bluuebunny/crossref_metadata_2025_split huggingface dataset:
A comparison of granules prepared by pan granulation and by massing and screening
Authors: GANDERTON D , HUNTER B M 
Published: April 2011

Abstract
Granules of lactose and calcium phosphate were prepared by pan granulation and by massing and screening. Capillary forces and the gentle action of tumbling in the pan were inadequate to compact the fine cohesive calcium phosphate but were highly effective with the less cohesive lactose where the absence of shear gave very high densification. Whereas massing and screening provided the necessary forces for consolidating calcium phosphate, with lactose a more open structure resulted which further dilated during screening. Increase in both moisture content and time of mixing increased granule density but the degree varied with both method and material as did granule shape, strength and compressibility.
Solute migration during granule drying
Authors: RIDGWAY K , RUBINSTEIN M H 
Published: April 2011

Abstract
Spherical granules of magnesium carbonate, 12 mm diameter, have been dried under controlled conditions in a drying tunnel at 44°, the rate of moisture loss being continuously recorded. The granulating agent was polyvinylpyrrolidone (PVP). Granules were removed at various times for analysis. By controlled attrition, successive layers of powder were removed from the granules. The powder was analysed for PVP by infrared spectroscopy, and the friability, modulus of elasticity and Brinell hardness of the granules were measured as a function of depth from the granule surface. The radial distribution of the PVP and its physical effect on the granule properties were thus found.
A new buccal absorption model
Authors: DEARDEN J C , TOMLINSON ERIC 
Published: April 2011

Abstract
Buccal absorption tests indicate that loss of drug from the oral cavity cannot be accounted for solely in terms of passive diffusion into the buccal membrane. A model involving protein-binding is proposed, which satisfactorily explains the observed loss. Studies on two different physical simulations of buccal absorption confirm that the proposed model is consistent with the in vivo results.
The dissolution times of spherical particles
Authors: RIDGWAY K , PEACOCK D G 
Published: April 2011

Abstract
The differential equation governing the rate of change of radius of a spherical particle dissolving or growing in a fluid has been numerically integrated by computer. The particle radius, as a function of time, can thus be calculated, and the dependence of the overall particle lifetime upon physical parameters obtained. The effects of high mass flux, change of solubility with particle size, and progressive saturation due to dissolution into a finite volume of liquid can all be taken into account during the integration process. Results are presented for salicylic, boric and citric acids dissolving in and crystallizing from water; these represent the behaviour of sparingly soluble, moderately soluble and very soluble compounds respectively.
The determination of residual ethylene oxide and halogenated hydrocarbon propellants in sterilized plastics
Authors: WARREN B 
Published: April 2011

Abstract
A specific and sensitive method is described for the determination of residual ethylene oxide, dichlorodifluoromethane and trichlorofluoromethane in sterilized plastic surgical equipment. Residues are isolated from the plastics by high vacuum distillation and analysed by gas chromatography using an exponential dilution apparatus, to avoid the use of solvents. Under the conditions specified, a lower limit of 1 ppm of each component could be detected in blood giving sets of which the main plastics material was PVC. The rate of loss of each component has been studied, to indicate the necessary holding time of the material before it can be considered safe to use.
A polarographic method for the determination of flurandrenolone
Authors: HEASMAN M J , WOOD (IN PART) A J 
Published: April 2011

Abstract
A simple fast scan polarographic method has been developed for the determination of the Δ4-3 ketosteroid flurandrenolone in pharmaceutical formulations. The polarographic peak current due to steroid reduction is measured after ointments have been subjected to a preliminary extraction procedure and creams have been treated with tannic acid to precipitate interfering excipients. The method enables concentrations down to 0·01 % w/w of the steroid to be measured. Neomycin sulphate does not interfere and clioquinol is readily removed using an ion exchange resin. Evidence is presented to show that the carbon-fluorine bond rather than the enone is primarily reduced. The method is faster than a colorimetric method using tetrazolium blue and has a similar accuracy and precision.
Some bronchoconstricting and bronchodilating responses of human isolated bronchi: Evidence for the existence of α-adrenoceptors
Authors: MATHÉ A A , ÅSTRÖM A , PERSSON N-Å 
Published: April 2011

Abstract
Isolated strips of human bronchi obtained during thoracic surgery exhibited pharmacological responses very similar to those of other species (e.g. guinea-pig). Analysis of the action of some sympathomimetic amines indicated that the human bronchi also possess a sparse population of α-adrenoceptors. Propranolol (&gt;1 μg/ml) had a direct bronchoconstricting action, whereas another β-adrenoceptor blocking agent, alprenolol, produced bronchodilatation. Phentolamine (&gt;4 μg/ml) also produced a bronchodilatation of its own. Theophylline and dibutyryl cyclic AMP produced dose-dependent relaxations. The strips were effectively contracted by acetylcholine, histamine, prostaglandin F2α (PGF2α), slow reacting substance (SRS) and bradykinin. Bradykinin, regardless of the dose, produced bronchoconstriction in some preparations and dilatation in others. 5-Hydroxytryptamine produced bronchodilatation but at very high concentrations a constriction was obtained.
The reversal of phenoxybenzamine-produced α-adrenoceptor blockade by the isomers of propranolol and INPEA
Authors: DAVIS W G 
Published: April 2011

Abstract
Isomers of propranolol and N-isopropyl-p-nitrophenylethanolamine (INPEA) were used to demonstrate that there are two mechanisms by which the β-adrenoceptor blocking agents will reverse phenoxy-benzamine-produced α-adrenoceptor blockade. In the seminal vesicle preparation, prior administration of either isomer initially protected the receptors from phenoxybenzamine blockade when the contact time for phenoxybenzamine was short. The isomers were equi-effective, suggesting that this action is independent of β-adrenoceptor blocking activity. When the contact time of phenoxybenzamine was prolonged, the ability of the isomers to protect the α-receptors was lost. In the rat blood pressure preparation, after the development of phenoxybenzamine-produced α-adrenoceptor blockade, (-)- and (±)-propranolol or (-)- and (±)-INPEA, in doses that produced marked β-adrenoceptor blocking activity, partially reversed the α-adrenoceptor blockade. Identical doses of (+)-propranolol or (+)-INPEA, which exhibited weak β-adrenoceptor blocking activity did not produce any reversal. The reversal of phenoxybenzamine-produced α-adrenoceptor blockade in this situation appears therefore to be dependent upon the development of β-adrenoceptor blockade.
The binding of bupivacaine to maternal and foetal plasma proteins
Authors: MATHER L E , LONG G J , THOMAS J 
Published: April 2011

Abstract
The binding of bupivacaine to maternal and foetal plasma proteins has been investigated using a three-compartment dialysis apparatus, in which maternal and foetal plasma could be examined simultaneously. Maternal protein bound approximately twice as much bupivacaine as foetal protein per gram of protein at drug concentrations in the range 0·05 to 5·0 μg/ml. Over the same range of concentrations, 92–78% of bupivacaine was bound to maternal plasma protein but only 35–31% was bound to human albumin indicating that other proteins are involved in the binding of the drug to plasma proteins.
The influence of the moisture content of the fibrous support of a nasal inhaler upon the concentration of drug in the air stream
Authors: ARMSTRONG P A M , CARLESS J E , ENEVER R P 
Published: April 2011

Abstract
The moisture contents of cellulose acetate and paper fibrous support materials used in nasal inhalers have been determined by infrared drying and extraction techniques. The mutual solubilities of water and methylamphetamine have been investigated at various temperatures, and the results indicated that the system exhibited both upper and lower consolute temperatures. The effect of molar composition of water on the total and partial vapour pressures of methylamphetamine-water mixtures have also been investigated. Positive deviations from Raoult's Law were observed for both total and partial pressures. The present results have been related to data obtained previously with an inhaler system to show that the moisture contents of the fibrous supports are partially responsible for the discrepancy between the derived and absolute vapour pressure values for methylamphetamine.
Synthesis and pharmacology of 1-(2-thioxopyrrolidino)-4-pyrrolidino-2-butyne, the thiolactam analogue of oxotremorine
Authors: LINDEKE B , KARLÉN B , DAHLBOM R , GREEN R , JENDEN D J 
Published: April 2011

Abstract
The thiolactam analogue of oxotremorine (I) has been prepared and examined for muscarinic activity in mice and on guinea-pig ileal preparations. It is inactive in itself, but is transformed in vivo to oxotremorine (II), which has been identified in the urine of mice. The urine also contains 1-(2-oxopyrrolidino)-4-pyrrolidino-2-butanone (III) which is formed non-enzymatically from I under acidic conditions, but does not display any acetylcholine-like properties in vivo or in vitro. Oxotremorine is not formed from I in vitro.
Pharmacodynamic effects of dehydroemetine
Authors: SALAKO L A 
Published: April 2011

Abstract
The pharmacodynamics of dehydroemetine were studied in isolated preparations and in whole animals. Dehydroemetine had no effect on the guinea-pig isolated ileum but non-specifically antagonized the spasmogenic effect of histamine, acetylcholine and nicotine on this tissue. Dehydroemetine in small concentrations inhibited relaxations of the guinea-pig and rabbit ileum produced by stimulating the sympathetic nerve without inhibiting the effect of noradrenaline. Twitches of the guinea-pig ileum elicited by transmural stimulation were blocked by dehydroemetine while higher doses of the drug also inhibited the indirectly elicited contractions of the isolated rat diaphragm. In vivo, neuromuscular blocking action could not be demonstrated for dehydroemetine while toxic doses were required to demonstrate the presence of an adrenergic neuron blocking action. Dehydroemetine had no anaesthetic action when applied locally to the rabbit cornea. Concentrations of the drug which caused local anaesthesia when injected intradermally into guinea-pigs also caused skin necrosis. It is concluded that dehydroemetine lacks any specific adrenergic neuron blocking action or neuromuscular blocking action or local anaesthetic action. It is suggested that the effects demonstrated are due to non-specific action at the nerve endings.
Effect of amphetamines on tryptophan concentrations in mice and rats
Authors: SCHUBERT JOHAN , SEDVALL GÖRAN 
Published: April 2011

Abstract
(±)-Amphetamine and some of its analogues were administered intraperitoneally to mice and rats and the concentrations of tryptophan in tissues were analysed by fluorimetric and microbiologic techniques. The concentration of tryptophan in brain was markedly increased by (±)-amphetamine and reached a maximum about 80 min after drug administration. The effect was dose-dependent with a threshold dose below 1 mg/kg. (+)-Amphetamine was significantly more potent than p-chloroamphetamine and p-hydroxyamphetamine, indicating that the changes in tryptophan concentrations might be related to the central stimulating effect of the drugs. (±)-Amphetamine delayed the disappearance from brain of intravenously administered [3H]tryptophan. Inhibition of monoamine oxidase by nialamide (100 mg/kg) and tryptophan hydroxylase by H 22/54 (500 mg/kg) had no effect on the tryptophan concentration in brain.
The interaction of some oral contraceptive steroids with lipid monolayers and with erythrocytes
Authors: FLORENCE A T , RAHMAN R 
Published: April 2011

Abstract
Some steroids used in oral contraceptive combinations have been found to interact with cholesterol and lecithin spread as monolayers on water and to protect erythrocytes against haemolysis. No simple relation between steroid structure and these interactions was found, although in general the more water-soluble members of a group of structurally related compounds interacted to a lesser extent. No distinction could be observed in the behaviour of progestogens and oestrogens in the systems studied. It is suggested in the light of the evidence presented here and from data in the literature that these steroids may adsorb at lipid surfaces and may penetrate lipid membranes. This gives substance to the hypothesis that some steroids adsorb at platelet surfaces and alter the surface properties or the permeability of the platelet membrane sufficiently to cause increased platelet aggregation.
The effect of chlorthalidone on blood sugar and glucose tolerance in the rat
Authors: FURMAN B L , Boswell J 
Published: April 2011

Abstract
Chlorthalidone, in high doses, failed significantly to influence blood sugar or intravenous glucose tolerance in the rat, following the intraperitoneal injection of single doses or 28 day oral treatment with the drug (100 mg/kg daily). The significant effect of the drug in stimulating glucose transfer in everted sacs prepared from rat intestine may explain the trend towards altered oral glucose tolerance observed. Chlorthalidone failed significantly to influence the blood sugar of alloxan diabetic rats and did not modify glucose uptake by rat-hemidiaphragm muscle or epididymal adipose tissue incubated in vitro in the presence or absence of insulin.
The effects of corticosteroids on the reduction of α-adrenoceptor blockade produced by β-adrenoceptor blocking agents
Authors: DAVIS W G , BOURNE R K 
Published: April 2011

Abstract
The inhibition of the pressor effects of noradrenaline by phenoxybenzamine was reduced by propranolol and sotalol in the normal and acutely adrenalectomized, but not in the chronically adrenalectomized, rat. The administration of a glucocorticoid, but not a mineralocorticoid, to the chronically adrenalectomized rat, produced a preparation in which the phenoxybenzamine-produced α-adrenoceptor blockade was reduced by the β-adrenoceptor blocking agents, demonstrating that this action is glucocorticoid-dependent.
The uptake by Escherichia coli and growth inhibitory properties of benzyl alcohol and phenethyl alcohol
Authors: LANG MILDRED , RYE R M 
Published: April 2011

Abstract
The effects of benzyl alcohol (0–4 mg/ml) and phenethyl alcohol (0–2.5 mg/ml) on the rate of mass increase in cultures of E. coli were studied by absorbance measurements. Growth rate constants in the partially inhibited cultures were calculated. With both agents the growth rate was reduced on increasing the alcohol concentration, the extent of this reduction becoming progressively larger for equal increments in concentration. The inhibition of growth was shown to be reversible and to result from a uniform inhibition of the individual cells. The overall cellular uptake of benzyl alcohol was approximately the same as that of phenethyl alcohol. With both agents the uptake was proportional to the concentration of alcohol remaining in the medium and was independent of contact time within the range of 10–90 min. Phenethyl alcohol is, however, more effective than benzyl alcohol in inhibiting growth. This is attributed to a greater uptake of the former by the cellular membrane.
The sterols and tetracyclic triterpenoids of Digitalis purpurea L. seeds
Authors: EVANS F J 
Published: April 2011

Abstract
Three types of sterols were isolated from the non-saponified fraction of D. purpurea seed oil. These were the 4,4′-dimethylsterols, the 4α-methylsterols and the 4-desmethylsterols. By combination of t.l.c., g.l.c. and mass spectrometry, the first group were found to consist of cycloartenol and 24-methylenecycloartenol, the second group of 24-methyl-lophenol, 24-ethyl-lophenol, 24-methylenelophenol, 24-ethylidenelophenol, obtusifoliol, 4α-methylzymosterol and cycloeucalenol. The third group of true phytosterols consisted of cholesterol, campesterol, stigmasterol, β-sitosterol, fucosterol, 28-isofucosterol and 24-methylenecholesterol. Possibly present also in this group were 7-ene-cholestenol, 7-ene-campestenol, 7-ene-22-dihydrostigmastenol, 7-ene-24-methylenecholestenol and 7-ene-isofucostenol.
Enhanced migration of the ionized forms of acidic drugs from water into chloroform in the presence of phospholipids
Authors: FURUSAWA SHUNJI , OKUMURA KATSUHIKO , SEZAKI HITOSHI 
Published: April 2011

Abstract
The transfer process of various acidic drugs from water into chloroform containing phospholipids has been examined using a nonemulsifying system. The ionized forms of the drugs which have little lipid solubility show a marked increase in transfer to the chloroform phase containing lecithin at the physiological pH of the small intestine. The pH-profiles of salicylic acid, p-aminobenzoic acid and sulphisoxazole transfer are in good agreement with available in situ absorption data. These results suggest a role for phospholipids in the intestinal absorption of ionized acidic drugs which has not been clearly apparent with pH-partition hypothesis alone.
The effects of apomorphine, (+)-amphetamine and l-dopa on maximal electroshock convulsions—a comparative study in the rat and mouse
Authors: MCKENZIE G M , SOROKO F E 
Published: April 2011

Abstract
The anticonvulsant activity of apomorphine, (+)-amphetamine and pargyline + l-dopa was examined in the rat and mouse. Whereas all three treatments produced anticonvulsant effects in the rat, only (+)-amphetamine and l-dopa were anticonvulsant in the mouse. It is suggested that enhanced dopamine-like activity is responsible for the anticonvulsant activity of these three drugs in the rat. The anticonvulsant activity of (+)-amphetamine and l-dopa in the mouse may be unrelated to their pharmacological activity on dopaminergic neurons.
Hypothermic effect of apomorphine in the mouse
Authors: FUXE K , SJÖQVIST F 
Published: April 2011

Abstract
A new effect of apomorphine in lowering body temperature in mice is presented. The hypothermic effect is antagonized by haloperidol and pimozide, which block dopamine receptors in brain, and by desipramine and protriptyline which preferentially inhibit amine uptake in noradrenaline neurons. The finding may indicate that dopaminergic mechanisms are involved in temperature control in mice.
Determination of yield value of hectorite gels by the falling sphere method
Authors: CARLESS J E , OCRAN J 
Published: April 2011

Abstract
Two variations of the falling sphere method were used to measure the static yield values of aqueous dispersions of a synthetic hectorite and the results compared with those obtained using the Ferranti Shirley cone-plate viscometer. Yield values were calculated from three equations proposed by various workers but only one equation gave results in reasonable agreement with the cone-plate viscometer. Advantages of the falling sphere method and the derivation of the equations are discussed.
Some parameters describing the dissolution rate of salicylic acid at controlled pH
Authors: COLLETT J H , REES JUDITH A , DICKINSON N A 
Published: April 2011

Abstract
Rates of dissolution of salicylic acid have been determined at constant pH in the absence of buffer salts by use of a pH-stat. The dissolution rate increased with increasing pH up to a maximum of pH 4·0. An increase in stirring speed brought about an increase in dissolution rates at each pH. Diffusion layer thickness and diffusion coefficients have been determined utilizing viscosity and density measurements.
Sound-withdrawal hypertension in rats—a new form of experimental hypertension
Authors: Marwood J F , Lockett Mary F 
Published: April 2011

Abstract
Females of an inbred strain of Wistar rats, initially 160–180 g, develop hypertension when transferred from the stock (normal rat) room (NRR) to a sound-proofed semi-anechoic room (SPR). No hypertension develops when sounds in the NRR are relayed unchanged into the SPR. The hypertension reaches maximum at 4 weeks then decreases slightly to stabilize at a level approximately 30 mm Hg above normal before, and 20 mm Hg above normal after, pentolinium blockade. Histological changes are demonstrable in small arteries after 12 weeks in the SPR. Augmented pressor responses to fixed doses of noradrenaline and of tyramine, but not of angiotensin II and of vasopressin, and a general increase in organ/body wt ratios were evident in weeks 3–5 after entry to the SPR, but had reversed by week 12. These findings contrast with those made on salt-DOCA hypertensives.
Interactions between oxotremorine and inhibitors of Cholinesterase enzymes
Authors: Cox B , Tha S J 
Published: April 2011

Abstract
Interactions between oxotremorine and physostigmine or dyflos have been investigated in mice using doses giving approximately 50% inhibition of mouse brain cholinesterase. Oxotremorine LD50 was unaffected by pretreatment of mice with the anticholinesterases. Its ED50 (tremor) was decreased by physostigmine and neostigmine but not by dyflos. Dyflos antagonized oxotremorine hypothermia, physostigmine was without effect. Oxotremorine did not alter the inhibitory activity of the anticholinesterases. The lack of potentiation of oxotremorine by cholinesterase inhibitors suggests it acts directly in these tests by a mechanism independent of its ability to increase tissue acetylcholine concentration.
Alkaloids from the seeds of Strychnos wallichiana Steud. ex DC. (Strychnos cinnamomifolia Thwaites var. wightii A. W. Hill)
Authors: Bisset N G , Phillipson J D 
Published: April 2011

Abstract
The seeds of a south Indian sample of Strychnos wallichiana Steud. ex DC., previously analysed by Short (1924) under the name S. cinnamomifolia Thwaites and thought to contain mostly brucine with a little strychnine, have now been shown to contain a new base 4-hydroxy-3-methoxystrychnine (I) as the major alkaloidal constituent. Smaller amounts of strychnine, 4-hydroxystrychnine, brucine, vomicine, 4-hydroxy-3-methoxy-N-methyl-sec.-pseudostrychnine (II), and nova-cine and possibly also α-colubrine are present.
The tautomer ratio of histamine
Authors: Ganellin C R 
Published: April 2011

Abstract
The tautomeric equilibrium constant Kt for the two tautomeric forms (Nτ-H and Nπ-H) of histamine mono-cation is determined from the difference between the pKa values of Nπ- and Nτ-methylhistamines, and of Nπ- and Nτ-benzylhistamines. The ratio of concentrations of tautomers [Nτ-H]/[Nπ-H] = Kt is 4&#x006d;̇2 indicating that the histamine mono-cation exists in aqueous solution approximately 80% as the Nτ-H-tautomer and 20% as the Nπ-H tautomer. From the value of Kt and pKa1 of histamine the individual ionization constants at 25° of the two tautomers are derived. Tautomer Nτ-H (pKa1 6&#x006d;̇16) is a slightly weaker base than is tautomer Nπ-H (pKa1 6&#x006d;̇79).