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Background Dibutyl phthalate (DBP) is a common plasticizer in daily life and has been proved to be related to the exacerbation of allergic asthma. Domestic and foreign studies have shown that lipid peroxidation is closely related to the severity of asthma, which can be used as a basis for the diagnosis and treatment of asthma. Whether DBP can induce lipid peroxidation in allergic asthma remains to be further studied. Objective To investigate whether DBP aggravates allergic asthma by inducing lipid peroxidation in allergic asthma mice. Methods Eighty male BALB/c mice were randomly divided into 4 groups, namely control group, DBP group (40 mg·kg−1), 50 μg ovalbumin (OVA) group (allergic asthma model group), and DBP+OVA group. The DBP group and the DBP+OVA group were given DBP by gavage from Day 1 to 28, and the OVA group and the DBP+OVA group were sensitized by intraperitoneal injection of OVA, once every 3 d, a total of 5 injections, from Day 9 to 21. From Day 29 to 35, the OVA group and the DBP+OVA group were challenged by OVA atomization. After the exposure, samples of blood and lung were collected. The airway hyperresponsiveness of mice was observed by lung function analysis. The serum contents of immunoglobulin E (IgE), OVA-specific immunoglobulin E (OVA-IgE), and lung homogenate levels of interleukin 4 (IL-4) were detected by enzyme-linked immunosorbent assay (ELISA) to evaluate airway allergic inflammation. The pathological changes of lung tissues were observed after hematoxylin-eosin (HE) staining and collagen fiber (Masson) staining. The contents of reactive oxygen species (ROS), lipid ROS, glutathione peroxidase 4 (GPX4), reduced glutathione (GSH), malondialdehyde (MDA), and 4-hydroxynonenal (4-HNE) in lung homogenates were detected by ELISA to evaluate lipid peroxidation. Results The results of lung function analysis showed that compared with the control group, the inspiratory resistance (Ri) and expiratory resistance (Re) of the OVA group and the DBP+OVA group were increased, and the lung compliance (Cldyn) was decreased. The DBP + OVA group was more severe, and the difference between the OVA group and the DBP + OVA group was statistically significant (P<0.05 or P<0.01). Compared with the control group, the contents of IgE, OVA-IgE, and IL-4 in the OVA group and the DBP+OVA group were increased (P<0.05 or P<0.01), which indicated more severe allergic airway inflammation. The HE sections of the OVA group and the DBP+OVA group showed inflammatory cell infiltration around the airway, airway wall hyperplasia and thickening, and severe airway deformation, and the presentation of the DBP+OVA group was the most serious. After Masson staining, the OVA group and the DBP+OVA group showed depositions of a large number of collagen fibers, and the blue collagen fibrosis in the DBP+OVA group was even more serious. ROS, lipid ROS, MDA, and 4-HNE levels increased and GSH and GPX4 levels decreased in the OVA and DBP+OVA groups (P<0.05 or P<0.01), with the most severe effect in the DBP+OVA group. Conclusion DBP may induce lipid peroxidation in mice allergic asthma by producing excessive ROS which may aggravate the allergic asthma in mice.
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Objective: Using ultrafine hydroxypropyl cellulose (HPC) powders as coating material to prepare moisture barrier coating film for Compound Danshen Tablets by an innovative electrostatic powder coating technology. The effects of coating prescription and process parameters on coating efficiency and coating film properties were investigated, so as to provide new ideas for moistureproof coating of moisture sensitive traditional Chinese medicine such as Compound Danshen Tablets. Methods: Free films were prepared by applying an electrostatic deposition process, and the effects of liquid plasticizer on the mechanical properties and the water vapor permeability were investigated. And the Compound Danshen Tablets were dry coated with ultrafine powders by the electrostatic coating technology. The effects of coating formulations and processing conditions on the moisture sorption behavior of the barrier film coated tablets were studied. Results: The coating efficiency could be manipulated by adjusting the charging voltage of the electrostatic spray gun and the amount of the liquid plasticizer. Compared with static curing process, dynamic curing process was capable to produce a satisfactory film with an enhanced moisture barrier function for the herbal medicines. The best coating process parameters were plasticizer spraying time 3 min and titanium dioxide addition ratio 1%. The minimum hygroscopicity was achieved when the coating level was increased to 6.7%. Conclusion: The moisture-protective effect by using a novel electrostatic coating technology with ultrafine powders was efficiently achieved, suggesting that it was a promising alternative for the protection for the moisture sensitive drugs.
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The current research deals with formulation and evaluation of Benazepril hydrochloride transdermal films, by varying ratios of polymers Eudragit RL100, Eudragit RS100 by film casting technique. Preformulation studies were conducted to check the solubility, melting point and partition coefficient. The eleven formulations were analyzed for physicochemical parameters and drug dissolution potential of transdermal films. All the formulations are transparent with minimum weight variation and uniform thickness. The drug content uniformity of all the formulations vary between 96.84 ± 3.7% to 96.98 ± 1.6% indicate uniform drug distribution. The low water vapour transmission values indicate good water vapour permeation. The folding endurance is between 246 ± 4.60 to 315 ± 4.13 indicates that the transdermal films can withstand rupture. In vitro drug dissolution study indicates maximum amount of drug 96.8% (F2) released in 24 h when compared with marketed formulation 84.81%. The release order follows Fickian diffusion. The formulation F2 was optimized based on drug flux, permeability coefficient and enhancement ratio.
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Objective: To investigate the effect of di (2-ethylhexyl) phthalate (DEHP) on the uterus tissue of female rats, and to clarify the mechanism of uterine toxicity of DEHP in the female rats. Methods: A total of 48 Wistar female rats were randomly divided into control group (given corn oil), low, middle, and high doses of DEHP groups (given 300, 1 000, and 3 000 mg middot; kg-1 middot; d-1 DEHP; 1/100, 1/30, and 1/10 LD50) (n=12). The rats in various groups were sacrificed during anoestrum, the body weights were recorded and uterine organ coefficients of the rats in various groups were calculated. The pathomorphology of the uterus tissue of the rats in various groups was detected by HE staining. The expression levels of follicle stimulating hormonereceptor (FSHR) and luteinizing hormone receptor (LHR) in uterus tissue of the rats in various groups were detected by immunohistochemistry. Results: Compared with control group, the body weights of the rats in different doses of DEHP groups were decreased (P0. 05). Macroscopically, the morphology of the uterus of rats in control group was normal; in middle and high doses of DEHP groups, the uterus showed distorted and the tube wall became thinner; different degrees of hydrops, congestion and swelling were seen on the serosal surface of the uterus. The microscopic observation results showed that in different doses of DEHP groups the endometrium nuclei appeared pseudostratified phenomenon; the epithelial hyperplasia and endothelial fibrosis were found in the endometrium; the gland number in the lamina propria was decreased, and part of the glands were depauperate. Compared with control group, the expression levels of FSHR in uterus tissue of the rats in different doses of DEHP groups had no significant differences (P>0. 05), and the expression levels of LHR were decreased (P<0. 05); the expression levels of LHR in uterus tissue of the rats in middle and high doses of DEHP groups were significantly lower than that in low dose of DEHP group (P<0. 05). Conclusion: DEHP can lead to the weight loss and the pathological changes in the uterus tissue of the female rats, and has a uterine toxicity effect on the female rats.
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In the present study, Antimicrobial PVC films containing different amounts of clove oil as a plasticizer were prepared using traditional casting method. The physical and mechanical properties of the plasticized PVC membranes e.g. surface wettability were investigated. The increase of clove oil content demonstrated an increase in surface hydrophilicity and elongation to break the film. The thermogravimetric analysis revealed a decrease of polymer thermal stability by increasing clove oil concentration. The antibacterial activities against four different bacterial strains (two-gram positive: Staphylococcus aureus and Bacillus cereus & two-gram negative: Pseudomonas aeruginosa and Escherichia coli) were promoted by addition of clove oil. Although the natural source of clove oil, the bio-evaluation of plasticized membranes showed an increase in hemolysis percent (%) and thrombus weight. It can be concluded that the addition of clove to PVC need to further studies for applying in blood bags.
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Objective:To establish a GC-MS method for the simultaneous determination of 16 phthalate ester plasticizers in oral liquid preparations, compare the purification effect of liquid preparations by liquid-liquid extraction and solid phase extraction and opti-mize the operating parameters to determine the optimal experimental conditions. Methods:The samples were operated by liquid-liquid extraction and solid phase extraction, respectively. Selective ion monitor ( SIM) was adopt, phthalate esters were identified by the rela-tive abundance of major characteristic ions and the content was determined by an external standard method. Results:When the samples were operated by liquid-liquid extraction, the interference was strong with many impurity peaks. Therefore, the solid phase extraction was adopted for the sample pretreatment. GC-MS was used to detect the residues of 16 phthalate ester plasticizers in oral liquid prepara-tions. The detection limit was 0. 02μg·g-1 ,while the calibration curve showed good linearity within the range of 0. 25-8. 0μg·ml-1 with the correlation coefficient between 0. 990 7 and 0. 999 8. The average recoveries were 76. 0%-95. 4%. The relative standard devi-ations were between 2. 3% and 9. 6%(n=6). Conclusion: Pretreated by solid phase extraction, the residues of 16 phthalate ester plasticizers in oral liquid preparations can be detected by GC-MS with the properties of simple, fast, precise and sensitive, and it is suitable for the determination of phthalate esters in oral liquid preparations.
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Objective:To enhance the management level of drug emergency inspection. Methods: The emergency inspection of plasticizers was used as the example, and the management in the whole inspection procedures was reviewed to summarize the difficulties and solutions and analyze the management features of drug emergency inspection. Results and Conclusion: There are three keys in successful drug emergency inspection, including correct top-level design, high efficient execution teams and necessary guarantee sys-tems.
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Present research is aimed towards designing and development of environmental protection plasticizers using the fractionation heavy component in the industrial production of corn stalks as raw material. The plant-based rubber oil (PBRO) plasticizers are the reactants of the dihydric alcohols (Polyols) in heavy component with phthalic anhydride (PA) (the molar ratio of Polyols/PA as 2 : 1) at the temperature range of 180 -190ºC. The main advantage is that this substance does not contain any of the sixteen hazardous substances of PAHs (polycyclic aromatic hydrocarbons) and 38 hazardous substances of PAHs (polycyclic aromatic hydrocarbons) recorded in EU REACH regulation. In plasticization of NBR, the dosage of PBRO can reach 25 phr (parts per hundreds of rubber), but the plasticizing effects of PBRO is inferior to common rubber oil (paraffin oil, naphthenic oil, aromatic hydrocarbon oil and Dioctyl phthalate). In plasticization of SBR, the maximum amount of PBRO is 20 phr. Although the mechanical properties decrease; the aging resistance and thermal stability (the temperature of maximum weight losses of PBRO as 302ºC) are slightly higher than that of common rubber oil.
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With the development of modem technology,more and more plastic products are widely used in various fields,while bringing significant convenience to the society,it also leads to more and more environmental estrogen.The influence of plasticizer is increasing,especially on the development of children.Extensive contacting with plasticizer is considered to be closely related with gonadal digenesis,obesity and other problems in children.This review focuses on the latest research results about the basic and clinical experiments of Di (2-ethylhexyl) phthalate (DEHP),which illuminate the effects of DEHP on children's growth and metabolism,and lay foundations for rational clinical intervention and scientific plasticizer's application.
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OBJECTIVE: To develop GC/MS method in detect plasticizers in compound aluminum hydroxide tablets adsorbed from pharmaceutical packaging. METHODS: The column: HP-5MS silica capillary column (30 m × 0.25 μm, 0.25 mm) was used; Ion source temperature was 230°C; Quadrupole temperature was 150°C; The total ion scanning rang: m/z 50~500. RESULTS: The diethylhexyl phthafate linearity was in the range of 0.5 -20.0 μg · mL-1 with a regression coefficient of 0.9990. The average recovery of this method was 98.8%, and RSD was 1.4%. The RSD of intra-day and inter-day was 2.8% and 3.1% respectively. CONCLUSION: This method is specificity, sensitive, and can be applied to detect and research DEHP which may be adsorbed or penetrated into drugs. Copyright 2012 by the Chinese Pharmaceutical Association.
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OBJECTIVE: To establish a method for the determination the contents of dimethyl phthalate (DMP), diethyl phthalate (DEP) and dibutyl phthalate (DBP) in lansoprazole enteric-coated capsules. METHODS: Based on RP-HPLC/UV, the method used C18 column (4.6 mm × 250 mm, 5 μm) for separation, methanol-water (75: 25) as mobile phase for isocratic elution and detection wavelength 230 nm. RESULTS: The quantification of diethyl phthalate in four batches of lansoprazole enteric-coated capsules was carried. The concentration and UV peak area with a good linear relationship within the following: the linear equation of DMP was Y = 48.848ρ - 2.8112 (r = 0.9999) in range of 1.4 - 14 μg · mL-1, the linear equation of DEP was Y = 67.619ρ - 30.754 (r = 0.9990) in the range of 1.36 - 20.4 μg · mL-1. The linear equation of DBP was Y = 36.759X - 4.8507 (r = 0.9999) in the range of 1.5 - 15.5 μg · mL-1. The sample recovery of DMP, DEP and DBP was 91.3%, 96.1% and 94.7%. The RSD of sample recovery was 2.9%, 4.4% and 4.7%. CONCLUSION: The method is simple, sensitive and with a strong anti-interference ability. It can determination accurately the contents of DMP, DEP and DBP in lansoprazole enteric-coated capsules. Copyright 2012 by the Chinese Pharmaceutical Association.
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OBJECTIVES: The aim of the present investigation was to form matrix patches with ethyl cellulose (EC) as the base polymer, polyvinyl pyrrolidone (PVP) as the copolymer, plasticizer with dibutyl phthalate (DBP) or acetyl tributyl citrate (ATBC) and the drug glipizide (gz) by the solvent casting method. Physicochemical properties of the patches and in vitro drug release were determined in a modified Keshary-chien diffusion cell to optimize the patch formulations with the help of experimental data and figures for further studies. TECHNIQUES: EC and PVP of different proportions with different weight percentages of either DBP or ATBC and a fixed amount of glipizide were taken for matrix patch formations. The dried patches were used for measuring their drug contents as well as their thicknesses, tensile strengths, moisture contents and water absorption amounts in percentage. In vitro release amounts at different intervals were measured by UV-spectrophotometer. RESULTS: Drug contents varied from 96 - 99 percent. Thickness and tensile strength varied due to weight variation of the ingredients in the matrix patches. Moisture content and water absorption in wt percent were greater for the patches containing higher amount of PVP due to its hydrophilic nature. Variations in drug release were observed among various formulations. It was found that all of the releases followed diffusion controlled zero order kinetics. Two DBP patches yielded better and more adequate release. CONCLUSIONS: The two formulations with DBP were the preferred choice for making matrix patches for further studies.
O objetivo da presente pesquisa foi formar matrizes para bandagens de liberação transdérmica com etilcelulose (EC) como polímero base, polivinilpirrolidona (PVP), como copolímero, plastificante com ftalato de dibutila (DBP) ou citrato de tributilacetila (ATBC) e o fármaco glipizida (gz) pelo método de evaporação do solvente (moldagem com solvente). As propriedades físico-químicas das bandagens e a liberação do fármaco in vitro na célula de difusão de Keshary-chien modificada foram determinadas para aperfeiçoar as formulações das bandagens com o auxílio de dados experimentais e figuras para estudos posteriores. EC e PVP em diferentes proporções com porcentagens diferentes de massa tanto de DBP quanto de ATBC e quantidade fixa de glipizida foram utilizadas como matrizes para a formação de bandagens de liberação transdérmica. As bandagens secas foram empregadas para medir seus conteúdos em fármaco e, também, a sua espessura, resistência à tensão, conteúdos de umidade e porcentagem de absorção de água. As quantidades liberadas in vitro em diferentes intervalos de tempo foram medidas por espectrofotômetro de UV. Os conteúdos de fármaco variaram de 96 a 99 por cento. A espessura e a resistência à ruptura variaram devido à variação de massa dos componentes da matriz das bandagens. O conteúdo de umidade e a água absorvida, em porcentagem de massa, foram maiores para as bandagens que continham grandes quantidades de PVP devido à sua natureza hidrofílica. As variações na liberação de fármaco foram observadas entre as várias formulações. Todas as liberações seguiram a cinética de difusão controlada de ordem zero. Duas bandagens DBP resultaram em melhor e mais adequada liberação. As duas formulações com DBP foram escolhidas para a preparação de matriz de bandagens para estudos posteriores.