Influence of Xiaoshuan enteric-coated capsules + aniracetam therapy on cerebral blood perfusion and nerve function in patients with convalescent cerebral infarction

Objective: To investigate the influence of Xiaoshuan enteric-coated capsules + aniracetam therapy on cerebral blood perfusion and nerve function in patients with convalescent cerebral infarction. Methods: A total of 177 cases of patients with convalescent cerebral infarction were retrospectively reviewed and then divided into the control group (n=109) and the Xiaoshuan enteric-coated capsules group (n=68). Control group received aniracetam therapy on the basis of routine treatment, and Xiaoshuan enteric-coated capsules group received Xiaoshuan enteric-coated capsules + aniracetam therapy on the basis of routine treatment. The differences in ultrasound cerebral blood perfusion parameter levels as well as serum neurotrophy index and nerve injury index contents were compared between the two groups. Results: Before treatment, there was no statistically significant difference in ultrasound cerebral blood perfusion parameter levels as well as serum neurotrophy index and nerve injury index contents between the two groups. After treatment, ultrasound cerebral blood perfusion parameters PSV and TMV levels in Xiaoshuan enteric-coated capsules group were higher than those in control group whereas RI level was lower than that in control group;serum neurotrophy indexes bFGF, BDNF and VEGF contents were higher than those of control group;serum nerve injury indexes GFAP, NSE, UCH-L1 and S100B contents were lower than those of control group. Conclusion: Xiaoshuan enteric-coated capsules + aniracetam therapy can significantly increase cerebral blood perfusion and optimize nerve function in patients with convalescent cerebral infarction.

高效液相色谱法测定泮托拉唑钠肠溶微丸胶囊的含量

目的建立高效液相色谱(HPLC)法测定泮托拉唑钠肠溶微丸胶囊的含量。方法采用HPLC法,色谱柱为Symetry C18柱(4.6mm×150mm,5μm),流动相:0.025mol·L-1磷酸二氢钾缓冲液-乙腈(70:30),柱温35℃,流速1.0mL·min-1,检测波长:288nm。结果所选定的条件下样品峰分离良好,泮托拉唑钠在36～84mg·L-1范围内线性关系良好,线性回归方程为Y=13130C+155709(r=0.9997),精密度、回收率RSD均<3%,平均回收率100.40%,RSD=1.23%。3批泮托拉唑钠肠溶微丸胶囊的标示含量平均值为99.53%。结论该法简便快速,灵敏准确,可用于测定泮托拉唑钠肠溶微丸胶囊的含量。

泮托拉唑钠肠溶微丸胶囊剂的人体生物等效性

目的评价单剂量口服2种泮托拉唑钠制剂后的人体生物等效性。方法20名男性健康受试者随机分成2组,采用自身对照交叉给药的方式,单剂量口服试验制剂和参比制剂各40mg,在设定时间点抽取静脉血,采用HPLC-UV检测方法测定血药浓度。结果试验制剂和参比制剂的t_(max)分别为(2.68±0.54)、(3.43±0.67)h,ρ_(max)为(1 966±781)、(2 265±772)μg·L^(-1),MRT为(4.55±0.98)、(5.22±1.03)h,t_(1/2)为(1.94±0.50)、(1.68±0.37)h,AUC_(0→15h)为(7 787±5 391)、(7 989±4 492)μg·h·L^(-1),AUC_(0→∞)为(7 955±5 634)、(8 143±4 715)μg·h·L^(-1)。结论试验制剂平均相对生物利用度为(94.4±14.1)%,试验制剂与参比制剂生物等效。

萘普生肠溶微丸胶囊的毒理学研究

目的考察萘普生肠溶微丸胶囊对小鼠的急性毒性和对大鼠急性胃部刺激性的影响.方法采用两种不同的给药途径对昆明种小鼠进行急性毒性研究;灌胃给予萘普生肠溶微丸胶囊和萘普生胃溶胶囊对大鼠胃部刺激性进行比较.结果灌胃给药LD50为1329.6(1148.1～1539.6)mg*kg-1,腹腔注射给药LD50为596.3(557.1～638.3)mg*kg-1;萘普生肠溶微丸胶囊和萘普生胃溶胶囊给药剂量为100、200、400mg*kg-1时,致溃疡指数分别为0.2、0.1、0.2和2.6、3.4、3.6,与溶媒对照组比较,萘普生肠溶微丸胶囊对胃部无刺激作用(P＞0.05),萘普生胃溶胶囊对胃部有明显的刺激作用(P＜0.01).结论萘普生肠溶微丸胶囊毒性较低,对胃部无明显刺激作用.

复方利福平微丸胶囊的溶出度与释放度测定

目的采用高效液相色谱法与紫外分光光度法测定复方利福平微丸胶囊溶出度的方法。方法异烟肼与吡嗪酰胺色谱柱AlltechAlltimaCN(5μm,250mm×4.6mm);柱温30℃;流动相0.01mol/L庚烷磺酸钠溶液(用稀磷酸调节pH至2.0)-乙腈(44∶56);流速1.0ml/min;检测波长254nm;检测灵敏度为0.1aufs,进样量10μl。利福平紫外分光光度法,测定波长474nm。结果异烟肼在1～22μg/ml浓度范围内,峰面积与其浓度线性关系良好,r=0.9999,平均回收率为99.3%;吡嗪酰胺在3～58μg/ml浓度范围内,峰面积与其浓度线性关系良好,r=0.9999,平均回收率为99.6%;重复性试验RSD均小于1.5%(n=9)。利福平在2～50μg/ml浓度范围内,吸收度与其浓度线性关系良好,r=0.9996,平均回收率为99.5%。结论本方法快速简便,精密度好,灵敏度高,可作为控制复方利福平微丸胶囊溶出度与释放度的方法。

Effect of Weikang Capsule(胃康胶囊)on Aspirin-Related Gastric and Small Intestinal Mucosal Injury

Objective To investigate the effects of Weikang Capsule(胃康胶囊,WKC)on aspirin-related gastric and small intestinal mucosal injury by magnetically controlled capsule endoscopy(MCCE).Methods Patients taking enteric-coated aspirin aged 40-75 years were enrolled in Beijing Anzhen Hospital,Capital Medical University from January 2019 to December 2019.The patients continued taking aspirin Tablet(100 mg per day)and underwent MCCE before and after 1-month combined treatment with WKC(0.9 g per time orally,3 times per day).The gastrointestinal symptom score,gastric Lanza score,the duodenal,jejunal and ileal mucosal injury scores were used to evaluate the gastrointestinal injury before and after treatment.Adverse events including nausea,vomiting,abdominal pain,abdominal distension,abdominal discomfort,dizziness,or headache during MCCE and combined treatment were observed and recorded.Results Twenty-two patients(male/female,13/9)taking enteric-coated aspirin aged 59.5±11.3 years with a duration of aspirin use of 28.0(1.0,48.0)months were recruited.Compared with pre-treatment,the gastrointestinal symptom rating scale scores,gastric Lanza scores,and duodenal mucosal injury scores were significantly reduced after 1-month WKC treatment(P<0.05),and jejunal and ileal mucosal injury scores showed no obvious change.No adverse events occurred during the trial.Conclusions WKC can alleviate gastrointestinal symptoms,as well as gastric and duodenal mucosal injuries,in patients taking enteric-coated aspirin;it does not aggravate jejunal or ileal mucosal injury,which may be an effective alternative for these patients(Clinical trial registry No.ChiCTR1900025451).

缓控释微丸胶囊仿制药处方工艺研究的审评考虑

缓控释微丸胶囊是常见的缓控释制剂,已逐渐成为缓控释制剂研究开发的热点之一。缓控释微丸胶囊处方工艺研究是否充分,不仅是保证药品质量的基本前提,还是满足临床用药的基础。原辅料控制全面、处方设计合理、生产工艺稳定重现等是处方工艺研究的重点。基于国际人用药品注册技术协调会指导原则和国内外相关文献以及审评中接触到的实际案例,并结合缓控释微丸胶囊制剂特点,围绕缓控释微丸胶囊处方工艺研究关注点,提出处方工艺开发过程中的一般考虑,以期为缓控释微丸制剂的研究和注册申报提供思路和建议。

Oral fibrinogen-depleting agent lumbrokinase for secondary ischemic stroke prevention： results from a multicenter, randomized, parallel- group and controlled clinical trial

Background Elevated fibrinogen （Fg） level is a known risk factor for ischemic stroke. There are few clinical trials on oral fibrinogen-depleting therapies for secondary ischemic stroke prevention. We aimed to assess the effects of one-year therapy with oral lumbrokinase enteric-coated capsules on secondary ischemic stroke prevention.