Improved properties of fine active pharmaceutical ingredient powder blends and tablets at high drug loading via dry particle coating
Document Type
Article
Publication Date
5-30-2018
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.
Identifier
85044923198 (Scopus)
Publication Title
International Journal of Pharmaceutics
External Full Text Location
https://doi.org/10.1016/j.ijpharm.2018.04.002
e-ISSN
18733476
ISSN
03785173
PubMed ID
29625168
First Page
288
Last Page
299
Issue
1-2
Volume
543
Grant
EEC-0540855
Fund Ref
National Science Foundation
Recommended Citation
Kunnath, Kuriakose; Huang, Zhonghui; Chen, Liang; Zheng, Kai; and Davé, Rajesh, "Improved properties of fine active pharmaceutical ingredient powder blends and tablets at high drug loading via dry particle coating" (2018). Faculty Publications. 8650.
https://digitalcommons.njit.edu/fac_pubs/8650
