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http://dx.doi.org/10.4333/KPS.2011.41.6.363

Effect of Manufacturing Method and Acidifier on the Dissolution Rate of Carvedilol from Solid Dispersion Formulations  

Lim, Dong-Kyun (Department of BIN Fusion Technology, Department of Polymer Nano Science Technology & Polymer Fusion Research Center, Chonbuk National University)
Bae, Jeong-Woo (Department of BIN Fusion Technology, Department of Polymer Nano Science Technology & Polymer Fusion Research Center, Chonbuk National University)
Song, Byung-Joo (Department of BIN Fusion Technology, Department of Polymer Nano Science Technology & Polymer Fusion Research Center, Chonbuk National University)
Jo, Han-Su (Department of BIN Fusion Technology, Department of Polymer Nano Science Technology & Polymer Fusion Research Center, Chonbuk National University)
Kim, Hyoung-Eun (Department of BIN Fusion Technology, Department of Polymer Nano Science Technology & Polymer Fusion Research Center, Chonbuk National University)
Lee, Dong-Won (Department of BIN Fusion Technology, Department of Polymer Nano Science Technology & Polymer Fusion Research Center, Chonbuk National University)
Khang, Gil-Son (Department of BIN Fusion Technology, Department of Polymer Nano Science Technology & Polymer Fusion Research Center, Chonbuk National University)
Publication Information
Journal of Pharmaceutical Investigation / v.41, no.6, 2011 , pp. 363-369 More about this Journal
Abstract
In this study, we demonstrated the release behavior of carvedilol with the content of polyvinylpyrrolidone K-30 (PVP K-30) and the effect of citric acid and fumaric acid as acidifiers on the release behavior of drug. In addition, it tries to inquire into the release behavior difference of the carvedilol according to the manufacturing method. The release behavior of the tablets was compared with Dilatrand$^{(R)}$ in the simulated gastric fluid (pH1.2). Differential scanning calorimeter (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) were characterized for the physicochemical properties of the tablets. In case of mixing the carvedilol and PVP K-30, in case the ratio of the carvedilol and PVP K-30 was 1:5, the release behavior was the highest among. As well as the dissolution rate of tablets manufactured by lyophilization and rotary evaporator was higher than physical mixture. The dissolution rate of containing acidifiers was more improved. But, rather the excessive amount of the acidifier addition reduced the dissolution rate.
Keywords
Carvedilol; Kollidon K-30; Kollidon CL; Citric acid; Fumaric acid;
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Times Cited By KSCI : 4  (Citation Analysis)
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1 Srinarong, P., Faber, J.H., Visser, M.R., Hinrichs, W.L.J., Frijlinl, H.W., 2009, Strongly enhanced dissolution rate of fenofibrate solid dispersion tablets by incorporation of superdisintegrants, Eur J Pharm BioPharm, 73(1), 154-161.   DOI   ScienceOn
2 Doherty, C., York, P., 1989, Microenvironmental pH control of drug dissolution, Int J Pharm, 50, 223-232.   DOI
3 Siepe, S., Lueckel, B., Kramer, A., Ries, A., Gurny, R., 2006, Strategies for the design of hydrophilic matrix tablets with controlled microenvironmental pH, Int J Pharm, 316, 14-20   DOI
4 Thao, T.D., Phuong, H.L., Choi, H.G., Han, H.K., Lee, B.J., 2010, The role of acidifier in solid dispersion and physical mixtures, Int J Pharm, 384, 60-66.   DOI
5 Cui, Y., Kim, S.S., Park, E.S., Chi, S.C., 2002, Formation of sustained- release matrix tablets of nipedifine, J Kor Pharm Sci, 32(2), 95-101.
6 Virtanen, S., Salokangsa, H., Yliruusi, J., 2008, The effect of mixing time of the magnesium stearate on crushing strengths of tablets, Eur J Pharm Sci, 34S, S25-S29.
7 Guchardi, R., Frei, M., John, E., Kaerger J.S., 2008, Influence of fine lactose and magnesium stearate on low dose dry power inhaler formations, Int J Pharm, 348, 10-17.   DOI
8 Mehrotra, A., Llusa, M., Faqih, A., Levin, M., Muzzio, F.J., 2007, Influence of shear intensity and total shear on properties of blends and tablets of lactose and cellulose lubricated with magnesium stearate, Int J Pharm, 336, 284-291.   DOI
9 Oh, M.J., Shim, J.B., Lee, E.Y., Yoo, H., Cho, W.H., Lim, D.K., Lee, D., Khang, G., 2011, Molecular effect of PVP on the release property of carvedilol solid dispersion, J Pharma Investi, 41(3), 179-184.   DOI
10 Kubo H., Mizobe, M., 1997, Improvement of dissolution rate and oral bioavailability of a sparingly water-soluble drug, (${\pm}$)-5- [[2-(2-naphthalenylmethyl)-5-benzoxazolyl]-methyl]-2,4-thiazolidinedione, in co-ground mixture with D-mannitol, Biol Pharm Bull, 20, 460-463.   DOI
11 Kawashima, Y., Saito M., Takenaka, H., 1975, Improvement of solubility and dissolution rate of poorly water-soluble salicylic acid by a spray-drying technique, J Pharm Pharmacol, 27, 1-5.   DOI
12 Sekiguchi, K., Obi, N., 1961, Studies on the absorption of a eutectic mixture. I. A comparison of the behavior of a eutectic mixture of sulfathiazole and that of ordinary sulfatiazole in man, Chem Pharm Bull, 9, 193-198.
13 Leuner, C., Dressman, J., 2000, Improving drug solubility for oral delivery using solid dispersions, Eur J Pharm Biopharm, 50, 47-60.   DOI
14 Chiou, W.L., Riegelman, S., 1971, Pharmaceutical applications of solid dispersion systems, J Pharm Sci, 60, 1281-1302.   DOI
15 Shah, U., Augsburger, L., 2001, Evaluation of the functional equivalence of crospovidone NF from different sources, Pharm Dev Technol, 6, 39-51.   DOI
16 Hirasawa, N., Ishise, S., Miyata, H., Danjo, K., 2003, Physicochemical characterization and drug release studies of nilvadipine solid dispersions using a water-insoluble polymer as a carrier, Drug Dev Ind Pharm, 29, 339-344.   DOI
17 Jeong, J.K., Khang, G., Rhee, J.M., Shin, H.C., Lee, H.B., 2000. Effect of molecular weight and mixture ratio of PVP on improving the bioavailability of ipriflavone, J Korean Pharm. Sci. 30(4), 235-239.   과학기술학회마을
18 Jeong, J.K., Kim, J.H., Khang, G., Rhee, J.M., Lee, H.B., 2002. The preparation and characterization of solid dispersion of ipriflavone with PVP, J Korean Pharm Sci. 32(3), 173-179.   과학기술학회마을   DOI
19 McTavish, D., Campoli-Richards, D., Sorkin, E.M., 1993, Carvedilol: a review of its pharmacological and pharmacokinetic properties, and therapeutic efficacy, Drugs 45, 232-258.
20 Dunn, C.J., Lea, A.P., Wagstaff, A.J., 1997, Carvedilol: a reappraisal of its pharmacological properties and therapeutical use in cardiovascular disorders, Drugs, 54, 161-185.   DOI
21 Robert, R., Ruffolo, R.R., Boyle, D.A., Brooks, D.P., Feuerstein, G.Z., Venuti, R.P., Lukas M.A., Paste, G., 1992, Carvedilol: a novel cardiovascular drug with multiple actions, Cardiovasc Drug Rev, 10(2), 127-157.   DOI
22 Tanwar, Y.S., Chauhan C.S., Sharma, A., 2007, Development and evaluation of carvedilol transdermal patches, Acta Pharm, 57, 151-159.   DOI
23 Neugebauer, G., Akpan, W., Mollendorff, E.V., Neuber P., Reiff, K., 1987, Pharmacokinetics and disposition of carvedilol in human, J Cardiovas Pharmacol, 10, 85-88.
24 Mcphillips, J.J., Schwerner, G.T., Scott, D.I., Zinny, M., Patterson, K., 1988, Effects of carvedilol on blood pressure in patients with mild to moderate hypertension, Drugs, 36, 82-91.   DOI
25 Kim, S.M., Shin, S.B., Kim, J.H., Kown, I.H., Kim, Y.H., Lee, S.N., Cho H.Y., Lee, Y.B., 2008, Bioequivalence of Cadilan tablet 12.5 mg to Dilatrend tablet 12.5 mg (Carvedilol 12.5 mg), J Kor Pharm Sci, 38(6), 413-419.   과학기술학회마을   DOI
26 Loftsson, T., Vogensen, S.B., Desbos, C., Jansook, P., 2008, Carvedilol: solubilization and cyclodextrin complexation: a technical note, AAPS Pharm Sci Tech, 9, 425-430.   DOI
27 Mura, P., Cirri M., Faucci, M.T., 2002, Investigation of the effects of grinding and co-grinding on physicochemical properties of glisentide, J Pharm Biomed Anal, 30, 227-237.   DOI