HPLC方法研究葛根素混合胶束在Beagle犬体内的药代动力学(英文)

采用高效液相色谱法测定Beagle犬口服葛根素原料药及自制葛根素混合胶束后葛根素的血药浓度, 并计算其药代动力学参数, 比较两者的生物利用度。Beagle犬随机分为两组, 采用单剂量灌胃给予葛根素原料药与葛根素混合胶束, 于不同的时间点取血并用HPLC法测定葛根素的血浆药物浓度。HPLC条件: 色谱柱为DIKMA ODS C18柱 (150 mm×4.6 mm, 5 μm), 保护柱为DIKMA ODS C18柱 (8 mm×4 mm); 流动相甲醇-水 (25:75, v/v); 柱温30 °C; 流速1 mL/min; 检测波长250 nm, 内标物为茶碱。采用WinNonlin 6.1软件求算药代动力学参数。葛根素原料药与葛根素混合胶束在Beagle犬体内的药物动力学参数Tmax分别为61.48和202.91 min, AUC分别为515.96和2796.43 min·μg/mL, CL/F分别为232.58和42.91 mL/min/kg。Beagle犬口服葛根素混合胶束与葛根素原料药的相对生物利用度为542.0%。混合胶束制剂明显提高了葛根素在Beagle犬体内的生物利用度, 且减缓消除速率, 延长达峰时间, 起到了长效、缓效的作用。     

Study on modified shengmai yin injection for prevention and treatment of brain impairment in endotoxin shock rats

Objective:To examine the effects of modified Shenmai Yin on invigorating vital energy, promoting blood flow, and protection against neural impairment in an endotoxin-induced shock rat model. Methods: Ninety-six SD rats were randomly divided into four groups: sham operation (saline 20 ml/kg), shock model (lipopolysaccharide, LPS, 8 mg/kg), Reformed Shengmai Yin (加味生脉饮 Pulse-activating Decoction) (LPS 8 mg/kg + reformed Shengmai Yin Injection 10 ml/kg), and dexamethasone (LPS 8 mg/kg + dexamethasone 5 mg/kg) groups. Each group was subdivided into 1 h, 2 h, 3 h, and 6 h time points for observation. The carotid artery was separated and connected with a biological functional system to monitor mean arterial pressure (MAP). Brain water levels, malonaldehyde (MDA) content, and superoxide dismutase (SOD) activity were also determined. Results: In the shock model group, MAP was progressively decreased after injection of LPS, brain water and MDA contents were increased, brain SOD activity was decreased, and capillary vessel edema in brain tissue was also observed. All these parameters were improved significantly in both treatment groups, although the effects were more marked with Shengmai Yin than with dexamethasone. Conclusion: Modified Shengmai Yin exhibits strong anti-shock and neuroprotective effects against Endotoxininduced shock.     

Avermectins菌丝提取液的分析与主要成分的分离富集

采用高效液相色谱（HPLC）-紫外检测（UVD）／蒸发光散射检测（ELSD）的方法分析avermectins菌丝提取液，发现主要成分为具有紫外吸收和无紫外吸收的物质。利用硅胶吸附柱层析方法分离富集了其中的主要成分。对几种有紫外吸收的组分（A1a、A2a、B1a、B2a）进行了核磁共振（NMR）分析，根据异核单量子相干谱（HSQC）对所有的^13C—NMR和^1H—NMR谱带进行了归属。鉴定了无紫外吸收的物质中含有糖类物质。     

卡培他滨联合顺铂治疗晚期乳腺癌的临床研究

目的 探讨卡培他滨联合顺铂治疗蒽环类及紫杉类耐药的晚期乳腺癌的临床效果.方法 选取解放军第三二三医院肿瘤中心的19例蒽环类及紫杉类耐药的晚期乳腺癌患者,给予卡培他滨联合顺铂治疗,21 d为1个周期,所有患者均治疗2个周期以上,观察临床疗效及不良反应.结果 19例患者中完全缓解1例,部分缓解9例,稳定6例,进展3例,总有效率为52.6％.中位无疾病进展生存期6.0个月（95％CI：4.4 ～7.6个月）,中位生存期15.0个月（95％ CI：13.0 ～ 16.9个月）.主要的毒性反应有骨髓抑制、乏力、胃肠道反应及手足综合征等,为可逆性,无治疗相关死亡.结论 卡培他滨联合顺铂疗效较好,毒性反应可耐受,可作为蒽环类及紫杉类耐药的晚期乳腺癌患者的治疗选择.     

右美托咪定对正颌患者术后恢复的影响

目的 观察应用右美托咪定对正颌患者术后恢复的影响.方法 选择40例正颌患者,随机分成右美托咪定组（A组）和安慰剂组（B组）,A组给予负荷剂量1 μg/kg（20 min）的右美托咪定,后0.5μg/（kg·h）泵注,B组则给予容量和外形相似的0.9％氯化钠注射液.手术结束前20 min左右停药,观察患者的术后恢复情况及血气分析结果变化.结果 A组的睁眼、气管拔管时间均比B组相比明显缩短（P＜0.05）;与术前相比两组患者在气管拔管后,PaO2和pH明显降低（P＜0.05）,PaCO2明显升高（P＜0.05）,B组PaO2下降更显著（P＜0.05）.结论 联合应用右美托咪定可缩短正颌患者的术后恢复时间,并改善氧合功能.     

Ranibizumab alone or in combination with photodynamic therapy vs photodynamic therapy for polypoidal choroidal vasculopathy:a systematic review and Meta-analysis

AIM: To compare the efficacy of intravitreal ranibizumab (IVR) alone or in combination with photodynamic therapy (PDT) vs PDT in patients with symptomatic polypoidal choroidal vasculopathy (PCV).METHODS: A systematic search of a wide range of databases (including PubMed, EMBASE, Cochrane Library and Web of Science) was searched to identify relevant studies. Both randomized controlled trials (RCTs) and non-RCT studies were included. Methodological quality of included literatures was evaluated according to the Newcastle-Ottawa Scale. RevMan 5.2.7 software was used to do the Meta-analysis.RESULTS: Three RCTs and 6 retrospective studies were included. The results showed that PDT monotherapy had a significantly higher proportion in patients who achieved complete regression of polyps than IVR monotherapy at months 3, 6, and 12 (All P≤0.01), respectively. However, IVR had a tendency to be more effective in improving vision on the basis of RCTs. The proportion of patients who gained complete regression of polyps revealed that there was no significant difference between the combination treatment and PDT monotherapy. The mean change of best-corrected visual acuity (BCVA) from baseline showed that the combination treatment had significant superiority in improving vision vs PDT monotherapy at months 3, 6 and 24 (All P<0.05), respectively. In the mean time, this comparison result was also significant at month 12 (P<0.01) after removal of a heterogeneous study.CONCLUSION: IVR has non-inferiority compare with PDT either in stabilizing or in improving vision, although it can hardly promote the regression of polyps. The combination treatment of PDT and IVR can exert a synergistic effect on regressing polyps and on maintaining or improving visual acuity. Thus, it can be the first-line therapy for PCV.     

脉络膜新生血管促进因子的研究进展

脉络膜新生血管(choroidal neovascularization,CNV)是危害视力的主要病变之一,为多种眼底疾病的最终结局,最终导致严重的视力丧失。脉络膜新生血管的产生与促进与血管内皮生长因子与促血管生成素有着密切的关系,我们就这两种细胞因子的来源与作用的研究进展进行综述。     

近视眼巩膜生物力学的研究进展

大量研究表明,巩膜生物力学在近视的发生发展中起着十分重要的作用。近视最主要的病理变化是眼轴的过度增长,其主要原因在于玻璃体腔的延长,而玻璃体腔的延长又是巩膜主动重塑、巩膜变薄、细胞外基质减少的结果,其中伴随着一系列巩膜生物力学的改变。因此,本文就巩膜生物力学的测量方式、近视眼巩膜生物力学的改变、巩膜胶原、蛋白聚糖等成分及成纤维细胞的改变对生物力学的影响等进行综述,以利于更深入地了解近视的发病机制,为将来有效预防和治疗近视提供思路。     

Effects of hypocrellin A on expression of vascular endothelial growth factor and endothelin-1 in human umbilical endothelial cells

Increased endothelin-1 (ET-1), vascular endothelial growth factor (VEGF) and activation of protein kinase C (PKC) are co-contributors to endothelial hyperpermeability in diabetes. Several lines of evidence have suggested a hypothesis that activation of specific PKC isoforms are the causative factor in ET-1 and VEGF mediated endothelial dysfunction. In the present study, we tested this hypothesis with hypocrellin A, a naturally occurring PKC inhibitor from a Chinese plant. Human umbilical vein endothelial cells (HUVECs) were incubated with 20 mM glucose in both the presence and absence of hypocrellin A, after which, the protein expression and release of VEGF and mRNA expression and release of ET-1 were measured. VEGF and ET-1 were released into the medium and expressions of VEGF protein and ET-1 mRNA were significantly increased in HUVECs incubated with 20 mM glucose. Hypocrellin A (150 nM) significantly decreased VEGF release (117 +/- 3 vs. 180 +/- 11 pg/mg, p < 0.05) and VEGF protein expression (from 130 +/- 14% to 88 +/- 18.5%, p < 0.05). ET-1 release was also reduced in hypocrellin A treated HUVECs (63.3 +/- 9.9 vs. 75.2 +/- 12.6 ng/mg). Hypocrellin A significantly reversed the effect of high glucose on ET-1 mRNA expression (p < 0.05). The results revealed that PKC activation plays a pivotal role in VEGF and ET-1 mediated endothelial permeability. The naturally occurring compound hypocrellin A may be a potentially novel treatment for endothelial dysfunction in diabetes.