04. October 2018
The aim of this work was to develop an ascending controlled-release pellet (ACRP) of paliperidone to improve poor solubility and provide a stable blood drug concentration. The inner core was produced by mixing different ratios of sodium chloride as an osmotic substance and microcrystalline cellulose (MCC) to offer a pressure drive when in contact with medium. After, the drug layer was processed by a liquid-layering method, with paliperidone ground to a nano-size in order to improve the...
04. October 2018
Praziquantel is an antiparasitic drug used for decades. Currently, the praziquantel commercial preparation is a racemic mixture, inwhich only the levo-enantiomer possesses anthelmintic activity. The knowledge of its properties in the solid state and other chemical-physical properties is necessary for improving its efficacy andapplications. Drug solid dispersions were prepared with calcium carbonate at 1:5 drug to excipient weight ratio by solventevaporation method. Then, the modification of the...
04. October 2018
n recent years there has been a growing interest in solid lipid-based systems, particularly in solid lipid microparticles (SLMs); however, only very few studies deeply investigated the dissolution behaviour of orally delivered-SLMs. The present study provides new insights about the release performance in different gastrointestinal fluids of SLMs containing a freely water soluble drug (caffeine, as BCS class I drug). Three different formulations of SLMs were prepared by spray congealing using...
02. October 2018
The production of 3D-printed drugs holds promise for future personalized medicine. Here, we prepared tablets containing naftopidil as a model drug using a semi-solid extrusion-type 3D bioprinter applicable for tissue engineering. A hydrogel is typically used as the printer ink for 3D bioprinters, and we incorporated various amounts of hydroxypropyl methylcellulose hydrogel (30%, 40% and 50% gel) into the printer ink. The resulting 3D-printed gel product was dried to obtain tablets. The...
02. October 2018
The formulation of amorphous solid dispersions (ASDs) is an effective way to improve the bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). The combination of an amorphous state of the drug and the presence of crystallization-inhibiting polymers retains a high amount of dissolved API over time. ASDs with ketoconazole and different polymers were manufactured by spray drying and their characteristics as well as performance were analyzed. Dissolution tests with a...
01. October 2018
The occurrence of protein aggregation during bioprocessing steps such as purification, formulation and fill-finish, impacts yield and production costs, and must be controlled throughout themanufacturing process. Understanding aggregation mechanisms and developing mitigating strategies are imperative to ensure the clinical efficacy of the protein drug product and to reduce costs. Thiscommentary reflects on recent progress made in the field of monoclonal antibody (mAb) aggregation with...
01. October 2018
In this study, a set of 24 experiments was designed to understand the combined effect of different process parameters, i.e. material feed rate, liquid-to-solid (L/S) ratio, screw speed, and screw configuration on the residence time distribution, granule morphology, and particle size distribution in twin screw wet granulation of microcrystalline cellulose. It was shown that residence times were longer at higher L/S and lower screw speeds. However, the most dominant effect on mean residence time...
01. October 2018
The controlled release of caffeine from the casein gel tablets has been achieved over release periods lasting from a few minutes to over a few days. A novel casein gel has been acidified at pH of 1.0 as the insoluble controlled-release matrix and spray-dried with coffee for microencapsulation. The optimal inlet temperature of spray drying for the casein-coffee mixtures has been found to be 150 °C. The elastic casein-coffee tablets have been engineered without denaturing the components (as...
30. September 2018
Partition coefficient (log P) is a key physicochemical characteristic of lipophilic drugs which plays a significant role in formulation development for oral administration. Lipid-based formulation strategies can increase lymphatic transport of these drugs and can enhance bioavailability many folds. The number of lipophilic drugs in pharmacopoeias and under discovery are continuously increasing and making the job of the formulation scientist difficult to develop suitable formulation of these...
29. September 2018
Appropriate lubrication is important in tablet manufacturing as it lowers punch sticking propensity and protects tooling by reducing friction between die wall and tablet during tablet manufacturing. Most commercial lubricants negatively impact tabletability and dissolution. A delicate balance is usually attained by trial and error to identify the optimal level of lubricant in a tablet formulation. In this work, we have evaluated the effectiveness of sodium lauryl sulfate (SLS), a surfactant, as...