Enhanced Gastrointestinal Absorption of Lipophilic Drugs

2006 ◽  
Author(s):  
Amnon Hoffman ◽  
Arik Dahan
Keyword(s):  
Gastrointestinal Absorption ◽  
Lipophilic Drugs

Chaotropic salts impact in HPLC approaches for simultaneous analysis of hydrophilic and lipophilic drugs

2021 ◽  
Author(s):  
Nataliia Shulyak ◽  
Marjan Piponski ◽  
Sergiy Kovalenko ◽  
Tanja Bakovska Stoimenova ◽  
Iryna Drapak ◽  
...  
Keyword(s):  
Simultaneous Analysis ◽  
Lipophilic Drugs ◽  
Chaotropic Salts

„IN SILICO“ PREDICTION OF PHARMACOKINETIC PROPERTIES AND DRUGLIKENESS OF NOVEL THIOUREA DERIVATIVES OF NAPROXEN

2021 ◽  
Author(s):  
Nikola V. Nedeljković ◽  
◽  
Vladimir D. Dobričić ◽  
Marina Ž. Mijajlović ◽  
Gordana P. Radić ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Aromatic Amines ◽  
Gastrointestinal Absorption ◽  
Skin Permeability ◽  
Thiourea Derivatives ◽  
Barrier Permeability ◽  
Brain Barrier Permeability ◽  
Pharmacokinetic Properties ◽  
Inhibitory Potential ◽  
Derivatives Of

Masking the carboxyl group of naproxen with other functional groups may be a promising strategy to decrease its gastrointestinal toxicity. Thiourea moiety has been described as an important pharmacophore in a variety of pharmacologically active compounds, including anti-inflammatory, antiviral, anticancer, hypoglycemic and antimicrobial agents. Our research group has previously designed twenty novel thiourea derivatives of naproxen, containing amino acids (glycine, L-alanine, β-alanine, L-valine and L-phenylalanine – compounds 1,2,3,4 and 5, respectively), their methyl (6–10) and ethyl esters (11–15), as well as aromatic amines (16–20). Pharmacokinetic properties and druglikeness of these compounds were predicted using SwissADME web tool (http://www.swissadme.ch/). Predicted pharmacokinetic properties include potential for gastrointestinal absorption, blood-brain barrier permeability, skin permeability, transport mediated by P-glycoproteins and enzyme inhibitory potential. Druglikeness was evaluated using Lipinski’s, Ghose’s, Veber’s, Egan’s and Muegge’s rules, as well as on the basis of bioavailability score. All tested compounds had high-predicted gastrointestinal absorption and low blood-brain barrier permeability. Also, derivatives 2, 4, 7, 9, 10, 12, 14, 15 and 18 were predicted to be substrates for P-glycoprotein. Derivatives with aromatic amines (16–20) showed inhibitory potential against all tested CYP isoforms. Derivative 19 had the highest, while derivative 13 demonstrated the lowest predicted skin permeability. Finally, derivatives 1–12, except 5 and 10, have druglike structures, since they obey to all imposed rules.

The Treatment of Iron-deficiency Anemia—Palatable but Ineffective Iron Medication

PEDIATRICS ◽  
1963 ◽  
Vol 31 (6) ◽  
pp. 1041-1044
Author(s):  
LOUIS K DIAMOND ◽  
J. LAWRENCE NAIMAN ◽  
DONALD M. ALLEN ◽  
FRANK A. OSKI,
Keyword(s):  
Iron Deficiency ◽  
Iron Deficiency Anemia ◽  
Ferrous Sulfate ◽  
Oral Iron ◽  
Gastrointestinal Absorption ◽  
Deficiency Anemia ◽  
Therapeutic Effects ◽  
Rapid Rise ◽  
Carbohydrate Complex ◽  
Therapeutic Results

Experience with a new oral iron-carbohydrate complex (Jefron) in the treatment of iron-deficiency anemia shows that the therapeutic results are inferior to those obtainable with ferrous sulfate. Many children showed no response after months of treatment with this drug and when subsequently placed on ferrous sulfate therapy showed a rapid rise in hemoglobin to normal levels. Preliminary studies suggest that poor gastrointestinal absorption may be a factor in the inadequate therapeutic effects.

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