DOI QR코드

DOI QR Code

폴록사머 및 프로필렌글리콜을 이용한 클로트리마졸 고형 좌제의 물리화학적 특성

Physicochemical Characterization of Clotrimazole-Loaded Solid Suppository Using Poloxamer and Propylene Glycol

  • 발행 : 2005.04.20

초록

To develop a clotrimazole-loaded solid suppository with poloxamer and propylene glycol, the melting points of various formulations composed of poloxamer 188 (P 188) and propylene glycol were investigated. The dissolution study of clotrimazole delivered by the suppository composed of P 188 and propylene glycol was performed. The mixtures composed of P 188 and propylene glycol were homogeneous. Propylene glycol affected the melting points of poloxamer mixtures. In particular, the mixture [P 188/propylene glycol (70/30%)] with the melting point of about $32^{\circ}C$ was a solid form at room temperature and instantly melted at physiological temperature. Furthermore, propylene glycol affected greatly the dissolution rates of clotrimazole from the suppository. Dissolution mechanism analysis showed the dissolution of clotrimazole was proportional to the time. Our results indicated that the solid suppository with P 188 and propylene glycol would be a candidate of rectal dosage form for clotrimazole.

키워드

참고문헌

  1. C.H. Huang, T. Tokumura, Y. Machida and T. Nagai, Formulation of double-layered suppository for prolonged stay in lower rectum, Yakuzaigaku, 47, 42-48 (1987)
  2. A.H. Burstein, K.M. Fisher, M.L. McPherson and C.A. Roby, Absorption of phenytoin from rectal suppositories formulated with a polyethylene glycol base, Pharmacotherapy, 20, 562-567 (2000) https://doi.org/10.1592/phco.20.6.562.35157
  3. C.J. Eboka, R.S. Okor, J.O. Akerele and S.O. Aigbavboa, Kinetics of absorption and elimination of ofloxacin in humans after oral and rectal administrations, J. Clin. Pharm. Ther., 22, 217-220 (1997) https://doi.org/10.1046/j.1365-2710.1997.95075950.x
  4. A. Nagatomi, M. Mishima, O. Tsuzuki, S. Ohdo and S. Higuchi, Utility of a rectal suppository containing the antiepileptic drug zonisamide, Biol. Pharm. Bull., 20, 892-896 (1997) https://doi.org/10.1248/bpb.20.892
  5. C.K. Kim, S.W. Lee, H.G. Choi, M.K. Lee, Z.G. Gao and I.S. Kim, Trials of in-situ gelling and mucoadhesive acetaminophen liquid suppository in human subjects, Int. J. Pharm., 174, 201-207 (1998) https://doi.org/10.1016/S0378-5173(98)00258-0
  6. H.G. Choi, J.H. Jung, J.M. Ryu, S.J. Yoon, Y.K. Oh and C.K. Kim, Development of in-situ gelling and mucoadhesive acetaminophen liquid suppository, Int. J. Pharm., 165, 33-44 (1998) https://doi.org/10.1016/S0378-5173(97)00386-4
  7. C.S. Yong, Y.K. Oh, J.A. Kim, Y.I. Kim, S.M. Park, J.H. Yang, J.D. Rhee and H.G. Choi, Development of poloxamer-based solid suppository containing diclofenac sodium, J. Kor. Pharm. Sci., 34(2), 91-94 (2004)
  8. M.O. Yun, H.G. Choi, J.H. Jung and C.K. Kim, Development of thermoreversible insulin liquid suppository with sodium salicylate, Int. J. Pharm., 189, 137-145 (1999) https://doi.org/10.1016/S0378-5173(99)00227-6
  9. H.G. Choi, Y.K. Oh and C.K. Kim, In-situ gelling and mucoadhesive liquid suppository containing acetaminophen: enhanced bioavailability, Int. J. Pharm., 165, 23-32 (1998) https://doi.org/10.1016/S0378-5173(97)00385-2
  10. S. Miyazaki, T. Nakamura, C. Yokouchi and M. Tanaka, Effect of pluronic gels on the rectal absorption of indomethacin in rabbits, Chem. Pharm. Bull., 35, 1243-1248 (1987) https://doi.org/10.1248/cpb.35.1243
  11. J.Y. Chang, Y.K. Oh, H.G. Choi, Y.B. Kim and C.K. Kim. Rheological evaluation of thermosensitive and mucoadhesive vaginal gels in physiological conditions. Int. J. Pharm., 241, 155-163 (2002) https://doi.org/10.1016/S0378-5173(02)00232-6
  12. E.M. Abdel-Moety, A.A. Alamein, F.I. Khattab, K.M. Kekani, Chromatographic determination of clotrimazole, ketoconazole and fluconazole in pharmaceutical formulations, Farmaco, 57, 931-938 (2002) https://doi.org/10.1016/S0014-827X(02)01270-3
  13. H.G. Choi, B.J. Lee, C. Yang, J.D. Rhee, J.H. Han, M.K. Lee, K.M. Park and C.K. Kim, Terfenadine-$\beta$-cyclodextrin inclusion complex with the anti-histaminic activity enhancement, Drug Dev. Ind Pharm., 27, 1259-1263 (2001)
  14. M. Iwata K. Takayama, Y. Takahashi, Y. Obata, Y. Machida, T. Nagai and S. Shirotake, Effect of temperature on drug release and drug absorption in mixed type diclofenac. sodium suppositories, Yakugaku Zasshi (Japan), 119, 170-177 (1999)
  15. N.A. Peppas, Analysis of Fickian and non-Fickian drug from release polymers. Pharm. Acta Helv., 60, 110-111 (1985)