Cyclosporin A osmotic pump tablets which can form supersaturated micelles
10.16438/j.0513-4870.2018-0939
- VernacularTitle:可形成过饱和胶束的环孢素A渗透泵片的研究
- Author:
Sha SONG
1
;
Hong-zhen YU
2
;
Chun-liu ZHU
2
;
Nian-xiu DUAN
1
;
Miao-rong YU
2
;
Yun LING
3
;
Yong GAN
2
Author Information
1. Pharmacy College of Nanchang University, Nanchang 330066, China; Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
3. Pharmacy College of Nanchang University, Nanchang 330066, China
- Publication Type:Research Article
- Keywords:
cyclosporine A;
supersaturated micelle;
osmotic pump tablet;
pharmacokinetics;
sustained- and controlled-release
- From:
Acta Pharmaceutica Sinica
2019;54(1):22-28
- CountryChina
- Language:Chinese
-
Abstract:
The poor solubility of cyclosporine A (CsA) in water limits its oral absorption. We prepared CsA/ Soluplus/SDS complex, which can form CsA/Soluplus/SDS supersaturated micelles (CSS-SM) after hydration. Then, We further prepared CSS-SM osmotic pump tablets (CSS-SM-T). CSS-SM had a particle size of 156 nm, where in encapsulation efficiency and drug loading efficiency of CsA were 89.0% and 17.5%, respectively. CSS-SM-T achieved zero-level drug release in vitro. Pharmacokinetic data from Beagle dogs (all animal experiments were conducted under the guidelines approved by the Institutional Animal Care and Use Committee of the Shanghai Institute of Materia Medica, Chinese Academy of Sciences) indicated that CsA in the ordinary osmotic pump tablets was hardly absorbed after orally administered; despite slightly lower bioavailability [relative bioavailability: (85.1 ± 47.4) %] than that of Sandimmum Neoral, CSS-SM-T displayed lower fluctuations in CsA plasma concentration and obvious sustained-release characteristics in vivo, implying lower toxicity. Therefore, CSS-SM-T provides a new research idea for the design and development of oral sustained- and controlled-release preparations of poorly water-soluble drugs.
