The prediction of pH-dependent interaction using micro-dissolution approach in bio-relevant media: Insights from model drug study of lapatinib

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dc.contributor.authorRajpurohit, AUSen_US
dc.contributor.authorPatil, PHen_US
dc.contributor.authorDesai, Men_US
dc.contributor.authorJagadisht, PC.en_US
dc.date.accessioned2024-11-30T11:21:20Z
dc.date.available2024-11-30T11:21:20Z
dc.date.issued2024-06
dc.description.abstractUnderstanding the impact of dynamic alterations in gastrointestinal fluid properties and intestinal dissolution of poorly soluble drugs, such as lapatinib, is crucial for predicting drug absorption in vivo. The current study employs a micro-dissolution pH shift model to forecast the dynamic dissolution of lapatinib in buffer and bio-relevant media by application of analytical design of experiments. The utilization of a Box-Behnken design has resulted in a robust analytical method. According to an in vitro micro-dissolving pH shift experiment in United States Pharmacopeia buffers, lapatinib displays a typical weak base pH-dependent solubility, with 15% drug release at pH 1.2 and dropping to 2% at pH 6.5 buffers. In contrast, the solubility of the compound was initially measured to be 0.0127 mg/ ml in fasted state-simulated gastric fluid; however, pH alterations by the addition of fasted state-simulated intestinal fluid 6.5 resulted in a significant increase to 0.0291 mg/ml. The in vitro pH-effect risk for dissolution experiment in biorelevant media is 0.80, suggesting that the existence of salts in fasted state-simulated intestinal fluid results in the formation of a macroaggregate that is accountable for improved solubility of lapatinib. Thus, using a bio-relevant buffer in a pH shift model may improve this in vitro technique’s predictive ability and aid weakly drug advancement in the intestinal environment.en_US
dc.identifier.affiliationsDepartment of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Indiaen_US
dc.identifier.affiliationsDepartment of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Indiaen_US
dc.identifier.affiliationsDepartment of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Indiaen_US
dc.identifier.affiliationsDepartment of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, India.en_US
dc.identifier.citationRajpurohit AUS, Patil PH, Desai M, Jagadish PC.. The prediction of pH-dependent interaction using micro-dissolution approach in bio-relevant media: Insights from model drug study of lapatinib. Journal of Applied Pharmaceutical Science. 2024 Jun; 14(6): 105-115en_US
dc.identifier.issn2231-3354
dc.identifier.placeIndiaen_US
dc.identifier.urihttps://imsear.searo.who.int/handle/123456789/237701
dc.languageenen_US
dc.publisherOpen Science Publishers LLPen_US
dc.relation.issuenumber6en_US
dc.relation.volume14en_US
dc.source.urihttps://doi.org/10.7324/JAPS.2024.170413en_US
dc.subjectAnalytical QbDen_US
dc.subjectbiorelevant dissolution mediaen_US
dc.subjectpH shiften_US
dc.subjectlapatiniben_US
dc.subjectintestinal absorption.en_US
dc.titleThe prediction of pH-dependent interaction using micro-dissolution approach in bio-relevant media: Insights from model drug study of lapatiniben_US
dc.typeJournal Articleen_US
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