DOI QR코드

DOI QR Code

[P(AA-co-PEGMM)] 공중합체 필름으로부터 Butorphanol Tartrate의 구강점막 투과 특성 및 투과촉진제의 검색

Transport Characteristics and Screening of Penetration Enhancer through Buccal Mucosa of Butorphanol Tartrate from [P(AA-co-PEGMM)] Copolymer Films

  • 발행 : 2003.09.20

초록

The feasibility of [P(AA-co-PEGMM)] film as a buccal mucoadhesive patch was previously reported by estimating mucoadhesiveness and release characteristics. To find a rational penetration enhancer of [P(AA-co-PEGMM)] film containing butorphanol tartrate (Bt), penetration of Bt from [P(AA-co-PEGMM)] film which contained various additives was estimated by measuring its flux, Papp and lag tme in in vitro buccal membrane of porcine. EDTA showed almost no increase of Bt permeability, wherease SGC, STDHF and SLS increased the permeability of Bt with the order of SGC > STDHF > SLS. The rational additive concentration of SGC was 4% and its Papp and lag time were $1.93{\times}10^{-4}{\pm}4.21{\times}10^{-6},\;126.60{\pm}21.88min\;(control\;:\;Papp\;0.45{\times}10^{-4};\;lag\;time\;211.01{\pm}16.77\;min)$, respectively.

키워드

참고문헌

  1. Y. Rojanasakul, L.Y. Wang, M. Bhat, D.D. Glover, C.J. Malanga and J.K.H. Ma, The transport barrier of epithelia: a comparative study on membrane permeability and charge selectivity in the rabbit, Pharm. Res., 9, 1029 (1992) https://doi.org/10.1023/A:1015802427428
  2. C.K Oh and W.A. Ritschel, Biopharmaceutical aspects of buccal absorption of insulin, Methods Find. Exp. Clin. Pharmacol. 12, 205-212 (1990)
  3. Y. Nakada, N. Awata, C. Nakamichi and S. Goto, The effects of additives on the oral mucosal absorption of human calcitonin in rats, J. Pharmacobio-Dyn. 11, 395-401 (1988) https://doi.org/10.1248/bpb1978.11.395
  4. Y. Nakada, N. Awata, Y. lkuta and S. Goto, The effects of bile salts on the oral mucosal absorption of' human calcitonin in rats, J. Pharmacobio-Dyn. 12, 736-743 (1989) https://doi.org/10.1248/bpb1978.12.736
  5. A. Stward, D.L. Bayley, and C. Howes, The effect of enhancers on the buccal absorption of hybrid (BDBB)interferon, Int. J. Pharm., 104,145 (1994) https://doi.org/10.1016/0378-5173(94)90189-9
  6. J. Pitha, S.M. Harman and M.E. Michel, Hydrophilic cyclodextrin derivatives enable effective oral administration of steroidal hormones, J. Pharm. Sci. 75, 165-167 (1986) https://doi.org/10.1002/jps.2600750213
  7. T. Murakmi, Y. Sasaki, R Yamajo and N. Yata: Effect of bile salts on the rectal absorption of sodium ampicillin in rats, Chem. Pharm. Bull., 32, 1948-1955 (1984) https://doi.org/10.1248/cpb.32.1948
  8. K. Sakai, T. M. Kutsuna, T. Nishino, Y. Fujihara and N. Yata : Contribution of calcium ion sequestration by polyoxyethylated nonionic surfactants to the enhanced colonic absorption of p-arninobenzoic acid, J. Pharm. Sci; 75, 387-389 (1986) https://doi.org/10.1002/jps.2600750414
  9. 西村憲一: 經皮經粘證吸收製齊の 開發と 新しい 試驗.實驗.評價法の 實濟 (日本科學技術協會編), テクノアイ出版部, 278-298(1986)
  10. S. Yamashita, S. Saitoh, H. Nalsanishi, M. Masada, T. Nadai and T. Kimura: Effects of diclofenac sodium and disodium ethylenediamine teh-a-acetate on electrical parameters of the mucosal membrane and their relation to the permeability enhancing effects in the mt jejunum, J. Pharm. Pharmacol, 39, 621-626 (1987) https://doi.org/10.1111/j.2042-7158.1987.tb03440.x
  11. M.M. Cassidy and C.S. Tidball: Cellular mechanism of intestinal permeability alterations produced by chelation depletion, J. Cell. BioI. 32, 685-698
  12. T. Suzuka, A. Furuya, A. Kamada, M. Yamazaki and T. Nishihata: Effect of diethyl maleate and sodium salicylate on cefmetazole transport in the in vitro rat everted sac: Influence of $Ca^{2+}$ and vanadate in the media, Chem. Pharm. Bull, 35,1619-1623 (1987) https://doi.org/10.1248/cpb.35.1619
  13. E. Hayakawa, A. Yamamoto, Y. Shoji and Y.H.L. Lee: Effect of sodium glycocholate and polyoxyethylene-9-lauryl ether on the hydrolysis of varying concentrations of insulin in the nasal homogenates of the albino rabbit, Life Sci., 45, 167-174 (1989) https://doi.org/10.1016/0024-3205(89)90291-9
  14. H. Kajii, T. Hoiie, M. Hayashi and S. Awazu : Fluorescence study on the mteraction of salicylate with rat small intestinal epithelial cells : possible mechanism for the promoting effects of salicylate on drug absorption in vivo. Life Sci., 37(6), 523-530 (1985) https://doi.org/10.1016/0024-3205(85)90464-3
  15. H. Kajii, T. Horie, M. Hayashi and S. Awazu: Fluorescence study of the membrane-perturbing action of sodium caprylate as related to promotion of drug absorption, J. Pharm. Sci., 77, 390 (1988) https://doi.org/10.1002/jps.2600770506
  16. H. Fulnii, M. Murakami, H. Yoshikawa, K. Takada and S. Muranishi: Studies on the promoting effect of lipid-suifactant mixed micelles (MM) on intestinal absorption of colloidal particles, J. Pharmacobio-Dyn., 10(6), 236-242 (1987) https://doi.org/10.1248/bpb1978.10.236
  17. M. Ishida, Y. Machida, N. Nambu and T. Nagai, New mucosal dosage form of insulin, Chem. Pharm. Bull. 29, 810-816 (1981) https://doi.org/10.1248/cpb.29.810
  18. J.S. Kim, J.S. Park and K. Han, Synthesis of [P(AA-co-PEGMM)] copolymer films and its physicochemical chaiactenstics, J. Kor. Pharm. Sci., 31(3), 173-180 (2001)
  19. J.S. Kim and K. Han, Evaluadon of buccal mucoadhesive [P(AA-co-PEGMM)] copolymer films containing butorphanol tartrate, J. Kor. Phann. Sci., 32(1), 1-6 (2002)
  20. S. Hirai, T. Yashiki and H. Mima, Effect of surfactants on the nasal absorption of insulin in rats, Int. J. Pharm., 9, 165-172 (1981) https://doi.org/10.1016/0378-5173(81)90009-0
  21. G.S.M.J.E Duchateau, J. Zuidema and S.W.J Basseleur, Influence of some surface-active agents on nasal absorption in rabbits, Int. J. Pharm., 39, 87-92 (1987) https://doi.org/10.1016/0378-5173(87)90201-8
  22. A.H. Shojaei and L. Xiaoling, Mechanisms of buccal mucoadhesion of novel copolymers of acrylic acid and polyethylene glycol monomethylether monomethacrylate, J. Control. Release 47, 151-161 (1997) https://doi.org/10.1016/S0168-3659(96)01626-4
  23. Y.W. Chien (Ed.), Transdermal Controlled Systemic Medi-cations, Marcel Dekker, New York, 1987, pp. 127
  24. R. Gandi and J.R. R.obinson, Mechamsm of penetration enhancement for transbuccal delivery of salicylic acid, Int. J. Pharm., 85, 129-140 (1985) https://doi.org/10.1016/0378-5173(92)90142-O