Pharmaceutical Research

, 35:113 | Cite as

Modulating Sticking Propensity of Pharmaceuticals Through Excipient Selection in a Direct Compression Tablet Formulation

Research Paper

Abstract

Purpose

To investigate how excipient matrix affects punch sticking propensity of active pharmaceutical ingredients (API), with the focus on the effect of bonding interactions between API-API (F2) and API-excipient (F3).

Method

Sticking kinetics of direct compression formulations, consisting of 20% of celecoxib (CEL) or ibuprofen (IBN) in different excipient matrices, i.e., microcrystalline cellulose (Avicel PH102 and Avicel PH105 dry coated with nano-sized silica (PH105(n)), hypromellose (K15 M), and a 3:1 mixture between starch and Avicel PH102 (S3P1), was assessed using a removable punch tip on a compaction simulator. The amount of material transferred to punch was determined gravimetrically every 10 compressions up to 50 compactions.

Results

CEL exhibited higher F2 than IBN. CEL also exhibited more sticking under otherwise identical compaction conditions in the same excipient matrix. Among different excipient matrices, sticking propensity of both APIs followed the ascending order: PH105(n) < PH102 < K15 M < S3P1. This order was exactly opposite to the order of F3, confirming that greater bonding strength of the formulation favors lower sticking propensity of a given API.

Conclusion

For an API prone to punch sticking, judicious use of excipients to render higher tablet mechanical strength can mitigate severity of punch sticking.

KEY WORDS

direct compression powder plasticity punch sticking tablet tensile strength 

ABBREVIATIONS

F2

API-API cohesive interaction

F3

API-excipient adhesive interaction

CEL

Celecoxib

εc

Critical porosity

F4

Excipient-excipient cohesive interaction

HPMC

Hydroxypropyl methyl cellulose

IBN

Ibuprofen

MCC

Microcrystalline cellulose

1/C

Plasticity parameter

F1

Punch-API adhesive interaction

S3P1

Starch + MCC (3:1)

σ

Tablet tensile strength

σ0

Tensile strength at zero porosity

Supplementary material

11095_2018_2396_MOESM1_ESM.docx (153 kb)
ESM 1 (DOCX 152 kb)

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Pharmaceutical Materials Science and Engineering Laboratory Department of Pharmaceutics, College of PharmacyUniversity of MinnesotaMinneapolisUSA

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