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Predicting the gastrointestinal behaviour of modified-release products: utility of a novel dynamic dissolution test apparatus involving the use of bicarbonate buffers.

Abstract：

:The establishment of physiologically relevant in vitro-in vivo correlations (IV-IVCs) is key for any biorelevant dissolution test. Historically, bicarbonate buffers have produced better correlations than compendial phosphate buffered media, though such tests are usually performed at a constant pH experiment, overlooking the notion that the pH of the luminal fluids is variable and fluctuating. In this work, we have devised a dynamic dissolution test method employing a physiological bicarbonate buffer under pH conditions of the proximal gut in order to assess the dissolution behaviour of various enteric polymer-coated (gastro-resistant) prednisolone tablets. The pH of the media is modulated and controlled by an Auto pH System™ which exploits the physiological equilibria between [H2CO3] and [HCO3(-)], to match it to the aboral change in pH with transit of the dosage form through the proximal small intestine (from pH 5.6 up to 6.8). The lag time values for an accelerated release and standard EUDRAGIT(®) L30D-55 coated formulation (25 min and 60 min, respectively) were close to the previously reported initial tablet disintegration time data obtained in-vivo by γ-scintigraphy (28 min and 66 min, respectively). Dissolution of alternative delayed release coated products was also better discriminated in the dynamic buffer system. These data confirm the dynamic dissolution system provides a robust and reliable platform to predict the in vivo fate of oral products in a laboratory setting.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Merchant HA,Goyanes A,Parashar N,Basit AW

doi

10.1016/j.ijpharm.2014.09.003

subject

Has Abstract

pub_date

2014-11-20 00:00:00

pages

585-91

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(14)00646-2

journal_volume

475

pub_type

杂志文章

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