FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2899386032> ?p ?o ?g. }

• W2899386032 endingPage "5696" @default.
• W2899386032 startingPage "5678" @default.
• W2899386032 abstract "The absolute bioavailability of many small molecule kinase inhibitors (smKIs) is low. The reasons for low bioavailability are multifaceted and include constraints due to first pass metabolism and poor absorption. For smKIs where absorption limits oral bioavailability, low aqueous solubility and high lipophilicity, often in combination with high-dose requirements have been implicated in low and variable absorption, food-effects, and absorption-related drug-drug interactions. The current study has evaluated whether preparation of smKIs as lipophilic salts/ionic liquids in combination with coadministration with lipid-based formulations is able to enhance absorption for examples of this compound class. Lipophilic (docusate) salt forms of erlotinib, gefitinib, ceritinib, and cabozantinib (as example smKIs demonstrating low aqueous solubility and high lipophilicity) were prepared and isolated as workable powder solids. In each case, the lipophilic salt exhibited high and significantly enhanced solubility in lipidic excipients (>100 mg/g) when compared to the free base or commercial salt form. Isolation as the lipophilic salt facilitated smKI loading in model lipid-based formulations at high concentration, increased in vitro solubilization at gastric and intestinal pH and in some cases increased oral absorption (∼2-fold for cabozantinib formulations in rats). Application of a lipophilic salt approach can therefore facilitate the use of lipid-based formulations for examples of the smKI compound class where low solubility limits absorption and is a risk factor for increased variability due to food-effects." @default.
• W2899386032 created "2018-11-09" @default.
• W2899386032 creator A5005273380 @default.
• W2899386032 creator A5029944399 @default.
• W2899386032 creator A5031843900 @default.
• W2899386032 creator A5033314447 @default.
• W2899386032 creator A5037277601 @default.
• W2899386032 creator A5039410506 @default.
• W2899386032 creator A5040786079 @default.
• W2899386032 creator A5049702051 @default.
• W2899386032 creator A5052059027 @default.
• W2899386032 creator A5053314890 @default.
• W2899386032 creator A5077450680 @default.
• W2899386032 date "2018-10-30" @default.
• W2899386032 modified "2023-10-12" @default.
• W2899386032 title "Enhancing the Oral Absorption of Kinase Inhibitors Using Lipophilic Salts and Lipid-Based Formulations" @default.
• W2899386032 cites W1532616880 @default.
• W2899386032 cites W1976487307 @default.
• W2899386032 cites W1985610919 @default.
• W2899386032 cites W1990392466 @default.
• W2899386032 cites W1991688187 @default.
• W2899386032 cites W1995303261 @default.
• W2899386032 cites W2017422444 @default.
• W2899386032 cites W2027440437 @default.
• W2899386032 cites W2048690056 @default.
• W2899386032 cites W2053386771 @default.
• W2899386032 cites W2057089852 @default.
• W2899386032 cites W2058839845 @default.
• W2899386032 cites W2077550414 @default.
• W2899386032 cites W2077804275 @default.
• W2899386032 cites W2081534823 @default.
• W2899386032 cites W2085075874 @default.
• W2899386032 cites W2090298153 @default.
• W2899386032 cites W2098554428 @default.
• W2899386032 cites W2107120363 @default.
• W2899386032 cites W2112099875 @default.
• W2899386032 cites W2120007372 @default.
• W2899386032 cites W2125956833 @default.
• W2899386032 cites W2128994331 @default.
• W2899386032 cites W2133061394 @default.
• W2899386032 cites W2138778824 @default.
• W2899386032 cites W2143555751 @default.
• W2899386032 cites W2144262303 @default.
• W2899386032 cites W2153132143 @default.
• W2899386032 cites W2157975224 @default.
• W2899386032 cites W2167305078 @default.
• W2899386032 cites W2279926204 @default.
• W2899386032 cites W2317033060 @default.
• W2899386032 cites W2333000505 @default.
• W2899386032 cites W2339649458 @default.
• W2899386032 cites W2531847064 @default.
• W2899386032 cites W2600787041 @default.
• W2899386032 cites W2606007141 @default.
• W2899386032 cites W2617754438 @default.
• W2899386032 cites W2618364642 @default.
• W2899386032 cites W2740583190 @default.
• W2899386032 cites W2760377394 @default.
• W2899386032 cites W2793476737 @default.
• W2899386032 cites W2800839241 @default.
• W2899386032 cites W2889102913 @default.
• W2899386032 doi "https://doi.org/10.1021/acs.molpharmaceut.8b00858" @default.
• W2899386032 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30376336" @default.
• W2899386032 hasPublicationYear "2018" @default.
• W2899386032 type Work @default.
• W2899386032 sameAs 2899386032 @default.
• W2899386032 citedByCount "31" @default.
• W2899386032 countsByYear W28993860322019 @default.
• W2899386032 countsByYear W28993860322020 @default.
• W2899386032 countsByYear W28993860322021 @default.
• W2899386032 countsByYear W28993860322022 @default.
• W2899386032 countsByYear W28993860322023 @default.
• W2899386032 crossrefType "journal-article" @default.
• W2899386032 hasAuthorship W2899386032A5005273380 @default.
• W2899386032 hasAuthorship W2899386032A5029944399 @default.
• W2899386032 hasAuthorship W2899386032A5031843900 @default.
• W2899386032 hasAuthorship W2899386032A5033314447 @default.
• W2899386032 hasAuthorship W2899386032A5037277601 @default.
• W2899386032 hasAuthorship W2899386032A5039410506 @default.
• W2899386032 hasAuthorship W2899386032A5040786079 @default.
• W2899386032 hasAuthorship W2899386032A5049702051 @default.
• W2899386032 hasAuthorship W2899386032A5052059027 @default.
• W2899386032 hasAuthorship W2899386032A5053314890 @default.
• W2899386032 hasAuthorship W2899386032A5077450680 @default.
• W2899386032 hasBestOaLocation W28993860321 @default.
• W2899386032 hasConcept C125287762 @default.
• W2899386032 hasConcept C155574463 @default.
• W2899386032 hasConcept C159985019 @default.
• W2899386032 hasConcept C178790620 @default.
• W2899386032 hasConcept C181389837 @default.
• W2899386032 hasConcept C185592680 @default.
• W2899386032 hasConcept C192562407 @default.
• W2899386032 hasConcept C201399114 @default.
• W2899386032 hasConcept C2780035454 @default.
• W2899386032 hasConcept C43617362 @default.
• W2899386032 hasConcept C71924100 @default.
• W2899386032 hasConcept C98274493 @default.
• W2899386032 hasConceptScore W2899386032C125287762 @default.
• W2899386032 hasConceptScore W2899386032C155574463 @default.

• next