期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 558, 期 -, 页码 284-290出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2019.01.004
关键词
Cilostazol; Poorly water-soluble drug; Binary polymeric blend; Double controlled-release matrix tablet; Enhanced dissolution; Surfactant-driven modulation; Patient centricity
资金
- Bio & Medical Technology Development Program of the National Research Foundation - Ministry of Science, ICT & Future Planning, 2013 Patient-centric R&D Project, Republic of Korea [2013M3A9B5075841]
Commercially available cilostazol (CIL) tablet releases drug immediately and is given twice a day as an antiplatelet and vasodilatory agent. However, clinical usefulness of immediate release (IR) preparation is limited due to its extremely poor water solubility and the difficulty in sustaining the blood concentration, resulting in unwanted side effects such as headaches, pyknocardia and heavy-headed symptoms. To achieve once a day dosage form with enhanced solubility and controlled release, double controlled release CIL matrix tablets (DCRT) were designed by modulating a sol-gel process of binary polymeric blends of a pH-independent hydro-xylpropylmethylcellulose (HPMC) and a pH-dependent polymer (carbomer) assisted with anionic surfactant (sodium lauryl sulfate, SLS). The release profiles of the DCRT were varied according to the ratio of the two polymers. This DCRT enhanced dissolution rate of CIL in a controlled manner due to the sol-gel and erosion process of HPMC, and SLS-driven modulation of charged carbomer via neutralization and micellar interaction. The near-infrared (NIR) chemical imaging and gravimetric behaviors of DCRT clearly showed dynamic modulation of CIL during the swelling and hydration process. Furthermore, the plasma concentration of CIL in DCRT was highly improved and sustained in beagle dogs in a controlled manner.
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