Iranian Journal of Pharmaceutical Sciences
Volume:3 Issue: 4, Autumn 2007

The aim of this study was to investigate the prevalence of Mg deficiency and effect of aminophylline infusion on urine magnesium concentration after magnesium loading test (MLT). To determine serum Mg, venous blood specimens were obtained just before the first MLT. Two MLTs were performed. The first one was done before starting aminophylline infusion and the 2nd one was done during aminophylline infusion. Urine samples were collected from the starting of Mg infusion in each phase. Although low serum Mg was present only in 2 patients, MLT showed Mg deficiency in 18 patients. MLT detected Mg deficiency in 13 out of 14 patients with normal serum Mg, in 2 out of 2 subjects with serum hypomagnesemia, and in 3 out of 5 cases with serum hypomagnesemia. There was no relationship between Mg retention, age and serum Mg concentrations. Aminophylline administration increased the 24-h urine Mg concentration by 29.3%.

Purpose of this study was to investigate the effect of the presence of the water soluble polymers viz HPMC, PVP and PEG 6000 on aqueous solubility and complexation abilities of felodipine with or without presence of β-cyclodextrin (βCD) and HPβCD by phase solubility studies. The data revealed the initial increase in drug solubility followed by plateau in the presence of relatively low polymer concentration i.e. 0.25-0.5 %w/v. Phase solubility diagrams of felodipine in ternary system showed similar behaviour to binary system without βCD. Addition of water soluble polymer to βCD solution improved βCD solubilizing efficiency due to increase in βCD complexing power toward felodipine. In binary system solubility was found 2.5 to about 10 times higher than in water which was further improved in the   presence of 0.25% w/v water soluble polymer. Ternary systems with βCD showed highest increments in solubility towards felodipine, with 78.8%, 81.8% and 74% improvement after the addition of 0.25% w/v HPMC, PVP and PEG6000, respectively. Our study confirmed that addition of small amounts of hydrophilic polymer is useful strategy for improving the solublization and complexing abilities of cyclodextrins thus allowing less cyclodextrin to be needed to solubilize given amount of drug. This offers economic advantage. All the polymers under study showed synergistic effect on felodipine cyclodextrin solublization by increasing complexation efficiency.The highest solubility improvement up to 81.8% was obtained for βCD ternary system when 0.25% w/v of PVP was used.

The complex formed as a consequence of the interaction between the electron-acceptor P-chloranilic acid and an electron donor tamoxifen citrate was employed in the assay of the drug in pure powder and tablets. Chloranilic acid was found to form a charge-transfer complex in a 1:1 stoichiometric ratio, with tamoxifen citrate. The wavelength of maximum absorption for the complex was found to be 550 nm while the absorbance was linear over the concentration range of 2-100 g/ml. Evaluations of the various thermodynamic parameters by means of the Scott equation was carried out and were found to decrease with increase in temperature. The free energy change ( G°) and the enthalpy of formation ( H°) as well as the entropy ( S°) were determined for various interactions. Results obtained suggest that the proposed method may be conveniently applied in the analysis of commercially available tamoxifen citrate tablets with a high degree of accuracy and reproducibility.

The cellular therapy and nerve tissue engineering will probably become a major therapeutic strategy for promoting axonal growth through injured area in central nervous system and peripheral nervous system in the coming years. The stem cell carrier scaffolds in nerve tissue engineering resulted in strong survival of cells and suitable differentiation into neural cells, so this pathway should be created a favorable environment for axon regeneration. Poly lactic-co-glycolic acid (PLGA) has been widely used for manufacturing three dimentional scaffolds for tissue engineering. The pluripotent nature and proliferative capacity of embryonic carcinoma cells such as P19 also makes them an attractive cell source for tissue engineering. This study was initiated to evaluate potential of biodegradable PLGA microspheres for P19-derived neurons for neural tissue engineering and axon regeneration. The PLGA microspheres were prepared by using solvent evaporation, water in oil in water, technique. The water phase was polyvinyl alcohol (PVA) solution and the oil phase was PLGA solution. Retinoic acid (RA) was added to bacterial dishes as a differentiation factor inducer. P19 cells were attached to the PLGA microspheres and differentiated into neural cells on them. PLGA microspheres were characterised for size and surface morphology by scanning electron microscopy. The in vitro experimental studies were performed via immunoflouresent staining, scanning electron microscopy (SEM), RT-PCR, and histology. The photomicrograph and histology staining show the surrounded microspheres by P19 cells. The SEM results demonstrated the attachment and axon formation. Immunoflouresent staining and RT-PCR analysis for MapII, β-Tubulin, Nestin and Pax6 indicated the differ-entiation of P19 cells into neural cells. This report shows that high surface area also allows rapid cell expansion and increases cell attachment on PLGA microspheres, so each microsphere contains high cell density that resulted in survival of transplan-tation into the straitum of host animals, therefore, PLGA microspheres can help the differentiation of P19 cells into neural cells.

This study was designed to explore the protective effects of ascorbic acid and water extract of Spirulina platensis (blue green algae) on methotrexate-induced lipid peroxidation using goat liver as the lipid source. This in vitro evaluation was done by measuring the malondialdehyde, 4-hydroxy-2-nonenal, reduced glutathione and nitric oxide content of tissue homogenates. The study reveals the lipid peroxidation induction capacity of methotrexate, the anti-peroxidative potential of ascorbic acid and aqueous extract of S. platensis on methotrexate-induced lipid peroxidation.

The anti-apoptotic gene bcl-2 is located in mitochondria, but it is uncertain whether its expression affects hepatocyte survival in ischemia/reperfusion (I/R) injury. This experiment was designed to evaluate the role of folic acid in expression of bcl-2 in I/R in rat liver. Eighteen Wister rats were divided into sham-operated controlgroup (C) (n=6), I/R group (n=6), folic acid treated group which received 1 mg/kg/day folic acid by oral route for 7 days before induction of I/R (n=6). Bcl-2 expression was measured by RT-PCR and western blot methods. Folic acid significantly increased Bcl-2 mRNA expression in comparison to the I/R group. Quantification of apoptotic and necrotic hepatocytes, measured by fluorescence microscopy and terminal deoxynucleotidyl transferase (TdT)-mediated dUDP-biotin nick end labeling (TUNEL) method, showed a significant decrease in apoptosis and necrosis of hepatocytes in folic acid-treated group. Histopathologi-cal examination of the liver revealed that folic acid protected from severe hepatic degeneration from I/R injury. The biochemical parameters like alanine transaminases and aspartate transaminases were significantly decreased in folic acid-treated group compared to I/R group. In conclusion, folic acid afforded significant protection against I/R injury due to its ability to inhibit I/R-induced apoptosis.

In view of potential biological activities of small molecule polyamides, we synthesized some novel N-(2-aminoethyl)-1-benzyl-2- (alkylthio)-1H-imidazole-5-carboxamide (7a,b), and N-(2-(1-benzyl-2-(alkylthio) -1H-imidazole- 5-carboxamido) ethyl)-1-benzyl-2- (alkylthio)-1H-imidazole-5-carboxamides (8a,b) as antitumor agents. The antitumor activity of compounds 7a,b and 8a,b was studied at concentrations of 0.01, 0.1 and 1 mg/ml, using the potato disk bioassay technique. Vincristine at 0.25 mg/ml employed as positive control and had -67.24% tumor inhibition. Maximum % inhibition for potato tumors was found to be -75.52 for 7b at 1 mg/ml.

Keeping in view the promising potential of carbonic anhydrase inhibitor based antimicrobials and enhancement of carbonic anhydrase inhibitory activity by metal complexes of sulfonamides, with an aim to develop better antimicrobial agents we have attempted investigation of antimicrobial activity of metal complexes of 4-(2'-hydroxy phenyl imino) phenyl sulphonamide. Sulfanilamide was taken as the starting material to synthesize 4-(2'-hydroxy phenyl imino) phenyl sulphonamide. Cu (II), Zn (II), Co (II), Ni (II) and Pb (II) complexes were synthesized following reported methods. The in vitro screening was carried out using two gram positive bacteria (S. aureus, E. faecalis) and two gram-negative bacteria (E. coli, P. aeruginosa) by disc diffusion method. Metal complexes were found to enhance theantimicrobial potental of the ligand.

A series of novel indeno[1, 2-b]quinoxalin-11-ylidenamines 2-9 have been synthesized via condensation of indane[1, 2-b]quinoxalin-11-one (1) with various primary aromatic amines in presence of AcOH for 3 h. Compound 1 was synthesized by condensation of indane-1,2,3-trione with benzene-1,2-diamine in presence of AcOH. The synthesized compounds were characterized by IR, 1H-NMR, mass spectra and elemental analysis. Compounds 2-9 were screened for anti-nociceptive, anti-inflammatory and antiepileptic activity by AcOH induced writhing method, carrageenan induced paw edema method and maximal electroshock induced convulsion method respectively. Out of the eight synthesized compounds, indeno[1, 2-b]quinoxalin-11-ylidine (4-nitrophenyl)amine (3) exhibited promising anti-inflammatory activity and anti-nociceptive activity. N-(2,4-dinitrophenyl)-N' -(indeno[1,2-b]quinoxalin-11-ylidene)hydrazine (7) showed promising anti-inflammatory activity, anti-nociceptive activity, and antiepileptic activity, whereas N4-indeno[1, 2-b]quinoxalin-11-ylidene biphenyl-4,4'-diamine (8) showed promising anti-inflammatory activity.