Abstract：Rifapentine crystals with different habits were prepared by recrystallization from selected solvents, such as methanol, ethanol, chloroform, and acetic acid. Scanning electron microscopy, X-ray powder diffractometry, infrared spectrometry, and differential scanning calorimetry were used to investigate the physicochemical characteristics of the prepared crystals. The comparative dissolution behaviors of the newly developed crystals and of rifapentine without being treated were also studied. Results show that the newly developed crystals were different from each other with respect to physical properties but were identical chemically. Needle-shaped crystals were obtained from methanol, ethanol, and chloroform solvents, and the block-shaped crystals were obtained from acetic acid solvent. X-ray diffraction spectra and differential scanning calorimetry investigation on those developed crystals clearly indicate that rifapentine has different crystal structure modification. When the crystal was obtained from acetic acid, the change of crystal habit was originated from the crystal structure modification. The dissolution rate of newly developed crystals was found to be higher than that of rifapentine without being treated. However, the modified crystal obtained from acetic acid shows the lower dissolution rate than crystals obtained from other solvents.
出版日期: 2010-03-05
引用本文:
. Crystal modification of rifapentine using different
solvents[J]. Front. Chem. Sci. Eng., 2010, 4(1): 65-69.
Kun ZHOU, Jun LI, Jianhong LUO, Dongsheng ZHENG, . Crystal modification of rifapentine using different
solvents. Front. Chem. Sci. Eng., 2010, 4(1): 65-69.
Kapoor A, Majumdar D K, Yadav, M R. Crystal forms of nimesulide-asulfonanilide (non-steriodalanti inflammatory drug). Indian J Chem, 1988, 37B: 572–575
Shekunov B Y, Grant D J W, Latham R J, Sherwood J N. In situ optical interferometric studiesof the growth and dissolution behavior of paracetamol (acetaminophen)crystals. 3: Influence of growth in the presence of p-acetoxyacetanilide. J Phys Chem, 1997, B101: 9107–9112 doi: 10.1021/jp9720505
Nokhodchi A, Bolourtchian N, Dinarvand R. Crystal modification of phenytoin using different solventsand crystallization conditions. Int J Pharm, 2003, 250: 85–97 doi: 10.1016/S0378-5173(02)00488-X
Adhiyaman R, Basu S K. Crystal modification of dipyridamoleusing different solvents and crystallization conditions. Int J Pharm, 2006, 321: 27–34 doi: 10.1016/j.ijpharm.2006.04.021
Finnie S, Ristic R I, Sherwood J N, Zikic A M. Characterisationof growth behaviour of small paracetamol crystals grown from puresolutions. Chem Eng Res Design (Trans IChemE), 1996, A74: 835–838
Chen J X, Wang J K, Zhang Y, Wu H, Chen W, Guo Z C. Crystal growth, structure and morphology of hydrocortisone methanolsolvate. J Crystal Growth, 2004, 265: 266–273 doi: 10.1016/j.jcrysgro.2004.01.055
Prasad K V R, Ristic R I, Sheen D B, Sherwood J N. Crystallization of paracetamol from solution in the presence andabsence of impurity. Int J Pharm, 2001, 215: 29–24 doi: 10.1016/S0378-5173(00)00653-0
Chow A H L, Grant D J W. Modification of acetaminophencrystals. III: Influence of initial supersaturation during solution-phasegrowth on crystal properties in the presence and absence of p-acetoxyacetanilide. Int J Pharm, 1988, 42: 123–133 doi: 10.1016/0378-5173(88)90168-8
Zhou K, Li J, Ren Y S. Solubility of rifapentine in different organic solvents. J Chem Eng Data, 2008, 53: 998–999 doi: 10.1021/je7007457
Zhou K, Li J, Zheng D S. Solubility of rifapentine in the binary system of aceticacid and n-octanol solvent mixtures. J Chem Eng Data, 2008, 53: 1978–1979 doi: 10.1021/je8002578
Nie Q, Wang J K, Wang Y L, Bao Y. Effects ofsolvent and impurity on crystal habit Modification of 11α-Hydroxy-16α, 17α-epoxyprogesterone. Chin J Chem Eng, 2007, 15: 648–653 doi: 10.1016/S1004-9541(07)60140-2
Hassan M A, Salem M S, Sueliman M S, Najib N M. Characterizationof famotidine polymorphic forms. Int JPharm, 1997, 149: 227–232 doi: 10.1016/S0378-5173(97)04872-2
Dalton J T, Straughn A B, Dickason D A, Grandolfi G P. Predictive ability of level A in vitro-in vivo correlation for ringcapcontrolled-release acetaminophen tablets. Pharm Res, 2001, 18: 1729–1734 doi: 10.1023/A:1013326714345
