수용성 고분자 PVP K-30로 제조된 레르카니디핀 고체분산체의 용출 특성

정현기; 박진영; 김수영; 차세롬; 이선의; 장나금; 이원택; 이진표; 송정은; 강길선; Hyun Ki Jeong; Jin Young Park; Su Young Kim; Se Rom Cha; Seon Eui Lee; Na Keum Jang; Won Taek Lee; Jin Pyo Lee; Jeong Eun Song; Gilson Khang

Polymer(Korea), Vol.40, No.1, 33-41, January, 2016

DOI10.7317/pk.2016.40.1.33 Export Citation

수용성 고분자 PVP K-30로 제조된 레르카니디핀 고체분산체의 용출 특성

Dissolution Properties of Lercanidipine Solid Dispersion Manufactured Water . Soluble Polymer PVP K-30

정현기, 박진영, 김수영, 차세롬, 이선의, 장나금, 이원택, 이진표, 송정은 , 강길선 ^†

전북대학교 BIN융합공학과, 고분자나노공학과

Hyun Ki Jeong, Jin Young Park, Su Young Kim, Se Rom Cha, Seon Eui Lee, Na Keum Jang, Won Taek Lee, Jin Pyo Lee, Jeong Eun Song , and Gilson Khang^†

Dept. of BIN Fusion Technology and Dept. of Polymernano Science & Technology, Chonbuk National University, 567 Baekje-daero, Jeonju 54898, Korea

E-mail:

초록

레르카니디핀 염산염은 디하이드로 피리딘의 칼슘채널 차단제로서 혈액이 체내에서 더 자유롭게 순환할 수 있도록 혈관을 확장시켜주는 고혈압 치료제이다. 레르카니디핀은 난용성 약물로 약물 전달 시스템에 적용하는데에 어려움이 많다. 이번 연구에 있어서 우리는 레르카니디핀에 수용성 고분자인 PVP K-30을 첨가하여 용출률을 개선시키기 위한 방법으로 분무건조와 회전증발법을 이용한 고체 분산체를 제조하였다. 또한 물질의 방출 거동은 invitro로 평가하였으며 재료의 용출 거동 결과에서 고체분산체는 약물의 화학 구조 변화로 인하여 물질의 용해도가 증가되는 것으로 나타났다.

Lercanidipine hydrochloride is a calcium channel blocker of the dihydropyridine, which opens the blood vessels for allowing the blood to circulate more freely around the body. Lercanidipine is a poorly water soluble drug and quite difficult to deliver. Taking this into account, in the study, we have designed lercanidipine loaded water soluble polymer PVP K-30 via solid dispersion method using spray drying and rotary evaporation to improve the dissolution properties. Further, the dissolution behavior of the materials were evaluated by in vitro assays. Results showed that solid dispersion has increased the dissolution properties of the materials owing to the change in the drug chemical structure.

Keywords:lercanidipine;PVP K30;solid dispersion;spray drying;rotary evaporation

[References]

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Gannu R, Palem CR, Yamsani VV, Yamsani SK, Yamsani MR, Int. J. Pharm., 388, 231 (2010)
Parmar N, Amin S, Singla N, Kohli K, Pharm. Develop. Tech., 17, 730 (2012)
Kaila HO, Ambasana MA, Thakkar RS, Saravaia HT, Shah AK, Indian J. Pharm. Sci., 72, 381 (2010)
Janssens S, Anne M, Rombaut P, Mooter G, Eur. J. Pharm. Sci., 37, 241 (2009)
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Park JS, Park JY, Kim HM, Oh SC, Yang J, Lee CJ, Jeong HK, Khang G, Inter. J. Tissue Regen., 5, 31 (2014)
Calahan JL, Zanon RL, Alvarez-Nunez F, Munson EJ, Molecul. Pharm., 10, 1949 (2013)
Shastri PN, Kim MC, Quan FS, D'Souza MJ, Kang SM, J. Pharm. Sci., 101, 3623 (2012)
El-Badry M, Fathy M, Drug Dev. Ind. Pharm., 32, 141 (2006)
Ochi M, Kawachi T, Toita E, Hashimoto I, Yuminoki K, Onoue S, Hashimoto N, Int. J. Pharm., 474, 151 (2014)
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Thybo P, Pedersen BL, Hovgaard L, Holm R, Mullertz A, Pharm. Develop. Tech., 13, 375 (2008)
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Hardy IJ, Windberg-Baarup A, Neri C, Byway PV, Booth SW, Fitzpatrick S, Int. J. Pharm., 337, 246 (2007)
Beck-Broichsitter M, Ruppert C, Schmehl T, Gunther A, Seeger W, Acta Biomater., 10, 4678 (2014)
Ozguney I, Kardhiqi A, Yildiz G, Ertan G, Eur. J. Drug Met. Pharm., 39, 283 (2013)
Lee EY, Oh MJ, Kim SH, Seong KY, Lee YH, Kim SJ, She HS, Lee D, Khang G, Polym.(Korea), 35(2), 113 (2011)
Muller CR, Schaffazick SR, Pohlmann AR, de L. Freitas L, da Silveira NP, Costa TD, Guterres SS, Die Pharmazie, 56, 864 (2001)
Shim JB, Lee JK, Jo H, Hwang JH, Jeong SM, Jo JI, Lee D, Yuk SH, Khang G, Macromol. Res., 21, 42 (2012)
Giovagnoli S, Palazzo F, Michele AD, Schoubben A, Blasi P, Ricci M, J. Pharm. Sci., 103, 1255 (2014)
Khang G, Rhee JM, Jeong JK, Lee JS, Kim MS, Cho SH, Lee HB, Macromol. Res., 11(4), 207 (2003)
Jain SK, Gupta Y, Jain A, Rai K, Drug Deliv., 15, 141 (2008)
Chambers RE, Clamp JR, Biochem. J., 125, 1009 (1971)
Nichols AV, Lux S, Forte T, Gong E, Levy RI, Biochim. Biophys. Acta, 270, 132 (1972)
Cheuka PM, Cabrera DG, Paquet T, Chibale K, Bioorg. Med. Chem. Lett., 24, 5207 (2014)
Martinez JO, Evangelopoulos M, Bhavane R, Acciardo S, Salvatore F, Liu X, Ferrari M, Tasciotti E, Curr. Drug Targets, 15, 13 (2014)
Heng D, Lee SH, Ng WK, Tan RB, Expert Opin. Drug Del., 8, 965 (2011)
Shin JH, Lee HG, Lee SU, Kim SY, Jeong HK, Lee DH, Lee D, Khang G, Inter. J. Tissue Regen., 6, 19 (2014)
Tamilvanan S, Bangale GS, Ananthi JJ, Sivakumar V, Vinothapooshan G, Palanivelu M, Viswanathan MB, J. Pharm. Sci. Tech., 63, 196 (2009)
Oh MJ, Shim JB, Yoo H, Lee GY, Jo H, Jeong SM, Yuk SH, Lee D, Khang G, Macromol. Res., 20(8), 835 (2012)

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