Search for dissertations about: "P-gp inhibition"

Showing result 1 - 5 of 6 swedish dissertations containing the words P-gp inhibition.

2. 1. ATP-Binding Cassette Efflux Transporters and Passive Membrane Permeability in Drug Absorption and Disposition

   Author : Pär Matsson; Per Artursson; Ulf Norinder; Peter Swaan; Uppsala universitet; []
   Keywords : Pharmaceutics; ATP-binding cassette; ABC transporter; P-gp; P-glycoprotein; ABCB1; BCRP; Breast cancer resistance protein; ABCG2; MRP2; Multidrug-resistance associated protein 2; ABCC2; Membrane permeability; Drug transport; Active transport; Passive diffusion; Multivariate data analysis; PLS; OPLS; QSAR; Galenisk farmaci;

   Abstract : Transport into and across the cells of the human body is a prerequisite for the pharmacological action of drugs. Passive membrane permeability and active transport mechanisms are major determinants of the intestinal absorption of drugs, as well as of the distribution to target tissues and the subsequent metabolism and excretion from the body. READ MORE

4. 2. Molecular heterogeneity of prostate cancer bone metastasis

   Author : Erik Bovinder Ylitalo; Pernilla Wikström; Anders Bergh; Maria Brattsand; Vessela Kristensen; Umeå universitet; []
   Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Prostate cancer; CRPC; castration-resistant; androgen receptor; splice variant; abiraterone; cabazitaxel; ABCB1; cholesterol; Mdr1; P-gp; bone metastasis; immune response; metabolism; osteoblast; osteoclast; BMP; methylation;

   Abstract : Castration-resistant prostate cancer (CRPC) develops after androgen deprivation therapy of advanced PC, often with metastatic growth in bone. Patients with metastatic CRPC have very poor prognosis. Growth of CRPC, in most but not all patients, seems to involve androgen receptor (AR) activity, despite castrate levels of serum testosterone. READ MORE

5. 3. Drug Dissolution under Physiologically Relevant Conditions In Vitro and In Vivo

   Author : Eva Persson; Hans Lennernäs; Bertil Abrahamsson; Peter Langguth; Uppsala universitet; []
   Keywords : Biopharmacy; solubility; drug dissolution; food effects; poorly soluble drugs; P-gp inhibition; drug absorption; pemeability; bile acids; phospholipids; human intestinal fluid; simulated intestinal fluid; neutral lipids; solid phase extraction; HPLC; Efflux; Biofarmaci;

   Abstract : The general aim of the present project was to increase the understanding of the in vivo dissolution of poorly soluble drugs and thereby improve possibility to predict in vivo solubility from substance properties. Increased understanding of the in vivo limitations of drug solubility could potentially also generate ideas for improved formulation principles for poorly soluble compounds and more relevant in vitro dissolution test methods used in formulation development. READ MORE

6. 4. Blood-Brain Barrier Transport : Investigation of Active Efflux using Positron Emission Tomography and Modelling Studies

   Author : Stina Syvänen; Margareta Hammarlund-Udenaes; Mats Bergström; Gunnar Blomquist; Jashvant Unadkat; Uppsala universitet; []
   Keywords : Pharmaceutical biosciences; pharmacokinetics; P-glycoprotein; blood-brain barrier; modelling; PET; active efflux; species differences; [11C]verapamil; drug development; Farmaceutisk biovetenskap;

   Abstract : This thesis examines the transport of exogenous molecules across the blood-brain barrier (BBB), focusing on active efflux, using positron emission tomography (PET), computer simulation and modelling. P-glycoprotein (P-gp) inhibition was studied using [11C]verapamil and [11C]hydroxyurea was investigated as a new marker for active efflux transport. READ MORE

7. 5. Intestinal Permeability and Presystemic Extraction of Fexofenadine and R/S-verapamil

   Author : Christer Tannergren; Hans Lennernäs; Dirk KF Meijer; Uppsala universitet; []
   Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Biopharmacy; Bioavailability; Fexofenadine; Verapamil; P-glycoprotein; CYP3A4; OATP; Enantioselective; Permeability; Caco-2; Intestinal perfusion; Biofarmaci; Biopharmacy; Biofarmaci;

   Abstract : The main objective of this thesis was to investigate the in vivo relevance of membrane transporters and cytochrome P450 (CYP) 3A4-mediated metabolism in the intestine and liver for the bioavailability of drugs in humans after oral administration.In the first part of the thesis, the main transport mechanisms involved in the intestinal absorption and bioavailability were investigated for fexofenadine, a minimally metabolized drug, which is a substrate for P-glycoprotein (P-gp) and members of organic anion transporting polypeptide (OATP) family. READ MORE