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Cyclosporin A osmotic pump tablets which can form supersaturated micelles
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Sha SONG1, 2, Hong-zhen YU2, Chun-liu ZHU2, Nian-xiu DUAN1, 2, Miao-rong YU2, Yun LING1, *, Yong GAN2, *
Acta Pharmaceutica Sinica | 2019, 54(1) : 22 - 28
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Acta Pharmaceutica Sinica | 2019, 54(1): 22-28
• Special Reports: Promoting the Dissolution of Poorly Soluble Drugs •
Cyclosporin A osmotic pump tablets which can form supersaturated micelles
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Sha SONG1, 2, Hong-zhen YU2, Chun-liu ZHU2, Nian-xiu DUAN1, 2, Miao-rong YU2, Yun LING1, *, Yong GAN2, *
Affiliations
  • 1. Pharmacy College of Nanchang University, Nanchang 330066, China
  • 2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Published: 2019-01-12 doi: 10.16438/j.0513-4870.2018-0939
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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.

cyclosporine A  /  supersaturated micelle  /  osmotic pump tablet  /  pharmacokinetics  /  sustained-and controlled-release
Sha SONG, Hong-zhen YU, Chun-liu ZHU, Nian-xiu DUAN, Miao-rong YU, Yun LING, Yong GAN. Cyclosporin A osmotic pump tablets which can form supersaturated micelles[J]. Acta Pharmaceutica Sinica, 2019 , 54 (1) : 22 -28 . DOI: 10.16438/j.0513-4870.2018-0939
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Article Info
doi: 10.16438/j.0513-4870.2018-0939
  • Receive Date：2018-10-16
  • Online Date：2026-01-26
  • Published：2019-01-12
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History
  • Received：2018-10-16
  • Revised：2018-12-07
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    1. Pharmacy College of Nanchang University, Nanchang 330066, China
    2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
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表12种不同金属材料的力学参数
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小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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