Innovation of novel ‘Tab in Tab’ system for release modulation of milnacipran HCl: optimization,formulation and in vitro investigations

The study was aimed toward development of modified release oral drug delivery system for highly water soluble drug, Milnacipran HCl (MH). Novel Tablet in Tablet system (TITs) comprising immediate and extended release dose of MH in different parts was fabricated. The outer shell was composed of admixture of MH, lactose and novel herbal disintegrant obtained from seeds of Lepidium sativum. In the inner core, MH was matrixed with blend of hydrophilic (Benecel^®) and hydrophobic (Compritol^®) polymers. 3² full factorial design and an artificial neuron network (ANN) were employed for correlating effect of independent variables on dependent variables. The TITs were characterized for pharmacopoeial specifications, in vitro drug release, SEM, drug release kinetics and FTIR study. The release pattern of MH from batch A10 containing 25.17% w/w Benecel^® and 8.21% w/w of Compritol^® exhibited drug release pattern close proximal to the ideal theoretical profile (t_50% = 5.92?h, t_75% = 11.9?h, t_90% = 18.11 h). The phenomenon of drug release was further explained by concept of percolation and the role of Benecel^® and Compritol^® in drug release retardation was studied. The normalized error obtained from ANN was less, compared with the multiple regression analysis, and exhibits the higher accuracy in prediction. The results of short-term stability study revealed stable chataracteristics of TITs. SEM study of TITs at different dissolution time points confirmed both diffusion and erosion mechanisms to be operative during drug release from the batch A10. Novel TITs can be a succesful once a day delivery system for highly water soluble drugs.     

玛咖多糖抗氧化保健作用研究

探讨南美药食两用植物玛咖多糖成分的体外抗氧化保健作用。采用邻苯三酚自氧化法、H2O2诱导红细胞氧化溶血以及CCl4致豚鼠肝脏脂质过氧化的方法,观察体外给予玛咖多糖对这些氧化反应的影响。结果表明,玛咖多糖对邻苯三酚的自氧化有微弱的抑制作用,对H2O2诱导红细胞氧化溶血有显著的抑制作用,最大抑制率达76.9%,显著减少CCl4所致豚鼠肝脏脂质过氧化代谢产物丙二醛的产生。玛咖多糖体外具有一定的抗氧化保健作用。     

Macamides present in the commercial maca (Lepidium meyenii) products and the macamide biosynthesis affected by postharvest conditions

Macamides are bioactive and marker compounds of maca (Lepidium meyenii). Thirty-five commercial maca products were surveyed for macamide composition and content by HPLC-UV/MS. Significant variations of macamide content were found in these products (69–2738 μg/g). Analysis of the macamide biosynthetic pathway suggests that: (a) glucosinolate catabolism, (b) lipid hydrolysis, and (c) amide formation are key steps controlling macamide accumulation in the tissues during the postharvest drying process. Therefore, we further investigated the effects of sample forms, drying temperatures, and storage times on macamide accumulation. Our results show that (1) powdered maca provided the largest macamide accumulation followed by sliced hypocotyls, while whole roots displayed a significantly reduced amide-generating potential; (2) the ideal temperature for macamide formation is about 30°C; (3) macamide content increases continuously along with storage time; (4) exposure to air results in the percentage of unsaturated macamides decreasing. These findings provide useful insights which can be applied in the industrial manufacture of maca products with higher content of bioactive amides.     

玛咖(Lepidium meyenii.)干粉的营养成分及抗疲劳作用研究

本文对南美药食两用植物玛咖(LepidiummeyeniiWalp.)干粉的营养成分进行了分析,其中蛋白质含量达到8.87%,并发现含有大量的支链氨基酸和一定量的牛磺酸、矿物质锌等多种具有抗疲劳作用的营养成分,且通过动物试验证明了玛咖干粉具有显著抗疲劳功效。     

Possible Mechanism of Inhibition of 6-Methoxy-Benzoxazolin-2(3H)-One on Germination of Cress (Lepidium sativum L.)

6-Methoxy-benzoxazolin-2(3H)-one (MBOA) inhibited the germination of cress (Lepidium sativum L.) seeds at concentrations greater than 0.03 mM. Inhibition was overcome by sucrose, suggesting that MBOA may inhibit sugar metabolism in cress seeds. Induction of α-amylase activity in seeds was also inhibited by MBOA at concentrations greater than 0.03 mM. Inhibition of both germination and induction of α-amylase activity increased with increasing concentrations of MBOA, and the extent of germination correlated positively with the activity of α-amylase in the seeds. MBOA added to a reaction mixture for α-amylase assay did not affect enzyme activity, indicating that MBOA does not inhibit in vitro α-amylase activity. Cress seeds germinated approximately 16 hr after incubation, and inhibition of α-amylase by MBOA occurred within 6 hr after incubation. These results suggest that MBOA may inhibit the germination of cress seeds by inhibiting the induction of α-amylase activity, because α-amylase plays a key role in the conversion of reserve carbohydrate into soluble sugars, a prerequisite for seed germination.     

Evaluation of Lepidium sativum seed and guar gum to improve dough rheology and quality parameters in composite rice–wheat bread

The effects of hydrocolloids in rice–wheat flour were studied. Hydrocolloids at 0%, 0.3%, 0.6% and 1% w/w (flour basis) and guar (G), Lepidium sativum seed (L) and guar-L. sativum seed (GL) gum were tested as additives to the rice/flour in various combinations. The quality parameters for the experiment were assessed with farinography, extensography, amylography and texture profile analysis. The evaluation of dough rheology showed that water absorption, dough development time, dough stability and viscosity all increased with the addition of hydrocolloids alone or in a combination. It was demonstrated that G₁L₁ promoted the highest effect. The mixing tolerance index and gelatinization temperature decreased with an increased hydrocolloid concentration. Extensibility value for the dough that incorporated guar and L. sativum seed gum increased with increasing hydrocolloid concentration from 0.3% to 0.6% and then decreased at 1%. The water activity of all bread didn't have significant differences with increasing hydrocolloids concentration but this parameter 24 decreased during storage. Firmness decreased with increasing hydrocolloid concentration and increased with increasing storage time. The sensory evaluation by a consumer panel gave the higher score for overall acceptability to G_0.3L_0.3 and G_0.3L_0.6 samples. The results also showed that G₁L₁, G₁L_0.6 and G_0.6L₁ samples had high specific volume and porosity.     

云南种植的三种颜色玛咖体外抗氧化活性分析?

采用铁离子还原能力(FRAP)、Fenton 反应体系、DPPH 法及邻苯三酚自氧化体系评价种植于云南的玛咖乙醇提取物体外抗氧化能力。结果表明：在云南种植的3 种颜色玛咖乙醇提取物均表现出抗氧化活性,且呈现一定的量效关系,但在4 种抗氧化体系中的结果有所不同;紫色玛咖的总还原能力最强,黄色次之,白色最弱,3200m 海拔地区种植的玛咖高于其他相对低海拔地区的玛咖;紫色和黄色玛咖的清除DPPH 自由基能力高于白色,3200m 海拔地区种植的玛咖高于其他相对低海拔地区的玛咖;3 种颜色玛咖对羟自由基的清除能力明显,各样品的清除率在加入量为200μL 时均达到90% 以上,3000m 海拔地区种植的黄色玛咖最强;3 种颜色玛咖对超氧阴离子自由基的清除能力在实验范围内均较弱。     

云南栽培玛咖总生物碱提取工艺优化研究

以云南栽培玛咖干粉为原料,对其中总生物碱的提取工艺进行优化。采用热水为提取溶剂,以提取温度、提取时间和料液比为考察对象,在单因素优化的基础上设计3因素3水平正交实验,研究玛咖总生物碱的最优提取条件。结果表明,各因素对玛咖总生物碱提取得率的影响顺序依次为:提取时间>料液比>提取温度。最优提取工艺为:料液比1:20(g:mL),温度70℃,时间100min,在此条件下,玛咖总生物碱提取得率为1.58%。      

玛卡及其制品的PCR方法鉴别研究

本研究通过玛卡的defensin基因序列,设计了玛卡的特异性引物,建立了玛卡及其制品中玛卡源性成分检测的一种新方法。通过物种特异性测试,所设计的引物能够特异性扩增玛卡基因,并且,DNA浓度的检测灵敏度达到0.1 ng/μL以上,重量灵敏度达到0.1%以上。并结合芜菁源性成分基因检测方法对市场随机抽取的21份玛卡及其制品进行检测,21份样品均检出了玛卡源性成分而未检出芜菁源性成分。本研究所建立的PCR检测方法快速,准确,高效,适用于市场上玛卡及其制品真伪的快速鉴别。