IngentaConnect The bioequivalence of standard sumatriptan tablets and two encaps...

Abstract:

The bioequivalence of encapsulated vs standard (commercial) sumatriptan was assessed before comparative eletriptan–sumatriptan efficacy studies in the acute treatment of migraine were conducted. Commercially acquired sumatriptan was encapsulated to ensure the double-blind nature of these studies.

The pharmacokinetics of three single oral doses of sumatriptan 100 mg – the standard tablet, an encapsulated tablet, and a stressed encapsulated tablet – were compared in an open, randomized, three-way crossover study. Stressed capsules were produced by storing capsules for 12 weeks at 40°C/75% humidity; conditions chosen to accelerate any effects potentially induced by long-term storage under normal conditions. Blood samples were obtained from 22 males at baseline and at intervals over 24 h post-dose. Bioequivalence parameters were calculated as mean ratios and associated 90% confidence intervals, and between-drug differences were assessed using standard criteria. A prior dissolution study confirmed similar dissolution of the encapsulated and standard forms; though stressed tablets had decreased dissolution.

For standard, encapsulated and stressed encapsulated sumatriptan, the area under the plasma concentration–time curve from 0 to infinity (AUC) values were 201.95, 199.74 and 203.98 ng h/ml, respectively. Maximum observed plasma concentration (max) values were 58.91, 56.09 and 52.56 ng/ml, respectively. The times to the first occurrence of max (max) were 1.69, 1.83 and 1.98 h, respectively. All forms were bioequivalent using the standard range of 80–125%, with the exception of a 1% out of range max for the stressed form. This parameter was within range using max/AUC, a more sensitive absorption rate estimate.

These results demonstrate that the encapsulated and stressed sumatriptan used in these studies are bioequivalent to commercial sumatriptan. The max data suggest a similar rate of absorption.

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The bioequivalence of standard sumatriptan tablets and two encapsulated forms of sumatriptan