Yet Another Doctor Blog On The Internet

Evaluation of DNA adduction of AZT in peripheral blood leukocytes of HIV-infected individuals by (32)P-post-labeling thin-layer chromatography: a feasibility study.


The pharmacokinetics of two naproxen tablet formulations were compared after oral administration. The 250-mg naproxen tablets, tablet I from AFI, Oslo, Norway, and tablet II Naprosyn, Astra-Syntex, were taken by 12 healthy volunteers in a randomized two-period crossover study. Plasma levels of naproxen were measured by a sensitive and specific HPLC method. The data were analyzed by means of two-way analysis of variance to test for significant differences between tablet formulation and differences between the first and second trial periods. Rapid absorption, with most Cmax values from 50-60 micrograms/ml reached within 1.5-3 h, was found for both tablet formulations. No significant difference was found in the rate and extent of absorption between the two formulations: the relative bioavailability of tablet I compared to tablet II was 1.05 +/- 0.21 (mean +/- SD). The naproxen concentration 2 h after ingestion and the Cmax were higher on the second occasion, regardless of preparation, suggesting that the subjects were clinically different on the two occasions.

Our purpose was to compare the effects of high-intensity transcutaneous electrical nerve stimulation and oral naproxen (500 mg) on intrauterine pressure and menstrual pain.

Detection of nonsteroidal anti-inflammatory drugs (NSAIDs) in equine plasma is a significant analytical problem in veterinary anti-doping controls.

Analgesics are the most commonly consumed over-the-counter preparations in the United States. They are used in the treatment of various pain syndromes and other medical conditions. Although analgesics are generally perceived to be safe agents, serious toxicity may occur in the setting of acute overdose, chronic abuse, or overuse. The indications for therapeutic drug monitoring in patients using these medications appropriately is as yet not well defined. The emphasis of this discussion, therefore, is on recommendations for monitoring in situations where toxicity is suspected. Preanalytical, analytical, and practice issues including drug interactions, frequency of monitoring, pertinent ancillary tests, reporting, and special patient groups at risk for toxicity are reviewed. Recent information from a major manufacturer of evacuated tubes arguing against the use of gel tubes for blood collection for drug monitoring is included. Colorimetric/enzymatic/immunoassays for the routine/stat monitoring of acetaminophen and salicylate and diflunisal cross-reactivity with most of the currently used salicylate assays are presented. Achiral and chiral chromatographic assays and newly introduced columns such as restricted access media and/or automated chromatographic systems are reviewed for the analysis of ibuprofen, naproxen, and the recently introduced tramadol. Finally, concepts regarding future directions including drug chirality and chiral analysis are presented.

The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to that estimated from theoretical equations.

Naproxen might be accepted as an important inducer for LP, especially for the eruptive form.

In the enantioselective esterification of racemic Naproxen with trimethylsilyl methanol in isooctane by Candida cylindracea lipase, improvements in (S)-naproxen ester productivity and enzyme selectivity were demonstrated by adding bis(2-ethylhexyl) sodium sulfosuccinate (AOT) as the best surfactant. The effect of water content on the enhancement of enzyme activity was elucidated from the reduced adsorption of surfactant molecules on the lipase. A competitive inhibition by the alcohol and a noncompetitive inhibition by the surfactant to the enzyme were found from the kinetic analysis. By using a two-phase extraction, a complete separation of the surfactant from the organic solution was obtained.

Changes in naproxen (NAP) 13C-chemical shifts were measured as a function of the concentration of alpha-, beta-, and gamma-cyclodextrin (alpha Cd, beta Cd, and gamma Cd, respectively) in aqueous solution in order to obtain details on the mechanism, geometry, and stoichiometry of the respective interactions. The probable structures of the inclusion compounds of NAP with natural cyclodextrins were constructed using a molecular graphics program. The higher stability of the beta Cd:NAP 1:1 (mol/mol) complex in comparison with alpha Cd:NAP 2:1 (mol/mol) and gamma Cd:NAP 1:1 or 1:2 (mol/mol) complexes was accounted for in terms of a deeper, more complete, and better fitting inclusion of the drug into the cavity of beta Cd. The inclusion behavior of NAP with some statistically substituted beta Cd derivatives [hydroxyethyl-beta Cd (HE beta Cd), hydroxypropyl-beta Cd (HP beta Cd), and methyl-beta Cd (M beta Cd)] was also investigated through 13C-NMR, UV, circular dichroism spectroscopy, and phase-solubility analysis. The stoichiometry of host:guest interactions was the same as with beta Cd, as were thermodynamics and basic complexation mechanisms. The binding between the host and guest molecules is thought to be mainly due to van der Waals, dipole-dipole, and hydrophobic interactions. The inclusion ability of the parent beta Cd was enhanced by the introduction of methyl, hydroxyethyl, and hydroxypropyl groups. The M beta Cd formed the most stable inclusion complex (apparent formation constant K(1:1) = 6892 L.mol-1 at 298 K); it was about three times more stable than those with HP beta Cd or HE beta Cd and four times more stable than that with beta Cd.(ABSTRACT TRUNCATED AT 250 WORDS)