Chloramphenicol sodium succinate

The antibiotic is administered orally as the palmitate, which is tasteless this is hydrolysed to chloramphenicol in the gastrointestinal tract. The highly water-soluble chloramphenicol sodium succinate is used in the parenteral formulation, and thus acts as a pro-drug. 

F. Shann, M. Linnemann, A. Mackenzie, J. Barker, M. Gratten, and N. Crinis, Absorption of chloramphenicol sodium succinate after intramusclar administration in children, N. Engl. J. Med., 313, 410... 

CHLORAMPHENICOL SODIUM SUCCINATE STERILE USP 1 GRAM VIAL 1Q/BOX 6505007540280 BX 37,33 ... 

IV administration Chloramphenicol sodium succinate is intended for IV use only it is ineffective when given IM. Administer IV as a 10% solution injected over at least 1 minute. Substitute oral dosage as soon as feasible. 

Burke, J. T., W. A. Virgin, R. J. Sherertz, K. L. Sanders, M. R. Blum, and F. A. Sarubbi. 1982. Pharmacokinetics of intravenous chloramphenicol sodium succinate in adult patients with normal renal and hepatic function. J. Pharmacokin. Biopharrrl0 601-614. 

Glazko, A. J., W. A. Dill, A. W Kinkel, J. R. Goulet, W. J. Holloway, and R. A. Buchanan. 1977. Absorption and excretion of parenteral doses of chloramphenicol sodium succinate (CMS) in comparison with peroral doses of chloramphenicol (CM Iin. Pharmacol. Thei21 104. 

Prochlorperazine Edisylate Prochlorperazine edisylate is not compatible with sodium chloride solutions containing methyl hydroxybenzoate and propyl hydroxy-benzoate as preservatives, but is compatible with solutions containing benzyl alcohol. Prochlorperazine edisylate salts are incompatible with a number of drugs such as aminophylline, amphotericin, ampicillin sodium, some barbiturates, ben-zylpenicillin salts, calcium gluconate, cefmetazole sodium, cephalothin sodium, chloramphenicol sodium succinate, chlorothiazide sodium, chloramphenicol, morphine sulfate containing phenol, magnesium trisilicate mixture, sodium succinate, chlorothiazide sodium, dimenhydrinate, heparin sodium, hydrocortisone sodium succinate, midazolam hydrochloride, and some sulfonamides.166... 

Prodrugs can be used to increase or decrease the aqueous solubility, mask bitterness, increase lipophili-city, improve absorption, decrease local side effects, and alter membrane permeability of the parent molecule. For example, chloramphenicol has an aqueous solubility of 2.5mg/ml, but chloramphenicol sodium succinate, a prodrug, has an aqueous solubility of lOOmg/ml. Hydantoins also possess low aqueous solu-bilites that result in low and variable availability and precipitation following injection. In an effort to increase the aqueous solubility of phenytoin, Stella et prepared the ethyl and triethylamine esters... 

A water-soluble formulation of chloramphenicol sodium succinate is available for i.v. use. Chloramphenicol succinate is hydrolyzed to chloramphenicol in the liver. Chloramphenicol palmitate is an insoluble ester suitable for p.o. administration. Chloramphenicol palmitate is hydrolyzed to chloramphenicol in the gastrointestinal tract. Chloramphenicol (generic and veterinary labeled) is also available in a variety of tablet and capsule strengths. A long-acting formulation of florfenicol is approved for i.m. and s.c. administration to cattle. This formulation contains three carriers... 

Because it is bitter, this antibiotic is administered orally cither in capsules or as the palmitatc e.ster. Chloramphenicol palmitate is insoluble in water and may be suspended in aqueous vehicles for liquid dosage forms. The ester forms by reaction with the hydroxyl group on C-3. In the alimentary tract, it is hydrolyzed slowly to the active antibiotic. Chloramphenicol is administered parenterally as an aqueous suspensiuti of very fine cry.stals or as a solution of the sodium salt of the succinate ester of chloramphenicol. Sterile chloramphenicol sodium succinate has been used to prepare aqueous. solutions for intravenous injection. 

Chloramphenicol sodium succinate. 361 Chlorcyclizinc hydrochloride. 706. 707 Chlordia/cpoxide hydrochloride. 489. 490 Chlorhcxidinc gluconate. 225-227 Chlorinated pesticides, drug metabolism and. 131... 

Carboxylic half-esters (e.g. hemisuccinates) of phenols are easily hydrolyzed in aqueous solution and are therefore not recommended for the solubilization of phenolic compounds. Even hemisuccinates of alcohols suffer somewhat from stability problems and must be supplied as lyophi-lized (freeze-dried) powders for reconstitution in water and used within 48 h (see, for example, the monographies chloramphenicol sodium succinate or hydrocortisone sodium succinate in The Handbook on Injectable Drugs,see also Anderson et... 

On the other hand, formation of a prodrug such as a phosphate ester may increase hydrophilicity, thus enhancing solubility. For example, the solubility and dissolution rate of the 77-hydroxymethyl derivative of lomefloxacin is higher than those of the parent compound, and it can be converted readily back to the original molecule. Commonly used prodrugs are procaine penicillin metronidazole phosphate and chloramphenicol sodium succinate. 

Chloramphenicol sodium succinate (Fig. 8.24) is an ester that contains an anionic group that can be formulated as the sodium salt. Salts are water soluble and can therefore be formulated as a solution for parenteral administration, such as in eye drops. Plasma esterases release the parent drug once it is in the systemic circulation. 

Chloramphenicol sodium succinate Figure 8.24 Chloramphenicol ester prodrugs. 

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