Justyna Kołodziejska

Diclofenac in the treatment of pain in patients with rheumatic diseases

Diclofenac, a phenylacetic acid derivative, is a drug demonstrating high efficacy after oral administration in the treatment of pain and physical disability in rheumatic diseases. In view of the adverse effects associated with using diclofenac, it is necessary to consider all known drug safety information before the drug is selected for therapy and the dosage regimen is set for individual patients. Selecting an oral dosage form with specific properties determined by excipients is a method to improve the availability of the drug substance and, at the same time, minimize adverse drug reactions. An alternative to tablet or capsule dosage forms is diclofenac application to the skin. The proven efficacy of this method is further improved through the use of transdermal penetration enhancers and vehicle ingredients which provide dosage forms with specific physical properties.

The use of the Gelot emulsifier in diclofenac sodium semi-solid preparations

Abstract In topical formulations, the rheological parameters and pharmaceutical availability of many active agents have been improved by the addition of modern excipients. This translates into increased interest in the topical use of NSAIDs. The aim of this study was to create series of effective oil in water (O/W) diclofenac sodium cream formulations that differ in the applied fatty phase, utilizing Gelot TM64 (Gattefosse) (a modern non-ionic emulsifier). In the produced prescriptions, estimation was made of the effect of this on the rheological parameters and the pharmaceutical availability of the diclofenac sodium. Herein, the hydrophilic petrolatum-based cream demonstrated the highest rate of release of the active agent, as well as the best set of beneficial rheological parameters.

The influence of the viscosity of the ointment vehicles magisterial topical preparations, on the speed transfer of biologically active substances

Abstract The aim of this study was to analyze the morphological parameters (viscosity, viscous elasticity and the rate of volatile component loss) of salicylic and boric acid-containing magisterial formulae (ointments). Moreover, the effects of these parameters on the diffusion rate of a therapeutic agent (salicylic acid) to an in vitro external compartment were analyzed. Finally, the applicatory properties of the ointments prepared by way of a conventional technique (in a mortar) and with the aid of an unguator, were compared. The rheological parameters of the analyzed ointments suggest that the preparations made with an aid of an unguator, irrespective of the physicochemical characteristics of their vehicles, are characterized by higher values of diffusion coefficient (D). In addition, conventionally-prepared formulae containing salicylic were shown to be characterized by better viscous elasticity. Surprisingly, irrespective of the preparation technique, the ointments based on an absorptive vehicle (containing lanolin) were characterized by similar viscous elasticity. The rate of volatile (water) component loss from ointments containing a 3% solution of boric acid suggests that such formulae lose no more than 2.3% of their mass when exposed at 37℃. Therefore, the viscosity of such ointments applied onto a patient’s skin should remain relatively stable.

Teat tablet with sodium ibuprofen: the effect of sorbitol on therapeutic agent pharmaceutical availability and on physicochemical parameters of a drug form

Dosing pediatric drugs available on pharmaceutical markets of analgesic, antifebrile and anti-inflammatory activity to children up to 3 years of age is not precise and frequently causes problems. The aim of the study was to work out a pediatric teat form of a drug with sodium ibuprofen and to determine the effect of sorbitol content on pharmaceutical availability of the therapeutic agent. Three variants of tablets containing 50 mg of sodium ibuprofen differing in the percentage content of sorbitol (from 37% - batch I to 79% - batch III) were produced. Quality tests of the produced forms of drugs (PPVI) were performed and the tests of therapeutic agent pharmaceutical availability by spatula method and by a method with a teat. Tablets of all batches had a smooth surface and same shape. The content of the therapeutic agent was within the limit of 95-105% of the declared value. The highest value of Q coefficient in the release test by pharmacopeal method and the shortest disintegration time (12 minutes) were obtained for tablets with 79% content of sorbitol. In conclusion, teat tablets with sodium ibuprofen of the highest sorbitol content (79%) demonstrated the expected physicochemical parameters and high pharmaceutical availability.