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Biomedical subjects

A Kamada

Publications and source records attributed to A Kamada.

At least 73 records · Page 4Linked to original sources

Possible mechanism of uptake for several compounds in ionized form through human erythrocyte membrane.

The mechanism underlying uptake of certain compounds in ionized form across human red blood cell membrane was examined. The ionized forms of salicylate, 5-methoxy-salicylate and phenylalanylphenylalanine were significantly taken up into the interior space of human red blood cells instead of remaining in the membrane. Inhibition of the uptake of these compounds by 4,4'-diisothiocyano-2,2'-disulfonate stilbene and phlorizin indicates that their permeation of the erythrocyte membrane may involve the membrane protein fraction. Chelation at the protein site does not appear to occur. Instead, an amino group in the protein structure may mediate the transport of these ionized compounds.

Absorption↗

Salicylate-promoted permeation of cefoxitin, insulin and phenylalanine across red cell membrane. Possible mechanism.

Uptake of sodium cefoxitin, D-phenylalanine and insulin into human red blood cells was significantly enhanced by the presence of salicylate and 5-methoxysalicylate in the medium. The mechanism of adjuvant action appeared to depend on an affinity between the adjuvant and the protein fraction in the erythrocyte membrane. The inhibitory effect of DIDS and phlorizin on the salicylate-enhanced uptake of these compounds strongly suggests that the ability of salicylate to permeate the membrane may be essential for it to act as an adjuvant.

4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid↗

Enhanced intestinal absorption of amino acids and amino acid-like drug by possible formation of enamine in administered solution by the presence of ethylacetoacetate.

Ethylacetoacetate promoted the colonic and the jejunal absorption of amino acids such as L-phenylalanine and D-phenylalanine when administered in aqueous solution. Enhanced absorption of these isomers of amino acid might occur via a formation of enamine, which was observed in aqueous solution by monitoring ultraviolet absorbance at 288 nm. Since mixture of L- or D-phenylalanine and ethylacetoacetate in aqueous solution enhanced colonic absorption of cefmetazole while the solution did not affect so much on the jejunal absorption of cefmetazole compared to the colonic absorption of it, enhancing action of enamine probably produced in aqueous solution may be more effective at the colonic compartment.

Acetoacetates↗

The effects of the administration routes on the biliary excretion of antibiotics.

The effects of the administration routes on the biliary excretion of gentamicin and cefazolin were investigated in male white rabbits. The administration routes studied were intravenous, intramuscular injection and injection into portal vein. In both antibiotics, total excretion into bile was the highest when drug was administered by the injection into portal vein. In case of gentamicin, the bile level above MIC (against P.aeruginosa) could be obtained only by the administration into portal vein. These results indicate that the administration into portal vein is useful clinically, for the drug delivery to biliary tract, especially in drugs like aminoglycoside antibiotics which have an extremely low rate of transfer to the bile.

Animals↗

Effect of adjuvants on the rectal absorption and lymphatic uptake of pepleomycin in rats.

The rectal absorption of pepleomycin sulfate (PEPS) in rats was increased significantly by the coadministration with each of diclofenac (DC), sodium 5-methoxysalicylate (5-MSA) and phenylalanine enamine of ethylacetoacetate (Enamine). 5-MSA increased the lymphatic uptake of PEPS after rectal administration while DC and Enamine did not. The mechanism behind the enhancing action of 5-MSA on the lymphatic uptake of PEPS may be due to the suppressing action of 5-MSA on the vascular permeability to PEPS. DC increased the vascular permeability to PEPS but Enamine did not affect it. Findings obtained in this study may indicate that adjuvant used acts independently at the rectal mucosal membrane and at the vascular membrane for membrane for membrane permeability to PEPS.

Adjuvants, Pharmaceutic↗

Study of the mechanism behind adjuvant action of diethylethoxymethylene malonate enhancing the rectal absorption of cefmetazole and lysozyme.

Diethylethoxymethylene malonate (DEEMM) and diethyl maleate (DEM) enhanced the rectal absorption of cefmetazole in rats when studies were carried out using in vivo, in situ rectal loop and in vitro rectal everted sac method. Since an increase of cefmetazole transport was found when concentration of nonprotein sulfhydryls in rectal tissue was decreased by the presence of either DEEMM or DEM in the study using in vitro everted sac method and the enhancement of cefmetazole absorption by the coadministration of either DEEMM or DEM was suppressed by the treatment with dimercaprol, membrane permeability of rectal tissue seems to be regulated by the concentration of nonprotein sulfhydryls in rectal tissue. On the other hand, it was also found that there were differences between the action of DEEMM and the action of DEM from the following two results: 1) enhancing action of DEEMM was suppressed by the presence of calcium ion in microenema while action of DEM was not so much influenced, and 2) DEEMM enhanced the rectal absorption of lysozyme in rabbits but DEM did not.

Adjuvants, Pharmaceutic↗

Adjuvant effects of glyceryl esters of acetoacetic acid on rectal absorption of insulin and inulin in rabbits.

The promoting effect of glyceryl esters of acetoacetic acid on the rectal absorption of insulin and inulin was studied. A decrease in the serum glucose level was observed in rabbits following the administration of an insulin suppository containing glyceryl-1,3-diacetoacetate (adjuvant II) or 1,2-isopropylideneglycerine-3-acetoacetate (adjuvant IV). The promoting effects of adjuvants II and IV on the rectal absorption of insulin and inulin were suppressed by the addition of calcium and magnesium to the suppository. This indicates that adjuvant interaction with the calcium and magnesium ion located in the rectal membrane is involved in the enhanced absorption of insulin and inulin. Adjuvant release from the suppository formulation in addition to adjuvant lipid solubility were found to be other important factors for enhanced absorption of insulin and inulin.

Acetoacetates↗

Effect of enamine derivatives on the rectal absorption of insulin in dogs and rabbits.

Enamine derivatives resulting from the reaction between ethyl acetoacetate and amino acids were found to promote rectal absorption of insulin in normal rabbits, with the enamine of sodium DL-phenylalanate being the most effective adjuvant tested. Results of glucose tolerance tests in fasted alloxan diabetic rabbits showed that after oral administration of glucose, insulin suppositories containing enamines derived from either sodium phenylalanine or leucine were able to lower the serum glucose level to within the normal range for more than 2.5 h. The absorption-promoting effect of the sodium DL-phenylalanate enamine on rectal absorption of insulin in dogs was studied in two different formulations, gelatin microenema and suppository. The gelatin microenema containing the insulin solution caused a greater increase in the plasma insulin level than that obtained after administration of an insulin suppository.

Adjuvants, Pharmaceutic↗

Enhancement of rectal absorption of insulin using salicylates in dogs.

Sodium salicylate and 5-methoxysalicylate both increased the rectal absorption of insulin in dogs when co-administered with insulin in various formulations. Microenema formulations containing 4% gelatin showed the highest insulin bioavailability of the formulations studied whereas microenemas (without gelatin) and suppository formulations were not as effective in enhancing the rectal absorption of insulin.

Animals↗