Bollettino chimico farmaceutico最新文献

Purified African oil bean seed lipoxygenase was used to bleach water yam tubers that were browned by exposing their cut surfaces to air. The enzyme solution destroyed the polyphenols extracted from the browned water yams and the polyphenols at the browned yam tubers which resulted in the bleaching of the browned yam tubers to their original white colour. The destruction of the polyphenol extract and the bleaching of the browned yam tubers were found to be dependent on the enzyme concentration of the enzyme.

Ketoprofen lysine salt (Oki Fiale, PG060) is a non steroidal anti-inflammatory agent frequently administered by intramuscular route in association regimen with other drugs, such as steroidal anti-inflammatory, muscle relaxant, local anaesthetic and anti-spastic drugs or vitamins. The aim of this study was to investigate the physicochemical compatibility between ketoprofen lysine salt (Oki Fiale, PG060) and other injectable drugs frequently used in association. Physicochemical properties of ketoprofen lysine salt mixtures with different drugs, including colour, clarity, pH and drug content were observed or measured before and after (up to 3 hours) mixing at room temperature and under light protection. Results show that the association of Oki Fiale (PG060) with different drugs does not cause, up to three hours from mixing, any significant variation in the physicochemical parameters mentioned above. In conclusion, the results obtained demonstrated the physicochemical compatibility of Ketoprofen lysine salt (Oki Fiale, PG060) with several injectable drugs, except for Spasmex fiale (chemical incompatibility) and Xylocaina Astra 2% iniettabile mixed whit a volume ratio of 2/1 (physical incompatibility).

Cyclodextrins are able to form inclusion complexes with a number of drugs if their molecular dimensions correspond to those of the cyclodextrin cavity which leads to change of physicochemical and biopharmaceutical properties of drugs. 2-Hydroxypropyl beta cyclodextrin (HP beta CD) is suitable for parenteral application because of its considerable solubility in water and low hemolytic activity. Digoxin is insoluble in water, sensitive to light and is a subject of acidic hydrolysis, it is a challenge to the technologists of parenteral dosage forms. Dexamethasone (Dex) has a very small solubility in water (0.1 mg/ml), which caused troubles by preparing liquid medicine forms. The inclusion of hydroxy acids in CD-complexes in the necessary molar proportions leads to considerable increase in the solubility of a medicine and to several times decrease of the amount of CD used. Inclusion complexation was confirmed by the results from the studies of Differential Scanning Calorimetry. The present investigation demonstrated that Digoxin/CD complex shows stability in water medium and the optimum molar ratio Digoxin/HP beta CD is 1:6. The same results can be achieved through HP beta CD, by including Dex in a multicomponent composition containing HP beta CD and citric acid in a molar ratio of 1:4:1.

A new synthesis of chromonyl based on the reaction of formylfurochromone (4,9-dimethoxy-5-oxo-5H-furo[3,2-g][1] benzopyran-6-carbaldebyde) 1 with semicarbazide hydrochloride and thiosemicarbazide afforded 4,9-dimethoxy-5-oxo-5H-furo[3,2-gl]][1] benzopyran-6-yl-(1-aminovinyl) hydrazone derivatives 2a,b. Also 4,5-Diphenyl-2-(4,9-dimethoxy-5-oxo-5H-furo[3,2-g][1] benzopyran-6-yl)-imidazole 3 was obtained by refluxing compound 1 with 1,2-diketone in presence of ammonium acetate. Reaction of compound 1 with different amines afforded 3-(4,9-dimethoxy-5-axo-5H-furo[3,2-g][1] benzopyran-6-yl)-aryliminoethyl derivatives 4a-g. Condensation reaction of compounds 4a-d to C-Hacid compounds were given 4-aminosubstituted-5-(6-hydroxy-4,7-dimethoxy-5-axo-5H- benzofuranyl)-pyrano[2,3-b] cyclobexa-2,3-diene 5a-d and 2-methyl-3-methoxy-4-(4-methoxypheny-lamine)-5-(6-hydroxy-4,7- dimethoxy-5-oxo-5H-benzofuranyl) 6. Refluxing compound 4d with thiosemicarbazide formed 6-methanimine-(4,9-dimethoxy-5-axo-5H-furo[3,2-g][1] benzopyran-6-yl)-(1E)-1-phenylethan-1-one thiosemicarbazide 7. Also, the reaction of compound 4d with p-aminoacetophenone gave the aryliminoethyl compound 8. The reaction of compound 4d with different aldehydes were given 3-(4,9-dimethoxy-5-oxo-5H-furo[3,2-g][1] benzopyran)-iminomethyl-(1-aryl-1-oxo-3-proponyl substituted) 9a-d. Condensation of formyl fuorochromone 1 with phenolic compounds yielded 3-(4,9-dimethoxy-5-axo-5H-furo[3,2-g][1] benzopyran-6-yl)-derivatives 10a-d. All the tested compounds a significant increase in PT & APTT when compared with that of the control group. Only the compound IIa treated rats induced significant increase Ast, alkaline phosphatase and urea during experimental period, while other tested compounds did not cause any significant changes in liver and kidney function. Concomitantly, all the tested compound caused a significant decrease in serum cholesterol and triglyceride levels.

Hydrophilic matrices of gum karaya (GK) and guar gum (GG) using theophylline (TH) as a model drug were prepared for oral controlled release. In vitro release studies were performed for these matrix systems to find out the suitable drug-carrier ratio, which extend the drug release up to 24 h. Promising matrix systems were subjected for in vitro degradation studies in the presence of rat caecal contents. These matrices were also evaluated for their in vivo performance in healthy human volunteers. Matrix systems containing 40% w/w of polysaccharide (GK or GG) have shown uniform and similar in vitro drug release profile for 24 h in the Sorenson's phosphate buffer (pH 7.4). However, TH release from GG-TH matrix system in the presence of rat caecal contents was significantly higher than that from GK-TH matrix system. This is because of the susceptibility of GG for degradation by microorganisms present in the rat caecal content. Though there was no significant difference between the peak plasma concentration (Cmax) and time of its occurrence (Tmax) for TH from GG-TH and GK-TH matrix systems, it was found that oral bioavailability of TH from former matrix was significantly higher than that of later. Therefore, the present study disclosed that the usage of colon degradable polymer offers an advantage in the design of controlled release dosage forms of drugs, which has good absorption properties throughout the gastrointestinal tract.

The meningitis and the meningoencefalitis is 29% from all of the organic diseases of the Central Nerve System. The actuality of this problem is determined by the following factors: 1. Social-only the childish group and the active group of workers among the adults are concerned; 2. The diseases are taking their course seriously with a high percentage of lethality-30%; 3. When there is untimely and inadequate therapy, there occurred additional manifestations of the disease.

A series of new 4-[2'-(6'-nitro)benzimidazolyl]benzoyl amino acids and peptides have been synthesized by coupling the 4-[2'-(6'-nitro)benzimidazolyl]benzoic acid with amino acid methyl esters/dipeptides using DCC as the coupling agent. All the synthesized compounds were found to exhibit potent anthelmintic activity along with moderate antimicrobial activity.

A new series of 5-(5-nitro-2-thienyl)-2-(piperazinyl, piperidinyl and morpholinyl)-1,3,4-thiadiazole derivatives(5a-g) have been synthesized and evaluated against Mycobacterium tuberculosis H37Rv as apart of TAACF TB screening program under direction of the US National Institute of Health, NIAID division. Primary screening was conducted at the single concentration, 6.25 mg/ml against Mycobacterium tuberculosis H37Rv (ATCC 27294) in BACTEC 12B medium using a broth microdilution assay, the Microplate Alamar Blue Assay (MABA). The minimum inhibitory concentration (MIC) determined for compounds demonstrating 90% growth inhibition in the primary screening. The tested compounds showed a varying degree of inhibitory activity (Inhibition = 0-100%). The most active compounds were 4-methyl and 4-benzoylpiperaxinyl analogues(5b and 5g) with the same MIC value of 3.13 micrograms/ml.

The optimization of RP-HPLC method defined the simultaneous influence of some important conditions, such as the mobile phase composition, pH of the mobile phase and temperature, on the separation and determination. The RP-HPLC method was done for the determination of paracetamol, caffeine and propyphenazone in a multicomponent pharmaceutical dosage form. The separation factor values define the optimal conditions, which were confirmed by analysing the appropriate mathematical models. The chromatographic system Hewlett Packard 1100 consisted of a HP 1100 pump, HP 1100 UV-VIS detector and HP integrator. Separations were performed on a Beckman Ultrasphere ODS 4.6 x 150 mm, 5 microns particle size column. Samples were introduced through a Rheodyne injector valve with a 20 microL sample loop. UV detection was performed at 265 nm and phenobarottons was used as an internal standard. The optimization was performed within the pH range from 2.5 to 6.0; temperature range from 20 degrees C to 55 degrees C and composition of the mobile phase methanol-water from (30:70 V/V) to (65:35 V/V). The three-D graphs, constructed with sixty-four experimental points, confirmed the optimal conditions for the determination of the investigated analgetic drugs.

The interaction of glimepiride with b-cyclodextrin (b-CD) has been studied by several analytical techniques, including 1H NMR, infrared spectroscopy (FTIR), powder x-ray diffractometry (XRD), thermal analysis (DSC) and scanning electron microscopy (SEM). The existence of an inclusion complex was proved in solution by phase solubility techniques and 1H NMR, and in the solid state by DSC, FTIR and XRD, being isolated by sealed heating and freeze drying procedures.