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Relative Bioavailability and Pharmacokinetics of Nimesulide Capsules in Volunteers

Mengqiu Li

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Abstract

Objective: to compare the pharmacokinetics and bioavailability of nimesulide capsules with nimesulide tablets. Method: a single 200 mg oral dose of nimesulide capsule or tablet was given to 10 healthy male volunteers in a randomized double cross-over study. Plasma levels of nimesulide were detected by HPLC-U V method. Results: The pharmacokinetic parameters of nimesulide capsules and tablets were as follewed: T1/2K (h):4. 25 ±0. 58 and 4. 67 ±0. 45;Cmax (mg. L -1 ):9. 28 ± 2. 20 and 8. 92 ± 2. 48;Tmax (h):2. 88 ± 0. 51 and 2. 79 ±0. 55;MRT(h):9. 30 ± 0. 92 and 9. 50 ± 0. 60; AUC0-24 (mg. h. L - 1 ): 87. 02 ± 26. 88 and 86. 98 ± 25. 33 respectively. The relative bioavailability of nimesulide capsule was 100. 54 ± 11. 01 %. There were no significant differences between pharmacokinetic parameters for the two formulations of nimesulide(P 0. 05 ). The nimesulide capsules showed bioequivalence compared with the tablets.

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What this paper is about

Objective: to compare the pharmacokinetics and bioavailability of nimesulide capsules with nimesulide tablets. Method: a single 200 mg oral dose of nimesulide capsule or tablet was given to 10 healthy male volunteers in a randomized double cross-over study. Plasma levels of nimesulide were detected by HPLC-U V method. Results: The pharmacokinetic parameters of nimesulide capsules and tablets were as follewed: T1/2K (h):4. 25 ±0. 58 and 4. 67 ±0. 45;Cmax (mg. L -1 ):9. 28 ± 2. 20 and 8. 92 ± 2. 48;Tmax (h):2. 88 ± 0. 51 and 2. 79 ±0. 55;MRT(h):9. 30 ± 0. 92 and 9. 50 ± 0. 60; AUC0-24 (mg. h. L - 1 ): 87. 02 ± 26. 88 and 86. 98 ± 25. 33 respectively. The relative bioavailability of nimesulide capsule was 100. 54 ± 11. 01 %. There were no significant differences between pharmacokinetic parameters for the two formulations of nimesulide(P 0. 05 ). The nimesulide capsules showed bioequivalence compared with the tablets.

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Available abstract

Objective: to compare the pharmacokinetics and bioavailability of nimesulide capsules with nimesulide tablets. Method: a single 200 mg oral dose of nimesulide capsule or tablet was given to 10 healthy male volunteers in a randomized double cross-over study. Plasma levels of nimesulide were detected by HPLC-U V method. Results: The pharmacokinetic parameters of nimesulide capsules and tablets were as follewed: T1/2K (h):4. 25 ±0. 58 and 4. 67 ±0. 45;Cmax (mg. L -1 ):9. 28 ± 2. 20 and 8. 92 ± 2. 48;Tmax (h):2. 88 ± 0. 51 and 2. 79 ±0. 55;MRT(h):9. 30 ± 0. 92 and 9. 50 ± 0. 60; AUC0-24 (mg. h. L - 1 ): 87. 02 ± 26. 88 and 86. 98 ± 25. 33 respectively. The relative bioavailability of nimesulide capsule was 100. 54 ± 11. 01 %. There were no significant differences between pharmacokinetic parameters for the two formulations of nimesulide(P 0. 05 ). The nimesulide capsules showed bioequivalence compared with the tablets.

Key concepts: Nimesulide, Bioavailability, Pharmacokinetics, Bioequivalence, Cmax, Pharmacology, Capsule, Chemistry

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