Kollicoat IR Research Articles

Development of Taste Masked Fast Disintegrating Films of Levocetirizine Dihydrochloride for Oral Use

Fast disintegrating films of levocetirizine dihydrochloride useful for the treatment of acute allergic rhinitis and chronic urticaria have been developed by using the taste masking ability of cyclodextrins. The fast disintegrating films were prepared by solvent casting method. The films contained water-soluble polymers such as Kollicoat IR or pullulan, aspartame and sucralose as sweeteners and pre-gelatinized starch as disintegrant. Levocetirizine dihydrochloride was incorporated into these films by in-situ complex formation with hydroxy propyl beta-cyclodextrin. The optimized films were evaluated for weight variation, film thickness, folding endurance, tackiness, tensile strength, assay, content uniformity, in vitro disintegration and dissolution, in vivo disintegration and taste masking ability by human gustatory sensation test. Results revealed that the organoleptic properties of levocetirizine dihydrochloride were improved by complexation with hydroxy propyl beta-cyclodextrin and the complex could be successfully formulated into a fast disintegrating film.

Effects of Kollicoat IR® and hydroxypropyl-β-cyclodextrin on the dissolution rate of omeprazole from its microparticles and enteric-coated capsules

Omeprazole microparticles were prepared by different drying techniques using Kollicoat IR® and hydroxypropyl-β-cyclodextrin hydrophilic polymers. Physico-chemical properties were investigated using differential scanning calorimetry and powder X-ray diffractometry. Dissolution rate was determined and compared to the physical mixtures and the morphology was studied using a scanning electron microscope. Omeprazole transformed from the crystalline state to the amorphous state as confirmed by the disappearance of its melting peak and the characteristic of the crystalline peaks. Omeprazole dissolution rate was enhanced significantly from its spray- and freeze-dried microparticles as compared to the corresponding physical mixtures and drug alone (P < 0.05). F3 and F5 formula possessed superior release rate over other formulations. In acidic medium, the release of drug from enteric-coated capsules was not detectable, while it is completely released within 40 min after changing dissolution medium to phosphate buffer (pH 7.4). The transformation of OME from crystalline to amorphous state by using either Kollicoat IR® or hydroxylpropyl-β-cyclodextrin is considered a promising way to improvement of drug dissolution.

Spray drying from complex solvent systems broadens the applicability of Kollicoat IR as a carrier in the formulation of solid dispersions

The presented study aims to explore the feasibility of preparing solid dispersions of the poorly soluble drug, itraconazole, with Kollicoat IR via spray drying, in order to broaden the application window of the polymer. In order to circumvent the need for a common solvent, Kollicoat IR was dissolved in a 50/50 (v/v) water/ethanol mixture and itraconazole was dissolved in a 50/50 (v/v) dichloromethane/ethanol mixture. In a first approach these two solutions were simultaneously spray dried via a spray nozzle with two inlets. In a second approach the two solutions were mixed prior to spray drying and the metastable solution was spray dried via a spray nozzle with a single inlet. This approach was also varied by adding HCl to the water phase of the Kollicoat IR solution. The resulting solid dispersions were characterized with MDSC, XRPD and their dissolution was followed in SGF. The results of the three data sets show that as the mixing between itraconazole and Kollicoat IR improves, the dissolution improves as well. Using the first approach, no mixing was observed between polymer and drug. The second approach on the other hand led to a reasonable degree of mixing as the solid dispersions were XRPD amorphous and no glassy mesofase of itraconazole was observed.

Improvement of dissolution rate of ibuprofen by solid dispersion systems with Kollicoat IR using a pulse combustion dryer system

We prepared solid dispersions (SDs) of ibuprofen (IBU) with Kollicoat IR as the carrier using a newly developed pulse combustion dryer system-Hypulcon. We investigated the physicochemical properties of the prepared SDs by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), and Fourier Transform IR spectroscopy (FT-IR). The results showed that the dissolution property of IBU in SDs was markedly enhanced. The dissolution test showed that after 5 min of dissolution, the concentration of IBU in 1:10 SD with Kollicoat IR as the carrier was 23.05 μg/mL, corresponding to 37.8-fold higher than that of pure IBU. The dissolution rate of IBU in SDs was 1:10 SD 49.7-fold higher than that of pure IBU. It can therefore be said that the pulse combustion dryer system is effective for preparing SDs of IBU with Kollicoat IR, a new carrier.

Prediction of Tablet Film-coating Thickness Using a Rotating Plate Coating System and NIR Spectroscopy

The purpose of this research was to create a calibration model based on near-infrared (NIR) spectroscopy data obtained during a small-scale coating process to predict in-line the coating layer thickness of tablets coated in a side-vented drum coater. The developed setup for the small-scale coating process consisted of a rotating plate with 20 tablets molds that pass a spraying unit, a heating unit, and an in-line NIR spectroscopy probe during one rotation. High-density polyethylene (HDPE) was compressed to flat-faced tablets, and these were coated with a sustained release coating suspension containing Kollicoat IR and Kollicoat SR 30D. The film thickness of these tablets was determined for each tablet individually with a digital micrometer. A calibration model of predicted film thickness versus real-film thickness using PLS regression was developed. This model was tested against in-line NIR data obtained from a coating drum process, in which biconvex HDPE tablets were film-coated with the same film-coating suspension. The model predicted a final coating thickness of 240 mum, while the measured average thickness (n = 100 tablets) was 210 mum. Taking into account the use of a different setup and differently shaped tablets, it was possible to predict the coating thickness with accuracy comparable to the one of the digital micrometer. Thus, the small-scale rotating plate system was found to be an efficient means of preparing calibration model for a tablet-coating drum process.

The use of a new hydrophilic polymer, Kollicoat IR ®, in the formulation of solid dispersions of Itraconazole

Kollicoat IR ®, a new pharmaceutical excipient developed as a coating polymer for instant release tablets, was evaluated as a carrier in solid dispersions of Itraconazole. The solid dispersions were prepared by hot stage extrusion. Modulated temperature differential scanning calorimetry and X-ray powder diffraction were used to evaluate the miscibility of the drug and the carrier. The pharmaceutical performance was evaluated by dissolution experiments, performed in simulated gastric fluid without pepsin (SGF sp). In the X-ray diffractograms no Itraconazole peaks were visible; the polymer on the other hand appeared to be semi-crystalline. Moreover, its crystallinity increased during the extrusion process due to exposure to heat and shear forces. Modulated temperature differential scanning calorimetry analysis showed that the drug and the polymer formed a two phase system. Separate clusters of glassy Itraconazole were present for drug loads of 40% or higher, indicating further phase separation. Dissolution measurements demonstrated a significantly increased dissolution rate for the solid dispersions compared to physical mixtures. Interestingly the physical mixture made up of glassy Itraconazole and Kollicoat IR ® (20/80, w/w) showed a dissolution rate and maximum that was much higher than that of the physical mixture made up of crystalline Itraconazole and that of pure glassy Itraconazole. The results of this study show that Kollicoat IR ® is a promising excipient for the formulation of solid dispersions of Itraconazole prepared by hot stage extrusion.