目的 采用高效液相色谱-质谱联用法研究盐酸多奈哌齐口腔崩解片的人体药物代谢动力学，并评价其生物等效性。 方法 2009年9月－11月对22例健康男性受试志愿者单次交叉口服盐酸多奈哌齐口腔崩解片（试验制剂）和盐酸多奈哌齐普通片（参比制剂），测定给药后不同时间点血浆中多奈哌齐经时血药浓度，采用DAS 2.0软件进行药物代谢动力学参数计算和生物等效性评价。 结果 受试者单次口服试验制剂与参比制剂后，达峰时间分别为（2.95 ± 1.16）、（3.19 ± 0.98） h，峰浓度分别为（9.98 ± 2.93）、（9.13 ± 2.05） ng/mL，药时曲线下面积（0-t）分别为（470.76± 142.64）、（446.57 ± 137.30）ng/mL·h；药时曲线下面积（0-∞）分别为（517.74 ± 169.79）、（489.47 ± 162.13）ng/mL·h。试验制剂与参比制剂的生物等效性结果为104.7%，其90%置信区间为（98.4%，111.4%）。结论 盐酸多奈哌齐口腔崩解片与普通片生物等效。
目的 采用高效液相色谱-质谱联用法（HPLC-MS/MS）研究普罗布考片的人体药物代谢动力学变化规律。 方法 2010年10月－11月，24例健康男性受试者单次口服普罗布考片0.5 g，采用HPLC-MS/MS法测定给药后不同时间点血浆中普罗布考的经时血药浓度，采用DAS 2.0软件进行药动学参数计算。 结果 受试者单次口服普罗布考片，达峰时间为（11.50 ± 6.66）h，峰浓度为（2 894.72 ± 1 320.53）ng/mL，药-时曲线下面积（AUC）0-t为（238 876.96 ± 131 873.67） ng/mL· h，AUC0-∞为（259 989.08 ± 146 112.88）ng/mL· h，半衰期为（278.52 ± 164.72） h。结论 普罗布考片体内过程符合二室模型，单次口服具有较好的安全性。
ObjectiveTo study the pharmacokinetics of lovastatin/niacin sustained-release tablets in healthy Chinese volunteers. MethodsEligible subjects were enrolled to receive a single dose of 20/500, 20/750 and 20/1 000 mg lovastatin/niacin sustained-release tablets and multiple dose of 20/1 000 mg lovastatin/niacin sustainedrelease tablets, one time per day, sustained for 5 days, respectively. Blood samples were obtained before dosing and up to 10, 20, 30, and 45 minutes, and 1 hour, 1.5, 2, 2.5, 3, 3.5, 4, 5, 7, 9, 12, and 15 hours after dosing. Niacin, niacinamide, nicotinuric acid and lovastatin were detected by high performance liquid chromatography-tandem mass spectrometry method. ResultsThe peak concertration and the area under the plasma concentration-time curve (0-t) of nicotinuric acid had linear dynamics characteristics with the dosage when the dose of niacin was between 500 and 1 000 mg. After multiple dosing, pharmacokinetics parameters of nicotinuric acid and lovastatin were close. No significant diTherence was found between male and female subjects. ConclusionLovastatin/niacin sustained-release tablets possess linear kinetics. Accumulation is not significant after multiple dosing. Gender doesn't affect the pharmacokinetics parameters.
ObjectiveTo summarize the relevant studies of pharmacological mechanism of tamoxifen and its influence on ovary function in order to provide information and evidence for the therapy of breast cancer. MethodsPapers published from January 1950 to January 2014, were retrieved in MedLine, OVID, CBM, CNKI databases using the keywords on tamoxifen, drug metabolism, ovary, sex hormone, etc, 1286 papers were retrieved in English literatures, and 621 in Chinese literatures. Criteria of paper adoption:①The clinical and basic studies about metabolism of tamoxifen, metabolic effect of tamoxifen, and gene polymorphism of CYP2D6.②The role played by estrogen receptor and protein cofactors in tamoxifen effect.③The clinical and basic studies about tamoxifen induced ovulation, caused endometrial thickening, changed sex hormone levels. According to the above criteria, 152 papers were selected, and 77 papers out of them were finally analyzed and reviewed. Results①The tamoxifen metabolite 4-OH-N-tamoxifen was the main working component, the decreased levels could predict the poor prognosis.②The CYP2D6 gene polymorphism could affect the metabolic effect of tamoxifen and the therapeutic effect of patients with breast cancer.③The metabolic effect of tamoxifen needed the participation of the estrogen receptors and protein cofactors.④Tamoxifen could affect the reproductive system function through the estrogen receptor of H-P-O axis, ovary, and endometrium. ConclusionsMetabolic effect of tamoxifen is regulated by gene, it could affect reproductive system functions through estrogen receptor. the mechanism that tamoxifen cowld affect the hormone levels and wherther it could reflect the ovarian function by monitering the hormone levels continuously for patients with breast cancer need to be researched.
Three-dimensional (3D) printing, an emerging rapid prototyping technology, has been widely used in biomedical field. 3D printing was originally used to construct the visualization models and molds in medicine. With the development of 3D printing in biomedical field, the technology was gradually applied in complex tissue regeneration and organ reconstruction. Artificial tissues and organs obtained by 3D printing are expected to be used for organ transplantation, new drug development and drug toxicity evaluation in the field of medicine and health care research. This paper describes the individualized application of 3D printing technology in liver surgery and introduces the research progress of 3D bioprinting technology in liver transplantation, drug metabolism and hepatotoxicity evaluation, and prospects its future development trend to provide a reference for further study.