The release of some substituted benzoic acids from micellar solutions of polysorbate 20.
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Benzoates↗
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The influence of micellar concentrations of polysorbate 20 on the in vivo absorption of some substituted benzoic acids.
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Absorption↗
[A comparative clinical assessment of the efficacy of polysorb and gelevin in the local treatment of suppurative wounds].
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Adult↗
[Alternatives for closure of the rectal "stump" in Hartmann's operation. A comparative experimental study which includes the resorbable mechanical suture (polysorb)].
Five different kinds of sutures which can be used for closure of the rectal stump in Hartmann's operation are evaluated in the same animal. They are compared at six different phases of the cicatrization process: 7-30-45-60-90 and 150 days. In the analysis, the degree of complete cicatrization is considered as well as the thickness of the cicatriced tissue, and other factors such as persistence of suture material and the result of it. All of the sutures involved accomplished the goal of a good joint of the planes of intestinal suture. Although, two of them, the metal stapler and Polyglactin (Vicryl) in extramucosal surgery fulfill almost in an ideal way the goals concerning security, rare reaction to suture material, and consequently less thickness in the cicatriced tissue (2 x 2 and 1 x 1 mm respectively) as well as complete cicatrization in ninety days. Stapler is performed quicker and in a more aseptic way, but the scar resulting from Polyglactin is smaller. In separate extramucosal points, silk produces a more important tissue reaction with a thicker scar (3 x 3 mm) coming to an end in 150 days. "Albert Lembert" type suture is really far away from being a good mean because it creates an important tissue reaction with a thick scar (3 x 3 mm), with late consolidation (150 days) and granulomatous reaction. Resorbable stapler--Polisorb--has a considerable volume and it causes an important tissue reaction which determines a very thick (4.5 x 4.5 mm) and "unfinished" scar within 150 days; really far away for practical use.
Absorption↗
Efficacy of inactivators against 14 disinfectant substances.
More than 24 inactivators were tested for their suitability against 14 disinfectant substances by a quantitative suspension test. Even simple inactivators were found to be efficace: 0.1% cysteine and 0.5% sodium thiosulfate for mercuric chloride and the iodophor; 0.1% sodium sulfite for these two substances and for the QAC in the lower concentration; 1.0% polysorbate 80 for hexylresorcinol, o-phenylphenol and the QAC in the lower concentration; 0.5% sodium thioglycolate for mercuric chloride, the iodophor and chloramine-T. The inactivator active against most disinfectants was the combination LPHT or 0.3% lecithin / 3.0% polysorbate 80 /0.1% histidine / 0.5% sodium thiosulfate. Also active were: LPWT (0.5% lecithin / 1.0% polysorbate 80 /1.0% Lubrol W / 1.0% sodium thiosulfate), LPT (2.0% lecithin / 2.0% polysorbate 80 / 0.5% sodium thiosulfate) and PS (3.0% polysorbate 80 / 3.0% saponin).
Disinfectants↗
Growth, survival, antigenic stability, and virulence of Leptospira interrogans serotype canicola.
Leptospira interrogans serotype canicola (strain NADL A-13) grew from inocula as small as two cells in liquid polysorbate 80 medium (P-80 medium, in P-60, P-40 and P-20 media, and in P-80 medium from which polysorbate, NH4C1 or thiamine had been omitted. It grew well initially in vitamin B12-deleted P-80 medium, but only with inocula as large as 26 x 10(4) cells per ml. P-80 medium lacking both polysorbate and NH4Cl supported light growth from small inocula, but the omission of thiamine and vitamin B12 in addition seriously affected the properties of the medium. Where readily detectable growth did not develop in liquid nutrient-deleted medium, viable ortanisms could often be demonstrated indirectly by subculture to semisolid medium, and their occurrence was influenced by the presence of albumin, thiamine, and vitamin B12. Growth on semisolid media was comparable with that in liquid media of similar composition. The absence of polysorbate 80, thiamine, or vitamin B12 prevented the appearance of Dinger's zones of growth from small inocula. Antigenic composition as measured by microscopic agglutination tests with homologous and heterologous antisera was not appreciably affected by repeated subculturing in various complete and incomplete media. Homogenates of infected-hamster-kidney tissue in bovine serum-albumin diluent still contained viable organisms after 60 days' storage at 23-25 degrees C. Organisms derived from this material after 3 and 16 days' storage showed no loss of virulence. Organisms grown in artificial culture showed no loss of virulence after storage in bovine albumin diluent or phosphate buffer for 7 days at 23-25 degrees C. Cultures of the organism survived without loss of virulence for 15 months in 13 semisolid media of differing complexity. Single colonies derived from five different solid media were grown in semisolid forms of the parent media and stored at 23-25 degrees C for 10 months without loss of virulence.
Animals↗
Pharmacokinetics of parenteral 13-cis-retinoic acid formulations in rats.
The pharmacokinetics of three 13-cis-retinoic acid formulations were studied after intraperitoneal (ip) administration to rats. Rats were given ip injections of 2.5 mg of 13-cis-retinoic acid per 360 g of body weight; the drug was administered as an alkaline solution, suspended in corn oil, or as a mixture with polysorbate 80. The alkaline solution was also given intravenously (iv) via the tail vein as a control. The mean elimination rate constant, calculated from data from iv administration, was 0.72 +/- 0.088 h-1 (r = 0.988). The peak concentration in plasma and the time to reach this maximum were 14 mg/L and 0.5 h, 22 mg/L and 2 h, and 10 mg/L and 1 h for the drug administered as an alkaline solution, suspended in corn oil, and as a mixture with polysorbate 80, respectively. The areas under the concentration-time curve (concentration in plasma versus time) were 34.9 +/- 8.78 mg.h/L for the iv dose and 34.1 +/- 9.97, 62.4 +/- 32.3, and 25.9 +/- 12.0 mg.h/L for the ip doses of alkaline solution, suspension in oil, and mixture with polysorbate 80, respectively. Because of the rapid increase of concentration in plasma, which is identical to that of the iv profile, and the ease of its handling and preparation, the ip administered alkaline solution is the preferable formulation.
Animals↗
Solubilization and dissolution properties of a leukotriene-D4 antagonist in micellar solutions.
7-[3-(4-Acetyl-3-hydroxy-2-propylphenoxy)propoxy]-3,4-dihydro-8- propyl-2H-1-benzopyran-2-propionic acid (1) is a leukotriene-D4 antagonist that is quite insoluble in aqueous media. Increased solubilization of 1 was achieved in micellar solutions of polysorbate 80, sodium glycocholate, sodium taurocholate, lysolecithin, and sodium taurocholate plus monoolein. The intrinsic dissolution rate of 1 was measured in the presence and absence of polysorbate 80 at pH 7.0, 8.0, and 10.0. In all the micellar solutions tested, the solubility of 1 was significantly increased. The intrinsic dissolution rate of this compound was also enhanced in micellar solutions of polysorbate 80 and with increasing values of pH. However, the magnitudes of the enhancement of the intrinsic dissolution rate were much less than expected from the enhancement of aqueous solubility.
Benzopyrans↗
Development of an agar-diffusion method for the assay of quaternary ammonium germicides.
Five quaternary ammonium germicides (QAGs) were tested for their adsorption by agar. This was found to be in the following ascending order: alkylbenzylmethyl-ammonium chloride, alkyltrimethylammonium bromide, cetyltrimethylammonium bromide, cetylpyrimidinium chloride and cetylbenzyldimethylammonium chloride. An inverse relationship was established between the extent of agar binding of the QAGs and their inhibition zones. In an attempt to develop a sensitive cup-plate assaying technique suitable for QAGs, important factors affecting the agar-diffusion of QAGs were investigated. These included the influence of various polysorbates, buffer ions, agars and test organisms. Furthermore, the effect of the pH and/or the concentration of the selected polysorbate and the buffer were studied. The best medium developed for the sensitive agar-diffusion assay of QAGs was nutrient agar-Tris (0.05 M, pH 8) provided that distilled water and polysorbate 20 (0.5%) were used as diluents for the mixed alkyl and the pure cetyl QAGs, respectively.
Adsorption↗
Effects of lipids on bioavailability of sulfisoxazole acetyl, dicumarol, and griseofulvin in rats.
The effects of hexadecane, oleyl alcohol, polysorbate 80, trioctanoin, and triolein on the bioavailability of sulfisoxazole N1-acetyl, dicumarol, and griseofulvin were investigated. Compared to administration of the drugs in water, the rate of absorption of the drugs was either decreased or not changed by the lipids. The extent of absorption of sulfisoxazole acetyl and dicumarol was significantly increased by polysorbate 80 and triolein and not affected by hexadecane or oleyl alcohol. Tricotanoin increased the extent of abosrption of sulfisoxazole acetyl but had no effect on the absorption of dicumarol. Compared to the aqueous vehicle, the extent of absorption of greiseofulvin was decreased by hexadecane, oleyl alcohol, and triolein, increased by polysorbate 80, and not affected by trioctanoin. The extent of absorption of sulfisoxazole acetyl was not affected by the amount of triolein in which it was administered nor by emulsification of triolein prior to administration.
Animals↗
Effects of bis(2-ethylhexyl) phthalate on chromosomes of human leukocytes and human fetal lung cells.
Blood from two male and two female donors was exposed at 37degrees for 4 hr to concentrations of 60.0, 6.0, 0.6, and 0.06 mug of a widely used plasticizer, bis (2-ethylhexyl) phthalate, per milliliter of blood. The bis(2-ethylhexyl) phthalate was solubilized with polysorbate 80. Appropriate polysorbate and nonpolysorbate controls also were established. Following the 4 hr of incubation, phytohemagglutinin was added and tissue cultures were established. In addition, human fetal lung cells were exposed in tissue culture to a medium containing 6.0 mug/ml of bis(2-ethylhexyl) phthalate in polysorbate 80 for 5 days. Similar controls also were established for these experiments. Analysis of chromosome preparations from all cultures obtained failed to show any increased evidence of isochromatid and chromatid breaks or gaps or abnormal forms at any studied concentration when compared to the control cultures. In addition, analysis of fetal lung cell preparations for aneuploidy failed to reveal any differences between cells from study and control cultures. This study involved a short-term exposure to bis(2-ethylhexyl) phthalate in various concentrations which did not cause damage in leukocytes or fetal lung cells.
Cells, Cultured↗
Non-ionic surfactants and membrane transport of thioridazine in goldfish.
Polysorbate 80, which has been widely used in studies of the effects of surfactants on drug absorption, increases the rate of absorption of some drugs at concentrations near its critical micelle concentration (cmc). To determine whether all non-ionic surfactants were capable of inducing this effect, the effects of six commercial non-ionic surfactants on thioridazine absorption in goldfish have been compared with the effect of polysorbate 80. The reciprocal death time (T-1) determined when the fish were immersed in the solution under study was the index of absoprtion rate used. Not all surfactants tested increased T-1. Cremophor EL (polyoxyethylated castor oil), Atlas G1295 (a polyoxyethylene fatty glyceride), Atlas G1300 (a polyoxyethylene glyceride ester) had no effect below their cmc's. Those surfactants that did increase T-1 [polysorbate 80 (a polyoxyethylene lanolin derivative), G2162 (a polyoxyethylene oxypropylene monosterate) and Renex 650 (a polyoxyethylene alkyl aryl ether)] display the concentration-dependent behaviour reported previously - a decrease in absorption rate when the surfactant concentration is increased above its cmc. The factor determining whether or not the surfactant will increas absorption rate appears to be the configuration of the surfactant molecule rather than its hydrophile-lipophile balance or its surface activity.
Animals↗
Griseofulvin---phenobarbital interaction: a formulation-dependent phenomenon.
The reported interaction of griseofulvin with phenobarbital was studied in the rat following oral administration of different dosage forms. A single oral dose of 15 mg of phenobarbital/kg 24 hr prior to the oral administration of a suspension of 100 mg og griseofulvin/kg in 0.5% polysorbate 80 significantly reduced plasma griseofulvin levels. An increase in the concentration of polysorbate 80 to 2% reduced the extent of the interaction from 50 to 32%. Phenobarbital did not influence plasma griseofulvin levels when griseofulvin was given in either 70% polyethylene glycol 300 (suspensions of 20 or 100 mg/kg) or 100% polyethylene glycol 600 (solution of 50 mg/kg). It is concluded that the observed interaction is formulation dependent and is a result of diminished dissolution and, consequently, reduced absorption of griseofulvin.
Animals↗
Some relations between dissolution rates and physical parameters of a drug in aqueous micellar solutions of a non-ionic surfactant.
Dissolution rates of salicylic acid from a constant surface area into a series of aqueous micellar polysorbate 20 solutions at pH 1-0 to 4-0 have been measured using two different methods; a stirred beaker and a rotating disc technique. The micellar molecular weight of polysorbate 20 has been obtained from light scattering and differential refractometry data and used with other independently determined physical data to calculate diffusion coefficients of the diffusing species. Linear multiple regression analysis was used to assess the dependence of drug dissolution rate on the diffusion coefficient and the viscosity of the dissolution medium.
Colloids↗
Physiological effects of sucrose substitutes and artificial sweeteners on growth pattern and acid production of glucose-grown Streptococcus mutans strains in vitro.
The synergistic effects of four sucrose substitutes, polysorbate and five artificial sweeteners were studied in vitro on growth pattern and acid production of seven glucose-grown Streptococcus mutans strains, representing the five serological groups after Bratthall. Four distinct growth patterns during glucose fermentation were observed: high rate of growth with low acid production, moderate growth rate with moderate acid production, moderate growth rate with high acid production, and slow rate of growth with moderate acid production. Depending on the strain used, the final OD at 546 nm ranged from 0.55 to 0.99 and the final pH of the medium varied between 4.65 and 4.15. While added sucrose substitutes, with exceptions, usually enhanced growth rate, most artificial sweeteners suppressed or, at higher concentrations, even inhibited growth of S. mutans; addition of polysorbate to the medium always increased growth rate of S. mutans significantly. The presence of sucrose substitutes during glucose fermentation had no effect on final pH of the medium, but addition of artificial sweeteners, especially sodium saccharin, elevated final pH up to 1.8 units. The observed physiological patterns and differences within the several strains of S. mutans during glucose fermentation in vitro do not necessarily relate to the five serological groups of the species.
Fructose↗
Succinylsulfathiazole crystal forms. III: Crystal growth studies.
Crystal growth accompanying the transformation of succinylsulfathiazole crystal forms in aqueous suspensions was studied using a projecting microscope. The effects of increase of temperature, agitation, inclusion of seeds of Form II (the water-stable dihydrate), sulfathiazole, methylcellulose, and polysorbate 80 on the particle-size distribution of anhydrous succinylsulfathiazole Form I were examined. Rates of crystal growth, calculated as increase of diameter per unit time, were given under different experimental conditions. Increase of temperature, agitation, and seeding with nuclei of Form II had significant growth-accelerating effects. Sulfathiazole and polysorbate 80 had growth-retarding effects. Methylcellulose inhibited the crystal growth of Form I for over a year. Aqueous suspensions of Form II did not show any change in particle-size distribution. The crystal growth was shown to be a direct consequence of the transformation of the crystal form. Physical conditions and additives which had accelerating or retarding effects on the rate of succinylsulfathiazole in aqueous suspensions.
Chemical Phenomena↗
Simultaneous solubilization of steroid hormones II: androgens and estrogens.
The simultaneous solubilization of some androgens and estrogens in aqueous polysorbate 40, tetradecyltrimethylammonium bromide, and sodium lauryl sulfate was studied. The solubilizations of estradiol and testosterone were independent of each other in all three association colloids. However, if the estrogen component was ethinyl estradiol, the solubilization was dependent on the addition order. The estrogen precipitates more readily than testosterone in polysorbate 40 and tetradecyltrimethylammonium bromide, but the opposite is true in sodium lauryl sulfate. The simultaneous solubilizations of methyltestosterone or ethisterone with the estrogens tested were different from those of testosterone. The solubilization behavior of the steroids is discussed, starting with the pseudophase model and different solubilization loci. Results indicated that the free energy change of micellar binding, delta Gb, decreases with increased steroid polarity. The simultaneous solubilization cannot be predicted by delta Gb but may be explained by differences in the solubilization mechanism.
Androgens↗
Bactericidal activity of 40 potential disinfectant inactivators.
Forty commonly used inactivators, both simple substances and mixtures, were tested by a quantitative suspension test for the property of being non-toxic to the bacterial cell. Some inactivators proved to be too inhibitory, even for undamaged organisms, namely cysteine in concentrations of 1.0% and higher, 0.3% and 2.0% lecithin (both especially for P. aeruginosa), and the mixtures 0.3% lecithin/2.0% polysorbate 80/0.1% histidine/2.0% turkey-oil red (for St. aureus) and 0.3% lecithin/3.0% polysorbate 80/0.4% sodium laurylsulfate (for both test organisms).
Bacteriolysis↗