Improved dosage form of the combined alendronate and calcitriol (Maxmarvil) on the absorption of alendronate in Korean postmenopausal women

다국어 초록 (Multilingual Abstract)

Alendronate is one of the most potent antiosteoporoticagents for postmenopausal osteoporosis.
However, high doses of alendronate cause esophagealirritation, myalgia, gastrointestinal discomfort and decreaseof serum calcium level. Recently, Maxmarvil wasdeveloped as an enteric-coated tablet containing alendronate(5 mg) and calcitriol (0.5 lg) to minimize these sideeffects of alendronate. In the present study, we evaluatedthe pharmacokinetic profile and examined the incidence ofunfavorable effects after oral administration of Maxmarvil in Korean healthy postmenopausal women without aprevious history of fracture. In the in vitro dissolution test,alendronate was not released from Maxmarvil in pH 1.2phosphate buffer solution but released in pH 6.0 and 6.8phosphate buffer solutions and completely dissolved in30 min. After oral administration of Maxmarvil, three outof 18 (16.7 %) women showed mild adverse effects; twomyalgia and one upper gastrointestinal discomfort withoutheartburn. Most of these complaints disappeared during thestudy without additional treatment. The peak (Umax) andthe average (Uave) urinary excretion rate of alendronate andthe time to reach Umax (Tmax) were 2.94 lg/h, 0.901 lg/hand 6.77 h, respectively. The total cumulative urinaryexcretion of alendronate (Ae0–24 h) was 21.6 lg (0.432 %of oral alendornate), which was similar to the reportedvalues. Taken together, enteric-coated Maxmarvil is lessharmful for the esophagus and gastrointestinal mucosa,shows the same pharmacokinetic profile to conventionalalendronate (70 mg) and improves the tolerability ofmedication in clinical practice.

참고문헌 (Reference)

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