• 약학회지
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• 제39권6호
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• pp.593-599
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• 1995

Erythromycin was formulated as enteric-coated pellets in order to reduce degradation in stomach and gastromtestmal irritation, and to maximize the absorption in intestine followmg its oral administration. Core pellets were prepared using fluid-bed granulator with two different methods (powder layering and solvent spraying) and enteric-coated with two different coating polymers (HPMCP and Eudragit E30D). Physical characteristics md dissolution rates of core pellets and enteric-coated pellets were evaluated to optimize the formulation. Powder layering method resulted in shorter initial dissolution time than solvent spraying method, but physicochmical properties of the product were worse than solvent spraying method with respect to hardness, ftiability and density. The dissolution rate of the drug was increased with the addition of surfactants, showing concentration-dependence. The scanning electron microscopic observation of pellets revealed significant differences on the surface appearances prepared with solvent spraying method. The core pellet made with powder layering method had crystals on the surface, which resulted in poor physical properties of the pellets. The dissolution profiles of erythromycin pellets coated with HPMCP or Eudragit L30D were close to that of commercially available erythromycin enteric-coated product.

• Journal of Pharmaceutical Investigation
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• 제23권1호
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• pp.41-49
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• 1993

The bioequivalence of two omeprazole enteric-coated products was evaluated in 16 normal male volunteers (age 26-32 yr, body weight 57-75 kg) following single oral administration. Test product was enteric-coated KD-182 tablet (Chong Kun Dang Corp., Korea) and reference product was $Rosec^{\circledR}$ capsule containing enteric-coated pellets of omeprazole (Yuhan Corp., Korea). Both products contain 20 mg of omeprazole. One tablet or capsule of the test or the reference product was administered to the volunteers, respectively, by randomized two period cross-over study ($2\;{\times}\;2$ Latin square method). Average drug concetrations at each sampling time and pharmacokinetic parameters calculated were not significantly different between two products(p>0.05); the area under the concentrationtime curve to last sampling time (8 hr) $(AUC_{0-8hr})$ $(1946.5{\pm}675.3\;vs\;2018.3{\pm}761.6\;ng{\cdot}hr/ml)$, AUC from time zero to infinite $(AUC_{o-\infty})$ $(2288.6{\pm}1212.8\;vs\;2264.9{\pm}1001.3\;ng{\cdot}hr/ml)$, maximum plasma concentration $(C_{max})$ $(772.5{\pm}283.3\;vs\;925.8{\pm}187.7\;ng/ml)$, time to maximum plasma concentration $(T_{max})$ $(2.38{\pm}1.06\;vs\;2.34{\pm}1.09\;hr)$, apparent elimination rate constant $(k_{\ell})$ $(0.5339{\pm}0.2687\;vs\;0.5769 {\pm}0.2184\;hr^{-I})$, apparent absorption rate constant $(k_a)$ $(1.1536{\pm}0.5278\;vs\;0.9739{\pm}0.9507 hr^{-1})$ and mean residence time (MRT) $(3.13{\pm}0.73\;vs \;3.41{\pm}1.04\;hr)$. The differences of mean $(AUC_{0-8hr})$, $C_{max}$, $T_{max}$ and MRT between the two products (3.69, 19.83, 1.32 and 8.99%, respectively) were less than 20%. The power $(1-{\beta})$ and treatment difference $(\triangle)$ for $AUC_{o-8hr}$ $C_{max}$ and MRT were more than 0.8 and less than 0.2, respectively. Although the power for $T_{max}$ was under 0.8, $T_{max}$ of the two products was not significantly different each other(p>0.05). These results suggest that the bioavailability of KD-182 tablet is not significantly different from that of $Rosec^{\circledR}$ capsule. Therefore, two products are bioequivalent based on the current results.