Bollettino chimico farmaceutico最新文献

A series of 1-methyl-4-(4-X-arylsulfonyl)pyrrolo[2,3-d]imidazo-le-5-carboxylates were synthesized and tested as anti-inflammatory agents. Indomethacin was used as reference drug. Two of the synthesized compounds 7a and 7b had an effect equal to 0.1 of indomethacin. Our result showed that the electron-withdrawing substituents in the para position of the benzensulfonyl moiety increase activity.

In samples of normal table water, the level of pH is significantly lower than that of reference samples, when an aliquot of water originating from the springs close to the sanctuary to the Virgin Mary at Lourdes at a final dilution rate of 1:400,000 parts has been added to the sample of water tested. The differences as compared to the reference waters, that is those samples to which the aliquot of Lourdes water were not added, were tested by analysis of the variance and were found to be highly significant. The measurements were conducted on approximately 600 samples. It was demonstrated that the phenomenon observed could not be attributed to chemical species present in the Lourdes water which can justify the lowering of the pH in relation to the dilution rate with which the work was performed.

The objective of this study was to formulate a hydrogel-forming bioadhesive drug delivery system for oral administration of verapamil HCl (VP). This system is a non-distintegrating gastro-retentive tablet to allow continuous slow release of VP in the stomach medium where it is more soluble. Different formulate of VP tablets were prepared by compression using various proportions of hydroxypropyl cellulose (HPC) and carbopol 934p (CP). The effect of polymer concentration on the release profile, water uptake and in vitro bioadhesion was studied. Five formulae (F3-F7) exhibited slow release profiles. Formulations F6 (40% HPC and 30% CP) and F7 (40% HPC and 40% CP) had the slowest. They showed 63.6 and 52.2% drug release, respectively, after 12 hours. The kinetic analysis of the release data demonstrated that the bigbest linearity were achieved when data fitted in Higuchi equation rather than zero or first order equations. They had n values close to 0.5 that confirming their Higuchi diffusion. F3 showed the highest swelling index (101.2%), however, the detachment force was intermediate (1.427 N/cm2). Formulae (F4-F7) showed relatively strong in-vitro bioadhesive force. They had detachment forces higher than 1 N/cm2. In general, a delay in drug release and an increase in the in-vitro bioadhesion was seen with the increase in both polymer concentrations. The in vitro data revealed that Formulae F4-F7 served the dual purpose of bioadhesion and sustained release.

This issue is an attempt to be compared the compliance, respectively non-compliance among pharmacy patients between the years 1998 and 2001. The authors make an attempt to elucidate the factors that influence the non-compliance of the patients in order to improve it and to increase the rate of compliance among them. A questionnaire is applied for assessment the state of compliance and non-compliance among the pharmacy patients. The results of the analysis of the received data show that the level of compliance was 69% in 1998 and has decreased to 53% in 2001. The main reasons that influence the non-adherence of the patients are shown.

Two novel series of 1,4-naphthoquinone derivatives have been synthesized namely; N-ethoxycarbonyl-2-ethoxycarbonyloxy-3- alkyl-1,4-naphthoquinon-1-substituted phenylhydrazones 3a-f and 2-chlorocetyloxy-3-alkyl-1,4-naphthoquinone-1-substituted phenylhydrazones 4a-d. The antimicrobial activity as well as anticancer activity of these compounds have been evaluated. The acute toxicity of the active compounds was determined.

The paper presents synthesis of ethyl 6-methyl-4-arylamine-4-sulfonamide-2-phenyl-5-carboxypyrimidine derivatives and the results of microbiological tests of new derivatives performed on selected bacterial strains.

A rapid and sensitive high-performance liquid chromatographic method for the determination of cyproterone acetate in human plasma has been developed. The chromatographic separation was performed on an analytical mbondapak C8 column (125 yen 4.6 mm, i.d) with an isocratic mobile phase consisting of methanol-water (62.38 v/v). Using ultra violet detection at 282 nm, the detection limit for cyproterone acetate in plasma was 10 ng/ml. The calibration curve was linear over the concentration range 50-160. 0 ng/ml. Cyproterone was isolated from plasma by liquid-liquid extraction and the recovery was about 90% for plasma. The inter-day and intra-day assay coefficients of variation were found to be less than 10%.

New complexes of the general formula MCl3.L where L1 = [N-p-chlorophenyl)-alpha-(2-xanthatonaphthol)nitrone, L2 = [N-(p-anisole)-alpha-(2-xanthatonaphthol)nitrone]; M = Ge(IV) and Sn(IV) have been synthesized and characterized by elemental analyses, i.r. and molar conductances. The antibacterial activities of these ligands and their complexes have been studied against six species of bacteria in vitro at concentration ranging from 1-10 micrograms/ml. No activity were observed for the both ligands while a remarkable activities were exhibited by some complexes of both ions Ge(IV) and Sn(IV) against S. aureus, B. subtilis and P. mirabilis even more than the effect of antibacterial used in this study.