Total paeony glycoside (TPG) is extracted and purified from a traditional Chinese herbal medicine. It has many biological and pharmacological activities. However, there are few dosage forms of TPG in the market because of its low bioavailability. Self-microemulsifying drug delivery system (SMEDDS) is a vital tool in solving low bioavailability of poor absorption drugs. So the objective of this study is to develop a new TPG-SMEDDS for the oral delivery of poorly soluble TPG. Through the construction of pseudo-ternary phase diagrams, the optimum prescription was obtained, which consisted of 18.70% TPG, 16.27% ethyl oleate as oil, 43.34% Cremophor RH40 as surfactant and 21.73% Transcutol P as cosurfactant. The characterizations of TPG-SMEDDS including morphological characterization, droplet size, zeta-potential, emulsification time, and dissolution study of TPG-SMEDDS were evaluated. The results showed that TPG-SMEDDS is stable and its release rate is high in four different media (0.1 mol x L(-1) HCl, pH 6.8 PBS, pH 7.4 PBS, and water). The relative bioavailability of SMEDDS was dramatically enhanced in an average of 1.52-fold that of TPG-suspension. It is concluded that the bioavailability of TPG is enhanced greatly by SMEDDS.
Administration, Oral ; Animals ; Biological Availability ; Drug Delivery Systems ; Drug Stability ; Emulsions ; Ethylene Glycols ; chemistry ; Glycosides ; administration & dosage ; chemistry ; isolation & purification ; pharmacokinetics ; Oleic Acids ; chemistry ; Paeonia ; chemistry ; Particle Size ; Pharmaceutical Vehicles ; chemistry ; Plants, Medicinal ; chemistry ; Polyethylene Glycols ; chemistry ; Rats ; Solubility

Hydroxypropyl methylcellulose (HPMC) propels self-emulsifying drug delivery systems (SEDDS) to achieve the supersaturated state in gastrointestinal tract, which possesses important significance to enhance oral absorption for poorly water-soluble drugs. This study investigated capacities and mechanisms of HPMC with different viscosities (K4M, K15M and K100M) to inhibit drug precipitation of SEDDS in the simulated gastrointestinal tract environment in vitro. The results showed that HPMC inhibited drug precipitation during the dispersion of SEDDS under gastric conditions by inhibiting the formation of crystal nucleus and the growth of crystals. HPMC had evident effects on the rate of SEDDS lipolysis and benefited the distribution of drug molecules across into the aqueous phase and the decrease of drug sediment. The mechanisms were related to the formed network of HPMC and its viscosities and molecular weight. These results offered a reference for selecting appropriate type of HPMC as the precipitation inhibitor of supersaturatable SEDDS.
Caprylates ; chemistry ; Chemical Precipitation ; drug effects ; Crystallization ; Drug Delivery Systems ; methods ; Emulsifying Agents ; chemistry ; Emulsions ; Ethylene Glycols ; chemistry ; Glycerides ; chemistry ; Hypromellose Derivatives ; administration & dosage ; chemistry ; pharmacology ; Indomethacin ; administration & dosage ; chemistry ; Lipolysis ; drug effects ; Molecular Weight ; Polyethylene Glycols ; chemistry ; Viscosity

OBJECTIVETo investigate the effects of labrasol, solutol HS 15 and transcutol P on the corneal permeability of mangiferin in vitro.

METHODThe effects of three penetration enhancers on the corneal permeability of mangiferin were investigated in vitro by using isolated rabbit corneas.

RESULTThe apparent Papp enhancements were increased 1.80, 3.27, 3.41 and 4.76-folds with Lab at 1.0%, 1.5%, 2.0% and 3.0% (P < 0.01), respectively. The apparent Papp increased 1.98 and 3.07-folds with Sol at 0.2% and 0.4% (P < 0.01), respectively, but reduced with 0.010%-0.03% Trans.

CONCLUSIONThe Papp value of mangiferin is significantly enhanced by 1.0%-3.0% Lab, 0.2% and 0.4% Sol, however the Papp value of mangiferin is reduced by 0.01%-0.03% Trans.

Animals ; Cornea ; drug effects ; metabolism ; Drug Carriers ; chemistry ; Ethylene Glycols ; chemistry ; Glycerides ; In Vitro Techniques ; Organic Chemicals ; chemistry ; Permeability ; Plant Extracts ; pharmacokinetics ; Polyethylene Glycols ; chemistry ; Rabbits ; Stearic Acids ; chemistry ; Xanthones ; pharmacokinetics

OBJECTIVETo establish a gas chromatographic method for detecting 2-butoxy ethanol in the air of workplaces.

METHODSAfter the air samples were collected with activated carbon tubes and desorbed with methylene chloride/methanol, the target toxicant was separated with FFAP capillary columns and detected with flame ionization detector, qualified by retention time and quantified by peak area.

RESULTSThe linear range of 2-butoxy ethanol in air of workplace was 56.3 ∼ 901.0 µg/ml, the correlation coefficient was 09999. The limit of detection was 2.0 µg/ml. The limit of quantity was 5.0 µg/ml. The minimal detecting concentration was 0.27 mg/m(3) in the condition of 7.5L sampling volume and 1ml desorbed volume. Relative standard deviation was 3.04% ∼ 7.93% and the recovery was 92.7% ∼ 95.5%.

CONCLUSIONIn present study the detecting method with high sensitivity, precision and accuracy can be used to determine 2-butoxy ethanol in the air of workplaces.

Air Pollutants, Occupational ; analysis ; Chromatography, Gas ; methods ; Ethylene Glycols ; analysis ; Workplace

The aim of this study is to prepare self-microemulsifying drug delivery system (SMEDDS) of the mixture of paeonol (Pae) and borneol (Bor). Solubility test, ternary phase diagrams and simplex lattice method were employed to screen and optimize the formulation of the mixture of Pae and Bor-loaded SMEDDS. After formed into microemulsions, the particle diameter (PD) was determined and a TEM was employed to observe the microemulsions' morphology. The contents of Pae and Bor were determined by gas chromatography. As a result, while ethyl oleate (EO) as the oil phase, cremophor EL35 (EL35) as surfactant and Transcutol HP (HP) as cosurfactant, the range of the microemulsion on the ternary phase diagram was larger than other combinations. And at a ratio of 20:45:35, the microemulsions' PD was about 34 nm and the polydispersity index (PI) was about 0.2. There were 16% of Pae, 2% of Bor, 16% of EO, 37% of EL35 and 29% of HP in the prepared SMEDDS. The preparation process of the Pae and Bor-loaded SMEDDS based on Xingbi Fang is simple and feasible. This study provides a reference for the researches on the related traditional Chinese medicine and the related components.
Acetophenones ; administration & dosage ; toxicity ; Administration, Intranasal ; Animals ; Bornanes ; administration & dosage ; toxicity ; Bufonidae ; Cilia ; drug effects ; Drug Combinations ; Drug Delivery Systems ; methods ; Drugs, Chinese Herbal ; administration & dosage ; toxicity ; Emulsions ; Ethylene Glycols ; chemistry ; Female ; Male ; Nasal Mucosa ; drug effects ; Oleic Acids ; chemistry ; Particle Size ; Polyethylene Glycols ; chemistry ; Solubility ; Surface-Active Agents ; chemistry

OBJECTIVE: To explore the effect of cephalomedullary nails for elderly intertrochanteric fractures: proximal femoral nail antirotation (PFNA) versus zimmer natural nail (ZNN) to provide the data support for clinical perioperative management. METHODS: A retrospective study was used to analyze the clinical data of elderly intertrochanteric fractures cases which were treated with PFNA or ZNN fixation from May 2016 to May 2017. In the study, 59 cases were followed up completely, in which 28 cases accepted PFNA, and the other 31 cases accepted ZNN. The operation time, amount of bleeding, fracture healing time, postoperative complication, postoperative radiographic measurement (tip apex distance, TAD) and the last follow-up of hip function score were analyzed. RESULTS: The patients were followed up for 6 to 19 months, with an average (10.8±4.0) months. In PFNA group, the operation time was (62.7±14.2) min, the amount of bleeding was (56.8±20.6) mL, the fracture healing time was (4.6±0.8) months, the postoperative complication was 3.6%, the TAD was (17.7±5.5) mm, and the last follow-up hip function score was 91.8±3.6. In ZNN group, the operation time was (73.6±18.3) min, the amount of bleeding was (68.7±31.6) mL, the fracture healing time was (4.5±0.7) months, the postoperative complication was 3.2%, the TAD was (16.5±4.7) mm, and the last follow-up hip function score was 92.2±3.8. The two groups of comparative experiments were carried out, the operation time of the PFNA group was less than that of the ZNN group (P<0.05). There was no significant difference in the amount of bleeding, fracture healing time, postoperative complication, TAD, postoperative hip score between the two groups (P>0.05). CONCLUSION Although group ZNN had significant longer operation time than group PFNA, both implants were useful tools in the treatment of elderly intertrochanteric fractures. The operation of PFNA was simpler,while the design of the anterior bow of ZNN might be more suitable for the patients with a large femoral anterior bow.
Aged ; Bone Nails ; Ethylene Glycols ; Femoral Fractures ; Fracture Fixation, Intramedullary ; Hip Fractures ; Humans ; Retrospective Studies ; Treatment Outcome

The aim of this paper is to compare the cytotoxicity and cellular uptake efficiency of three kinds of poly(b-benzyl-L-amino) block-poly(ethylene glycol) nanoparticles (PXA-PEG-NPs) using Calu-3 cells, and select one as a nasal drug delivery vector for curcumin (Cur). Poly(gamma-benzyl-L-glutamate) block-poly(ethylene glycol) nanoparticles (PBLG-PEG-NPs), poly(gamma-benzyl-L-lysine) block-poly(ethyleneglycol) nanoparticles (PZLL-PEG-NPs) and poly(gamma-benzyl-L-aspartate) block-poly(ethylene glycol) nanoparticles (PBLA-PEG-NPs) were prepared by emulsion-solvent evaporation method. MTT assays were used to evaluate the cytotoxicity of PXA-PEG-NPs against Calu-3 cells. The cellular uptake of nanoparticles was visualized by an inverted fluorescence microscope and quantified by a flow cytometer. The results indicated that even at high concentration of 2 mg x mL(-1) the three nanoparticles had no cytotoxicity on Calu-3 cells. Compared to the curcumin solution, the three curcumin-loaded PXA-PEG-NPs showed significantly higher cellular uptake efficiency on Calu-3 cells (at equal concentration of curcumin with 5 microg x mL(-1) Cur solution), PBLG-PEG-NPs group was the highest. The cellular uptake increased with incubation time, and has positive correlation with nanoparticle concentration. In brief, PXA-PEG-NPs are conducive to delivery Cur into cells, and PBLG-PEG-NPs might be provided as a good nasal drug delivery carrier.
Adenocarcinoma ; metabolism ; pathology ; Administration, Intranasal ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; metabolism ; Aspartic Acid ; chemistry ; toxicity ; Cell Line, Tumor ; Cell Survival ; drug effects ; Curcumin ; administration & dosage ; metabolism ; Drug Carriers ; Ethylene Glycol ; chemistry ; toxicity ; Humans ; Lung Neoplasms ; metabolism ; pathology ; Lysine ; chemistry ; toxicity ; Nanoparticles ; Particle Size ; Polyethylene Glycols ; chemistry ; toxicity ; Polyglutamic Acid ; analogs & derivatives ; chemistry ; toxicity

BACKGROUNDThere was a hospital outbreak of venous diethylene glycol poisoning in Guangzhou, China. It is the only massive episode of venous diethylene glycol poisoning in history. Here we report its clinical features, laboratory findings, and imaging appearances.

METHODSThe clinical features of 15 venous diethylene glycol poisoning patients with liver disease were analyzed and summarized. Their laboratory findings and imaging appearances were comparatively analyzed before and after poisoning.

RESULTSAll poisoned patients presented with oliguric acute renal failure with anuria after a mean of 6 days. Carbon dioxide combination power of 13 patients dropped after a mean of 9 days with valley value on the 10th day, when metabolic acidosis developed. Gastroenteric symptoms or aggravation of gastroenteric symptoms were displayed in 11 patients after a mean of 9 days. Neurological system impairment was observed in 10 patients after a mean of 14 days. Seven patients had low fever after a mean of 6 days. Causes of death of 14 patients included multiple organ dysfunction syndrome, severe lung infection and massive haemorrhage of digestive tract. Blood creatinine and urea nitrogen were abnormal after a mean of 5 days with peak value on the 11th and 14th days, respectively. Serum calcium had no obvious change, and phosphorus was distinctively increased. Liver functions did not change significantly. Poisoned patients had higher white blood cell counts, but lower red blood cell counts and hemoglobin value. Of the 7 patients who exhibited mild, moderate or severe patchy consolidation shadowing in the lung, 2 manifested mild or severe gaseous distention and dilation of gastroenteric tract.

CONCLUSIONSMain features of venous diethylene glycol poisoning in patients with liver disease include oliguric acute renal failure, metabolic acidosis, gastroenteric symptoms or aggravation of gastroenteric symptoms, neurological system impairment and low fever, with a mortality rate of 93.33% in poisoned patients. There is also higher white blood cell counts and anemia, patchy consolidation shadowing in the lung, gaseous distention and dilation of gastroenteric tract, which occurs later than mild patchy consolidation shadowing and earlier than moderate patchy consolidation shadowing in the lung.

Acute Kidney Injury ; chemically induced ; Adolescent ; Adult ; Aged ; Benzopyrans ; poisoning ; Child ; Child, Preschool ; Drug Contamination ; Ethylene Glycols ; poisoning ; Female ; Humans ; Liver Diseases ; drug therapy ; Male ; Middle Aged

OBJECTIVES: This study was designed to evaluate exposure levels of various chemicals used in wafer fabrication product lines in the semiconductor industry where work-related leukemia has occurred. METHODS: The research focused on 9 representative wafer fabrication bays among a total of 25 bays in a semiconductor product line. We monitored the chemical substances categorized as human carcinogens with respect to leukemia as well as harmful chemicals used in the bays and substances with hematologic and reproductive toxicities to evaluate the overall health effect for semiconductor industry workers. With respect to monitoring, active and passive sampling techniques were introduced. Eight-hour long-term and 15-minute short-term sampling was conducted for the area as well as on personal samples. RESULTS: The results of the measurements for each substance showed that benzene, toluene, xylene, n-butyl acetate, 2-methoxyethanol, 2-heptanone, ethylene glycol, sulfuric acid, and phosphoric acid were non-detectable (ND) in all samples. Arsine was either "ND" or it existed only in trace form in the bay air. The maximum exposure concentration of fluorides was approximately 0.17% of the Korea occupational exposure limits, with hydrofluoric acid at about 0.2%, hydrochloric acid 0.06%, nitric acid 0.05%, isopropyl alcohol 0.4%, and phosphine at about 2%. The maximum exposure concentration of propylene glycol monomethyl ether acetate (PGMEA) was 0.0870 ppm, representing only 0.1% or less than the American Industrial Hygiene Association recommended standard (100 ppm). CONCLUSION: Benzene, a known human carcinogen for leukemia, and arsine, a hematologic toxin, were not detected in wafer fabrication sites in this study. Among reproductive toxic substances, n-butyl acetate was not detected, but fluorides and PGMEA existed in small amounts in the air. This investigation was focused on the air-borne chemical concentrations only in regular working conditions. Unconditional exposures during spills and/or maintenance tasks and by-product chemicals were not included. Supplementary studies might be required.
2-Propanol ; Arsenicals ; Bays ; Benzene ; Carcinogens ; Ether, Ethyl ; Ethylene Glycol ; Ethylene Glycols ; Ethylenes ; Fluorides ; Humans ; Hydrochloric Acid ; Hydrofluoric Acid ; Ketones ; Korea ; Leukemia ; Nitric Acid ; Occupational Exposure ; Occupational Health ; Phosphines ; Phosphoric Acids ; Propylene Glycol ; Propylene Glycols ; Semiconductors ; Sulfur ; Sulfuric Acids ; Toluene ; Xylenes

PURPOSE: Pediatric sedation is an important factor for obtaining the images of good quality. We performed this study to analyze the efficacy of our sedation protocol using chloral hydrate. MATERIALS AND METHODS: We collected prospectively 151 sedation records of children(1 day-15 years old), who were sedated with chloral hydrate for MR(n=112) or CT(n=39) studies. We initially administered 50mg/Kg orally(n=94) or rectally(n=57) 30 minutes before the scheduled examinations, and then administered additionali dose (second dose :25-35mg/Kg, third dose:10-15mg/Kg) to patients whom initial dose failed to sedate. RESULTS: Satisfactory sedation was achieved by initial administration in 109 patients(72%) without si difference between oral(per oral: P.O.) and rectal(per rectal: P.R.) administration. Second dose was required in 28% and third dose in 5%. MR and CT examinations required second dose in 36(32%) and 6 patients(15%), respectively. P.O. -patients vomited in 5%. P.R. -patients defecated in 22% after initial administration. There were no other serious complications. Time interval from the drug administration to the start of examinations was 33 minutes in initial-dose-group and 64 minutes in additional-dose-group. Two patients could not complete MR examination due to early arousal. Prolonged sedation, requiring more than 30 minutes for alertness after MR and CT examinations, was encountered in twenty(18%) and two patients(5%), respectively. CONCLUSION: Our protocol using chloral hydrate(P.O. or P.R.) is thought to be an effective and safe method for pediatric sedation for MR or CT imaging.
Arousal ; Child* ; Chloral Hydrate* ; Humans ; Prospective Studies