Moisture sorption by polymeric excipients commonly used in amorphous solid dispersions and its effect on glass transition temperature: III. Methacrylic acid-methyl methacrylate and related copolymers (Eudragit®).

Moisture sorption by polymeric carriers used in amorphous solid dispersion (ASD) plays a critical role in the physical stability of the dispersed drug as it can increase molecular mobility of drug in ASD by decreasing the glass transition temperatures (T) of the drug-polymer system, leading to drug crystallization. The present report describes Part III of a systematic investigation of moisture sorption by different polymers used in ASDs, where the results for four chemically different methacrylic acid-methyl methacrylate and related copolymers, namely, Eudragit® EPO, Eudragit® L100-55, Eudragit® L100, and Eudragit® S100, as the function of relative humidity (RH) are presented. Effects of moisture sorption on T of the polymers were also determined.

Improving drug release rate, drug-polymer miscibility, printability and processability of FDM 3D-printed tablets by weak acid-base interaction.

Slow drug release, low drug-polymer miscibility, poor printability of polymers used, and high processing temperature are major challenges in developing FDM 3D-printed tablets. These challenges were addressed in this investigation by having a model basic drug, haloperidol (mp: 151.5 °C), interact with a weak acid, malic acid (mp: 130 °C), during the melt extrusion of formulations into filaments used for 3D-printing.

Moisture Sorption by Polymeric Excipients Commonly Used in Amorphous Solid Dispersions and its Effect on Glass Transition Temperature: II. Cellulosic Polymers.

Moisture sorption by polymeric carriers used for the development of amorphous solid dispersions (ASDs) plays a critical role in the physical stability of dispersed drugs since moisture may decrease glass transition temperature (T) and thereby increase molecular mobility of drugs leading to their crystallization. To assist the selection of appropriate polymers for ASDs, we conducted moisture sorption by five types of cellulosic polymers, namely, hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), hydroxypropyl methyl cellulose acetate succinate (HPMCAS), hydroxypropyl methyl cellulose phthalate (HPMCP), and ethyl cellulose (EC), as functions of relative humidity (10 to 90% RH) and temperature (25 and 40 °C). The moisture sorption was in the order of HPC>HPMC>HPMCP>HPMCAS>EC, and there was no significant effect of the molecular weights of polymers on moisture uptake.

Moisture sorption by polymeric excipients commonly used in amorphous solid dispersion and its effect on glass transition temperature: I. Polyvinylpyrrolidone and related copolymers.

Moisture plays a critical role in the stability of amorphous solid dispersions (ASD) as it can lower the glass transition temperature (T) and thereby increase molecular mobility resulting in drug crystallization. A systematic study on moisture sorption by four polyvinylpyrrolidone (PVP) having different molecular weights (Kollidon® 12, 17, 30, and 90) and two related copolymers (Kollidon® VA64; Soluplus®) was conducted at 25 and 40 °C as a function of relative humidity to determine effects of absorbed moisture on T and potential stability of ASDs. A VTI dynamic moisture sorption analyzer was used, where experimental conditions were first established such that equilibrium was reached and there was no significant hysteresis loop between sorption and desorption isotherms.

Nortriptyline Hydrochloride Solubility-pH Profiles in a Saline Phosphate Buffer: Drug-Phosphate Complexes and Multiple pH Domains with a Gibbs Phase Rule "Soft" Constraints.

The solubility of a model basic drug, nortriptyline (Nor), was investigated as a function of pH in phosphate and/or a chloride-containing aqueous suspension using experimental practices recommended in the previously published "white paper" (Avdeef et al., 2016). The pH-Ramp Shake-Flask (pH-RSF) method, introduced in our earlier work (Marković et al.

Development of FDM 3D-printed tablets with rapid drug release, high drug-polymer miscibility and reduced printing temperature by applying the acid-base supersolubilization (ABS) principle.

Some of the major issues with the development of FDM 3D printed tablets are slow drug release, lack of drug-polymer miscibility, high processing temperature, and poor printability. In this investigation, these issues were addressed by using a novel physicochemical principle called acid-base supersolubilization (ABS) previously developed in our laboratory. The aqueous solubility of a basic drug, haloperidol, was increased to ~300 mg/g of solution by adding glutaric acid, and, upon drying, the concentrated solutions produced amorphous materials.