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Objective To investigate the clinical curative effect of α-lipoic acid combined with lipid microsphere alprostadil in treating elderly early diabetic kidney disease .Methods One hundred and sixty-four cases of early diabetic kidney disease treated in this hospital from January 2014 to January 2016 were selected and randomly divided into the experimental group and the control group according to the random number table method ,82 cases in each group .The control group was given lipid microsphere alpros-tadil ,while on this basis the experimental group was added with α-lipoic acid .The various biochemical indexes ,clinical efficacy and subcutaneous bruising ,fundus event occurrence were compared between the two groups .Results The levels of U-RBP and NAG after treatment in the two groups were significantly decreased compared with before treatment ,the difference was statistically sig-nificant (P<0 .05) .Although other indicators such as serum Scr ,BUN ,CysC andβ2-MG had different degrees of decline ,but the difference was not statistically significant (P>0 .05) .The effective rate in the experimental group was 91 .46% ,which was signifi-cantly higher than 78 .05% in the control group ,the difference was statistically significant (P<0 .05) .Subcutaneous bruising and fundus events in the experiment group had the increasing trend ,but the difference between the two groups had no statistical signifi-cance (P>0 .05) .Conclusion α-lipoic acid combined with lipid microsphere alprostadil in treating elderly early diabetic kidney dis-ease can better improve glomerular and renal tubular function .
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OBJECTIVE: To prepare freeze-dried alprostadil lipid microspheres and investigate their stability and pharmacokinetic characteristics. METHODS: The alprostadil lipid microspheres were prepared by two-step emulsifying method and then freeze-dried. The physicochemical properties were characterized.The stability in vitro and pharmacokinetics in Beagle dogs were also studied. RESULTS: The freeze-dried alprostadil lipid microspheres presented a good appearance and the rehydrated time was short. The size after reconstruction was (164.1±3.9) nm, the encapsulation efficiency was (92.5±3.3)% and the content of PGA1 was (1.38±0.21)%. It showed good stability after storing for 6 months as indicated by the size and contents of alprostadil and PGA1. After intravenous injection in Beagle dogs, the half time and peak time were (7.5±3.7) and (7.6±2.9) min respectively, and the peak plasma concentration of PGE1 was (105±40.4) ng·L-1, which was similar to the reference formulation. CONCLUSION: The freeze-dried alprostadil lipid microspheres can significantly improve the stability of alprostadil lipid microspheres with good pharmacokinetic characteristics, which indicates a promising prospect in clinic use.
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Lipid microsphere drug delivery system is a hot issue in pharmceutics studies .In this paper , the mechanism , prep-aration method and the key influence factors of lipid microsphere drug delivery system were reviewed respectively .Some new discovery and development were introduced in order to enhance the development and application of lipid microsphere drug delivery system as a drug delivery tool .
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OBJECTIVE: To prepare stable flurbiprofen axetil lipid microsphere for intravenous injection. METHODS: The optional formulation and prepared procedure were obtained through the single factor and crosscut design of experiment, and the stability constant of centrifugation Ke, particle size, Zeta potential, the pH of the product were studied. RESULTS: The optional formulation and procedure were 10% soybean oil for intravenous injection, 1.2% soybean lecithin, 0.6% F68, 0.4% oleic acid, 2.0% glycerol and 90% water for injection. pH was adjusted to 8.0 before homogenization and the sample was homogenized at a pressure of 80 MPa for 6 times. Finally, the lipid microspheres were sterilized for 15 min by sterilizing at 121°C and exhibited good stability after sterilization. The content of Flurbiprofen Axetil lipid microspheres was 95.59%. CONCLUSION: The preparation process is feasible to prepare lipid microsphere with good physical stability.
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OBJECTIVE: To investigate whether substituting the solubilizer with lipid microspheres in vitamin K1 injection can eliminate the anaphylactoid reaction.
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Objective: To compare the pharmacokinetics in rats and tissue distribution in mice of tanshinone IIA (TNS) lipid microsphere and sodium tanshinone IIA silate (STS) injection after iv injection. Methods: A sensitive and specific RP-HPLC method was established to determine the concentration of TSN and STS in rat plasma and mice tissue. The TSN and STS levels in plasma of rats and tissues of mice were compared after iv single dose administration of TSN lipid microsphere (5.40 mg/kg) and STS injection (7.27 mg/kg), and the results were fitted by pharmacokinetic and statistic analyses. Results: The bioavailability (AUC0-∞) and peak concentration (Cmax) values of TSN were 2.14 and 2.22 folds as those of STS, the clearance (CL), apparent volume of distribution (V), and mean repair time (MRT) values of TSN were lower (P < 0.01), and other pharmacokinetic parameters had no significant deviation. The results on the tissue distribution of TSN and STS in mice showed that the contents of TSN in heart, liver, spleen, lung, and kidney tissues were 1.94, 0.11, 0.98, 1.65, and 0.28 folds as those of STS with the same molar dose, and the content of TSN in brain tissue increased more significantly than that of STS which has not been detected. Conclusion: The pharmacokinetics and tissue distribution of TSN and STS at the same molar dose have significant differences, the AUC and Cmax values of TSN are higher, and the concentration of TSN could be increased in heart, brain, and lung tissues significantly, compared with those of STS.