Release behavior of cilostazol according to the fabrication methods and ratio of HPMC/PVP

Guk Bin Park; Hyeon Yoon; Jung Woo Bae; Young Un Kim; Dae Yeon Jeon; Jeong Eun Song; Dongwon Lee; Gilson Khang

Macromolecular Research, Vol.21, No.9, 971-976, September, 2013

DOI10.1007/s13233-013-1126-2 Export Citation

Release behavior of cilostazol according to the fabrication methods and ratio of HPMC/PVP

Guk Bin Park, Hyeon Yoon, Jung Woo Bae, Young Un Kim, Dae Yeon Jeon, Jeong Eun Song , Dongwon Lee , and Gilson Khang^†

Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, Chonbuk National University, Jeonbuk, 561-756, Korea

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In this study, we manufactured a polymer blend, using hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (PVP), by spray drying method to improve the characteristics of polymers. This polymer blend was used to improve the drug delivery of cilostazol, a phosphodiesterase inhibitor that decreases serum triglycerides, is a direct arterial vasodilator, and inhibits platelet aggregation and smooth muscle cell proliferation. Compatibility with this drug was achieved when the polymer blend of HPMC and PVP were spray dried. Various ratios of the two ingredients were blended to determine optimum release rate of this poorly soluble drug. Cilostazol blended with different ratios of HPMC and PVP was analyzed by scanning electron microscopy (SEM) and transmission electron microscopy (TEM) to confirm surface morphology and combination of drug and polymer. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) were conducted to confirm thermodynamic properties and chemical structure change, respectively. Change in the drug release of cilostazol was expected by adjusting the HPMC and PVP blend ratio in gastric juice (pH 1.2).

Keywords:cilostazol;hydroxypropyl methylcellulose (HPMC);polyvinylpyrrolidone (PVP);solid dispersion;blend

[References]

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Fujimura M, Kamio Y, Saito M, Hashimoto T, Matsuda T, Am. J. Respir. Crit. Care Med., 51, 222 (1995)
Shimizu T, Osumi T, Niimi K, Nakagawa K, Arzneimittelforschung, 35, 1117 (1985)
Uchikawa T, Murakami T, Furukawa H, Arzneimittelforschung, 42, 322 (1992)
Sakurai K, Maegawa T, Takahashi T, Polymer, 41(19), 7051 (2000)
Nyamweya N, Hoag SW, Pharm. Res., 17, 625 (2000)
Fox TG, Bull. Am. Phys. Soc., 1, 123 (1956)
Gordon M, Taylor JS, J. Appl. Chem., 2, 493 (1952)
Karavas E, Georgarakis E, Bikiaris D, J. Therm. Anal. Calorim., 84, 125 (2006)
Van den Mooter G, Weuts I, De Ridder T, Blaton N, Int. J. Pharm., 316, 1 (2006)
Morris KR, Griesser UJ, Eckhardt CJ, Stowell JG, Adv. Drug Deliv. Rev., 48, 91 (2001)

[Related Articles]

[1] Lee WF, Tu YM, J. Appl. Polym. Sci., 76(2), 170 (2000)

[2] Siepmann J, Peppas NA, Adv. Drug Deliv. Rev., 48, 139 (2001)

[3] Karavas E, Georgarakis E, Bikiaris B, Thomas T, Katsos VD, Xenakis A, Prog. Colloid Polym. Sci., 118, 149 (2001)

[4] Okimoto K, Miyake M, Ibuki R, Yasumura M, Ohnishi N, Nakai T, Int. J. Pharm., 159, 85 (1997)

[5] Mitchell SA, Reynolds TD, Dasbach TP, Int. J. Pharm., 250, 3 (2003)

[6] Itai S, Nemoto M, Kouchiwa S, Chem. Pharm. Bull., 33, 5464 (1985)

[7] Kleinebudde P, Int. J. Pharm., 96, 119 (1993)

[8] Ravin HA, Seligman AM, Fine J, Engl. J. Med., 247, 921 (1952)

[9] Sethia S, Squillante E, Int. J. Pharm., 272, 1 (2004)

[10] Valero M, Revuelta BI, Rodrigues LJ, Int. J. Pharm., 253, 97 (2003)

[11] Ford LJ, Drug Dev. Ind. Pharm., 13, 9 (1987)

[12] Shin SC, Oh IJ, Koh IB, J. Kor. Pharmaceut. Sci., 20, 193 (1990)

[13] Mura P, Manderioli A, Bramanti G, Ceccareli L, Drug Dev. Ind. Pharm., 22, 909 (1996)

[14] Moneghini M, Carcano A, Zingone G, Perissutti B, Int. J. Pharm., 175, 177 (1988)

[15] Serajuddin ATM, Sheen PC, Augustine MA, J. Pharm. Sci., 77, 414 (1988)

[16] Timkom RJ, Lord NG, J. Pharm. Sci., 68, 601 (1979)

[17] Akibama H, Kudo S, Shimizu T, Arzneimittelforschung, 35, 1133 (1985)

[18] Fujimura M, Kamio Y, Saito M, Hashimoto T, Matsuda T, Am. J. Respir. Crit. Care Med., 51, 222 (1995)

[19] Shimizu T, Osumi T, Niimi K, Nakagawa K, Arzneimittelforschung, 35, 1117 (1985)

[20] Uchikawa T, Murakami T, Furukawa H, Arzneimittelforschung, 42, 322 (1992)

[21] Sakurai K, Maegawa T, Takahashi T, Polymer, 41(19), 7051 (2000)

[22] Nyamweya N, Hoag SW, Pharm. Res., 17, 625 (2000)

[23] Fox TG, Bull. Am. Phys. Soc., 1, 123 (1956)

[24] Gordon M, Taylor JS, J. Appl. Chem., 2, 493 (1952)

[25] Karavas E, Georgarakis E, Bikiaris D, J. Therm. Anal. Calorim., 84, 125 (2006)

[26] Van den Mooter G, Weuts I, De Ridder T, Blaton N, Int. J. Pharm., 316, 1 (2006)

[27] Morris KR, Griesser UJ, Eckhardt CJ, Stowell JG, Adv. Drug Deliv. Rev., 48, 91 (2001)