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Pharmacokinetics of five phthalides in volatile oil of Ligusticum sinense Oliv.cv. Chaxiong, and comparison study on physicochemistry and pharmacokinetics after being formulated into solid dispersion and inclusion compound.
Hu, Peng-Yi; Zhong, Ying-Huai; Feng, Jian-Fang; Li, Dong-Xun; Deng, Ping; Zhang, Wen-Liu; Lei, Zhi-Qiang; Liu, Xue-Mei; Zhang, Guo-Song.
Afiliación
  • Hu PY; Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
  • Zhong YH; Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
  • Feng JF; Guangxi University of Chinese Medicine, Nanning, 530200, China.
  • Li DX; Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
  • Deng P; Guangxi University of Chinese Medicine, Nanning, 530200, China.
  • Zhang WL; Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
  • Lei ZQ; Nanchang Hangkong University, Nanchang, 330063, China.
  • Liu XM; Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
  • Zhang GS; Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
BMC Complement Med Ther ; 21(1): 129, 2021 Apr 22.
Article en En | MEDLINE | ID: mdl-33888111
ABSTRACT
BACKGROUNDS The dried rhizome of Ligusticum sinense Oliv.cv. Chaxiong has been used to treat cardiovascular and cerebrovascular diseases, atherosclerosis, anemia and stroke. A high purity extract from chaxiong (VOC, brownish yellow oil) was extracted and separated. Its main components were senkyunolide A (SA, 33.81%), N-butylphthalide (NBP, 1.38%), Neocnidilide (NOL, 16.53%), Z-ligustilide (ZL, 38.36%), and butenyl phthalide (BP, 2.48%), respectively. Little is known about the pharmacokinetics of these phthalides in Chaxiong, and different preparations to improve the physicochemistry and pharmacokinetics of VOC have not been investigated.

METHODS:

At different predetermined time points after oral administration or intravenous administration, the concentrations of SA, NBP, NOL, ZL and BP in the rat plasma were determined using LC-MS/MS, and the main PK parameters were investigated. VOC-P188 solid dispersion and VOC-ß-CD inclusion compound were prepared by melting solvent method and grinding method, respectively. Moreover, the physicochemical properties, dissolution and pharmacokinetics of VOC-P188 solid dispersion and VOC-ß-CD inclusion compound in rats were assessed in comparison to VOC.

RESULTS:

The absorptions of SA, NBP, NOL, ZL and BP in VOC were rapid after oral administration, and the absolute bioavailability was less than 25%. After the two preparations were prepared, dissolution rate was improved at pH 5.8 phosphate buffer solution. Comparing VOC and physical mixture with the solid dispersion and inclusion compound, it was observed differences occurred in the chemical composition, thermal stability, and morphology. Both VOC-P188 solid dispersion and VOC-ß-CD inclusion compound had a significantly higher AUC and longer MRT in comparison with VOC.

CONCLUSION:

SA, NBP, NOL, ZL and BP in VOC from chaxiong possessed poor absolute oral bioavailability. Both VOC-P188 solid dispersion and VOC-ß-CD inclusion compound could be prospective means for improving oral bioavailability of SA, NBP, NOL, ZL and BP in VOC.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Benzofuranos / Aceites de Plantas / Ligusticum Límite: Animals Idioma: En Revista: BMC Complement Med Ther Año: 2021 Tipo del documento: Article País de afiliación: China

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Benzofuranos / Aceites de Plantas / Ligusticum Límite: Animals Idioma: En Revista: BMC Complement Med Ther Año: 2021 Tipo del documento: Article País de afiliación: China