Literature DB >> 25630224

Improving the dissolution and bioavailability of 6-mercaptopurine via co-crystallization with isonicotinamide.

Jian-Rong Wang1, Xueping Yu2, Chun Zhou1, Yunfei Lin3, Chen Chen4, Guoyu Pan5, Xuefeng Mei6.   

Abstract

6-Mercaptopurine (6-MP) is a clinically important antitumor drug. The commercially available form was provided as monohydrate and belongs to BCS class II category. Co-crystallization screening by reaction crystallization method (RCM) and monitored by powder X-ray diffraction led to the discovery of a new co-crystal formed between 6-MP and isonicotinamide (co-crystal 1). Co-crystal 1 was thoroughly characterized by X-ray diffraction, FT-IR and Raman spectroscopy, and thermal analysis. Noticeably, the in vitro and in vivo studies revealed that co-crystal 1 possesses improved dissolution rate and superior bioavailability on animal model.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  6-Mercaptopurine; Bioavailability; Crystal structure; Pharmaceutical co-crystal

Mesh:

Substances:

Year:  2015        PMID: 25630224     DOI: 10.1016/j.bmcl.2015.01.022

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

Review 1.  Pharmaceutical Cocrystals: Regulatory and Strategic Aspects, Design and Development.

Authors:  Dipak Dilip Gadade; Sanjay Sudhakar Pekamwar
Journal:  Adv Pharm Bull       Date:  2016-12-22

2.  A Brief Discussion of Multi-Component Organic Solids: Key Emphasis on Co-Crystallization

Authors:  Braham Dutt; Manjusha Choudhary; Vikas Budhwar
Journal:  Turk J Pharm Sci       Date:  2022-04-29

3.  Superior Dissolution Behavior and Bioavailability of Pharmaceutical Cocrystals and Recent Regulatory Issues.

Authors:  Meng Y Xia; Bing Q Zhu; Jian-R Wang; Ze E Yang; Xue F Mei
Journal:  ACS Med Chem Lett       Date:  2021-12-30       Impact factor: 4.345

Review 4.  Recent advances in improving oral drug bioavailability by cocrystals.

Authors:  Shahram Emami; Mohammadreza Siahi-Shadbad; Khosro Adibkia; Mohammad Barzegar-Jalali
Journal:  Bioimpacts       Date:  2018-05-31

5.  Preparation, Characterization, Pharmacokinetic, and Therapeutic Potential of Novel 6-Mercaptopurine-Loaded Oral Nanomedicines for Acute Lymphoblastic Leukemia.

Authors:  Yaru Zou; Dong Mei; Jinjie Yuan; Jiaqi Han; Jiamin Xu; Ning Sun; Huan He; Changqing Yang; Libo Zhao
Journal:  Int J Nanomedicine       Date:  2021-02-12

6.  Mechanistic In Situ and Ex Situ Studies of Phase Transformations in Molecular Co-Crystals.

Authors:  Alexander E Clout; Asma B M Buanz; Yuying Pang; Wing-Mei Tsui; Dongpeng Yan; Gary Parkinson; Timothy J Prior; Dejan-Krešimir Bučar; Simon Gaisford; Gareth R Williams
Journal:  Chemistry       Date:  2020-10-07       Impact factor: 5.236

Review 7.  Advances in Thiopurine Drug Delivery: The Current State-of-the-Art.

Authors:  Ahmed B Bayoumy; Femke Crouwel; Nripen Chanda; Timothy H J Florin; Hans J C Buiter; Chris J J Mulder; Nanne K H de Boer
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2021-09-06       Impact factor: 2.441

Review 8.  Obtaining Cocrystals by Reaction Crystallization Method: Pharmaceutical Applications.

Authors:  Isabela Fanelli Barreto Biscaia; Samantha Nascimento Gomes; Larissa Sakis Bernardi; Paulo Renato Oliveira
Journal:  Pharmaceutics       Date:  2021-06-17       Impact factor: 6.321

  8 in total

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