The Effect of Poorly Compressible Ascorbic Acid on Dilution Potential of Co-processed Excipients

SEDLÁČKOVÁ, Lucie, Martin DOMINIK and Aleš FRANC. The Effect of Poorly Compressible Ascorbic Acid on Dilution Potential of Co-processed Excipients. In 50th Conference SYNTHESIS AND ANALYSIS OF DRUGS. 2022. ISBN 978-80-280-0110-0.

Basic information

• Original name: The Effect of Poorly Compressible Ascorbic Acid on Dilution Potential of Co-processed Excipients
• Name in Czech: Vliv špatně lisovatelné kyseliny askorbové na diluční potenciál společně zpracovaných excipientů
• Authors: SEDLÁČKOVÁ, Lucie, Martin DOMINIK and Aleš FRANC.
• Edition: 50th Conference SYNTHESIS AND ANALYSIS OF DRUGS, 2022.

Other information

• Type of outcome: Conference abstract
• Confidentiality degree: is not subject to a state or trade secret
• WWW: URL
• ISBN: 978-80-280-0110-0
• Keywords (in Czech): tableta; přímé lisování; MA index; index diluční kapacity
• Keywords in English: tablet; direct compression; MA index; dilution capacity index

Abstract

Direct compression is a common method consisting of compression dry powder blend of active pharmaceutical ingredient (API) and excipients to tablet. Appropriate choice of excipients and their optimal ratio can compensate for poor compressible and tabletable properties of API. An example of such a substance is ascorbic acid (AA). The ability of excipients to retain their tabletability even after dilution with another ingredient is called dilution potential. The study aimed to find the dilution potential of six co-processed excipients (CPE) – Advantose® FS95, Cellactose® 80, CombiLac®, MicroceLac® 100, Pearlitol® Flash and StarLac®. From each CPE were prepared four batches containing 1 % of sodium stearyl fumarate and 0, 25, 50 or 75 % of AA. Tablets from each batch were compressed at five compaction forces (3, 4, 5, 6, 7 kN) and were evaluated on the pharmacopoeial requirement. The results of work potential (determined by Minchom and Armstrong), MA index and dilution capacity index (proposed by Habib et. al.) were calculated by determination of area under the curve of tensile strength versus compression pressure profile. The obtained values of dilution potential of all CPE were over 70 weights % of AA. But none of the batches of tablets containing 75 % AA did not meet to require properties (friability and disintegration). The tablets which met these requirements were: Cellactose® 80 with 25 % AA compressed by forces 5–7 kN; CombiLac® with 25 % AA compressed by forces 4–7 kN, MicroceLac® 100 with 25 % AA compressed by forces 3–6 kN and MicroceLac® 100 with 50 % AA compressed by force 7 kN.