Synthesis, Oral Bioavailability Determination, and in vitro Evaluation of Prodrugs of the Antiviral Agent 9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA)

1994 ◽  
Vol 37 (12) ◽  
pp. 1857-1864 ◽  
Author(s):  
John E. Jr. Starrett ◽  
David R. Tortolani ◽  
John Russell ◽  
Michael J. M. Hitchcock ◽  
Valerie Whiterock ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Antiviral Agent ◽  
In Vitro Evaluation

ChemInform Abstract: Synthesis, Oral Bioavailability Determination, and in vitro Evaluation of Prodrugs of the Antiviral Agent 9-(2-(Phosphonomethoxy)ethyl) adenine (PMEA).

ChemInform ◽  
2010 ◽  
Vol 25 (44) ◽  
pp. no-no
Author(s):  
J. E. JUN. STARRETT ◽  
D. R. TORTOLANI ◽  
J. RUSSELL ◽  
M. J. M. HITCHCOCK ◽  
V. WHITEROCK ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Antiviral Agent ◽  
In Vitro Evaluation

Enhanced Solubility and Oral Bioavailability of Hydrophobic Drugs Using Pluronic Nanomicelles: An In‐Vitro Evaluation

2021 ◽  
Vol 6 (28) ◽  
pp. 7040-7048
Author(s):  
Sofiya J. Shaikh ◽  
Hemil S. Patel ◽  
Debes Ray ◽  
Vinod K. Aswal ◽  
Sushmita Singh ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Hydrophobic Drugs ◽  
In Vitro Evaluation ◽  
Enhanced Solubility

scholarly journals Pharmacokinetics of the Antiviral Agent β-d-2′-Deoxy-2′-Fluoro-2′-C-Methylcytidine in Rhesus Monkeys

2007 ◽  
Vol 51 (8) ◽  
pp. 2877-2882 ◽  
Author(s):  
Ghazia Asif ◽  
Selwyn J. Hurwitz ◽  
Junxing Shi ◽  
Brenda I. Hernandez-Santiago ◽  
Raymond F. Schinazi
Keyword(s):  
Oral Bioavailability ◽  
Rhesus Monkeys ◽  
Antiviral Agent ◽  
Parent Drug ◽  
Pharmacokinetic Studies ◽  
Effective Inhibitor ◽  
Noncompartmental Analysis ◽  
Absorption Time ◽  
Human Whole Blood

ABSTRACT β-d-2′-Deoxy-2′-fluoro-2′-C-methylcytidine (PSI-6130) is an effective inhibitor of hepatitis C virus (HCV) replication in vitro. The purpose of this study was to evaluate the single-dose pharmacokinetics of PSΙ-6130 in rhesus monkeys following intravenous (i.v.) and oral administration. Noncompartmental analysis of the serum data obtained following oral and i.v. administration was performed. Pharmacokinetic studies with rhesus monkeys indicated slow and incomplete absorption with a mean absorption time (MAT) of 4.6 h and an oral bioavailability of 24.0% ± 14.3% (mean ± standard deviation), with comparable mean apparent half-lives following i.v. (4.54 ± 3.98 h) and oral (5.64 ± 1.13 h) administrations. The average percentages of the total dose recovered unchanged and in deaminated form in the urine were 32.9% ± 12.6% and 18.9% ± 6.6% (i.v.) and 6.0% ± 3.9% and 3.9% ± 1.0% (oral), respectively. The total bioavailability, taking into account the parent drug and its deaminated metabolite 2′-deoxy-2′-fluoro-2′-C-methyluridine (PSI-6206), was 64% ± 26%. PSI-6130 was present in the cerebrospinal fluid after oral and i.v. dosing. However, no deamination of radiolabeled PSI-6130 was detected after 8 h of incubation in monkey and human whole blood. An N 4-modified prodrug of PSI-6130 (PSI-6419) was orally administered to monkeys, but it failed to improve the oral bioavailability of PSI-6130. Further studies are warranted to improve the oral bioavailability and reduce the deamination of PSI-6130 in order to explore the potential of this drug for the treatment of HCV-infected individuals.

scholarly journals The oral bioavailability, excretion and cytochrome P450 inhibition properties of epiberberine: an in vivo and in vitro evaluation

2017 ◽  
Vol Volume 12 ◽  
pp. 57-65 ◽  
Author(s):  
Ning Chen ◽  
Xiao-yan Yang ◽  
Chang-e Guo ◽  
Xin-ning Bi ◽  
Jian-hua Chen ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Oral Bioavailability ◽  
In Vitro Evaluation

scholarly journals Fabrication, characterization and in vitro evaluation of silibinin nanoparticles: an attempt to enhance its oral bioavailability

2017 ◽  
Vol Volume 11 ◽  
pp. 1453-1464 ◽  
Author(s):  
Muhammad Umar Khayam Sahibzada ◽  
Abdul Sadiq ◽  
Shahzeb Khan ◽  
Hani S Faidah ◽  
Naseem Ullah ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
In Vitro Evaluation

In vitro evaluation of IL-18 effects in Crohn's disease

2001 ◽  
Vol 120 (5) ◽  
pp. A316-A317
Author(s):  
P MAERTEN ◽  
S COLPAERT ◽  
Z LIU ◽  
K GEBOES ◽  
J CEUPPENS ◽  
...  
Keyword(s):  
Crohn’S Disease ◽  
Crohn's Disease ◽  
In Vitro Evaluation

52: In Vitro Evaluation of Ureteral Stent Compression

2006 ◽  
Vol 175 (4S) ◽  
pp. 18-18
Author(s):  
Kari Hendlin ◽  
Krishna Vedula ◽  
Christina Horn ◽  
Manoj Monga
Keyword(s):  
Ureteral Stent ◽  
In Vitro Evaluation
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