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1.
Acta Pharmaceutica Sinica ; (12): 134-141, 2022.
Article in Chinese | WPRIM | ID: wpr-913178

ABSTRACT

Nanotechnology has shown broad application prospects in the diagnosis and treatment of cancer. Currently, nearly 80 cancer nanomedicines are under clinical investigation, and many have been approved with enhanced anti-tumor efficacy and decreased side effects. However, the presence of various barriers in related basic research, process control and clinical trials lead to extremely low translation rate. From the perspective of clinical commercialization, we summarized the progress, clinical status, challenges and opportunities of cancer nanomedicine, and presented a cutting-edge prospect on the rational design of nanomedicine and clinical trial strategies.

2.
Acta Pharmaceutica Sinica ; (12): 2513-2521, 2021.
Article in Chinese | WPRIM | ID: wpr-886964

ABSTRACT

italic>Tert-butanol is an organic solvent, widely used in the medical field and chemical industry. It could be characterized by high crystallization temperature and vapor pressure. It could be easily sublimed and removed during the freeze-drying process. This review mainly describes the use of tert-butanol in the lyophilized formulations of poorly soluble drugs, the lyophilization solvent of porous structure productions, and as an ice crystal growth guider. In addition, the application of tert-butanol in nano drugs and aerogels has also been reviewed, as well as the current research progress in its quality and safety.

3.
Chinese Journal of School Health ; (12): 1093-1096, 2021.
Article in Chinese | WPRIM | ID: wpr-886350

ABSTRACT

Objective@#To understand the Implementation of Comprehensive Evaluation of School Health (GB/T 18205-2012) and associated factors, so as to provide rationalization proposals for future revision of standards.@*Methods@#A questionnaire survey was conducted on 436 schools, 56 health supervision agencies and 55 disease control agencies in Liaoning Province, and the main contents include the investigation of awareness rate, training, application, rationality and application of evaluation items and indicators.@*Results@#Totally 44 supervision agencies and 29 CDCs had independent school health departments, with significant differences in faculty equipment ( t =8.53, P <0.05). The standard was trained in 100% of municipal supervision agencies, 22.50% of district and county level, 46.15% of municipal CDC ,50.00% of district county CDC; 61.54% of municipal and 45.00% of district and county supervision agencies conducted evaluations in accordance with this standard, 53.85% of the municipal CDC, 60.00% of county CDC jointly completed the standard; 30.77% of municipal and 52.50% of district and county supervisory bodies informed the educational administration of the results of the comprehensive evaluation.@*Conclusion@#The establishment of school health professional departments and the training of management objects affect the implementation of comprehensive evaluation of school health, so it is necessary to combine the actual work to modify some of the important indicators, and strengthen the application of comprehensive evaluation results.

4.
Article in Chinese | WPRIM | ID: wpr-879086

ABSTRACT

Methotrexate(MTX) is a commonly used antimetabolite, which can be used in the treatment of a variety of diseases. However, hepatotoxicity in the use of MTX severely limits its clinical use. Therefore, how to prevent and treat hepatotoxicity of MTX has become an urgent clinical problem. This paper summarizes and analyzes relevant literatures on the prevention and treatment of hepa-totoxicity caused by MTX with traditional Chinese medicines and natural medicines in recent years. MTX-induced hepatotoxicity mechanisms include folate pathway, oxidative stress damage and adenosine pathway, of which oxidative stress theory is the main research direction. A total of 14 kinds of traditional Chinese medicine and natural medicine extracts including white peony root, and 21 kinds of natural monomer compounds, including berberine, play an anti-MTX-induced hepatotoxic effect by resisting oxidative stress, inhibiting inflammation and regulating signal pathways. According to current studies on the prevention and treatment of hepatotoxicity induced by MTX with traditional Chinese medicines and natural medicines, there are insufficiencies, such as partial and superficial mechanism studies, inadequate combination of experimental research and clinical practice, non-standard experimental design and lack of application of advanced technologies and methods. This paper systematically reviewed the effects and mechanisms of traditional Chinese medicines and natural medicines against hepatotoxicity induced by MTX and defined current studies and deficiencies, in the expectation of proposing new study strategies and directions and providing scientific basis for rational clinical use of MTX and development of new drugs against MTX hepatotoxicity.


Subject(s)
Chemical and Drug Induced Liver Injury/prevention & control , Drug-Related Side Effects and Adverse Reactions , Humans , Liver/metabolism , Medicine, Chinese Traditional , Methotrexate/toxicity , Oxidative Stress
5.
Article in Chinese | WPRIM | ID: wpr-879015

ABSTRACT

The volatile oil from Mastiche and Olibanum medicinal materials was extracted by steam distillation, and the chemical components of the volatile oil were analyzed by GC-MS technology. The differences of the volatile oil components were compared and study on the Helicobacter pylori in vitro antimicrobial activitiy was conducted. The results showed that the yields of the volatile oil from Mastiche and Olibanum were 11.93% and 2.40%, respectively. A total of 46 compounds(91.31%) were identified from the volatile oil from Mastiche annd 35 compounds(92.49%) from Olibanum. The classification and comparison study of the components showed that the content of monoterpenes in the volatile oil from Mastiche was the highest(40.69%), followed by alcohols(28.48%); while the content of alcohols in the volatile oil from Olibanum was the highest(35.81%), followed by esters(24.92%). There were significant differences in the components of volatile oil from Mastiche and Olibanum, which might be one of the reasons for the difference in efficacy and application. In vitro bacteriostatic experiments showed that the minimum inhibitory concentration(MIC) of the volatile oil from Mastiche against H. pylori was 1 mg·mL~(-1), and the MIC of the volatile oil from Olibanum against H. pylori was more than 1 mg·mL~(-1). In combination with the results of the oil yield experiment, Mastiche had the advantage of inhibiting H. pylori activity. The research results provide scientific basis for the rational application of Mastiche and Olibanum.


Subject(s)
Anti-Bacterial Agents/pharmacology , Frankincense , Gas Chromatography-Mass Spectrometry , Helicobacter pylori , Monoterpenes/analysis , Oils, Volatile/pharmacology
6.
Chinese Journal of School Health ; (12): 1423-1425, 2021.
Article in Chinese | WPRIM | ID: wpr-904564

ABSTRACT

Objective@#To explore the associated factors in the implementation of the "random" sampling inspection of the lighting institutions in kindergartens, outofschool training institutions and primary and secondary schools in 2019 (Supervision Letter [2019] No. 314 of National Health Office) (hereinafter referred to as the "Plan"), and to provide reference for better implementation of the Plan.@*Methods@#A survey of schoolbased myopia prevention and control was conducted in 23 provincial, municipal and countylevel health supervision institutions in China. The main contents of the survey focused on the introduction, implementation and implementation of the program.@*Results@#The implementation of the "plan" was significantly associated with the specific work organized and coordinated by the health administrative department, clear responsibility of various departments, and collaboration with educational institutions[OR(95%CI)=1.57(1.05-2.36), 0.05(0.03-0.10), 0.31(0.19-0.52), 0.03(0.01-0.09), 0.12(0.04-0.37), P<0.05]. It was also associated with independent school health supervision department, one and two fulltime school health supervision staff equipment, onsite quick inspection of health supervision institutions, school selfexamination[OR=1.87(1.33-2.62), 0.62(0.40-0.97), 2.37(1.82-3.09), 1.62(1.09-2.40), P<0.05].@*Conclusion@#The program needs to be implemented through multiple departments and is associated with multiple factors. It is of great importance to strengthen multisector collaboration and clarify the responsibility of various departments for the health supervision of schoolbased myopia prevention and control.

7.
Article in Chinese | WPRIM | ID: wpr-878838

ABSTRACT

The aim of this paper was to explore the potential molecular mechanism of Banxia Xiexin Decoction in the treatment of colon cancer through pharmacology network and molecular docking methods. The chemical constituents and action targets of 7 herbs from Banxia Xiexin Decoction were collected by using TCMSP database,Chinese Pharmacopoeia and literatures consultation. GeneCards database was used to predict the potential targets of colon cancer. GO biological process analysis and KEGG pathway enrichment analysis of the disease and drug intersection targets were carried out through DAVID database. "Component-target-pathway" network and protein-protein interaction(PPI) network were construction by using Cytoscape and STRING database,and then the core components and targets of Banxia Xiexin Decoction in the treatment of colon cancer were selected according to the topological parameters. Finally, Autodock Vina was used to realize the molecular docking of core components and key targets. The prediction results showed that there were 190 active compounds and 324 corresponding targets for Banxia Xiexin Decoction,involving 74 potential targets for colon cancer. Cytoscape topology analysis revealed 11 key targets such as STAT3,TP53,AKT1,TNF,IL6 and SRC, as well as 10 core components such as quercetin,β-sitosterol,baicalein,berberine,and 6-gingerol.In bioinformatics enrichment analysis, 679 GO terms and 106 KEGG pathways were obtained, mainly involving PI3 K-AKT signaling pathway,TNF signaling pathway and TP53 signaling pathway. The results of molecular docking showed that baicalein,berberine,licochalcone A and 6-gingerol had a high affinity with SRC,STAT3,TNF and IL6. The results suggested that Banxia Xiexin Decoction could play an anti-colon cancer effect by inhibiting cell proliferation, regulating cell cycle, inducing apoptosis and anti-inflammatory function. The study revealed the multi-components,multi-targets and multi-pathways molecular mechanism of Banxia Xiexin Decoction,which could provide scientific basis and research ideas for the clinical application of Banxia Xiexin Decoction and the treatment of colon cancer with compound Chinese medicines.


Subject(s)
Colonic Neoplasms , Drugs, Chinese Herbal , Humans , Molecular Docking Simulation , Technology
8.
Acta Pharmaceutica Sinica ; (12): 1225-1233, 2019.
Article in Chinese | WPRIM | ID: wpr-780225

ABSTRACT

Sangzhi alkaloids (SZ-A) are derived from traditional Chinese medicine Ramulus Mori, serving well as an innovative antidiabetic drug, due to α-glucosidase inhibition. To evaluate the potency of glucosidase inhibitory effect of SZ-A, the enzyme-based screening platforms, including sucrase, maltase and amylase were established, and IC50 was calculated. The effects of SZ-A on postprandial blood glucose at a single dose, oral sucrose, starch and glucose loading were determined in normal ICR mice and alloxan-induced hyperglycemic mice. To confirm the anti-diabetic effects of SZ-A on glucose and lipid metabolism after long-term administration, the postprandial and fasting blood glucose, serum insulin, urinary glucose levels, glycosylated serum proteins and blood lipid levels were determined in high-fat fed C57 obese mice (pre-diabetic HFC57 mice) and diabetic rats induced by streptozotocin (STZ). The Experimental Animal Welfare Ethics Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College approved all of the protocols for this research. We found that SZ-A exhibited a significant inhibitory effect on the sucrase and maltase. SZ-A showed no effect on amylase. In normal ICR mice and alloxan-induced hyperglycemic mice, SZ-A at a single dose significantly delayed and reduced the peak of blood glucose after sucrose or starch loading, but showed no effect on the increase of blood glucose after glucose loading. In STZ diabetic rats, SZ-A significantly reduced the postprandial or fasting blood glucose levels, glycosylated serum proteins and urinary glucose. SZ-A also reduced serum triglyceride (TG) and cholesterol (TC) levels after 3 weeks of treatment. SZ-A ameliorated the postprandial blood glucose or the fasting blood glucose elevation, and reduced the incidence of hyperglycemia in HFC57 mice. SZ-A decreased the basal insulin level, improved insulin sensitivity, and ameliorated glucose intolerance in pre-diabetic HFC57 mice. Our results indicated that SZ-A had a novel inhibitory activity on α-glucosidase, especially on disaccharidases. SZ-A at a single dose significantly reduced the peak of blood glucose elevation and delayed the increase of blood glucose in normal and diabetic mice after disaccharide and polysaccharide loading. Long-term SZ-A treatment improved glucose and lipid metabolic profiles by delaying carbohydrate absorption from the intestine and reduced the postprandial blood glucose levels in both pre-diabetic and diabetic animal models. Therefore, SZ-A application may display a beneficial role in preventing the development and complications of diabetes.

9.
Article in Chinese | WPRIM | ID: wpr-802281

ABSTRACT

Objective:To establish HPLC-UV fingerprints of Ilex pubescens pieces,and simultaneously determine two components in 46 batches of I. pubescens in pieces of I. pubescens saponin A1 and B1,in order to provide a reference for the quality standard of I. pubescens slices. Method:Methanol was used to extract the I. pubescens saponin samples,and the extracts were measured by HPLC-UV with the absorption wavelength at 210 nm. Kromasil C18 column (4.6 mm×250 mm,5 μm) was used for determining the extracts at a flow rate of 1.0 mL·min-1. The mobile phase condition was acetonitrile-0.1% phosphoric acid aqueous solution with gradient mode. The chromatographic fingerprint similarity evaluation system of traditional Chinese medicine (2012 edition) was used to analyze I. pubescens fingerprints. SPSS 20.0 software was used to cluster the peak area of common peaks. Principal component analysis was performed to reduce the dimension of common peaks. Result:There were great differences between the root and stem parts in I. pubescens fingerprints. The fingerprints of roots and stems of I. pubescens were established respectively,cluster results assorted the roots of I. pubescens into three categories andthe branches of I. pubescens into two categories. The integrity and difference of I. pubescens decoction pieces from different parts and places of origin were compared,and the principal component analysis was performed to screen out the common components that played a decisive role in fingerprint of I. pubescens pieces. And the common peaks were determined. The content of saponin A1 and saponin B1 in Radix I. pubescens were determined. Conclusion:The established I. pubescens fingerprints and content determination methods are simple and suitable. Cluster analysis and principal component analysis are used to screen out the key components of quality control of I. pubescens. The results can provide references for quality control of I. pubescens.

10.
Acta Pharmaceutica Sinica ; (12): 403-409, 2018.
Article in Chinese | WPRIM | ID: wpr-779889

ABSTRACT

The development of tumor tissue is a complicated process, which is closely related to tumor microenvironment. In order to simulate the tumor tissue in vivo, non-contact co-culture of human breast adenocarcinoma cells (MCF-7 cells) and human umbilical vein endothelial cells (HUVECs cells) using transwell cell culture plate was developed in this study. The cell viability, morphology, cell resistance, cell cycle and vascular endothelial growth factor (VEGF) protein content of co-cultured MCF-7 and HUVECs cells were investigated, and compared with those of separately cultivated MCF-7 and HUVECs cells during the same period. Different to the separately cultured MCF-7 and HUVECs cells, co-cultured MCF-7 and HUVECs cells exhibited higher cell viability, deformed cell morphology, lower cell resistance, higher proportion of S and G2/M phases and higher VEGF protein content (about 1.4−2 times). The double cell model via non-contact co-culture of MCF-7 and HUVECs cells constructed in this study could simulate the interaction between tumor cells and tumor vascular endothelial cells in vivo, which may provide a more realistic model for subsequent study of drug release system in the control of breast cancer in vitro.

11.
Article in Chinese | WPRIM | ID: wpr-279195

ABSTRACT

Based on DPPH method, the antioxidant activities of Shenqi Tongmai Yizhi particles with different extraction processes were compared. The contribution to the anti-oxidant capacity in vitro was explored by means of grey relational analysis on different chemical compositions in the fingerprint. The results showed that the IC₅₀ concentration values of water extract, water extract from alcohol precipitation, alcohol extract, and alcohol and water extract were 0.801 4, 0.859 1, 0.796 1, 0.918 0 g•L⁻¹; and the alcohol extract is the best method to extract antioxidative components, with the highest antioxidant activity and lowest IC₅₀. When the mass concentration of the herbs reached a certain degree, its free radical clearance rate was similar to that of vitamin C control group. The order of different chemical contributions of constituents to the antioxidant activity in the fingerprint was 4>3>33>53>9>10>11>34>15>59>8>61>52>20>42>18>29. The preliminary exploration for the spectrum efficiency relations provides reference for studying traditional Chinese medicine compound processing method and the pharmacodyamic material basis.

12.
Article in Chinese | WPRIM | ID: wpr-246111

ABSTRACT

Microscopic identification and NIRS methods were applied to identify Clematidis Radix et Rhizoma of two different origins. The results showed that both methods could identify the samples. NIRS could identify the two samples nondestructively, and provides a basis for establishment of a standard herbs radix clematidis NIRS fingerprint in the future.


Subject(s)
China , Clematis , Chemistry , Classification , Drugs, Chinese Herbal , Chemistry , Rhizome , Chemistry , Spectroscopy, Near-Infrared , Methods
13.
Article in Chinese | WPRIM | ID: wpr-246108

ABSTRACT

L9 (3(4)) orthogonal experiment was used to design the extraction technology of compound Clematidis Radix spray. Weight coefficients of active ingredients and dry extract rate were solved by information entropy. Support vector machine (SVM) was established and the model parameters were optimized through the genetic algorithm. Grid search algorithm was used for optimization of extraction technology of Clematidis Radix spray. The optimal extraction technology was to extract Clematidis Radix spray in water with 6 times the weight of herbal medicine for 3 times, with 2 h once. Bias of value between real and predicted by SVM was 1.23%. SVM was compared with traditional intuitive analysis of orthogonal design. It indicates that the new method used to optimize the extraction parameters of compound Clematidis Radix spray is more accurate and reliable.


Subject(s)
Clematis , Chemistry , Drugs, Chinese Herbal , Chemistry , Plant Roots , Chemistry , Support Vector Machine , Technology, Pharmaceutical
14.
Article in Chinese | WPRIM | ID: wpr-279072

ABSTRACT

<p><b>OBJECTIVE</b>To explore the effects of body mass index (BMI) and the levels of serum inflammatory cytokines on asthma control in children with asthma.</p><p><b>METHODS</b>One hundred and sixteen children with asthma were divided into three groups: normal (n=59), thin (n=31), and obesity (n=26) based on their BMI. The levels of interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α) were determined using ELISA, and the level of high-sensitivity C-reactive protein (hs-CRP) was measured by immunoturbidimetric assays. Asthma control status in each group was evaluated by the Childhood Asthma Control Test (C-ACT) after 4 weeks of treatment.</p><p><b>RESULTS</b>The serum levels of IL-6, hs-CRP, and TNF-α were highest in the obesity group, followed by the thin group and the normal group (P<0.05), while the C-ACT score was highest in the normal group, followed by the thin group and obesity group (P<0.05). The normal group had significantly higher complete controlled and partially controlled rates than the thin and obesity groups (P<0.05); however, there were no significant differences between the thin and obesity groups (P>0.05). The levels of IL-6, hs-CRP, and TNF-α were negatively correlated with the C-ACT score (P<0.05). There were no significant correlations of BMI with the C-ACT score and levels of IL-6, hs-CRP, and TNF-α (P>0.05).</p><p><b>CONCLUSIONS</b>When BMI is too high or too low, the levels of serum inflammatory cytokines are all increased, which is harmful to asthma control. Maintaining a healthy weight in children with asthma may reduce the levels of serum inflammatory cytokines and improve the asthma control rate.</p>


Subject(s)
Asthma , Allergy and Immunology , Therapeutics , Body Mass Index , C-Reactive Protein , Child , Child, Preschool , Cytokines , Blood , Female , Humans , Interleukin-6 , Blood , Male , Tumor Necrosis Factor-alpha , Blood
15.
Article in Chinese | WPRIM | ID: wpr-279043

ABSTRACT

<p><b>OBJECTIVE</b>To study the risk factors for moderate and severe iron deficiency anemia (IDA) in infants aged 6-12 months, and to preliminarily investigate the effects of IDA on the neuromotor development and temperament characteristics of infants.</p><p><b>METHODS</b>A total of 326 infants aged 6-12 months with IDA were classified into three groups: mild IDA (n=176), moderate IDA (n=111), and severe IDA (n=39) according to the severity of anemia. The risk factors for moderate or severe IDA were investigated by multivariate logistic regression analysis. Three hundred and forty-six infants without IDA who showed matched age, sex, and other backgrounds were selected as the control group. The Gesell Development Diagnosis Scale was used to evaluate children's mental development. The Temperament Scale for infants was used for evaluating children's temperament.</p><p><b>RESULTS</b>The univariate analysis showed that the severity of IDA was associated with sex, birth weight, gestational age, multiple birth, maternal anemia during pregnancy, and mother's lack of knowledge about IDA (P<0.05). Setting the mild IDA group as control, the multivariate logistic regression analysis showed that multiple birth, premature birth, low birth weight (<2500 g), maternal anemia during pregnancy, breast feeding, and mother's lack of knowledge about IDA were the risk factors for severe IDA (OR>1; P<0.05); premature birth, breast feeding, and mixed feeding were the risk factors for moderate IDA (OR>1; P<0.05). The IDA group had significantly lower scores in Gesell general development quotient, gross motor, adaptive behavior, and fine motor than the control group (P<0.05). The IDA group had higher percentages of children with difficulty and intermediate difficulty temperaments than the control group (P<0.05). The IDA group had significantly higher scores in activity level, rhythmicity, adaptability, and perseverance than the control group (P<0.05).</p><p><b>CONCLUSIONS</b>The severity of IDA is associated with premature birth, multiple birth, low birth weight, feeding pattern, maternal anemia during pregnancy and mother's lack of knowledge about IDA in infants aged 6-12 months. Infants with IDA have delayed neuromotor development and most of them have negative temperaments. More attention should be paid to mental and behavior problems for the infants. It is necessary to provide guidance for their parents in feeding and education.</p>


Subject(s)
Anemia, Iron-Deficiency , Child Development , Female , Humans , Infant , Infant, Low Birth Weight , Logistic Models , Male , Psychomotor Performance , Risk Factors
16.
Article in Chinese | WPRIM | ID: wpr-236031

ABSTRACT

The research aimed to evaluate the intestinal absorption of alkaloids extracted by decoction and alcohol extraction proces- ses from Rhizoma Coptidis-Rheum rhabarum herbal pair via everted gut sacs. Berberine, palmatine, coptisine and epiberberine were the main alkaloids in this herbal pair and taken as the standard indexes in the quantitative analysis with multi-components by single marker (QAMS) method, in order to calculate absorption rate constant (Ka) and evaluate intestinal absorption characteristics of these four alkaloids extracted by different extraction methods in different intestinal segments in rats. The results showed that the four alkaloids extracted by two different processes in high, medium and low doses had linear absorption properties in the small intestine segment, which conformed to zero-order absorption rate, intestinal segment than 0.99. The absorption rate constant (Ka) of decoction group was higher than that of alcohol extraction group.


Subject(s)
Alkaloids , Pharmacokinetics , Animals , Coptis , Chemistry , Intestinal Absorption , Male , Rats , Rats, Sprague-Dawley , Rheum , Chemistry
17.
Article in Chinese | WPRIM | ID: wpr-854557

ABSTRACT

Objective: To determine the rheological properties of Dange ophthalmic in-situ gel and its common gel by using dynamic rheological experiments. Methods: Dange ophthalmic in-situ gel was prepared by adopting Poloxamer as thermosensitive material, and Dange gel was prepared by carbopol. Anton Paar MCR302 Rheometer was used to determine the rheological parameters of above two kinds of gel at different temperatures which speculated the phase transition time and gelling temperature of in-situ gel. Results: Dange ophthalmic in-situ gel was Newtonian liquid at low temperature, with its viscous modulus dominated. It was shear-thinning pseudoplastic fluid under the conditions of phase transition at room temperature, with its elastic modulus dominated. The phase transition temperature (Tg) was (24.4 ± 0.1)°C, and the gelling time was 9 s. Dange gel existed in network structure among a certain temperature range, it was stable and did not change with temperature. Conclusion: The test has established the rheological evaluation system of Dange ophthalmic in-situ gel or its common gel, accurately evaluated the rheological properties of the two gels by dynamic rheological parameters, and it can be used as the basis for the quality control of products.

18.
Article in Chinese | WPRIM | ID: wpr-300253

ABSTRACT

In this study, superfine comminution technique was applied to destroy the cell wall of the Panax notoginseng, and then the influence of the particle sizes and the content of effective composition of the P. notoginseng powders were learned, comparing with the common powders. Superfine comminution technique was used for 0.5, 1, 1.5, 2 h, respectively and the particle sizes, unifirmity were regarded as the evaluation index. Then, the sizes of the powders was measured that were crashed with different time by Malvern Mastersizer 2000 + Scricco 2000 and the total content of ginsenoside Rg1, ginsenoside Rb1, notoginsenoside R1 in the superfine powder of P. notoginseng were determined by HPLC-ELSD. Finally, the powder that crashed for two hours possess the more uniform in sizes that is at cell level, D50 is about 9.599 microm, the size distribution was presented as one peak, the other three samples were two peaks. The total content of the three saponins in the four samples that crashed for 0.5, 1, 1.5, 2 h by superfine comminution technique were 7.7%, 7.5%, 7.5%, 8.3%. However, the total content of the three ingredients in the common powder was 5.0%. This investigation indicated that superfine comminution technique has remarkable effect on particle size and uniformity of the common powder of P. notoginseng. By comparing the superfine powder and common powder, it was found that the method obviously improved the total content of the saponins and provided a basis for reducing dosage of notoginseng in clinical application, but the content and the crashed time were not the linear relationship. The crashed time can be chosen by combining with the demand partical sizes in the production.


Subject(s)
Chemistry, Pharmaceutical , Methods , Drugs, Chinese Herbal , Chemistry , Panax notoginseng , Chemistry , Particle Size , Powders , Chemistry
19.
Acta Pharmaceutica Sinica ; (12): 956-962, 2014.
Article in Chinese | WPRIM | ID: wpr-299183

ABSTRACT

Injectable lipid emulsions have been routinely used in patients since 1960s as a nutritional supplement for patients requiring parenteral nutrition. In recent years, lipid injectable emulsions have been extensively studied as a kind of novel drug carrier, also the quality problems of the lipid emulsion attract more and more attentions gradually. Large diameter tail of injectable lipid emulsions as a significant quality control indicator should pay more attention. Regarding to the defect of detecting large diameter tail of lipid injectable emulsions in our country, the purpose of this article is to summarize the techniques of detecting large diameter tail, illustrate the impacts of large lipid droplet on the quality of lipid injectable emulsions, emphasize the importance of detecting large diameter tail in lipid emulsions and provide guidance for researching and developing lipid emulsions in domestic market.


Subject(s)
Drug Stability , Fat Emulsions, Intravenous , Chemistry , Lipids , Chemistry , Parenteral Nutrition Solutions , Chemistry , Particle Size , Quality Control
20.
Acta Pharmaceutica Sinica ; (12): 1600-1606, 2014.
Article in Chinese | WPRIM | ID: wpr-299090

ABSTRACT

Bicyclol with benzyl alcohol structure, is a poorly water-soluble drug, used for the treatment of chronic hepatitis B. To increase the drug solubility and oral bioavailability, a Bicyclol-phospholipid complex was studied on its preparation, formation mechanism, and the influence on drug physicochemical properties and oral absorption. The complex was prepared by a solvent evaporation method. The optimal formulation was selected by orthogonal experimental design, and a reasonable evaluating method of the complexation rate was established. Various methods, such as differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and 31P nuclear magnetic resonance (31P-NMR), were used to explore the phase state and formation mechanism of the complex. The solubility of drug in complex was investigated in water/n-octanol. Preliminary study of its absorption and liver tissue distribution in rats was also carried out. The results showed that Bicyclol and phosphatidylcholine can be complexed entirely in the molar ratio 1 : 2. Bicyclol was dispersed in phospholipids as amorphous state. They were combined by intermolecular hydrogen bond due to charge transfer effect which occurred between the two polarities of the double bond between phosphorus and oxygen (P=O) of phosphatidylcholine and benzalcohol group of Bicyclol. The solubility of the complex compared to the active pharmaceutical ingredient (API) was effectively enhanced 5.75 times in water and 7.72 times in n-octanol, separately. In addition, drug concentrations were also enhanced 43 times in plasma and 13 times in liver with one hour after administering the complex to rats via oral gavage. All of these indicated that Bicyclol with benzalcohol group can interact with phospholipids to form complex, improving drug's physicochemical properties, thus further increasing its absorption and target tissue distribution. This study also provided theoretical reference for the research of other benzalcohol derivatives complexed with phospholipids.


Subject(s)
1-Octanol , Animals , Biological Availability , Biphenyl Compounds , Pharmacokinetics , Calorimetry, Differential Scanning , Chemistry, Pharmaceutical , Phospholipids , Pharmacokinetics , Rats , Solubility , Spectroscopy, Fourier Transform Infrared , Tissue Distribution , X-Ray Diffraction
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