Open Access

International Journal of Pharmaceutics

, volume 631 , pages 122461

Rucaparib cocrystal: Improved solubility and bioavailability over camsylate

Mengyuan Xia ^{1, 2}

Yihua Jiang ^{1, 2}

Yinxiang Cheng ^{1, 2}

Wenjuan Dai ¹

Xiaoyi Rong ¹

Bingqing Zhu ¹

Xuefeng Mei ^{1, 2}

Hide authors affiliations Show authors affiliations: 2 affiliations

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555, Zuchongzhi Road, Shanghai 201203, China |

University of Chinese Academy of Sciences, No. 19A, YuQuan Road, Beijing 100049, China |

Publication type: Journal Article

Publication date: 2023-01-01

Elsevier

International Journal of Pharmaceutics

scimago Q1

wos Q1

SJR: 0.988

CiteScore: 10.1

Impact factor: 5.2

ISSN: 03785173, 18733476

DOI: 10.1016/j.ijpharm.2022.122461

Copy DOI

PubMed ID: 36462737

Pharmaceutical Science

Abstract

Rucaparib (Ruc) is a drug used to treat advanced ovarian cancer associated with deleterious BRCA mutations. Its commercial form, the camsylate salt (Ruc-Cam), suffers from poor aqueous solubility and thus causes low and erratic oral bioavailability. In this work, we aimed to improve the oral exposure of Ruc through cocrystallization. Liquid-assisted grinding, slurry, and solvent evaporation methods were employed to prepare new solid forms of Ruc. Cocrystals of rucaparib-theophylline monohydrate (Ruc-Thp MH), rucaparib-maltol (Ruc-Mal), and rucaparib-ethyl maltol (Ruc-Emal) were obtained. Powder X-ray diffraction, Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, and dynamic vapor sorption were utilized to characterize these multi-component systems. All cocrystals dissolve faster than Ruc-Cam at pH 2.0 and 4.5, and Ruc-Thp MH displays the highest apparent solubility in pH 4.5 and 6.8 buffers. Pharmacokinetic studies in rats show that Ruc-Thp MH exhibits 2.4 times the Cmax and 1.4 times the AUC0-24h at a single dose compared with Ruc-Cam. The enhanced solubility and bioavailability of Ruc-Thp MH showcase the power of cocrystallization in addressing absorption issues in drug development.

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GOST |

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GOST Copy

Xia M. et al. Rucaparib cocrystal: Improved solubility and bioavailability over camsylate // International Journal of Pharmaceutics. 2023. Vol. 631. p. 122461.

GOST all authors (up to 50) Copy

Xia M., Jiang Y., Cheng Y., Dai W., Rong X., Zhu B., Mei X. Rucaparib cocrystal: Improved solubility and bioavailability over camsylate // International Journal of Pharmaceutics. 2023. Vol. 631. p. 122461.

RIS |

Cite this

RIS Copy

TY - JOUR

DO - 10.1016/j.ijpharm.2022.122461

UR - https://doi.org/10.1016/j.ijpharm.2022.122461

TI - Rucaparib cocrystal: Improved solubility and bioavailability over camsylate

T2 - International Journal of Pharmaceutics

AU - Xia, Mengyuan

AU - Jiang, Yihua

AU - Cheng, Yinxiang

AU - Dai, Wenjuan

AU - Rong, Xiaoyi

AU - Zhu, Bingqing

AU - Mei, Xuefeng

PY - 2023

DA - 2023/01/01

PB - Elsevier

SP - 122461

VL - 631

PMID - 36462737

SN - 0378-5173

SN - 1873-3476

ER -

BibTex

Cite this

BibTex (up to 50 authors) Copy

@article{2023_Xia,

author = {Mengyuan Xia and Yihua Jiang and Yinxiang Cheng and Wenjuan Dai and Xiaoyi Rong and Bingqing Zhu and Xuefeng Mei},

title = {Rucaparib cocrystal: Improved solubility and bioavailability over camsylate},

journal = {International Journal of Pharmaceutics},

year = {2023},

volume = {631},

publisher = {Elsevier},

month = {jan},

url = {https://doi.org/10.1016/j.ijpharm.2022.122461},

pages = {122461},

doi = {10.1016/j.ijpharm.2022.122461}

}

Publisher

Elsevier

Journal

International Journal of Pharmaceutics

scimago Q1

wos Q1

SJR

0.988

CiteScore

10.1

Impact factor

5.2

ISSN

03785173 (Print)

18733476 (Electronic)

Profiles

Xuefeng Mei