Pharmaceutics & Pharmacokinetics Division, CSIR - Central Drug Research Institute, Lucknow, 226031, India.
Academy of Scientific & Innovative Research, Ghaziabad, 201002, India.
Bioanalysis. 2023 Jul;15(13):711-725. doi: 10.4155/bio-2023-0074. Epub 2023 Jun 24.
To study the preclinical pharmacokinetics of 4-hydroxy isoleucine (4-HIL) targeted for polycystic ovary syndrome. The quantitative bioanalysis of 4-HIL in different biological matrices in female Sprage-Dawley rats using LC-MS/MS. At 50 mg/kg, 4-HIL had 56.8% absolute oral bioavailability. It was quickly absorbed and distributed in various tissues in order of small intestine > kidney > ovary > spleen > lung > liver > heart > brain after oral administration. Moreover, 11.07% of 4-HIL was recovered in urine and feces within 72 h. 4-HIL levels in vital organs were found safe, as per tissue distribution results. Hence, 4-HIL could be used as promising therapeutics for management of polycystic ovary syndrome.
研究用于多囊卵巢综合征的 4-羟基异亮氨酸（4-HIL）的临床前药代动力学。采用 LC-MS/MS 法对雌性 Sprage-Dawley 大鼠不同生物基质中的 4-HIL 进行定量生物分析。在 50mg/kg 剂量下，4-HIL 的绝对口服生物利用度为 56.8%。口服后，4-HIL 迅速吸收并分布于各种组织，顺序为小肠>肾脏>卵巢>脾脏>肺>肝>心>脑。此外，4-HIL 在 72 小时内以 11.07%的剂量从尿液和粪便中回收。根据组织分布结果，发现 4-HIL 在重要器官中的水平是安全的。因此，4-HIL 可用作治疗多囊卵巢综合征的有前途的疗法。
