Marisa Dal Zotto

Possibilities of conveying a cationic drug in Carbomer hydrogels.

A drug with cationic characteristics such as procaine can be conveyed in a Carbomer hydrogel in two different ways: (i) in the form of salt in solution in the aqueous phase, and (ii) in the base form salified with the same polymer. Introduction of the drug into the hydrogel with different concentrations of polymer produced, in both cases, a reduction in viscosity in relation to drug concentration. The gels with procaine salified with the polymer showed greater viscosity. The drug release rate, in general, diminished with the increase in polymer concentration. Nevertheless, when this concentration was maintained, there was no variation in release rate when the viscosity produced as a consequence of drug concentration was changed. Gels with procaine salified with the carboxyvinylic polymer had a faster release rate than those with procaine in the hydrochloride form dissolved in the aqueous phase. These results have also been confirmed by a simulated absorption test.

Layered excipient suppositories: The possibility of modulating drug availability

The release rate of a drug dose from suppositories is affected by characteristics of the excipient (melting temperature and rate, viscosity at rectal temperature, hydro-lipophilic characteristics). Release kinetics from excipients commonly available do not always respond to clinical requirements, even after the introduction of auxiliary agents. Release curves which were differentiated and adaptable to therapeutic conditions were obtained by vehicling a drug in suppositories of two superimposed layers of lipophilic excipients with different characteristics and hence with a difference in drug availability. The two distinct excipient layers release the drug from these suppositories contemporaneously but independently. The amount of drug released in the time course is the sum of the single amounts individually released by the two suppository layers. By previously mixing the two excipients, release rate becomes uniform in the suppository body overall and is conditioned only by the assumed characteristics of the mixture. The release mechanism for superimposed layer suppositories is confirmed by the good agreement between experimental and calculated curves. By using a pair of excipients with different characteristics in superimposed layers between which the drug is distributed, it is possible to modulate drug release kinetics by regulating the reciprocal ratio between the two suppository fractions.

Effects of Silicium Dioxide on Drug Release from Suppositories

AbstractSilica gel is frequently introduced into lipophilic excipients for suppositories as a viscosity agent, to prevent drug sedimentation in the melted mass, and to decrease release rate. The effect of silica gel (Aerosil 200) concentration on the availability of some drugs frequently used in suppositories in different unitary doses was studied. When silica gel concentration in the excipient was increased, a decrease in aminophylline and aminophenazone release rate was observed. Paracetamol in small unitary doses has shown a tendency to increase release rate at higher silica gel concentrations. This behavior was even more evident in suppositories containing promethazine hydrochloride, while for those containing benzydamine hydrochloride the increase in release rate with increasing silica gel concentration was evident for all drug doses. However, the behavior was a consequence of the trend of suppository viscosity during drug release. As a consequence of both the drug and silica gel being discharged, th...