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To analyze the effect of radiofrequency ablation on serum parathyroid hormone, biochemical index, blood routine test, EPO dosage, kt/V and urea decrease rate in uremic patients with secondary hyperparathyroidism. From January 2013 to May 2016, 40 patients with uremia secondary hyperparathyroidism and radiofrequency ablation were selected to analyze the whole serum parathyroid hormone, biochemical indicators, blood routine, EPO dosage, kt/V, urea reduction rate, albumin (ALB), total cholesterol (TC), triglyceride (TG), body mass index (BMI) before and after treatment, triceps brachii skinfold thickness (TSF), upper arm muscle circumference, serum iron, ferritin, C-reactive protein (CRP) changes. the adverse symptoms were significantly improved before and after treatment, the difference was statistically significant (P; After treatment, the level of parathyroid hormone in the whole segment decreased significantly, and the level of calcium and phosphorus in the blood of the patients was stable three months and six months after treatment, which was statistically significant compared with that before treatment (P < 0.05); after treatment, the amount of EPO in the patients decreased significantly, the difference was statistically significant (P < 0.05). After three months of treatment, ALB level was significantly higher than before treatment (P < 0.05), TG level was significantly lower than before treatment (P < 0.05), BMI and TSF levels were significantly higher than before treatment (P < 0.05). There was no significant difference in serum iron, ferritin and CRP levels between before and after treatment (P > 0.05). radiofrequency ablation is effective in the treatment of uremic patients with secondary hyperparathyroidism. Although it has little effect on the decrease rate of kt/V and urea, less bleeding, less risk and operation time, it can effectively reduce the level of parathyroid hormone in the whole blood, stabilize the level of calcium and phosphorus in the blood and the equality of HB water, reduce the amount of EPO, improve the nutritional status and anemia of the patients, and the treatment effect is good. [ABSTRACT FROM AUTHOR]

The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complex of tamibarotene with hydroxypropyl-β-cyclodextrin (Am80-HP-β-CD) was prepared through a freeze-drying method at the mole ratio of 1:1 (Am80: HP-β-CD). Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) indicated the formation of Am80-HP-β-CD. In vitro dissolution studies showed that the solubility and dissolution percentage of Am80-HP-β-CD was improved substantially compared to Am80. An improved dissolution with approximately 97% drug release in 3 min was observed, in comparison with Am80 with approximately 60% release in 45 min. In vivo studies indicated that the AUC0-∞ has increased 2.79 times and the Cmax 4.37 times after the formation of inclusion complex. The decrease of tmax indicated the Am80-HP-β-CD inclusion complex can be absorbed into blood faster. In short, the solubility and bio-availability of Am80 has notably increased with the complexation of HP-β-CD.Therefore, using the inclusion technique is a promising method to improve the solubility of insoluble drugs. [ABSTRACT FROM AUTHOR]

Temozolomide plays a critical role in curing glioma at present. The purpose of this work was to develop a suitable drug delivery system which could prolong the half-life, improve the brain targeting, and reduce the systemic effect of the drug. Temozolomide-liposomes were formulated by the method of proliposomes. They were found to be relatively uniform in size of 156.70 ± 11.40 nm with a narrow polydispersity index (PI) of 0.29 ± 0.04. The average drug entrapment efficiency and loading capacity were 35.45 ± 1.48% and 2.81 ± 0.20%, respectively. The pH of temozolomide-liposomes was 6.46. In vitro release studies were conducted by a dynamic dialysis. The results showed that temozolomide released slowly from liposomes compared with the solution group. The release behavior of temozolomideliposomes was in line with First-order kinetics and Weibull equation. The pharmacokinetics study was evaluated by pharmacokinetics parameters. The t1/2β and MRT of temozolomideliposomes were 3.57 times and 1.27 times greater than that of temozolomide solution. The Cmax and AUC values of temozolomide-liposomes were 1.10 times and 1.55 times greater than that of temozolomide solution. The results of pharmacokinetics study showed temozolomideliposomes prolonged the in vivo circulation time and increased AUC. Furthermore, the biodistribution in mice showed that temozolomide-liposomes preferentially decreased the accumulation of temozolomide in heart and lung and increased the drug concentration in brain after i.v. injection, which implied that temozolomide-liposomes improved the therapeutic effect in the brain and reduced the toxicity in lung and heart. [ABSTRACT FROM AUTHOR]

The aim of the current work was to develop generic sustained-release tablets containing 35 mg trimetazidine dihydrochloride and to establish an in vitro-in vivo correlation that could predict the bioavailability. The marketed sustained release tablet (Vastarel MR) used as reference, a sustained-release matrix tablet was prepared using hydroxypropyl methylcellulose (HPMC) as matrix by wet granulation and the in vitro dissolution profiles of the self-made tablets were determined in four different dissolution media (0.1 M HCl, pH 4.5 PBS, pH 6.8 PBS and water). A higher similarity between prepared tablets and Vastarel MR was established, with similarity factor (ƒ2) ranging from 60 to 75 in the four media. The in vivo pharmacokinetics was studied in six healthy beagles. Compared with Vastarel MR, the Cmax of self-made tablets was slightly decreased, while the Tmax and MRT0-t were slightly prolonged, but with no significant difference (P > 0.05). The average of relative bioavailability (F) was 102.52% based on AUC0-t. For log-transformed AUC0-t and Cmax, the upper confidence limit on the appropriate criterion is <0, indicating these two formulations were population bioequivalent. The in vivo-in vitro correlation coefficient obtained from point-to-point analysis of self-made tablets was 0.9720. In conclusion, the prepared tablets were bioequivalent to the marketed tablets, according to both the in vitro release rate and extent of absorption, and a good in vivo-in vitro correlation was established for the self-made tablets that indicated in vitro dissolution tests could be used as a surrogate for bioavailability studies. [ABSTRACT FROM AUTHOR]

The impact strength of nylon 6 (polyamide 6) can be improved by blending impact strength modifier at ambient temperature and then the applications of nylon 6 can be expanded widely. Polyamide (6) PA 6/poly(ethylene-1-octene) elastomer (POE)/poly(ethylene-1-octene) elastomer grafted by maleic anhydride (POE-g-MA) ternary blends were prepared in corotating twin-screw extruder by two kinds of extrusion processes, more than 10-fold increase of impact strength at ambient temperature was obtained from impact test of specimens, not at much expense of tensile properties. The influence of extrusion process, that is, one- and two-step extrusion, on the micromorphology of toughing nylon 6 blends was investigated systematically. Scanning electron microscopy was used to observe the fracture surfaces of bars prepared by injection-molding machine. In addition to particle size and distribution, interparticle distance (τ) between neighboring dispersed phase particles in PA6/POE-g-MA/POE ternary blends was calculated and used to characterize the micromorphology. Supertoughness was obtained in both ternary blends, and the interparticle distances (τ) were 0.228 and 0.179 µm, respectively, which were less than the critical τ c (0.3 µm) in nylon/rubber blends. The results showed that more homogeneous distribution of POE phase in nylon 6 matrix was found in blends prepared by two-step extrusion method, in which the average particle size of POE phase was 0.313 µm, while the average particle size in blends prepared by one-step method was 0.399 µm. The half-peak width of Gaussian distribution curve of particle size in blends prepared by one-step extrusion method was 0.278, which is higher than that of blends prepared by two-step method with the value of 0.248. [ABSTRACT FROM AUTHOR]

Vancomycin hydrochloride (VANH), the first glycopeptide antibiotic, is a water-soluble drug for the treatment of acute osteomyelitis. Liposomal formulations of VANH have already been manipulated and characterized, which was a mean of increasing their therapeutic index, reducing their toxicity and altering drug biodistribution. One of the challenges for preparing VANH-Lips is their low encapsulation efficiency (EE). In the present study, we aim to improve the liposomal formulation of VANH for higher EE, longer systemic circulation, reduced nephrotoxicity and enhanced antimicrobial activities. Vancomycin hydrochloride-loaded liposomes (VANH-Lips) were formulated by the method of modified reverse phase evaporation. Based on the optimization of formulation with orthogonal experimental design, the average drug encapsulation efficiency and the mean particle size of VANH-Lips were found to be 40.78 ± 2.56% and 188.4 ± 2.77 nm. In vitro drug release of VANH-Lips possessed a sustained release characteristic and their release behavior was in accordance with the Weibull equation. After intravenous injection to mice, the mean residence time (MRT) of VANH-Lips group was significantly prolonged in vivo and the AUC value was improved as well compared with the vancomycin hydrochloride solution (VANH-Sol) group. Furthermore, the biodistribution results in mice showed that VANH-Lips decreased the accumulation of VANH in kidney after intravenous injection. In conclusion, VANH-Lips may be a potential delivery system for VANH to decrease nephrotoxicity in the treatment of osteomyelitis. [ABSTRACT FROM AUTHOR]