The Score Card Approach: A First Step Toward an Evidence-based Differentiation Assessment for Tablets.

Background: The differentiation of tablets by their physical appearance is a contributing factor to the safe use of medications. In this study, a "score card" was developed to assess how well one tablet is differentiated from another tablet on the basis of the physical attributes of color, size, and shape.

Methods: The score card was derived from a "2-out-of-5" difference test, in which participants were presented with groups of 5 tablets with varying color, size, and shape, and were asked to identify the 2 tablets that were different from the other 3 tablets.

Development of Tablet Formulation of Amorphous Solid Dispersions Prepared by Hot Melt Extrusion Using Quality by Design Approach.

The objective of the study was to identify the extragranular component requirements (level and type of excipients) to develop an immediate release tablet of solid dispersions prepared by hot melt extrusion (HME) process using commonly used HME polymers. Solid dispersions of compound X were prepared using polyvinyl pyrrolidone co-vinyl acetate 64 (PVP VA64), Soluplus, and hypromellose acetate succinate (HPMCAS-LF) polymers in 1:2 ratio by HME through 18 mm extruder. A mixture design was employed to study effect of type of polymer, filler (microcrystalline cellulose (MCC), lactose, and dicalcium phosphate anhydrous (DCPA)), and disintegrant (Crospovidone, croscarmellose sodium, and sodium starch glycolate (SSG)) as well as level of extrudates, filler, and disintegrant on tablet properties such as disintegration time (DT), tensile strength (TS), compactibility, and dissolution.

Hot Melt Extrusion: Development of an Amorphous Solid Dispersion for an Insoluble Drug from Mini-scale to Clinical Scale.

The objective of the study was to develop an amorphous solid dispersion (ASD) for an insoluble compound X by hot melt extrusion (HME) process. The focus was to identify material-sparing approaches to develop bioavailable and stable ASD including scale up of HME process using minimal drug. Mixtures of compound X and polymers with and without surfactants or pH modifiers were evaluated by hot stage microscopy (HSM), polarized light microscopy (PLM), and modulated differential scanning calorimetry (mDSC), which enabled systematic selection of ASD components.

Characterization and performance assessment of solid dispersions prepared by hot melt extrusion and spray drying process.

The present study investigated effect of manufacturing methods such as hot melt extrusion (HME) and spray drying (SD) on physicochemical properties, manufacturability, physical stability and product performance of solid dispersion. Solid dispersions of compound X and PVP VA64 (1:2) when prepared by SD and HME process were amorphous by polarized light microscopy, powder X-ray diffractometry, and modulated differential scanning calorimetry analyses with a single glass transition temperature. Fourier transform infrared (FT-IR) and Raman spectroscopic analyses revealed similar molecular level interactions between compound X and PVP VA64 as evident by overlapping FT-IR and FT Raman spectra in SD and HME solid dispersions.

Effects of lipophilic components on the compatibility of lipid-based formulations with hard gelatin capsules.

The present study investigated the effect of lipophilic components on the compatibility of propylene glycol (PG)-containing lipid-based drug delivery system (LBDDS) formulations with hard gelatin capsules. The presence of a lipophilic active pharmaceutical ingredient (API) (log P approximately 6.1) and an additional lipophilic excipient (Capmul MCM) significantly affected the activity of PG in the fills and the equilibrium of PG between capsule shells and fills.

Drug-excipient complexation in lipid based delivery systems: an investigation of the Tipranavir-1,3-dioctanolyglycerol complex.

This report describes the solubility properties of a poorly soluble drug-excipient complex in a lipid based formulation. Tipranavir (TPV) was used as the model drug and 1,3-dioctanoylglycerol (DOG) as the excipient. The TPV-DOG complex was prepared by dissolving TPV and DOG in ethanol at 60 degrees C followed by evaporation of ethanol.