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Gambogic acid is the main active component of Garcinia hanburyi Hook. f. ，which can inhibit the growth of a variety of tumor cells. However ，its low solubility ，short half-life and poor stability limit its clinical application to a certain extent. In order to improve the above shortcomings and improve the bioavailability of gambogic acid ，many studies have used covalent binding and physical encapsulation methods to obtain a new gambogic acid delivery system with targeting ，high permeability ，stability， biocompatibility，in vivo long circulation and other properties ，such as polymer prodrug delivery system ，anoxic prodrug delivery system，magnetic field responsive prodrug delivery system ，multi environment sensitive prodrug delivery system ，bionic nano drug delivery system. This paper reviews the new drug delivery system and its characteristics of gambogic acid. The results show that the design of drug carrier has greatly improved the defects of gambogic acid ，and the introduction of more responsive groups into gambogic acid drug carrier may make it achieve better antitumor effect.
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Objective To establish an UPLC method for the determination of sinomenine in Sinomenine External Applied Powder. Methods The UPLC method was carried out on a C18 column by using acetonitrile-water-ethylene diamine (50:50:0.25) as mobile phase. The flow rate was 0.2 mL/min; the sample quantity was 2 μL; the detection wavelength was 283 nm. Results The peak time was within 1 min or so. The calibration curve of sinomenine was in the linear range of 34.2–2188.0 ng. Conclusion The method is simple, rapid, stable and reliable, which can be used for the determination of sinomenine in Sinomenine External Applied Powder.
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OBJECTIVE:To optimize the preparation technology of Sinomenine topical paste. METHODS:Using“initial vis-cous force”,“holding viscous force”and“peeling strength”as index,heating and stirring time (A,h),heating temperature (B,℃) and the sequence of adding composition (softening agent,blank matrix and sinomenine)(C) as influential factors,the preparation technology of Sinomenine topical paste was optimized by orthogonal test and verified. At the same time,the content of sinomenine was determined by HPLC method. RESULTS:The optimal preparation technology of Sinomenine topical pasta was as follows as adding blank matrix and sinomenine,and then adding softening agent,heating at 80 ℃,stirring for 1 h. In verification test,RSD of comprehensive score for 3 batches of samples were 2.09%(n=3);average contents of samples were 6.7 mg/g, which was in line with the requirement of ≥6.0 mg/g. CONCLUSIONS:The optimal preparation technology of Sinomenine topical pasta is reasonable,stable and feasible. The paste shows good adhesiveness and is qualified in content.
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OBJECTIVE:To explore the regularity of relative correction factor (RCF) in multi-components by single marker (QAMS). METHODS:With the source of CNKI,literature retrieval was used to collect the relevant documents of multi-compo-nents by single marker (QAMS) and extract the calculated values by quantitative analysis of multi-components by single marker QAMS and measured values by external standard method (ESM),SPSS 19.0 software was used to calculate the percentage value (RSD,%) of relative standard deviation between calculated values and measured values,and the correlation between RSD and RCF was analyzed by drawing a scatter plot. RESULTS:Most of RCF values distributed in the range of >0.62-1.53,accounting for 76.7%to all data. Calculated values and measured values showed high similarity in this range and the RSD<3.0%data account-ed for 88.8% to all data,which had good credibility. Meanwhile,the similarity of calculated values and measured values was influ-enced by the differences of structure and physicochemical property of parent nucleus between other components under measured and internal references. The high degree of similarity between calculated values and measured values were decisive by very similar struc-tures of parent nucleus;the low degree was decisive by discrepant structures;and the low degree was also decisive by very similar structures and discrepant physicochemical property of parent nucleus. CONCLUSIONS:RCF will affect the credibility of content de-termination results for components under measured in QAMS,it is necessary to establish database of RCF,RSD and related param-eters.
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Objective To evaluate the potential influencing factors associated with pathologic complete response ( pCR) after neoadjuvant chemoradiotherapy for locally advanced rectal cancer ( LARC) . Methods A retrospective analysis was performed on the clinical data 265 patients with stageⅡandⅢ( the 7th version of AJCC) rectal cancer admitted to our hospital from 2011 to 2013. All patients underwent neoadjuvant concurrent chemoradiotherapy ( CCRT ) followed by surgery with/or without induction chemotherapy during the interval between the complete of CCRT and surgery. The predictors associated with pCR were analyzed by univariate and multivariate logistic regression analyses. With the use of the independent predictive variables for pCR from multivariate analysis, a clinical risk score model was established according to the following criteria:no?risk group (0 factor);low?risk group (1 factor);high?risk group ( 2 factors) . Results Among these 265 patients, 50( 18. 9%) achieved pCR. The univariate analysis showed that carcinoembryonic antigen ( CEA) level before CCRT ( P=0. 017) , T stage before CCRT ( P=0. 001), interval between complete of CCRT and surgery (P=0. 000), and the maximum tumor thickness before CCRT ( P=0. 040) were significantly associated with pCR. The multivariate analysis showed that pre?CCRT CEA level ( P=0. 021 or 0. 446) and interval between the complete of CCRT and surgery ( P=0. 000 or 3. 774) were significant predictors of pCR. When stratifying for smoking status, only low pre?CCRT CEA level was significantly associated with pCR in the non?smoking patients ( P=0. 044) . For the prediction of pCR by the clinical risk score model, the sensitivity was 0. 805, the specificity was 0. 460, the area under the receiver operating curve was 0. 690 ( 95% CI= 0. 613?0. 767 ) , the positive predictive value was 35 . 4 9%, the negative predictive value was 8 6 . 5%, and the predictive accuracy was 7 3 . 9%. Conclusions For locally advanced rectal cancer, pCR can be achieved in some patients after neoadjuvant therapy. Low pre?CCRT CEA level and long interval time between CCRT and surgery are independent factors associated with pCR, and only low pre?CCRT CEA level is an associated factor in the group of nonsmokers. The clinical risk score model based on pre?CCRT CEA level>5 ng/ml and time interval from CCRT completion to surgery≤8 weeks can be used to predict pCR after neoadjuvant chemoradiotherapy for LARC.
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Objective To establish a method for the determination of content in Sinomenine Hydrochloride external applied powder. Methods Diamonsil ODS C_(18) (250 mm ? 4.6 mm, 5 ?m) column was used in HPLC with mobile phase of phosphate buffer (0.01 mol/L K_2HPO_4 solution, and 1%0 triethylamine, pH was adjusted to 3.0)-MeOH (80 : 20). The flow rate was 1.0 mL/min and the detection wavelength was 265 rim. Results The linear range of Sinomenine Hydrochloride was 0.446～4.46 ?g and the regression equation was Y=9.01 ? 10~6X+102803 (r=0.9999). The average recovery was 99.2%, RSD=0.68% (n =9). Conclusion This method is rapid and accurate with good reproducibility. It can be applied to control the quality of Sinomenine Hydrochloride external applied powder.
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Objective To establish the optimum preparation process for Syrigopicroside Dropping Pills.Methods The preparation conditions,such as the proportion between the extracts and matrix,dripping temperature,the ratio of matrix,were studied with orthogonal test.The obtained results were tested by three indexes,such as the variation coefficient of weight of pill,time limit of dissolution and appearance of the dropping pills with analysis of variance.The preparation process was optimized.Results The optimal technical conditions were as follows:the ratio of PEG4000 and PEG6000 as matrix was 4∶1,the ratio of syrigopicroside to matrix was 1∶4,and the dripping temperature was 80 ℃.Conclusion The preparation technology can meet the requirement for dripping pill specified in China Pharmacopeia(2005 Edition).