53
Views
0
CrossRef citations to date
0
Altmetric
Research Article

Intestinal Permeability and Role of P-Glycoprotein in Intestinal Absorption of Novel Triethylamine Containing Thiophene S006–830 Using Single-Pass Intestinal Perfusion in Rats

, &
Pages 163-171 | Received 05 Jan 2017, Accepted 18 May 2017, Published online: 13 Jul 2017

References

  • Eedara BB , VeerareddyPR , JukantiR , BandariS . Improved oral bioavailability of fexofenadine hydrochloride using lipid surfactants: ex vivo, in situ and in vivo studies . Drug. Dev. Ind. Pharm.40 ( 8 ), 1030 – 1043 ( 2014 ).
  • Singh Y , HidauMK , SinghSK . Rifabutin reduces systemic exposure of an antimalarial drug 97/78 upon co-administration in rats: an in vivo & in vitro analysis . Asian Pac. J. Trop. Dis.8 ( 8 ), 630 – 635 ( 2015 ).
  • Bergström CA , HolmR , J⊘rgensenSAet al. Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs . Eur. J. Pharm. Sci.57 , 173 – 199 ( 2014 ).
  • Seddon B , WorkmanP . The role of functional and molecular imaging in cancer drug discovery and development . Br. J. Radiol. ( 2014 ).
  • Amidon GL , SinkoPJ , FleisherD . Estimating human oral fraction dose absorbed: a correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds . Pharm. Res.5 ( 10 ), 651 – 654 ( 1988 ).
  • Artursson P , KarlssonJ . Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells . Biochem. Biophys. Res. Commun.175 ( 3 ), 880 – 885 ( 1991 ).
  • Cook TJ , ShenoySS . Intestinal permeability of chlorpyrifos using the single-pass intestinal perfusion method in the rat . Toxicology184 ( 2–3 ), 125 – 133 ( 2003 ).
  • Prentis RA , LisY , WalkerSR . Pharmaceutical innovation by the seven UK-owned pharmaceutical companies (1964–1985) . Br. J. Clin. Pharmacol.25 ( 3 ), 387 – 396 ( 1988 ).
  • Lennernas H . Regional intestinal drug permeation: biopharmaceutics and drug development . Eur. J. Pharm. Sci.57 , 333 – 341 ( 2014 ).
  • Lennernas H . Human in vivo regional intestinal permeability: importance for pharmaceutical drug development . Mol. Pharm.11 ( 1 ), 12 – 23 ( 2014 ).
  • Lennernas H , AaronsL , AugustijnsPet al. Oral biopharmaceutics tools - time for a new initiative - an introduction to the IMI project OrBiTo . Eur. J. Pharm. Sci.57 , 292 – 299 ( 2014 ).
  • Papadopoulou V , ValsamiG , DokoumetzidisA , MacherasP . Biopharmaceutics classification systems for new molecular entities (BCS-NMEs) and marketed drugs (BCS-MD): theoretical basis and practical examples . Int. J. Pharm.361 ( 1–2 ), 70 – 77 ( 2008 ).
  • Cook J , AddicksW , WuYH . Application of the biopharmaceutical classification system in clinical drug development – an industrial view . AAPS J.10 ( 2 ), 306 – 310 ( 2008 ).
  • Eurosurveillance Editorial Team . WHO publishes Global tuberculosis report 2013 . Euro Surveill.18 ( 43 ), pii: 20615 ( 2013 ).
  • Zaman K . Tuberculosis: a global health problem . J. Health. Popul. Nutr.28 ( 2 ), 111 – 113 ( 2010 ).
  • Weiner J , KaufmannS . Recent advances towards tuberculosis control: vaccines and biomarkers . J. Intern. Med.275 ( 5 ), 467 – 480 ( 2014 ).
  • Sloot R , Schim Van Der LoeffMF , KouwPM , BorgdorffMW . Risk of tuberculosis after recent exposure. A 10-year follow-up study of contacts in Amsterdam . Am. J. Respir. Crit. Care Med.190 ( 9 ), 1044 – 1052 ( 2014 ).
  • Trauner A , BorrellS , ReitherK , GagneuxS . Evolution of drug resistance in tuberculosis: recent progress and implications for diagnosis and therapy . Drugs74 ( 10 ), 1063 – 1072 ( 2014 ).
  • Diacon AH , PymA , GrobuschMPet al. Multidrug-resistant tuberculosis and culture conversion with bedaquiline . N. Engl. J. Med.371 ( 8 ), 723 – 732 ( 2014 ).
  • Mitike G , KebedeD , YenenehH . HIV infection and antituberculosis drug resistance among pulmonary tuberculosis patients in Harar Tuberculosis Centre, Ethiopia . East. Afr. Med. J.74 ( 3 ), 154 – 157 ( 1997 ).
  • Chanteau S , RasolofoV , RamarokotoHet al. Anti-tuberculosis drug resistance in Madagascar in 1994–1995 . Int. J. Tuberc. Lung Dis.1 ( 5 ), 405 – 410 ( 1997 ).
  • Ma Z , LienhardtC , McilleronH , NunnAJ , WangX . Global tuberculosis drug development pipeline: the need and the reality . Lancet375 ( 9731 ), 2100 – 2109 ( 2010 ).
  • Kashyap VK , GuptaRK , ShrivastavaRet al. In vivo activity of thiophene-containing trisubstituted methanes against acute and persistent infection of non-tubercular Mycobacterium fortuitum in a murine infection model . J. Antimicrob. Chemother.67 ( 5 ), 1188 – 1197 ( 2012 ).
  • Parai MK , PandaG , ChaturvediV , ManjuYK , SinhaS . Thiophene containing triarylmethanes as antitubercular agents . Bioorg. Med. Chem. Lett.18 ( 1 ), 289 – 292 ( 2008 ).
  • Das SK , PandaG , ChaturvediV , ManjuYS , GaikwadAK , SinhaS . Design, synthesis and antitubercular activity of diarylmethylnaphthol derivatives . Bioorg. Med. Chem. Lett.17 ( 20 ), 5586 – 5589 ( 2007 ).
  • Pailla UR , AravaVR , RavindranathL . Total synthesis of an experimental antitubercular drug CDRI-830 . Synth. Commun.44 ( 23 ), 3408 – 3413 ( 2014 ).
  • Singh Y , HidauMK , MisraAet al. UFLC method development and validation of a novel triethylamine containing thiophene S006–830 - an antitubercular molecule and its application to pharmacokinetic and bioavailability studies in SD rats . Drug Test. Anal.7 ( 8 ), 721 – 726 ( 2015 ).
  • Singh P , MannaSK , JanaAKet al. Thiophene containing trisubstituted methanes [TRSMs] as identified lead against Mycobacterium tuberculosis . Eur. J. Med. Chem.95 , 357 – 368 ( 2015 ).
  • Oshikoya KA , OreagbaIA , LawalSet al. Potential drug–drug interactions in HIV-infected children on antiretroviral therapy in Lagos, Nigeria . HIV AIDS (Auckl)6 , 49 – 59 ( 2014 ).
  • Zhou W , DiLQ , ShanJJ , BiXL , ChenLT , WangLC . Intestinal absorption of forsythoside A in different compositions of Shuang-Huang-Lian . Fitoterapia82 ( 3 ), 375 – 382 ( 2011 ).
  • Zhou W , DiLQ , WangJet al. Intestinal absorption of forsythoside A in in situ single-pass intestinal perfusion and in vitro Caco-2 cell models . Acta Pharmacol. Sin.33 ( 8 ), 1069 – 1079 ( 2012 ).
  • Doherty MM , PangKS . First-pass effect: significance of the intestine for absorption and metabolism . Drug Chem. Toxicol.20 ( 4 ), 329 – 344 ( 1997 ).
  • Li M , SiL , PanHet al. Excipients enhance intestinal absorption of ganciclovir by P-gp inhibition: assessed in vitro by everted gut sac and in situ by improved intestinal perfusion . Int. J. Pharm.403 ( 1–2 ), 37 – 45 ( 2011 ).
  • Fagerholm U , JohanssonM , LennernasH . Comparison between permeability coefficients in rat and human jejunum . Pharm. Res.13 ( 9 ), 1336 – 1342 ( 1996 ).
  • Svensson US , SandstromR , CarlborgO , LennernasH , AshtonM . High in situ rat intestinal permeability of artemisinin unaffected by multiple dosing and with no evidence of P-glycoprotein involvement . Drug Metab. Dispos.27 ( 2 ), 227 – 232 ( 1999 ).
  • Sandstrom R , LennernasH . Repeated oral rifampicin decreases the jejunal permeability of R/S-verapamil in rats . Drug Metab. Dispos.27 ( 8 ), 951 – 955 ( 1999 ).
  • Rabba AK , SiL , XueK , LiM , LiG . In situ intestinal perfusion of irinotecan: application to P-gp mediated drug interaction and introduction of an improved HPLC assay . Res. Rev. J. Pharm. Pharm. Sci.14 ( 2 ), 138 – 147 ( 2011 ).
  • Song NN , LiQS , LiuCX . Intestinal permeability of metformin using single-pass intestinal perfusion in rats . World J. Gastroenterol.12 ( 25 ), 4064 – 4070 ( 2006 ).
  • Salphati L , ChildersK , PanL , TsutsuiK , TakahashiL . Evaluation of a single-pass intestinal-perfusion method in rat for the prediction of absorption in man . J. Pharm. Pharmacol.53 ( 7 ), 1007 – 1013 ( 2001 ).
  • Takagi T , RamachandranC , BermejoM , YamashitaS , YuLX , AmidonGL . A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan . Mol. Pharm.3 ( 6 ), 631 – 643 ( 2006 ).
  • Vogelpoel H , WelinkJ , AmidonGet al. Biowaiver monographs for immediate release solid oral dosage forms based on biopharmaceutics classification system (BCS) literature data: Verapamil hydrochloride, propranolol hydrochloride, and atenolol . J. Pharm. Sci.93 ( 8 ), 1945 – 1956 ( 2004 ).

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.