Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Preparation and Characterization of Enrofloxacin／Carbopol Complex in Aqueous Solution

  • Published : 2004.06.01
Download PDF
⟨ Previous Next ⟩

Abstract

Since the bitter taste of enrofloxacin apparently limit the patient compliance in the oral formulations of the antibacterial agent, the masking of the taste is essential for the improvement of the therapeutic effectiveness. Therefore, this study was carried out to examine the feasibility of taste masking of enrofloxacin by the retardation of its dissolution rate using the formation of complex between the drug and Carbopol. The complexation between Carbopol and enrofloxacin was confirmed by turbidity, UV spectrophotometry, wide angle X-ray diffraction, and differential scanning calorimetry. The enrofloxacin content in the complexes was 34％ （Carbo-enrofloxacin complex I） and 57％ （Carbo-enrofloxacin complex II） depending on the prepara-tion method. The dissolution rate of enrofloxacin from the complex increased as the pH was reduced. The dissolution rate of enrofloxacin from the Carbo-enrofloxacin complex I was significantly lower than that of the enrofloxacin powder. Therefore, these observations suggest that Carbo-enrofloxacin complex I can be used to mask the taste of enrofloxacin.

Keywords

References

  1. Agarwal, R., Mittal, R., and Singh, A., Studies of ion-exchange resin complex of chloroquine phosphate. Drug Dev. Ind Pharm., 26, 773-776 (2000) https://doi.org/10.1081/DDC-100101297
  2. Borodkin, S. and Sundberg, D. P., Polycarboxylic acid ionexchange resin adsorbates for taste coverage in chewable tablets. J. Pharm. Sci., 60, 1523-1527 (1971) https://doi.org/10.1002/jps.2600601018
  3. Fu Lu, M.-Y. and Borodkin, S., Antibiotic-polymer compositions. US Patent, 4, 808,411, (1989)
  4. Fu Lu, M.-Y. , Borodkin, S., Woodward, L., Li, P., Diesner, C., Hernandez, L., and Vadnere, M., A polymer carrier system for taste masking of macrolide antibiotics. Pharm. Res., 8, 706-712(1991)
  5. Harris, D., Fell, J. T, Taylor, D. C., Lynch, J., and Sharma, H. L., GI transit of potential bioadhesive systems in the rat. J. Control Release , 12, 55-65 (1990) https://doi.org/10.1016/0168-3659(90)90183-T
  6. Lizondo, M., Pons, M., Gallardo, M., and Estelrich, J., Physicochemical propertiesof enrofloxacin. J. Pharm. Biomed. Anal., 15, 1845-1849 (1997) https://doi.org/10.1016/S0731-7085(96)02033-X
  7. Miyanaga, Y., Inoue, N., Ohnishi, A., Fujisawa, E., Yamaguchi, M., and Uchida, T, Quantitative prediction of the bitterness suppression of elemental diets by various flavors using a taste sensor. Pharm. Res., 20, 1932-1938 (2003) https://doi.org/10.1023/B:PHAM.0000008039.59875.4f
  8. Miyanaga, Y, Tanigake, A., Nakamura, T, Kobayashi, Y, Ikezaki, H., Taniguchi, A., Matsuyama, K., and Uchida, T., Prediction of the bitterness of single, binary-and multiple-component amino acid solutions using a taste sensor. Int. J. Pharm., 248, 207-218 (2002) https://doi.org/10.1016/S0378-5173(02)00456-8
  9. Raghunathan, Y, Amsel, L., Hinsvark, O., and Bryant, W. J., Sustained-release drug delivery system I: Coated ionexchange resin system for phenylpropanolamine and other drugs. J. Pharm. Sci., 70, 379-384(1981) https://doi.org/10.1002/jps.2600700409
  10. Rosenstiel, N. and Adam, D., Quinolone antibacterials. An update of their pharmacology and therapeutic use. Drugs, 47 ,872-901 (1994) https://doi.org/10.2165/00003495-199447060-00003
  11. Takagi, S., Toko, K., Wada, K., and Ohki, T , Quantification of suppression of bitterness using an electronic tongue. J. Pharm. Sci., 90, 2042-2048 (2001) https://doi.org/10.1002/jps.1155
  12. Tanigake, A., Miyanaga, Y, Nakamura, T., Tsuji，E., Matsuyama, K., Kunitomo, M., and Uchida, T, The bitterness intensity of clarithromycin evaluated by a taste sensor. Chem. Pharm Bull., 51, 1241-1245 (2003) https://doi.org/10.1248/cpb.51.1241
  13. Wolfson, J. S. and Hooper, D. C., Fluoroquinolone antimicrobial agents. Clin. Microbiol. Rev., 2, 378-424 (1989) https://doi.org/10.1128/CMR.2.4.378
  14. Zhang, G., Jiang, M., Zhu, L., and Wu, C., Intermacromolecular complexation because of specific interactions 11. Ionic interaction complexation and its comparison with hydrogenbonding complexation. Polymer, 42, 151-159 (2001) https://doi.org/10.1016/S0032-3861(00)00332-3