Chloramphenicol solution

FIGURE 3-6 Differential pulse (a) and DC (b) polarograms for a 1.3 x 10 5 M chloramphenicol solution. (Reproduced with permission from reference 7.)... 

A Aguiar, M Weiner. Percutaneous absorption studies of chloramphenicol solutions. J Pharm Sci 58 210, 1969. 

Tryptone (5 g), yeast extract (2.5 g) and NaCl (5 g) were dissolved in distilled water, the volume was adjusted to 500 mL and then autoclaved (20 min, 120 °C). A small portion of this Luria-Bertani (LB) medium (10 mL) was placed into a sterile 100 mL shake flask and ampicillin and chloramphenicol solutions were added (LBamp+cm) to final concentrations of 100 p,g mL and 20 p.g mL respectively. The solution was inoculated with E. coli JM109 pGro7 pJOE4072.6 and shaken overnight at 37 °C and 200 rpm. This overnight culture (2 mL) was used to inoculate 200 mL LBamp+cm in a... 

Chloramphenicol solution (0.5 mM) in distilled water— Sigma catalog C-0378... 

Chloramphenicol solution—Dissolve 16.2 mg of Sigma catalog C-0378 in 100 ml of distilled water. Store at — 20°C in small aliquots. 

Chloramphenicol Solution 0.5% Chloramphenicol (Ivax) Chloromycetin (Monarch)... 

Topical application of chloramphenicol solution or ointment is effective against most bacterial infections of the external eye. However, because aplastic anemia has also occurred after topical ocular use of chloramphenicol, its use must be limited to infections for which less toxic antibiotics prove ineffective. 

Sodium metabisulfite has been used to photostabilize solutions of minoxidil (48) and promethazine hydrochloride (120). Sodium metabisulfite, however, was found to decrease the photostability of chloramphenicol solution (86). 

Table 99 below gives an example of a formulation for a 3% chloramphenicol solution developed on a laboratory scale for application to the eye. 

Skin tests of the immediate type, with 1% chloramphenicol solution as well as Prausnitz-Kiistner tests have been performed, but no positive results were obtained with either method (Korossy et al. 1962). 

Regioselective Acylation of Hydroxy Compounds. AUphatic diols can be selectively acylated at the primary position by a number of Upases in nonaqueous solvents. For example, PPL suspended in solutions of various diols in ethyl carboxylates catalyzes transesterification in a highly regioselective manner, producing primary monoesters in up to 97% yield (93). Similarly, chloramphenicol [56-75-7] (72) (R = NO2) can be acylated by a number of Upases to produce optically pure, water-insoluble 3-0-palmitate in a highly selective manner (94). 

The synthetic route to chloramphenicol is described in U.S. Patent 2,4B3,BB4 as follows 1.1 g of sodium is dissolved in 20 cc of methanol and the resulting solution added to a Solution of 5 g of benzaldehyde and 4.5 g of /3-nitroethanol in 20 cc of methanol. After standing at room temperature for a short time the gel which forms on the mixing of the reactants changes to a white insoluble powder. The precipitate is collected, washed with methanol and ether and then dried. The product thus produced is the sodium salt of... 

Other drugs in combination with a sweetening agent were also studied, dextromethorphan hydrobromide [21], doxycycline hydrochloride [21], erythromycin [23], chloramphenicol [23], ampicillin [23] and cefpodoxime proxetil [23] as bitter drugs and simple syrup (2.5M sucrose solution, used as a flavoring agent prescribed by The Japanese... 

FIG. 28 Correspondence of the lower potential of the first pulse, b,sds in the presence of antibiotics to bitterness scores of aqueous solution containing antibiotics and 1% ethanol in phase wl (O) ampicillin, ( ) er5dhromycin, (A) chloramphenicol, and (V) cefpodoxime proxetil. Phases w2 and o the same as in Fig. 8. (Ref. 23.)... 

Surfactants. The use of surfactants is greatly restricted in formulating ophthalmic solutions. The order of surfactant toxicity is anionic > cationic >> nonionic. Several nonionic surfactants are used in relatively low concentrations to aid in dispersing steroids in suspensions and to achieve or to improve solution clarity. Those principally used are the sorbitan ether esters of oleic acid (Polysorbate or Tween 20 and 80), polymers of oxyethylated octyl phenol (Tyloxapol), and polyoxyl 40 stearate. The lowest concentration possible is used to perform the desired function. Their effect on preservative efficacy and their possible binding by macromolecules must be taken into account, as well as their effect on ocular irritation. The use of surfactants as cosolvents for an ophthalmic solution of chloramphenicol has been described [271]. This com-... 

When drug polymorphs cannot interconvert as a result of being suspended in aqueous solution, a different bioavailability of the two forms usually results [126], For instance, the peak concentration of chloramphenicol in blood serum was found to be roughly proportional to the percentage of the B-polymorph of chloramphenicol palmitate present in a matrix of the A-polymorph [133]. The same concept has been found to apply to hydrate species, where the higher solubility and dissolution rate of the anhydrous phase relative to the trihydrate phase resulted in measurably higher blood levels when using the anhydrate as... 

For the experiment, the dorsal skin of young rats (Wistar or a comparable strain) is shaved and washed with an antibiotic solution (containing, e.g., streptomycin, penicillin, chloramphenicol, and amphotericin in concentrations inhibiting bacterial growth). After skin excision, excess fat is peeled off and the skin is placed over the end of a polytetrafluoroethylene tube with the epidermal side in touch with the hollow cylinder. The skin is fixed with an O-ring and the tube interior is sealed. The side of the dermis is then submersed in a magnesium sulphate solution (154 mM). The samples are applied at 30°C to the epidermal side of the skin in such a way that the skin interface is fully covered. After the incubation time, the substances are removed with prewarmed water the skin surface tension is decreased with ethanol which is subsequently replaced with magnesium sulphate solution (154 mM). 

Benzoic acids substituted with a basic side chain also are also of interest as pro-moieties whose physicochemical properties and rates of enzymatic hydrolysis can readily be modulated. A number of drugs have been converted to prodrugs with this type of pro-moiety, e.g., hydrocortisone, prednisolone, acyclovir, chloramphenicol, and paracetamol [148] [149], These prodrugs appear well suited as parenteral formulations, being water-soluble, stable in slightly acidic solution, and readily hydrolyzed enzymatically. As examples, we consider here the hydrolysis in human plasma of a number of (aminomethyl)ben-zoates of metronidazole (8.109-8.115, Sect. 8.5.5.1, Table 8.9) [138], These prodrugs are very rapidly activated, which may be beneficial for parenteral administration. However, this type of pro-moiety may be cleaved too rapidly after oral administration to be of interest for poorly absorbed drugs. 

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. 

Incompatibilities Do not mix IV minocycline before or during administration with any solutions containing the following Adrenocorticotropic hormone (ACTH), aminophylline, amobarbital sodium, amphotericin B, bicarbonate infusion mixtures, calcium gluconate or chloride, carbenicillin, cephalothin sodium, cefazolin sodium, chloramphenicol succinate, colistin sulfate, heparin sodium, hydrocortisone sodium succinate, iodine sodium, methicillin sodium, novobiocin, penicillin, pentobarbital, phenytoin sodium, polymyxin, prochlorperazine, sodium ascorbate, sulfadiazine, sulfisoxazole, thiopental sodium, vitamin K (sodium bisulfate or sodium salt), whole blood. 

Buffered cellulase solution - transfer 20 g cellulase (also called polysac-charase in the kit) and 0.1 g chloramphenicol to a 2-1 wide-neck conical flask. Add 1 I of acetate buffer solution, shake and incubate for at least 1 h at 40°C. 

Immunoaffinity cleanup was first applied in drug residue analysis for the determination of chloramphenicol in swine muscle tissue by LC (113). The lAC column was prepared using monoclonal antibodies originally developed for an enzyme-linked immunosorbent assay (ELISA) method (171) specific for chloramphenicol. Meat samples were extracted with water, and a concentrated phosphate buffer was added to the filtered extracts before immunoaffinity cleanup. A phosphate buffer was used in the washing process, whereas chloramphenicol was eluted from the column with a glycine/sodium chloride solution of pH 2.8. For subsequent LC analysis, this eluate was extracted with ethyl acetate, evaporated, and reconstimted in the mobile phase. The same analytical scheme was later successfully applied for the determination of chloramphenicol in eggs and milk as well (170, 172). 

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