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OBJECTIVE: To study the effects of Wuzhi capsule/schisantherin A (SchA) combined with cyclophosphamide on the pharmacokinetics of cyclophosphamide (CTX) in rats. METHODS: A total of 36 rats were randomly divided into CTX group (via tail vein, iv, CTX solution 300 mg/kg), CTX+WZC group (ig, Wuzhi capsule 300 mg/kg+via tail vein, iv, CTX solution 300 mg/kg), CTX + SchA low-dose, medium-dose, high-dose and excessive high-dose groups (ig, SchA 30, 300, 3 000, 30 000 μg/kg+via tail vein, iv, CTX solution 300 mg/kg) with 6 rats in each group. Blood samples were collected from orbital venous plexus of rats before medication and 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48 h after medication.UPLC-MS/MS method was applied for concentration determination of CTX and its metabolites [de-chloroethyl CTX (DC-CTX), 4-ketone CTX (4-keto CTX), carboxyl phosphamide (CPM)] in plasma of rats. The plasma concentration-time curve was obtained. The pharmacokinetic parameters were fitted by using DAS 2. 0 software. RESULTS: The maximum plasma concentration (cmax) of DC-CTX in CTX group, CTX+WZC group, CTX+SchA low-dose, medium-dose, high-dose and excessive high-dose groups were (22 167. 85 ±2 844. 93), (10 920. 53 ± 1 490. 89), (18 951. 29 ± 1 558. 81), (18 622. 08 ± 791. 19), (18 515. 20 ± 2 560. 61), (15 133. 21 ± 1 305. 07) μg/mL, respectively; the area under the curves (AUCo-48 h) were (173 864. 01 ± 65 342. 21), (100 996. 98 ± 33 530. 02), (137 028. 16 ± 45 975. 19), (131 650. 18 ± 53 196. 41), (113 699. 40 ± 34 131. 36), (110 773. 27 ± 30 307. 15) μg·mL/h, respectively. Compared with CTX group, cmax of DC-CTX in CTX group, CTX+SchA low-dose, medium-dose, high-dose and excessive high-dose groups were decreased by 50. 74％, 14. 51％, 16. 10％, 16. 48％, 31. 73％, respectively. AUC0-48 h were decreased by about 42. 23％, 21. 45％, 24. 63％, 33. 37％, 36. 55％, respectively; with statistical significance (P<0. 05). The pharmacokinetic indexes as t1/2, tmax had no significant change. CONCLUSIONS: To some degree, both WZC and SchA can reduce the generation of DC-CTX, which indicates both of them can inhibit CTX toxicity metabolism pathway so as to reduce the generation of toxic metabolite chloroacetaldehyde. The inhibitory effect of SchA on toxicity metabolism pathway is weaker than that of WZC, and does not have a dose-dependent inhibitory effect.
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Objective To confirm the hepatotoxicity of valproic acid (VPA ) and its metabolites (2-propyl-4-pentenoic acid ,3-hydroxy valproic acid ,5-hydroxy valproic acid) on human liver cells .Methods Cells were divided into control group and VPA-treated group .The control group was conventionally cultured while the VPA-treated group was treated with valproic acid and its metabolites . The rate of cell proliferation was assayed by CCK 8 protocol . The mRNA levels of CYP1A1 , CYP1A2 ,PCNA ,Bax and Bcl-2 were measured by real time PCR .The correlated protein levels were measured by Western Blotting .The activity of LDH ,AST and ALT were also detected .Results Compared to the control group ,with the increases of concentrations and reaction time of VPA and its metabolites ,the proliferation rate of L02-cell was reduced ,the mRNA and protein levels of CYP1A1 ,CYP1A2 ,and Bax was increased ,the mRNA and protein level of PCNA and Bcl-2 was decreased , AST ,ALT ,and LDH were also elevated in the treated group .Conclusion Valproic acid and its metabolites were positively re-lated to hepatotoxicity .
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Objective To establish the quality standard for Quban oral liquid .Method Thin layer chromatography (TLC)was used for quality identification of Codonopsis pilosula ,Astragalus membranaceus ,Paeonia veitchii ,Paeonia lacti‐flora,AtractylodesmacrocephalaandAngelicasinensis.ThepaeoniflorinwasdeterminedbyRP‐HPLC.Result Clearspots were obtained with good separation in TLC identification which was highly specific .The paeoniflorin area and content showed a good linear relationship at the range of 18 .20‐2 330 .00 μg/ml (r= 0 .999 9) .The average recovery was 99.72% (RSD=1.25% ) .Conclusion This method is simple ,rapid ,accurate ,and which can be used for the quality control of Quban oral liquid .
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Objective To establish a quality standard forZishen Tongguan Capsules.Methods Anemarrhneae Rhizoma and Phellodendri Chinensis Cortex were qualitatively identified by TLC method. The contents of neomangferin, phellodendrine hydrochloride, mangiferin and berberine hydrochloride inZishen Tongguan Capsules were quantitatively determined by HPLC method.Results The spots of qualitative identification method were clear without interference. Neomangferin in Anemarrhneae Rhizoma and phellodendrinehy drochloride in Phellodendri Chinensis Cortex were identified. Neomangferin, phellodendrinehy drochloride, mangiferin and berberine hydrochloride showed good linearity in the range of 0.025 25–2.02 μg (r=0.999 7), 0.025 5–2.04 μg (r=0.999 7), 0.026–2.08 μg (r=0.999 7), and 0.025 5–2.04 μg (r=0.999 6) respectively. The average recoveries of neomangferin, phellodendrinehy drochloride, mangiferin and berberine hydrochloride were 99.99%, 101.06%, 103.05%, and 100.55%, respectively. The RSD were 2.69%, 5.62%, 2.49%, and 2.06%, respectively.Conclusion The method is accurate and rapid, with good stability, reliability and reproducibility, which can be used for the quality control and evaluation of the preparation of Zishen Tongguan Capsules.
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Objective To establish quality standards forAnshu Liquid.Methods Phellodendri Chinensis Cortex and Kochiae Fructus were qualitatively identified by TLC method. The contents of berberine hydrochloride and phellodendrine hydrochloride in the preparation were determined by HPLC method. The chromatographic column was ZORBAX SB-C18 (4.6 mm×250 mm, 5μm); the mobile phase was acetonitrile-0.1% phosphoric acid (0.5% diethylamine) gradient elution; the flow rate was 1.0 mL/min; the detection wavelength was 284 nm.Results Berberine hydrochloride and phellodendrine hydrochloride in Phellodendri Chinensis Cortex and saponin Ic in Kochiae Fructus were detected by TLC method. The linear relationship of berberine hydrochloride in the preparation was Y=23.109X?30.548,r2=0.999 8, RSD=2.97%, showing that the linear range of berberine hydrochloride was 0.050 5– 2.525 0 μg. The linear relationship of phellodendrine hydrochloride in the preparation wasY=10.038X?2.446 6, r2=0.999 9, RSD=1.24%, showing that the linear range of phellodendrine hydrochloride was 0.050 0–2.500 0 μg. Conclusion The method is accurate, rapid, stable and reliable, with good reproducibility, which can be used for the quality control and evaluation ofAnshu Liquid.
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OBJECTIVE:To establish the quality standard for Xianrengu oral liquid. METHODS:Thin layer chromatography (TLC) was used for qualitative identification of Epimedii Folium,Astragali Radix,lycium barbarum,Atractylodes macrocephala and Panax ginseng in Xianrengu oral liquid;RP-HPLC was preformed on the column of Dikma Diamonsil C18 with the mobile phase of acetonitrile-0.1% phosphoric acid (30∶70,V/V)at the flow rate of 1.0 ml/min,the detection wavelength was 270 nm,the temperature was 30℃and the volume was 10μl. RESULTS:TLC identification had good separation,clear spots and high specifica-tion. The linear range of icariin was 7.97-510.00 μg/ml(r=0.999 3);RSDs of precision,stability and reproducibility tests were no more than 0.83%;and the average recovery was 97.69%(RSD=1.30%,n=6). CONCLUSIONS:This method is simple,accu-rate and simple,which can be used for the quality control of Xianrengu oral liquid.
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In recent years , many studies have found that vitamin D insufficiency is associated with osteomalacia , hyperten-sion, diabetes, metabolic syndrome and other diseases .Vitamin D must be hydroxylated in the liver by a 25-hydroxylase for the first time, and then in the kidney by a 1α-hydroxylase for the second time to form the active metabolite 1,25-dihydroxy vitamin D ,which binds to the intracellular vitamin D receptor and exerts its effects .This paper reviewed the relationship between vitamin D and disease , present research situation of gene polymorphism of vitamin D receptor , and the advantages and limitations of several methods of vitamin D detection, and proposed the best method for detecting vitamin D receptor gene polymorphism and the importance of the detection state to guide clinicians to use drug rationally .
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Objective To investigate the application of ultrasound visualization in instantly evaluation and supplement therapeu-tics in the treatment of uterine fibroids and adenomyosis with high intensity focused ultrasound (HIFU ) .Methods 57 patients with 67 uterine fibroids and 31 patients with 41 adenomyosis were treated with JC-200 HIFU treatment system and monitored the blood flow change in the lesion with B-ultrasound .Evaluated the curative effect with ablation ratio and ablation ratio after supplement therapeutics .Results The average ablation ratio of 57 uterine fibroids was(84 .6 ± 16 .1)% and the increased to(87 .0 ± 10 .7)% af-ter supplement therapeutics to 9 lesions with blood flow in the border of all .The changes were no significance(P>0 .05) .The aver-age ablation ratio of 31 adenomyosis was(62 ± 22 .7)% and increased to(74 ± 14 .7)% after supplement therapeutics to 11 lesions with blood flow in the border of all .The changes were statically significance(P<0 .05) .Conclusion Ultrasound visualization could be used to evaluate the area and extent of ablation with HIFU therapy ,it can clear lesions remaining parts and guiding the supple-ment therapeutics to improve the ablation ratio .Ultrasound visualization provided an evidence of therapeutics in the early period .
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AIM:To observe the contents of ursolic acid and oleanolic acid in Liuwei Dihuang Pill(Radix Rehmanniae praeparata,Rhizoma Dioscoreae,Fructus Corni,Rhizoma Alismatis,etc.) from different manufacturers and explore their effects on quality of Liuwei Dihuang Pill.METHODS:Ursolic acid and oleanolic acid in Liuwei Dihuang Pill were determined by HPLC-PAD method using Kromasil C_ 18 column(4.6 mm?250 mm,5 ?m) as chromatographic column,methanol-water-phosphate(88∶12∶0.02) as the mobile phase at the rate of 1.0 mL/min.RESULTS:6.462-0.718 ?g of ursolic acid and 3.132-0.348 ?g of oleanolic acid presented a good linear relationship.The average recoveres were 99.73% and 97.59%,RSD were 1.5% and 1.7%,respectively.There were significant differences in the contents of ursolic acid and oleanolic acid in Liuwei Dihuang Pill from four different manufacturers.CONCLUSION:The method is simple,rapid and feasible to set up determination of ursolic acid and oleanolic acid in Liuwei Dihuang Pill by HPLC-PAD.Although the contents of ursolic acid and oleanolic acid have significant differences in different manufactures,the results show good consistency in the content variation of the two acids.