In the present study, liquiritigenin-phospholipid complex (LPC) was developed and evaluated to increase the oral bioavailability of liquiritigenin. A single-factor test methodology was applied to optimize the formulation and process for preparing LPC. The effects of solvent, drug concentration, reaction time, temperature and drug-to-phospholipid ratio on encapsulation efficiency were investigated. LPCs were characterized by UV-visible spectroscopy, differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and powder X-ray diffractometry (PXRD). The apparent solubility and n-octanol/water partition coefficient were tested. The pharmacokinetic characteristics and bioavailability of the LPC were investigated after oral administration in rats in comparison with liquiritigenin alone. An LPC was successfully prepared. The optimum level of various parameters for liquiritigenin-phospholipid complex was obtained at the drug concentration of 8 mg·mL
Administration, Oral ; Animals ; Biological Availability ; Flavanones/pharmacokinetics* ; Phospholipids/pharmacokinetics* ; Rats ; Solvents

Curcumin-ethyl-cellulose (EC) sustained-release composite particles were prepared by using supercritical CO2 anti-solvent technology. With drug loading and yield of inclusion complex as evaluation indexes, on the basis of single factor tests, orthogonal experimental design was used to optimize the preparation process of curcumin-EC sustained-release composite particles. The experiments such as drug loading, yield, particle size distribution, electron microscope analysis (SEM) , infrared spectrum (IR), differential scanning calorimetry (DSC) and in vitro dissolution were used to analyze the optimal process combination. The orthogonal experimental optimization process conditions were set as follows: crystallization temperature 45 degrees C, crystallization pressure 10 MPa, curcumin concentration 8 g x L(-1), solvent flow rate 0.9 mL x min(-1), and CO2 velocity 4 L x min(-1). Under the optimal conditions, the average drug loading and yield of curcumin-EC sustained-release composite particles were 33.01% and 83.97%, and the average particle size of the particles was 20.632 μm. IR and DSC analysis showed that curcumin might complex with EC. The experiments of in vitro dissolution showed that curcumin-EC composite particles had good sustained-release effect. Curcumin-EC sustained-release composite particles can be prepared by supercritical CO2 anti-solvent technology.
Carbon Dioxide ; chemistry ; Cellulose ; administration & dosage ; analogs & derivatives ; chemistry ; Curcumin ; administration & dosage ; chemistry ; Delayed-Action Preparations ; Solubility ; Solvents ; Technology, Pharmaceutical

OBJECTIVES: This study was conducted to provide accurate exposure evaluation of workers in a biologicallymonitored state who were simultaneously exposed to benzene and toluene. For the purpose of this study, an animal experiment was conducted. METHODS: The following concentrations of solvents were administered orally to Sprague-Dawley rats : benzene at 2.26 mg/kg body weight (equivalent concentration to the 2.5 ppm, Threshold Limit Value-ShortTerm Exposure Limit, in the USA) and 9.02 mg/kg body weight (equivalent concentration to the 10 ppm, Threshold Limit Value-TimeWeighted Average in Korea), simultaneously with toluene at 106.42 mg/kg body weight (equivalent concentration to the 100 ppm, Threshold Limit Value-TimeWeighted RESULTS: The following results were obtained from the analysis of reading taken at 3hour intervals of S-phenylmercapturic acid (SPMA) and phenol concentration in urine metabolites of benzene after oral administration for 30 hours. 1. The concentrations of phenol and SPMA in urine were markedly decreased in the initial phase of the mixed group (both benzene and toluene administered group) as compared with the benzeneonly administered group, and the concentrations were slightly elevated. 2. The total excreted amounts of phenol and SPMA in urine decreased in the mixed group compared with the benzene-only group, and these decreases were more remarkable at the benzene administration concentration of 9.02 mg/kg than at 2.26 mg/kg. 3. The urinary excretions of phenol and SPMA were delayed in the case of the mixed group, and the extent of the delay was dependent on the amount of benzene administrat CONCLUSIONS: Benzene metabolism was suppressed by toluene, and hence the excretion of phenol and SPMA as urinary metabolites of benzene was delayed. This result will have applications in the interpretation of results from future biological monitoring of workers exposed to mixed solvents. We should not underestimate the importance of carefully interpreting the results of biological monitoring data when workers are exposed to mixed solvents. We should not underestimate the importance of carefully interpreting the results of biological monitoring data when workers are exposed to mixed benzene and toluene.
Administration, Oral ; Animal Experimentation ; Animals ; Benzene* ; Body Weight ; Environmental Monitoring ; Metabolism ; Phenol* ; Rats* ; Rats, Sprague-Dawley ; Solvents ; Toluene*

OBJECTIVE: We retrospectively assessed the results of performing ethanol embolization for pelvis arteriovenous malformations (AVMs). MATERIALS AND METHODS: During the past 10 years, eight patients (8 females, age range: 27-52 years) with AVMs in the pelvic wall (n = 3) and uterus (n = 5) underwent staged ethanol embolizations (range: 1-5, mean: 2.5) under general anesthesia. Ethanol embolization was performed by the use of the transcatheter and/or direct puncture techniques. Clinical follow-up was performed for all of the patients, and imaging follow-up was available for seven patients. The therapeutic outcomes were established by evaluating the clinical outcome of the signs and symptoms, as well as the degree of devascularization observed on post-procedural angiography. RESULTS: During the 20 sessions of ethanol embolization, the solitary transarterial approach was used 14 times, the transvenous approach was used three times and direct puncture was used once. For two patients, the transarterial and transvenous or direct puncture approaches were used together in one session. For four patients, ethanol and coils were used as embolic agents, and n-butyl cyanoacrylate (NBCA) and ethanol were used in one patient. Seven (88%) of eight patients were cured of their AVMs and one patient (12%) displayed improvement. Major complications were seen in two patients (25%). CONCLUSION: Ethanol embolization is effective for the treatment of pelvic arteriovenous malformations, though there is a chance of a major complication.
Adult ; Arteriovenous Malformations/*therapy ; Embolization, Therapeutic/adverse effects/*methods ; Enbucrilate/administration & dosage ; Ethanol/administration & dosage ; Female ; Humans ; Middle Aged ; Pelvis/*blood supply ; Retrospective Studies ; Solvents/administration & dosage ; Tissue Adhesives/administration & dosage ; Uterus/*blood supply

To study the rheological properties of sucrose acetate isobutyrate (SAIB) in situ gel and the influencing factors. Measurements of shear stress and viscosity were carried out at different shear rate. The rheological properties of SAIB solution were similar to those of Newtonian fluid. The factors such as the type of solvent, concentration, additive, drug and temperature had effect on the rheological properties. Ethanol was a suitable solvent compared with ethyl lactate and N-methylpyrrolidone (NMP). The solution viscosity of SAIB was reduced from 1.29 to 0.11 Pa x s with only increasing the content of ethanol from 10% to 20%. Polylactic acid (PLA) and risperidone could increase the intermolecular force and viscosity. However, adding 10% (w/w) PLA, the initial release of risperidone was reduced from 20.2% to 3.5%. The solution viscosity reduced significantly by stepping up the temperature. The results obtained support the using of SAIB is satisfactorily injectable in situ gel formulation.
Antipsychotic Agents ; administration & dosage ; Delayed-Action Preparations ; Drug Carriers ; Ethanol ; Lactates ; Lactic Acid ; Polyesters ; Polymers ; Pyrrolidinones ; Rheology ; Risperidone ; administration & dosage ; Solvents ; Sucrose ; administration & dosage ; analogs & derivatives ; chemistry ; Temperature ; Viscosity

AIMTo evaluate the safety and efficacy of an extract of Ganoderma lucidum that shows the strongest 5alpha-reductase inhibitory activity among the extracts of 19 edible and medicinal mushrooms by a double-blind, placebo-controlled, randomized and dose-ranging study in men with lower urinary tract symptoms (LUTS).

METHODSIn this trial, we randomly assigned 88 men over the age of 49 years who had slight-to-moderate LUTS to 12 weeks of treatment with G. lucidum extract (6 mg once a day) or placebo. The primary outcome measures were changes in the International Prostate Symptom Score (IPSS) and variables of uroflowmetry. Secondary outcome measures included changes in prostate size, residual urinary volume after voiding, laboratory values and the reported adverse effects.

RESULTSG. lucidum was effective and significantly superior to placebo for improving total IPSS with 2.1 points decreasing at the end of treatment (mean difference, -1.18 points; 95% confidence interval, -1.74 to -0.62; P < 0.0001). No changes were observed with respect to quality of life scores, peak urinary flow, mean urinary flow, residual urine, prostate volume, serum prostate-specific antigen or testosterone levels. Overall treatment was well tolerated with no severe adverse effects.

CONCLUSIONThe extract of G. lucidum was well tolerated and improved IPSS scores. These results encouraged a further, large-scale evaluation of phytotherapy for a long duration using the extract of G. lucidum on men with LUTS.

Aged ; Drugs, Chinese Herbal ; administration & dosage ; adverse effects ; Ethanol ; Humans ; Male ; Middle Aged ; Phytotherapy ; Placebos ; Reishi ; Solvents ; Treatment Outcome ; Urination Disorders ; drug therapy ; Urodynamics ; drug effects

In order to test the equilibrium solubility of puerarin in different solvents and solubilizer,cilia toxicity and irritation of these excipient, the balance method, toad in the ciliary body toxicity and rat nasal mucosa irritation were used respectively. Results showed that puerarin solubility was 56.44 g x L(-1) in combined solvent of 30% PEG200 and 10% Kolliphor HS 15. With normal saline solution as negative control and sodium deoxycholate as positive control, the effects of 30% PEG200, 30% PEG 400, 10% Kolliphor HS 15 and combination of 30% of PEG200 and 10% Kolliphor HS 15 on toad palate cilium were observed and cilia movement duration was recorded. The results indicated that there was no significant difference in cilia movement duration among 30% PEG200, 10% Kolliphor HS 15 and normal saline group. The rats long-term nasal mucous membrane irritation of 30% PEG 400, 10% Kolliphor HS 15, which had no cilia toxicity, was studied, with normal saline solution as negative control. There were no significant difference revealed on rat nasal mucosa epithelial thickness among 30% PEG 400, 10% Kolliphor HS 15 and normal saline. Above researches showed 30% PEG 400, 10% Kolliphor HS 15 was ideal for solubility of puerarin nasal drops and showed a lower cilia toxicity and irritation, and can be used as the solvent and solubilizer of puerarin nasal drops.
Administration, Intranasal ; methods ; Animals ; Anura ; Cilia ; chemistry ; Female ; Isoflavones ; chemistry ; Male ; Nasal Mucosa ; Polyethylene Glycols ; chemistry ; Rats ; Rats, Sprague-Dawley ; Solubility ; Solvents ; chemistry

AIMTo establish an efficient method for preparation of solid lipid nanoparticles with high recovery.

METHODSMonostearin solid lipid nanoparticles was prepared by solvent diffusion method in aqueous system. The recovery of the method was greatly improved by adjusting the Zeta potential.

RESULTSThe drug-loaded solid lipid nanoparticles suspension was quickly produced and easily separated with centrifugation at 4,000 r.min-1 under acidic condition. Compared with the nanoparticles made without adjusting the Zeta potential, the recovery of nanoparticles prepared in this way was significantly increased. The release behavior in vitro showed an initial burst effect in the first 3 hours followed by a slower rate stage of 4 days with nearly 6% drug released in each day.

CONCLUSIONThe solvent diffusion method in aqueous system might be used as a new method to prepare solid lipid nanoparticles in the future. The loaded drug can be released in a controlled manner.

Clobetasol ; administration & dosage ; analogs & derivatives ; Delayed-Action Preparations ; chemistry ; Diffusion ; Drug Carriers ; Drug Delivery Systems ; Glycerides ; chemistry ; Nanotechnology ; Particle Size ; Solvents ; Technology, Pharmaceutical ; methods

OBJECTIVEThe influence of spray drying technology on the damp proof effect of microcapsules and the mechanism were studied.

METHODThe microcapsules prepared with different spray drying parameters have been put in certain surroundings for 12 hours, then the hygroscopic curves were gotten; the mechanism was studied from the following aspects: solvent residue, film's shrink and particle size.

RESULTThe damp proof effect enhanced with the increase of inlet air temperature and the decrease of flow rate and air pressure. The properties of the wall, the solvent residue and particle size can influence the damp proof effect of the microcapsules.

CONCLUSIONThe physical properties of microcapsules are different because of the different spray drying parameters, which lead to different damp proof effect of microcapsules.

Acrylic Resins ; Capsules ; Desiccation ; methods ; Drug Compounding ; methods ; Lindera ; chemistry ; Particle Size ; Plants, Medicinal ; chemistry ; Solvents ; Tannins ; administration & dosage ; isolation & purification ; Temperature

Although intravesical instillation of Mycobacterium bovis bacillus Calmette-Guérin (BCG) is the most successful cancer immunotherapy for superficial bladder cancer, the serious side effects are frequently arisen by using live mycobacteria. To allow less toxic and more potent immunotherapeutic agents following intravesical BCG treatment for superficial bladder cancer, noninfectious immunotherapeutic drug instead of live BCG would be highly desirable. Recently, immune-enhancing adjuvants are considered an effective vaccine immunotherapy for cancer, providing enhanced antitumor effects and boosted immunity. The BCG-cell wall skeleton (BCG-CWS), the main immune active center of BCG, is a potent candidate as a noninfectious immunotherapeutic drug instead of live BCG against bladder cancer. However, the most limited application for anticancer therapy, it is difficult to formulate a water-soluble BCG-CWS due to the aggregation of BCG-CWS in both aqueous and nonaqueous solvents. To overcome the insolubility and improve the internalization of BCG-CWS into bladder cancer cells, it should be developed the lipid nanoparticulation of BCG-CWS, resulting in improved dispensability, stability, and small size. In addition, powerful technology of delivery systems should be applied to enhance the internalization of BCG-CWS, such as encapsulated into lipid nanoparticles using novel packaging methods. Here, we describe the progress in research on effects of BCG-CWS for cancer immunotherapy, development of lipid-based solvent, and packaging method using nanoparticles with drug delivery system.
Administration, Intravesical ; Bacillus ; Cell Wall Skeleton ; Drug Delivery Systems ; Immunotherapy ; Methods ; Mycobacterium bovis ; Nanoparticles ; Product Packaging ; Skeleton ; Solvents ; Urinary Bladder Neoplasms ; Urinary Bladder