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      • SBA 렉틴 활성에 Ca^2+Mn^2+ 이온이 미치는 영향

        왕훈식,이형철,이광표,김하형 중앙대학교 약학연구소 1998 약학 논총 Vol.12 No.-

        Soybean agglutinin (SBA) is the Ca^2+, Mn^2+ dependent lectin and the specificity of carbohydrates are D-galactose and N-acetyl-D-galactosamine. However, the effect of Ca^2+ and Mn^2+ ions to the activity of SBA is still unknown in detail. In the present study, hemmaglutination assay and enxyme-linked lectin assay (ELLA) have been applied. First, the carbohydrate-binding specificity of the crude SBA extract was examined, and D-galactose and N-acetyl-D-galactosamine exhibited the activity of the inhibition. The effect of Ca^2+ and Mn^2+ on the activity of SBA was observed by increasing the concentration of the ions, 1 to 50mM. SBA revealed the maximum activity when it contains 2mM Ca^2+ and/or Mn^2+ ion. Using these results, to isolate the SBA from crude extract, GaINAc-affinity column was applied containing Ca^2+ and Mn^2+ ions, and then eluted by same buffer without Ca^2+ and Mn^2+. SBA lectin which has hemagglutination activity was successfully isolated using its Ca^2+ and Mn^2+ dependent properties.

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        Bioequivalence of tacrolimus formulations with different dynamic solubility and in-vitro dissolution profiles

        권민창,염대일,김남아,최두형,박준상,왕훈식,유선동,정성훈 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.1

        This study was to evaluate the pharmacokineticsand bioequivalence of two tacrolimus formulationswhich had different in vitro drug release profiles. Dynamicsolubility, in vitro dissolution profiles of the two formulations,and their influence on pharmacokinetics wereexamined. The male volunteers were randomly assigned toreceive a single 1-mg capsule of the test or reference formulationand pharmacokinetic parameters were determinedusing a noncompartmental method. The two formulationsreleased [85 % of tacrolimus in water within 30 min,which passed the criterion of evaluating the test formulation. However, the test formulation produced a faster initialrelease rate and plateaued in about 15 min, while the referenceshowed almost zero order initial release profiles. The AUC0-? values were 145.92 (reference) and140.49 ng h/mL (test). The mean Cmax was 15.70 (reference)and 16.08 ng/mL (test) with Tmax values of 1.63 and1.60 h, respectively. The t1/2 for the reference and testformulations was 29.12 and 27.85 h, respectively. Relativebioavailability was calculated to be 96.28 %. The pointestimates for the mean ratio of the test to reference for theAUC0-t and Cmax were 0.969 and 1.026, respectively,satisfying the criterion for bioequivalence. The resultssuggest that the test formulation is pharmacokineticallyequivalent to the reference in terms of both rate and extentof absorption. Even though the in vitro dissolution profilesof the formulations might not be equivalent, the pharmacokineticsindicated bioequivalence. Therefore, whendeveloping poorly soluble drugs, it might be beneficial topay attention to the dynamic solubility as well as dissolution profiles.

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