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OBJECTIVE: To prepare zedoary turmeric oil compound liposomes (ZTOC-LPS) and evaluate its quality.METHODS: The preparation method of liposome, the addition amount of soybean phosphatidylcholine (SPC), ratio of SPC to cholesterol (CH) in lipid, drug-lipid ratio of zedoary turmeric oil (ZTO), drug-lipid ratio of tretinoin in formulation, and water bath temperature were screened using encapsulation efficiency and drug-loading amount of ZTO (represented by germacrone) and tretinoin as investigation indexes. Quality evaluation and primary stability investigation were conducted for liposomes prepared by optimal preparation technology. RESULTS: The optimal preparation method was ethanol injection method; The optimal preparation technology were SPC 4 mg in 1 mL lipid, the mass ratio of SPC to CH 3:1, the ratio of ZTO to lipid 1:9, the ratio of tretinoin to lipid 1:70, water bath temperature of 55 ℃. Encapsulation efficiencies of ZTO and tretinoin were (64. 63 ± 1. 00)％ and (90. 33 土 0. 72)％ in 3 batches of ZTOC-LPS, respectively. Drug-loading amount of ZTO and tretinoin were (9. 09 ± 0. 14)％ and (1. 43 ± 0. 02)％, respectively. Particle size was (257. 41 ± 7. 58) nm, Zeta potential was (-38. 77 ± 0. 81) mV,PDI was 0. 10 ± 0. 04; the results of centrifugal acceleration test showed that the liposomes had good physical stability. No obvious change was found in each investigation index of ZTOC-LPS that stored at (4 ± 2) ℃ for 1 month. CONCLUSIONS: Established preparation technology is simple and feasible, the quality of the prepared ZTOC-LPS conforms to the requirements, and it can provide reference for the following research of ZTOC-LPS.
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OBJECTIVE:To investigate toxic reaction of Compound zedoary turmeric oil cream in experimental rats with long-term consecutive transdermal administration,and to provide reference for safe use of it in the clinic. METHODS:60 SD rats were randomly divided into blank control (cream matrix) group,Compound zedoary turmeric oil cream intact skin and damaged skin low-dose and high-dose(5%,10%)groups,with 12 rats in each group,half male and half female. All of them were given relevant medicine twice a day. 92 d consecutive medication later,general situation of rats were observed,and body weight,blood routine(WBC,RBC,HGB,LYMPH,etc.)and blood biochemical indicators(AST,ALT,PA,etc.)were all detected;systemati-cal observation of organs,organ coefficient calculation and histopathology examination were carried out. RESULTS:There was no statistical significance in those indicators between Compound zedoary turmeric oil cream groups and blank control group (P>0.05),except hemoglobin decreased in intact skin low-dose group,while hemoglobin decreased,LYMPH and PA increased in dam-aged skin high-dose group(P<0.05). Pathology results showed that Compound zedoary turmeric oil cream had no significant toxici-ty for the main organs. CONCLUSIONS:Compound zedoary turmeric oil cream has no long-term toxicity to experimental rats.
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OBJECTIVE: To investigate the effects of compound preparation of Cordyceps sinensis and Tripterygium hypoglaucum (CSTHC) on survival time of grafted pigskin after allogeneic transplantation and its mechanism. METHODS: The pigskin was treated with CSTHC solution before allogeneic transplantation, and CSTHC ointment was applied for external use on the grafted pigskin after skin transplantation. Cyclosporine A (CsA) and normal saline were served as control. The survival time, the appearance and the histomorphological changes of the grafted pigskin were observed. The histomorphological changes of testicles in pigs were also examined. The CD4 and CD8 expressions in the grafted pigskins were measured by immunohistochemical method. The white blood cell count in peripheral blood and the liver and renal functions were also examined. RESULTS: The survival time of the grafted pigskin in the CSTHC-treated group was (28.50+/-3.26)d, which was much longer as compared with (10.60+/-1.52)d in the untreated group (P<0.01). The survival time of the grafted pigskin in the CsA-treated group was (28.33+/-3.50)d, and there was no remarkable difference in the survival time of the grafted pigskin between the CsA-treated group and the CSTHC-treated group. The expressions of CD4 and CD8 were lower in the CSTHC-treated group than those in the untreated group on the 7th and 14th day after skin graft (P<0.05), while there was no significant difference in the indices between the CSTHC-treated group and the CsA-treated group. The WBC count was higher in the untreated group than that in the CSTHC-treated group or CsA-treated group on the 7th day after skin graft (P<0.05). CONCLUSION: CSTHC can prolong the survival time of allogeneic grafted pigskin. Its mechanism of inhibiting the immunological rejection may relate to decreasing the expressions of CD4(+) and CD8(+) in the grafted pigskin and reducing the local inflammatory reaction.
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OBJECTIVE:To detect the blood drug level of digoxin in order to offer reference about clinical safety and utility and rational use of cardiac glycoside drugs. METHODS: The plama concentration of digoxin was determined by fluorescence polarization immunization, and the monitoring rssults were subjected to statistical analysis. RESULTS: Of the total 126 cases who treated with digoxin, the blood drug concentration in 32(25.4%) was above 2.0 ng?mL-1,and it was 0.8～2.0 ng?mL-1 in 83(65.9%) and less than 0.8 ng?mL-1 in 11(8.7%); Toxic symptoms were noted in 16 cases(12.7%). CONCLUSION: To ensure clinical efficacy and reduce incidence of toxic reactions, it is of great importance to monitior the blood drug level and formulate individual dosage regimen.
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OBJECTIVE:To study the pharmacokinetics of emodin(an active component of Qingyi-Ⅱgranula) in rats after i.g administration of Qingyi-Ⅱgranula.METHODS:Rats were i.g administered with Qingyi -Ⅱgranula(2.5 g?kg~(-1) and 5.0 g?kg~(-1)).Serum concentrations of emodin were determined at different time points by HPLC,and the pharmacokinetic parameters were computed.RESULTS:The pharmacokinetic parameters of emodin in rats after administration of Qingyi-Ⅱgranula(2.5g?kg~(-1) and5.0g?kg~(-1)) were asfollows:t_(1/2?):(9.468?8.46) hand(21.68?17.867) h;t_(1/2?):(15.388?5.46) h and.(39.63?24.39) h;t_(max):(2.500?3.479) h and(5.333?3.266) h;C_(max):(0.058?0.004) mg?L~(-1)and(0.101?0.007) mg?L~(-1);CL:(33.027?9.365) L?h~(-1)?kg~(-1) and(9.405?5.846) L?h~(-1)?kg~(-1);AUC_(0-∞):(0.652?0.201) mg?h~(-1)?L~(-1)and (1.364?0.267) mg?h~(-1)?L~(-1).The pharmacokinetic process was in line with two-compartment model.CONCLUSION:The method for the detection of serum concentration of emodin in rats and the related pharmacokinetic parameters had been established in our study,which serves as a theoretic basis for the pharmacokinetic study of Qingyi-Ⅱgranula.
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Objective To establish a determination method for the hyperoside in Jintu Liangguang Capsules. Methods Reverse-phase HPLC with Dikma Diamons C18 column was applied. The chromatographic conditions were as follows:methanol-0.025 mol/L of thophosphoric acid (40 ∶60) as the mobile phase,detection wavelength at 370 nm,column temperature set at 40 ℃and the flow rate being 0.8 mL/min. Results The linear range of calibration curve was 0.303 ～1.818 ug/uL for the hyperoside (r=0.999 6). The average recovery was 95.2 %and RSD was 1.3 %. Conclusion The method is simple and accurate,and can be used for quantitative analysis of Jintu Liangguang Capsules.