bluuebunny/crossref_metadata_2025_split huggingface dataset:
The effect of carbenicillin on the haemostatic mechanism
Authors: Lederer D A , Davies T , Connell G , Davies J A , McNicol G P 
Published: April 2011

Abstract
Carbenicillin has no effect on the thrombin time, partial thromboplastin time, prothrombin time, platelet factor 3 availability, fibrinogen and plasminogen levels, Factor XIII, fibrin plate lysis or euglobulin lysis time in vitro in concentrations from 20–1280 μg ml−1. After incubation with plasma, carbenicillin inhibited platelet aggregation to ADP at all the concentrations examined (20–1280 μg ml−1). The same coagulation tests were unaffected 30 min and 4 h after intravenous administration of 5 g of carbenicillin to six normal subjects, though some impairment of platelet response to ADP occurred in three subjects. This impairment of platelet function is considered unlikely to contribute towards a bleeding tendency in normal subjects but might perhaps be a contributory factor in haemostatic failures in patients with uraemia.
The distribution of Δ1-tetrahydrocannabinol and 7-hydroxy-Δ1-tetrahydrocannabinol in the mouse brain after intraventricular injection
Authors: Gill E W , Lawrence D K 
Published: April 2011

Abstract
Δ1-Tetrahydrocannabinol (Δ1-THC) and 7-hydroxy-Δ1-THC were injected into the cerebral ventricles of mice by an improved technique, and the potencies of the drugs were measured by the mouse catalepsy test. Both drugs were found to have the same activity when administered by this route as after intravenous injection. Autoradiographic experiments with tritium-labelled compounds showed that at the time of the peak behavioural effect almost all the injected dose of 3H-Δ1-THC (1.6 mg kg−1) or 3H-7-hydroxy-Δ1-THC (0.6 mg kg−1) remained in the intraventricular space and had not penetrated the brain tissue. Δ1-THC was found to remain in the ventricles after the behavioural effect had disappeared; 3% of the injected dose was still present 2 days after injection of 3H-Δ1-THC (1.6 mg kg−1).
The transfer of salicylic acid across a Cellophane membrane from micellar solutions of polysorbates 20 and 80
Authors: Withington R , Collett J H 
Published: April 2011

Abstract
In the pH range 1 to 5 there is a linear relation between the rate constant for salicylic acid transfer across a cellophane membrane and the fraction of ionized drug present at each pH. The rate constant for ionized molecules is about 60% of that for unionized molecules. The presence of polysorbates 20 and 80 in the drug solution markedly decreases the apparent transfer rate constant of salicylic acid at low pH. When transfer rate constants obtained in the presence of surfactant are calculated in terms of the non-micellar concentration of salicylic acid they compare favourably with those obtained in the absence of surfactant. These results indicate that micellar drug does not participate in the transfer process.
Serum and blood concentration of sodium cephalexin in man given single intramuscular and intravenous injections
Authors: Gower P E , Dash C H , O'Callaghan Cynthia H 
Published: April 2011

Abstract
Healthy volunteers were given a single intramuscular (i.m.) injection of a solution of 1 g, 500 or 250 mg sodium cephalexin or an intravenous (i.v.) injection of 1 g. Following i.m. injection, mean peak serum levels were estimated by computer analysis to be 18.3, 17.9 and 8.2 μg ml−1 respectively. The mean serum level 15min after i.v. injection was 52.5 μg ml−1. The rate of recovery of cephalexin in the urine after i.m. injection was slower than after both i.v. injection and oral administration. Concentrations of cephalexin in the urine reached a higher maximum after i.v. than after i.m. injection, but were maintained for a shorter time. Analysis of the data after i.m. injection suggests the occurrence of a depot-like effect.
Gas-liquid chromatographic separation of the optical isomers of some “ephedrines” and “pseudoephedrines”
Authors: Beckett A H , Testa B 
Published: April 2011

Abstract
Gas-liquid chromatographic separation of the optical isomers of norephedrine, norpseudoephedrine, ephedrine, pseudoephedrine, N-ethylnorephedrine and N-ethylnorpseudoephedrine by means of their N-trifiuoroacetyl-L-prolyl derivatives has been investigated. A quantitative determination of the enantiomeric percentages was possible for the primary amines, and for all secondary amines except pseudoephedrine. The method is suitable for metabolic studies.
The effect of pH and of temperature on the stability and bioactivity of nystatin and amphotericin B
Authors: Hamilton-Miller J M T 
Published: April 2011

Abstract
In the presence of phosphate-citrate buffers, nystatin and amphotericin B are optimally stable between pH 5 and 7. Loss of biological activity followed first-order kinetics, except under acid conditions. Apparent energies, enthalpies, free energies and entropies of activation of the two antibiotics have been calculated at pH 7, and the two sets of figures are similar. Variation in pH between 5 and 8 appeared to have little effect of the activity of amphotericin B against Candida albicans, while nystatin was more active at pH values between 6 and 8. Nystatin was more active at lower incubation temperatures (30-25°), while amphotericin B appeared to be more active at 41°.
Rapid gas-liquid chromatographic estimation of antipyrine in plasma
Authors: Prescott L F , Adjepon-Yamoah K K , Roberts Elizabeth 
Published: April 2011

Abstract
A simple gas-liquid chromatographic method for the estimation of antipyrine in plasma is described. The drug is extracted from alkaline plasma into chloroform and after concentration is chromatographed directly using a mixed liquid phase of 0.5 % SE 30 and 0.5% Carbowax 20M. The standard deviation of the method for plasma containing 10–50 μg ml−1 of antipyrine was 2.8%. Compared with the standard spectrophotometric assay, antipyrine plasma concentrations were lower and the mean plasma half life in 12 patients was slightly but not significantly shorter.
A new modification for studying 5-HT uptake by blood platelets: a re-evaluation of tricyclic antidepressants as uptake inhibitors
Authors: Tuomisto Jouko 
Published: April 2011

Abstract
The effect of imipramine and other antidepressive drugs on 5-HT uptake by rabbit platelets was re-evaluated, since it had become obvious that, in previous studies, too high substrate concentrations and too long incubation times had been used. A Km of 1·8 times 10−7m was obtained for 5-HT uptake when 1 min incubation in plasma was used. Imipramine caused a half-maximal inhibition at 10−7m or lower concentration. When the platelet-rich plasma was diluted with buffer solution, only about 2 times 10−8m imipramine was required for 50% inhibition. This concentration is only 1/500 to 1/100 of concentrations described in most earlier data. In this study, other tricyclic drugs and phenothiazine derivatives were also much more effective than previously demonstrated. Their rank of potency order was, however, very similar to that earlier described. The correlation of uptake inhibition in platelets with 5-HT uptake inhibition in brain synaptosomes was found to be highly significant. It is concluded that the previous studies give valuable information on the relative potency of different drugs inhibiting 5-HT uptake. When the technique is modified as suggested by the present results, the level of uptake-inhibiting potency in an absolute sense is close to that described for other tissues, especially brain synaptosomes or slices. Therefore, platelets can more reliably be used as an easily obtainable model for nerve endings in uptake studies.
Bioassay of vasopressin on the rabbit isolated urinary bladder
Authors: Angelucci L , Erspamer G Falconieri , Negri L 
Published: April 2011

Abstract
The rabbit isolated urinary bladder contracted in the presence of Lys8-vasopressin from threshold concentrations of 5 to 30 μ ml−1 (0·02 to 0·11 ng ml−1). Responses were proportional to the dose used. The tissue gave satisfactory results either fresh or after storage for several days in cold Tyrode or Krebs solution (3–4°). The preparation also contracted in the presence of oxytocin, but it was 7 to 20 times less sensitive to this peptide. A number of other peptides and amines known to stimulate smooth muscle showed low activity on the rabbit urinary bladder and, occasionally, intense tachyphylaxis.
An assay for phenylephrine applicable to stability studies
Authors: Shotton E , Priaulx D J 
Published: April 2011

Abstract
An assay specific for phenylephrine, in the presence of decomposition products, is described. The procedure depends on the separation of the active constituent by cationic exchange resin and the subsequent determination of the ultraviolet absorbance at two selected wavelengths. The method was evaluated using a grossly decomposed buffered solution of phenylephrine hydrochloride, and it was found that phenylephrine could be assayed selectively under these severe conditions. Several other reported methods were also evaluated under these conditions.
Relation between structure of sulphonamides and inhibition of H2-pteroate synthesis in Escherichia coli
Authors: Thijssen H H W 
Published: April 2011

Abstract
Inhibitory activities for cell-free H2-pteroate synthesis in E. coli have been estimated for a heterogeneous series of N1-substituted sulphonamides and for N1N1-dialkyl-sulphonamides. The relation between the cell-free activities and the acid dissociation constants of the N1-substituted sulphonamides showed a parabolic dependency, indicating that the common parabolic relation between antibacterial activity and acidity of sulphonamides is not, as stated by the Breuckner and Cowles theory, a penetration phenomenon. The extent of ionization of the sulphonamides significantly affects the amount of inhibition of H2-pteroate synthesis. Evidence has been obtained that not only the ionized sulphonamide molecules interfere with the enzyme system, but the unionized molecules also contribute to affinity for the enzyme. The non-acidic N1N1-dialkyl-sulphonamides inhibited cell-free H2-pteroate synthesis. Some of the N1N1-dialkyl-sulphonamides showed higher affinity for the enzyme than their mono-substituted parent compounds. The relations between sulphonamide structure and cell-free activity are explainable by the Bell and Roblin theory.
Effect of l-dopa in 54Mn incorporation by tissues
Authors: Bonilla Ernesto , Diez-Ewald Maria , Medrano José Finol 
Published: April 2011

Abstract
54Mn incorporation by tissues was studied in 24 rats fed with excess manganese diet and in 31 fed a normal diet. The effect of intraperitoneally administered l-dopa (100 mg kg−1) on randomly selected rats in each group was determined. Manganese uptake in liver was higher in normally fed rats that received l-dopa; however, the manganese loaded rats showed a lower level of 54Mn incorporation than those on a normal diet. No difference in 54Mn incorporation was found in submaxillary glands from any of the groups studied. In brain tissue, 2 h after injection of l-dopa, the 54Mn radioactivity was the same in normal and manganese-loaded animals and significantly higher than in rats not given the amine. The reverse effect was found in serum which from l-dopa-treated rats showed lower radioactivity than the controls, suggesting an increased passage of the tracer to the tissues. The different response of tissues from manganese-loaded rats could mean that the enzyme adenyl cyclase may be affected by the excess of manganese. Since dopamine does not cross the blood brain barrier, the l-dopa increase of 54Mn uptake by brain could occur in the endothelial cells of the capillaries.
Multicomponent analysis of ultraviolet spectra: application to pharmaceutical dosage forms
Authors: Madsen B W , Robertson J S 
Published: April 2011

Abstract
Assay of sulphacetamide and physostigmine eye drops, sulphadi-midine and tri-sulphonamide tablets, and a triple barbiturate capsule has been possible without prior extraction or purification of the ingredients. Concentration estimates were found using the method of least squares, and safeguards were incorporated in the computer program to determine confidence levels. The method should be applicable to other agents and dosage forms and lend itself to automation.
Solute migration during granule drying
Authors: Rubinstein M H , Ridgway K 
Published: April 2011

Abstract
Spherical granules of magnesium carbonate, incorporating polyvinylpyrrolidone (PVP) as granulating agent, have been dried at various temperatures under controlled conditions in a drying tunnel. At each drying temperature the rate of loss of moisture was continuously recorded. The PVP distribution, modulus of elasticity, Brinell hardness and friability of the granules were measured as a function both of moisture content and of depth from the granule surface. The radial distribution of PVP at different stages of the drying process and at three drying temperatures, and its effect on the physical properties of the granules, were thus found. This gave a picture of binder distribution within the granule and its effect on local strength as drying occurred and also of the overall change caused by alteration in drying temperature.
Inhibitory effects of L-glutamine on the aspirin-induced gastric lesions in the rat
Authors: Okabe S , Takeuchi K , Nakamura K , Takagi K 
Published: April 2011

Abstract
The effects of an amino acid, L-glutamine, on aspirin-induced gastric lesions and gastric secretion were studied in either intact or pylorus-ligated rats. L-Glutamine had a pronounced inhibitory effect on gastric lesions induced by aspirin administered by oral, intraperitoneal, or intraduodenal routes to intact or pylorus-ligated rats. By the oral route the inhibition was dose-related. However, L-glutamine given either intraduodenally or intraperitoneally did not show any appreciable effects on gastric lesions induced by orally administered aspirin in pylorus-ligated rats. One mechanism of L-glutamine protection was inhibition of a back diffusion of gastric acid caused by aspirin and this was demonstrated in pylorus-ligated rats. The reduction in H+ and increase in Na+ concentrations in the lumen caused by aspirin was returned to normal by increasing doses of L-glutamine. In addition, L-glutamine was considered to inhibit the back diffusion of acid caused by pylorus ligation per se, because the amino-acid produced an increment of H+ and reduction of Na+ and K+ in comparison with the control group. The role of pepsin on L-glutamine protection was negligible.
Some pharmacological actions of 2,5-dimethoxy-4-ethylamphetamine (DOET) in rats and mice
Authors: Huang Jen-Tzaw , Ho Beng T 
Published: April 2011

Abstract
DOET, like DOM, exhibited pressor action in rats. This increase of blood pressure was blocked by pretreatment with cinanserin. DOET at high doses decreased the spontaneous locomotor activity of mice at the first hour but increased the activity at the second hour; a low dose was less effective. DOET also increased the rectal temperature of rats and this hyperthermic action was suppressed by pretreating the animals with cinanserin or methysergide. These actions of DOET were compared with those of DOM.
The effect of 5-hydroxytryptophan on food intake and on the anorexic action of amphetamine and fenfluramine
Authors: Blundell J E , Leshem M B 
Published: April 2011

Abstract
5-Hydroxytryptophan (5-HTP), amphetamine and fenfluramine suppressed food intake in normal rats and in animals with lesions of the lateral hypothalamus. The anorexic effect of amphetamine was reduced in lesioned animals compared with controls while the effect of 5-HTP like that of fenfluramine was increased. When administered in conjunction with the anorexic drugs, 5-HTP markedly potentiated the anorexic effect of amphetamine in both control and lesioned animals. However, 5-HTP potentiated fenfluramine anorexia only in lesioned rats. These findings provide further evidence for the role of 5-hydroxytryptamine (5-HT), in the anorexic effect of fenfluramine, and suggest that a 5-HT mechanism, inhibitory for feeding, produces particularly severe suppression of food intake in rats with lateral hypothalamic lesions.
Binding of chlorpromazine and imipramine to red cells, albumin, lipoproteins and other blood components
Authors: Bickel M H 
Published: April 2011

Abstract
The binding of model drugs to human blood and individual blood components has been determined by equilibrium dialysis and expressed in terms of classes of binding sites, association constants and binding capacities. Chlorpromazine and imipramine are bound to three major components: membranes of red cells, albumin, and lipoproteins. The affinity and capacity of lipoprotein binding is at least as high as that of albumin and is equally distributed on HDL, LDL, VLDL, and on the chylomicrons. White blood cells and platelets are of minor importance in terms of binding capacity. No binding was detected with γ-globulins or α- and β-globulins other than lipoproteins. In contrast, salicylic acid was not bound to red cells or lipoproteins.
The pharmacology of 14-hydroxyazidomorphine
Authors: Knoll J , Fürst Susanna , Makleit S 
Published: April 2011

Abstract
6-Deoxy-6-dihydroazido-14-hydroxyisomorphine (14-hydroxyazidomorphine) was synthesized, its analgesic potency in mice and rats, its antitussive effect in rats and its dependence liability in mice, rats and monkeys were studied. Azidomorphine, the 14-nonhydroxylated parent molecule, morphine, hydromorphone and oxymorphone were used for comparison. 14-Hydroxyazidomorphine proved to be as potent an analgesic as azidomorphine, even more potent as an antitussive, and showed the same low tolerance and dependence capacity. It was 11.6 times less toxic than azidomorphine in mice and 6.5 times less toxic in rats.
A simultaneous determination of acetylsalicylic acid, salicylic acid and salicylamide in plasma by gas liquid chromatography
Authors: Rance Michael J , Jordan Bernard J , Nichols John D 
Published: April 2011

Abstract
A novel method for the simultaneous determination of acetylsalicylic acid, salicylic acid and salicylamide in biological fluids by gas liquid chromatography is described. The assay has been used to determine the plasma concentration of salicylates in 10 volunteers after oral ingestion of three commercially available aspirin-containing formulations. No difficulty was encountered in determining low concentrations of acetylsalicylic acid in the presence of higher concentrations of salicylic acid. The in vivo plasma half life of acetylsalicylic acid in man was found to be 15.5 min.
Synthesis and characteristics of the enantiomers of the cyclic metabonate of methadone
Authors: Beckett A H , Essien E E , Antiri-Penrose C 
Published: April 2011

Abstract
2-Ethylidene-l,5-dimethyl-3,3-diphenylpyrrolidine (II), a cyclic metabonate of methadone was synthesized from methadone (I) and methadone-N-oxide (III). m-Chloroperbenzoic acid was used to oxidatively demethylate I while sulphur dioxide reductively demethylated III to give II. The importance of these syntheses lies in the fact that there is no attack on the asymmetric carbon atom in I or III, thus providing direct methods of obtaining the optical isomers of II.
A comparison of solute migration in a test granulation dried by fluidization and other methods
Authors: Travers D N 
Published: April 2011

Abstract
The intragranular migration of sodium chloride in granules made by the wet massing of heavy kaolin B.P. with salt solution has been studied in batches dried by fluidization and a vacuum tumbling method. The larger granules from the fluidized batch exhibited considerable intragranular variation with the outer crust containing over twice the average salt concentration. Solute loss from this layer by abrasion on prolonged fluidization was slight but the dust eluted from the dryer had a salt content above average. Analysis of sieved fractions of the dust showed that this enrichment was concentrated in the fine material passing a 53 μm mesh. The vacuum dried granules had less migration and were less resistant to crushing than those dried by fluidization. The dust produced had a salt content only slightly greater than the average composition and the overall solute content of the sized fractions were all close to this average. The same system was used to study intergranular migration in a fixed bed when the granules were dried by infrared radiation, by microwave radiation, by convection from air and in a vacuum. The greatest migration occurred in samples dried by infrared radiation and the maximum solute concentration was near the middle of the bed. The air dried granules had less migration and the maximum concentration was in the surface layer. The granules dried in a vacuum and by microwave radiation were fairly uniform in composition throughout the bed. The above results are explained on the basis of the capillary theory of drying together with the modifying influence of the drying method on the probable heat and mass transfer rates.
Trialkylsilyl moieties as potential pharmacokinetic modifying groups for aminoalcohols
Authors: Beckett A H , Taylor D C , Gorrod J W 
Published: April 2011

Abstract
Water soluble derivatives of the aminoalcohols methylephedrine, ephedrine and norephedrine have been synthesized to contain various trialkyl silyl groups attached to the hydroxyl group of the aminoalcohol hydrochloride. Variation of the alkyl substituents on the silyl group produces a wide variety of derivatives possessing differing lipid solubilities and rates of hydrolysis to the parent aminoalcohol.
The percutaneous absorption of phenolic compounds: the effect of vehicles on the penetration of phenol
Authors: Roberts M S , Anderson R A 
Published: April 2011

Abstract
The effects of interactions between drug and skin, drug and vehicle, and vehicle and skin on the overall penetration rate of a drug through the skin may be evaluated by comparison of penetration rates through excised skin and an inert reference membrane such as polyethylene. Dimethyl sulphoxide, dimethyl formamide, ethanol and water increase the permeability of the skin but because of reduced thermodynamic activities in the vehicles low penetration rates are observed.
Enhancement of permeability of ethyl cellulose films for drug penetration
Authors: Donbrow M , Friedman M 
Published: April 2011

Abstract
Permeability constants of salicylic acid, caffeine and benzoic acid have been measured at 37° for heterogeneous films of ethyl cellulose containing up to 50% PEG 4000, the latter component undergoing leaching out. For the first two compounds, steady state constants were independent of film thickness and solute concentration but increased linearly and sharply with PEG content and were reproducible. The films were impermeable to NaOH and permeation rates were independent of receiver compartment pH. Solubility coefficients and diffusion coefficients of the substances in the films were measured using sorption and/or time lag methods and were low as compared with polyethylene films. High solubility seemed to be associated with the presence of a free activated hydrogen, shown by sorption studies on other substances. From the evidence, it appeared that mass transfer was controlled by the solubility diffusion process in the ethyl cellulose of the membranes with all three substances. Enhancement of permeability by PEG thus seemed due to increased porosity, equivalent to reduction in the effective thickness of the matrix, which nevertheless retained its barrier properties. Enhancement coefficients calculated from the slopes of PEG concentration plots may be useful for predicting the increased mass transfer of drugs through such membranes and could enable the porosity and thickness factors to be balanced against each other for formulation of coated products.