed View Article
  Shimizu, T., T. Osumi, K. Niimi, and K. Nakagawa. 1985. Physico-chemical properties and stability of cilostazol.
• 作者单位：Jun-Hyung Park (1)
  Hoo-Kyun Choi (1)
  
  1. College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-Gu, Gwangju, 501-759, Korea
  
• 刊物主题：Pharmacy; Pharmacology/Toxicology;
• 出版者：Springer Netherlands
• ISSN：1976-3786

文摘

Cilostazol is practically insoluble in water and thus results in poor bioavailability. Only a few approaches have been reported for improving the bioavailability of cilostazol. Solid dispersion technique via solvent evaporation method was applied to improve the solubility and dissolution of cilostazol. Various polymers, mixture of polymer and surfactant, and mixture of polymers were screened as a carrier for the solid dispersion. Solubility of cilostazol was improved significantly when Eudragit? L100 was used as a carrier. However, addition of surfactant to Eudragit? L100 decreased the solubility slightly. Whereas, the mixture of Eudragit? L100 and Eudragit? S100 as a carrier system further increased the solubility. Based on the highest solubility obtained among the carriers screened, 1:1 ratio of Eudragit? L100 and Eudragit? S100 was selected as a carrier, and drug to carrier ratio was optimized to 1:5. Differential scanning calorimetry and X-ray diffraction studies showed that the characteristic peak of cilostazol disappeared in the solid dispersion, indicating that cilostazol existed in amorphous form in this formulation. Spray drying method was superior to vacuum drying method in terms of dissolution rate. Meanwhile, it was observed that the disintegration rate and the concentration of polymer had some effect on the crystallization of cilostazol in dissolution medium. Tablet formulation containing spray dried solid dispersion showed significant improvement in dissolution as compared to the commercial tablet.