Novel gastroretentive dosage forms: evaluation of gastroretentivity and its effect on riboflavin absorption in dogs.

Abstract:

PURPOSE:[corrected] The purpose of this study was to design novel gastroretentive dosage forms (GRDFs) based on unfolding multilayer polymeric films, to investigate the mechanism of their gastroretentivity in dogs, and to assess the effect of compounding a narrow absorption window drug in a GRDF on the drug's absorption properties. METHODS:Dosage forms (DFs) with different dimensions and mechanical properties were administered to beagle dogs with acidic buffer (pH = 1.5), whose gastric retention time (GRT) was then determined by X-ray pictures. Concurrent administration of radiopaque markers was used to assess the effect of the GRDF and/or acidic buffer on GRT. The absorption of riboflavin from a prototype GRDF was compared with a nongastroretentive controlled-release DF and to an oral solution of the drug. RESULTS:Large DFs (> or = 2.5 x 2.5 cm) containing rigid frame had prolonged GRT (>4 h). Administration of 400 mL of acidic buffer (or water) prolonged GRT whereas the GRDF did not cause additional prolongation. The extended absorption phase (>48 h) of riboflavin administered in a GRDF led to 4-fold increased bioavailability. CONCLUSION:The combination of large dimensions with rigidity produce gastroretentivity that can be used to improve absorption properties of a model of narrow absorption window drugs in the gastrointestinal tract.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Klausner EA,Lavy E,Stepensky D,Friedman M,Hoffman A

doi

10.1023/a:1020412817716

subject

Has Abstract

pub_date

2002-10-01 00:00:00

pages

1516-23

issue

10

eissn

0724-8741

issn

1573-904X

journal_volume

19

pub_type

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