NucleationCrystal growth dispersion Thermodynamic a b s t r a c t In recent years, engineering the total morphology of pharmaceutical materials particles to desirable shape, size and surface area has long been actively increased because it has many advantages especially for improving physicochemical properties of Active Pharmaceutical Ingredients (APIs). This article therefore considers the potential utility of crystal engineering as a tool for controlling and designing properties of pharmaceutical solid particles in purpose to developing efficacious performance of solid dosage form, fundamentals of crystallization process, applications. In addition, understanding the relationship between molecular recognition, thermodynamic, and kinetics which controls the crystallization process so that it benefits in designing successful experiments to have desirable crystal habit for materials.
Taste masking of paracetamol was achieved by preparing amorphous solid dispersion (ASD) using modified coacervation method. The method is based on dissolving the drug and polymeric carrier in water adjusted to certain pH level. Then, precipitation of ASD granules is performed by gradually changing pH level. Therefore, the chosen drug and polymer should obtain appropriate acidic or basic groups to enable pH-dependent solvation. Moreover, using solubility enhancing additives such as sodium lauryl sulphate (SLS) and low viscosity polyethylene glycol (PEG 400) found to be essential in aiding drug/polymer aqueous solvation which enhanced amorphization, hence taste masking and drug loading. Solid dispersion between Paracetamol and Eudragit E was formed and that proved by FT-IR, DSC, PXRD and SEM. Also, Paracetamol was released after 2 min in 0.1 N hydrochloric acid medium and the taste of masking forms are accepted from all volunteers. Modified coacervation method does not involve organic solvents, high temperatures, or sophisticated instruments commonly used in taste masking methods. Using PEG 400 resulted in significantly higher drug loading and dissolution rate compared to SLS granules. Moreover, using previously reported scoring system for the evaluation of taste masking methods shows that pH dependent coacervation obtained high scoring over common methods and thus display a robust potential for industrial applications.
Self-nanoemulsifying drug delivery systems (SNEDDS) were used to enhance the dissolution rate of furosemide as a model for class IV drugs and the system was solidified into liquisolid tablets. SNEDDS of furosemide contained 10% Castor oil, 60% Cremophor EL, and 30% PEG 400. The mean droplets size was 17.9 ± 4.5 nm. The theoretical model was used to calculate the amounts of the carrier (Avicel PH101) and coating materials (Aerosil 200) to prepare liquisolid powder. Carrier/coating materials ratio of 5/1 was used and Ludipress was added to the solid system, thus tablets with hardness of 45 ± 2 N were obtained. Liquisolid tablets showed 2-folds increase in drug release as compared to the generic tablets after 60 min in HCl 0.1 N using USP apparatus-II. Furosemide loaded SNEDDS tablets have great prospects for further in vivo studies, and the theoretical model is useful for calculating the adequate amounts of adsorbents required to solidify these systems.
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