Release Characteristics of Quetiapine Fumarate Extended Release Tablets Under Biorelevant Stress Test Conditions

Abstract

Abstract. The aim of the present work was the investigation of robustness and reliability of drug release from 50 to 400 mg quetiapine extended release HPMC matrix tablets towards mechanical stresses of biorelevant intensity. The tests were performed under standard conditions (USP apparatus II) as well as under simulated gastrointestinal stress conditions. Mechanical stresses including pressure and agitation were applied by using the biorelevant dissolution stress test apparatus as it has been introduced recently. Test algorithms already established in previous studies were applied to simulate fasting gastrointestinal conditions. The dissolution experiments demonstrated striking differences in the product performance among standard and stress test conditions as well as dose strengths. In USP apparatus II, dissolution profiles were affected mainly by media pH. The dissolution experiments performed in biorelevant dissolution stress test device demonstrated that stress events of biorelevant intensity provoked accelerated drug release from the tablets.

Dissolution of mesalazine modified release tablets under standard and bio-relevant test conditions

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Resolving the physiological conditions in bioavailability and bioequivalence studies: Comparison of fasted and fed state

“…The asterisks (*) indicate temporary data loss during gastric transit.The observed varying pressure values and gastric residence times under fasting conditions can contribute to a variable in vivo performance of large, monolithic dosage forms. Especially for hydrogel matrix tablets a pressure sensitive dissolution behavior was shown[9].The maximum pressures measured in the small intestine as well as in the large intestine were clearly below those in stomach. The highest pressures during small intestinal passage went up to 103 mbar ± 65 mbar under fasting conditions.…”

Formulation and pharmaceutical development of quetiapine fumarate sustained release matrix tablets using a QbD approach

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