Tags

Type your tag names separated by a space and hit enter

Reduced Fine API Agglomeration After Dry Coating for Enhanced Blend Uniformity and Processability of Low Drug Loaded Blends.
Pharm Res. 2022 Dec; 39(12):3155-3174.PR

Abstract

PURPOSE

The impact of dry coating on reduced API agglomeration remains underexplored. Therefore, this work quantified fine cohesive API agglomeration reduction through dry coating and its impact on enhanced blend uniformity and processability, i.e., flowability and bulk density of multi-component blends API loading as low as 1 wt%.

METHODS

The impact of dry coating with two different types and amounts of silica was assessed on cohesion, agglomeration, flowability, bulk density, wettability, and surface energy of fine milled ibuprofen (~ 10 µm). API agglomeration, measured using Gradis/QicPic employing gentler gravity-based dispersion, resulted in excellent size resolution. Multi-component blends with fine-sized excipients, selected for reduced segregation potential, were tested for bulk density, cohesion, flowability, and blend content uniformity. Tablets formed using these blends were tested for tensile strength and dissolution.

RESULT

All dry coated ibuprofen powders exhibited dramatic agglomeration reduction, corroborated by corresponding decreased cohesion, unconfined yield strength, and improved flowability, regardless of the type and amount of silica coating. Their blends exhibited profound enhancement in flowability and bulk density even at low API loadings, as well as the content uniformity for the lowest drug loading. Moreover, hydrophobic silica coating improved drug dissolution rate without appreciably reducing tablet tensile strength.

CONCLUSION

The dry coating based reduced agglomeration of fine APIs for all three low drug loadings improved overall blend properties (uniformity, flowability, API release rate) due to the synergistic impact of a minute amount of silica (0.007 wt %), potentially enabling direct compression tableting and aiding manufacturing of other forms of solid dosing.

Authors+Show Affiliations

New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, NJ, 07102, USA.New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, NJ, 07102, USA.New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, NJ, 07102, USA.New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, NJ, 07102, USA. dave@njit.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

35882741

Citation

Kim, Sangah S., et al. "Reduced Fine API Agglomeration After Dry Coating for Enhanced Blend Uniformity and Processability of Low Drug Loaded Blends." Pharmaceutical Research, vol. 39, no. 12, 2022, pp. 3155-3174.
Kim SS, Castillo C, Sayedahmed M, et al. Reduced Fine API Agglomeration After Dry Coating for Enhanced Blend Uniformity and Processability of Low Drug Loaded Blends. Pharm Res. 2022;39(12):3155-3174.
Kim, S. S., Castillo, C., Sayedahmed, M., & Davé, R. N. (2022). Reduced Fine API Agglomeration After Dry Coating for Enhanced Blend Uniformity and Processability of Low Drug Loaded Blends. Pharmaceutical Research, 39(12), 3155-3174. https://doi.org/10.1007/s11095-022-03343-6
Kim SS, et al. Reduced Fine API Agglomeration After Dry Coating for Enhanced Blend Uniformity and Processability of Low Drug Loaded Blends. Pharm Res. 2022;39(12):3155-3174. PubMed PMID: 35882741.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Reduced Fine API Agglomeration After Dry Coating for Enhanced Blend Uniformity and Processability of Low Drug Loaded Blends. AU - Kim,Sangah S, AU - Castillo,Chelsea, AU - Sayedahmed,Muhammad, AU - Davé,Rajesh N, Y1 - 2022/07/26/ PY - 2022/02/12/received PY - 2022/07/13/accepted PY - 2022/7/27/pubmed PY - 2022/7/27/medline PY - 2022/7/26/entrez KW - API agglomeration KW - blend processability KW - blend uniformity KW - dry coating KW - low API loading SP - 3155 EP - 3174 JF - Pharmaceutical research JO - Pharm Res VL - 39 IS - 12 N2 - PURPOSE: The impact of dry coating on reduced API agglomeration remains underexplored. Therefore, this work quantified fine cohesive API agglomeration reduction through dry coating and its impact on enhanced blend uniformity and processability, i.e., flowability and bulk density of multi-component blends API loading as low as 1 wt%. METHODS: The impact of dry coating with two different types and amounts of silica was assessed on cohesion, agglomeration, flowability, bulk density, wettability, and surface energy of fine milled ibuprofen (~ 10 µm). API agglomeration, measured using Gradis/QicPic employing gentler gravity-based dispersion, resulted in excellent size resolution. Multi-component blends with fine-sized excipients, selected for reduced segregation potential, were tested for bulk density, cohesion, flowability, and blend content uniformity. Tablets formed using these blends were tested for tensile strength and dissolution. RESULT: All dry coated ibuprofen powders exhibited dramatic agglomeration reduction, corroborated by corresponding decreased cohesion, unconfined yield strength, and improved flowability, regardless of the type and amount of silica coating. Their blends exhibited profound enhancement in flowability and bulk density even at low API loadings, as well as the content uniformity for the lowest drug loading. Moreover, hydrophobic silica coating improved drug dissolution rate without appreciably reducing tablet tensile strength. CONCLUSION: The dry coating based reduced agglomeration of fine APIs for all three low drug loadings improved overall blend properties (uniformity, flowability, API release rate) due to the synergistic impact of a minute amount of silica (0.007 wt %), potentially enabling direct compression tableting and aiding manufacturing of other forms of solid dosing. SN - 1573-904X UR - https://www.unboundmedicine.com/medline/citation/35882741/Reduced_Fine_API_Agglomeration_After_Dry_Coating_for_Enhanced_Blend_Uniformity_and_Processability_of_Low_Drug_Loaded_Blends_ DB - PRIME DP - Unbound Medicine ER -