| Title | Improved Stability of a Stable Crystal Form C of 6S-5-Methyltetrahydrofolate Calcium Salt, Method Development and Validation of an LC-MS/MS Method for Rat Pharmacokinetic Comparison |
| Authors | Lian, Zenglin Chen, Hong Liu, Kang Jia, Qianghua Qiu, Feng Cheng, Yongzhi |
| Affiliation | Beijing Jinkang Hexin Pharmaceut Technol Co Ltd, Beijing 101111, Peoples R China Capital Med Univ, Sch Tradit Chinese Med, Beijing Key Lab TCM Collateral Dis Theory Res, Beijing 100069, Peoples R China Lianyungang Jinkang Hexin Pharmaceut Co Ltd, Lianyungang 222115, Peoples R China Beijing Univ, Chinese Med DongFang Coll, Beijing 100029, Peoples R China |
| Keywords | FOLIC-ACID SUPPLEMENTATION FOLATE PREVENTION |
| Issue Date | Oct-2021 |
| Publisher | MOLECULES |
| Abstract | Folate is a vitamin beneficial for humans that plays an important role in metabolism, but it cannot be well supplemented by food; it is necessary to supplement it in other ways. Based on this consideration, a novel crystal form C of 6S-5-methyltetrahydrofolate calcium salt (MTHF CAC) was obtained. To explore the difference between MTHF CAC and the crystal form I of 6S-5-methyltetrahydrofolate calcium salt (MTHF CA) as well as an amorphous product of 6S-5-methyltetrahydrofolate glucosamine salt (MTHF GA), their stability and pharmacokinetic behaviours were compared. The results of high-performance liquid chromatography coupled with ultraviolet detection analysis indicated that MTHF CAC showed a better stability than MTHF CA and MTHF GA. After oral administration of MTHF CAC, MTHF CA, and MTHF GA to male rats, the MTHF concentrations were analysed using a validated liquid chromatography-tandem mass spectrometry, and the pharmacokinetic parameters were compared. The mean residence times (0-t) of MTHF CAC, MTHF CA, and MTHF GA were 3.7 & PLUSMN; 1.9 h, 1.0 & PLUSMN; 0.2 h (p < 0.01), and 1.5 & PLUSMN; 0.3 h (p < 0.05), respectively. The relative bioavailability of MTHF CAC was calculated to be 351% and 218% compared with MTHF CA and MTHF GA, respectively, which suggests that MTHF CAC can be better absorbed and utilized for a longer period of time. |
| URI | http://hdl.handle.net/20.500.11897/629330 |
| DOI | 10.3390/molecules26196011 |
| Indexed | SCI(E) |
| Appears in Collections: | 待认领 |
