In Vivo Evaluation of Thiamine Hydrochloride with Gastro-Retentive Drug Delivery in Healthy Human Volunteers Using Gamma Scintigraphy

A floating tablet system containing thiamine hydrochloride, a model drug with a narrow absorption window, was evaluated. The tablet was found to have a floating lag time of less than 30 s with a sustained drug release over 12 h during in vitro dissolution studies. The gastro-retentive property of th...

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Published inPharmaceutics Vol. 15; no. 2; p. 691
Main Authors Kam, Li-Ying, Wong, Jia-Woei, Yuen, Kah-Hay
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 01.02.2023
MDPI
Subjects
Bioavailability
Cellulose
Chemical properties
Dosage and administration
Drug delivery systems
Drug dosages
Drugs
Evaluation
floating tablet
gamma-scintigraphy
gastro-retentive drug delivery
Methods
Radioisotope scanning
Scintigraphy
Small intestine
Stomach
Structure
thiamine hydrochloride
Vehicles
Vitamin B
Vitamin B1
Malaysia
United States > US
Germany
gamma-scintigraphy
thiamine hydrochloride
floating tablet
gastro-retentive drug delivery
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Summary:A floating tablet system containing thiamine hydrochloride, a model drug with a narrow absorption window, was evaluated. The tablet was found to have a floating lag time of less than 30 s with a sustained drug release over 12 h during in vitro dissolution studies. The gastro-retentive property of the tablet in relation to the bioavailability of thiamine was determined in healthy human volunteers using gamma scintigraphy under fasted and fed conditions. The gastro-retentive time of the floating tablet could be prolonged up to 10 h under the fed state, compared to about 1.8 h in the fasted state. The prolonged gastric retention under the fed state resulted in a 2.8-fold increase in oral bioavailability of thiamine compared to that of the fasted state. There was also a 1.4-fold increase in thiamine absorption compared to that of a conventional immediate release tablet in the fed state. In the fasted state, the extent of thiamine absorption from the floating tablet was only about 70% of that absorbed from the immediate release tablet. Thus, to achieve a better performance, such floating tablet systems should be administered under a fed condition, to prolong the gastric retention time.
Bibliography:ObjectType-Article-1
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ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15020691