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1995| July-August | Volume 57 | Issue 4
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Influence of viscosity on nitrofurantoin absorption from w/o/w emulsions.
CO Onyeji, SA Adesegun
July-August 1995, 57(4):166-169
The bioavailability of nitrifurntoin was evaluated in eight healthy volunteers, in a crossover fashion, after administration of 100-mg dose of the drug in water-in-oil-in-water (W/O/W) emulsions with and without viscosity imparting agents. The bioavailabilitiy of the drug was assessed from urinary excretion data of the unchanged drug. The extent of absorption,maximum excretion rate and period of minimum effective urine concentration were all significantly higher (p < 0.05) in the w/o/w emulsion with viscosity imparting agents compared with the corresponding values for the reference w/o/w emulsion (containing no viscosity agent). From these results, it is suggested that the bioavailability and therapeutic efficacy of nitrofurantoin administered in w/o/w formulations could be further enhanced by increasing the viscosity of the formulation. Also the nature of the viscosity imparting agent plays a significant role in determining the extent of improvement of nitrofurantoin absorption.
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Formulation and evaluation of ophthalmic drops containing sulphacetamide sodium and trimethoprim.
AA Shirwaikar, PG Rao
July-August 1995, 57(4):143-147
Eye drops containing sulphacetamide sodium and trimethoprim were formulated and tested for their antibacterial activity and stability. The microorganisms were found to be more susceptible to this formulation containing only sulphacetamide sodium. The accelerated stability studies showed a shelf life of 4 1/2 years.
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Visible spectrophotometric methods for the determination of diltiazen hydrochloride.
C SP Sastry, K Sreedhar, MN Reddy, DG Sankar
July-August 1995, 57(4):170-172
Two simple spectrophotometric methods are described for the determination of Diltiazen Hydrochloride (DZH) based on oxidising it with a known excess of ferric chloride [Fe(III)]or N-Bromosuccinimide (NBS) and estimating the reduced, Fe (II) or unreacted NBS with 1, 10-phenanthroline (PTL) or metolsulfanilamide (SA) in methods A or B respectively.
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Spectrophotometric determination of febendazole.
SP Chudasama
July-August 1995, 57(4):173-175
A simple spectrophotometric method for the determination of febendazole by hydroxamic acid formation in dosage forms is described. Febendazole reacts with hydroxylamine hydrochloride in alkaline medium to give hydroxamic acid, which forms a reddish violet coloured complex with Iron (III) in acidic medium having maximum absorbance at 500 nm, molar absorptivity of 5.0 x 10 (3) 1.mol(-1) cm(-1).
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Dehydrozingerone inhibits nitrite-induced oxidation of hemeoglobin.
RS Narla, M NA Rao
July-August 1995, 57(4):181-184
Dehydrozingerone protects hemoglobin from nitrite-induced oxidation to methemoglobin. The protection was observed when added before or during, and not after the autocatalytic stage of the oxidation. The ability of dehydrozingerone to scavenge oxygen free radicals may be responsible for the activity since these radicals are implicated in promoting the auticatalytic stage of the oxidation of hemoglobin by nitrite. The acetyl derivative of dehydrozingerone was also active in inhibiting the oxodation indication that the phenolic group is not essential for the activity.
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Dissolution enhancement of ibuprofen-hydrolyzed gelatin kneaded mixtures.
MC Gohel, MM Patel, AF Amin, SM Trivedi
July-August 1995, 57(4):176-180
The objective of this investigation was to evaluate the joint effects of variables such as kneading time, amount of hydrolyzed gelatin and drying temprature on the dissolution effciency (PDE) was chosen as the response in the 2(3) full factorial design. The PDE was significantly affected by the selected variables. A polynomial equation, with interaction terms, was generated and step-wise multiple linear regression analysis was carried out to identify the key variables. The higher levels of kneading time, 10 min. and hydrolyzed geletin, 50 mg per 200 mg ibuprofen favoured the dissolution of ibuprofen from the kneaded mixture. A checkpoint was chosen to verify validity of the equation.
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Quantitative structure - activity relationship study of antihistaminic thiazolidin-4-ones.
P Singh, TN Ojha, RC Sharma, S Tiwari
July-August 1995, 57(4):162-165
The quantitative structure-activity relationship (QSAR) studies of some substituted thiazolidin-4-ones have yielded statistically sound correlation between the observed potency of histamine antagonism, pA2, which in turn is nearly linearly correlated with the inhibitory activity,-logIC50 and physicochemical parameters such as the overall field effect,F, and hydrophobic effect at the 4-position,pi4, generated by R-substituents in the phenyl ring. In the light of our present findings a compound with pA2 approaching 2 orders of magnitude greater than that of the most active compound of the parent series is predicted.
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Antifungal potential of some transition metal - chelates of p-amino-salycylic acid (PAS).
PV Khadikar, BD Heda, R Saxena, T Khaddar
July-August 1995, 57(4):157-161
Metal chelates of P-amino-salycylic acid (PAS) with VO(II),Cu(II),Ni(II)Co(II)Fe(II),Mn(II) and Zn(II) have been prepared and characterised by analytical IR-Spectral and thermal studies. They have been screened for antifungal activities against a series of pathogenic and non-pathogenic fungi. The in vitro filter paper disk method was used exclusively for testing activities. The chelates in comparison to PAS were found to posses remarkable antifungal potential.
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Solubility behaviour of 3-phenylsydnone in binary solvents.
CV Subrahmanyam, KK Mohan, K Satyanarayana
July-August 1995, 57(4):151-156
The solubility of a type A meso-ionic compound, 3 - phenylsydnone was determined in dioxane-water and ethylacetate-methanol, methanol-water solvent series. The experimental mole fraction solubility was well below the ideal solubility, indicating strong self-association of solvent or solute or both. However, the solubility parameter values obtained by Fedors and Hoy group contribution methods, peak solubility and regression methods were found to be in good agreement. A value of 11.3 H is assigned to the solubility parameter of 3-phenylsydnone.
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Effect of temperature on the granule formulation of new antimalarial compounds (80/53) n1-3'-acetyl-4',5'-dihydro-2'-furanyl-n4-(6-methoxy, 8-quinolinyl) 1,4-pentane diamine.
AK Dwivedi, D Kulkarni, P Prakash, S Singh
July-August 1995, 57(4):185-186
The chemical stability of antimalarial compound N1-3'-acetyl-4',5'-dihydro-2'-furanyl-N4-(6-methoxy, 8-quinolinyl)-1,4 pentane diamine (80/53) (I) in the granuale formulation at various temperature was investigated. The order of reaction degradation rate constant were computed by least square linear regression.
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Decontamination of veegum by gamma radiation.
S Shidhaye, A Damle
July-August 1995, 57(4):187-188
Veegum was irradiated at graded doses of 5-25 KGy and monitored for changes in physcochemical characteristics. Microbiological and accelerated stability studies were carried out to determine the minimum decontamination dose and post-irradiation stability, respectively. Veegum was successfully decontaminated at 25 KGy and found to be stable upto 25 KGy dose of gamma radiation.
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In vitro evaluation of antihepatotoxic activity of quinazolines.
A Kapil, IB Koul
July-August 1995, 57(4):148-150
Hepatopropective efficacy of synthetic quinazolines was established by evaluating their inhibitory effects on CCI4- induced microsomal lipid peroxidation and scavenging of hydroxyl radical formation. The protective potential of these compounds was compared with that of a standard liver-protective compound silymarin.
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