bluuebunny/crossref_metadata_2025 huggingface dataset:
The Mydriatic Response of Mice to Atropine
Authors: Quinton R M
Published: April 2011

The time after subcutaneous injection at which atropine produces most mydriasis in male mice increases with increased body-weight. If the response is measured when it is greatest, and is expressed as a percentage of the maximum mydriatic response obtainable in mice of the weight-range used, the mydriatic response to a dose of atropine is constant in male mice weighing from 16 to 50 g. The time-courses of the mydriatic response to atropine in mice of widely differing weights are parallel to the time-courses of the atropine concentration in the cardiac blood of the mice of the same weight-range given a high dose of atropine subcutaneously. The mydriatic response to atropine is found to be increased at times of poor ambient lighting (such as dusk): if however the mice are tested under conditions of artificial lighting (supplemented by daylight when present), the mydriatic response to a standard dose of atropine is nearly constant at all times from 8 a.m. to 2 a.m.
The Quantitative Conversion of Barbaloin to Aloe-Emodin and its Application to the Evaluation of Aloes
Authors: Fairbairn J W , Simic S
Published: April 2011

Barbaloin can be quantitatively converted into aloe-emodin by heating a solution in 4 N hydrochloric acid, containing 4 per cent ferric chloride, for 4 hr. in a boiling water bath under reflux. Each of these numerical conditions can be varied ±10 per cent without significantly altering the yields. The reaction has been successfully applied to the assay of commercial samples of aloes.
A Note on the Preparation of Ricinoleic Acid by Urea Complexing
Authors: Chakravarty Diptish , Bose Arun
Published: April 2011

Some fatty acids were separated from hydrolysed castor oil by successive additions of urea. The method was utilised to prepare ricinoleic acid of B.P. 1948 standard from castor oil.
A Note on the Synthesis of Esters of N-Methylpyrrolidinylalkanols
Authors: Perks F , Russell P J
Published: April 2011

The preparation of a series of esters of 1-methyl-2, 5-di-2-hydroxy-2-phenylethyl)pyrrolidine is described. They are assigned trans configurations on the basis of their pKa values.
Blockade of 5-Hydroxytryptamine Antidiuresis in Rats by 2-Bromlysergic Acid Diethylamide Tartrate and 1-Methyl-Lysergic Acid Butanolamide
Authors: Chodera A
Published: April 2011

The effects of two lysergic acid derivatives, 2-bromlysergic acid diethylamide ‘BOL 148’ and 1-methyl-lysergic acid butanolamide ‘UML 491’ on the antidiuresis induced by 5-hydroxytryptamine ‘5-HT’ has been studied in rats given a dose of 1 mg./kg. 5-HT subcutaneously. BOL 148, 5 mg./kg., and UML 491, 2·5 mg./kg., counteracted the induced antidiuresis. By contrast, the antidiuretic effect of posterior pituitary extract was not blocked or diminished by BOL 148 or by UML 491. BOL 148 and UML 491 alone did not have a diuretic or antidiuretic action.
Reversal of the Effect of α-Methyldopa by Monoamine Oxidase Inhibitors
Authors: van Rossum J M , Hurkmans J A Th M
Published: April 2011

L-α-Methyldopa, which normally causes sedation, induces a strong central excitation in mice pretreated with a monoamine oxidase inhibitor after a lag of a few hours. It is concluded that this excitation is caused by accumulation of free catecholamines liberated by amines which are slowly formed by decarboxylation of α-methyldopa. The hypotensive and sedative effects of α-methyldopa given alone are attributed to the slow release of catecholamines and subsequent breakdown by monoamine oxidase so that a partial depletion of catecholamines ensues.
A Note on the Antifungal Activity of Pentachlorophenyl Dodecanoate
Authors: McAllister Ronald A
Published: April 2011

The antifungal activity of pentachlorophenyl dodecanoate against certain dermatophytes has been studied. The substance, in Sabouraud's maltose agar in 2 per cent concentration, inhibited the growth of Microsporum canis, Trichophyton interdigitale, Trichophyton rubrum, and Microsporum audouini. No activity was observed against Candida albicans, and only a slight inhibition in the growth of Epidermophyton floccosum. A 3 per cent concentration of the ester in an ointment base effected complete inhibition of Trichophyton interdigitale and Microsporum canis alone, and in mixed cultures.
Some Observations on the Physical and Pharmacological Properties of Picrotoxin Solutions
Authors: Ramwell P W , Shaw Jane E
Published: April 2011

A slow and spontaneous decrease in pH was observed with freshly prepared aqueous solutions of commercially available picrotoxin and this change was catalysed by the addition of potassium chloride crystals or by contact with a calomel electrode. The pH at which the solution stabilised was dependent upon the original pH of the solvent and the concentration of the solution. Potassium chloride had little effect upon the pH of freshly prepared saline solutions of picrotoxin. There was no difference in pharmacological activity between freshly prepared picrotoxin solutions, solutions after addition of potassium chloride, or solutions which had been stored.

Since freshly prepared solutions of pure samples of the two recognised constituents of picrotoxin (picrotoxinin and picrotin) were found to be electrometrically stable, the factor responsible for the change of pH may be an impurity; an impurity was detected in commercially prepared samples of picrotoxin by paper chromatography.

Picrotoxinin was the active principle and picrotin was relatively inactive. Slight elevation of the pH markedly reduced the activity of picrotoxin solutions thus supporting an earlier suggestion that for clinical reliability, picrotoxin should be prepared in a buffered solution. No evidence was found to support the belief that Picrotoxin Injection B.P. 1958 should be protected from light.
An Investigation into the Effects of Gamma-Rays on Aqueous Solutions of p-Aminobenzoic Acid
Authors: Marriott P H
Published: April 2011

Aqueous solutions of p-aminobenzoic acid (0·3 per cent) were irradiated with gamma-rays under both oxygen-saturated and oxygen-free conditions. By means of paper chromatography, p-nitrobenzoic acid has been isolated from the irradiated, oxygenated aqueous solution and 4-amino-3-hydroxybenzoic acid isolated from the irradiated, oxygen-free aqueous solution.

These products were probably produced by indirect action of the Co-60 gamma-rays.
Self-Administration of Pralidoxime in Nerve Gas Poisoning with A Note on the Stability of the Drug
Authors: Barkman Rolf , Edgren Bo , Sundwall Anders
Published: April 2011

Plasma concentrations of pralidoxime methane sulphonate (P2S) have been determined in man after self-administration by an automatic injector. After administration of 10 mg./kg. P2S in a 50 per cent w/v solution, concentrations over 4 μg./ml. were reached within 6 min. and maintained for about 90 min. After 20 mg./kg., plasma concentrations over 4 μg./ml. were maintained for about 170 min. Except for pain at the site of injection, which disappeared after a few hr., no serious side reactions could be detected. The drug can be stored for 5 years at 5° with less than 7 per cent decomposition. The decomposition products were found to be less toxic than the unchanged oxime. N-Methylpyridinium-2-carboxamide was identified as a major degradation product.
Effect of Pronethalol on Some Inhibitory Actions of Catecholamines
Authors: Vanov S
Published: April 2011

On the blood pressure of the pithed rat isoprenaline produced a vasodepressor, noradrenaline a pressor, and adrenaline a biphasic response consisting of a rise followed by a fall in the pressure. The magnitude of the responses to increasing doses of adrenaline was not proportional to the doses. An intravenous injection of pronethalol (nethalide) hydrochloride (1 mg./kg.) changed the responses to adrenaline into purely pressor, well-graded responses; they were also increased. The responses to isoprenaline after pronethalol were reduced, but those to noradrenaline remained usually unaltered. Similar results were obtained in anaesthetised rats, rabbits and guinea-pigs, but the augmentation of the pressor effect of adrenaline was not so marked as in pithed rats. The vasodepressor action of dopamine in rabbits and guinea-pigs was not blocked by pronethalol (2·5 to 10 mg./kg.). The inhibitory actions of adrenaline, noradrenaline and isoprenaline on the isolated rat uterus and rabbit colon were not consistently antagonised by concentrations of pronethalol up to 1·0 μg./ml. In experiments on the rabbit duodenum and ileum, pronethalol, 0·2 to 1·0 μg./ml., reduced the relaxations produced by all three catecholamines. These results are discussed in relation to Ahlquist's theory of a dual adrenergic receptor mechanism.
The Application of the Coulter Counter to Problems in the Size Analysis of Insoluble Drugs
Authors: Thornton M J
Published: April 2011

A method of programming an electronic computer has been developed which fits the results of size analyses obtained by means of a Coulter counter to a logarithmic normal curve from which a specific surface area figure is derived. Applications of the method to suspensions of phenothiazine are discussed.
A Spectrophotometric Method for the Determination of β-Glycyrrhetic Acid (Enoxolone) and its Esters in Biological Materials
Authors: Coleman T J , Parke D V
Published: April 2011

A method for the determination of β-glycyrrhetic acid (enoxolone) and its readily-hydrolysable esters in biological materials is described. The material containing the glycyrrhetic acid or its esters is hydrolysed with ethanolic sodium hydroxide, the glycyrrhetic acid is extracted from the acidified hydrolysate, submitted to two-dimensional, thin-layer chromatography on alumina, eluted with ethanol and estimated spectrophotometrically at 248 mμ. Mean recoveries of 100 μg. β-glycyrrhetic acid were 102 per cent (s.e.m. ± 4 per cent) from pure solution; 92 per cent (s.e.m. ± 4 per cent) from rat blood; 90 per cent (s.e.m. ± 4 per cent) from human urine; and recoveries of 20 μg. and 50 μg. from rat bile were 91 to 95 per cent. Mean recoveries of 100 μg. of ±-glycyrrhetic acid hydrogen succinate were 95 per cent (s.e.m. ± 5 per cent) from pure solution; 100 and 110 per cent from rat blood; and 92 and 109 per cent from human urine.
The hydrolysis of propyl benzoate in aqueous solutions of surface-active agents
Authors: Mitchell A G
Published: April 2011

The effect of cetrimide and sodium lauryl sulphate on the alkaline hydrolysis of emulsions and solutions of n-propyl benzoate has been investigated and compared with results obtained previously in cetomacrogol solutions. Evidence is presented to show that the rate of reaction depends on the degree of saturation of the dispersion expressed as a “Saturation Ratio”, which is the ratio of ester concentration to its solubility in a given concentration of surface-active agent. The hydrolysis rate of solubilised ester decreases with increase in surface-active agent concentration while the effect of such an increase in concentration on the hydrolysis rate of emulsified ester depends on the nature of the surface-active agent. The initial rate in sodium lauryl sulphate and cetomacrogol is independent of concentration, but in cetrimide the rate increases with cetrimide concentration until sufficient is present to solubilise the ester.
Preliminary chemical examination of digitalis tissue cultures for cardenolides
Authors: Büchner Stanislaw A , Staba E John
Published: April 2011

Three Digitalis species were grown as callus or suspension tissue cultures, extracted and examined by paper chromatography. Kedde-positive substances (cardenolide glycosides) were found.
Capillary permeability responses to snake venoms
Authors: Fearn H J , Smith Caroline , West G B
Published: April 2011

Russell’s viper venom is many times more toxic to mice on intravenous administration than is saw-scaled viper venom, and yet on local intradermal injection the two venoms have equal capillary permeability effects in mice, rats, guinea-pigs and rabbits. Their effects are completely prevented by drugs possessing both antihistamine and anti-5-ht properties. It is concluded that the increased capillary permeability induced by the venoms is largely mediated through the release of histamine and 5-ht.
Determination of vitamin D by isomerisation
Authors: Dechene Earl B
Published: April 2011

Conditions have been established in which the spectral change produced by the isomerisation of vitamin D2 and D3 to the trans-isomers can be used as an accurate measurement of vitamin D. Vitamin D was successfully determined by isomerisation in commercial products containing only vitamin D at a relatively high potency, without the use of chromatographic procedures.
The action of reserpine and α-methyl-m-tyrosine on the analgesic effect of morphine in rats and mice
Authors: Medaković M , Banić B
Published: April 2011

The actions of α-methyl-m-tyrosine (mmt) and reserpine upon the analgesic effect of morphine has been studied in rats and mice. In rats, reserpine antagonised the effect of morphine, while mmt did not cause any appreciable change of the effect of morphine, injected either 2 or 24 hr after mmt. Reserpine also produced its antagonistic action to morphine in rats which were previously (24 hr) treated with mmt. Both mmt and reserpine potentiated the effect of morphine in rats pretreated (24 hr previously) with iproniazid. In mice, both mmt and reserpine antagonised the effect of morphine. Reserpine failed to do so in mmt pretreated animals. The effect of morphine was restored 24 hr after the injection of mmt. It is suggested that the inhibitory action of reserpine upon the analgesic effect of morphine is due to the antagonistic action of brain 5-ht, which is activated after being released from its stores by reserpine. The pattern of reserpine—mmt—morphine interactions in rats probably differs from that in mice.
Method for recording respiratory changes induced in guinea-pigs by aerosols of histamine or of specific antigen, and for assessing drugs which antagonise bronchoconstriction
Authors: Bennett A , Lockett MARY F
Published: April 2011

A lightly-anaesthetised guinea-pig is made to breathe an aerosol of histamine or of specific antigen pumped into a breathing chamber. The guinea-pig’s respiration produces pressure changes which are recorded on a smoked drum. Isoprenaline and the antihistamine thenyldiamine, administered as aerosols or by injection, have been used to inhibit the reduction in “tidal volume” due to the bronchoconstrictor agents.
Determination of o-methoxycinnamaldehyde in cassia oil by infra-red spectrophotometry
Authors: Chowdhury M A , Williams W D
Published: April 2011

The determination of o-methoxycinnamaldehyde is described, based upon an absorption measurement at 1266 cm−1 in the infra-red region of the spectrum together with the normal assay for total aldehydes. Comparison of the absorption at 1266 and 1312 cm−1 may be used qualitatively to distinguish between oils derived from the bark of Cinnamomum cassia Blume and those from the leaves and twigs.
Response of standardised suspensions of Escherichia coli to iodine
Authors: Newton J M , Vickers J A
Published: April 2011

Suspensions of Escherichia coli prepared from agar slopes by a standardised method were compared with washed suspensions, prepared by a centrifuging process, the dry weight of which was less than that of the unwashed suspensions for the same number of viable cells. In a series of experiments the dry weight of a given number of washed cells proved to be more constant than the dry weight of the same number of unwashed cells. The washed bacteria were more susceptible to iodine than the unwashed bacteria.
The role of histamine and 5-hydroxytryptamine in inflammatory processes
Authors: Bhatt K G S , Sanyal R K
Published: April 2011

During aseptic inflammation there is a rise in the histamine and 5-hydroxytryptamine (5-HT) contents of the skin and several internal organs in mice and rats. The time course of this rise has been worked out. Depletion of histamine or 5-HT, adversely affects the exudative or reparative phases of inflammation in the rat. Reserpine, the agent used to deplete 5-HT, produces an effect which resembles the action of antiinflammatory steroids like prednisolone.
Preparation and surface-active properties of glycyrrhizic acid and its salts
Authors: Gilbert R J , James K C
Published: April 2011

Methods are given for the preparation in a pure form of glycyrrhizic acid and its salts. From conductivity and surface tension measurements and unsuccessful solubilisation studies it would appear that micelle formation does not occur in pure solutions of these substances.
Absolute configuration of dextropropoxyphene at the C-3 asymmetric centre
Authors: Casy A F , Myers J L
Published: April 2011

The configuration at the C-3 asymmetric centre of dextropropoxyphene has been related by a stereospecific route to that of the analogous centre of (-)-isomethadone and hence to (R)-α-methyl-β-alanine.
Kinetics of degradation of 2-hydroxyiminomethyl-1-methylpyridinium methanesulphonate
Authors: Fan Moung Choung , Nairn J Graham , Walker George C
Published: April 2011

The decomposition of 2-hydroxyiminomethyl-1-methylpyridinium methanesulphonate (P2S) was studied at different temperatures and pH values. The initial rate of decomposition was found to be first order with respect to P2S concentration. The pH for maximum stability appears to be about 5.
Release of phosphorus-32-containing compounds from Micrococcus lysodeikticus treated with chlorhexidine
Authors: Rye R M , Wiseman David
Published: April 2011

Chlorhexidine has been shown to cause the release of cellular constituents from phosphorus-32 labelled cells of Micrococcus lysodeikticus suspended in distilled water or in phosphate buffer. An initial rapid release is followed by a slower secondary release. This secondary release is inhibited by high concentrations of chlorhexidine. The release depends on the chlorhexidine to cell ratio and not on the absolute bactericide concentration.
Bactericidal activity of chloroxylenol in aqueous solutions of cetomacrogol
Authors: Mitchell A G
Published: April 2011

The bactericidal activity of chloroxylenol in water and in solutions of the non-ionic surface-active agent cetomacrogol is shown to be related to the degree of saturation of the system, expressed as a Saturation Ratio, which is the ratio of the amount of chloroxylenol present to its solubility. A saturated solution of chloroxylenol in water is shown to have the same bactericidal activity as saturated surfactant solutions containing up to 100 times as much chloroxylenol. It is apparent that bactericidal activity depends on the amount of chloroxylenol in the true aqueous “phase” and not the total amount present. The bactericidal activity of undersaturated solutions of chloroxylenol in cetomacrogol falls markedly as the Saturation Ratio is reduced. This is attributed to a change in the distribution of chloroxylenol in favour of the micelles where it is apparently without bactericidal activity.
Action of N-o-Chlorobenzyl-N′N″-dimethylguanidine (BW 392C60), a bretylium-like drug in lowering the intraocular pressure of rabbit eyes
Authors: Gessa G L , Sangiorgi G
Published: April 2011

N-o-Chlorobenzyl-N′N″-dimethylguanidine (BW392C60), a potent bretylium-like drug, lowers the intraocular pressure in rabbits either when injected intravenously or when instilled into the conjunctival sac. The lowering of the intraocular pressure is accompanied by miosis and relaxation of the nictitating membrane.
Some aspects of the use of thin-layer chromatography in a limit test for related foreign steroids
Authors: Clifford C J , Wilkinson J V , Wragg J S
Published: April 2011

To attain the maximum separation of the steroid impurities in pharmaceutically important synthetic corticosteroids the running of two or more chromatograms using different solvent systems is recommended. Using adsorption chromatography, solvent systems of the type 1,2-dichloroethane: methanol:water, 95:5:0·2, give the most satisfactory general separations. Some steroids can best be separated by partition chromatography, using formamide as the stationary phase and chloroform:ether:water, 80:20:0·5, or cyclohexane:tetrachloroethane:water, 50:50:0·1, as the mobile phase. A spray reagent of 0·05% tetrazolium blue and 8% sodium hydroxide in methanol is recommended. The amounts of foreign related steroids can be limited by running standard amounts of impurities alongside the steroid under test and comparing the colour intensities of the impurities in the steroid with those of the standards.
The detection and identification of other 17,21-dihydroxy-20- oxosteroids in corticosteroids
Authors: Johnson C A , Fowler SYLVIA
Published: April 2011

A method is described for the separation of corticosteroids by paper chromatography. It is more sensitive than the present official test and will control the presence of related foreign steroids to a uniform degree and in a reproducible manner. Details of the application of this test to many pharmaceutically important steroids are given and the relationship of molecular structure to mobility in the solvent systems used is discussed.
Effect of Polysorbate (Tween) 80 on the resistance of Pseudomonas aeruginosa to chemical inactivation
Authors: Brown M R W , Richards R M E
Published: April 2011

Log phase cultures of Pseudomonas aeruginosa in nutrient broth containing polysorbate 80 were much less resistant to the action of benzalkonium chloride, chlorhexidine diacetate and polymyxin B sulphate than cells grown in plain broth.
An isolated parasympathetically-innervated oesophagus preparation from the chick
Authors: Bowman W C , Everett SALLY D
Published: April 2011

An isolated parasympathetically-innervated preparation from the chick oesophagus is described. This preparation is essentially similar to mammalian parasympathetically-innervated smooth muscles in its responses to drugs, and because of its simplicity, robustness and cheapness it is recommended for use in student practical classes.
Umbelliferous fruit identification by thin-layer chromatography
Authors: Betts T J
Published: April 2011

Unknown umbelliferous fruits, including powders, may be identified by thin-layer chromatography of petroleum extracts on silicic acid containing fluorescein. The constituents of the essential oils thus extracted are usually diagnostic. The method is particularly useful in distinguishing Indian dill (Anethum sowa Roxb.) from dill (A. graveolens L.), and will detect an admixture of one part of the former in four parts of the latter.
Preparation and fungicidal properties of (phenylthio)-acetohydroxamic acids and related compounds
Authors: Zayed S M A D , Aboulezz A F , Salama A M , El-Hamouly W S
Published: April 2011

1-Chloro-4,5-dimethoxy-2-nitrobenzene and 1-bromo-2,5-dimethoxy-4-nitrobenzene condensed readily with thioglycollic acid in alkaline medium to give the corresponding sulphides. (4,5-Dimethoxy-2-nitrophenylthio)- and (2,5-dimethoxy-4-nitrophenylthio)acetic acid, as well as the corresponding amides and hydroxamic acids, have been prepared and tested for their fungicidal properties against Aspergillus niger and Rhizoctonia solani. The (phenylthio)acetohydroxamic acids were found to be more fungicidal than the corresponding carboxylic acids against the phytopathogenic fungus Rhizoctonia solani.
Salicylate and aminotransferases
Authors: Gould B J , Smith M J H
Published: April 2011

Enzymic transfer of the amino-group of each of 20 amino-acids to α-oxoglutarate has been studied using lyophilised extracts of rat heart, liver, brain, kidney and skeletal muscle as enzyme source. The glutamate produced was estimated from the carbon dioxide liberated by a bacterial decarboxylase in an autoanalyser. Only asparagine was completely inactive in the transfer. Aminotransferase activity was otherwise unevenly distributed in the tissues. Salicylate (10 mm) was generally inhibitory but it activated the l-tryptophan-α-oxoglutarate aminotransferase.
An automatic apparatus for repeated stimulation of isolated organs by agonist drugs
Authors: Wilson A B
Published: April 2011

A simple commutator for attachment to a standard laboratory kymograph has been designed to operate automatically an apparatus for producing repeated contractions of isolated organs by agonist drugs.
The estimation of anthracene derivatives in senna and rhubarb
Authors: Lemli J
Published: April 2011

An assay is described for the estimation of total anthracene derivatives in senna, rhubarb or their preparations. The extracted glycosides are oxidised by ferric chloride in aqueous solution followed by hydrolysis in acid solution. The free anthraquinones are estimated colorimetrically.
Influence of temperature on the responses of the guinea-pig hypogastric nerve-vas deferens preparation
Authors: Bella D Della , Gandini A , Preti M
Published: April 2011

Over a temperature range of 32 to 20°, responses of the vas deferens to hypogastric stimulation at 50 shocks/sec became gradually smaller, while those to 10 shocks/sec increased gradually. A parallel study, under the same temperature conditions, of drugs known to interfere with peripheral sympathetic transmission revealed a marked reduction of the inhibitory properties of the adrenergic neurone blocking agents bretylium and xylocholine at the lower temperatures. The mechanism by which cooling modified the responses of the preparation to nerve stimulation as well as to the activity of the drugs on the vas is discussed and tentative hypotheses are advanced.
Application of the Ferguson principle to the antimicrobial activity of quaternary ammonium salts
Authors: Weiner Norman D , Hart Fanchon , Zografi George
Published: April 2011

The activity of three quaternary ammonium salts, dodecyltrimethylammonium chloride, dodecyldimethylethylammonium chloride and dodecylpyridinium chloride, against M. aureus, E. coli and C. albicans has been determined and correlated with the surface properties of these compounds. The Ferguson principle has been applied by using surface concentration to estimate thermodynamic activity. Results obtained for the three quaternary ammonium salts and a particular micro-organism species were found to be in good agreement with each other when microbiological and surface studies were conducted under identical conditions.
Effects of acetylcholine, vagal stimulation and tyramine on the isolated atria of the tortoise
Authors: Kim Yung In , Shin Park Chang
Published: April 2011

In the vagus-atrial preparation of the tortoise (Amyda japonica), a cold-blooded animal, acetylcholine and vagal stimulation, in the presence of atropine, produced positive inotropic effects which were inhibited by dichloroisoprenaline or pronethalol. Hexamethonium blocked the excitatory effect of acetylcholine but only slightly inhibited that of vagal stimulation. Tyramine exerted a positive inotropic action in this preparation, but had little effect on atria prepared from reserpine-treated animals. Tyramine was shown to release a substance from the tortoise atria which caused contraction of aortic strips taken from reserpine-treated rabbits, and which appeared to be a catecholamine.
Effect of body weight changes on the formation of cotton pellet-induced granuloma
Authors: Dipasquale G , Meli A
Published: April 2011

Cotton pellet-induced granuloma formation in intact animals is intimately dependent upon body growth and general anabolic processes. Deposition of connective tissue around the pellet continues up to (and probably beyond) the observation period of 90 days after implantation. Anorexic or catabolic agents, or both, or restricted food intake markedly impairs granuloma formation as a result of an impaired body growth. By expressing the amount of granuloma formed in mg/100 g body weight, the true anti-granulomatous properties of a drug can be easily dissociated from those attributable to an impaired body growth. The mechanism by which impairment in body growth affects granuloma formation is discussed.
Some physical properties of lactose and magnesia
Authors: Jones T M , Pilpel N
Published: April 2011

Anomalies in some of the physical properties of spray dried lactose and granulated magnesium oxide have been traced to the presence of fines. These are strongly adsorbed onto particles of about 1,000 μ diameter, being held in position by van der Waals’ and electrostatic forces. Although they are not displaced during sieving, they can be removed by washing the powders with organic solvents.
Method of making spore papers of reproducible resistance
Authors: Cook A M , Brown M R W
Published: April 2011

A method of making papers impregnated with Bacillus stearothermophilus spores is described. Replicate experiments testing the resistance of these papers to steam at different temperatures have given reproducible results.
Some studies of friction and lubrication using an instrumented tablet machine
Authors: Lewis C J , Shotton E
Published: April 2011

Samples of crystalline aspirin, hexamine, and sodium chloride, and a granulation of hexamine were compressed on an instrumented tablet machine. Further samples of these materials, together with samples of sucrose and sucrose granulation, were lubricated with 2% magnesium stearate −100 mesh powder and compacted under similar conditions. The effect of magnesium stearate on die wall friction depends on the ease of deformation of the base particles. For the materials used there is a linear relationship of the form Fa = kd(Pm.A) and a linear relationship exists between Fe and Fd up to the point where Fe becomes constant. Granulations required larger ejection forces at a given pressure than the corresponding crystalline material, particularly when the materials were lubricated; constant values of Fe were associated with compaction pressures at which the density of the ejected tablets became maximal. Values of Fe for tablets of unlubricated sodium chloride and hexamine granulation depend on particle size; the size of other materials used caused no such effect. Lubrication eliminated this size effect.
Accelerated crystal growth of sulphathiazole by temperature cycling
Authors: CARLESS J E , FOSTER A A
Published: April 2011

A novel method is suggested for accelerating the physical changes in suspensions. The suspension is stirred in a jacketed vessel and is alternately heated and cooled. Results indicate a rectilinear relationship between the median particle size of sulphathiazole in suspension and the number of temperature cycles. Crystal growth is measured by the Coulter counter and growth rates are compared arithmetically to indicate which additives (surface-active agents) may be used to inhibit crystal growth.
A calcium requirement for release of 3H-guanethidine by sympathetic nerve stimulation
Authors: BOULLIN D J
Published: April 2011

Cat colons were labelled with 3H-guanethidine by close intra-arterial injection. Two hr later the colons were removed and the vascular bed was perfused with Krebs solution containing 0, 2·5 or 5 mM calcium. The spontaneous efflux of 3H-guanethidine was not changed by alterations in the calcium concentration, but stimulation of the post-ganglionic sympathetic nerves failed to enhance the output of 3H-guanethidine unless calcium was present in the perfusion fluid. It is concluded that extracellular calcium is essential for release of 3H-guanethidine by sympathetic nerve stimulation and that the neural release of the inactive transmitter substitute is related to the pharmacological action of the drug.
A note on the effects of some psychotropic drugs on the aggressive behaviour in the ant, Formica rufa
Authors: KOSTOWSKI WOJCIECH
Published: April 2011

AGGRESSIVE behaviour in lower animals has not been analysed pharmacologically. Inhibition of the motor activity with simultaneous outbursts of aggressiveness seems to be characteristic in ants treated with reserpine (Kostowski, Beck & Mészáros, 1965; 1966). Among the invertebrates, ants are a suitable subject for studies on aggressiveness because of their tendency to attack other species.

We have assessed the influence of drugs on aggressive behaviour in ants and mice.
Coating of pharmaceutical tablets: the spray-pan method
Authors: ANDERSON W , SAKR ADEL M
Published: April 2011

A new method of coating tablets uses the revolving coating pan, but the coating materials are applied in solution or suspension, as a spray from a centrifugal disc atomiser. Addition of coating materials is uniform, controlled, and at a rate which allows even deposition on the tablet. Dry powders need not be used and the process is therefore dust-free. The products of the method compare favourably with tablets coated commercially and with tablets coated by the standard method in laboratory size (16 inch) pans when assessed by uniformity of weight tests, roundness measurement, and radiographic examination.
Determination of micro amounts of 3-(dithien-2-ylmethylene)-1-methylpiperidine, a non-narcotic antitussive
Authors: YUIZONO T , KASÉ Y , KAWANO A , OKUBO H , KATAOKA M
Published: April 2011

A specific colorimetric method for the determination of micro amounts of 3-(dithien-2-ylmethylene)-1-methylpiperidine, a new antitussive and expectorant, is described. Depending on amount, a characteristic colour varying from rose pink to deep bluish purple appears when 2 volumes of a 0·01% solution of ninhydrin in concentrated sulphuric acid are added to 1 volume of an aqueous solution of the drug. After 24 hr at room temperature the colour produced has an absorption maximum at 590 mμ and follows Beer's Law over the range 1–25 μg/ml. The colour is specific for the drug and is sensitive at the μg/ml level. Recoveries from aqueous solution and human urine were 97·4 ± 2·1 and 97·4 ± 1·7% respectively.
The drug-receptor complex
Authors: BURGEN A S V
Published: April 2011

The rate of association of drug and receptor when limited by diffusion alone will correspond to a basic rate of 2·5 × 109 litres/mole sec and will have a net activation energy of 3–4 kcal/mole. This rate will not be significantly increased by attractive forces between drug and receptor but could be reduced by repulsive forces. It could be considerably reduced by the presence of bound water and ions, by the requirement of activation energy for combination and by geometrically restricted access to the receptor. Complex formation is due to the stabilisation of the drug in the force field from which it can escape only on acquisition of kinetic energy greater than the potential energy of the field; the fraction of molecules acquiring this threshold kinetic energy can be calculated from the Boltzman equation. The rate of dissociation of the complex is the rate of loss by free diffusion multiplied by the Boltzman factor. The lifetime of drug receptor complexes is long enough to enable molecules undergoing collision in the non-ideal aspect or conformation time to present in the ideal state.
Transformations in glycyrrhetinic acid: rearrangement of ring A
Authors: ASKAM V , BAINES C M , SMITH H J
Published: April 2011

Methyl 11-oxo-18 β-A-neo-oleana-3, 12-dien-30-oate and the corresponding 18α-isomer have been prepared and tested for anti-inflammatory and antidiuretic activity. Relative to methyl glycyrrhetinate, both kinds of activity and toxicity are reduced by the rearrangement. Features of interest in the nuclear magnetic resonance spectra of 18α- and 18 β-derivatives of glycyrrhetinic acid are recorded.
The effect of humidity and temperature on the cohesion of powders
Authors: SHOTTON E , HARB N
Published: April 2011

The cohesion of wheat, maize and potato starch, acacia, tragacanth, alginic acid, lactose, dextrose and sucrose powders has been determined at different relative humidities and temperatures. For maize, wheat and potato starches, cohesion was a maximum at an intermediate moisture content, whilst for acacia, tragacanth and alginic acid it was independent of the moisture content over the range considered. Lactose, dextrose and sucrose remained free flowing except at high relative humidities.
A note on the determination of pilocarpine in solutions containing methylcellulose
Authors: STEELE J W , THIESSEN J
Published: April 2011

Low results obtained by a colorimetric method for the determination of pilocarpine in ophthalmic solutions are attributed to pilocarpine-methylcellulose interaction. Low results were not obtained with a second colorimetric method. Other factors affecting this interaction are discussed.
The polarographic determination of chlorpromazine and chlorpromazine sulphoxide
Authors: PORTER G S , BERESFORD JEAN
Published: April 2011

Cathodic polarography of solutions containing between 0·1 and 5·0 μg/ml of both chlorpromazine and its sulphoxide enables the sulphoxide to be determined directly. Reductive polarography of the solution after bromination gives an additive wave from which the chlorpromazine is determined by subtraction. The method has been applied to urine, interfering substances being removed by ion-exchange on Amberlite resins.
Anticurare activity of tacrine (THA) in vitro
Authors: REES J M H
Published: April 2011

Tacrine (tha) has been found to be a relatively weak anticurare agent having a significant anticurare activity on the rat isolated phrenic nerve diaphragm preparation in concentrations above 10−7 m. It is about 20 times less potent than neostigmine. Between 10−5 m and 10−4 m, anticurare activity of tha ceases to be reproducible, and in concentrations above 10−4 m the compound exerts a depressant action directly on the muscle. The qualitative and quantitative differences between the anticurare activities of tha and neostigmine are discussed.
Effect of desipramine on directly or indirectly elicited catecholamine pressor responses in rats
Authors: Bonaccorsi A , Garattini S
Published: April 2011

Desipramine enhances the pressor effect induced by noradrenaline, adrenaline, dopamine and dimethylphenylpiperazinium in pithed rats, while indirectly acting sympathomimetic amines, such as tyramine and phenethylamine were inhibited. With a similar degree of noradrenaline potentiation, desipramine was more effective than cocaine as an inhibitor of the tyramine pressor response. Desipramine, but not cocaine, was effective in blocking the hypertension induced by small doses of reserpine in animals pretreated with tranylcypromine.
The effect of chlorhexidine on the electrophoretic mobility, cytoplasmic constituents, dehydrogenase activity and cell walls of Escherichia coli and Staphylococcus aureus
Authors: HUGO W B , LONGWORTH A R
Published: April 2011

Chlorhexidine does not cause lysis of isolated cell walls, nor does it prevent the synthesis of the mucopeptide component of the cell wall. Low concentrations of the drug stimulate dehydrogenase activity but higher concentrations inhibit the activity. Chlorhexidine reacts with and precipitates proteinaceous and pentose-containing components of a solution of cell-free cytoplasmic constituents in concentrations greater than those causing their maximum leakage. The effect of chlorhexidine concentration on the electrophoretic mobility of bacterial cells is consistent with the hypothesis that the drug accumulates in aggregates at the cell surface rather than in the form of a monolayer or multilayers of drug.
Simple methods for the detection of tropinesterase activity in rabbits
Authors: QUINTON R M
Published: April 2011

In experiments in which rabbits are to be given atropine or certain atropine-like agents, it is important to select animals whose plasma is deficient in the enzyme tropinesterase (atropinesterase). Three simple procedures for assessing the presence of this enzyme in rabbits in vivo have been examined. It is concluded that a different procedure is needed for albino rabbits than for animals with dark irides. In this way, 95–98% correct assessments of the presence or absence of tropinesterase have been made by simple procedures within 1 hr. Fully reliable assessments could only be made by in vitro methods, two of which (one quantitative and the other qualitative) are described. The latter enabled a reliable all-or-none assessment of tropinesterase activity to be made with only 0·'02 ml of plasma within 1–2 hr.
The relationship between thin-layer chromatographic behaviour and the stereochemistry of some heteroyohimbine alkaloids
Authors: PHILLIPSON J D , SHELLARD E J
Published: April 2011

ANUMBER of thin-layer chromatography systems have been used to distinguish and identify some indole and oxindole alkaloids isolated from various species of the genus Mitragyna (Shellard & Phillipson, 1964). It has been suggested moreover that a relationship exists between the stereochemistry of these alkaloids and their behaviour on thin-layer chromatograms (Phillipson & Shellard, 1966). Two new heteroyohimbine alkaloids, mitrajavine and hirsutine, have recently been isolated from Mitragyna species (Shellard, Beckett, Tantivatana, Phillipson & Lee, 1966) and their behaviour on thin-layers has been compared with some related alkaloids of known stereochemistry. Based on this, certain suggestions have been made about the stereochemistry of these two new alkaloids.
Determination of the homologue composition of some alkyltrimethyl quaternary ammonium antibacterial agents by gas chromatography
Authors: LAYCOCK H H , MULLEY B A
Published: April 2011

RECENT work has shown that the micellar properties of quaternary ammonium surface-active agents may be linked with their antibacterial action (Weiner, Hart & Zografi, 1965). Micelle formation and antibacterial activity both depend markedly on the chain length of the hydrocarbon groups attached to the quaternary nitrogen, and other biological properties may also depend on this aspect of their structure (Hart & Nissim, 1966). Commercially produced materials are mixtures of homologues and a method is described below for measuring the homologue composition.
Sizing Bacillus megaterium spore populations as a basis for studying their viability
Authors: HIBBERT H R , TALLENTIRE A
Published: April 2011

SEVERAL reports have described microbiological applications of the Coulter Counter, particularly for determining the total count of viable and non-viable vegetative bacteria (Garrett & Miller, 1965) or bacterial spores (Kubitschek, 1958) in suspension. The value of the instrument would be greatly increased if it could be used to differentiate between viable and non-viable bacteria.
Some studies of the diffusion of sodium ions through protein solutions and phospholipid sols
Authors: CASTLEDEN JENNIFER A , FLEMING R
Published: April 2011

Diffusion of sodium-22 in solutions containing sodium chloride, calcium chloride, bovine plasma albumin, lecithin and cholesterol has been examined by two methods which were modifications of the open-end capillary technique of Anderson & Saddington (1949) and the continuous monitoring technique of Mills & Godbole (1958). Preliminary investigations of semi-infinite systems consisting of lecithin sols layered on albumin solutions have been made. The activity in the capillary at various times during diffusion has been compared with the theoretical activity and good agreement has been found.
The absorption by Escherichia coli of phenols and their bactericidal activity
Authors: BEAN H S , DAS A
Published: April 2011

The uptake of several phenols by E. coli may be represented by absorption isotherms. The uptake pattern for dilute solutions suggests partitioning between the cells and aqueous solution but at higher concentrations a change in the uptake pattern suggests protein precipitation. An inflexion in the absorption isotherms corresponds with concentrations producing high levels of activity and can be used to forecast concentrations needed to produce rapid rates of kill.
A note on spectrophotometric methods for the determination of norethynodrel and mestranol in tablets
Authors: BASTOW R A
Published: April 2011

The method for assay of norethynodrel involves acid catalysed rearrangement of the Δ5,10 system to a Δ4,3-ketone with stronger ultraviolet absorption. Mestranol is determined from its absorption at 280 mμ after elimination of the interfering ketonic absorption by reduction with borohydride. Residual interference is allowed for by a three point correction.
The autoxidation of sodium salicylate in aqueous solution
Authors: BEYNON C B , JAMES K C
Published: April 2011

The induction period of the auto-oxidation of aqueous alkaline solutions of sodium salicylate has been examined by following the oxygen concentrations polarographically. The reaction is photochemical, and is catalysed by copper, iron and manganese, although the increase in rate is less than 150% of the rate of the uncatalysed reaction. Bicarbonate ions are not necessary for reaction, which is first order with respect to light intensity and oxygen and salicylate concentrations.
Effect of desipramine on the depolarized isolated renal artery
Authors: HRDINA P , GARATTINI S
Published: April 2011

Depolarization of the isolated renal artery of the rat by a potassium-rich solution caused a triphasic response. The artery contracted submaximally then relaxed partially, this relaxation being followed by a slowly developing contracture. Desipramine reduced the height of the initial contraction, increased the relaxation and reduced the contracture. The latter action was antagonized by increasing the calcium ion concentration of the depolarizing solution. Calcium caused a contraction of the depolarized artery and the contraction was reduced by the drug. The results suggest that the relaxation of the depolarized artery produced by desipramine may be due to interference with the action of calcium in initiating and maintaining a contraction of the arterial smooth muscle.
The effect of reserpine and α-methyldopa on the analgesic action of morphine in the mouse
Authors: ROSS JANET W , ASHFORD A
Published: April 2011

In the tail clip test, reserpine inhibited the analgesic action of morphine, and this action of reserpine was prevented by pretreatment with α-methyldopa. In the hot plate test reserpine potentiated the action of morphine, and α-methyldopa pre- treatment had no inhibitory action on reserpine. α-Methyldopa alone, and in combination with reserpine, showed an analgesic action in the hot plate test.
A quantitative comparison of the antagonism of tubocurarine and diallylnortoxiferine by four anticurare agents
Authors: PLEUVRY BARBARA J , HUNTER A R
Published: April 2011

The antagonism of tubocurarine and diallylnortoxiferine by neostigmine, physostigmine, edrophonium and ambenonium, has been examined on the rat phrenic nerve diaphragm preparation. Ambenonium showed the greatest activity and physostigmine and edrophonium were the least potent and equally active. This order applied to both neuromuscular blocking agents, but all four antagonists show significantly greater activity against diallylnortoxiferine. The possibility that neostigmine and physostigmine have some qualitative differences in anticurare mechanism compared with edrophonium and ambenonium, on this preparation, is discussed.
The effect of concentration, time and temperature on the viability of Penicillium notatum spores exposed to phenols
Authors: CHAUHAN N M , WALTERS V
Published: April 2011

Spores of Penicillium notatum exposed to resorcinol, p-chlorophenol, m-cresol, chlorocresol and hexylresorcinol, give values for the concentration exponent, n, from 7.3 to 3.7 when calculated from first order reaction velocities; higher values are obtained from the times for fixed mortality levels. Values of the temperature coefficient, θ, vary from 1.045–1.331. The log survivor-time curves are convex to the axes for resorcinol and increasingly concave in the order of decreasing water solubility for the other phenols. Equitoxic (99% mortality in 20 min) molar concentrations of the phenols have about a 680-fold range, but Ferguson values, except for resorcinol, vary only from 0.10 to 0.26.