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ObjectiveTo evaluate the clinical effect of Silybum marianum preparation in the prophylactic treatment of antitubercular agent-induced liver injury (ATB-DILI), since there have always been controversies over the development of Silybum marianum preparation for the prophylactic treatment of ATB-DILI. MethodsMEDLINE, PubMed, Embase, and Cochrane Central Register of Controlled Trials were searched for randomized controlled trials (RCTs) on Silybum marianum preparation versus placebo in preventing ATB-DILI published up to November 30, 2018. STATA 12.0 software was used for statistical analyses. Standardized mean difference (SMD) and risk ratio (RR) with 95% confidence intervals (CI) were used to evaluate the effect of Silybum marianum preparation. The Cochrane handbook was used to assess the quality of RCTs, and funnel plots and Egger’s tests were used to evaluate publication bias. A sensitivity analysis was conducted to assess the influence of each RCT on overall effect. ResultsA total of five RCTs with 1198 patients were included, and among these patients, 585 received Silybum marianum preparation and 613 received placebo. Silybum marianum preparation significantly reduced the risk of the onset of ATB-DILI at week 4 (RR=0.33, 95%CI: 0.15-0.75, P=0.008). In addition, Silybum marianum preparation had a protective effect on liver function in patients receiving antitubercular agents (alanine aminotransferase: SMD=-0.15, 95%CI: -0.24 to -0.07, P＜0.001; aspartate aminotransferase: SMD=-0.14, 95%CI: -0.23 to -0.06, P=0.001; alkaline phosphatase: SMD=-0.12, 95%CI: -0.20 to-0.03, P=0.008). Silybum marianum preparation had a similar risk of adverse events as placebo (RR=1.09, 95%CI: 0.86-1.39, P=0.47). ConclusionIn patients with tuberculosis, prophylactic treatment with Silybum marianum preparation can significantly reduce the risk of the onset of ATB-DILI after 4 weeks of treatment. In addition, Silybum marianum preparation can also improve the liver function of patients treated with antitubercular agents.
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Mogroside V is the most abundant [approximately 0.50%] cucurbitane-type triterpene glycoside in Siraitia grosvenorii and exhibits significant antitussive, expectorant, anti-carcinogenic, and anti-inflammatory effects. A sensitive, robust and selective liquid chromatography tandem with mass spectrometry [LC-MS/MS] was developed and validated for the determination and pharmacokinetic investigation of mogroside V in rat plasma. Samples were prepared through an one-step deproteinization procedure with 250 microL of methanol to a 75-microL plasma sample. Plasma samples were effectively separated on a Shiseido Capcell Pak UG120 C18 column [2.0 × 50mm, 3.0microm] using a mobile phase consisting of methanol: water [60:40, v/v] with an isocratic elution program. The running time for each sample was 7.0 min and the elution times of mogroside V and IS were 2.0 and 4.8 min, respectively. The detection relied on a triplequadrupole tandem with mass spectrometer equipped with negative-ion electrospray ionization interface by selectedreaction monitoring [SRM] of the transitions at m/z 1285.6 - 1123.7 for mogroside V and m/z 1089.6 - 649.6 for IS. The calibration curve was linear over the range of 96.0-96000 ng/mL with a limit of quantitation [LOQ] of 96.0ng/mL. Intra-day and inter-day precisions were both <10.1%. Mean recovery and matrix effect of mogroside V in plasma were in the range of 91.3-95.7% and 98.2-105.0%, respectively. This method was successfully applied in the pharmacokinetic study of mogroside V after intravenous or intraperitoneal administration of 1.12mg/kg mogroside V in rats
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OBJECTIVE:To provide reference for promoting rational use of vancomycin in the clinic. METHODS:Referring to vancomycin instruction,Guiding Principles for Clinical Use of Antibacterials (2015 edition) and Chinese Expert Consensus on Clinical Use of Vancomycin (2011 edition),720 inpatient medical records of vancomycin were collected from our hospital during Jan. 2013-Dec. 2014,and then drug use of those inpatients were analyzed retrospectively. RESULTS:Among 720 cases,male (428 cases)was more than female(292 cases),and most of them aged 41-65(45.83%). There were 50 cases of prophylactic drug use(6.94%)and 670 cases of therapeutic drug use(93.06%). The patients came from 36 departments. Among 720 cases,the dose of 19 cases were higher than 2 g/d,and there were 13 ADR cases(1.81%). Among 670 cases of therapeutic drug use,587 cases of microbiological samples (87.61%) were detected,and other antibacterials were used in 522 cases additionally (77.91%). DUI of vancomycin was equal to 0.96 in 549 cases no younger than 18 years old of herapeutic drug use. There were 240 cases of unsuit-able drug use (33.33%) in total,including 192 cases of unsuitable solvent (26.67%),28 cases of unsuitable usage and dosage (3.89%)and 20 cases of unsuitable drug combination(2.78%). CONCLUSIONS:The use of vancomycin in our hospital is basi-cally rational;vancomycin is widely used in departments;drug combination is a common phenomenon;the inspection rate of mi-crobiological samples is qualified;no drug abuse is found. However,there still is inappropriate use in the clinic. It is recommended to strengthen special evaluation and training about rational use of vancomycin,and further standardize monitoring for vancomycin use so as to guarantee the safety of drug use.
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Objective To review pharmacological mechanism, pharmacokinetics, clinical research progress and prospects of pradefovir, a liver targeted medicine for hepatitis B.Methods The studies of pradefovir were summarized by searching literature databases of Web of Science,Elsevier ScienceDirect,Springer Link,Wiley Online Library, Pubmed, CNKI, Wanfang and VIP datebase.Results Pradefovir is a prodrug that targets to the liver, which absorbs rapidly by oral administration.Pradefovir could be quickly converted to adefovir with hepatic drug metabolizing enzyme CYP3A4. Compared with adefovir dipivoxil, it has shown smaller nephrotoxicity and larger liver targeting.Conclusion Pradefovir has shown favorable safety and effectiveness in the clinical study and has no durg resistance to be found.The approval Ⅲ clinical trial has been acquired of pradefovir in USA and has enteredⅠ clinical trial currently in our country, which has good prospects for clinical application in future.
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Objective To determine serum concentration of methotrexate in children with acute lymphoblastic leukemia by HPLC and explore the application practice.Methods The separation was performed in a Wondasil C18-WR column (4.6 mm ×150 mm, 5 μm) with a mobile phase of methanol-0.15%phosphoric acid solution(21:79 ) and determined at 306 nm.The sample of serum was centrifuged after protein precipitation with perchloric acid.Detected results for children to establish monitoring files.ResuIts The linearity was well at 0.02 ~50 μg/mL of methotrexate ( r =0.9990,n=6).The average recovery was 96.50%, RSD of within day and between days were less than 15%.Established monitoring files for six children and after 3 courses of treatment, the blood concentration of methotrexate in 4 children were small and they were in a safe range , which could reduce the frequency of monitoring.ConcIusion This method is simple, sensitive and accurate for methotrexate detection in serum.The children with stable concentration and within safety range, can reduce monitioring frequency.It could bring the children less pain and relieve the burden of family.
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Objective To investigate effect of high glucose on the function of endothelial and the underlying mechanisms in human umbilical vascular endothelial cells (HUVECs).Methods The experiment was divided into 4 groups: normal group (NG), low dose group (LG), middle dose group (MG) and high dose group ( HG) .The concentration of glucose in the culture medium was 5.5, 10, 20, 30 mmol/L in the 4 groups, respectively.The HUVECs was cultured for 0, 24, 48 h.At different time point, the cell viability were measured by MTT.The secretary content of nitric oxide (NO) in the supernatant were detected using test kit.The extraction of protein were extracted for Western blot analysis to detect the expression of endothelial nitric oxide synthase (eNOS).ResuIts Compared with normal group at same time point (cultured for 24 h), the cell viability and the content of NO were significantly decreased in LG, MG(P<0.05).The expression of eNOS in HG were markedly reduced (P<0.01).Compared with normal group at same time point (cultured for 48 h), the cell viability decreased significantly in HG (P <0.05).The expression of eNOS were markedly decreased 11.91, 25.72 and 34.50% in LG, MG and HG, respectively.A rising trend of cell viability were found in NG, LG and MG, but a descending trend were found in HG within 48 h.ConcIusion The cell viability were significantly affected by high glucose.The endothelial dysfunction induced by high glucose may be associated with the reduction of eNOS and NO production.
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Objective To prepare butenafine hydrochloride plastics,investigate the prescription composition and make a quality control standard for the preparation.Methods Film-forming time and appearance quality as the evaluation index,the quality control standard of butenafine hydrochloride according to the Chinese pharmacopoeia two section ( 2010 edition ) was made.ResuIts The prescription of butenafine hydrochloride plastics was identified as:1%butenafine hydrochloride(w/w),10%glycerol(w/w),3%carbomer 971PNF(w/w),0.1% ethyl p-hydroxybenzoate(w/w),moderate anhydrous sodium sulfite(pH adjusting agent) and 95% ethanol (solution).The preparation was colorless,transparent and viscous semi-solid with pH4.5.A content determination method of butenafine hydrochloride with HPLC was established and the result was stable and reliable .ConcIusion The butenafine hydrochloride has several advantages such as preparation simply , stable property,application convenience and quality control.It is a potential preparation to develop.
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Objective To prepare pemirolast potassium nasal spray which could be used in treatment of allergic rhinitis and make a quality control standard for the preparation.Methods The preparation materials of nasal spray was selected which could meet the physical and chemical properties of pemirolast potassium as well as the characteristics of intranasal administration.The quality control standards for pemirolast potassium nasal spray was made according to the nasal spray quality standards for the formulation pH, property, loading capacity, total bottle spray times, puff volume, sedimentation volume ratio and detection of content of “Chinese Pharmacopoeia” two section (2010 edition).Results The formulation prescription of pemirolast potassium nasal spray was:0.1% potassium pemirolast, 0.8% CMC-Na, 0.01% benzalkonium bromide, glacial acetic acid ( pH adjusting agent) and the solution was 5% mannitol.The formulation was a white suspension, pH=7.The mean value of installed capacity was (25.12 ±0.16) mL and installed capacity of each bottle was above 23.75 mL(95%); total spray times of each bottle was above 160 sprays and spray volume was above 0.140 0 g/press; sedimentation volume ratio was 1, the above testing programmes of quality standard met the requirements and were controlled.The standard curve of pemirolast potassium reference substance was Y=81085X+15264(r=0.999 8), linearity range was 0.5~25.0μg/mL.The average recovery rate of pemirolast potassium sample was 99.39%, and precision met the requirements.The pemirolast potassium content of test sample was 99.2% of labeled amount.Conclusion The formulation prescription of pemirolast potassium nasal spray is suitable and the preparation is possessed several advantages such as stability, well-distributed spray, application convenience and quality controlled.Therefore, nasal administrated formulation of pemirolast potassium is potentially in further.
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Objective To investigate the extracting technology of the Northeast tussah pupa oil and analyze the composition of the oil. Methods The Northeast tussah pupa were crushed and dried at 60℃. The oil was extracted from the Northeast tussah pupa powder with super critical fluid extraction technology-CO2 (SFE-CO2) at the extracting temperature as 45 ℃,pressure as 50 MPa and operating time as 6 hours according to the results of homogeneous design. The composition of the oil was detected by gas chromatography (GC).Results The extracting rate of the oil from the Northeast tussah pupa powder was 17.93% (w/w)and the percent of compositions of the oil were C15:0 fatty acid 37.03%,hexadecanoic acid 5.63%,C17:0 fatty acid 32.81%,octadecanoic acid 1.79%,leic acid 3.75%,octadecadienoic acid 11.98% and α-1inoleic acid 7.00%. Conclusion The technology of SFE-CO2 can be used in extraction of Northeast tussah pupa with High extraction efficiency.