Cephalotin

The structures of the drugs used as a small test set for the model are listed in Table 17.1. Loperamide and asimadoline are P-gp substrates terfenadine and ebastine are compounds that are rapidly metabolized alprazolam, dobazam, di-and mono-hydroxy-L66858 [11] are benzodiazepines testosterone and corticosterone are hormones and cefadroxyl, cefaclor, cephalotin and cefmetazole are cephalosporins [12]. Finally, peptides 1 to 10 are peptidomimetic drugs [13]. 

Cefadroxyl and cefaclor are beta-lactam antibiotics which show high affinity for the PepTl carrier system, whereas the other two beta-lactams, cephalotin and cef-metazole, are not recognized by PepTl protein and are not actively transported in the intestine. However, as the VolSurf Caco-2 model predicts that all the beta-lactams are nonpenetrating compounds, it is very probable that, as they rely only the diffusion mechanism, cefadroxyl and cefaclor will not cross the cell monolayer. 

Other antibiotics still require freeze drying, e. g. Na-Cephalotin (Na-CET). Takeda [ 1.32] showed, that thermal treatment of Na-CET was not sufficient to produce pure crystalline Na-CET, as the amorphous fraction discolors during storage and must be avoided. Takeda described the production of pure crystalline Na-CET by adding microcrystals of Na-CET to a saturated solution of Na-CET. If this mixture was frozen and freeze dried, then no amorphous or quasi-crystalline were found. Koyama et al. [3.35] described, that after thermal treatment for 24 h some parts remained incompletely crystallized. After adding 5 % (w/w) isopropylalcohol, a thermal treatment of 1 h was sufficient. Furthermore, the product could be dried at a higher pressure. Thus the drying time could be reduced and 100 % of the product could be used. 

Pedersen-Bjergaard J. Cephalotin in the treatment of penicillin-sensitive patients. Acta Allergol 1967 22 299. 

Klastersky J, Hensgens C, Debusscher I. Empiric therapy for cancer patients comparative study of ticarcillin-tobramycin, ticarcillin-cephalothin, and cephalotin-tobramycin. Antimicrob Agents Chemother 1975 7 640-645. 

Sodasone - Prednisolone phosphate sodium Sodelut G Medroxyprogesterone acetate Sodium Cephalotin - Cephalothin sodium Sodiuretic Bendroflumethiazide Sofalead Diphenidol Sofarin - Diclofenac sodium Sofmin Methotrimeprazine Sofro - Pemoline Solacen -Tybamate Solacil Proxazole citrate Solantal - Tiaramide Solantyi - Phenytoin Solaquin - Hydroquinone Solaskil Levamisole HCi I Solatene - /3-Carotene Solatran Ketazolam Solaxin - Chlorzoxazone Solazine - Trifluoperazine Solbrine - Dimenhydrinate Solcillin-C - Cloxacillin Solco H Hydroxocobalamin Soldactone - Canremoate potassium... 

Erbeldinger M, Ni X, HaUing PJ (1998) Effect of water and enzyme concentration on thennolysin-catalyzed solid-to-sohd peptide synthesis. Biotechnol Bioeng 59(l) 68-72 Fernandez-Lafuente R, Alvaro G, Blanco RM et al. (1991) EquUibrium controlled synthesis of cephalotin in water-cosolvent systems by stabiDzed peniciUin acylase. Appl Biochem Biotechnol 27 277-289... 

Hematological disorders induced by the cephalosporins have been reported but the incidence of hemolytic anemia in no way parallels the occurrence of positive Coombs tests. Hemolytic anemia has been reported after cephalotin (Molthan 1969 Gralnick et al. 1972), cephalexin (Ford 1967 Forbes et al. 1972), and ce-phaloridine (Kaplan and Weinstein 1967) therapy. Thrombocytopenia (Sheiman et al. 1968 Gralnick et al. 1972) and granulocytopenia (Davis et al. 1964 Levin et al. 1971 Silber and Dioknoa 1973 Dicato and Ellmann 1975) have also been reported. 

Schneider CH, de Week AL (1981) Allergy towards )S-lactam antibiotics. In Mitsuhashi S (ed) Beta-lactam antibiotics, JSSP. Springer, Berlin Heidelberg New York, p 299 Schneider CH, de Week AL, Stauble E (1971) Carboxy-methylcellulose. Additives in penicillins and the elicitation of anaphylactic reactions. Experientia 27 167 Schneider CH, Pfeuti C, de Week AL (1973) Aspects of formation of the D-penicillamine antigenic determinant from penicilloyl compounds. Helv Chim Acta 56 1235 Schneierson SS, Perlman E, Shore B (1964) Cephalotin antigenicity and cross-reactivity with penicillin G. Clin Med 71 1933... 

FIGURE 14. Structures of beta-lactam antibiotics examples. A benzyl penicillin sodium. B carbenicillin. C cephalotin. 

Fig. 1 A, Effect of changing isopropanol volume fraction in the mobile phase on the elution profiles of cefonicid (1), cefaclor (2), cephazoUn (3), cefodizime (4), cephaloridine (5), cephamandole (6), and cephalotin (7), using a mobile phase of 0.1 M acetate buffer (pH 5.00)/isopropanol (v/v) a = (96.5/3.5), b = (95/5), c = (93/7), and d = (90/10) at a column temperature of 30°C. B, Effect of column temperature on the elution profiles of cephalosporins studied [numbering as in (A)], using a mobile phase of 0.1 M acetate buffer (pH 5.00)/isopropanol (95/5) (v/v). C, Isocratic elution profile under optimal conditions. Mobile phase 0.1 Af acetate buffer (pH 5.00)/isopro-panol (95.4/4.6) (v/v), column temperature, 32 C, numbering as in (A).

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