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Daru. 2011;19(3):224-30.

In vivo bioavailability studies of sumatriptan succinate buccal tablets.

Author information

1
Acharya and B M Reddy College of Pharmacy, Bangalore-560090, India.

Abstract

BACK GROUND AND THE PURPOSE OF STUDY: Sumatriptan succinate is a Serotonin 5- HT1 receptor agonist, used in treatment of migraine. It is absorbed rapidly but incompletely when given orally and undergoes first-pass metabolism, resulting in a low absolute bioavailability of about 15%. The aim of this work was to design mucoadhesive bilayered buccal tablets of sumatriptan succinate to improve its bioavailability.

METHODS:

Mucoadhesive polymers carbopol 934 (Carbopol), HPMC K4M, HPMC K15M along with ethyl cellulose as an impermeable backing layer were used for the preparation of mucoadhesive bilayered tablets. In vivo bioavailability studies was also conducted in rabbits for optimized formulation using oral solution of sumatriptan succinate as standard.

RESULTS:

Bilayered buccal tablets (BBT) containing the mixture of Carbopol and HPMC K4M in the ratio 1:1 (T1) had the maximum percentage of in vitro drug release within 6 hrs. The optimized formulation (T1) followed non-Fickian release mechanism. The percentage relative bioavailability of sumatriptan succinate from selected bilayered buccal tablets (T1) was found to be 140.78%.

CONCLUSIONS:

Bilayered buccal tablets of sumatriptan succinate was successfully prepared with improved bioavailability.

KEYWORDS:

Bilayered Buccal Tablets (BBT); Carbopol; HPMC K15M.; HPMC K4M

PMID:
22615661
PMCID:
PMC3232104
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