DOI QR코드

DOI QR Code

Evaluation of buccal mucoadhesive [P(AA-co-PEGMM)] copolymer films containing butorphanol tartrate

Butolphanol tartrate 함유 구강점막 점착성 [P(AA-co-PEGMM)] 공중합체 필름의 평가

  • Kim, Joun-Sik (College of Pharmacy, Chungbuk National University) ;
  • Han, Kun (College of Pharmacy, Chungbuk National University)
  • 김준식 (충북대학교 약학대학) ;
  • 한건 (충북대학교 약학대학)
  • Published : 2002.03.20

Abstract

The mucoadhesive characteristics of [P(AA-co-PEGMM)] films by estimating the glass transition temperature $(T_g)$, analyzing surface energy and studying FT-IR was previously reported. In this study, the possibility of buccal mucoadhesive dosage form of [P(AA-co-PEGMM)] films by mucoadhesive force measurements and dissolution tests were also investigated. Mucoadhesiveness of [P(AA-co-PEGMM)] films was compared with cr-PAA and cr-PEGMM films crosslinked with 3% ethyleneglycol dimethacrylate (EGDMA). The buccal mucoadhesive force of [P(AA-co-PEGMM)] films increased with increasing content of PEGMM. [P{AA-co-PEGMM (18 mole%)}] films showed a significantly greater mucoadhesiveness than cr-PAA and cr-PEGMM films. The mucoadhesive force measured in normal saline (pH 5.0) was higher than that measured in phosphate buffer (pH 6.8) because of the pH dependence of hydrogels with carboxyl ions within the PAA. Moreover, the mucoadhesive force of [P{AA-co-PEGMM (18 mole%)}] films was at maximum after 2 hr attachment of buccal mocosa and it was maintained over $1\;N/cm^2$ for up to 10 hr. In dissolution studies, the release of butorphanol tartrate from [P(AA-co-PEGMM)] films increased with increasing PEGMM content, and films prepared with 18 mole% PEGMM gave almost zero order release kinetics.

Keywords

References

  1. R. Gurny and H.E. Junginger, Bioadhesion : possibilities and future trends, Proceedings of the 1st international joint workshop of the Association for Pharmaceutical Technology and the Controlled Release Society, Leiden, The Netherlands (1989)
  2. T. Nagai and R Konishi, Buccal/gingival drug delivery systems, J. Control. Rel., 6, 353-360 (1987) https://doi.org/10.1016/0168-3659(87)90088-5
  3. B.J. Aungst and N.J. Rogers, Site dependence of absorption-promoting actions of laureth-9, Na salicylate,$Na_2$ EDTA and aprotinin on rectal, nasal and buccal insulin delivery, Pharm. Res., 5, 305-308 (1988) https://doi.org/10.1023/A:1015930821648
  4. B.J. Aungst and N.J. Rogers, Comparison of the effects of various transmucosal absorption promoters on buccal insulin delivery, Int. J. Pharm., 227-235 (1989)
  5. M.A. Hussain, B.J. Aungst and E. Shefter, Buccal and oral bioavailability of nalbuphine in rats, J. Pharm. Sci., 75(2), 218-219 (1986) https://doi.org/10.1002/jps.2600750226
  6. C. Li, V.A. Raul, P.I.P. Bhatt, P.L. Koch and T.P. Johnson, Transbuccal delivery of a model tripeptide, Proceedings of the American Association of Pharmaceutical Scientists Meeting, Orlando, U.S.A., pp. S-201 (1993)
  7. J.S. Kim, J.S. Park and K. Han, Synthesis of [P(AA-co-PEGMM)] copolymer films and its physicochemical characteristics, J. Kor. Pharm. Sci., 31(3), 173-180 (2001)
  8. M.E. de Vries, H.E. Boddé, J. C. Verhoef, M. Ponec, W.I.H.M. Craane and H.E. Junginger, Localization of the permeability barrier inside porcine buccal mucosa : a combination in vitro study of drug permeability, electrical resistance and tissue morphology, Int. J. Pharm., 76, 25-32 (1991) https://doi.org/10.1016/0378-5173(91)90340-T
  9. S.A. Mortazavi and J.D. Smart, An in-vitro method for assessing the duration of mucoadhesion, J. Control. Rel., 31, 207-212 (1994) https://doi.org/10.1016/0168-3659(94)00044-1
  10. T.A. Willey, G.F. Duncan, L.K. Tay, K.A. Pittman and R.H. Farme, High-performance liquid chromatographic method for the quantitative determination of butorphanol, hydroxybutor- phanol, and norbutorphanol in human urine using fluorescence detection, J. Chromatography B., 652, 171-178 (1994) https://doi.org/10.1016/0378-4347(93)E0400-K
  11. S.S. Leung and J.R. Robinson, Polymer structure features contributing to mucoadhesion. II, J. Control. Rel., 12, 187-194 (1990) https://doi.org/10.1016/0168-3659(90)90099-F
  12. K. Park and J.R. Robinson, Bioadhesive polymers as platforms for oral-controlled drug delivery; method to study bioadhesion, Int., J. Pharm., 19, 107-127 (1984) https://doi.org/10.1016/0378-5173(84)90154-6
  13. N.A. Peppas and P.A. Buri, Surface, interfacial and molecular aspects of polymer bioadhesion on soft tissues, J. Control. Rel., 2, 257-275 (1985)
  14. H.S. Ch'ng, H. Park, P. Kelly and J.R. Robinson, Bioadhesive polymers as platforms for oral-controlled drug delivery. II. Synthesis and evaluation of some swelling, water-insoluble bioadhesive polymers, J. Pharm. Sci., 74, 399-405 (1985) https://doi.org/10.1002/jps.2600740407
  15. K. Park and J.R. Robinson, Mechanisms of mucoadhesion of poly (acrylic acid) hydrogels, Pharm. Res., 4, 457-464 (1987) https://doi.org/10.1023/A:1016467219657

Cited by

  1. Preparation of Poloxamer-based Hydrogels Using Electron Beam and Their Evaluation for Buccal Mucoadhesive Drug Delivery vol.36, pp.2, 2012, https://doi.org/10.7317/pk.2012.36.2.182