2.Preparation of Celecoxib Nanostructured Lipid Carriers and Tissue Distribution in Rats
Qiuyan LI ; Min WANG ; Peng XIE ; Yanrong DAI
China Pharmacist 2016;19(2):277-281
Objective:To prepare celecoxib nanostructured lipid carriers and investigate the characteristics of tissue distribution in rats. Methods:Celecoxib nanostructured lipid carriers were prepared by a melt-emulsion ultrasonication and low temperature-solidifi-cation method. The physicochemical properties of nanostructured lipid carriers were studied, such as particle size distribution, zeta po-tential and morphology. The concentration of celecoxib in different tissues was determined after tail vein injection of celecoxib nano-structured lipid carriers in rats. Results:The obtained celecoxib nanostructured lipid carriers were spherical with the average particle size of (103. 5 ± 32. 6) nm and zeta potential of ( -37. 3 ± 5. 1) mV. The re of celecoxib nanostructured lipid carriers in liver, spleen, brain and muscle respectively was 3. 43, 2. 99, 2. 38 and 2. 93 times higher than that of celecoxib injection. Conclusion:The biodistribution of celecoxib is changed by the nanostructured lipid carriers. Celecoxib nanostructured lipid carriers have the characteris-tics of liver, spleen and muscle targeting, which is benefit to improving the efficacy.
3.Preparation and Pharmacokinetics in Rats of Celecoxib Nanosuspension
Qiuyan LI ; Min WANG ; Peng XIE ; Juntao LI ; Qiang XUE
China Pharmacist 2016;19(2):258-261
Objective:To prepare celecoxib nanosuspension ( CXB-NSs) and study the pharmacokinetics of CXB-NSs in rats. Methods:CXB-NSs were prepared by an anti-solvent precipitation and high pressure homogenization method. The particle size, polydispersion index ( PdI) and zeta potential of the nanosuspension were studied. Totally 12 Wistar rats were randomly divided into CXB-NSs group and CXB suspension group, and gastric drug dose was 100 mg·kg-1 . CXB concentration in plasma was determined by HPLC and the pharmacokinetic parameters were calculated by 3P97 software. Results: The particle size, polydispersion index, zeta potential of CXB-NSs was (442. 5 ± 61. 9) nm, 0. 312 ± 0. 057 and ( -31. 6 ± 3. 9) mV, respectively. AUC (0-t) of CXB suspension and CXB-NSs was (5.13 ±0.77) and (13.51 ±3.18) mg·L-1·h, half time (t1/2) was (12.31 ±1.91) and (12.73 ±1.83) h, Tmax was (2. 48 ± 0. 37) and (1. 41 ± 0. 27) h and Cmax was (0. 94 ± 0. 31) and (2. 38 ± 0. 25) mg·L-1 , respectively. Conclusion:CXB-NSs can remarkably increase bioavailability in rats.
4.Preparation and Characterization of Celecoxib-loaded PLGA Nanoparticles
Min WANG ; Peng XIE ; Yimin YANG ; Qiuyan LI ; Qiang XUE
China Pharmacy 2015;(25):3561-3564
OBJECTIVE:To prepare and characterize celecoxib-loaded PLGA nanoparticles. METHODS:Emulsification-solvent evaporation method was adopted to prepare celecoxib-loaded PLGA nanoparticles. With encapsulation efficiency and particle size as the indexes,Plackett-Burman design was preferred to screen the formulation and variables which had a significant effect on the property of nanoparticles. And then Box-Behnken response surface method was used to further optimize selected variables including mass concentration of PLGA,ultrasonic power and ultrasonic time,followed by verification. Malvern particle size analyzer was used to determine the particle size distribution of nanoparticles and Zeta potential of nanoparticle by the optimal formulation technol-ogy,and transmission electron microscope was used to observe the morphology of the nanoparticles,and their drug release in vitro behavior and stability(25,5 ℃)were also observed. RESULTS:The optimal formulation and technology was as follows as PLGA mass concentration of 30.0%,ultrasonic power of 180 W and ultrasonic time of 8 min. For the prepared nanoparticles,encapsula-tion efficiency and particle size were (85.7 ± 4.1)% and (226.1 ± 36.1) nm (n=3) respectively;particle size distribution was (176.2±41.2)nm,polydispersity index was 0.211±0.021,and Zeta potential was(-37.3±1.6)mV. Under the electron micro-scope,the nanoparticles were homogeneous in particle size and distributed spheroidally,with 24 h accumulative release of 52.4%. They were stable within 3 months at 5℃. CONCLUSIONS:Celecoxib-loaded PLGA nanoparticles have been prepared successfully.
5.Preparation and In Vitro/In Vivo Evaluation of Celecoxib Self-microemulsifying Drug Delivery Systems
Haichun LI ; Min WANG ; Peng XIE ; Jingbo QI ; Hui XIAO
Herald of Medicine 2017;36(5):549-553
Objective To investigate celecoxib self-microemulsifying drug delivery system (CXB-SMEDDS) that was developed to increase the dissolution rate and oral bioavailability of celecoxib.Methods The formulation of CXB-SMEDDS was optimized by pseudo-ternary phase diagrams analysis.The appearance, morphology, particle size distribution and in vitro drug release behavior of CXB-SMEDDS were investigated after diluted by water.The bioavailability of CXB-SMEDDS was determined by oral administration to rats compared with CXB suspension.Results An optimized formulation was selected: Medium chain triglycerides as oil phase, Tween 20 as surfactant, Transcutol HP as cosurfactant.The ratio of oil phase, surfactant and cosurfactant was 2∶9∶9.Upon mixing with water, CXB-SMEDDS formed a clear and transparent microemulsion solution with homogeneous small spherical under transmission electron microscopy.For particle size of CXB-SMEDDS was found to be (57.6±14.2) nm.The in vitro dissolution test indicated a significant improvement in release characteristics of CXB.The AUC of CXB-SMEDDS and CXB suspension were (5.54±0.94) and (3.32±0.59) mg·L-1·h, respectively.The relative bioavailability was 166.9%.Conclusion The SMEDDS can significantly increase celecoxib dissolution in vitro and bioavailability in vivo.
6.Case-control study on the treatmentof the fifth metatarsal base fractures by cardboard compression pad versus short leg plaster.
Ying-peng XU ; Li-min XIE ; Chao XU ; Yue ZHANG ; Yu-bin LI ; Xin QIAO
China Journal of Orthopaedics and Traumatology 2014;27(10):823-828
OBJECTIVETo compare the effect,safety,and advantage of flexible fixation with paperboard and pad versus short leg plaster in treating the fifth metatarsal base fracture,and establish the standard of diagnosis and treatment of the fifth metatarsal base fractures in flexible fixation with paperboard and pad.
METHODSFrom June 2010 to March 2013,59 patients with the fifth metatarsal base fracture were treated with paperboard and pad fixation or short leg plaster. Patients were enrolled and divided into paperboard and pad treatment group (paperboard group) and short leg plaster treatment group (plaster group) randomly according to the random number table. In paperboard group,there were 29 cases including 9 males and 20 females with an average age of (51.79±11.40) years old; the average course of injury was (11.59±6.58) hours. In plaster group, there were 30 cases including 9 males and 21 females with an average age of (52.13+17.34) years old ;the average course of injury was (11.03±7.06) hours. According to whether the fracture line across the articular surface, in paperboard group there were 14 cases of type A,15 of type B; in plaster group,16 of type A, 14 of type B. According to the degree of dislocation,in paperboard group there were 16 cases of degree I ,13 of degree II ; in plaster group,20 were degree I ,10 were degree II. Fracture was restored according to the type in manual. Patients in paperboard group were treated with paperboard and pad, and patients in plaster group were treated with short leg plaster. Fracture was fixed for 4 to 6 weeks according to fracture healing. On the 2nd, 4th,6th, 8th week and 3rd, 6th month after fixation, patients were followed up, and the foot function score was used to evaluate the function of injured foot. X-ray of injured foot was taken on the 2nd, 4th, 6th and 8th week were used to assess fracture healing.
RESULTSAll patients got complete follow-up. The X-ray result showed that all fracture reached at clinical healing on the 8th week after fixation without skin ulcer,nonunion and displacement of fracture. From the 4th to 8th week after fixation, paperboard group had a higher X-ray score than plaster group, but the difference between two groups had no statistically significance. Repeated analysis result showed that there was interact at different time point and between groups,the difference had statistically significance (P<0.01). The foot function score showed that at all time point, paperboard group had a higher score than plaster group, and on the 2nd, 4th, and 6th week, it had statistically significant difference(P<0.01) between two groups. On the 6th months after fixation,the excellent and good rate of paperboard group was 93.10%, higher than that of plaster group, which was 86.67%. But it had no statistically difference(P=0.483) between two groups.
CONCLUSIONUsing paperboard and pad fixation to treat the fifth metatarsal base fracture has the advantage of simplicity operating,reliable fixation, satisfactory effects, easily obtainable material.
Adult ; Aged ; Casts, Surgical ; Female ; Foot Injuries ; physiopathology ; surgery ; Fracture Fixation ; instrumentation ; methods ; Fracture Healing ; Fractures, Bone ; physiopathology ; surgery ; Humans ; Male ; Metatarsal Bones ; injuries ; physiopathology ; surgery ; Middle Aged
8.Evaluating the bony canal structure of the posterior superior alveolar artery using cone-beam computed tomography.
Zhitian DUAN ; Ping YE ; Runfa WU ; Peng BAI ; Rui RUI ; Min HUANG ; Chen XIE
West China Journal of Stomatology 2014;32(6):581-583
OBJECTIVEThis study aims to examine the prevalence and diameter of the bony canal structure of the posterior superior alveolar artery (PSAA), residual alveolar bone height, and distance of its inferior border from the alveolar crest using cone-beam computed tomography (CBCT).
METHODSCBCT images of maxilla in 116 patients were randomly selected from patients who underwent maxillary sinus augmentation procedure and/or posterior teeth implant therapy from April 2011 to September 2012. The lower border of the bony canal to the alveolar crest, diameter of the bony canal, and residual alveolar bone height below the sinus floor to the ridge crest were measured from CBCT scans. Data were presented using descriptive statistics.
RESULTSThe prevalence of the bony canal was 75.14% (133/177). The mean diameter of the bony canal was (0.96 ± 0.29) mm. The residual alveolar bone height was (7.14 ± 3.64) mm. The distance of the bony canal's inferior border from the alveolar crest was (17.92 ± 5.68) mm. No statistically significant differences between the right and left sides were observed (F = 0.295, P > 0.05). The mean diameter of the bony canal was significantly smaller in females than that in males (F = 0.187, P < 0.05). The maxillary alveolar dimension was significantly correlated with the residual alveolar bone height.
CONCLUSIONThe results from this study suggest that CBCT is a valuable tool in evaluating the presence of the bony canal of the PSAAs efore maxillary sinus surgery.
Alveolar Process ; Arteries ; Cone-Beam Computed Tomography ; Humans ; Maxilla ; Maxillary Sinus ; Sinus Floor Augmentation
9.Imaging and pathologic study of intravertebral vacuum phenomenon in vertebral compression fracture
Gang SUN ; Peng JIN ; Min LI ; Xunwei LIU ; Fandong LI ; Zhiyong XIE ; Xuping ZHANG ; Changling LIN
Chinese Journal of Radiology 2010;44(2):165-168
Objective To investigate the features of intravertebral vacuum phenomenon (IVP)in vertebral compression fractures (VCFs). Methods Two hundred and nine patients with VCFs underwent percutaneous vertebroplasty (PVP) and percutaneous kyphoplasty (PKP). The biopsies and the images of X-ray, CT, MRI of VCFs were obtained. The consistency between IVP and osteonecrosis on histology and the positive predictive value (PPV), negative predictive value (NPV), sensitivity, specificity and Youden index of IVP for diagnosing local osteonecrosis in VCFs were analyzed. Fisher exact probability test was used to analyze the coherence between IVP and osteonecrosis. Results Histological examination revealed 146(69.9%) osteoporoses, 10 (4.8%) osteonecroses with osteoporoses, 53 (25.4%) neoplasms. Prior to surgery,10 cases of IVP were found. Plain radiograph showed horizontally oriented lucent cleft in the vertebral body;CT further confirmed the location of gas;T_1-weighted MR image appeared hypointensity,while the signal intensity of T_2-weighted MR image differed, depending on the duration of recumbency. Nine of 10 patients with IVP showed osteonecrosis on histology, while 9 of 10 patients with osteonecrosis contained IVP. The association of osteonecrosis on histology and the IVP was statistically significant(P <0.01). The PPV, NPV, sensitivity, specificity, and Youden index for diagnosing local osteonecrosis was 90% (9/10), 99.5% (198/199), 90.0% (9/10), 99.5% (198/199), and 0.9, respectively. Conclusion The IVP is stongly suggestive of local osteonecrosis in vertebral compression fracture.
10.Enantioseparation of 38 Racemates on Four Chiral Columns in High Performance Liquid Chromatography
Mei ZHANG ; Wenhui XI ; Min ZI ; Ya PENG ; Shengming XIE ; Liming YUAN
Chinese Journal of Analytical Chemistry 2010;38(2):181-186
The enantioseparations of 38 racemates on Chiralcel OD, Chiralpak AD, Chiralpak IA and(S, S)-Whelk-01 were presented by HPLC. Those enantiomers come from the amines, alcohols, ethers, ketones, aromatic derivatives, heterocyclic compounds, amide acids and medicines etc. With the mobile phase of n-hexane)/isopropanol(90∶ 10, V/V), n-hexane/isopropanol/trifluoracetic acid(90∶ 10∶ 0.2, V/V) or n-hexane/isopropanol/triethylamine(90∶ 10∶ 0.2, V/V), over 70% enantioseparations were obtained for OD, AD and IA columns). The order of enantioseparation selectivity for four columns was OD>AD>IA>(S,S)-Whelk-01, and among those columns there was a big chiral discriminating complementarity. This investigation was useful for choosing chiral columns to separate chiral compounds.