Form conversion of anhydrous lactose during wet granulation and its effect on compactibility.

The purpose of this study was (a) to evaluate the factors affecting the form conversion of anhydrous lactose to the monohydrate form during wet granulation using water as the granulating agent and (b) study the effect of lactose form conversion on its compaction properties. A two-level full factorial design with two center points was used to evaluate the factors affecting form conversion. The three variables evaluated were percentage of microcrystalline cellulose (low 0 and high 20), water to intragranular solids ratio (low 0.

Assessment of segregation potential of powder blends.

Pharmaceutical blends consist of several components each with its own unique characteristics, with different size, shape, density, and particle-particle interactions. With so many degrees of complexity, prediction of segregation behavior becomes intractable. The objective of this study was to develop a segregation test method or a segregation tool that would assess the segregation potential of blends.

Microenvironmental pH modulation in solid dosage forms.

There are many reports in the literature referring to the effect of microenvironmental pH on solid dosage form performance, particularly stability and dissolution profiles. Several techniques have been proposed for the measurement of the microenvironmental pH. Those techniques use certain assumptions and approximations and many of them employ a solution calibration curve of a probe to predict hydrogen ion activity in a substantially dry solid.

Formulation of solid dosage forms to overcome gastric pH interaction of the factor Xa inhibitor, BMS-561389.

Purpose: The purpose of the study was to investigate the specific mechanism by which elevated gastric pH reduces the absorption of BMS-561389, a factor Xa inhibitor, and to develop a solid formulation strategy to overcome this gastric pH interaction.

Methods: A dissolution method in an acetate buffer at pH 5.5 was used to evaluate the dissolution behavior of the tablet formulation.

A study on the effect of wet granulation on microcrystalline cellulose particle structure and performance.

Purpose: The aim of this study was to investigate the mechanism of the effect of wet granulation process on the compaction properties of microcrystalline cellulose (MCC).

Methods: MCC alone and with hydroxypropyl cellulose (HPC) as a binder were wet granulated by a high-shear process using different granulation parameters (over- and undergranulated). Overgranulated batches were also ball milled after drying and compared to the unmilled material.

Effect of starting material particle size on its agglomeration behavior in high shear wet granulation.

The effect of anhydrous lactose particle size distribution on its performance in the wet granulation process was evaluated. Three grades of anhydrous lactose were used in the study: "as is" manufacturer grade and 2 particle size fractions obtained by screening of the 60M lactose. Particle growth behavior of the 3 lactose grades was evaluated in a high shear mixer.