ABSTRACT
Aim To study the effect of pectin-adriamy-cin conjugate ( PAC) on cardiac toxicity .Methods 50 female SD rats were randomly divided into 5 groups with 10 animals in each group .Adriamycin ( ADM ) group received 3 mg? kg -1 , ip, every other day for 6 times.PAC group received ADM equivalent 1.5,3 and 6 mg? kg -1 , ip, every other day for 6 times.Control group received normal saline parallel to ADM .Rats were sacrificed and the echocardiogram , cardiac en-zymes , the oxidative stress levels in myocardial cells and histopathological changes after 48 h administration were detected.S180 ascites tumor bearing mice models were established to investigate the antitumor activity of PAC.Results The survival rate of ADM group was 50% and that of PAC each group was 100%.PAC could significantly increase body weight ,heart index and immune index and increase HR ,EF,FS,reduce LVIDd, LVIDs.PAC could also significantly increase the AST , LDH, CK, CK-MB level in serum .GSH-Px and SOD activities of PAC group were significantly increased and MDA contents were reduced , and histopathological changes decreased .PAC could effectively inhibit the growth of tumor cells and extend the survival period of mice.Conclusion PAC induces a significant reduc-tion in cardiotoxicity by increasing survival rate , im-mune and cardiac function , improving cardiac en-zymes ,oxidative stress and myocardial cell injury , and also PAC has obvious antitumor effect .
ABSTRACT
Pectin, a polysaccharide extracted from the cell wall of plants, was used as the drug carrier to synthesize the pectin-adriamycin conjugates (P(A)n). The structure of the conjugates was confirmed by UV and IR. The degree of esterification (DE) of the pectin was assessed, and it was found that DE significantly influenced the carboxy group contents, inherent viscosity and galacturonic acid contents of the pectin. The results of drug release test in vitro showed that the conjugate was stable in normal saline, but was gradually enzymolyzed to release the adriamycin in blood plasma and in lymph nodes. The results of lymphatic targeting study of P(A), demonstrated that the modification of DE or drug coupling capacity of pectin significantly influenced the lymphatic targeting characteristics of P (A)n. The adriamycin concentration of lymph nodes was 208 times higher than that of plasma after local injection of the P(A)n, of which the adriamycin content was 27.9% and the pectin was deesterificated 120 minutes by the use of hypothermy alkaline deesterification method.
Subject(s)
Animals , Rabbits , Antibiotics, Antineoplastic , Pharmacokinetics , Doxorubicin , Pharmacokinetics , Drug Carriers , Chemistry , Esterification , Lymph Nodes , Metabolism , Pectins , PharmacokineticsABSTRACT
OBJECTIVE:To establishment the method for the determination of content of vitamin A palmitate(VAP) and its related substances by HPLC. METHODS:The HPLC conditions were consisted of Phenomenex Luna C18 column with a mobile phase of a mixture of acetonitrile-isopropanol (90∶10) ,the detection wavelength of 328 nm,the column temperature of 30 ℃ and the flow rate of 1.0 mL?min-1. RESULTS:VAP was completely separated from impurities,the linearity range was 90～400 mg?L-1(r=0.999 2). The average recovery rate was 99.60% (RSD=1.32%). The average content of the related substances were lower than 2.53% . CONCLUSION: This accurate and reliable HPLC method is applicable for the quality control of VAP.
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OBJECTIVE:To establish an RP-HPLC method for content determination of s-omeprazole sodium and its related substances.METHODS:The separation of s-omeprazole sodium and the related substances was carried out on a Phenomenex Luna C18 column,the mobile phase consisted of methanol-0.033 mol?L-1 ammonium dihydrogen phosphate-triethylamine (58∶41.8∶0.2,adjusted to pH 7.0 by phosphate acid).The detection wavelength was 302 nm,the flow rate was 1.0 mL?min-1,the column temperature was 25 ℃,and the sample size was 20 ?L.RESULTS:The linear range of omeprazole sodium was 10～500 mg?L-1 (r=0.999 7).The average recovery rate was 100.27% (RSD=0.74%).The average content of the related substances in samples was 0.42%.CONCLUSION:This method is simple,accurate,specific and applicable for content determination of s-omeprazole sodium and its related substances.
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OBJECTIVE: To establish a HPLC method for the determination of content of entecavir and its related substances. METHODS: The HPLC condition was consisted of a Luna C18 column with a column temperature at 25 ℃, using gradient eluate method, the mobile phase was acetonitrile,with a flow rate of 1.0 mL?min-1 and detection at 254 nm. RESULTS: The calibrated linear curve of entecavir was within 0.033 45～0.167 2 mg?mL-1(r=0.999 98). The average recovery was 100.09%,RSD=0.20%, The content of related substance was 0.54%～1.48%. CONCLUSION: This accurate and reliable HPLC method is applicable for the quality control of entecavir and its related substances.