Development of piroxicam mini-tablets enabled by spherical cocrystallization

Hongbo Chen; Chenguang Wang; Sibo Liu; Changquan Calvin Sun

doi:10.1016/j.ijpharm.2020.119953

Development of piroxicam mini-tablets enabled by spherical cocrystallization

Hongbo Chen, Chenguang Wang, Sibo Liu, Changquan Calvin Sun

Research output: Contribution to journal › Article › peer-review

22 Scopus citations

Abstract

We examined the potential of the spherical cocrystallization (SCC) technology in simultaneously enhancing tablet manufacturability and dissolution of poorly soluble drugs by developing a mini-tablet formulation of piroxicam. The manufacturing of mini-tablets using a direct compression (DC) process is more challenging than conventional tablets because of the much stricter requirement on the micromeritic properties of formulated powders. The SCC process in this work involved two steps: 1) preparing a new piroxicam-ferulic acid (PRX-FA) cocrystal, and 2) forming spherical agglomerates with the aid of a suitable bridging liquid. The PRX-FA cocrystal exhibited enhanced solubility as well as improved plasticity. The bridging liquid, a mixture of chloroform and ethyl acetate (EA) (1: 2, v/v), was chosen based on the high computed adsorption energy of chloroform and EA on morphologically dominating crystal faces of PRX-FA. The improved flowability, tabletability, and dissolution rate of spherical PRX-FA enabled the successful development of a DC mini-tablet formulation with a high PRX loading (41 wt%). This example shows that SCC is a powerful enabling technology for DC tablet formulation development of challenging drugs.

Original language	English (US)
Article number	119953
Journal	International journal of pharmaceutics
Volume	590
DOIs	https://doi.org/10.1016/j.ijpharm.2020.119953
State	Published - Nov 30 2020

Bibliographical note

Funding Information:
H.C. was partially supported by a David J.W. Grant & Marilyn J. Grant Fellowship from the Department of Pharmaceutics, University of Minnesota (2019-2020). We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing resources that contributed to the research results reported in this paper. URL: http://www.msi.umn.edu. The Bruker-AXS D8 Venture diffractometer was purchased through a grant from NSF/MRI (#1229400) and the University of Minnesota. Portions of this work were conducted in the Minnesota Nano Center, which is supported by the National Science Foundation through the National Nano Coordinated Infrastructure Network (NNCI) under Award Number ECCS-1542202.

Funding Information:
H.C. was partially supported by a David J.W. Grant & Marilyn J. Grant Fellowship from the Department of Pharmaceutics, University of Minnesota (2019-2020). We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing resources that contributed to the research results reported in this paper. URL: http://www.msi.umn.edu . The Bruker-AXS D8 Venture diffractometer was purchased through a grant from NSF/MRI (#1229400) and the University of Minnesota. Portions of this work were conducted in the Minnesota Nano Center, which is supported by the National Science Foundation through the National Nano Coordinated Infrastructure Network (NNCI) under Award Number ECCS-1542202.

Publisher Copyright:
© 2020 Elsevier B.V.

Keywords

Dissolution
Mini-tablet
Piroxicam
Powder
Spherical cocrystallization

PubMed: MeSH publication types

Journal Article

Access

10.1016/j.ijpharm.2020.119953

OpenUrl availability

Full text

Cite this

@article{5840f37d6a4c4123ae0b897e6f9c87d8,

title = "Development of piroxicam mini-tablets enabled by spherical cocrystallization",

abstract = "We examined the potential of the spherical cocrystallization (SCC) technology in simultaneously enhancing tablet manufacturability and dissolution of poorly soluble drugs by developing a mini-tablet formulation of piroxicam. The manufacturing of mini-tablets using a direct compression (DC) process is more challenging than conventional tablets because of the much stricter requirement on the micromeritic properties of formulated powders. The SCC process in this work involved two steps: 1) preparing a new piroxicam-ferulic acid (PRX-FA) cocrystal, and 2) forming spherical agglomerates with the aid of a suitable bridging liquid. The PRX-FA cocrystal exhibited enhanced solubility as well as improved plasticity. The bridging liquid, a mixture of chloroform and ethyl acetate (EA) (1: 2, v/v), was chosen based on the high computed adsorption energy of chloroform and EA on morphologically dominating crystal faces of PRX-FA. The improved flowability, tabletability, and dissolution rate of spherical PRX-FA enabled the successful development of a DC mini-tablet formulation with a high PRX loading (41 wt%). This example shows that SCC is a powerful enabling technology for DC tablet formulation development of challenging drugs.",

keywords = "Dissolution, Mini-tablet, Piroxicam, Powder, Spherical cocrystallization",

author = "Hongbo Chen and Chenguang Wang and Sibo Liu and Sun, {Changquan Calvin}",

note = "Funding Information: H.C. was partially supported by a David J.W. Grant & Marilyn J. Grant Fellowship from the Department of Pharmaceutics, University of Minnesota (2019-2020). We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing resources that contributed to the research results reported in this paper. URL: http://www.msi.umn.edu. The Bruker-AXS D8 Venture diffractometer was purchased through a grant from NSF/MRI (#1229400) and the University of Minnesota. Portions of this work were conducted in the Minnesota Nano Center, which is supported by the National Science Foundation through the National Nano Coordinated Infrastructure Network (NNCI) under Award Number ECCS-1542202. Funding Information: H.C. was partially supported by a David J.W. Grant & Marilyn J. Grant Fellowship from the Department of Pharmaceutics, University of Minnesota (2019-2020). We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing resources that contributed to the research results reported in this paper. URL: http://www.msi.umn.edu . The Bruker-AXS D8 Venture diffractometer was purchased through a grant from NSF/MRI (#1229400) and the University of Minnesota. Portions of this work were conducted in the Minnesota Nano Center, which is supported by the National Science Foundation through the National Nano Coordinated Infrastructure Network (NNCI) under Award Number ECCS-1542202. Publisher Copyright: {\textcopyright} 2020 Elsevier B.V.",

year = "2020",

month = nov,

day = "30",

doi = "10.1016/j.ijpharm.2020.119953",

language = "English (US)",

volume = "590",

journal = "International journal of pharmaceutics",

issn = "0378-5173",

publisher = "Elsevier",

}

TY - JOUR

T1 - Development of piroxicam mini-tablets enabled by spherical cocrystallization

AU - Chen, Hongbo

AU - Wang, Chenguang

AU - Liu, Sibo

AU - Sun, Changquan Calvin

N1 - Funding Information: H.C. was partially supported by a David J.W. Grant & Marilyn J. Grant Fellowship from the Department of Pharmaceutics, University of Minnesota (2019-2020). We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing resources that contributed to the research results reported in this paper. URL: http://www.msi.umn.edu. The Bruker-AXS D8 Venture diffractometer was purchased through a grant from NSF/MRI (#1229400) and the University of Minnesota. Portions of this work were conducted in the Minnesota Nano Center, which is supported by the National Science Foundation through the National Nano Coordinated Infrastructure Network (NNCI) under Award Number ECCS-1542202. Funding Information: H.C. was partially supported by a David J.W. Grant & Marilyn J. Grant Fellowship from the Department of Pharmaceutics, University of Minnesota (2019-2020). We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing resources that contributed to the research results reported in this paper. URL: http://www.msi.umn.edu . The Bruker-AXS D8 Venture diffractometer was purchased through a grant from NSF/MRI (#1229400) and the University of Minnesota. Portions of this work were conducted in the Minnesota Nano Center, which is supported by the National Science Foundation through the National Nano Coordinated Infrastructure Network (NNCI) under Award Number ECCS-1542202. Publisher Copyright: © 2020 Elsevier B.V.

PY - 2020/11/30

Y1 - 2020/11/30

N2 - We examined the potential of the spherical cocrystallization (SCC) technology in simultaneously enhancing tablet manufacturability and dissolution of poorly soluble drugs by developing a mini-tablet formulation of piroxicam. The manufacturing of mini-tablets using a direct compression (DC) process is more challenging than conventional tablets because of the much stricter requirement on the micromeritic properties of formulated powders. The SCC process in this work involved two steps: 1) preparing a new piroxicam-ferulic acid (PRX-FA) cocrystal, and 2) forming spherical agglomerates with the aid of a suitable bridging liquid. The PRX-FA cocrystal exhibited enhanced solubility as well as improved plasticity. The bridging liquid, a mixture of chloroform and ethyl acetate (EA) (1: 2, v/v), was chosen based on the high computed adsorption energy of chloroform and EA on morphologically dominating crystal faces of PRX-FA. The improved flowability, tabletability, and dissolution rate of spherical PRX-FA enabled the successful development of a DC mini-tablet formulation with a high PRX loading (41 wt%). This example shows that SCC is a powerful enabling technology for DC tablet formulation development of challenging drugs.

AB - We examined the potential of the spherical cocrystallization (SCC) technology in simultaneously enhancing tablet manufacturability and dissolution of poorly soluble drugs by developing a mini-tablet formulation of piroxicam. The manufacturing of mini-tablets using a direct compression (DC) process is more challenging than conventional tablets because of the much stricter requirement on the micromeritic properties of formulated powders. The SCC process in this work involved two steps: 1) preparing a new piroxicam-ferulic acid (PRX-FA) cocrystal, and 2) forming spherical agglomerates with the aid of a suitable bridging liquid. The PRX-FA cocrystal exhibited enhanced solubility as well as improved plasticity. The bridging liquid, a mixture of chloroform and ethyl acetate (EA) (1: 2, v/v), was chosen based on the high computed adsorption energy of chloroform and EA on morphologically dominating crystal faces of PRX-FA. The improved flowability, tabletability, and dissolution rate of spherical PRX-FA enabled the successful development of a DC mini-tablet formulation with a high PRX loading (41 wt%). This example shows that SCC is a powerful enabling technology for DC tablet formulation development of challenging drugs.

KW - Dissolution

KW - Mini-tablet

KW - Piroxicam

KW - Powder

KW - Spherical cocrystallization

UR - http://www.scopus.com/inward/record.url?scp=85092458077&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85092458077&partnerID=8YFLogxK

U2 - 10.1016/j.ijpharm.2020.119953

DO - 10.1016/j.ijpharm.2020.119953

M3 - Article

C2 - 33039491

AN - SCOPUS:85092458077

SN - 0378-5173

VL - 590

JO - International journal of pharmaceutics

JF - International journal of pharmaceutics

M1 - 119953

ER -

Development of piroxicam mini-tablets enabled by spherical cocrystallization

Abstract

Bibliographical note

Keywords

PubMed: MeSH publication types

Access

OpenUrl availability

Other files and links

Fingerprint

Cite this