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Objective To investigate the expression of miR-124 in glioblastoma (GBM) cell lines LN229 and LN229R,as well as the regulatory mechanism of miR-124 on radiosensitivity of LN229R cells.Methods miR-124 mimic (miR-124) and negative control (miR-NC),STAT3 overexpression plasmid (STAT3) and pcDNA3.1 vector (pcDNA) were transfected or co-transfected into radioresistant glioma cells LN229R.qRT-PCR was employed to analyze the expression of miR-124 in LN229 and LN229R cells.The survival rate and sensitivity-related parameters of LN229R cells at different doses were analyzed by cloning formation assay.Cell apoptosis of LN229R was evaluated by flow cytometry.Targeting gene of miR-124 was predicted using Targetscan software and verified by the double-luciferase reporter assay.Western blot assay was performed to detect STAT3 protein expression.Results The expression of miR-124 in LN229R cells (0.32 ± 0.03) was significantly lower than that in LN229 cells (1.02 ± 0.09) (t =12.780,P＜0.05).Transfection of miR-124 mimics promoted the expression of miR-124 in LN229R cells (4.02±0.39) compared with miR-NC group (0.95±0.06) (t=13.476,P＜0.05).After 8 Gy irradiation,the survival rate of LN229R cells transfected with miR-124 mimics (0.003 ± 0.000 4) was significantly lower than that in miR-NC group (0.033±0.005 0) (t=5.655,P＜0.05),and the apoptosis rate (22.34±2.42) ％ was significantly higher than that in miR-NC group (4.69 ± 0.51) ％ (t =12.361,P＜0.05).STAT3 was identified to be a target gene of miR-124.Exogenous restoration of STAT3 reversed the inhibitory effect of miR-124 on LN229R cell survival.Conclusion miR-124 increases the radiosensitivity of LN229R cells by targeting STAT3.
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Objective To compare the effectiveness of stereotactic hematoma aspiration and conservative treatment for supratentorial hypertensive intracerebral hemorrhage (HICH) with hematoma volume 25-40 ml. Methods Patients with supratentorial HICH admitted to the Department of Neurosurgery, the Fifth Affiliated Hospital of Zhengzhou University from January 2014 to January 2017 were retrospectively enrolled. The incidence of rebleeding, good outcome (defined as the modified Rankin Scale score 0-2 at 3 months after onset) rate, and mortality were compared between the stereotactic hematoma aspiration group and the conservative treatment group. Results A total of 204 patients were enrolled. Their mean age was 61. 3 ±9. 2 years, 114 were males, and their median hematoma volume was 32 ml (interquartile range 25- 39 ml), median baseline Glasgow Coma Scale score was 11 (interquartile range 9-14), and there was no patient with brain herniation. One hundred and twenty patients (58. 8％) underwent stereotactic hematoma aspiration and 84 (41. 2％) received conservative treatment. Compared with the conservative treatment group, the incidence of rebleeding in the stereotactic hematoma aspiration group was significantly lower (2. 5％ vs. 22. 6％, χ2 =20. 788, P < 0. 001), and the rate of good outcome was significantly higher at 3 months after onset (85. 0％ vs. 70. 2％; χ2 = 8. 305, P = 0. 004 ), but there was no significant difference in mortality (5. 0％ vs. 11. 9％, χ2 =3. 259, P =0. 071). Multivariable logistic regression analysis showed that advanced age (odds ratio [OR] 1. 77, 95％ confidence interval [CI] 1. 25-2. 46; P = 0. 006), previous stroke history (OR 1. 36, 95％ CI 1. 12-1. 64; P =0. 032), and conservative treatment (OR 1. 42, 95％ CI 1. 25-1. 78; P = 0. 021) were the independent risk factors for poor outcomes. Conclusions Stereotactic hematoma aspiration can significantly reduce the incidences of rebleeding and risk of the poor outcome in the supratentorial HICH patients with hematoma volume 25-40 ml. Therefore, early active surgical treatment should be considered.
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Objective To study and analyze the current situation of patient medication guide in foreign countries, aiming to provide references for the preparation of patient medication guide in China. Methods The current situation of patient medication guide by consulting literatures was mastered. In addition,the design concept of patient medication guide in foreign countries was summarized, the existing problems were analyzed, and the need for improvement was discussed. Results America,Australia,European countries and some Asian countries have developed a mature patient medication guide system under the supervision of the government departments. Patient medication information overseas takes patients ' health literacy into consideration.It employs the concept of information design,focuses on risks and adverse reactions of drugs,and tells patients how to communicate with doctors and pharmacists.At the same time,it has some problems such as improper content and presentation, excessive emphasis on medication risk, not satisfying drug information demand of patients, as well as a lack of medication information for special groups such as the elderly. Conclusion The design,management and practice of patient medication guide in foreign countries set a good example for us.
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Objective:To determine the equilibrium solubility and the apparent oil/water partition coefficient of nebivolol hydrochloride to provide experimental basis for the development of new preparations.Methods:The concentration of nebivolol hydrochloride was determined by an HPLC method,and a saturated solution method and a shake-flask method were respectively applied to determine the equilibrium solubility and the apparent oil/water partition coefficient of nebivolol hydrochloride in water,0.1 mol·L-1 HCl solution and phosphate buffer solution with different pH values(pH2.0,pH6.8,pH7.4 and pH8.0).Results:At (37±0.5)℃,the equilibrium solubility of nebivolol hydrochloride in water and in 0.1 mol·L-1 HCl solution was 722.53 μg·ml-1and 56.07μg·ml-1,respectively.The apparent oil/water partition coefficient (Log P) of nebivolol hydrochloride was 1.17 and 1.32,respectively.Within the pH range of 2.0-7.4,with the increase of pH value, the equilibrium solubility and the Log P decreased and increased,respectively,while pH value increased from 7.4 to 8.0,the equilibrium solubility of nebivolol hydrochloride increased and Log P decreased.Conclusion:The method is accurate and reliable.Nebivolol hydrochloride has poor water solubility,and the equilibrium solubility and the Log P are both influenced by pH values.
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Objective:To optimize the formula of amlexanox nasal thermosensitive gel spray and establish the quality control meth-od. Methods:Amlexanox nasal thermosensitive gel spray was prepared by a cold dissolving method, and poloxamer 407 (P407) and poloxamer 188 (P188) were used as the carrier materials. Central composite design-response surface methodology was used to optimize the formula with the amount of P407 and P188 as the influencing factors and the gel temperature and the viscosity before gelling as the indices. The content of amlexanox was determined by HPLC. According to Chinese Pharmacopoeia (2010 edition), the other indices of the preparation such as appearance, pH, viscosity, content, total spray times of each bottle and the content of each spray were deter-mined as well. Results:The optimum ratio of P407 and P188 was 17. 0% and 0. 9%,respectively . The average recovery of amlexanox was 98. 8% and RSD was 1. 7%(n=9). The quality of 3 batches of amlexanox nasal thermosensitive gel spray met the related require-ments. Conclusion:The formula and preparation process of amlexanox nasal thermosensitive gel spray are reasonable and feasible with controllable quality, which is worthy of further research.
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Objective:To investigate the effects of three herb extracts on cell proliferation and collagen synthesis in cultured hu-man dermal fibroblasts. Methods:The human dermal fibroblasts were isolated and cultured with tissue explant culture technique. Im-munohistochemical staining was performed to observe vimentin in fibroblasts. The proliferation of fibroblasts was determined by MTT as-say. Hydroxyproline in the cultural medium was determined by a digestion method. Results:The cells were typical fibroblasts, and the immunohistochemistry staining of vimentin in the cells was positive. The three herb extracts could promote the proliferation of the fibro-blasts at appropriate concentrations in a time-dependent manner. After the 72-hour culture in the medium, 0. 312 5-5. 000 0 mg·ml-1 Aloe vera gel extract, 0. 156 3-2. 500 0 mg·ml-1 Bletilla striata extract and 0. 075 0 mg·ml-1 salvianolate showed significant effects on the proliferation of fibroblasts (P<0. 05 or P<0. 01 vs the blank group). Compared with that in the blank group, the amount of hydroxyproline in the three herb extracts cultural medium was also increased (P<0. 05 or P<0. 01). The effect of salvianolate on the cell proliferation was closely related with time and concentration, and the high concentration group could inhibit the growth of fibroblasts as the extension of time. Conclusion:Aloe vera gel extract, bletilla striata extract and salvianolate can promote the proliferation of fi-broblasts and the production of hydroxyproline, which may contribute to the wound healing.
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Objective:To optimize the formula of 5-aminosalicylic acid enema in situ gel. Methods:5-Aminosalicylic acid ene-mas in situ gel was prepared using a cold dissolution method with carbomer as the gel matrix and xanthan gum as the thickener. A 32 full factorial design was used to investigate the effects of the concentrations of carbomer and xanthan gum on the viscosity before and af-ter the gelling, duration of inversion tube and sedimentation rate. Response surface methodology was used to optimize the formula. Re-sults:The quantitative relationships between the two factors and the four evaluation indices were obtained. The optimum formula was as follows:the concentration of carbopol and xanthan gum in the enema was 0. 7% and 0. 15%, respectively. The viscosity before and af-ter the gelling was 500-1 000 mPa·s and 2 200-2 700 mPa·s, respectively. The duration of inversion tube test was 40-80 min and the sedimentation rate was more than 98. 5%. Conclusion:The multi-objective simultaneous optimization of the formula of 5-aminosal-icylic acid enema in situ gel is accomplished by factorial design and response surface methodology.
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Objective:To optimize the formula of ropivacaine hydrochloride transdermal gel. Methods:The steady transdermal rate and cumulative transdermal percentage in 24 h of ropivacaine hydrochloride gel were used as the indices, an orthogonal design was applied to select the optimal formula, and Design Expert 8. 0. 5. 0 software was used to analyze the results. Results: The optimal formula con-tained 2% carbomer, 10% propylene-glycol and 5% Azone. The steady transdermal rate of the optimal formula was 0. 6951 mg·h-1 · cm-2 . The cumulative transdermal percentage in 24 h of the optimal formula was 91. 04%, which was 22. 79% higher than that of ropiva-caine hydrochloride solution with the same concentration. Design Expert 8. 0. 5. 0 software could predict the steady transdermal rate and cumulative transdermal percentage in 24 h of the optimal formula. Conclusion: The preparation design is reasonable, and the gel has promising properties, which is suitable for skin local application.
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Objective:To prepare PLGA nanoparticles modified with folic acid conjugated chitosan oligosaccharide containing pa-clitaxel (F-CS-PLGA-NPs) and study the inhibitory effect on SKOV-3. Methods:F-CS-PLGA-NPs were prepared by an interface dep-osition method, 30% ethanol was used as the release medium for the in vitro release profiles of nanoparticles, and MTT was adopted to evaluate the inhibitory effect of paclitaxel with different formulations and concentrations on SKOV-3. Results:The particle size and zeta potential of F-CS-PLGA-NPs was (321 ± 0. 76) nm and (22. 6 ± 0. 26) mV, respectively, the drug loading was (5. 1 ± 0. 25)%, and the encapsulation efficiency was (41. 96 ± 1. 96)%. F-CS-PLGA-NPs had a similar in vitro release profiles with the ordinary nanoparti-cles ( PLGA-NPs) . About 35% of paclitaxel was released from the nanoparticles in the initial 24 h, and then a near zero order release at a relative slow rate was shown, and the cumulative release rate in 144 h was about 75%. The results of cell experiments suggested that at the same paclitaxel concentration, the inhibition effect of F-CS-PLGA-NPs group was stronger than that of the PLGA-NPs group and the solution group. The inhibition effect of F-CS-PLGA-NPs could be reduced by free folic acid. Conclusion:PLGA nanoparticles modified with folic acid conjugated chitosan oligosaccharide can increase the targeting efficiency in SKOVS-3 tumor cells.
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Objective:To provide reference for the introduction and application of intelligent access system. Methods:The intelli-gent access system and its work process in our hospital were introduced. The application effects in the emergency pharmacy were inves-tigated and the key points that should be paid more attention in the practice were discussed. Results:Comparing with the situation be-fore the application, the system could decrease prescription time by about 26. 1% and reduce walking work intensity by about 5 times, and the drug store room was decreased by about 30%. No dispensing error happened in nearly half a year after the application of the in-telligent access system. Conclusion:The application of intelligent access system in emergency pharmacy is the development trend of the future.
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Objective:To establish a method to determine the content of lidocaine hydrochloride in buccal adhesive tablets contai-ning carbomer as an excipient by HPLC. Methods:Calcium chloride was used to precipitate carbomer in buccal adhesive tablets. The HPLC analysis was performed on a Welch C18 column(250 mm × 4. 6 mm,5 μm)with the column temperature of 40℃. The mobile phase was the mixture of 0. 05% sodium acetate solution(added 50 ml acetic acid into 930 ml distilled water,adjusting pH to 3. 40 with 1 ml·min-1 sodium hydroxide solution)and acetonitrile(70:30). The flow rate was 1. 0 ml·min-1 ,the detection wavelength was at 254 nm and the injection volume was 20 μl. Results:Within the range of 0. 10-2. 00 mg·ml-1 ,there was a good linear rela-tionship between the concentration and the peak area of lidocaine hydrochloride(r=0. 999 9). The average recovery was 100. 2%( RSD=1. 4%,n=9). Conclusion:The established method is simple,accurate and reproducible,which can be applied to determine the content of lidocaine hydrochloride in buccal adhesive tablets.
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Objective:To establish a determination method for the content and entrapment efficiency of ropivacaine hydrochloride-loaded multivesicular liposomes. Methods: The separation of the multivesicular liposomes from the free drug was achieved by low-speed centrifugation. The concentration of ropivacaine hydrochloride in the supernatant and the multivesicular liposomes was determined by HPLC, and the entrapment efficiency was calculated. Results: The linear range of ropivacaine hydrochloride was 1. 0-80. 0μg· ml-1(r=0. 999 8). The average recovery was 99. 95% and RSD was 0. 72%(n=9). The content and entrapment efficiency of three batches of ropivacaine hydrochloride-loaded multivesicular liposomes was within the range of 99. 1%-100. 3% and 80. 06%-82. 14%, respectively. Conclusion:The method is simple and accurate, and can be used in the determination of content and entrapment efficien-cy of ropivacaine hydrochloride-loaded multivesicular liposomes.
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Objective:To establish an HPLC method to determine 5-amino salicylic acid (5-ASA) and its related substances in the enemas. Methods:The liquid chromatograph was equipped with a Hypersil ODS C18 column (250 mm × 4. 6 mm,5. 0 μm) with gradient elution. The mobile phase A was composed of pH 7. 5 phosphate buffer ( PBS), tetrabutyl ammonium hydroxide solution (TBAH), methanol and water (600∶50∶50∶300), the mobile phase B was composed of pH 7. 5 PBS, TBAH, methanol and water (200∶50∶300∶450). The wavelength was 208nm, the column temperature was 40 ℃ and the injection volume was 20μl. Results:5-ASA and its two degradation products could be completely separated. The concentration of 5-ASA and the corresponding peak area had a good linear relationship within the range of 1-250μg·ml-1(r=0. 999 5). The average recovery was 99. 44%(RSD=0. 94%,n=9). Conclusion:The method is simple, sensitive and reproducible, and can be used in the determination of the content and related substances in the enemas.
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Objective To study the value and effectiveness of surgical management and mapping in supratentorial tumoral complicated with epilepsy and to study the correlations between tumor and the epileptogenic focus.Methods The clinical data of 121 patients with supratentorial cerebral tumor but epilepsy as initial symptom were retrospectively analyzed for the incidence of pre-and postoperative epileptic seizures,including grade Ⅰ glioma in 1 5 cases and grade Ⅱ glioma in 35 cases,grade Ⅲ-Ⅳglioma in 12 cases,menigoma in 32 cases,metastases in 10 cases,cavernous angiomas in 15 cases,and ependymomas in 2 cases.Results Surgery based on CT/MRI,seizure type and EEG changes was conducted.There was no death in operation.The highest incidence was in frontal lobe and the lowest in occipital lobe.Correlations between localization of tumor and the epileptogenic focus:there were 50 cases in the same location,near or beside tumors in 28 cases,far separate apart(＞2 cm)from tumors in 25 cases,no relationship was found in 18 cases.103 patients were followed up for one to nine years.31 patients had a few seizures in the early postoperative period.Epileptic seizures were cured without anti-epilepsy drugs in 83 cases.Conclusion There are some differences between tumors'location and epileptogenic focus in supratentorial tumoral epilepsy.The location and size of epileptogenic zone should be detected before and during operation.The resection of the tumor combined with the resection of the epileptogenic zone"epilepsy surgery"can provide good results.
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OBJECTIVE:To investigate the characteristics of drug release and the factors affecting the in vitro dissolubility of diclofenac potassium double-layer tablets(DPD).METHODS:UV-spectrophotometry and rotating basket method in the pha-rmacopeia of China 2000 edition were used to determine the in vitro dissolubility of DPD and Higuchi equation was adopeted to simulate the in vitro drug release.The main parameters of dissolution were stastistically analysed.RESULTS:Dissolution parameters of DPD were as follows:T0.3=0.10h,Td=3.30h,T0.9=9.19h.Hardness of tablets did not affect the dissolution rate significantly;pH of dissolution media significantly influenced on the rate.Rotation speed had a significant effect on dissolution action only at the beginning of test.CONCLUSION:DPD has good properties of fast and sustained release.Proper media is the key of in vitro drug release test,however,the ultimate results should be based on in vivo trial.
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OBJECTIVE:To prepare temperature sensitive hydrogel which is of strength.METHODS:The hygrogel was prepared using CS,PVA and GP as matrix with concentration of CS(A),weight ratio of CS to PVA(B) and pH value(C) as factors and with initial gelatination temperature,strength and dehydration as indexes.The formula was optimized by orthogonal experiment and verified.RESULTS:The optimal formula was as follows:A 20 mg?mL-1,B 1 :1,C 7.2.The prepared hydrogel was fluid at 4 ℃ or room temperature while gelatinized at 37 ℃ within 10 min with strength of about 1.4 kPa.Gelatination time reduced along with the increase of temperature.The pH value had hardly changed during degradation in vitro within 28 d.CONCLUSION:The CS/PVA/GP hydrogel is simple and practical in preparation technique and is temperature sensitive and of strength.