Preformulation approaches to improve the oral bioavailability of two novel piperidine renin inhibitors in dog

Arzneimittel-Forschung/Drug Research

Volumn 52, Issue 8, 2002, Pages 593-599

  Bittner, Beate ^a   Chou, Ruby ^a   Schleimer, Michael ^a   Morgenroth, Brita ^a   Zell, Manfred ^a   Lavé, Thierry ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

(R) 3 (3S,4R,5R) 4 4 3 (2 Methoxy benzyloxy) propoxy phenyl 5 (4 methoxy naphthalen 2 ylmethoxy) piperidin 3 ylmethoxy propane 1,2 diol

Indexed keywords

1 METHOXY 3 [4 [4 [3 (2 METHOXYBENZYLOXY)PROPOXY]PHENYL] 5 (4 METHOXYNAPHTHALEN 2 YLMETHOXY)PIPERIDIN 3 YLOXY]PROPAN 2 OL; 3 [4 [4 [3 (2 METHOXYBENZYLOXY)PROPOXY]PHENYL] 5 (4 METHOXYNAPHTHALEN 2 YLMETHOXY)PIPERIDIN 3 YLMETHOXY]PROPANE 1,2 DIOL; PIPERIDINE DERIVATIVE; RENIN INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AQUEOUS SOLUTION; ARTICLE; BIOAVAILABILITY; COMPUTER SIMULATION; CONTROLLED STUDY; DRUG METABOLISM; DRUG SOLUBILITY; LIPOPHILICITY; MISCIBILITY; NONHUMAN; PREFORMULATION;

EID: 0036354363     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1299936     Document Type: Article

References (30)

1. Maintenance of blood pressure by the renin angiotensin system in normal man
2. Recent developments in renin inhibitors
3. Renin inhibition
4. Substituted piperidines - Highly potent renin inhibitors due to induced fit adaption of the active site
5. Piperidine renin inhibitors: From leads to drug candidates
6. Prediction of the intestinal absorption of endothelin receptor antagonists using three theoretical methods of increasing complexity
7. Enhanced oral absorption and decreased elimination of paclitaxel in mice cotreated with cyclosporin A
8. Role of P-glycoprotein P 450 3A in limiting oral absorption of peptides and peptidomimetics
9. Intestinal drug absorption enhancement: An overview
10. Absorption enhancers
11. A physicochemical basis for the effect of food on the absolute oral F of halofantrine
12. Physicochemical and physiological mechanisms for the effects of food on drug absorption: The role of lipids and pH
13. Enhancement of oral bioavailability of D-α-tocopherol acetate by lecithin dispersed aqueous preparations containing medium-chain triglycerides in rats
14. Influence of a fat-rich meal on the pharmacokinetics of a new oral formulation of cyclosporin in a crossover comparison with the market formulation
15. A relation between the chain length of fatty acids and the slowing down of gastric emptying
16. Lipid digestion and absorption
17. Lipid-based vehicles for the oral delivery of poorly water-soluble drugs
18. Estimating the maximal potential for intestinal lymphatic transport of lipophilic drug molecules
19. Solubilization of drugs by co-solvents
20. Solubility principles and practices for parenteral drug dosage form development
21. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals
22. Gastric pH profiles of beagle dogs and their use as an alternative to human testing
23. Species similarities and differences in pharmacokinetics
24. A promising animal model in evaluation of first pass metabolism and maximum oral absorption
25. Overlapping substrate specificities of cytochrome P450 3A and p-glycoprotein for a novel cysteine protease inhibitor
26. Improved oral bioavailability of propranolol in healthy human volunteers using a liver bypass drug delivery system containing oleic acid
27. Effect of medium-chain glycerides on physiological properties of rabbit intestinal epithelium in vitro
28. A study of polar lipid drug carrier systems undergoing a thermoreversible lamellar to cubic phase transition
29. Cubic phases as delivery systems for peptide drugs