Sci. Pharm., Volume 70, Issue 2 (June 2002) – 9 articles , Pages 113-229

A survey of morphological and phytochemical data characteristic for several taxa of the Achillea millefoliurn group (A. aspleniifolia VENT., A. roseoalba EHREND., A. collina J. BECKER ex REICHENB., A. ceretanica SENNEN, A. setacea W. ET K., A. pratensis SAUKEL & LANGER, A. styriaca SAUKEL ined., A. pannonica SC H E ELE, A. distans W. ET K., A. millefolium s. I., A. millefolium ssp. sudetica OPIZ) and A. crithmifolia W. ET K. is presented. For each taxon a short morphological description and a guide for microscopic analysis is given as well as its sesquiterpene composition including the TLC characteristics. Based on GLC analyses of 1523 single plants collected in Central Europe the sums of sabinene + β-pinene + β-caryophyllene (SUM I), a-pinene + 1,8-cineole (SUM 2), camphene + camphor + borneol (SUM 3), camphene + camphor (SUM 4) and 1,8-cineole + borneol (SUM 5) were found to be highly significant for distinct taxa or groups of taxa. Full article

Matrix tablets of ketorolac trometharnine (KT) were prepared by direct compression technique and Carbopol 934, 940 and 1342 have been used as polymers in different concentrations (5-15 % ). For the quality control of tablets; physical tests as crushing strength, diameter-height ratio and fkiability, KT amount assay and in vitro dissolution techniques were performed and dissolution profiles were plotted and evaluated kinetically. The in vitro release kinetics of ten different formulations of KT matrix tablet were studied at pH 1.2 and pH 7.0 using the USP dissolution technique and apparatus with basket assembly. Dissolution results were evaluated kinetically and statistically. According to our results, different types and concentrations of carbopol to tablet formulations may effect in controlled drug release. Full article

Danazol, a weekly androgenic, heterocyclic compound with anabolic properties, is used primarily in the treatment of endometriosis and other gynecological complaints. Effects of co-administration of enalapril, an angiotensin converting enzyme inhibitor (ACE inhibitor) with danazol on some biochemical parameters in rats were studied. Treatment of rats with danazol (200mglkg i.p) for 15 days induced a significant elevation of serum aspartate transaminase activity (AST, EC: 2.6.1.1), triglycerides (TG) and induced a significant decrease in serum cholesterol. However, enalapril treatment (20mglkg i.p) for 15 days caused a significant elevation of serum alanine transaminase activity (ALT, EC: 2.6.1.2). Co-administration of danazol and enalapril significantly lowered the elevated levels of serum transaminases enzyme activities and serum TG. It could be concluded that long term treatment with enalapril might be beneficial in patients danazol in clinical situations through protection against undesirable side effects. Full article

Tris(dimethy1amino)phosphine 1 reacted with phenylarylidene barbituric acids 4 to yield the triaminophosphonium dipolar ion adduct 7. 2-Arylidene-1,3- cyclohexanedione 5 and 2-Arylidene-5,5-dimethylcyclohaxane1-,3 -diones 6 reacted with phosphine 1 to produce the dioxyxanthenes 10 and 12, respectively. Structural assignments are based on analytical, chemical, and spectroscopic evidences. A mechanism is proposed to explain the formation of these compounds. The biological acitivity of the new synthesized compounds against Aphis Craccivora, a serious pest infecting many crops in Egypt, was studied. Full article

We have evaluated vigabatrin (γ-vinyl γ-aminobutyric acid), an irreversible inhibitor of γ-aminobutyric acid (GABA)-transaminase responsible for GABA degradation, for its effects on food consumption, body weight changes, fluid intake, changes in hematological and biochemical parameters in plasma liver and kidney of Swiss albino mice. Mice received vigabatrin 0.26% wlv chronically in drinking water for 7, 14 and 21 days. Changes in all the parameters were recorded aRer 7, 14 and 21 days respectively in different groups. Food consumption was comparable to the control group with minor fluctuations. The body weight declined significantly but only after 3-week treatment with no appreciable change in organ indices or relative organ indices. There were essentially no adverse effects on hematological parameters (RBC, WBC, HGB, neutrophils, eosinophils, monocytes, lymphocytes and basophils) with this treatment. However, there was a decrease in monocyte counts during the first week and an increase in the neutrophil counts during the third week of vigabatrin treatment. In one part plasma biochemical parameters like AST, ALT, CK-MB, creatinine, glucose and urea were also assessed with the same dose regimen. It was observed that only CK-MB and GPT activity levels were altered slightly significantly and are thought to be a result of cross enzyme inhibitions. In this experiment it was observed that lipid peroxide levels measured, as malondialdehyde did not change appreciably in both liver and kidney tissues. However, the levels of glutathione (non-protein sulfhydryl; GSH) declined significantly in comparison to control in liver and kidney. A comparison of level of GSH in liver and kidney shows that this depletion was at early time points in the former. The depletion of GSH suggests the possible involvement of GSH in detoxification process and corroborates its role in protection. Full article

A certain type of titration methods have appeared with an increasing frequency during the last years, this being evident surveying the latest editions of the European Pharmacopeia (1997-2001) [1-3], where there are now more than fifty monographs on the assay of halide salt of organic bases by potentiometric titration of the sample dissolved in ethanol or in an ethanolwater mixture with sodium hydroxide after addition of a defined volume of diluted hydrochloric acid [...] Full article

The synthesis of a novel quinazolinone was accomplished by the reaction of quinazolin- 2,4-(1H,3H)-dione with trifluoromethanesulfonic anhydride in triethylamine. The antimicrobial activity was determined against eight microorganisms. The organisms were all susceptible to 3-(4-methoxyquinazolin-2-yl)-quinazolin-2,4-(1H,3H)-dione 3 at the concentrations used. The gram positive organisms showed more susceptibility than the gram negative ones. Full article

The title compound 2 - prepared by Komblum reaction - reacted with Hg(II)-edta in a two electron withdrawal to a bicyclic compound 6, which showed in solution an equilibrium of two species probably of diastereomers, which was deduced from NMR-measurements. Additionally, resulting of an threefold dehydrogenation two diastereomeric bicyclic lactams 11A and 11B were isolated. Full article