• Journal of Pharmaceutical Investigation
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• v.33 no.3
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• pp.157-162
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• 2003

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.

• Journal of Pharmaceutical Investigation
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• v.32 no.1
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• pp.1-6
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• 2002

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.