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OBJECTIVE:To prepare Tacrolimus niosomes (Tac-NS) and evaluate their characteristics in vitro. METHODS:Tac-NS were prepared by a film hydration-ultrasonic method. Using the comprehensive score of encapsulation efficiency (EE%), drug-loading amount,mean particle size and PDI as the evaluation index,orthogonal design was used to optimize the concentration of sorbitan monostearate(Span-60),mole ratio of Span-60 to cholesterol,mole ratio of Span-60 to SDC. The morphology,mean particle size,PDI,Zeta-potential and EE%of Tac-NS were investigated. Accumulative percutaneous penetration(Q)and accumula-tive retention amount(Qs)of Tac-NS and physical mixture of Tac and NS were compared by percutaneous penetration test in vitro. RESULTS:The optimal formulation was as follows as Span-60 0.025 mol/L,mole ratio of Span-60 to cholesterol 10∶1,mole ratio of Span-60 to SDC 15∶1,drug-loading amount of 5%. Tac-NS was spherical and distributed evenly,but hardly congregated.The mean particle size,PDI,Zeta-potential and EE% were (233.0 ± 6.48) nm,0.266 ± 0.021,(-41.7 ± 0.32) mV and (76.83 ± 4.61)%,respectively. The results of in vitro permeability study showed that Qs of Tac-NS was 2.4 times of physical mixture;in ad-dition,Q of the two were similar. CONCLUSIONS:Tac-NS,owning high EE%,small particle size,uniform distribution and ide-al permeation effect,is prepared successfully.
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Objective To compare the curative effect of perindopril and metoprolol in the treatment of diabetic patients with asymptomatic cardiac insufficiency.Methods According to the method of random numbers, 152 diabetic patients with asymptomatic cardiac insufficiency were divided into the observation group and control group,with 76 cases in each group.The observation group was given with perindopril treatment,while control group was given with metoprolol treatment.The cardiac function index,glycosylated hemoglobin,BNP levels,the incidence of cardiac insufficiency and the occurrence of adverse drug reactions before and after treatment were compared.Results There were no significant differences in LVEF,Tei index and E/A between two groups before treatment (all P >0.05 ).Compared with before treatment,the cardiac function indexes of the two groups were significantly improved after treatment(t=5.96,4.83,4.91,10.22,5.68,5.18,all P0.05),and the difference between the two groups was not statistically significant(all P>0.05).The BNP levels of the observation group before and after the treatment were (515.43 ± 58.85)pg/mL and (214.43 ±32.42)pg/mL respectively,of which the control group were (513.94 ±59.11)pg/mL and (263.32 ±43.31)pg/mL respectively,and after treatment,the BNP levels of the two groups were significantly decreased(t=23.45,17.68,all P0.05).Conclusion Using perindopril in treatment of diabetic patients with asymptomatic heart function can obviously improve cardiac function,reduce the incidence of BNP and cardiac insuffi-ciency.It has the clinical curative effect and high safety.
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OBJECTIVE:To determine and to compare the content of salvianolic acid B and tanshinoneⅡ A in compound danshen tablets and its drop pills.METHODS:The determination was performed on Eclipse XDB-C 18 with column temperature at30℃,the mobile phases were methanol-0.2%phosphoric acid solution(40∶60)and methanol-water(85∶15),respective_ ly with the flow rate at1.0ml/min and the detective wavelength at280nm.RESULTS:Good linear relations were obtained when the sample size of salvianolic acid B and tanshinoneⅡ A were within the range of0.1?g～2.0?g(r=0.9998for salvianol_ ic acid B and r=0.9999for tanshinoneⅡ A );The average recoveries of salvianolic acid B and tanshinoneⅡ A of compound danshen tablets were100.7%(RSD=1.9%)and101.0%(RSD=1.5%),respectively;And those for the compound danshen drop pills were98.6%(RSD=1.2%)and98.8%(RSD=1.4%),respectively.CONCLUSION:The method was accurate,re?liable and reproducible.The contents of salvianolic acid B and tanshinoneⅡ A in compound tanshen tablets are higher,while no fixed quantity were detected in the above2components in compound danshen drop pills.