AAPS PharmSciTech

, 20:155 | Cite as

Preparation and Evaluation of Mosapride Citrate Dual-Release Dry Suspension

  • Kuntang Liu
  • Zhengjie Meng
  • Yang Li
  • Jiwei Liu
  • Yan Xu
  • Yonglu WangEmail author
  • Xueming LiEmail author
Research Article


In this paper, a novel formulation of dual-release dry suspension of mosapride citrate (DRDS-MC) was designed which can be quickly released in the stomach while having sustained-release effect. Co-grinding mixture of mosapride citrate (MC) together with L-HPC as hydrophilic excipient was prepared in order to improve the solubility of MC. The co-grinding mixture was characterized by solubility studies, DSC, X-RD, SEM, FTIR, and size distribution before the preparation of the DRDS-MC. Then, the co-grinding mixture was used to prepare DRDS-MC via wet granulation method. The evaluation of DRDS-MC was focused on physicochemical properties, intestinal absorption, and pharmacokinetics. The results of DSC, X-RD, SEM, FTIR, and size distribution indicated that MC resides in co-grinding mixture with no crystalline changes, hydrogen bonds made L-HPC greatly improving the solubility of MC. Then, the dissolution of DRDS-MC reached 70% in pH 1.2 within 2 h, and the 12-h dissolution of MC in pH 6.8 was nearly 80%. The sedimentation volume after 3 h was 0.94 and redispersibility was good. The linear regression equation between in vitro release of DRDS-MC and intestinal absorption fraction in rats was: Y = 29.215 + 47.535*X (r = 0.952). At last, pharmacokinetic studies in beagle dogs demonstrated that DRDS-MC has prolonged effect compared with commercial formulation Gasmotin as a reference. All results indicated that the DRDS-MC could be quickly released in the stomach while having sustained-release effect.


dual-release dry suspension mosapride citrate co-grinding sustained release IVIVC 


Funding Information

This work was financially supported by the Jiangsu Synergetic Innovation Center for Advanced Bio-Manufacture (Nos.XTD1820) and the Postgraduate Research & Practice Innovation Program of Jiangsu Province (Nos.KYCX18_1104, KYCX18_1115).


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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  1. 1.College of PharmacyNanjing Tech UniversityNanjingPeople’s Republic of China
  2. 2.Nanjing Bestform Pharmaceutical Technology Co., Ltd.NanjingChina
  3. 3.College of Biotechnology and Pharmaceutical EngineeringNanjing Tech UniversityNanjingChina

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