OBJECTIVE:To prepare and characterize lansoprazole(LAP) cationic liposomes. METHODS:Liposomes were prepared by ethanol injection technique.An orthogonal test was utilized to optimize the formulation and preparation of LAP liposomes.The encapsulation efficiency was determined by ultrafiltration.The morphological examination of LAP liposomes was performed using transmission electron microscopy.The particle size and Zeta potential of the liposomes were measured.The release rate of LAP from liposomes was tested. RESULTS:The liposomes with spherical or ellipsoidal shape and better stability featured the encapsulation efficiency of(80?1.23)%,the mean partical size of (184?21)nm,and Zeta potential of (36.1?5)mV.The release kinetics in vitro obeyed first-order equation.The stability of LAP was better. CONCULSION:The selected formulation and preparation technic of lansoprazole liposomes were rational and stable and liposomes featured a sustained release in vitro.

OBJECTIVE: To establish a method for determining the entrapment efficiency of gemcitabine hydrochloride liposomes(GHL).METHODS: The liposome and the free gemcitabine hydrochloride were separated by ultrafiltration,and the content of free gemcitabine hydrochloride was determined by HPLC.The entrapment efficiency of gemcitabine hydrochloride liposomes was computed as well.RESULTS: The recovery rate in ultrafiltration methods was 97.8%～100.1% for blank substance versus 99.0%～100.1% for sample.The linear range of gemcitabine hydrochloride was 1.0～80.0 mg?L-1(r=0.999 3) and its average recovery rate was 98.7～101.2%,and its inter-day and intra-day RSD were all less than 3% and its average entrapment efficiency was 81.21%.CONCLUSION: The method is simple,accurate and applicable for the determination of the entrapment efficiency of gemcitabine hydrochloride liposomes.

OBJECTIVE: To investigate the effect of poloxamer 188 as co-emulsifier on the pharmaceutical property of emulsion.METHODS: Diclofenac sodium was used as model drug and poloxamer 188 as co-emulsifier,the emulsion was prepared by high pressure homogen-colostrum pH adjusting method,with its entrapment efficiency,particle size,?-electric potential etc determined.RESULTS: The emulsion which was added with poloxamer 188 showed decreased entrapment efficiency and ?-electric potential but increased particle size as comapred with the one without poloxamer 188.CONCLUSION: The pharmaceutical property of emulsion wouldn't necessarily be enhanced by adding poloxamer 188 as co-emulsifier.

OBJECTIVE:To develop a method for determining the entrapment efficiency of tetracaine hydrochloride liposome.METHODS:The microcolumn centrifugation was adopted to separate the free tetracaine hydrochloride from liposomes;the content of tetracaine hydrochloride was determined by HPLC and the entrapment efficiency was computed.RESULTS:By microcolumn centrifugation,the liposomes and the free tetracaine hydrochloride were well-separated.The recovery rate of the blank liposomes was 90.4%～100.1%;the absorption rate of free tetracaine hydrochloride was 96.6%～99.2%;and the entrapment efficiencies of tetracaine liposomes stood at about 80%.CONCLUSION:This method established for determining the entrapment efficiency of tetracaine hydrochloride liposome is simple,rapid and reproducible.

Objective To prepare a harmine hydrochloride liposome formulation with high encapsulation efficiency. Methods Preformulation investigation was carried out to obtain the drug physicochemical properties such as solubility and lgD in buffers of different pH value. Harmine hydrochloride was encapsulated into liposomes by active loading method. Encapsulation efficiency of liposomes was determined after the free drug was separated from liposome by ultrafiltration. The influence factors on the encapsulation efficiency including drug-lipid weight ratio, incubation temperature, pH value of external water phase were investigated. Results As the pH value increasing, the solubility of harmine hydrochloride was decreased, while the apparent oil-water distribution coefficient was increased. By active loading method, the encapsulation efficiency could be over 80% when the drug to lipid weight ratio was under 1∶5. The pH gradient between intervesicle and intravesicle obviously influenced the encapsulation efficiency, while incubation temperature had little effect on encapsulation efficiency. Conclusion Active loading is suitable for preparing harmine hydrochloride liposome with high encapsulation efficiency.

BACKGROUND:Total knee arthroplasty for knee osteoarthritis accompanied with extra-articular deformity is stil chal enging. An individual replacement plan should be designed to obtain good mechanical axis and to recover suitable soft-tissue balance. OBJECTIVE:To observe the safety and feasibility of individual y designed one-stage total knee arthroplasty for knee osteoarthritis combined with ipsilateral femoral extra-articular deformity. METHODS:A total of eight patients with knee osteoarthritis combined with ipsilateral femoral extra-articular deformity were enrol ed in this study. According to preoperative plan, five patients underwent intra-articular compensatory osteotomy, and the remaining three received extra-articular corrective osteotomy. Multi-planar deformities as wel as soft-tissue conditions were recorded. Main outcome measures included the hospital for special surgery score, Western Ontario and McMaster Universities Arthritis Index score and alignments deviation. RESULTS AND CONCLUSION:The patients were averagely fol owed up for 29 months. The hospital for special surgery score changed from preoperative 32.5 points to postoperative 87.5 points. The Western Ontario and McMaster Universities Arthritis Index score was increased from preoperative 37.1 points to postoperative 88.8 points (P<0.05). Mean mechanical axis deviation (either varus or valgus) changed from preoperative 17.1° to postoperative 1.4° (P<0.05). Al cases with extra-articular corrective osteotomy healed within 3 months, and none had postoperative infection, loosening or venous thromboembolic events. One patient was with 5° residual knee anti-sheets. Results verified that one-stage total knee arthroplasty procedures are effective in the treatment of knee osteoarthritis accompanied with ipsilateral femoral extra-articular deformity in accordance with individual preoperative plan.

OBJECTIVE:To study the effect of oil phase,emulsifier and drugs on reverse microemulsion.METHODS:Pseudo-ternary phase diagram was adopted to study the effect of Span-80/Tween-80(emulsifier),thymopentin(model drug), long-chain glyceride,medium-chain glyceride,non-glyceride(oil phase).on the preparation of reverse microemulsions.Optimal formula of reverse microemulsions was selected.RESULTS:The largest water-in-oil(W/O)area was obtained in reverse microemulsion which was prepared using medium-chain glyceride as oil phase.Final formula was confirmed and contained distilled water/ Span-80/Tween-80/caprylic/capric triglyceride(2∶3∶6∶9).In addition,thymopentin was incorporated into the aqueous phase.CONCLUSIONS:The preparation of reverse microemulsions will be influenced by emulsifier,constitution of oil phase and drug.The influence factors for the actual preparation of reverse microemulsions should be optimized.

Objective:To summarize the clinical features, genetic testing and treatment efficacy of 6 children with Dent disease.Methods:Six children diagnosed with Dent disease in Guangzhou Women and Children′s Medical Center from January 2014 to March 2019 were enrolled.Their medical history, clinical manifestations, laboratory results, genetic test results, and proteinuria level, calciuria level and renal function after medication were measured.Results:All patients were male, with the onset age ranged from 1 to 9 years old.They were followed up for 6 months to 4 years.All the children had low molecular weight proteinuria.Urine protein electrophoresis showed that the ratio of low molecular weight proteinuria in only 2 cases was more than 50%.Renal biopsy suggested that all cases were combined with glomerular lesions.Five cases had hypercalciuria.Under the microscope, there were 5 cases of hematuria.Two case had rickets, and there was no renal calcium deposition and hypophosphatemia.Five cases were detected with CLCN5 mutations, of which p. C160Yfs*49 and p. G523D were first reported.One case had an OCRL1 mutation.Patients were treated with Hydrochlorothiazide and angiotensin converting enzyme inhibitor (ACEI). The 24 h urinary calcium level after treatment was lower than that before treatment [0.40 (0.24, 0.43) mmol/kg vs.0.12 (0.11, 0.14) mmol/kg, U=2.00, P<0.01]. However, there was no significant decrease in the 24 h-urinary protein level before and after treatment [77.09 (62.41, 88.01) mg/kg vs.80.33 (66.03, 92.52) mg/kg, U=12.00, P>0.05]. Conclusions:Dent disease is mainly characterized by low molecular weight proteinuria, and some patients may not be associated with hypercalciuria.Gene tests help to identify the disease type.ACEI and Hydrochlorothiazide can reduce the urinary calcium level, but cannot improve the level of urinary protein.

Objective To explore the effect of urine neutrophil gelatinase-associated lipocalin(uNGAL) and urine interleukin-18(uIL-18) on the ill condition and prognosis in critically ill patients with acute kidney injury (AKI) at inception of continuous veno-venous hemofiltration (CVVH).Methods Children came from Department of Nephrology,PICU and health examination center in Guangzhou Women and Children's Medical Center were divided into 4 groups:critically ill patients with AKI receiving CVVH group(group A),critically ill patients with non-AKI receiving CVVH group(group B),critically ill patients with AKI didn't recevie CVVH group(group C),and healthy control group(group D).Serum creatinine(SCr),uNGAL and uIL-18 in all patients were analyzed.Results The uNGAL in group A and group C [(161.56 ± 71.44) μg/L,(153.69 ±51.33) μg/L] increased obviously when compared with group B and group D [(33.50 ± l 0.76) μg/L,(16.37 ± 6.20) μg/L] (all P ＜ 0.05).The uIL-18 in group A and group C[(4.16 ±1.13) μg/L,(3.81 ± 1.05) μg/L] was higher than that in group B and group D [(0.25 ± 0.04) μg/L,(0.19 ± 0.15) μg/L] (all P ＜ 0.05).There was no significance of uNGAL and uIL-18 between group B and group D(all P ＞ 0.05).The peak level of uNGAL[(241.76 ± 53.60) μg/L vs (196.32 ± 39.28) μg/L] and uIL-18[(5.15 ±0.78) μg/L vs (4.30 ±0.89) μg/L] in critically ill patients with AKI was higher in renal recoveries than in renal non-recoveries(P ＜0.05).The levels of uNGAL and uIL-18 critically ill patients at initiation of CVVH were higher in non-survivors when compared with survivors [(213.50 ± 104.78) μg/L vs (79.91 ± 55.81) μg/L,P ＜ 0.05],[(4.48 ± 2.32) μg/L vs (1.94 ± 1.88) μg/L,P ＜ 0.05].The levels of uNGAL and uIL-18 of critically ill patients with AKI at initiation of CVVH were higher in non-survivors than in survivors [(256.99 ± 49.33) μg/Lvs (127.11 ±38.99) μg/L,P＜0.05],[(5.48±0.67) μg/Lvs (3.65 ±0.98) μg/L,P＜0.05].The levels of uNGAL and uIL-18 at the first diagnosis time of AKI were higher in non-survivors than in survivors (P ＜ 0.05).Conclusions uNGAL and urine IL-18 at commencement of CVVH predicts short-term prognosis in critically ill patients with AKI.uNGAL and urine IL-18 can be as a prognostic value in the prediction of the need for renal replacement therapy initiation or mortality in critically ill patients with AKI.

OBJECTIVE:To prepare bovine serum albumin(BSA)liposomes coated with N-trimethyl chitosan(TMC) and study the factors influencing the quality of the preparation.METHODS:BSA liposomes were prepared by the method of reverse-phase evaporation.TMC polymers for coating liposomes were synthesized by quaternary amination reaction between chitosan and methyl iodide.The TMC-coated BSA liposomes were prepared.The entrapment efficiency of BSA liposomes was determined by high speed centrifugation-Coomassie brilliant blue G-250 dye method.The effects of the composition ratio of soybean lecithin(PC):cholesterol(CH):phospbatidylserine(PS),the mass ratio of TMC to total lipid and the ionic strength on particle size and entrapment efficiency were investigated.RESULTS:All the factors investigated had influences on particle size and entrapment efficiency.The optimal formulation was as follows:PC:CH:PS was 8:9:1,TMC to lipid phase ratio was 0.25:1 and ionic strength was less than 20 mmol?L~(-1).The entrapment efficiency prepared in the above conditions was (46.82?2.07)%.CONCLUSION:The TMC-coated BSA liposomes were obtained successfully and the preparation had uniform particle size and good stability.