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Pharmacokinetics of three new cocrystals of pioglitazone hydrochloride in rats
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De-wen KONG1, Zheng-yu FANG2, Ning-bo GONG2, Ying WANG2, Li-da DU3, Sen ZHANG1, Nan JIANG4, Hai-guang YANG1, Lian-hua FANG1, Yang LV2, Guan-hua DU1
Chinese Journal of New Drugs | 2023, 32(10) : 1057 - 1063
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Chinese Journal of New Drugs | 2023, 32(10): 1057-1063
Pharmacokinetics of three new cocrystals of pioglitazone hydrochloride in rats
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De-wen KONG1, Zheng-yu FANG2, Ning-bo GONG2, Ying WANG2, Li-da DU3, Sen ZHANG1, Nan JIANG4, Hai-guang YANG1, Lian-hua FANG1, Yang LV2, Guan-hua DU1
Affiliations
  • 1Beijing Key Laboratory of Drug Targets Identification and Drug Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2Research Centre of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 3Shandong Jishi Pharmaceutical Co., Ltd., Jinan 250101, China
  • 4School of Pharmacy, Henan University, Kaifeng 475004, China
Published: 2023-05-30
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Objective:

To evaluate the absorption of pioglitazone hydrochloride (PGH) cocrystals in SD rats and improve the problems of poor solubility and low bioavailability of PGH.

Methods:

Cocrystals of pioglitazone hydrochloride-para aminobenzoic acid, pioglitazone hydrochloride-para-aminosalicylic acid and pioglitazone hydrochloride-gallic acid were prepared by suspension method. PGH and 3 cocrystals were characterized by a variety of analytical techniques, and the concentration of PGH in rat plasma was determining by high performance liquid chromatography-mass spectrometry (HPLC-MS) to analyze the pharmacokinetic parameters of cocrystals.

Results:

The 3 cocrystals all showed good stability and solubility. Cocrystals of pioglitazone hydrochloride-para aminobenzoic acid and pioglitazone hydrochloride-gallic acid could significantly improve the bioavailability, peak concentration (Cmax), and area under the curve (AUC) of oral PGH in rats.

Conclusion:

Cocrystallization is an important method to change PGH solubility and absorption characteristics in vivo.

pioglitazone hydrochloride  /  cocrystal  /  HPLC-MS  /  pharmacokinetics  /  plasma concentration
De-wen KONG, Zheng-yu FANG, Ning-bo GONG, Ying WANG, Li-da DU, Sen ZHANG, Nan JIANG, Hai-guang YANG, Lian-hua FANG, Yang LV, Guan-hua DU. Pharmacokinetics of three new cocrystals of pioglitazone hydrochloride in rats[J]. Chinese Journal of New Drugs, 2023 , 32 (10) : 1057 -1063 .
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Year 2023 volume 32 Issue 10
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Article Info
  • Online Date：2026-03-05
  • Published：2023-05-30
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History
  • Accepted：2022-12-08
Funding
Affiliations
    1Beijing Key Laboratory of Drug Targets Identification and Drug Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2Research Centre of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    3Shandong Jishi Pharmaceutical Co., Ltd., Jinan 250101, China
    4School of Pharmacy, Henan University, Kaifeng 475004, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
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Genus		 种数
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
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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