Design, development and in-vitro evaluation of diclofenac taste-masked orodispersible tablet formulations.

Context: Fast onset of action is prerequisite for acute pain medication. A palatable orodispersible medicine of diclofenac providing rapid analgesic effect should improve patient compliance and treatment.

Objective: In the present study, diclofenac taste-masked orodispersible tablets (ODTs) with fast release characteristics were developed.

Design of biorelevant test setups for the prediction of diclofenac in vivo features after oral administration.

Purpose: Design of biorelevant test setups mimicking the physiological conditions experienced by drugs after oral administration along the passage through the mouth and the GI tract for the in vitro evaluation of diclofenac exhibiting multiple-peak phenomenon during absorption.

Methods: The biorelevant models simulated successively saliva (SSF, pH 6.2-6.

Development of oral taste masked diclofenac formulations using a taste sensing system.

To achieve patient compliance, organoleptic aspects of drug substances play a key role in the development of oral pharmaceutical preparations. In this study, the ability of an electronic tongue to help in selecting a drug candidate and rationalize the development of oral taste masked formulations was evaluated. As drug, diclofenac, in the form of acid, sodium salt and potassium salt, was used.

Potential use of fluorocarbons in lung surfactant therapy.

Exogenous surfactant therapy based on animal lung extract preparations has been developed successfully for the treatment of neonatal respiratory distress syndrome. However, because of the inherent limitations of these natural preparations, the development of new synthetic surfactants is a major objective. We report here that a perfluorocarbon gas (perfluorooctyl bromide, gPFOB) inhibits the formation of the semi-crystalline domains that occur during compression of a Langmuir monolayer of dipalmitoyl phosphatidylcholine (DPPC), taken as a simplified model of lung surfactant.

Long lived microbubbles for oxygen delivery.

Exceptionally long lived microbubbles containing a fluorocarbon as part of their filling gas have been obtained by using a fluorinated phospholipid instead of a standard phospholipid as shell component. An unexpected, strong synergistic effect between the fluorocarbon gas and the fluorinated phospholipid has been discovered. Such bubbles could be used for in vivo oxygen delivery, ultrasound contrast imaging and drug delivery.

The detrimental effect of serum albumin on the re-spreading of a dipalmitoyl phosphatidylcholine Langmuir monolayer is counteracted by a fluorocarbon gas.

We have recently reported that fluorocarbon gases exhibit an effective fluidizing effect on Langmuir monolayers of dipalmitoyl phosphatidylcholine (DPPC), preventing them from crystallizing up to surface pressures of approximately 40 mN m(-1), i.e. well above the DPPC's equilibrium surface pressure.

Fluidization of a dipalmitoyl phosphatidylcholine monolayer by fluorocarbon gases: potential use in lung surfactant therapy.

Fluorocarbon gases (gFCs) were found to inhibit the liquid-expanded (LE)/liquid-condensed (LC) phase transition of dipalmitoyl phosphatidylcholine (DPPC) Langmuir monolayers. The formation of domains of an LC phase, which typically occurs in the LE/LC coexistence region upon compression of DPPC, is prevented when the atmosphere above the DPPC monolayer is saturated with a gFC. When contacted with gFC, the DPPC monolayer remains in the LE phase for surface pressures lower than 38 mN m(-1), as assessed by compression isotherms and fluorescence microscopy (FM).

Practical aspects of fast reversed-phase high-performance liquid chromatography using 3 microm particle packed columns and monolithic columns in pharmaceutical development and production working under current good manufacturing practice.

The potential and limitations of fast reversed-phase high-performance liquid chromatographic separations for assay and purity of drug substances and drug products were investigated in the pharmaceutical industry working under current good manufacturing practice using particle packed columns and monolithic columns. On particle packed columns, the pressure limitation of commercially available HPLC systems was found to be the limiting factor for fast separations. On 3 microm particle packed columns, HPLC run times (run to run) for assay and purity of pharmaceutical products of 20 min could be achieved.