Search

Two new complexes Zn(TBimE)Cl2 1 and Cd(TBimE)(I)2 2 based on a semi-rigid ligand TBimE (TBimE = (E)-1,2-bis(2-benzimidazolyl)ethane) have been synthesized and their structures have been determined...

To enhance in vitro dissolution of Cur by preparing Cur solid dispersions. The ability of HPMCAS-HF,HPMCAS-MF,HPMCAS-LF and PVPK30 to maintain supersaturated solution was investigated by supersaturation test. Amorphous solid dispersions were prepared by the solvent-evaporation method. The prepared samples were characterized using infrared spectroscopy( IR) and differential scanning calorimetry( DSC),and in vitro dissolution was investigated. DSC and IR results showed that in 1 ∶3 and 1 ∶9 solid dispersions,Cur was amorphously dispersed in the carrier,and the interaction existed between drug and carrier. The supersaturation test showed that the order of the ability of polymer to inhibit crystallization of Cur was MFHFLFK30. The dissolution results showed that Cur-K30 amorphous solid dispersion had the highest drug release rate; Cur-K30 and Cur-LF amorphous solid dispersions had a quicker but not stable dissolution rate,and the drug concentration decrease after 4 h; Cur-MF and Cur-HF solid dispersions had a low dissolution,which however increased steadily,attributing to the strong ability of the polymers to inhibit the crystallization of Cur. HPMCAS could inhibit the degradation of Cur better than K30,especially MF and HF. The amorphous solid dispersions of cur significantly enhanced the dissolution of Cur and improved the chemical stability of Cur. This study can provide a basis for the rational selection of the polymer used for Cur solid dispersion.

Background Acute uncomplicated lower urinary tract infection (UTI) is one of the most common bacterial infections. Patients usually present with dysuria, urinary urgency, urinary frequency and suprapubic pain or tenderness. Approximately 150 million people are diagnosed with UTI each year worldwide. The high recurrence rate of lower UTI is a common problem of clinical treatment. The misuse of antibiotics has led to the emergence of a number of resistant bacterial strains. Thus, traditional Chinese medicine is considered as an alternative option for treating acute uncomplicated lower UTI. Thus, this study aims to evaluate the efficacy and safety of Sanjin tablets (SJT) for the treatment of acute uncomplicated lower UTI; explore whether SJT can reduce or substitute the use of antibiotics and reduce the recurrence rate in the treatment of acute uncomplicated lower UTI. Methods/design In this study, a randomized, double blind, double dummy, parallel control of positive drug, multicentre clinical study will be established. A total of 252 patients with acute uncomplicated lower UTI (syndrome of dampness-heat in the lower jiao) will be randomly allocated in the ratio of 1:1:1 to three groups: experimental group, control group 1 and control group 2. The experimental group receives Sanjin tablets plus levofloxacin tablets (LT) placebo; the control group 1 receives LT plus SJT placebo; and the control group 2 receives SJT plus LT on the first 5 days, SJT plus LT placebo on the last 2 days. Each group will be treated for 7 days and followed-up for 1-2 times. The primary outcome measures of effective rate and recurrence rate are symptoms. Secondary outcome measures of effective rate and recurrence rate are the urine leukocyte, bacteriology examination and safety assessment. Outcomes will be assessed at baseline and after treatment. Discussion This study protocol will provide the research data of efficacy and safety of SJT for the treatment of acute uncomplicated lower UTI. The first aim is to determine whether Sanjin tablets can reduce the use of antibiotics; the second aim is to determine whether Sanjin tablets can substitute the use of antibiotics. The recurrence rate will be assessed after cured to determine whether SJT can reduce the recurrence rate. The results of this study will improve the rational use of drugs, especially the rational application of antibiotics. It will also enable safety evaluation from laboratory indices and adverse events, which will provide reliable evidence for clinical treatment. Trial registration Clinical Trials.gov, NCT03658291. Registered on 4 September 2018.

A new binuclear complex [Ag2(ntb)2](NO3)2·(CH3OH)1.5·(CH3CN)0.5 based on a tripodal ligand ntb (ntb = tris(2-benzimidazolylmethyl)amine) has been synthesized and structurally characterized by X-ray single crystal diffractometry. In the structure of the complex each center Ag(I) ion is coordinated by two N atoms from two benzimidazole arm of one ntb ligand and one N atoms from one benzimidazole arm of the other in a trigonal coordinated geometry, resulting in the construction of a binuclear complex. The complex units are further linked into a 1-D chain by hydrogen bonds. The emission spectrum of the complex has been investigated and shows a red-shift of the emission peak compared to the ligand and the existence of ligand-to-metal charge transfer process (emission peak at 468.2 nm). Cyclic voltammogram of the complex indicates a pair of quasi-reversible redox couple, corresponding to the Ag+/Ag electrochemical process. In the structure of the complex each center Ag(I) ion is coordinated by two N atoms from two benzimidazole arm of one ntb ligand and one N atoms from one benzimidazole arm of the other in a trigonal coordinated geometry, resulting in the construction of a binuclear complex.

A new candidate [Cu(PPh3)2Him]Br (1, PPh3=triphenylphosphine, Him=1-H-imidazole) for nonlinear optical (NLO) materials has been synthesized and characterized crystallographically. The third-order NLO optical properties were measured by the Z-scan technique with an 8 ns pulsed laser at 532 nm. Compound 1 exhibits strong NLO absorptive abilities [a2=(61 +/- 5) x 10(-12)] and effective self-focusing performance [n2=(15 +/- 3) x 10(-18) m2.W-1] in 1.01 x 10(-4) mol.dm(-3) DMF solution. The compound also exhibits luminescence in DMF solution at room temperature and shows narrow emission with maximum at 382 nm. The electronic structure and photoluminescent process were investigated by means of TD-DFT calculations. The results suggest that the contribution to the frontier orbitals from the Cu?Br d bond plays a crucial role in its linear optical properties, and the origin of luminescence is attributable to the p*??n transitions.

Three new complexes ([Cu(OBimB)2](Cl)2·(EtOH)2·(H2O)2 1, [Cu(OBimB)2](NO3)2·(EtOH)2 2, [Ni(OBimB)2](NO3)2·(MeCN)2 3 based on a rigid bis(benzimidazoles) ligand OBimB (OBimB = 1,2-bis(2-benzimidazolyl)benzene) have been synthesized and structurally characterized by X-ray single crystal diffractometry. In the structures of the three complexes each metal ion is coordinated by four N atoms from two twisted V-shaped conformational OBimB ligands in a square-planar geometry. The complex units are further linked into a 2D layer supramolecular network by hydrogen bonds and π···π stacking interactions. The electronic absorption spectra of 1, 2, 3 have also been investigated and show that the two transitions around 220 and 280 nm are mainly assigned to intramolecular charge transfer transitions of the ligand (IL).

A new copper(II) complex based on the rigid ligand OBimB (OBimB = 1,2-bis(2-benzimidazolyl)benzene) has been synthesized and structurally characterized by X-ray single-crystal diffraction. In the structure of the complex, each Cu(II) atom is coordinated by four N atoms from two twisted V-shaped OBimB ligands in a square-planar geometry. The complex has been used as a bulk modifier to fabricate a carbon paste electrode (Cu-CPE). Electrochemical studies of the Cu-CPE in 0.1 M pH 2.0 phosphate buffer solution reveal that the Cu2+/Cu+ redox process is quasi-reversible. Electrocatalytic studies of the Cu-CPE indicate that it has good electrocatalytic activities toward reduction of bromate, hydrogen peroxide, and nitrite.

Two isomorphous new candidates [M(mu(4)-pz25dc)](n) (M = Cd, 1; Zn, 2; pz25dc = pyrazine-2,5-dicarboxylato)for nonlinear optical (NLO) materials have been synthesized hydrothermally and characterized crystallographically as pillared-layer three-nodal frameworks with one four-connected metal nodes and two crystallographically different four-connected ligand nodes. Their optical non-linearities are measured by the Z-Scan technique with an 8 ns pulsed laser at 532 nm. These two coordination polymers both exhibit strong NLO absorptive abilities [alpha(2) = (63 +/- 6) x 10 (12) mW (1) 1, ( 46 +/- 6) x 10 (11) mW (1) 2] and effective self-focusing performance [n(2) = (67 +/- 5) x 10 (18) 1, (13 +/- 3) x 10 (18) m(2) W (1) 2] in 1.02 x 10 (4) 1 and 1.05 x 10 (4) mol dm (3) 2 DMF solution separately. The values of the limiting threshold are also measured from the optical limiting experimental data. The heavy atom effect plays important role in the enhancement of optical non-linearities and optical limiting properties. (C) 2009 Elsevier B. V. All rights reserved.

A multi-center large scale study is needed to confirm the efficacy and safety of domestic peritoneal dialysis (PD) solutions. Some researchers believe that 6 L/d is enough for adequate dialysis, but there is no multi-center prospective study on Chinese population to confirm this. In this study, we evaluated the efficacy and safety of domestic PD solution (Changfu) and its difference between 6 L and 8 L dosage.Adult PD patients who had taken PD therapy for at least one month were selected and divided into four groups according to two dialysis solution brands and two dialysis dosages, i.e., 6 L dose with Changfu dialysis solution, 6 L dose with Baxter dialysis solution, 8 L dose with Changfu dialysis solution, and 8 L dose with Baxter dialysis solution. After 48 weeks, the changes of primary and secondary efficacy indices were compared between different types and different dosages. We also analyzed the changes of safety indices.Changes of Kt/V from baseline to 48 weeks between Changfu and Baxter showed no statistical differences; so did those of creatinine clearance rate (Ccr). Normalized protein catabolic rate (nPCR) from baseline to 48 weeks between Changfu and Baxter showed no statistical differences; so did those of net ultrafiltration volume (nUF) and estimated glomerular filtration rate (eGFR). Changes of nPCR from baseline to 48 weeks between 6 L and 8 L showed no statistical differences; so did those of nUF and eGFR. The decline of Kt/V from baseline to 48 weeks in 6 L group was more than that in 8 L group. Change of Ccr was similar. During the 48-week period, the mean Kt/V was above 1.7/w, and mean Ccr was above 50 L×1.73 m(-2)×w(-1). More adverse events were found in Changfu group before Changfu Corporation commenced technology optimization, and the statistical differences disappeared after that.The domestic PD solution (Changfu) was proven to be as effective as Baxter dialysis solution. During 48-week period, a dosage of 6 L/d was enough for these patients to reach adequate PD. Clinical study promotes technological optimization, further helps to improve the safety indices of the medical products.

Background Diabetic nephropathy (DN) is a major microvascular complication with diabetes. In China, an estimated 34.7 percent of people diagnosed with diabetes have renal complications and a further 50 percent die of renal failure. Hence, identification of alternative treatments for these patients should be given priority. The Shenyan Kangfu tablet (SYKFT) is a new formulation of an existing and widely acclaimed Chinese herbal tea for treating qi-yin deficiency syndrome. Because a considerable portion of DN patients presenting with symptoms of swelling, fatigue and weak limbs would be diagnosed with qi-yin deficiency syndrome according to the traditional Chinese medicine (TCM) diagnostic criteria, we hypothesize that SYKFT may represent a complementary drug for DN patients with the corresponding syndrome. In view of this, we have designed a trial to assess the efficacy and safety of SYKFT for patients with diabetic nephropathy exhibiting signs of qi and yin deficiency. Methods This is a multicenter, double-blind, randomized controlled trial (RCT). The total target sample size is planned at 80 participants, with a balanced (1:1) treatment allocation. The experimental intervention will be SYKFY plus irbesartan (SI regimen) and the control intervention will be a placebo plus irbesartan (PI regimen). Participants will receive two courses of medication treatment each lasting 8 weeks. The primary outcome will be the composite of the quantitative 24-hour urinary protein level and urinary albumin excretion rate (UAER). Changes in urine albumin-to-creatinine ratio (UACR) and DN staging, and TCM symptom improvement will be the secondary outcome measures. Adverse events (AEs) will be monitored throughout the trial. Discussion This study will be the first placebo-controlled RCT to assess whether SYKFT plus irbesartan will have beneficial effects on enhancing overall response rate (ORR), changing DN staging, improving clinical symptoms, and reducing the frequency of AEs for DN patients with qi-yin deficiency syndrome. The results of this trial will help to provide evidence-based recommendations for clinicians. Trial registration Chinese Clinical Trials Register, Identifier: ChiCTR-TRC-12002182

To observe the clinical efficacy of Shen No. 9 Recipe (SR) combined with Qingre Moshen Granule (QMG) in treatment of idiopathic membranous nephropathy (IMN) patients with no efficacy after treated by hormone or immunosuppressive agent, and further to explore the possible mechanism of this method in treatment of IMN by detecting the cellular immune function and cytokine interleukin-2 (IL-2).Forty-four IMN patients with no efficacy after treated by multiple Western drugs were recruited from October 2007 to October 2009. They took SR (one dosage daily, oral administration in two portions) and QMG (each package each time, thrice daily) for 24 weeks. The 24-h urine protein, glomerular filtration rate (GFR), plasma albumin (Alb), serum creatinine (SCr), urea nitrogen (BUN), triglyceride (TG), serum total cholesterol (TC), levels of cellular immune function (CD4+, CD8+, CD4+/CD8+ ratio), and IL-2 were detected before and after treatment. The changes of Chinese medicine syndrome and adverse reactions were observed and recorded.After treatment the complete remission rate, the basic remission rate, and the total effective rate was 4.5%, 68.2%, 84.1%, respectively. The total markedly-effective rate of Chinese medicine syndrome was 90.9%. The Chinese medicine syndrome was significantly lower than before treatment (P0.01). The 24-h urine protein obviously decreased (P0.01), Alb obviously increased (P0.01), levels of TC and TG obviously decreased (P0.01, P0.05). There was no obvious change in levels of SCr and BUN (P0.05). The GFR significantly increased (P0.05). CD4+ and the ratio of CD4+/CD8+ were obviously elevated (P0.01) and the CD8+ obviously decreased (P0.01). The expression level of IL-2 obviously increased, but it still was lower than the normal value, showing statistical difference (P0.01).SR + QMG showed definite efficacy in treatment of IMN patients with no efficacy after treated by multiple Western drugs. It could improve the level of cellular immunity and improve abnormal expression levels of IL-2.

To evaluate the therapeutic effect of integrative Chinese and Western medicine in treating mid-advanced crescentic nephritis (MACN).Thirty-two patients, their diagnosis was confirmed as MACN by renal biopsy, were divided, adopting randomized, controlled method, into two groups, the treated group and the control group, they were all, excepting one, treated with impact therapy of methyl-prednisolone followed with oral intake of prednisone, to part of them cyclophosphamide or mycophenolate mofetil was given in addition, to those with hypo-hemoglobin (90 g/L), subcutaneous injection of erythropoietin was administered. Decoction of Qingre Huoxue recipe (QHR), consisted of oldenlandia herb 30 g, honey-suckle stem 30 g, violet herb 30 g, red peony root 15 g, rehmannia root 15 g, solomonseal rhizome 15 g, asiabell root 30 g, red sage root 30 g, prepared rhubarb 12 g and giant-hyssop herb 12 g, were additionally given one dose per day to patients in the treated group. The renal function, improvement of anemia and immunosuppressive agents needed in patients were observed after 3 months treatment.After treatment, renal function was improved in both groups, but the effect in the treated group was better than that in the control group (P0.05). Anemia was partially alleviated in the two groups with no significant difference. The dosage of glucocorticoids used in the treated group was obviously lesser than that used in the control group (P0.01).Integrative Chinese and western medicine could treat crescentic nephritis to obtain good effect, and reduce the quantity of glucocorticoid necessity for treatment.