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Improved properties of fine active pharmaceutical ingredient powder blends and tablets at high drug loading via dry particle coating.
Int J Pharm. 2018 May 30; 543(1-2):288-299.IJ

Abstract

It has been shown that dry coating cohesive active pharmaceutical ingredients (APIs) with nano-silica can improve packing and flow of their blends, facilitating high speed direct compression tableting. This paper examines the broader scope and generality of previous work by examining three fine APIs; micronized Acetaminophen (mAPAP), coarse Acetaminophen (cAPAP) and micronized Ibuprofen (mIBU), and considers dry coating with both hydrophobic or hydrophilic nano-silica to examine the effect not only on packing density and flow of their blends, but also dissolution and tensile strength of their tablets. The impact of the excipient size on blend and tablet properties are also investigated, indicating blend flow is most improved when matching API particle size with excipient particle size. In all cases where the API is dry coated, the blend packing and flow improve, so as to suggest such high drug loaded blends could enable direct compression. Using dry coated API along with finer excipients in blends lead to improved hardness of the corresponding tablets. Interestingly, dissolution profiles show dry coated API tablets generally have faster dissolution rates, regardless of silica hydrophilicity, suggesting API powder deagglomeration via nano-silica coating plays a crucial role. The most significant conclusion is that, although there are differences in properties of blends that depend on the API, hydrophobic or hydrophilic nano-silica coating, as well as large or fine excipients, in all cases, dry coating of APIs significantly improves the possibility of using the specific blend at high drug loading in direct compression tableting.

Authors+Show Affiliations

New Jersey Center for Engineered Particulates, New Jersey Institute to Technology, Newark, NJ 07102, USA.New Jersey Center for Engineered Particulates, New Jersey Institute to Technology, Newark, NJ 07102, USA.New Jersey Center for Engineered Particulates, New Jersey Institute to Technology, Newark, NJ 07102, USA.New Jersey Center for Engineered Particulates, New Jersey Institute to Technology, Newark, NJ 07102, USA.New Jersey Center for Engineered Particulates, New Jersey Institute to Technology, Newark, NJ 07102, USA. Electronic address: dave@njit.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29625168

Citation

Kunnath, Kuriakose, et al. "Improved Properties of Fine Active Pharmaceutical Ingredient Powder Blends and Tablets at High Drug Loading Via Dry Particle Coating." International Journal of Pharmaceutics, vol. 543, no. 1-2, 2018, pp. 288-299.
Kunnath K, Huang Z, Chen L, et al. Improved properties of fine active pharmaceutical ingredient powder blends and tablets at high drug loading via dry particle coating. Int J Pharm. 2018;543(1-2):288-299.
Kunnath, K., Huang, Z., Chen, L., Zheng, K., & Davé, R. (2018). Improved properties of fine active pharmaceutical ingredient powder blends and tablets at high drug loading via dry particle coating. International Journal of Pharmaceutics, 543(1-2), 288-299. https://doi.org/10.1016/j.ijpharm.2018.04.002
Kunnath K, et al. Improved Properties of Fine Active Pharmaceutical Ingredient Powder Blends and Tablets at High Drug Loading Via Dry Particle Coating. Int J Pharm. 2018 May 30;543(1-2):288-299. PubMed PMID: 29625168.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improved properties of fine active pharmaceutical ingredient powder blends and tablets at high drug loading via dry particle coating. AU - Kunnath,Kuriakose, AU - Huang,Zhonghui, AU - Chen,Liang, AU - Zheng,Kai, AU - Davé,Rajesh, Y1 - 2018/04/03/ PY - 2018/01/16/received PY - 2018/03/25/revised PY - 2018/04/02/accepted PY - 2018/4/7/pubmed PY - 2018/9/25/medline PY - 2018/4/7/entrez KW - Direct compression KW - Dry coating KW - Fine excipients KW - Pharmaceutical blends SP - 288 EP - 299 JF - International journal of pharmaceutics JO - Int J Pharm VL - 543 IS - 1-2 N2 - It has been shown that dry coating cohesive active pharmaceutical ingredients (APIs) with nano-silica can improve packing and flow of their blends, facilitating high speed direct compression tableting. This paper examines the broader scope and generality of previous work by examining three fine APIs; micronized Acetaminophen (mAPAP), coarse Acetaminophen (cAPAP) and micronized Ibuprofen (mIBU), and considers dry coating with both hydrophobic or hydrophilic nano-silica to examine the effect not only on packing density and flow of their blends, but also dissolution and tensile strength of their tablets. The impact of the excipient size on blend and tablet properties are also investigated, indicating blend flow is most improved when matching API particle size with excipient particle size. In all cases where the API is dry coated, the blend packing and flow improve, so as to suggest such high drug loaded blends could enable direct compression. Using dry coated API along with finer excipients in blends lead to improved hardness of the corresponding tablets. Interestingly, dissolution profiles show dry coated API tablets generally have faster dissolution rates, regardless of silica hydrophilicity, suggesting API powder deagglomeration via nano-silica coating plays a crucial role. The most significant conclusion is that, although there are differences in properties of blends that depend on the API, hydrophobic or hydrophilic nano-silica coating, as well as large or fine excipients, in all cases, dry coating of APIs significantly improves the possibility of using the specific blend at high drug loading in direct compression tableting. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/29625168/Improved_properties_of_fine_active_pharmaceutical_ingredient_powder_blends_and_tablets_at_high_drug_loading_via_dry_particle_coating_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(18)30213-8 DB - PRIME DP - Unbound Medicine ER -