Aqueous quaternary ammonium compounds and rabies treatment.
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Sterile-male-release technique is currently used to control the sea lamprey (Petromyzon marinus) population in the Great Lakes. The chemosterilant (bisazir) used in this program is extremely hazardous; special safety measures are necessary when handling this chemical. Therefore, replacement of bisazir with safer agents is desirable. In this study, we examined the effects of low-toxicity compounds with previously described spermicidal activity (mainly against mammalian sperm) on motility and fertilizing ability of sea lamprey spermatozoa. Nonoxynol-9, benzalkonium chloride, zinc acetate, cupric chloride, cysteamine, tannic acid and propranolol were able to inhibit both sperm motility and fertilizing ability. Effective concentrations of these spermicides ranged from 0.15 to 1%. Therefore, they can be potentially used in further study directed at in vivo sterilization of male sea lampreys.
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A method for measurement of nasal mucociliary clearance in vivo is described. A drop, containing saccharine sodium and indigo carmine is placed on the edge of the ciliary epithelium in the entrance to the nose. The time between placement and the sensing of the sweet taste as well as the appearance of a blue line in the nasopharyngeal cavity is measured and called the transport time. Two preservatives, two nasal drops and one viscosity-increasing substance have been investigated and the results are compared with their effects on the ciliary beat frequency of chicken embryo tracheas in vitro. The more the transport time is increased by a compound the more the ciliary beat frequency is decreased. Chlorbutol 0.5% increases transport time more and decreases ciliary beat frequency more than benzalkonium chloride 0.006% + EDTA 0.1%. Otrivin 0.1% increases transport time more and decreases ciliary beat frequency more than Rhinoguttae xylometazolini 0.1% (F.N.A.). These results support those obtained with the photo-electric registration device applicated on chicken embryo tracheas and human adenoids as described in earlier publications.
A double-blind crossover study was performed on 33 children with asthma to compare the effectiveness of nebulized solutions of preservative-containing and preservative-free ipratropium bromide. Both solutions produced bronchodilation. No significant differences were found between the two solutions at any time after nebulization in minimum and maximum changes from baseline value or in the areas under the lung function time curves. The presently formulated preservative-containing ipratropium bromide solution was not shown to be inferior to a preservative-free compound.
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A rapid, simple and sensitive method for the determination of lysine (Lys) using sodium 1,2-naphthoquinone-4-sulfonate (NQS) and tetradecyl benzyl dimethyl ammonium chloride (Zeph) is presented in this paper. The method is based on the russety product formed from Lys, NQS and Zeph in a buffer solution of pH 9.60, and the stoichiometric ratio of the product is 1:2:2. Beer's law is obeyed in a range of 0.09-18 microg ml(-1) of Lys at the maximum absorption of 474 nm (epsilon(474) is 8.1 x 10(5)l mol(-1)cm(-1)). The equation of linear regression is A=0.40427+0.06112C, with a linearly correlation coefficient of 0.9972. The limit of detection is 0.07 microg ml(-1), R.S.D. 0.8%, and average recovery rate in a range of 98.9-100.1%. This paper further optimizes the determination of Lys compared with the previous methods, and the reaction mechanism is studied intensively. The proposed method has been successfully applied to the determination of Lys in pharmaceutical and biological samples. The common components as nutritional additives in pharmaceuticals and other compounds in biological samples nearly do not interfere with the proposed method.
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Fifty-two (52) compounds were tested for spermicidal activity by titration against human spermatozoa. The gradual decrease in mean sperm size was measured against increasing concentration of spermicide and the end-point was taken as the point at which all the peripheral cytoplasm had been removed and only the sperm core of nucleus and tail fibres remained. There were 14 compounds that produced this total effect. All were detergents, of various types, and the effect was purely physical. The most potent compounds caused complete stripping at 0.5-50 pmol/cell and most are already used in spermicidal preparations. A further 11 compounds, including sodium hypochlorite and some phenols, caused partial stripping, while 4 compounds caused sperm swelling. The test was not suitable for assessment of metabolic cell poisons.
A series of alkyldimethylbenzylammonium chlorides have been synthesized with n-alkyl chain lengths of C1 leads to C18. Octanol/water partition coefficients were determined and the antimicrobial activity assessed as the minimum growth inhibitory concentrations towards twelve strains of micro-organisms, representative of Gram-negative and Gram-positive bacteria, yeasts and fungi. The data were subjected to a numerical analysis. Antimicrobial activity of the compounds was found to be a parabolic function of their lipophilicity and maximized with n-alkyl chain lengths of between C12 and C16. The data fit to quadratic functions estimated for low (C1-C7) and high (C8-C16) alkyl chain length compounds was better than for a single quadratic describing the activity of the complete series (C1-C18). These maximized at log P values corresponding to alkyl-chain lengths of approximately C7 and C14 respectively, and were suggestive of low and high affinity binding sites upon the cell surface. The data analysis allowed the chain lengths of compounds with optimal activity towards the various groups of organisms to be determined. Generally yeasts and fungi were most sensitive towards C12, Gram-positive bacteria towards C14, and the Gram-negative bacteria towards C16. Gram-negative cells were the most resistant towards all the compounds and Gram-positive cells the least.
A test was developed to assess the surface activity of disinfectants against dried viral preparations. In this preliminary study a variety of disinfectants was tested against herpes virus. The results showed that 2% alkaline glutaraldehyde and 70% ethanol or isopropanol were effective in 1 min. Hypochlorite solutions (2500 ppm av. Cl2) were effective in 5 min, but povidone-iodine (10%) was slower in action and a clear soluble phenol showed uncertain activity at 5 and 10 min. High concentrations of alcohols (above 95%), two quaternary ammonium compounds and 0.5% aqueous chlorhexidine showed little activity in 10 min.