In vitro methods to assess drug precipitation

Dai, Wei

doi:10.1016/j.ijpharm.2010.03.040

Cited by 43 publications

(44 citation statements)

References 119 publications

(146 reference statements)

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“…Not only that the lipase may negatively affect the emulsification and dispersion efficiency of the lipid components, but also the solubilization capacity of the system becomes hampered and the loaded drug tends to precipitate in vivo (Dai, 2010). The sharp change of pH and dilution of the delivery platform in the body fluids are also contributing factors of in vivo drug precipitation.…”

Section: Possibility Of In Vivo Precipitation Of Drugsmentioning

confidence: 99%

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

et al. 2016

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Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an aqueous medium with mild agitation. SEDDS is considered as a potential platform for oral delivery of hydrophobic drug in order to overcome their poor and irregular bioavailability challenges. In spite of fewer advantages like improved solubility of drug, bypassing lymphatic transport etc., SEDDS faces different controversial issues such as the use of appropriate terminology (self-microemulsifying drug delivery system; SMEDDS or self-nanoemulsifying drug delivery system; SNEDDS), presence of high amount of surfactant, correlation of in vitro model to in vivo studies, lack of human volunteer study and effect of conversion of SEDDS to final administrable dosage form on pharmacokinetic behavior of the drug. In this review, potential issues or questions on SEDDS are identified and summarized from the pharmacokinetic point of view. Primarily this review includes the conflict between the influences of droplet size, variation in correlation between in vitro lipolysis or ex-vivo intestinal permeation and pharmacokinetic parameters, variation in in vivo results of solid and liquid SEDDS, and potential challenges or limitation of pharmacokinetic studies on human volunteers with orally administered SEDDS. In the past decades, hundreds of in vivo studies on SEDDS have been published. In the present study, only the relevant article on in vivo pharmacokinetic studies with orally administered SEDDS published in past 5-6 years are analyzed for an up to date compilation. KeywordsPoor bioavailability, self-nanoemulsifying delivery system, self-microemulsifying delivery system, in vitro lipolysis, pharmacokinetic of SEDDS History

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Section: Possibility Of In Vivo Precipitation Of Drugsmentioning

confidence: 99%

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

et al. 2016

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“…The precipitation from supersaturated pharmaceutical system has been extensively investigated; however, literature comparisons with this study are limited for a range of reasons. The majority of methods create a ‘standard’ meta‐stable supersaturated system, examine the influence of excipients on time taken for a precipitate to form ‘naturally’ and report results based on an excipient‐induced precipitation time delay when compared to a free drug system .…”

Section: Discussionmentioning

confidence: 99%

The influence of non-ionisable excipients on precipitation parameters measured using the CheqSol method

Etherson

Halbert

Elliott

2016

Journal of Pharmacy and Pharmacology

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Objectives: The aim of this study was to determine the influence of non-ionisable excipients hydroxypropyl--cyclodextrin (HPCD) and poloxamers 407 and 188 on the supersaturation and precipitation kinetics of ibuprofen, gliclazide, propranolol and atenolol induced through solution pH shifts using the CheqSol method.Methods: The drug's kinetic and intrinsic aqueous solubility was measured in the presence of increasing excipient concentrations using the CheqSol solubility method. Experimental data for example rate of change of pH with time was also examined to determine excipient induced parachute effects and influence on precipitation rates.Key Findings:The measured kinetic and intrinsic solubilities provide a determination of the influence of each excipient on supersaturation index and the area under the CheqSol curve can measure the parachute capability of excipients. The excipients influence on precipitation kinetics can be measured with novel parameters for example the precipitation pH or percentage ionized drug at the precipitation point which provide further information on the excipient induced changes in precipitation performance.Conclusion: This method can therefore be employed to measure the influence of non-ionisable excipients on the kinetic solubility behavior of supersaturated solutions of ionisable drugs and to provide data, which discriminates between excipient systems during precipitation.

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“…An early appreciation of the potential for PDP has important implications in clinical situations, and a rapid in‐vitro screening method would be valuable for parenteral formulation development. Extensive research efforts have been made to develop in‐vitro models for prediction of intestinal absorption . Various in‐vitro screening tools, such as static dilution and dynamic injection methods, have also been developed to detect precipitation of the drugs from intravenous injectable formulations .…”

Section: Introductionmentioning

confidence: 99%

“…Extensive research efforts have been made to develop in‐vitro models for prediction of intestinal absorption . Various in‐vitro screening tools, such as static dilution and dynamic injection methods, have also been developed to detect precipitation of the drugs from intravenous injectable formulations . The use of the in‐vitro dynamic model in place of animals for preliminary phlebitis testing of new intravenous injectables in relation to drug precipitation has been suggested …”

Section: Introductionmentioning

confidence: 99%

In-vitro prediction of bioavailability following extravascular injection of poorly soluble drugs: an insight into clinical failure and the role of delivery systems

Hassan

Shaw

2013

Journal of Pharmacy and Pharmacology

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In vitro methods to assess drug precipitation

Cited by 43 publications

References 119 publications

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

The influence of non-ionisable excipients on precipitation parameters measured using the CheqSol method

In-vitro prediction of bioavailability following extravascular injection of poorly soluble drugs: an insight into clinical failure and the role of delivery systems

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