期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 588, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2020.119779
关键词
Carbinoxamine maleate; Drug-resin complex; Suspension; Sustained release; Ion exchange kinetics; Ion exchange thermodynamics
资金
- National Mega-project for Innovative Drugs [2019ZX09721001]
- Major Project of National Science and Technology 'Creation of Major New Drugs' from China [2018ZX09721002-002]
- China Postdoctoral Science Foundation [2019M651149]
- Liaoning Revitalization Talents Program [XLYC1907111, XLYC1908031]
- Liaoning Province Doctoral Start-up Fund Program [2019-BS-226]
- Liaoning Province Natural Science Fund Project [20180551031]
- Overseas Returnees Start-up Fund from Shenyang Pharmaceutical University [GGJJ2018102]
The short half-life and bitter taste of carbinoxamine maleate(2) (CAM) lead to poor compliance by pediatric patients who are being treated for allergic rhinitis. To address these issues, carbinoxamine-resin complexes(3) (CRCs) were prepared by ion exchange and then coated with Kollicoat SR 30D. The resultant microencapsulated carbinoxamine-resin complexes(4) (MCRCs) were dispersed into the medium to obtain the final suspensions. The drug loading kinetics and thermodynamics of CRCs, anti-swelling mechanism of the impregnant in MCRCs, in vitro release, and in vivo pharmacokinetics of the suspensions were systematically evaluated. The drug loading process was found to obey a first-order kinetic process that was spontaneous, entropy-reduced and exothermic, and the diffusion of CAM into the resin was the rate-limiting step. During microencapsulation, the impregnant could create a certain buffer space to control the swelling of CRCs and maintain the coating film intact. The homemade preparations had release behaviors similar to that of the reference in vitro and achieved sustained release in vivo. The low drug loading preparation had a higher relative bioavailability of 109% owing to its faster release and better dispersibility. Therefore, the suspensions based on MCRCs could be successfully applied to treating allergic rhinitis in children.
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