Pharmaceutisch weekblad. Scientific edition最新文献

This is part II of a review on the transport of drugs across the blood-brain barrier. In this part, the emphasis is on the various experimental techniques that can be used to characterize the blood-brain barrier transport of drugs. Generally speaking, three approaches can be distinguished: in vitro techniques using isolated brain capillaries, cerebrovascular endothelial cells in primary culture or endothelium-derived cell lines; in vivo techniques (both single-passage and multi-passage techniques) and in situ perfusion techniques. Each of these techniques has specific advantages and disadvantages associated with it. Therefore, in many instances, a combination of different approaches is needed to study the fundamental aspects of drug transport across the blood-brain barrier.

Sedation is frequently required in children undergoing magnetic resonance imaging (MRI). 172 Paediatric patients (82 female and 90 male, age 42 +/- 26 months, weight 14.7 +/- 5.6 kg) entered an open, non-comparative, prospective study to assess the utilization of oral chloral hydrate. Chloral hydrate syrup (70 mg/ml) was administered 20-30 min prior to the procedure. Effective sedation was reached in 80.3% with an average initial dose of 55 mg/kg and in 93.6% with an average total dose of 65 mg/kg. Significant differences in effectivity were correlated with the dose (54 +/- 11 mg/kg in failure cases versus 66 +/- 16 mg/kg in effective cases; p < 0.05) and diagnosis (effectivity falls to 62.5% and 76.0% in children with medullar tumours and encephalic white matter alterations, respectively; p < 0.01). Average sleep induction time was 30 +/- 19 min, and average duration of sleep was 62 +/- 24 min. Adverse reactions occurred in 4.7%, with nausea, vomiting and stomach pain being the most common side-effects (3.5%). Multivariate statistical analysis selects total dose and age into the discriminant function, with a 100% relative percentage of correct classification. A simple method for optimizing the chloral hydrate dose in children is proposed: the dose in mg/kg is calculated as half the age in months + 50.

The essential oils as well as solvent extracts of 11 hop cultivars, 1 hop variety and a wild type of hop were screened for their antimicrobial activities using the agar overlay technique. The oils were isolated from the cones of the various hop plants by hydrodistillation, the extracts were obtained by soaking the hop cones in chloroform. The oils and the extracts showed activity against the Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) and the fungus (Trichophyton mentagrophytes var. interdigitale), but almost no activity against the Gram-negative bacterium (Escherichia coli) and the yeast (Candida albicans) used in the screening. The peak area percentages of the main volatile components and the contents of the bitter acids of the extracts were determined for all cultivars using chromatographic methods.

A rapid isocratic technique was developed for the analysis of four anthracyclines (doxorubicin, epirubicin, daunorubicin and pirarubicin) in parenteral solutions using high pressure liquid chromatography (HPLC) with fluorescence detection and a C18 Hypersil ODS column. The availability and compatibility of these drugs from solutions infused via PVC infusion bags through PVC administration sets have been examined. No significant drug loss was observed during simulated infusions (n = 4) for 24 h using PVC infusion bags and administration sets. No significant difference was found between infusion solutions (5% glucose or 0.9% NaCl), except for pirarubicin. The reconstitution of pirarubicin in 0.9% NaCl was impossible, because we observed a precipitation of the compound in solution. The stability of the drugs was also studied in solution, in PVC bags after storage at 4 degrees C with protection from light. The results show the stability of doxorubicin, epirubicin and daunorubicin during 7 days of storage to be satisfactory, irrespective of the infusion solution (5% glucose or 0.9% NaCl). In the case of pirarubicin, the stability of the drug was satisfactory during 5 days of storage in 5% glucose, but beyond, we observed a degradation of the compound with formation of doxorubicin in the infusion solution.

The approach in treatment in medical oncology and particularly in the management of solid tumours has to integrate--at least--two targets: the enhancement of therapeutic efficacy, and the respect of global budget assigned to health. Different teams are implicated in such an approach and especially physicians and pharmacists. We decided to conduct a comparative study of three techniques of administering drugs as a continuous infusion. We analysed time and materials required for the preparation in the centralized preparation unit, and for dispensing and nursing in the health units. The use of programmable pumps (CADD-1) leads to overall saving costs of 27 to 40% compared to administration by means of an infusion bag or a motor-drive syringe.