Info

Chlorhexidine digluconate

>700

a Lauryl sulfate ester of erythromycin propionate

derived from the base in solution decreases with time as the drug is converted to the hydrochloride. At pH 1.6 the rate of solution of the two forms is identical, and at pH 2.1 the hydrochloride has a higher solubility owing to its effect on local pH around the dissolving particles.

Erythromycin (XX) is labile at pH values below pH 4, and hence is unstable in the stomach contents. Erythromycin stearate (the salt of the tertiary aliphatic amine and stearic acid), being less soluble, is not as susceptible to degradation. The salt dissociates in the intestine to yield the free base, which is absorbed. There are differences in the absorption behaviour of the erythromycin salts and differences in toxicity, which may be related to their aqueous solubilities. Erythromycin ethylsuccinate was originally developed for paediatric use because its low water solubility and relative tastelessness were suited to paedi-atric formulations. The soluble lactobionate is used in intravenous infusions.

5.7.3 Drug solubility and biological activity

There should be a broad correlation between aqueous solubility and indices of biological activity. On the one hand, as drug solubility in aqueous media is inversely related to the

Structure XX Erythromycin
0 0

Post a comment