两种紫外-可见分光光度法测定黄芪中总皂苷含量的比较研究

目的 建立香草醛-硫酸法和香草醛-高氯酸法测定黄芪中总皂苷含量的紫外-可见分光光度法,并比较其差异.方法 对香草醛-硫酸法和香草醛-高氯酸法测定黄芪中总皂苷含量的测定条件和方法学进行研究,比较2种方法测定结果的差异.结果 香草醛-硫酸法的测定结果高于香草醛-高氯酸法,香草醛-硫酸法在精密度、重复性和准确度方面均优于香草醛-高氯酸法.结论 香草醛-硫酸法比香草醛-高氯酸法更适用于测定黄芪中总皂苷的含量.     

3种紫外分光光度法测定甘草酸二铵含量的比较

目的:比较测定甘草酸二铵含量的3种紫外分光光度法.方法:紫外分光光度法.用水作溶剂,甘草酸二铵测定波长为252 nm,烟酰胺波长为261 nm,吸收系数(E1m)用5台紫外分光光度计测定.结果:甘草酸二铵浓度在9.64～57.84μg/mL之间与吸收度线性良好,r=0.999 8,吸收系数法,甘草酸二铵对照品法及烟酰胺对照品法的回收率分别为99.64%,99.32%及95.84%,RSD均为0.7%(n=6).结论:用吸收系数和甘草酸二铵对照品法测定本品含量,结果基本一致,而烟酰胺对照品法测定结果偏低.     

甘草中甘草酸的含量测定

目的：摸索甘草中-E-草酸的含量测定方法。方法：采用煎煮法进行提取,并用紫外分光光度法对甘草酸进行含量测定。结果：含量测定的加样回收率为96．4％,RSD为2．07％。结论：含量测定简便可靠,可较好的控制质量。     

复方甘草酸铵凝胶剂制备

目的:制备复方甘草酸铵凝胶剂。方法:以甘草酸铵、苦参碱为主药,卡泊姆为基质制备凝胶剂。用紫外分光光度法分别测定甘草酸铵和苦参碱的含量并进行稳定性试验。结果:甘草酸铵的线性范围为10～70μg·ml~(-1)平均回收率为100.38%;苦参碱的线性范围为10～100μg·ml~(-1)平均回收率为100.6%。结论:该制剂制备工艺可行,凝胶性质稳定,质控方法简单、可靠。     

紫外分光光度法测定甘草酸单铵含量

目的建立复方甘草酸单铵S氯化钠注射液(CAGSSCI)中甘草酸单铵(AGS)的含量测定方法.方法紫外分光光度法(UV).结果AGS在11.92～35.77 mg·L-1浓度范围内呈良好线性关系(r=0.999 4),平均回收率为100.15%,RSD为0.28%.结论此法操作简便准确,可作为该制剂的质量控制方法.     

紫外法测定硫酸阿托品注射液含量

硫酸阿托品注射液含量测定方法有中和滴定法、可见光分光光度法(420nm).本文采用紫外分光光度法(257nm)测定其含量.     

吉林省不同产地西洋参中人参总皂苷含量的测定

目的:建立西洋参中人参总皂苷的测定方法,并对吉林省6个产地西洋参中人参总皂苷含量进行了测定。方法:采用紫外-可见分光光度法测定,检测波长544 nm。结果:紫外-可见分光光度法测定的线性范围为20～200μg(r=0.999 4);平均加样回收率99.9%,RSD为0.82%(n=5)。6个产地中,临江西洋参中人参总皂苷含量最高,敦化较之略低。结论:香草醛-硫酸法比色测定西洋参中人参总皂苷,操作简便,实验的精密度、重现性和稳定性均较好,吉林省6个产地的西洋参中所含人参总皂苷均大于6%。     

盐酸普鲁卡因注射液含量两种测定方法的比较

目的:对用盐酸普鲁卡因注射液含量测定项下第二法与永停滴定法测定盐酸普鲁卡因注射液的含量进行比较。方法:采用紫外分光光度法,永停滴定法对8批样品进行含量测定。结果:紫外分光光度法测定结果与永停滴定法的测定结果无显著性差异。回收率99.0％,RSD=0.6％。结论:采用紫外分光光度法可以作为测定盐酸普鲁卡因注射液中间体的含量测定方法。     

太阳神口服液中甘草酸的HPLC测定

太阳神口服液中甘草酸的ＨＰＬＣ测定中国药品生物制品检定所１０００５０朱维华，俞如英甘草的主要活性成分甘草酸的定量方法有重量法、比色法、薄层层析法、紫外分光光度法、ＧＣ法及ＨＰＬＣ梯度洗脱法等［１～３］。这些方法仅用于甘草酸含量较高的甘草提取物以及甘草...     

双波长系数倍率法测定盐酸普鲁卡因注射液含量

盐酸普鲁卡因注射液的含量测定,文献报道中有永停滴定法、紫外分光光度法、比色法、高效液相色谱法等,各测定方法均有优缺点。本文采用双波长系数倍率法卜引,消除了采用紫外分光光度法测定其含量时,其分解产物对氨基苯甲酸对测定的干扰;     

Influence of honey on the gastrointestinal metabolism and disposition of glycyrrhizin and glycyrrhetic acid in rabbits

To investigate the effects of honey on the pharmacokinetics of glycyrrhizin and glycyrrhetic acid, administration of glycyrrhizin or glycyrrhetic acid with and without honey was carried out in rabbits in a randomized crossover design. An in vitro study using rabbit fecal flora was employed to elucidate the mechanism of the interaction. HPLC methods were used for the determination of glycyrrhizin, glycyrrhetic acid and 3-dehydroglycyrrhetic acid concentrations in serum and feces. Paired and unpaired Student's t-tests were used for statistical comparisons for in vivo and in vitro studies, respectively. Our study indicated that the area under the curve (AUC0-t) of glycyrrhetic acid was significantly enhanced by 53% when honey was concomitantly given with glycyrrhizin, whereas that of glycyrrhizin was not significantly altered. Nevertheless, lack of effect was observed when honey was concurrently given with glycyrrhetic acid. Fecal study indicated that both the hydrolysis of glycyrrhizin to glycyrrhetic acid and subsequent oxidation of glycyrrhetic acid to 3-dehydroglycyrrhetic acid were significantly affected in the presence of honey to result in more glycyrrhetic acid available for absorption. It could be concluded that honey significantly affected the gastrointestinal metabolism of glycyrrhizin and resulted in the increased glycyrrhetic acid exposure. Therefore, honey might enhance the efficacy and adverse effects of glycyrrhizin.     

Novel formulations of a liver protection drug glycyrrhizin

In Japan, glycyrrhizin injections have been used as a therapeutic drug for allergy inflammation since 1948 and for chronic hepatitis since 1979. A 20 ml injection of glycyrrhizin contains 53 mg of monoammonium glycyrrhizinate (40 mg as glycyrrhizin acid), 400 mg of glycine, and 20 mg of L-cysteine. Patients receiving glycyrrhizin injections two or three times per week are forced to accept a decline in quality of life. Because administering glycyrrhizin by injection has some disadvantages, many researchers have systematically searched for novel glycyrrhizin formulations that can be administered through oral, rectal, intranasal, and subcutaneous routes. There are two problems, however, in developing new formulations: (1) glycyrrhizin has low membrane permeability and is thus poorly absorbed, and (2) highly concentrated glycyrrhizin readily forms gels in aqueous solutions. Here, we describe the utility of glycyrrhizin formulations prepared in safe solubility agents and absorption-enhancing agents, as assessed in animal experiments. We also discuss pharmaceutical issues in developing various glycyrrhizin formulations. In the near future, convenient pharmaceutical preparations of glycyrrhizin will be developed for chronic hepatitis patients who require glycyrrhizin therapy.     

RP-HPLC法测定复方珍珠咽喉宁含片中梓醇和甘草酸含量

目的:同时测定复方珍珠咽喉宁制剂中的梓醇和甘草酸含量,以控制复方珍珠咽喉宁含片质量.方法:超声提取,采用ODS-C18反相柱(4.6 mm×250 mm,5 μm),分别用流动相水-乙腈(99.4∶0.6)和乙腈-ψ(乙酸)0.1%的水溶液(33∶67),检测波长似)分别为210 nm和254 nm对梓醇和甘草酸进行测定. 结果:采用ψ(甲醇)50%为溶剂,超声30 min,梓醇的平均回收率98.33%,RSD 0.78%;甘草酸的平均回收率96.89%,RSD 0.45%. 结论:该法简便、快速、专属性强,适用于咽喉宁含片的含量控制.     

Simultaneous determination of glycyrrhizin metabolites formed by the incubation of glycyrrhizin with rat feces by semi-micro high-performance liquid chromatography

A method for semi-micro high-performance liquid chromatography (HPLC) has been established for the simultaneous determination of 3alpha-hydroxyglycyrrhetic acid and 3-dehydroglycyrrhetic acid together with glycyrrhizin, glycyrrhetic acid and glycyrrhetic acid mono-glucuronide formed by incubation of glycyrrhizin with rat feces. The analysis was accomplished within 25 min with a TSKgel ODS-80TsQA (150 x 2.0 mm i.d.) column by linear gradient elution using a mobile phase containing aqueous phosphoric acid and acetonitrile at a flow rate of 0.2 ml.min(-1), a thermostatic oven at 25 degrees C, and detection at 254 nm. The detection limits of these compounds were 0.2 pmol per injection (5 microl). The metabolites of glycyrrhizin, by anaerobic or aerobic incubation with rat fecal suspension over 48 h, were determined. Glycyrrhizin was almost completely converted to metabolite glycyrrhetic acid, and metabolites 3alpha-hydroxyglycyrrhetic acid and 3-dehydroglycyrrhetic acid in negligible amounts in anaerobic conditions. However, the metabolic time courses of 3-dehydroglycyrrhetic acid when incubated in aerobic conditions revealed that it apparently continued increasing during the whole incubation period.     

肝细胞靶向甘草酸表面修饰白蛋白纳米粒的制备工艺

目的研究能主动靶向于肝实质细胞的甘草酸表面修饰白蛋白纳米粒的制备工艺。方法去溶剂化法制备普通纳米粒，以高碘酸盐氧化法制备甘草酸-白蛋白纳米粒偶联物。用2,4,6-三硝基苯磺酸显色法与凝胶柱色谱法验证是否偶联成功，HPLC法测定修饰纳米粒表面甘草酸密度。结果修饰纳米粒表面活性氨基数量较对照组减少19.6%；偶联于纳米粒表面的甘草酸密度为9.2%。纳米粒形态圆整，平均粒径为73 nm，在25 ℃和37 ℃条件下放置10 d后，性质稳定。结论甘草酸表面修饰白蛋白纳米粒制备成功，为进一步研究其对肝细胞的靶向性奠定了实验基础。     

Application of pressure-controlled colon delivery capsule to oral administration of glycyrrhizin in dogs

A colon delivery system has been used to improve the bioavailability of glycyrrhizin, a glycoside of glycyrrhetic acid. The bioavailability of glycyrrhizin is low when administered in conventional oral galenic dosage forms because glycyrrhizin is enzymatically hydrolysed both in the stomach and in the intestine. It was reasoned that if large amounts of glycyrrhizin were directly delivered to the colon, enzymatic activity should be reduced due to saturation so that intact glycyrrhizin could be absorbed into the systemic circulation. Based on this assumption, pressure-controlled colon delivery capsules (PCDCs) were used as a colon delivery system. Eight types of glycyrrhizin solution were prepared and were introduced into PCDCs. After oral administration of the test PCDCs to beagle dogs, blood samples were obtained over 24 h and plasma glycyrrhizin concentrations were measured by an HPLC method. With PCDCs containing aqueous glycyrrhizin and propylene glycol solutions, plasma glycyrrhizin levels were extremely low and the bioavailabilities of glycyrrhizin were 0.6% and 0.4%, respectively. When Labrasol was added to both types of glycyrrhizin solution, the bioavailability was improved to 4.6% for aqueous solution and 3.8% for propylene glycol solution. When a surfactant, Polysorbate 80, was added in combination with Labrasol, synergistic effects were not obtained. Furthermore, dose-dependent effects of Polysorbate 80 were not obtained. Labrasol, which is a component of self-emulsifying drug delivery systems (SEDDS), has been shown to strongly improve the bioavailability of glycyrrhizin from the colon.     

Therapeutic basis of glycyrrhizin on chronic hepatitis B

Glycyrrhizin, a major component of a herb (licorice), has been intravenously used for the treatment of chronic hepatitis B in Japan and improves liver function with occasional complete recovery from hepatitis. This substance modifies the intracellular transport and suppresses sialylation of hepatitis B virus (HBV) surface antigen (HBsAg) in vitro. This study was designed to clarify the pharmacological basis for its effectiveness. The structure-bioactivity relationship of glycyrrhizin, glycyrrhetic acid 3-O-monoglucuronide and glycyrrhetic acid was determined, and glycyrrhetic acid was found to be the most active of them. The amounts of three substances bound to the liver were evaluated in guinea pigs after intravenous administration of glycyrrhizin. Glycyrrhizin and glycyrrhetic acid 3-O-monoglucuronide were detected at concentrations of 31.8-1.3 μg/g of liver, but glycyrrhetic acid was not detected. When glycyrrhizin attained these concentrations in the cellular fraction of the PLC/PRF/5 cell culture, it suppressed the secretion of HBsAg as reported previously. These results indicated that glycyrrhizin administered intravenously might bind to hepatocytes at the concentration at which glycyrrhizin could modify the expression of HBV-related antigens on the hepatocytes and suppress sialylation of HBsAg.     

HPLC法测定复方甘草酸苷片中有关物质的含量

目的建立用高效液相色谱法,测定复方甘草酸苷片中有关物质的含量。方法采用Kromasil100A C18柱（250mm×4．6mm ID,5μm）,以2％的醋酸-乙腈（65：35）为流动相;检测波长为254nm;流速为1．0ml·min^-1。结果在选定的色谱条件下,甘草酸单铵与有关物质可较好的分离。结论该方法简便可靠,专属性强,适用于复方甘草酸苷片中有关物质的检查。     

An analysis of the efficacy and safety of compound glycyrrhizin injections in the treatment of drug-induced liver injury using a nationwide database

Background Drug-induced liver injury (DILI) refers to liver damage caused by drugs. DILI poses a significant challenge in the development of new drugs. The management of DILI mainly involves the withdrawal of the offending drug, and there is a lack of specific therapy. This study sought to evaluate the efficacy and safety of compound glycyrrhizin (CG) injections in DILI patients. Aim To evaluate the efficacy and safety of compound glycyrrhizin injections in DILI treatment. Methods The clinical data of DILI patients were collected from a nationwide DILI database. Patients were divided into two groups: the compound glycyrrhizin (CG) group who received CG injections, and the control group who received no treatment. The propensity score matching (PSM) method was applied to obtain an even distribution of characteristics between the two groups. The efficacy of the CG injections was assessed by the analysis of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels between the two groups. Results There were 152 patients in the compound glycyrrhizin group and 512 patients in the control group. The PSM method was used to acquire 152 matched pairs. The compound glycyrrhizin group had a significantly higher overall ALT and AST normalization rate than the control group (43.42% vs. 24.34%, p?=?0.0004 and 63.82% vs. 38.82%, p?≤?.0001). There was no difference in the levels of renal and serum biochemical parameters between the two groups. Conclusions CG injections are effective in reducing ALT and AST levels in DILI patients, and their safety is comparable to the control group.

     

甘姜苓术汤HPLC指纹图谱及含量测定方法的建立

目的:制备甘姜苓术汤对应实物,建立适用于甘姜苓术汤对应实物HPLC含量测定以及指纹图谱方法.方法:依照古籍记载制备甘姜苓术汤对应实物;应用HPLC对15批对应实物进行有效成分含量测定和指纹图谱建立,流动相为乙腈-0.05％磷酸水,梯度洗脱,检测波长237 nm.结果:建立甘姜苓术汤的HPLC含量测定和指纹图谱的分析方法...