Contrasting the crospovidones functionality as excipients for direct compression

Daniel García Ramírez,Leopoldo Villafuerte Robles

doi:10.1590/s1984-82502015000100016

Abstract

Specific values of technological properties of excipients allow the establishment of numerical parameters to define and compare their functionality. This study investigates the functionality of Polyplasdones XL and XL10. Parameters studied included tablet disintegration profiles, compactibility profiles and powder flow. The results allowed the establishment of quantitative surrogate functionalities of technological performance, such as absolute number, and as a value relative to the known microcrystalline cellulose type 102. Moreover, the establishment of an explicit functionality to improve the technological performance of two diluents and a model drug was investigated, as was setting up of these functionalities, as quantitative values, to determine the input variables of each material and its probable functionality in a drug product. Disintegration times of pure Polyplasdone XL and its admixtures were around half that of Polyplasdone XL10. The improvement in tablet compactibility was 25-50% greater for Polyplasdone XL10 than Polyplasdone XL. Crospovidones proportions of up to 10% have little effect on the flow properties of other powders, although pure Polyplasdone XL10 and its admixtures display compressibility indexes about 20% greater than Polyplasdone XL. The observed results are in line with a smaller particle size of Polyplasdone XL10 compared to Polyplasdone XL.

Highlights

Cross-linked polyvinylpyrrolidones or crospovidones are synthetic, insoluble, cross-linked homopolymers containing less than 1.5% of soluble material
The materials used in this study were Polyplasdone XL and Polyplasdone XL10 obtained from Ashland-ISP Technologies Inc., amoxicillin trihydrate obtained from Química Alkano, magnesium stearate and Pharmatose M200 obtained from Helm, and calcium phosphate from DROTASA
The current results and those found in the literature are coincident, showing a similar qualitative functionality, but different quantitative functionality, of the Polyplasdones XL and XL10

Summary

Introduction

Cross-linked polyvinylpyrrolidones or crospovidones are synthetic, insoluble, cross-linked homopolymers containing less than 1.5% of soluble material. Crospovidone particles are granular, highly porous and do not form complexes with drugs. These disintegrants accelerate tablet disintegration by the absorption of great quantities of water when exposed to aqueous media. Variation of the medium pH does not affect the disintegrant action of crospovidones. Crospovidone readily forms a hydration layer around the particles, gradually filling and saturating their internal pores. The cross-linked structure of crospovidone behaves as a mesh to prevent the loss of water trapped within the internal pores; its mechanism of action resembles the sponge model proposed for microcrystalline cellulose (Jain et al, 2010)

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Conclusion