Drugs online research references
J Pharm Sci. 1975 May;64(5):869-72.
Oral absorption efficiency of acid-labile antibiotics from lipid-drug delivery systems.
Patel SP, Jarowski CI.
The utility of cholesterol, cholesteryl acetate, and beta-sitosterol in protecting and improving the oral absorption efficiency of acid-labile antibiotics is discussed. The potassium salts of penicillin G and penicillin V and erythromycin lactobionate were studied. The stability of the two penicillins in simulated gastric fluid was determined iodometrically. The rank order of acid protective activity was: cholesteryl acetate greater than beta-sitosterol greater than cholesterol. Oral administration of erythromycin lactobionate coated with cholesteryl acetate produced a twofold increase in human urinary excretion of erythromycin when compared with the uncoated material. Potassium salts of penicillin G and penicillin V coated with cholesteryl acetate yielded 1.6- and 2-fold higher urine levels, respectively, as compared with the uncoated candidates.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=807706&dopt=Abstract
J Med Chem. 1975 May;18(5):486-90.
Preparation and properties of 5-phenylphenoxymethylpenicillin.
Vanderhaeghe H, Thomis J.
Cycloaddition of azidoacetyl chloride to benzyl D-5,5-dimethyl-5-phenyl-2-thiazoline-4-carboxylate (1a) gave 5-phenyl-6alpha-azidopenicillanate (2a). By catalytic reduction of 2a and reaction with phenoxyacetyl chloride, 5-phenyl-6-epiphenoxymethylpenicillin benzyl ester (4a) was obtained. Oxidation of 4a gave the sulfoxide 6, which was isomerized in the presence of DBN. The sulfoxide 7 with the normal configuration could be isolated but deoxygenation of the sulfoxide was not successful. Isomerization of 4a with DBN, either with or without silylation of the side chain, gave a mixture from which 5-phenylphenoxymethylpenicillin benzyl ester (5) was isolated. Compound 5 was debenzylated to 5-phenylphenoxymethylpenicillin potassium salt (8). The antibacterial activity of 8 was low, whereas the 6-epimer 9 was inactive. Contary to published information, the 5-phenylpenam derivative 4c could be prepared by the same method.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=807731&dopt=Abstract
MMW Munch Med Wochenschr. 1975 Sep 5;117(36):1405-8.
[Penicillin V potassium in tonsillar tissue and serum (author's transl)]
[Article in German]
Backmann H, Drees H, Geisen D, Mundnich K, Ritzerfeld W.
1.2 mega U Penicillin V potassium was given to 20 patients 2 hours (group 1) and another 19 patients 3 hours (group 2) before tonsillectomy. After the operation biological determinations of the levels of active principle were made from tonsillar tissue and serum with statistical evaluation of the results (Spearman's rank correlation). There was a significant connection between the serum and tonsillar tissue concentrations (in children and adults) in both groups. The level of the active principle in group 2 was only slightly lower than in group 1. Many of the micro-organisms responsible for tonsillitis can be influenced by the concentrations found here, so that application of Penicillin V can often be expected to have a good therapeutic effect.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=809683&dopt=Abstract
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