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Boll Chim Farm [journal]
- [Cystic fibrosis]. [Journal Article]
- Boll Chim Farm 2005; 144(5):7-8.
- [Biotech]. [Journal Article]
- Boll Chim Farm 2005; 144(5):5-6.
- Oral delivery system of insulin microspheres: effect on relative hypoglycemia of diabetic albino rats. [Journal Article, Research Support, Non-U.S. Gov't]
- Boll Chim Farm 2004 Oct; 143(8):315-8.
The aim of the present work was to investigate the effectiveness of a dosage form approach for monitoring both the inactivation and the absorption process by targeting insulin delivery to the upper region of small intestine. The dosage form is based on the incorporation of insulin with protease inhibitor and absorption enhancer into polyacrylic polymer Eudragit L-100. Insulin microspheres were prepared by solvent evaporation technique. And also study the effect of these microspheres upon the relative hypoglycemia (RH) effect in white diabetic albino rats has been studied in comparison to that produced after subcutaneous injection of bovine insulin solution. The oral administration of formulation with aprotinin and bile salts gave significant (p< 0.01) hypoglycemia when compared with formulation with insulin alone and with insulin and bile salts. However, the duration, course and the intensity of effect were different for each formulation. It was interesting to observe that the co-administration of aprotinin and bile salts produce prolonged and significant reduction of blood glucose level. A reduction of 4.47-36.81% in plasma glucose levels and RH of about 11.7% relative to subcutaneous injection of soluble insulin solution can be achieved by encapsulation along with protease inhibitor and bile salts.
- Effect of 5-substituted benzylideneaminosalicylic acid on carrageenan-induced ulcerative colitis. [Journal Article]
- Boll Chim Farm 2004 Oct; 143(8):309-13.
Mesalazine, a drug of choice in the management of ulcerative colitis, was chemically modified as 5-(E)-substituted benzylideneaminosalicylic acid by condensing 5-aminosalicylic acid with selected aryl aldehydes with an intention to improve its pharmacological profile. The tests were performed to study their anti-inflammatory effect on carrageenan-induced ulcerative colitis in albino rats. The histopathological findings, serum transaminase level and lipid peroxide content in the intestine and liver were taken as indices of pharmacological activity. The azomethine derivative formed from salicylaldehyde (5-ASASB3) was found to have maximum activity and it reversed the disease symptoms in experimental animals The azomethine derivative markedly reduces the ulcerative colitis when compared with parent molecule, mesalazine.
- Synthesis and biological evaluation of novel naphthoquinone derivatives as potential anticancer and antimicrobial agents. [Journal Article]
- Boll Chim Farm 2004 Oct; 143(8):299-307.
Four novel series of 1,4-naphthoquinone derivatives namely 2,3-disubstiuted 4-[(benzothiazol-2-yl)hydrazono]-1,4-dihydronaphthalen-1-one 4a-c, N1-(2,3-disubstituted-4-oxo-1,4-dihydronaphthalen-1-ylidene)-N2-(benzotriazol-1-yl)acetic acid hydrazide 5a-c, 2,3-disubstituted 4-[(5-aryl-2,3-dihyrothiazol-2-ylidene)hydrazono]-1,4-dihydronaphthalen-1-one 7a-c, and 3-methyl-2-substituted carbamoyl or thiocarbamoyl-hydrazinocarbonylmethylthio-1,4-dihydronaphthalene-1,4-dione 9a-c were synthesized. Three of the new compounds were chosen by NCI to be evaluated as anticancer agents and they showed promising activity. All the prepared compounds were tested as antimicrobial agents.
- Behavior of cinnamoyl-isothiocyanate towards carbon, nitrogen and oxygen reagents. [Journal Article]
- Boll Chim Farm 2004 Oct; 143(8):291-7.
Cyclization of cinnamoyl isothiocyanate with nucleophilic reagents either spontaneously or with added a reagents is reported.
- Studies on the development of taste-masked suspension of chloroquine. [Journal Article, Research Support, Non-U.S. Gov't]
- Boll Chim Farm 2004 Dec; 143(10):377-82.
A non-bitter chloroquine suspension formulation for pediatric use was prepared in the form of an ion-pair of chloroquine with pamoic acid. Various parameters involved in the formulation of a stable and palatable suspension have been optimized. The suspension was characterized for particle size analysis, viscosity, physical and chemical stability and taste. Release of chloroquine from the ion-pair conducted as dissolution rate studies in simulated gastric media showed near to 100% release instantaneously. In-vivo bioavailability study conducted in albino rats indicated comparable bioavailability of chloroquine from the suspension with that of chloroquine phosphate syrup taken as standard. Stability study conducted over a period of 3 months showed the intactness of the ion-pair and the tasteless behavior of the suspension throughout the period of storage.
- Novel nicotinate esters of vasodilatation activity. [In Vitro, Journal Article]
- Boll Chim Farm 2004 Dec; 143(10):365-75.
A variety of 2-substituted-4, 6-diaryl-3-pyridinecarboxylates 4 were obtained through aromatic nucleophilic substitution. reaction of secondary amines with 2-bromo-3-pyridinecarboxylate derivatives 3. The latters were obtained through bromination of 3-aryl-4-benzoyl-2-cyanobutyrates 2 in glacial acetic acid. However; reaction of primary aromatic amines with 2-bromopyridines 3 afforded 2-arylamino-3-pyridinecarboxylates 5 beside the unexpected 2-amino analogues 6. On the other hand, 3-hydroxy-1H-pyrazolo[3,4-b]pyridines 7 were isolated via reaction of 3 with hydrazine hydrate. Good to complete muscle relaxation of rabbit's jejunium, rat's uterus and rabbits aorta was observed during screening representative examples (3a, 4c, Sd, 5f and 6b) of the newly synthesized 3-pyridinecarboxylates indicating the vasodilatation and antihypertension activity for the tested compounds.
- Evaluation of crosslinked chitosan hydrogel beads as a carrier for prolonged delivery of diclofenac sodium: in vitro and in vivo studies. [Journal Article, Research Support, Non-U.S. Gov't]
- Boll Chim Farm 2004 Dec; 143(10):359-64.
Chitosan hydrogel beads containing diclofanac sodium were prepared using ionotropic gelation technique in which tripolyphosphate solution was used as a counterion. Chitosan molecular weight, tripolyphosphate concentration and crosslinking time were found to have an effect on the percentage of the drug loading. The loading efficiency of diclofenac sodium was very high (more than 90%). A longer-period of contact with the counterion ions decreased the efficiency of drug loading. The beads produced all had good spherical geometry. The beads showed a narrow size distribution in which 95% of the beads prepared were in the range of 2-3 mm. Comparison of release rate-time plots of dissolution data of marketed product with the newly developed dosage form indicated the ability of the later to sustain more diclofenac sodium release. The beads were evaluated for their bioavailability in six beagle dogs relative to the commercial enteric-coated Voltaren tablets. The in vivo availability study, reveled that the prepared beads filled in hard gelatin capsules had a 126.22% bioavailability relative to that of the commercial Voltaren tablets. The beads showed comparable pharmacokinetic parameters to that of the commercial tablets. The results suggested the possibility of producing a promising sustained drug delivery system for diclofenac sodium.
- Immobilization and release of etophylin from hydrogels, based on polyacrylic acid and macrodiisocyanates. [Journal Article]
- Boll Chim Farm 2004 Dec; 143(10):353-7.
Hydrogels, based on polyacrylic acid and various macrodiisocyanates that contain polyethylene glycol, polypropylene glycol or polytetramethylene glycol in the main chain are synthesized. The obtained hydrogels are studied as possible polymer carriers of drug substances. Etophylin was applied as a model drug. It is exposed that the etophylin release rate from the hydrogel depends on the way of drug comprise in the polymer net, from its density from the chemical nature of the crosslinking agent and from the pH of the environment. The carried out studies let us to conclude that the obtained hydrogels are possible materials as drug carriers.