Particle Engineering of Chitosan and Kaolin Composite as a Novel Tablet Excipient by Nanoparticles Formation and Co-Processing.

Chonwipa Yarangsee,Phanphen Wattanaarsakit,Phuriwat Leesawat,Jakkapan Sirithunyalug

doi:10.3390/pharmaceutics13111844

Chonwipa Yarangsee, Phanphen Wattanaarsakit + Show 2 more

Open Access

https://doi.org/10.3390/pharmaceutics13111844

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Abstract

Chitosan is not a common excipient for direct compression due to poor flowability and inadequate compressibility. Co-processing of chitosan and kaolin is a challenging method to overcome the limitations of the individual excipients. The purpose of the present study was to develop co-processed chitosan–kaolin by the spray drying technique (rotary atomizer spray dryer) and to characterize the excipient properties. The formation of chitosan nanoparticles was the major factor for desirable tablet hardness. The ratio of chitosan/tripolyphosphate of 10:1 and 20:1 had a significant effect on hardness. The successful development of co-processed chitosan–kaolin as a novel tablet excipient was obtained from a feed formulation composed of chitosan and kaolin at a ratio of 55:45 and the optimum chitosan/tripolyphosphate ratio of 20:1. Co-processing altered the physical properties of co-processed chitosan–kaolin in such a way that it enhanced the flowability and tableting performance compared to the physical mixture.

Highlights

Tablets have been an attractive choice for pharmaceutical manufacturing over several decades and are a commonly used dosage form for drug administration
The results show that the optimal ratio of chitosan to kaolin was 55:45 and a chitosan/TPP ratio at 20:1 can enhance the physical properties of the resulting Co-Processed Chitosan-Kaolin (CCK) prepared by spray drying, in terms of flowability and tablet hardness
The results show that the optimal ratio of chitosan to kaolin was 55:45 and aHardness chitosan/TPP ratio at 20:1 can enhance the physical propDisintegration time erties of the resulting CCK prepared by spray drying, in terms of flowability and tablet hardness

Summary

Introduction

Tablets have been an attractive choice for pharmaceutical manufacturing over several decades and are a commonly used dosage form for drug administration. Consideration of the tableting approach is dependent on the characteristic properties of the active pharmaceutical ingredient (API), the excipients, and their stability during the manufacturing process [1]. Direct compression (DC) is the preferable method for tablet preparation since it requires fewer processing steps, avoids exposure to heat and moisture, resulting in good stability of the therapeutic drug [2], and offers lower production costs. API that can be processed into tablets by DC are limited due to poor flowability and compactibility properties. Excipients that enhance powder flowability and compactibility are required in order to increase the use of DC in tablet production and ensure robust manufacturing [1]. Many DC carriers are commercially available, most of them cannot be classified as multifunctional excipients; several excipients have to be used in a DC formulation in the tablet manufacturing industry

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