1.Preparation and Transdermal Absorption in vitro of Piroxicam Nanostructured Lipid Carrier
Yang LI ; Chen CHEN ; Zhiwen FANG
China Pharmacist 2017;20(3):416-420
Objective: To prepare piroxicam nanostructured lipid carrier and investigate its transdermal absorption behavior in vitro. Methods:Piroxicam nanostructured lipid carrier was prepared by a melt-emulsion ultrasonication and low temperature-solidifica-tion method. The physicochemical properties such as appearance, morphology, particle size distribution, PdI and zeta potential of pi-roxicam nanostructured lipid carrier were evaluated. The transdermal absorption in vitro was investigated using Franz diffusion cells. Results:Piroxicam nanostructured lipid carrier was clear and transparent with small spherical shape as seen under a transmission elec-tron microscope. The particle size distribution, PdI and zeta potential was (106. 4 ± 31. 6) nm, (0. 217 ± 0. 07) and ( -31. 6 ± 2. 5) mV, respectively. Piroxicam nanostructured lipid carrier had higher cumulative transdermal amount in 12 h than piroxicam solution. Conclusion:The nanostructured lipid carrier can remarkably improve piroxicam permeation into skin, which provides reference for the new dosage form for the topical use of piroxicam.
2.Bioavailability and pharmacokinetics of two sustained release formulations of mizolastine in healthy volunteers
Zhiwen ZHANG ; Lijun ZHANG ; Jiang WU ; Xianyi SHA ; Xiaoling FANG
Fudan University Journal of Medical Sciences 2007;34(2):216-222
Purpose The aim of this study was to compare the pharmacokinetic(PK) profile and relative bioavailability of two sustained release tablets containing 10 mg mizolastine in healthy, young Chinese volunteers. Methods A single oral dose of mizolastine was given under fasting conditions to volunteers aged from 21 to 24 years in this open-label, randomized, crossover study. A ten-day washout period was applied between each of the two formulations. Plasma samples were obtained before dosing and at predetermined time points after dosing up to 48 hours and were analyzed for plasma concentration with a high-performance-liquid chromatography-UV method. PK parameters representing the extent and the rate of absorption of mizolastine were obtained. An analysis of variance, 90% confidence intervals, and two one-sided tests were employed for statistical analysis of relative difference between the two formulations. Results According to the pharmacokinetic and statistical analysis, parameters were not statistically different between the two formulations except the peak concentration (cmax). The point estimates of the ratios of AUC0→t, AUC0→∞ of mizolastine were (101.26 + 9.82) % and (102.52 + 8.61)% with 90% confidence intervals (CIs) of 95. 5% - 106. 5% and 97. 7% -106.9% respectively, comprised in the stipulated 80% - 125% range; for cmax values, the ratios was 82.17% - 15.32% with the 90% CIs of 71. 7% - 91.1%, fell in the recommended range of 70% -143%. Conclusions The results indicate that there is no statistically significant difference in PK parameters except cmax between the two sustained release tablets of mizolastine. The 90% CIs of AUC0→t,AUC0→∞ and cmax are within the predefined range. Thus, the two sustained release tablets of mizolastine are considered bioequivalent and generally well tolerated.
3.Awareness and protection of ultraviolet irradiation among people in Urumqi area
Shan YANG ; Haoyue YANG ; Fang XIANG ; Ya'nan ZHAO ; Caixia AN ; Zhiwen SUN ; Xiongming PU
Chinese Journal of Medical Aesthetics and Cosmetology 2014;20(5):369-372
Objective To survey the knowledge of the Urumqi population in Xinjiang on the awareness and the protection of ultraviolet (UV) irradiation.Methods Three hundred and twentyfour subjects from Urumqi were investigated with a questionnaire about the basic knowledge of UV,the UV protection methods,the awareness and application of sunscreens,and the channels through which they acquired the knowledge.Results A total of 324 subjects completed the questionnaire.Only 78.0% knew the harmful effects of UV,62.0% of them knew that UV could lead to skin photo-aging,and 54.9% knew that UV irradiation could cause skin cancer.Sunscreens were the main choice for UV protection (58.0%).Regarding sunscreens,38.3% subjects knew the meaning of SPF,and only a small percentage of subjects (17.3%) were aware of the meaning of PA.About 25.3% of subjects applied sunscreens every day,43.2% used sunscreens sometimes,and 18.5% did not use it at all.The main factor of choosing sunscreens was brand popularity and the main information sources to get the knowledge of UV and UV protection were TV advertisements.Conclusions This study shows that the knowledge of UV and UV protection of the Urumqi population is acceptable,but the protections are insufficient,which should be strengthened and guided through dermatologists and multiple media.
4.Effect of Maiqi-Jiangtang pill on the glycolipid level in type 2 diabetic ob/ob mice
Fang FANG ; Xiaoye TIAN ; Na?Wuken SHA ; Xiaoli TANG ; Jinying WU ; Zhiwen QIAO ; Xiaoxue CHEN ; Xiaohong CHEN ; Jianning SUN
International Journal of Traditional Chinese Medicine 2019;41(1):39-43
Objective To investigate the effects of Maiqi-Jiangtang pill on the glycolipid level in type 2 diabetic ob/ob mice.Methods The 8-week old male ob/ob mice were randomly divided into Maiqi-Jiangtang pill high- (8 g/kg), medium- (4 g/kg), low- (2 g/kg) dose groups. All the mice orally adiministered with the drugs once a day for 10 weeks. The same week age normal C57BL/6J control mice and ob/ob model group mice were orally administered with the equal volume solvent. The body weight per week were recorded. The fasting blood-glucose (FBG) was measured by glycemic instrument. The content of TG, TC, HDL-C, LDL-C in serum, and TG and TC content in liver were determined by biochemical method. The liver index was calculated.Results Compared with ob/ob model group, there was no significant change in body weight of mice administered with Maiqi-Jiangtang pill for 10 weeks. Compared with the model group, the low-, medium- dose Maiqi-Jiangtang pill could significantly decrease the FBG (7.43 ± 1.71 mmol/L,7.84 ± 1.09 mmol/L vs.8.95 ± 0.96mmol/L), the high- dose Maiqi-Jiangtang pill could significantly reduce the TG (0.93 ± 0.16 mmol/L vs.1.18 ± 0.26 mmol/L) and LDL-C (2.10 ± 0.51 mmol/L vs.2.56 ± 0.44 mmol/L) content in serum of ob/ob mice (P<0.05), increase the HDL-C/LDL-C ratio (2.40 ± 0.39vs.1.96 ± 0.24) in serum (P<0.01), decrease the liver weight (3.52 ± 0.26 gvs. 3.98 ± 0.35 g) and the liver index (0.063 ± 0.004vs. 0.071 ± 0.006) (P<0.05). Compared with the model group, the low dose Maiqi-Jiangtang pill could also significantly decrease the TG level (0.63 ± 0.25 mmol/gvs. 1.05 ± 0.67 mmol/g) in liver and significantly increase the HDL-C/LDL-C ratio (2.30 ± 0.44vs. 1.96 ± 0.24) in serum (P<0.05).Conclusions The Maiqi-Jiangtang pill can reduce lipid in serum and liver of ob/ob mice while it can decrease the blood glucose, which need to further study its mechanism.
5.Effects of metformin on human oral cancer KB cell proliferation and apoptosis in vitro.
Fang WANG ; Jincheng XU ; Fei XIA ; Zhe LIU ; Surong ZHAO ; Hao LIU ; Zhiwen JIANG
Journal of Southern Medical University 2014;34(2):159-163
OBJECTIVETo investigate the effects of metformin on the proliferation and apoptosis of human oral cancer cell line KB in vitro.
METHODSHuman oral cancer cell line KB was exposed to different doses of metformin (0, 1.25, 2.5, 5, 10, and 20 mmol/L), and the changes in cell viability were detected using MTT assay. Colony formation of the cells was observed following an 8-day metformin exposure. The changes in mitochondrial membrane potential were measured by JC-1 assay, and PI staining was used to observe the cell apoptosis. Western blotting was employed to detect the changes in the protein expressions of GRP78 and activated caspase-3.
RESULTSMetformin exposure caused time- and dose-dependent suppression of KB cell proliferation, and exposure to 5 mmol/L metformin for 24, 48 and 72 h resulted in cell survival rates of 68.0%, 36.9%, and 14.5%, respectively. Metformin significantly inhibited KB cell colony formation. Exposure of the cells to increased concentrations of metformin gradually increased the apoptotic rate and decreased mitochondrial membrane potential. Metformin caused an initial up-regulation followed by a down-regulation of GRP78 expression in KB cells and increased the expression of activated caspase-3.
CONCLUSIONMetformin can inhibit the proliferation and induce apoptosis of KB cells, the mechanism of which may involve the activation of the mitochondrial apoptotic pathway and endoplasmic reticulum stress.
Apoptosis ; drug effects ; Caspase 3 ; metabolism ; Cell Proliferation ; drug effects ; Heat-Shock Proteins ; metabolism ; Humans ; KB Cells ; Membrane Potential, Mitochondrial ; drug effects ; Metformin ; pharmacology
6.Research progress on the reconstruction of mandibular defects in adolescents
BIN Zhiwen ; WANG Fang ; HOU Jinsong
Journal of Prevention and Treatment for Stomatological Diseases 2021;29(10):711-715
Mandibular defects in adolescents are mostly caused by surgical resection of benign and malignant tumors, trauma and jaw inflammation. The reconstruction of mandibular defects in adolescents is challenging. In addition to solving the problem of jaw reconstruction in adults, some clinical factors, including the influence of surgery on the growth of donor and recipient areas, the long-term effects of reconstruction, and the outcome of bone grafts, must also be considered. At present, the main reconstructive methods include autogenous bone grafts and distraction osteogenesis. Autogenous bone grafts are still the gold standard due to their long-term effects. Favorable growth potential after repair was shown in adolescent cases of mandibular reconstruction with fibula flap. Normal occlusion was restored, and a long-term stable effect was achieved in cases of condylar reconstruction with costal cartilage. The safety and clinical effects of distraction osteogenesis have been confirmed, but the long-term effects of large-scale mandibular defects are still uncertain. In addition, other tissue engineering techniques also have good application prospects for the repair and reconstruction of adolescent mandible defects, but more in-depth basic research and more extensive clinical trials should be performed to verify the efficacy.
7.Tubridge flow diverter for the treatment of recurrent internal carotid blood blister-like aneurysms after stent-assisted embolization
Yina WU ; Zhiwen LU ; Guoli DUAN ; Yibin FANG ; Kaijun ZHAO ; Yi XU ; Qinghai HUANG
International Journal of Cerebrovascular Diseases 2021;29(10):750-754
Objective:To investigate the safety and efficacy of Tubridge flow diverter for the treatment of recurrent internal carotid blood blister-like aneurysms after stent-assisted embolization.Methods:From June 2018 to April 2021, patients with recurrent internal carotid blood blister-like aneurysms treated with Tubridge flow diverter in the Department of Neurosurgery, Changhai Hospital, Naval Medical University were enrolled retrospectively. The perioperative safety, immediate postoperative and follow-up results were analyzed.Results:A total of 6 patients with recurrent internal carotid blood blister-like aneurysm after stent-assisted embolization were enrolled. The time interval from the first stent-assisted embolization to Tubridge placement was 14 to 90 d. Tubridge implantation alone was used in 4 patients, and Tubridge was implanted in the other 2 patients after the coils were packed. There were no complications during the perioperative period, and no rebleeding was observed after clinical follow-up for 5 to 36 months. Five patients were followed up by angiography for 1-3 months, and the aneurysms disappeared completely.Conclusion:Tubridge flow diverter for the treatment of recurrent internal carotid blood blister-like aneurysms is safe and effective.
8.Efficacy and safety of endovascular recanalization 6-24 h after onset in patients with acute basilar artery occlusion
Zhiwen HOU ; Zongjie SHI ; Fang LIU ; Sheng ZHANG ; Shunyuan GUO ; Yu GENG
Chinese Journal of Neuromedicine 2020;19(2):113-119
Objective To investigate the efficacy and safety of endovascular recanalization 6-24 h after onset in patients with acute basilar artery occlusion,and explore the related factors for their prognoses.Methods Clinical data of 37 patients with acute basilar artery occlusion,received endovascular recanalization in our hospital from January 2016 to July 2019,were retrospectively collected;23 patients were into group of onset-to-puncture time (OPT)>6 h (6-24 h),and 14 patients were into group of OPT ≤ 6 h (0-6 h).Statistical methods were used to compare the postoperative symptomatic intracranial hemorrhage rate,good prognosis rate (modified Rankin scale [mRS] scores ≤ 3) and mortality 3 months after onset between the two groups;clinical data between the subgroups with good and poor prognoses in patients of group of OPT>6 h were compared.Results The postoperative symptomatic intracranial hemorrhage rate,and good prognosis rate and mortality of patients from group of OPT>6 h were 30.4%,47.8% and 43.5%,respectively;and there were no statistically significant differences as compared with those in patients from group of OPT≤6 h (35.7%,35.7%,and 42.9%,P>0.05).Scores of scales based on preoperative CTA images (posterior circulation-Alberta stroke program early CT scale [pc-ASPECTS],scale of posterior circulation on CTA [pc-CTA],and scale of basilar artery on CTA [BATMAN]) showed significant differences between the good prognosis subgroup and poor prognosis subgroup in patients fiom group of OPT>6 h (P<0.05).Conclusion Endovascular recanalization 6-24 h after onset is effective in patients with acute basilar artery occlusion,and the safety does not obviously decrease;scores of pc-ASPECTS,pc-CTA and BATMAN may be related to the clinical prognoses.
9.Effects of recombinant human epidermal growth factor on epithelial recovery and tear film stability after enhanced transepithelial corneal crosslinking
Zhirong LIN ; Huping WU ; Shunrong LUO ; Zhiwen XIE ; Xie FANG ; Xianwen XIAO ; Lei YAN ; Nuo DONG ; Xumin SHANG ; Zhaosheng LIU
Chinese Journal of Experimental Ophthalmology 2020;38(12):1052-1059
Objective:To investigate the impact of recombinant human epidermal growth factor (rh-EGF) on the epithelial recovery and the tear film stability after trans-epithelial corneal collagen crosslinking in patients with progressive keratoconus.Methods:A randomized controlled clinical trail was designed.Consecutive 66 patients (37 males and 29 females) with an average age of (21.27±3.80) years old diagnosed with primary progressive keratoconus and hospitalized in Xiamen Eye Center Affiliated to Xiamen University from October, 2016 to January, 2017 were enrolled and treated with unilateral enhanced transepithelial corneal crosslinking surgery by iontophoresis, and the patients were randomly divided into control group and experimental group according to random number table method, with 33 patients 33 eyes in each group.The eyes in the control group were treated with carboxy-methylcellulose sodium lubricant eye drops and the eyes in the experimental group were treated with rh-EGF eye drops.The ocular surface disease index (OSDI) questionare, slit lamp examination, Schirmer Ⅰ test, corneal fluorescein sodium staining scoring, non-contact tonometry, uncorrected visual acuity, best corrected visual acuity, bulbar conjunctival congestion scoring, lacrimal sevretion test, non-invasive break-up time of tear film (NIBUT), as well as tear meniscus height analysis were performed before surgery, and on day 1, day 3, day 5, day 7, day 14 and day 28 after surgery.This study followed the Declaration of Helsinki.The study protocol was approved by the Ethics Committee of Xiamen Eye Center Affiliated to Xiamen University (No.2016-ME-003).Results:On day 7 after surgery, the OSDI values were increased in both groups than the preoperative value, while the value in the experimental group was significantly lower than that in the control group ( P<0.05). There were statistically significant differences in the overall corneal epithelial staining score values between the two groups at different time points ( Fgroup=16.701, P<0.01; Ftime=454.418, P<0.01). The corneal epithelial staining score in the experimental group on day 3 and day 5 after surgery were significantly lower than those in the control group (1.79±0.65 vs. 2.70±0.68; 0.91±0.46 vs. 1.55±0.51) (both at P<0.01). The conjunctival congestion score in the experimental group was significantly lower than that of the control group on day 3 and day 5 after surgery (both at P<0.05). There were statistically significant differences in the overall NIBUT values between the two groups at different time points ( Fgroup=13.084, P<0.01; Ftime=34.383, P<0.01). The NIBUT values were significantly decreased rapidly on day 7, day 14 and day 28 after surgery in both groups (all at P<0.01), but gradually recovered.The NIBUT of the experimental group on day 7 and day 14 after surgery were significantly higher than those of the control group ([8.18±2.26]seconds vs. [5.93±2.33]seconds; [9.49±1.95]seconds vs. [7.52±2.27]seconds) (both at P<0.01). No statistical differences were found in the tonometry value, visual acuity, value of Schirmer I test as well as tear meniscus height at any time point before or after surgery between the two groups (all at P>0.05). Conclusions:Recombinant human epidermal growth factor has positive effects in the patients received enhanced transepithelial corneal crosslinking surgery, presenting with promotion of epithelial healing, relief of post-operative discomfort, and the recovery of tear film stability.
10.Quality study of Perillae caulis formula granules based on standard decotion
Jie YANG ; Weisheng LYU ; Fang CHEN ; Liping DENG ; Ruoyun SHI ; Zhiwen DUAN ; Minyou HE ; Mei WEI ; Zhenyu LI
International Journal of Traditional Chinese Medicine 2022;44(10):1144-1149
Objective:To establish the quality evaluation method of Perillae caulis formula granules based on the three kind of quality indexes of standard decoction. Methods:Eighteen batches of Perillae caulis were collected from different habitats according to different technical requirements, eighteen batches of standard decoction and three batches of formula granules were prepared and the paste-forming rates were calculated. The content of Caffeic acid and Rosmarinic acid were determined and calculated by Ultra High Performance Liquid Chromatography (UPLC). Then the fingerprints of standard decoction of and formula granules of Perillae caulis were established by UPLC . The similarity values of fingerprints between formula granules and standard decoction were calculated. Results:The average paste-forming rate of standard decoction was (7.16±1.97)%. The paste-forming rates of three batches of formula granules were 5.52%, 5.25% and 5.34%, respectively. The average content of Caffeic acid and Rosmarinic acid in standard decoction was (12.06±3.37)mg/g. The contents of three batches of formula granules were 5.52, 5.82, 5.77 mg/g, respectively. Seven common fingerprint peaks were identified in the fingerprints of standard decoction and formula granules, three of which were identified as Caffeic acid, N-Feruloyl Octopus amine and Rosmarinic acid by comparison of reference substance. The fingerprints similarity of Perillae caulis dispensing granules and standard decoction were 1.000, 0.995 and 0.997, respectively. Conclusions:The quality indexes of three batches of formulation granules are consistent with standard decoction. This method can provide basis for the establishment of quality standard of Perillae caulis dispensing granules.