Bollettino chimico farmaceutico最新文献_第6页

Bleaching of browned water yam (Dioscorea alata) with African oil bean seed lipoxygenase (Part 2). 非洲油豆种子脂氧合酶漂白褐水山药(第二部分)。

Bollettino chimico farmaceutico Pub Date : 2004-01-01

M N Anokwulu

引用次数: 0

Physicochemical compatibility between ketoprofen lysine salt injections (OKi Fiale, PG060) and pharmaceutical products frequently used for combined therapy. 酮洛芬赖氨酸盐注射剂(OKi Fiale, PG060)与经常用于联合治疗的药品之间的理化相容性。

Bollettino chimico farmaceutico Pub Date : 2004-01-01

G Carlucci, M M Gentile, S Bartolini, R Anacardio

{"title":"Physicochemical compatibility between ketoprofen lysine salt injections (OKi Fiale, PG060) and pharmaceutical products frequently used for combined therapy.","authors":"G Carlucci, M M Gentile, S Bartolini, R Anacardio","doi":"","DOIUrl":"","url":null,"abstract":"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).","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 1","pages":"15-9"},"PeriodicalIF":0.0,"publicationDate":"2004-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24469034","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Study of insolubility problems of dexamethasone and digoxin: cyclodextrin complexation. 地塞米松与地高辛不溶性问题的研究:环糊精络合。

Bollettino chimico farmaceutico Pub Date : 2004-01-01

V Dilova, V Zlatarova, N Spirova, K Filcheva, A Pavlova, P Grigorova

{"title":"Study of insolubility problems of dexamethasone and digoxin: cyclodextrin complexation.","authors":"V Dilova, V Zlatarova, N Spirova, K Filcheva, A Pavlova, P Grigorova","doi":"","DOIUrl":"","url":null,"abstract":"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.","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 1","pages":"20-3"},"PeriodicalIF":0.0,"publicationDate":"2004-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24469036","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synthesis and pharmaceutical activity of new series of chromonyl derivatives. 新系列铬基衍生物的合成及药物活性研究。

Bollettino chimico farmaceutico Pub Date : 2004-01-01

N M Fawzy, S A Swelam, S A Batran

{"title":"Synthesis and pharmaceutical activity of new series of chromonyl derivatives.","authors":"N M Fawzy, S A Swelam, S A Batran","doi":"","DOIUrl":"","url":null,"abstract":"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.","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"143 1","pages":"24-33"},"PeriodicalIF":0.0,"publicationDate":"2004-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24469595","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Influence of colon degradation of polysaccharide on the oral bioavailability of theophylline from controlled release hydrophilic matrices. 多糖结肠降解对控释亲水性基质中茶碱口服生物利用度的影响。

Bollettino chimico farmaceutico Pub Date : 2003-12-01

G V Babu, K Himasankar, N Ravi Kumar, K V Murty

{"title":"Influence of colon degradation of polysaccharide on the oral bioavailability of theophylline from controlled release hydrophilic matrices.","authors":"G V Babu, K Himasankar, N Ravi Kumar, K V Murty","doi":"","DOIUrl":"","url":null,"abstract":"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.","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 10","pages":"454-60"},"PeriodicalIF":0.0,"publicationDate":"2003-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24400761","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Treatment of patients with bacterial infections of the central nervous system--a pharmaco-economical analysis. 中枢神经系统细菌性感染的治疗——药物经济学分析。

Bollettino chimico farmaceutico Pub Date : 2003-12-01

D Dimitrov

引用次数: 0

Synthesis and biological activity of a novel series of 4-[2'-(6'-nitro)benzimidazolyl]benzoyl amino acids and peptides. 新系列4-[2'-(6'-硝基)苯并咪唑]苯甲酰氨基酸和肽的合成及其生物活性。

Bollettino chimico farmaceutico Pub Date : 2003-12-01

M Himaja, Rajiv, M V Ramana, Boja Poojary, D Satyanarayana, E V Subrahmanyam, K Ishwar Bhat

引用次数: 0

Synthesis and evaluation of in vitro antimycobacterial activity of some 5-(5-nitro-2-thienyl)-2-(piperazinyl, piperidinyl and morpholinyl)-1,3,4-thiadiazole derivatives. 一些5-(5-硝基-2-噻吩基)-2-(哌嗪基、哌啶基和morpholin基)-1,3,4-噻二唑衍生物的合成及体外抑菌活性评价。

Bollettino chimico farmaceutico Pub Date : 2003-11-01

A Foroumadi, F Soltani, M Asgharian Rezaee, M H Moshafi

引用次数: 0

Optimization of the RP-HPLC method for multicomponent analgetic drug determination. 反相高效液相色谱法测定多组分镇痛药的优化。

Bollettino chimico farmaceutico Pub Date : 2003-11-01

D Ivanovic, M Medenica, A Malenovic, B Jancic, Dj Misljenovic

{"title":"Optimization of the RP-HPLC method for multicomponent analgetic drug determination.","authors":"D Ivanovic, M Medenica, A Malenovic, B Jancic, Dj Misljenovic","doi":"","DOIUrl":"","url":null,"abstract":"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.","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 9","pages":"386-9"},"PeriodicalIF":0.0,"publicationDate":"2003-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24400185","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Study of glimepiride-b-cyclodextrin complex. 格列美脲-b-环糊精配合物的研究。

Bollettino chimico farmaceutico Pub Date : 2003-11-01

J R Moyano, T Ventriglia, J M Ginés, F Muñoz, A M Rabasco

引用次数: 0