1.Preparation and releasing evaluation in vivo and in vitro of pH-dependent Yuchangning Tablet for colon-specific delivery
Ming YANG ; Xingliang XIE ; Hongyan MA ; Xuelan QIU ; Runchun XU
Chinese Traditional and Herbal Drugs 1994;0(05):-
Objective To prepare the pH-dependent Yuchangning Tablet for colon-specific delivery(PYTCSD) used in treating the ulcerative colitis and evaluating the releasing property in vivo and in vitro.Methods The coating prescription was screened by the in vitro delivery of matrine and oxymatrine.The in vitro releasing property of the preparation was examined by the method of in vitro delivery. The in vivo releasing property of the preparation was evaluated by the shadowgraph technique of barium sulfate.Results The preparation method of the PYTCSD was obtained.The core of the tablet was coated by the alcohol solution mixed with 3.70%(g/mL) Eudragit Ⅲ,0.37%(g/mL) DEP,and 0.93%(g/mL) talcum power.The weight of the core was increased 8%.From the in vitro delivery,matrine and oxymatrine were not detected in the simulated gastric fluid after 2 h.The quantities of matrine and oxymatrine were less 10% in the simulated intestinal fluid after 4 h.The quantities of matrine and oxymatrine were 86.5% and 86.8% in the simulated colon fluid after 1 h.On the basis of the in vivo delivery by treating eight volunteers,the PYTCSD could completely get to the ileocecum or ascending colon and disintegrate in that part.Conclusion The PYTCSD can be prepared and the preparation is significantly delivered in the specific colon.
2.Association of the rs10489070 polymorphism of SLC2A9 gene with primary gout in Northeast Sichuan of Chinese Han population
Min LI ; Jingguo ZHOU ; Yufeng QING ; Wenguang XIE ; Dan JIANG ; Qibin YANG ; Mingcai ZHAO ; Xingliang JIANG ; Mei ZENG
Chinese Journal of Rheumatology 2012;16(4):233-238
Objective To detect the distribution of SLC2A9 rs10489070 polymorphism genotypes in Chinese Han population,and to explore the association of this gene polymorphism with gout susceptibility,tophi,serum uric acid levels and other clinical and laboratory data.Methods A total of 151 primary gout patients and 176.healthy controls were enrolled into this study.The genotypes and alleles frequencies were calculated by using TaqMan(R) SNP Genotyping Assays and the possible association between gene polymorphism of SLC2A9 and gout was investigated.T test,Chi-square and Fisher exact probabilities were used for statistcal analysis.Results Genotypes distribution were in Hardy-Weinberg equilibrium in gout patients and controls (P>0.05).The frequency of CC genotype in gout patients was significantly higher than that in the controls (78.8% vs 68.5%,P<0.05),aand the frequency of CG genotype in gout patients was significantly lower (19.9% vs 30.1%,P<0.05).However,there were no statistical differences in the alleles frequencies of C and G between gout patients and controls (P>0.05).Interestingly,there was significant difference in the distribution of genotypes between tophaceous gout patients and non-tophaceous gout patients (P<0.05),and the frequency of CG genolype was much lower in tophaceous gout patients (0 vs 22.7%,P<0.05).Conclusion Results of present study suggest that rs10489070 polymorphism of the SLC2A9 gene might be associated with gout development.CC genotype predisposes to gout,and CG genotype might protect Chinese Han population from gout and tophi development.
3.Preparation and evaluation of the formulation of budesonide rectal in situ thermogel
Ting SHEN ; Lin CHEN ; Xingliang XIE ; Zhengshuang ZHANG ; Xiaohong XU ; Quan ZHANG
Journal of China Pharmaceutical University 2018;49(6):689-694
To prepare a budesonide rectal thermogel. The gel solution was prepared by cold method, and the gelation temperature of the gel solution was determined by reverse tube method. The amount of poloxamer 407(P407), poloxamer 188(P188)and hydroxy propyl methyl cellulose(HPMC)was optimized by central composite design/response surface method. The in vivo gelation character was investigated after rectal administration of the budesonide thermogel into the rat, and the in vitro drug release from the gel was examined by the Franz diffusion cell method. Finally, the optimal formulation includes 0. 002% budesonide, 0. 93% HPMC, 2. 00% P188, and 18. 31% P407. It is preferable to obtain the appropriate formulation for budesonide rectal in situ thermogel, which can achieve wide distribution and adhesion to the rectum, as well as long-term drug release.
4.Optimization of the Best Proportion of Astragalus membranaceus Injection Combined with Erigeron breviscapus Injection against Cerebral Ischemia-reperfusion Injury in Rats by Baseline Geometric Proportion Increasing and Decreasing Design
Feng TIAN ; Jicao LI ; Shaowei TANG ; Yushi SUN ; Shijia LIN ; Fangyan ZHANG ; Xingliang XIE ; Yanmei SHENG
China Pharmacy 2019;30(14):1885-1889
OBJECTIVE: To screen the best proportion of Astragalus membranaceus injection combined with Erigeron breviscapus injection against cerebral ischemia-reperfusion injury in rats. METHODS: Male SD rats were randomly divided into sham operation group, model group and administration group [different A. membranaceus injection-E. breviscapus injection proportion groups, being A(0 ∶ 10), B(2 ∶ 8), C(4 ∶ 6), D(6 ∶ 4), E(8 ∶ 2), F(10 ∶ 0)groups, set by baseline geometric proportion increasing and decreasing design], with 8 rats in each group. Except for sham operation group, reperfusion injury model of middle cerebral artery occlusion were induced by modified suture method in rats. The each administration group was given relevant medicine intraperitoneally once immediately after inducing model, and then given again after 24 hours (medication interval between the two injections of 30 min). Constant volume of normal saline was given to rats in sham operation group and model group. Forty-eight hours after reperfusion, Longa scoring method was used to evaluate neurological impairment of rats, and neurological impairment score was recorded. Serum content of MDA and activity of SOD were measured by colorimetry assay. TTC assay was used to detect cerebral infraction, and cerebral infarction rate was calculated. Kim’s formula was used to calculate the synergistic index (q) of rats in administration groups. RESULTS: Compared with sham operation group, neurological impairment score and serum content of MDA were increased significantly in model group, while activity of SOD was decreased significantly (P<0.01). The area of cerebral infarction increased significantly, and the rate of cerebral infarction increased significantly (P<0.01). Compared with model group, neurological impairment scores and serum contents of MDA were decreased significantly in group A, B, C, D and E; neurological impairment score of group C was significantly lower than those of group A and F; serum contents of MDA in group B, C, D and E were significantly lower than that of group F (P<0.05 or P<0.01). Activities of SOD in group A, B, C, D and E were increased significantly, and group C was significantly higher than group F (P<0.05 or P<0.01). The cerebral infarction area of rats in each administration group was reduced to varying degrees. The cerebral infarction rates of rats in group B, C, D and E were significantly reduced, and group C and D were significantly lower than group F, while group C was significantly lower than group A (P<0.05 or P<0.01). The q values of group B, C, D and E were 0.90, 1.30, 1.00, 0.70 (neurological impairment score) and 0.79, 1.27, 0.98, 0.82 (cerebral infarction rate). CONCLUSIONS: Different ratios of A. membranaceus injection and E. breviscapus injection have certain protective effects on cerebral ischemia-reperfusion injury model rats, can relieve their neurological deficits, alleviate their oxidative stress and reduce their cerebral infarction areas. The effect of the combination of the two drugs is better than that of single use, and the optimum ratio is 4 ∶ 6.