KINETICS STUDY ON KETOPROFEN RELEASE FROM MINI TABLETS AND MULTI-COMPARTMENT SYSTEMS.

Thanks to multi-compartment systems it is possible to modify drug release. Two types of mini tablets containing 12.5 mg of ketoprofen were made: mini tablets of immediate (IR) and sustained (SR) release. Some of the tablets of immediate release were coated with an enteric coating, thereby obtaining a delayed release effect (IRc). For each tablet type, release profiles were tested in three media: 0.1 M HCl, phosphate buffer pH 4.5 and phosphate buffer pH 6.8. Based on the obtained results, three appropriate multi-compartment models have been constructed and tested. The factor limiting the amount of available ketoprofen at the absorption place is pH of the environment. It was observed that the increase in pH caused the increase of ketoprofen solubility. Constructed multi-compartment systems allowed to change the composition and the dose of medicinal substances easily. Thanks to this it is possible to adjust the release profile of the active substance to the individual patient, which meets the expectations of personalized medicine.

The effect of conjugated linoleic acids (CLA) supplementation on the activity of enzymes participating in the formation of arachidonic acid in liver microsomes of rats--probable mechanism of CLA anticancer activity.

The aim of the present research was to examine the effect of conjugated linoleic acids (CLA) supplementation on the activity of enzymes that take part in the synthesis of arachidonic acid (AA) and also to investigate the relation between their activity and the neoplastic process. The enzyme activities were established indirectly, because their measure was the amount of AA formed in vitro, being developed from linoleic acid as determined in liver microsomes of Spraque-Dawley rats. In addition, the indices of Δ6-desaturase (D6D) and Δ5-desaturase (D5D) were determined. To this aim, the method of high per-formance liquid chromatography with UV/VIS detection was used. Between the examined groups, statistically significant differences were observed in the activities of enzymes as well as D6D. The carcinogenic agent applied (DMBA) was found to significantly increase the activity of the examined enzymes. Negative correlation was found between the activities of desaturases and CLA supplementation, whereas the activity of those enzymes was a little higher in the group of rats with chemically induced cancer process. The neoplastic process has a stimulating effect on the activity of D6D. The decrease of D6D activity, resulting from the presence of CLA in the animals' diet, may confirm the anticancer properties of these isomers.

Bovine corneal epithelial primary cultures as an in vitro model for ophthalmic drugs studies.

In the recent years a significant development of investigations with regard to bioavailability of ocular drugs has been noticed. The corneal epithelial barrier is the main pathway for ocular penetration of topically applied ophthalmic drugs into the anterior chamber. To work out an in vitro model of bovine corneal epithelial primary cultures and exercise it for permeability research with lipophilic and hydrophilic markers, permeability coefficients estimation of the 6-carboxyfluorescein and rhodamin B was made. The corneal epithelial cultures of the 3th or 4th passage were chosen for layered culture with inserts based on the liquid-liquid interface (for the first week) and the air-liquid interface (for the two following weeks). On the 7th, 12th, 18th, 21st experiment day TER values, and on the 21st day drug permeability coefficients, were determined. The mean TER values of the 7th, 12th, 18th, 21st day of corneal epithelial culture were: 122.14, 155.14, 198.43 and; 247.43 Wcm2, respectively. The mean values of permeability coefficients on the 21st day of culture for 6-carboxyfluorescein and rhodamin B were 3.87 +/-0.10 x 10(-6)cm/s and 3.65 +/- 0.06 x 10(-6)cm/s, respectively. We state that the in vitro bovine corneal epithelial primary culture model is useful for ocular studies.