Kollidon® SR: Formulation techniques and drug delivery applications.

Kollidon® SR is one of the recent versatile coprocessed excipients in the formulation of modified-release dosage forms. It is prepared by co-spray drying aqueous dispersions of polyvinylacetate and polyvinylpyrrolidone. This article gives a critical review of the physicochemical attributes and technological properties of Kollidon® SR.

Ethanol-induced dose dumping from sodium alginate matrix tablets: Investigation of the effects of medium viscosity and pH.

In this work, the swelling and disintegration of drug-free sodium alginate (SA) compacts and the release of metformin HCl from SA matrix tablets were investigated in acidic media of different ethanol concentrations (0, 10, 20, and 40 % v/v), pH (1.2 and 4.5) and HPMC K4M concentrations (0-1 % w/v).

Co-spray Drying Drugs with Aqueous Polymer Dispersions (APDs)-a Systematic Review.

Aqueous colloidal dispersions of water-insoluble polymers (APDs) avoid hassles associated with the use of organic solvents and offer processing advantages related to their low viscosity and short processing times. Therefore, they became the main vehicle for pharmaceutical coating of tablets and multiparticulates, a process commonly employed using pan and fluidized-bed machinery. Another interesting although less common processing approach is co-spray drying APDs with drugs in aqueous systems.

Co-Spray Drying of Paracetamol and Propyphenazone with Polymeric Binders for Enabling Compaction and Stability Improvement in a Combination Tablet.

Paracetamol (PCT) and propyphenazone (PRP) are analgesic drugs that are often combined in a single dosage form for enhanced pharmacological action. In this work, PCT and PRP were co-spray dried separately with hydroxypropyl methylcellulose (HPMC) and hydroxypropyl cellulose (HPC) using drug suspensions in polymer solutions as feed liquids. It was thought that because of polymer adherence to the surface of drug particles, the risk of PCT-PRP contact and interaction could be reduced.

siRNA as a Potential Therapy for COVID-19.

Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV2) is a highly contagious virus causing COVID-19 disease that severely impacted the world health, education, and economy systems in 2020. The numbers of infection cases and reported deaths are still increasing with no specific treatment identified yet to halt this pandemic. Currently, several proposed treatments are under preclinical and clinical investigations now, alongside the race to vaccinate as many individuals as possible.

Spray drying of naproxen and naproxen sodium for improved tableting and dissolution - physicochemical characterization and compression performance.

In this work, the tabletability and dissolution of spray-dried forms of naproxen and its sodium salt were compared with those of unprocessed drugs. Solutions of naproxen or naproxen sodium alone or with HPMC (5% w/w of drug content) were spray dried. Scanning electron micrographs showed that naproxen sodium spray-dried particles were spherical, whereas those of naproxen were non-spherical but isodiametric.

Mechanical properties of starch esters at particle and compact level - Comparisons and exploration of the applicability of Hiestand's equation to predict tablet strength.

Hydrophobic starch esters have potential as tablet matrix formers in controlled drug delivery. The mechanical properties of native starch (SN), starch acetate (SA) and starch propionate (SP) were studied at particle and compact level. Particle microhardness and modulus of elasticity were evaluated by nanoindentation.

The use of design of experiments to develop hot melt extrudates for extended release of diclofenac sodium.

The effect of formulation and processing parameters on processability and release from hot-melt extrusion (HME)-based matrices appears to be API and polymer dependent. Accordingly, the aim of this work was to design an extended-release formulation of diclofenac sodium by using HME technique and design of experiment (DoE). The extrudates were prepared using a vertical lab-scale single screw extruder.

Evaluation of Spironolactone Solid Dispersions Prepared by Co-Spray Drying With Soluplus and Polyvinylpyrrolidone and Influence of Tableting on Drug Release.

Solid dispersions of spironolactone with Soluplus and polyvinylpyrrolidone were prepared by spray drying according to a mixture experimental design and evaluated for moisture content, particle size, drug solubility, crystallinity (powder X-ray diffraction and differential scanning calorimetry), and physicochemical interactions (Fourier-transform infrared spectroscopy, Raman). In vitro dissolution was evaluated for the spray dried product itself and after compression into tablets, and prediction models were derived using multiple linear regression analysis. The spray dried products consisted of amorphous drug, indicated by the absence of crystalline powder X-ray diffraction peaks.

Ethanol effect on acid resistance of selected enteric polymers.

The aim of this study was to investigate under in vitro conditions the influence of ethanol on acid resistance of four commercially-available enteric polymers (Acryl-EZE, AQOAT, Hypromellose phthalate, and Sureteric). For this purpose, custom-prepared paracetamol tablets were coated with the enteric polymers and tested for release using the buffer-addition method. Ten different hydro-ethanolic media were used in the acid stage corresponding to five levels of ethanol (0, 5, 10, 20, and 40% v/v) in two acidic solutions representing low and high gastric pH (0.

Optimization of pH-independent chronotherapeutic release of verapamil HCl from three-layer matrix tablets.

The aim of this work was to evaluate and optimize formulation of three-layer matrix tablets based on xanthan gum (XG) and sodium alginate for chronotherapeutic pH-independent release of verapamil HCl (VH). Artificial neural networks (ANN) were applied in the optimization and compared with multiple linear regression (MLR). A face-centered central composite experimental design was employed with three factors (mass fraction of VH in intermediate layer, X1, and of XG in matrix former of intermediate and outer layers, X2 and X3).

Sustained release of diltiazem HCl tableted after co-spray drying and physical mixing with PVAc and PVP.

In this work, aqueous diltiazem HCl and polyvinyl-pyrrolidone (PVP) solutions were mixed with Kollicoat SR 30D and spray dried to microparticles of different drug:excipient ratio and PVP content. Co-spray dried products and physical mixtures of drug, Kollidon SR and PVP were tableted. Spray drying process, co-spray dried products and compressibility/compactability of co-spray dried and physical mixtures, as well as drug release and water uptake of matrix-tablets was evaluated.

Influence of ethanol on swelling and release behaviors of Carbopol(®)-based tablets.

The aim of this work was to investigate the effect of ethanol on the in vitro swelling and release behaviors of Carbopol(®)-based tablets. The swelling behavior of drug-free compacts and the release of model drugs (metformin HCl, caffeine and theophylline) from matrix tablets were evaluated in acidic and buffered media with 0, 20 and 40% (v/v) ethanol. Release data were analyzed by fitting to Higuchi and Peppas models and calculation of similarity factor (f2).

Evaluation of hydrophilic matrix tablets based on Carbopol(®) 971P and low-viscosity sodium alginate for pH-independent controlled drug release.

Background: The aim of this study was to evaluate matrix tablets containing different ratios of Carbopol(®) 971P (CP) to low-viscosity sodium alginate (SA) and assess their suitability for pH-independent controlled drug release.

Methods: Two processing methods (physical mixing, PM and spray-drying, SD) were applied before compaction and the release from corresponding matrices was compared. The release from CP-SA PM matrices was also investigated using three model drugs (paracetamol, salicylic acid, and verapamil HCl) and two dissolution media (0.

Optimization of extended-release hydrophilic matrix tablets by support vector regression.

Background: In this work, support vector regression (SVR) was applied to the optimization of extended release from swellable hydrophilic pentoxifylline matrix-tablets and compared to multiple linear regression (MLR).

Methods: Binary mixtures comprising ethylcellulose and sodium alginate were used as the matrix-former. The matrix-former : drug weight ratio and the percentage of sodium alginate in the matrix-former were the formulation factors (independent variables) and the percentages of drug release at four different time intervals were the responses (dependent variables).

Sustained-release of buspirone HCl by co spray-drying with aqueous polymeric dispersions.

Sustained-release of buspirone HCl (BUH) was attempted by spray drying after dissolving in two commercially available aqueous polymeric dispersions (Eudragit RS 30 D or Kollicoat SR 30 D) at five different drug:polymer ratios (1:1, 1:2, 1:3, 1:6 and 1:9). The produced spray-dried agglomerates were evaluated in terms of their particle size and morphology, production yield, encapsulation efficiency and in-vitro release of BUH. Possible drug-polymer interactions were checked by Differential Scanning Calorimetry (DSC) and FT-IR spectroscopy.