Composition optimization and stability testing of a parenteral antifungal solution based on a ternary solvent system.

An intravenous solution is a dosage forms intended for administration into the bloodstream. This route is the most rapid and the most bioavailable method of getting drugs into systemic circulation, and therefore it is also the most liable to cause adverse effects. In order to reduce the possibility of side effects and to ensure adequate clinical dosage of the formulation, the primarily formulated composition should be optimized.

[Difficulties encountered during formulation of a parenteral dosage form containing a poorly soluble drug].

Poor water solubility and consequently the difficulties in formulating a liquid dosage form is a great concern in pharmaceutical development. The importance of this issue is underlined by the fact that 10-30% of marketed drugs and 60-70% of drugs coming from early development stage have solubility problems. In this paper we summarize the existing solubility enhancing techniques that are applicable in parenteral dosage forms for overcoming the issue.

Aqueous solvent system for the solubilization of azole compounds.

Azoles have a wide spectrum antimycotic activity, but due to some derivatives exhibiting poor water solubility their parenteral administration is limited. The influence of solubilizers on the aqueous solubility of the itraconazole, ketoconazole and miconazole was investigated in order to enhance their solubility for a possible parenteral dosage form. The solubilizer effect of acetate, phosphate and gluconate solutions were studied, along with ethanol, glycerol, macrogol 400, propylene glycol and surfactants, such as polysorbate 20, 60, 80 and sodium taurocholeate.

[Formulation of advancing products of pulmonary medicine absorption].

The author introduces the various possibilities of the production of medical aerosols ensuring pulmonary absorption. He also mentions the method of selecting the auxiliary materials formulated with propellants, and describes the characteristics of norfluran Dymel 134 and apafluran HFC 227. In the experimental section, he handles the development of an anxiolitic byciclo-heptane-type aerosol, for which the aim was to develop a homogeneous liquid-phase aerosol.

[Transdermal therapeutic systems].

Transdermal therapeutic systems (TTS) gain continuously increasing importance in therapy due to their advantageous properties. They assure constant concentration of the active substance in the blood, a lower amount of the drug compared to the orally administered dose is sufficient, side effects decrease, and the therapy is painless. Since the appearance of the first products many TTSs have been developed containing a wide variety of active substances including hormonal, antihypertensive, antianginal, and analgesic plasters.