Chloramphenicol capsules

AJ Aguiar, LM Wheeler, S Fusari, JE Zelmar. Evaluation of physical and pharmaceutical factors involved in drug release and availability from chloramphenicol capsules. J Pharm Sci 57 1844-1850, 1968. 

Khalil, S. A., and Ali, M. M. Some formulation factors affecting disintegration and dissolution of chloramphenicol capsules. Acta. Pharm. Suec. 9 563-572, 1972. 

Fig. 15 Mean plasma levels for groups of ten human subjects receiving single 0.5-g doses (as two 250-mg capsules) of chloramphenicol preparations A, B, C, or D. Vertical lines represent one standard error on either side of the mean. (From Ref. 19.).

Although the feed additive uses of antibiotics have been emphasized, it should be noted that the uses as injectables for therapy, mammary infusions for mastitis, boluses, pills, capsules, medicated blocks, and drinking water formulations include a wider variety of antibiotics than are added to feeds. Many of these are currently used at the discretion of the meat producer or dairyman, others must be used under the direction of a veterinarian. For example, chloramphenicol is an antibiotic which the veterinarian has access to, but which the FDA has indicated should not be used in livestock destined for human consumption, primarily because of the... 

A reduction in particle size results in an increase in the surface area, which facilitates an increase in the dissolution rate and therefore, also, an increase in the rate of absorption. Drugs administered as suspension are generally rapidly absorbed because of the large available surface area of the dispersed solid. For solid dosage forms such as tablets and capsules, decreasing the particle size facilitates dissolution and thus absorption. Figure 6.8 shows the effect of particle size on absorption and resultant blood levels after oral administration of chloramphenicol in rabbits. Peak blood levels occurred much faster with the smaller... 

Pharmacokinetics. For oral use, chloramphenicol is available as the base in capsules to reduce the bitter taste and for i.v. or i.m. use as the succinate ester which is soluble. Chloramphenicol succinate is... 

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. 

Figure 16.6 Increase in the photostability of (A) nifedipine (B) chloramphenicol (C) furo-semide and (D) clonazepam. = capsule shell without curcumin A = capsule shell colored with curcumin.

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