Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Anders Buur"'
Publikováno v:
International Journal of Pharmaceutics. 156:67-77
Isothermal microcalorimetry was evaluated for the determination of the critical relative humidity (cRH) for three drug substances possessing different hygroscopic properties. Two extremely water-soluble substances (flupentixol,2HCl and Lu 25–109, w
Publikováno v:
International Journal of Pharmaceutics. 132:243-250
Various N1-alkoxycarbonyl prodrugs of 5-fluorouracil (5-FU) ranging from 5 to 18 carbon units in the pro-moiety were synthesized. The compounds were physico-chemically characterized by determining the ionization constant (Ka), aqueous solubility (S),
Publikováno v:
International Journal of Pharmaceutics. 129:223-231
The toxicity and permeability of 5-fluorouracil (5FU) and 13 5FU prodrugs was investigated in Caco-2 monolayers grown on permeable supports. Only one of the prodrugs (VII) was toxic to the cell monolayers at 1 × 10 −4 M, as assessed by an increase
Publikováno v:
Pharmaceutical Research. 12:387-392
A series of O-cyclopropane carboxylic acid ester prodrugs of various beta-blocking agents was synthesized. All prodrugs were hydrolyzed to give their parent compounds in aqueous phosphate buffer of pH 7.4 and in 80% human plasma. The half-lives in bu
Publikováno v:
Pharmaceutical Research. 10:68-74
Various aliphatic carboxylic acid esters and a carbonate ester of the tyrosine phenolic group in desmopressin were synthesized to assess their suitability as prodrugs with improved bioavailability compared to the parent peptide. The chemical stabilit
Autor:
Anders Buur, Niels Mørk
Publikováno v:
Pharmaceutical Research. :1290-1294
Testosterone has previously been used as a model compound for the determination of unstirred water layer thickness in the CACO-2 transport model. We have found, however, that testosterone is metabolized during in vitro transport across the CACO-2 cel
Publikováno v:
Pharmaceutical Research. :728-733
The main objective of this study was to investigate how enzymatic lability would affect the extent of corneal and conjunctival penetration of a series of alkyl, cycloalkyl, and aryl ester prodrugs of timolol in the pigmented rabbit. Enzymatic labilit
Publikováno v:
International Journal of Pharmaceutics. 66:183-191
The feasibility of improving the poor oral bioavailability of the tripeptide TRH (pGlu-His-Pro-NH 2 ) was examined using the prodrug approach. The prodrugs studied were various N -alkoxycarbonyl derivatives formed by reacting TRH with the appropriate
Publikováno v:
Journal of Controlled Release. 14:43-51
The penetration of 5-fluorouracil (5-FU) and five of its prodrugs across the duodenum, jejunum, ileum, colon and rectum of the albino rabbit was studied using the modified Ussing chamber. The prodrugs were the 1-ethoxycarbonyl, 1-isopropyloxycarbonyl
Autor:
Vincent H. L. Lees, Anders Buur
Publikováno v:
Drug Delivery System. 5:227-230
The transport of 5-fluorouracil (5-FU) and its prodrugs across the duodenum, jejunum, ileum, colon, and rectum of the albino rabbits was examined using the modified Ussing Chamber. 5-FU penetrated the jejunum, most readily, followed by the duodenum,