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.

[Nebulized drug aerosol systems].

To ensure the pulmonary absorption of medicines a developing technologist may choose from among several alternative possibilities. In the medical practice sprays made by mechanical spraying are of great importance. In this study depositions of fine mists made by OMRON ultrasonic nebulizer in Kirk Model apparatus were investigated.

[Comparative studies on freeze dryers of one and two chamber systems].

Authors carried out a comparative study on freeze--dryers of one--and two chamber-systems. Samples containing dextran and mannitol were used for the control of process-uniformity. Moisture content of the products were monitored during the sublimation process and after closing the ampules by colouring of the CoCl2 labelled samples.

[Drug technology of a parenteral preparation for trimethoprim monotherapy].

The formulation of Trimetoprim (TBP) injection has been studied. Use of N-N'-dimethylacetamide in nonaqueous medium, propylene glycol, N-beta-hydroxyethyl-lactamide-propylene glycol and Macrogol--400 resulted in the preparation of the solution in appropriate concentration. In the presence of adequate quantity of ascorbic acid the TBP is soluble in 0.

[Instrumentation and evaluation of the pharmacopoeia test of color].

Instrumental investigation of colorimetric matching fluids of the Hungarian Pharmacopoeia has been carried out. It has been established that by means of the internationally accepted CIELAB parameters the samples can be well characterized and comparative tests can be precisely accomplished.

[Absorption and distribution of 1-(2,5-dichlorophenoxy)-3-tert-butylaminopropen-2-ol in aerosols].

The absorption and distribution of the slightly water-soluble, carbon-14-labelled 1-(2,5-dichlorophenoxy)-3-tert-butylaminopropen-2-ol hydrochloride (1) from sprays and suspension aerosols have been studied in mice. It was found that the blood level and the organ concentrations achieved with suspension aerosols were higher than those obtained with sprays.

[Absorption and distribution of benzyloxyamine-containing aerosols (author's transl)].

The study of the blood levels and tissue concentrations in mice to which 14C-benzyloxyamine hydrochloride was applied in the form of a spray and of a suspensoid aerosol evidenced the good abosrption of this pharmacon. Maximum blood levels were observed 0.5 hour after administration of the spray.