Relative bioavailability estimation of carbamazepine crystal forms using an artificial stomach-duodenum model

Carino, Stephen R.; Sperry, David C.; Hawley, Michael

doi:10.1002/jps.20495

Cited by 122 publications

(97 citation statements)

References 16 publications

(21 reference statements)

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“…The different performances in both tests that might be attributed to the dynamic conditions presented some difficulty in choosing a more predictive in vitro test. The exposures of dissolved drug in ASD fluid have been successfully used to rank order systemic AUC and C max for several carbamazepine products (39). Therefore, adopting the same method, we could predict the rank order of in vivo AUC and C max for these tablets as HSWG>RCS=RCD, which was consistent with the clinical observation.…”

Section: Discussionsupporting

confidence: 68%

Assessment of In Vivo Clinical Product Performance of a Weak Basic Drug by Integration of In Vitro Dissolution Tests and Physiologically Based Absorption Modeling

Ding

Gueorguieva

Wesley

et al. 2015

AAPS J

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Abstract. Effective integration of in vitro tests and absorption modeling can greatly improve our capability in understanding, comparing, and predicting in vivo performances of clinical drug products. In this case, we used a proprietary drug candidate galunisertib to describe the procedures of designing key in vitro tests, analyzing relevant experimental and trial data, and integrating them into physiologically based absorption models to evaluate the performances of its clinical products. By simulating the preclinical study result, we estimated high in vivo permeability for the drug. Given the high sensitivity of its solubility to pH, supersaturation may play an important role in the absorption of galunisertib. Using the dynamic dissolution test, i.e., artificial stomach-duodenum (ASD) model and simulation, we concluded galunisertib in solution or tablet products could maintain supersaturation during the transit in the gastrointestinal tract (GIT). A physiologically based absorption model was established by incorporating these key inputs in the simulation of Trial 1 results of galunisertib solution. To predict the performance of three tablet products, we developed z-factor dissolution models from the multi-pH USP dissolution results and integrate them into the absorption model. The resultant biopharmaceutical models provided good prediction of the extent of absorption of all three products, but underestimated the rate of absorption of one tablet product. Leveraging the ASD result and optimization with the dissolution model, we identified the limitation of the model due to complexity of estimating the dissolution parameter z and its in vitro-in vivo correlation.

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Section: Discussionsupporting

confidence: 68%

Assessment of In Vivo Clinical Product Performance of a Weak Basic Drug by Integration of In Vitro Dissolution Tests and Physiologically Based Absorption Modeling

Ding

Gueorguieva

Wesley

et al. 2015

AAPS J

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“…On account of many factors such as crystal habit, size and even polymorphic forms of a drug, dissolution rates would enhance through habit recrystallization. A number of reports in the literature validated the effects of crystal morphology variation on solubility, in vitro dissolution rate, holding potentials for improving drug bioavailability (Kawashima et al, 1986;Carino et al, 2006). Several studies in this filed have shown that exposure of diverse crystal faces determines the nature of the wettability and consequent enhancements in dissolution rate of the drugs with different crystalline shapes (Heng et al, 2006).…”

Section: Solubility Dissolution and Bioavailability Of Drugsmentioning

confidence: 88%

Recrystallization of Drugs: Significance on Pharmaceutical Processing

Javadzadeh¹,

Hamedeyazdan²,

Asnaashari³

2012

Recrystallization

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“…This shows the significant progress that has been made since the first compendial dissolution test (USP I apparatus) was introduced in 1970 Consequently, to mimic and more closely reflect the possible in vivo dosage form surface exposure, have reliable dissolution data and be able to discriminate between release behaviour of various modified release formulations, it is therefore important that we gain a better understanding of the role of hydrodynamics in relation to delivery system and release mechanisms necessary for the development of alternative dissolution methods [136,137]. The other two compendial dissolution apparatuses are the USP III (reciprocating cylinder, Bio-Dis) and IV (flow-through cell) which offer the advantages of determining release from the dosage form under various, consecutive conditions simulating the GI physiology.…”

Section: Dissolution Apparatusesmentioning

confidence: 99%

Drug release from matrix tablets: physiological parameters and the effect of food

Nokhodchi

Asare-Addo

2014

Expert Opinion on Drug Delivery

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Introduction: As dissolution plays an important and vital role in the drug-delivery process of oral solid dosage forms, it is, therefore, essential to critically evaluate the parameters that can affect this process. Areas covered:The consumption of food as well as the physiological environment and properties of the gastrointestinal tract, such as its volume and composition of fluid, the fluid hydrodynamics, properties of the intestinal membrane, drug dose and solubility, pK a , diffusion coefficient, permeability and particle size, all affect drug dissolution and absorption rate. There are several dissolution approaches that have been developed to address the conditions as experienced in the in vivo environment, as the traditional dissolution being a quality control method is not biorelevant and as such do not always produce meaningful data. This review also describes the development of a systematic way that differentiates between robust and non-robust formulations by varying the effects of agitation and ionic strength through the use of the automated United States Pharmacopeia type III Bio-Dis apparatus. Expert opinion:With the improved understanding of the physiological parameters that can affect the oral bioperformance of dosage forms, strides have, therefore, been made in making dissolution testing methods more bio-logically based with the view of obtaining more in vitro--in vivo correlations.Keywords: agitation rate, biodissolution, drug release, effect of food, hydrophilic matrices, ionic strength Highlights -Understanding all the physiological parameters can serve as a basis for designing dissolution testing methods and systems that can more fully represent the gastrointestinal (GI) tract in humans and allow more in vitro-in vivo (IVIVC) correlations to be obtained thereby improving the oral bioperformance of dosage forms.-Simulation of GI conditions is essential to adequately predict the in vivo behaviour of drug formulations.-The choice of appropriate media for in vitro tests is crucial to their ability to correctly forecast the food effect in pharmacokinetic studies.-Several methods of dissolution testing have been conducted and are still ongoing that seek to further understand and develop media and dissolution methods to better represent the in vivo conditions and to aid in the better prediction of in vivo drug release.-Systematic change of agitation method and ionic strength evaluation may be used as additional tools in allowing for the identification of potential fed and fasted effects on drug release from hydrophilic matrices in the drive for developing dissolution methodologies that are more relevant in helping to achieve more IVIVC.

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Relative bioavailability estimation of carbamazepine crystal forms using an artificial stomach-duodenum model

Cited by 122 publications

References 16 publications

Assessment of In Vivo Clinical Product Performance of a Weak Basic Drug by Integration of In Vitro Dissolution Tests and Physiologically Based Absorption Modeling

Assessment of In Vivo Clinical Product Performance of a Weak Basic Drug by Integration of In Vitro Dissolution Tests and Physiologically Based Absorption Modeling

Recrystallization of Drugs: Significance on Pharmaceutical Processing

Drug release from matrix tablets: physiological parameters and the effect of food

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