Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
권호 표지
DOI QR코드

DOI QR Code

SMEDDS (Self-MicroEmulsifying Drug Delivery System) As An Intraurethral Prostaglandin E1 Delivery System

  • Published : 2007.10.21
Download PDF
⟨ Previous Next ⟩

Abstract

Prostaglandin $E_1\;(PGE_1)$ was formulated as two self-microemulsifying drug delivery systems (SMEDDS) composed of Cremophor $EL^{(R)}$ or Cremophor $ELP^{(R)}$ as a surfactant, ethanol as a cosurfactant and Labrafac $CC^{(R)}$ as an oil to develop liquid preparation for the treatment of erectile dysfunction. In pseudo-ternary phase diagram, viscous gel area and microemulsion area were defined. In the measurement of viscosity, the viscosity of two formulations increased gradually upon the addition of water and it decreased from the water contents over 40%. With excessive water, the present systems formed a microemulsion spontaneously. From these results, rte could expect that the present liquid $PGE_1$ SMEDDS formulations might stay within the urethra in the viscous state when contacting the moisture of the urethra and can be easily eliminated by urination. In long-term stability study, we could select one formulation more stable at the shelf storage condition of $4^{\circ}C$.

Keywords

References

  1. R. Virag, K. Shoukry, J. Floresco, E Nollet and E. Greco, Intracavemous self-injection of vasoactive drugs in the treatment of impotence: 8-year experience with 615 cases, The J. Urol., 145, 287-293 (1991) https://doi.org/10.1016/S0022-5347(17)38316-7
  2. H.P. Nathan, W.J.G Hellstrom, F.E. Kaiser, R.F. Labasky, T.F. Lue, W.E. Nolten, P.C. Norwood, C.A. Peterson, R. Shabsigh, P.Y. Tam, V.A. Place and N. Gesundheit, Treatment of men with erectile dysfunction with transurethral alprostadil, N. Engl. J. Med., 336, 1-7 (1997) https://doi.org/10.1056/NEJM199701023360101
  3. P. Werthman and J. Rajfer, Muse therapy: Preliminary clinical observations, Urol., 50, 809-811 (1997) https://doi.org/10.1016/S0090-4295(97)00448-2
  4. M. Waldhauser and P. Schramek, Efficiency and side effects of prostaglandin E1 in the treatment of erectile dysfunction, The J. Urol., 140, 525-527 (1988) https://doi.org/10.1016/S0022-5347(17)41709-5
  5. S.B. Levine, S.E. Althof, L.A. Turner, C.B. Risen, Bodner D.R., Kursh E.D. and M.L. Resnick, Side effects of self-administration of intracavemous papaverine and phentolamine for the treatment of impotence, The J. Urol., 141, 54-57 (1989) https://doi.org/10.1016/S0022-5347(17)40585-4
  6. E.D. Kim and K.T. Mcvary, Topical prostaglandin E1 for the treatment of erectile dysfunction, The J. Urol., 153, 1828-1830 (1995) https://doi.org/10.1016/S0022-5347(01)67323-3
  7. M. Maggi, S. Filippi and F. Ledda, Erectile dysfunction: from biochemical pharmacology to advances in medical therapy, Eur. J. Endocrinol., 143, 143-154 (2000) https://doi.org/10.1530/eje.0.1430143
  8. L.S. Palmer, M. Valcic and A. Melman, Characterization of cyclic AMP accumulation in cultured human corpus cavernosum smooth muscle cells, J. Urol., 152, 1308-1314 (1994) https://doi.org/10.1016/S0022-5347(17)32573-9
  9. R. Igarashi, T. Takenenage and T. Matsuda, Distribution of lipid microsphere preparation, Adv. Drug Deliv. Rev., 20, 147-154 (1996) https://doi.org/10.1016/0169-409X(95)00125-Q
  10. Y. Mizushima, Lipid microspheres (Lipid emulsions) as a drug carriers-overview, Adv. Drug Deliv. Rev., 20, 113-115 (1996) https://doi.org/10.1016/0169-409X(95)00114-M
  11. C.W. Pouton, Self-emulsifying drug delivery systems: Assessment of the efficiency of emulsification, Int. J. Pharm., 27, 335-348 (1985) https://doi.org/10.1016/0378-5173(85)90081-X
  12. N.H. Shah, M.T. Carvajal, C.I. Patel, M.H. Infeld and A.W. Malick, Self- emulsifying drug delivery systems with polygIycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs, Int. J. Pharm., 106, 15-23 (1994) https://doi.org/10.1016/0378-5173(94)90271-2
  13. M.J. Lawrence and G.D. Rees, Microemulsion-based media as novel drug delivery systems, Adv. Drug Deliv. Rev., 45, 89-121 (2000)
  14. S.M. Khoo, A.J. Humberstone, C.J.H. Porter, G.A Edward and W.N. Charman, Formulation design and biocompatibility assessment of lipidic self-emulsifying formulations of halofantrine, Int. J. Pharm., 167, 155-164 (1998) https://doi.org/10.1016/S0378-5173(98)00054-4
  15. K.C. Lee and P.P. Deluca, Simultaneous determination of prostaglandin E1, A1, and B1 by reversed-phase high-performance liquid chromatography for the kinetic studies of prostaglandin E1 in solution, J. Chromatogr., 555, 73-80 (1991) https://doi.org/10.1016/S0021-9673(01)87168-5
  16. D.L. Teagarden, B.D. Anderson and W.J. Peter, Dehydration kinetics of prostaglandin $E_1$ in a lipid emulsion, Pharm. Res., 6, 210-215 (1989) https://doi.org/10.1023/A:1015909432300
  17. Technical Leaflet; Cremophor ELP, BASF 1997
  18. Technical Leaflet; Cremophor EL, BASF 1997