Tags

Type your tag names separated by a space and hit enter

Modulating Sticking Propensity of Pharmaceuticals Through Excipient Selection in a Direct Compression Tablet Formulation.
Pharm Res. 2018 Mar 30; 35(6):113.PR

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.

Authors+Show Affiliations

Pharmaceutical Materials Science and Engineering Laboratory Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., Minneapolis, Minnesota, 55455, USA.Pharmaceutical Materials Science and Engineering Laboratory Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., Minneapolis, Minnesota, 55455, USA. sunx0053@umn.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29603027

Citation

Paul, Shubhajit, and Changquan Calvin Sun. "Modulating Sticking Propensity of Pharmaceuticals Through Excipient Selection in a Direct Compression Tablet Formulation." Pharmaceutical Research, vol. 35, no. 6, 2018, p. 113.
Paul S, Sun CC. Modulating Sticking Propensity of Pharmaceuticals Through Excipient Selection in a Direct Compression Tablet Formulation. Pharm Res. 2018;35(6):113.
Paul, S., & Sun, C. C. (2018). Modulating Sticking Propensity of Pharmaceuticals Through Excipient Selection in a Direct Compression Tablet Formulation. Pharmaceutical Research, 35(6), 113. https://doi.org/10.1007/s11095-018-2396-3
Paul S, Sun CC. Modulating Sticking Propensity of Pharmaceuticals Through Excipient Selection in a Direct Compression Tablet Formulation. Pharm Res. 2018 Mar 30;35(6):113. PubMed PMID: 29603027.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Modulating Sticking Propensity of Pharmaceuticals Through Excipient Selection in a Direct Compression Tablet Formulation. AU - Paul,Shubhajit, AU - Sun,Changquan Calvin, Y1 - 2018/03/30/ PY - 2018/01/19/received PY - 2018/03/23/accepted PY - 2018/4/1/entrez PY - 2018/4/1/pubmed PY - 2019/6/7/medline KW - direct compression KW - powder plasticity KW - punch sticking KW - tablet tensile strength SP - 113 EP - 113 JF - Pharmaceutical research JO - Pharm Res VL - 35 IS - 6 N2 - 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. SN - 1573-904X UR - https://www.unboundmedicine.com/medline/citation/29603027/Modulating_Sticking_Propensity_of_Pharmaceuticals_Through_Excipient_Selection_in_a_Direct_Compression_Tablet_Formulation_ L2 - https://doi.org/10.1007/s11095-018-2396-3 DB - PRIME DP - Unbound Medicine ER -
Try the Free App:
Prime PubMed app for iOS iPhone iPad
Prime PubMed app for Android
Prime PubMed is provided
free to individuals by:
Unbound Medicine.