Objective A high-performance liquid chromatography-tandem mass spectrometry(HPLC-MS/MS)method was developed to quantify galantamine concentrations in rat blood following intramuscular injection of galantamine hydrobromide and to investigate its pharmacokinetic profile.Methods Male and female SD rats were randomly divided into four groups,each with six rats(three males and three females).The single intramuscular injection group received a single intramuscular dose of hydrobromide galantamine at low,medium,and high doses(0.25,0.50 and 1.00 mg·kg1)in rats.The single intravenous injection group received a single intravenous dose of hydrobromide galantamine at 0.25 mg·kg-1.The multiple intramuscular injection group received hydrobromide galantamine at 0.50 mg·kg-1 via intramuscular injection once daily for 7 consecutive days with a 24-hour interval between doses.Pharmacokinetic parameters of galantamine were calculated for each treatment group.Results The peak concentrations(Cmax)of galantamine following a single intramuscular injection in the low,medium,and high-dose groups were(80.54±9.31),(168.25±47.92)and(314.33±46.51)ng·mL-1,respectively.The area under the concentration-time curve(AUC0-t)was(95.23±20.42),(182.21±36.63)and(380.43±70.71)ng·mL-1·h,respectively.Additionally,the accumulation index of galantamine in the multiple intramuscular dosing group was 1.09.Conclusion Intramuscular injection of galantamine hydrobromide has good bioavailability in rats.Meanwhile,when administered multiple times,the drug accumulates low in the body.The experimental results provide valuable reference for the clinical pharmacokinetic study and clinical application of hydrobromide galantamine injection.

Objective A high-performance liquid chromatography-tandem mass spectrometry(HPLC-MS/MS)method was developed to quantify galantamine concentrations in rat blood following intramuscular injection of galantamine hydrobromide and to investigate its pharmacokinetic profile.Methods Male and female SD rats were randomly divided into four groups,each with six rats(three males and three females).The single intramuscular injection group received a single intramuscular dose of hydrobromide galantamine at low,medium,and high doses(0.25,0.50 and 1.00 mg·kg1)in rats.The single intravenous injection group received a single intravenous dose of hydrobromide galantamine at 0.25 mg·kg-1.The multiple intramuscular injection group received hydrobromide galantamine at 0.50 mg·kg-1 via intramuscular injection once daily for 7 consecutive days with a 24-hour interval between doses.Pharmacokinetic parameters of galantamine were calculated for each treatment group.Results The peak concentrations(Cmax)of galantamine following a single intramuscular injection in the low,medium,and high-dose groups were(80.54±9.31),(168.25±47.92)and(314.33±46.51)ng·mL-1,respectively.The area under the concentration-time curve(AUC0-t)was(95.23±20.42),(182.21±36.63)and(380.43±70.71)ng·mL-1·h,respectively.Additionally,the accumulation index of galantamine in the multiple intramuscular dosing group was 1.09.Conclusion Intramuscular injection of galantamine hydrobromide has good bioavailability in rats.Meanwhile,when administered multiple times,the drug accumulates low in the body.The experimental results provide valuable reference for the clinical pharmacokinetic study and clinical application of hydrobromide galantamine injection.

Five new terpenoids, including two vibsane-type diterpenoids (1, 2) and three iridoid allosides (3-5), together with eight known ones, were isolated from the leaves and twigs of Viburnum odoratissimum var.sessiliflorum. Their planar structures and relative configurations were determined by spectroscopic methods, especially 2D NMR techniques. The sugar moieties of the iridoids were confirmed as β-D-allose by GC analysis after acid hydrolysis and acetylation. The absolute configurations of neovibsanin Q (1) and dehydrovibsanol B (2) were determined by quantum chemical calculation of their theoretical electronic circular dichroism (ECD) spectra and Rh₂(OCOCF₃)₄-induced ECD analysis. The anti-inflammatory activities of compounds 1, 3, 4, and 5 were evaluated using an LPS-induced RAW264.7 cell model. Compounds 3suppressed the release of NO in a dose-dependent manner, with an IC₅₀ value of 55.64 μmol·L^-1. The cytotoxicities of compounds 1-5 on HCT-116 cells were assessed and the results showed that compounds 2 and 3 exhibited moderate inhibitory activities with IC₅₀ values of 13.8 and 12.3 μmol·L^-1, respectively.
Terpenes/pharmacology* ; Viburnum/chemistry* ; Molecular Structure ; Diterpenes/chemistry* ; Plant Leaves/chemistry*

Objective:To investigate the relationship between the expression level of long non-coding RNA transforming growth factor β2-antisense RNA1 (lncRNA TGFB2-AS1) and placental spiral artery recasting in the placenta of preeclampsia.Methods:A total of 108 pregnant women with severe preeclampsia who were hospitalized in Zaozhuang Maternal and Child Health Hospital and delivered by cesarean section from Oct. 2019 to Jun. 2021 were selected as the research objects, and they were divided into the late-onset preeclampsia group (late-onset severe preeclampsia pregnant women, 56 cases) and early-onset preeclampsia group (early-onset severe preeclampsia pregnant women, 52 cases) ; at the same time, 58 normal pregnant women were selected as the normal pregnancy group. The general data of pregnant women were collected, such as age, systolic blood pressure and diastolic blood pressure. Real-time fluorescent quantitative PCR (qRT-PCR) method was used to detect the expression level of lncRNA TGFB2-AS1 in placental tissues, a scanning electron microscope was used to measure the lumen area and wall thickness of spiral arteries. Pearson correlation analysis method was used to analyze the correlation between the level of lncRNA TGFB2-AS1 in the placenta tissue and the thickness of the spiral artery wall and the area of the lumen of pregnant women with early-onset and late-onset severe preeclampsia.Results:The tube wall thickness [ (119.69±8.31) μm], systolic blood pressure [ (162.86±4.94) mmHg], diastolic blood pressure [ (103.09±2.35) mmHg], and 24-hour urine protein [ (2.17±0.31) g/24 h] in the early preeclampsia group were higher than those in the late preeclampsia group [ (101.04±5.78) μm, (146.95±6.43) mmHg, (92.13±4.74) mmHg, (1.62±0.23) g/24 h] and the normal pregnancy group [ (99.82±5.56) μm, (116.42±9.31) mmHg, (74.25±6.74) mmHg, (0.06±0.02) g/24 h], the placental tissue lncRNA TGFB2-AS1 level (0.62±0.16), lumen area [ (133.74±20.16) μm 2], gestational week of delivery [ (32.15±1.74) weeks], weight of the newborns [ (2.25±0.26) g] were lower than those in the late-onset preeclampsia group [ (0.99±0.21), (185.49±22.75) μm 2, (36.14±1.59) weeks, (3.37±0.32) g] and the normal pregnancy group [ (1.02±0.23), (186.42±23.71) μm 2, (38.19±1.56) weeks, (3.42±0.37) g] ( P<0.05). The systolic blood pressure, diastolic blood pressure, and 24-hour urine protein in the late preeclampsia group were higher than those in the normal pregnancy group, gestational week of delivery was lower than the normal pregnancy group ( P<0.05). Placental tissue lncRNA TGFB2-AS1 of pregnant women with early-onset severe preeclampsia was positively correlated with the lumen area, and negatively correlated with the thickness of the tube wall ( P<0.05). There was no correlation between lncRNA TGFB2-AS1 and the lumen area and wall thickness in the placental tissue of pregnant women with late-onset severe preeclampsia ( P>0.05) . Conclusion:The lncRNA TGFB2-AS1 expression in the placenta tissue of pregnant women with early-onset severe preeclampsia is abnormally low, which may be related to the insufficient recasting of the placental spiral artery.