2. Academic Validation
  3. Novel revaprazan-loaded gelatin microsphere with enhanced drug solubility and oral bioavailability

Novel revaprazan-loaded gelatin microsphere with enhanced drug solubility and oral bioavailability

  • J Microencapsul. 2018 Aug;35(5):421-427. doi: 10.1080/02652048.2018.1515997.
Jung Suk Kim 1,  Jong Hyuck Park 1,  Sung Chan Jeong 1,  Dong Shik Kim 1,  Abid Mehmood Yousaf 1 2,  Fakhar Ud Din 1 3,  Jong Oh Kim 4,  Chul Soon Yong 4,  Yu Seok Youn 5,  Kyung Taek Oh 6,  Sung Giu Jin 1 7,  Han-Gon Choi 1
Affiliations

Affiliations

  • 1 a College of Pharmacy & Institute of Pharmaceutical Science and Technology , Hanyang University , Sangnok-gu, Ansan , South Korea.
  • 2 b Department of Pharmacy, COMSATS University Islamabad, Lahore Campus , Lahore , Pakistan.
  • 3 c Department of Pharmacy , Quaid-I-Azam University , Islamabad , Pakistan.
  • 4 d College of Pharmacy , Yeungnam University , Gyongsan , South Korea.
  • 5 e School of Pharmacy , Sungkyunkwan University , Jangan-gu , South Korea.
  • 6 f College of Pharmacy , Chung-Ang University , Seoul , South Korea.
  • 7 g Department of Pharmaceutical Engineering , Dankook University , Cheonan , South Korea.
PMID: 30136606 DOI: 10.1080/02652048.2018.1515997
Abstract

To develop a novel revaprazan-loaded gelatine microsphere with enhanced solubility and oral bioavailability, numerous gelatine microspheres were prepared using a spray-drying technique. The impact of gelatine amount on drug solubility in the gelatine microspheres was investigated. The physicochemical properties of the selected gelatine microsphere, such as shape, particle size and crystallinity, were evaluated. Moreover, its dissolution and pharmacokinetics in rats were assessed in comparison with revaprazan powder. Amongst the gelatine microspheres tested, the gelatine microsphere consisting of revaprazan and gelatine (1:2, w/w), which gave about 150-fold increased solubility, had the most enhanced drug solubility. It provided a spherical shape, amorphous drug and reduced particle size. Furthermore, it gave a higher dissolution rate and plasma concentration than did revaprazan powder. Particularly, it gave about 2.3-fold improved oral bioavailability in comparison with revaprazan powder. Therefore, this novel gelatine microsphere system is recommended as an oral pharmaceutical product of poorly water-soluble revaprazan.

Keywords

Gelatine microsphere; drug solubility; oral bioavailability; revaprazan; spray-drying.

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