Formulation Study of a Co-Processed, Rice Starch-Based, All-in-One Excipient for Direct Compression Using the SeDeM-ODT Expert System.

Karnkamol Trisopon,Ornanong Suwannapakul Kittipongpatana,Phanphen Wattanaarsakit,Nisit Kittipongpatana

doi:10.3390/ph14101047

Karnkamol Trisopon, Ornanong Suwannapakul Kittipongpatana + Show 2 more

Open Access

https://doi.org/10.3390/ph14101047

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Journal: Pharmaceuticals	Publication Date: Oct 14, 2021
Citations: 3	License type: CC BY 4.0

Affiliation: Chiang Mai University, Chulalongkorn University

Abstract

A co-processed, rice starch-based excipient (CS), previously developed and shown to exhibit good pharmaceutical properties, is investigated as an all-in-one excipient for direct compression (DC). An SeDeM-ODT expert system is applied to evaluate the formulation containing CS, in comparison with those containing the physical mixture and the commercial DC excipients. The results revealed that CS showed acceptable values in all six incidence factors of the SeDeM-ODT diagram. In addition, the comprehensive indices (IGC and IGCB) were higher than 5.0, which indicated that CS could be compressed with DC technique without additional blending with a disintegrant in tablet formulation. The formulation study suggested that CS can be diluted up to 60% in the formulation to compensate for unsatisfactory properties of paracetamol. At this percentage, CS-containing tablets exhibited narrow weight variation (1.5%), low friability (0.43%), acceptable drug content (98%), and rapid disintegration (10 s). The dissolution profile of CS displayed that more than 80% of the drug content was released within 2 min. The functionality of CS was comparable to that of high functionality excipient composite (HFEC), whereas other excipients were unsuccessful in formulating the tablets. These results indicated that CS was a suitable all-in-one excipient for application in DC of tablets.

Highlights

Nowadays, tablet remains the most commonly used dosage form on the pharmaceutical market
The active pharmaceutical ingredients (APIs) was evaluated using a SeDeM diagram, which provided the characteristics of excipient powder in 5 factors derived from 12 parameters
Excipients were determined with a SeDeM-orally disintegrating tablets (ODT) diagram that included the three disgregability parameters (Figure 1 and Table 1)

Summary

Introduction

Tablet remains the most commonly used dosage form on the pharmaceutical market. Among the general tablet manufacturing methods, direct compression (DC) stands the most prominent due to the cost-effectiveness, simplicity, and high stability it offers to the drug products [4]. Manufacturing without a granulation process and recent advancement in pharmaceutical tableting, such as continuous manufacturing and high-speed tableting machines, could limit this production method with the conventional excipients [5,6]. It encourages the development of a new excipient to support tablet manufacturing under specific production conditions. A co-processed excipient outperforms the physical mixtures in terms of pharmaceutical properties because

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