首页|Co-amorphous formation of piroxicam-citric acid to generate supersaturation and improve skin permeation

Co-amorphous formation of piroxicam-citric acid to generate supersaturation and improve skin permeation

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  • NSTL
  • Elsevier
The objective of this study was to prepare a co-amorphous formulation of piroxicam (PIR), a non-steroidal anti-inflammatory drug, and citric acid (CA), and evaluate its skin permeation ability. A spray-drying method was employed to prepare the co-amorphous formulation and its physical properties were characterized. X-ray powder diffraction and thermal analysis confirmed a homogeneous amorphous state, and the infrared spectra revealed intermolecular interactions between PIR and CA, suggesting formation of a co-amorphous formulation of PIR and CA. The PIR-CA co-amorphous formulation exhibited no crystallization for 60 days at 4/25/40 degrees C with silica gel. The PIR-CA co-amorphous formulation increased the solubility of PIR in polyethylene glycol 400 compared with that of the pure drug, and physical mixture (PM) of PIR and CA, confirming a supersaturated state in the formulation. The PIR-CA co-amorphous formulation demonstrated higher skin permeation than PIR alone or PM of PIR and CA, and the flux value was consistent with the degree of saturation. Thus, the increase in the skin permeation of PIR from the PIR-CA co-amorphous formulation directly depended on the increased thermodynamic activity by supersaturation in the absence of interactions between the drug and co-former in the vehicle.

PiroxicamCitric acidCo-amorphousSupersaturationTransdermal drug delivery

Hirakawa, Yuya、Ueda, Hiroshi、Takata, Yusuke、Minamihata, Kosuke、Wakabayashi, Rie、Kamiya, Noriho、Goto, Masahiro

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Shionogi & Co Ltd, Lab Adv Med Res, Biol, 3-1-1 Futaba Cho, Toyonaka, Osaka 5610825, Japan

Shionogi & Co Ltd, Lab Med Chem Res, Phys Chem, 3-1-1 Futaba Cho, Toyonaka, Osaka 5610825, Japan

Kyushu Univ, Grad Sch Engn, Dept Appl Chem, Nishi Ku, Motooka 744, Fukuoka 8190395, Japan

2021

10.1016/j.ejps.2020.105667

European journal of pharmaceutical sciences

European journal of pharmaceutical sciences

ISTP
ISSN：0928-0987
年,卷(期)：2021.158
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