Biorelevant in-vitro performance testing of orally administered dosage forms

Reppas, Christos

doi:10.1111/j.2042-7158.2012.01474.x

Cited by 45 publications

(26 citation statements)

References 82 publications

(185 reference statements)

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“…Upon the publication of the BCS article,24 these type of studies triggered off the development of biorelevant media in particular for solubility–dissolution studies of class II compounds 66. A comprehensive complete review article on the use of biorelevant media for the in vitro testing of orally administered dosage forms was published recently 67…”

Section: Scientific Aspects Of Oral Drug Absorptionmentioning

confidence: 99%

Antituberculosis therapy-induced acute liver failure: Magnitude, profile, prognosis, and predictors of outcome

et al. 2010

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Section: Scientific Aspects Of Oral Drug Absorptionmentioning

confidence: 99%

Antituberculosis therapy-induced acute liver failure: Magnitude, profile, prognosis, and predictors of outcome

et al. 2010

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“…The importance of these particular parameters is evident as similar approaches have been adopted in the characterisation of other gastro-intestinal fluids [7][8][9][10][11][12][13]. Extensive research has been carried out over the past few decades in the design and development of, and application of, biorelevant media representing other gastro-intestinal fluids in both the fed and fasted states [11,[14][15][16][17][18][19][20]. However, saliva remains less well characterised.…”

Section: Introductionmentioning

confidence: 99%

Characterisation of human saliva as a platform for oral dissolution medium development

Gittings

Turnbull

Henry

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

128

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Human saliva is a biological fluid of great importance in the field of dissolution testing. However, until now, no consensus has been reached on its key characteristics relevant to dissolution testing. As a result, it is difficult to select or develop an in vitro dissolution medium to best represent human saliva. In this study, the pH, buffer capacity, surface tension, viscosity and flow rate of both unstimulated (US) and stimulated (SS) human saliva were investigated in order to provide a platform of reference for future dissolution studies using simulated salivary fluids. Age and gender related differences in a sample size of 30 participants for each parameter were investigated. Significant differences were established between US and SS for all characteristics except surface tension. Therefore, the requirement for using two simulated salivary fluids should be considered when developing an oral dissolution model.

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“…In vitro evaluation of dissolution from modified release products into the lumen of lower intestine is addressed by using various, typically multicompartmental, setups and focusing to the robustness of dosage form throughout the gastrointestinal (GI) lumen but, also, by using single‐compartment setups focusing on the impact of luminal composition and mechanical stresses on the dosage form performance …”

Section: Introductionmentioning

confidence: 99%

Two-Stage Single-Compartment Models to Evaluate Dissolution in the Lower Intestine

Markopoulos

Vertzoni

Symillides

et al. 2015

Journal of Pharmaceutical Sciences

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The purpose was to propose two-stage single-compartment models for evaluating dissolution characteristics in distal ileum and ascending colon, under conditions simulating the bioavailability and bioequivalence studies in fasted and fed state by using the mini-paddle and the compendial flow-through apparatus (closed-loop mode). Immediate release products of two highly dosed active pharmaceutical ingredients (APIs), sulfasalazine and L-870,810, and one mesalamine colon targeting product were used for evaluating their usefulness. Change of medium composition simulating the conditions in distal ileum (SIFileum ) to a medium simulating the conditions in ascending colon in fasted state and in fed state was achieved by adding an appropriate solution in SIFileum . Data with immediate release products suggest that dissolution in lower intestine is substantially different than in upper intestine and is affected by regional pH differences > type/intensity of fluid convection > differences in concentration of other luminal components. Asacol® (400 mg/tab) was more sensitive to type/intensity of fluid convection. In all the cases, data were in line with available human data. Two-stage single-compartment models may be useful for the evaluation of dissolution in lower intestine. The impact of type/intensity of fluid convection and viscosity of media on luminal performance of other APIs and drug products requires further exploration.

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Biorelevant in-vitro performance testing of orally administered dosage forms

Cited by 45 publications

References 82 publications

Antituberculosis therapy-induced acute liver failure: Magnitude, profile, prognosis, and predictors of outcome

Antituberculosis therapy-induced acute liver failure: Magnitude, profile, prognosis, and predictors of outcome

Characterisation of human saliva as a platform for oral dissolution medium development

Two-Stage Single-Compartment Models to Evaluate Dissolution in the Lower Intestine

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