Clinical Effect of Ilaprazole Enteric-Coated Tablets in Patients with Peptic Ulcer

Objective: To discuss the actual effect of ilaprazole enteric-coated tablets in the treatment of peptic ulcer patients. Methods: 200 peptic ulcer patients who received treatment from January to December 2023 were selected as the study sample, and all patients were randomly and evenly divided into the study group (n = 100) and the control group (n = 100), and the serum inflammatory factors and the disappearance time of symptoms were compared. Results: After treatment, the serum inflammatory factors in the observation group were better than those in the control group, and the time of belching and burning sensation in the observation group was shorter than that in the control group, all of which were statistically significant (P Conclusion: Ilaprazole enteric-coated tablets in the treatment of peptic ulcer have a good effect and can effectively improve the symptoms of patients with clinical signs, with reference significance.

Analysis of the Therapeutic Effect of Clopidogrel Bisulfate Tablets + Aspirin Enteric-Coated Tablets on Acute Myocardial Infarction

Objective:To investigate and analyze the clinical effect of clopidogrel bisulfate tablets combined with aspirin enteric-coated tablets on acute myocardial infarction(AMI)patients.Methods:The study period was from January 2020 to December 2023,the sample source was 82 AMI patients admitted to our hospital,grouped into an observation group(n=41)and a control group(n=41)by the numerical table method.The patients in the control group were treated with aspirin enteric-coated tablets,and the patients in the observation group were treated with aspirin enteric-coated tablets combined with clopidogrel bisulfate.The clinical efficacy,coagulation indexes,and the incidence of cardiovascular adverse events between the two groups were compared.Results:The clinical efficacy of the observation group was higher than that of the control group(P<0.05);the platelet aggregation rate(PAR)of the observation group was lower than that of the con-trol group after treatment(P<0.05),and there was no significant difference in the prothrombin time(PT)and activated partial thromboplastin time(APTT)between the two groups(P>0.05).The incidence of cardiovascular adverse events in the observation group was lower than that of the control group(P<0.05).Conclusion:The treatment effect of clopidogrel bisulfate tablets combined with aspirin enteric-coated tablets on AMI patients is remarkable.It reduces the PAR and the incidence of cardiovascular adverse events,so this treatment method should be popularized.

Gradient high performance liquid chromatography method for simultaneous determination of ilaprazole and its related impurities in commercial tablets

A methodology(HPLC)proposed in this paper for simultaneously quantitative determination of ilaprazole and its related impurities in commercial tablets was developed and validated.The chromatographic separation was carried out by gradient elution using an Agilent C8 column(4.6 mm×250 mm,5 mm)which was maintained at 25℃.The mobile phase composed of solvent A(methanol)and solvent B(solution consisting 0.02 mmol/l monopotassium phosphate and 0.025 mmol/l sodium hydroxide)was at a flow rate of 1.0 ml/min.The samples were detected and quantified at 237 nm using an ultraviolet absorbance detector.Calibration curves of all analytes from 0.5 to 3.5 mg/ml were good linearity(r≥0.9990)and recovery was greater than 99.5% for each analyte.The lower limit of detection(LLOD)and quantification(LOQ)of this analytical method were 10 ng/ml and 25 ng/ml for all impurities,respectively.The stress studies indicated that the degradation products could not interfere with the detection of ilaprazole and its related impurities and the assay can thus be considered stability-indicating.The method precisions were in the range of 0.41-1.21 while the instrument precisions were in the range of 0.38-0.95 in terms of peak area RSD% for all impurities,respectively.This method is considered stabilityindicating and is applicable for accurate and simultaneous measuring of the ilaprazole and its related impurities in commercial enteric-coated tablets.

Delayed-release oral mesalamine tablet mimicking a small jejunal gastrointestinal stromal tumor:A case report

BACKGROUND Enteric-coated medications are supposed to pass intact through the gastric environment and to release the drug content into the small intestine or the colon.Before dissolution of the enteric coating,they may appear hyperdense on computed tomography(CT).Unfortunately,few reports have been published on this topic so far.In this case report,the hyperdense appearance on contrastenhanced CT of an enteric-coated mesalamine tablet was initially misinterpreted as a jejunal gastrointestinal stromal tumor(GIST).CASE SUMMARY An asymptomatic 81-year-old male patient,who had undergone laparoscopic right nephrectomy four years earlier for stage 1 renal carcinoma,was diagnosed with a jejunal GIST at the 4-year follow-up thoraco-abdominal CT scan.He was referred to our hub hospital for gastroenterological evaluation,and subsequently underwent 18-fluorodeoxyglucose positron emission tomography,abdominal magnetic resonance imaging,and video capsule endoscopy.None of these examinations detected any lesion of the small intestine.After reviewing all the CT images in a multidisciplinary setting,the panel estimated that the hyperdense jejunal image was consistent with a tablet rather than a GIST.The tablet was an 800 mg delayed-release enteric-coated oral mesalamine tablet(Asacol®),which had been prescribed for non-specific colitis,while not informing the hospital physicians.CONCLUSION Delayed-release oral mesalamine(Asacol®),like other enteric-coated medications,can appear as a hyperdense image on a CT scan,mimicking a small intestinal GIST.Therefore,adetailed knowledge of the patients’medications and a multidisciplinary review of the images areessential.

酮洛芬分散片的研制及质量控制

目的 :利用普通制剂技术制成方便服用、快速起效的酮洛芬分散片。方法 :采用正交试验选择出cCMC Na为崩解剂 ,崩解剂内加和外加相结合的方法制成酮洛芬分散片 ,并对其热、湿、光等稳定性进行了考察。结果 :酮洛芬分散片工艺简单、稳定性良好 ,在 1min之内全部崩解 ,形成混悬液 ,符合分散片的各项质量指标。结论 :本品可作为医院制剂开发应用。

酮洛芬缓释片人体药动学和生物等效性研究

目的:评价受试酮洛芬缓释片与参比酮洛芬片的生物等效性。方法:采用反相高效液相色谱法测定24名健康男性志愿受试者交叉单剂量口服受试酮洛芬缓释片与参比酮洛芬片150mg后血浆中酮洛芬的浓度,用3p97程序进行数据处理。结果:口服受试和参比酮洛芬制荆后的AUC_(0-(?))分别是38.94±9.15μg·h·ml^(-1)、38.04±6.90μg·h·ml^(-1);AUC_(0-(?))分别是44.50±8.09μg·h·ml^(-1)、42.99±8.36μg·h·ml^(-1);T_(max)分别是3.87±0.55 h、1.96±0.60h;C_(max)分别是5.78±1.11μg·ml^(-1)、11.62±2.10μg·ml^(-1);t_(1/2)(Ke)分别是5.88±1.16h、1.70±1.40h。结论:受试酮洛芬缓释片与参比酮洛芬片具有生物等效性。

酮洛芬肠溶口腔崩解片的处方优化

目的优化酮洛芬肠溶口腔崩解片的处方,考察不同压片力和不同微晶纤维素与甘露醇比例对空白崩解片孔隙率、抗张强度和崩解时限的影响。方法采用乳化溶剂扩散法制备酮洛芬肠溶微球;以微球为原料,采用粉末直接压片法制备口腔崩解片。用Statistica统计软件对处方组成进行优化,确定微晶纤维素与甘露醇的比例。结果微晶纤维素用量一定时,随压片力的增大,空白崩解片的孔隙率减小,抗张强度增大,崩解时限延长;压片力一定时,随微晶纤维素用量的增加,空白崩解片的孔隙率和抗张强度增大,崩解时限延长;根据处方优化的结果,选择微晶纤维素与甘露醇质量比为3∶1。当片剂中加入质量分数为8%的PVPP作为崩解剂时,空白崩解片的抗张强度略微增加,崩解时限显著缩短。结论根据优化后的处方,采用粉末直接压片法制备的酮洛芬肠溶口腔崩解片符合设计要求。

酮洛芬羟丙基-β-环糊精分散片的处方研究和溶出度考察

目的:制备酮洛芬羟丙基-β-环糊精包合物(KP-HP-β-CD)分散片并考察体外溶出度。方法:以崩解时间为指标,采用正交设计方法对处方进行筛选和优化,转篮法考察分散片的体外溶出度。结果:分散片优化处方的崩解剂为羧甲基淀粉钠(CMS-Na),用量12%,表面活性剂十二烷基硫酸钠(SLS)用量1%,分散片崩解时间为(112.7±5.0)s。体外溶出参数分别为:T50=3.0 min,Td=5.4 min。结论:该分散片符合中华人民共和国药典2005年版的规定,溶出速度明显快于普通片。

酮基布洛芬单室型渗透泵片制备工艺的探讨

目的：探讨酮基布洛芬单室渗透泵型控释片的制工艺。方法：以酮基布洛芬24h内的累积释放度为考察指标，利用正交设计法考察氯化钠与羧甲基纤维素钠的用量以及PEG6000的浓度对酮基布洛芬单室渗透泵型渗透泵片累积释放度的影响。结果：找到原料药与两种辅料的最佳配比。确定制剂的制备工艺。24h内的累积释放度为93．51％，在2～20h内，以累积释放度对时间回归，得到的线性方程中相关系数为0．9988。结论：采用适当的制备方法和包衣工艺，可制得酮基布洛芬单室渗透泵型控释片。

酮洛芬渗透泵型控释片的体外释放与犬体内吸收的相关性

制备了酮洛芬渗透泵型控释片,并进行了体外释放度和犬体内药动学试验。体内试验采用单剂量交叉给药设计,给予家犬相同剂量的渗透泵片和参比制剂后测定血药浓度,以Wagner-Nelson法计算体内吸收分数。结果表明,本品的体外累积释放率与犬体内的吸收分数相关性较好(r=0.9884)。

酮洛芬骨架缓释片相对生物利用度研究

采用高效液相色谱法,以布洛芬为内标,对24 h酮洛芬骨架缓释片试验制剂以24名健康志愿者进行多剂量人体相对生物利用度试验.结果表明,试验制剂具有明显的缓释药动学特征,参比制剂的Cmax显著高于试验制剂(p<0.01),试验制剂给药后的tmax延迟,且吸收程度与作为标准参比制剂的市售缓释片相比无显著差异,人体相对生物利用度为103.76%.经统计学检验表明这两种制剂具有生物等效性,试验制剂具有峰谷浓度差异小、波动幅度小的特点,显示出缓释特征.

酮基布洛芬单室渗透泵片在家犬体内的药动学和相对生物利用度

目的:研究家犬口服酮基布洛芬单室渗透泵片的药动学和相对生物利用度。方法:家犬6只采用双周期交叉给药,用高效液相色谱法测定酮基布洛芬的血药浓度,用3P97处理药动学参数进而计算相对生物学利用度。结果:酮基布洛芬单室渗透泵片和市售普通片在家犬体内过程均符合单室模型,其主要的药动学参数Tmax,Cmax和AUC0-t分别是(2.51±0.67),(1.44±0.26)h;(7.12±1.27),(6.01±1.65)mg.L-1;(66.15±2.32),(59.28±3.69)μg.h.mL-1。结论:酮基布洛芬单室渗透泵片具有明显的缓释特征,生物利用度与市售普通片等效。

酮洛芬缓释片的制备及其体外释放度考察

目的:优化筛选酮洛芬缓释片的处方。方法:以体外释放度为指标,采用正交设计法优化酮洛芬缓释片的处方,并考察酮洛芬缓释片体外的释放机制。结果:最佳处方为:酮洛芬110 g,羟丙甲纤维素(HPMC)20 g,乳糖30 g,乙基纤维素(EC)40 g。酮洛芬缓释片体外释放行为符合Higuchi方程。结论:酮洛芬缓释片处方合理,工艺简单,缓释效果较好。

缓释酮基布洛芬片剂的初步研究

本文报道了选自常用的片剂辅料和国产聚合物为缓释基质,用正交试验设计法设计处方组成并用体外溶出法筛选出具有缓释效果的酮基布洛芬缓释片。该片于人工肠液中在30min,1,2,4,6和8 h的累积释放率分别为16.6％,26.7％,42.2％,63.6％,83.1％和93.4％。6名健康男性受试者口服单剂量该缓释片(100mg)后的血药浓度测定结果表明,本品在体内有缓释效果,维持有效浓度时间达12h以上,体外释放与体内吸收有较好的相关性(r=0.9689)。本文还初步考察了制片压力对酮基布洛芬释放的影响。

酮洛芬薄膜包衣脉冲控释片的制备

目的研制夜间服药、凌晨释放的酮洛芬脉冲控释片。方法采用湿法制粒压片法制备片芯,滚转包衣锅法包控释衣膜。通过对片芯、衣膜处方中崩解剂、填充剂、致孔剂、增塑剂、包衣增重进行单因素考察,并采用星点设计效应面法对处方进行优化。结果单因素考查表明崩解剂、致孔剂、包衣增重对释药时滞有明显影响,采用星点设计效应面法得到的最优处方为:片芯处方KPF 50 mg(25%),MCC 40 mg(20%),乳糖70 mg(35%),L-HPC 40 mg(20%);包衣液处方为Eudragit L100与EC比例是65∶35,PEG6000 15%,包衣增重9.0%。其体外释放时滞为3.75 h,释药时间为0.5 h。结论酮洛芬薄膜包衣片能实现脉冲释药,达到定时速释的要求。

通痹胶囊联合酮洛芬治疗类风湿性关节炎的临床研究

目的探讨通痹胶囊联合酮洛芬治疗类风湿性关节炎的临床疗效。方法选取2019年10月—2022年7月东营市东营区人民医院收治的128例类风湿性关节炎患者,按随机数字表法将所有患者分为对照组和治疗组,每组各64例。对照组口服酮洛芬肠溶片,50 mg/次,3次/d,饭后整片吞服。治疗组在对照组基础上口服通痹胶囊,1粒/次,3次/d,饭后口服。两组治疗疗程均为12周。观察两组的临床疗效,比较治疗前后两组主要临床表现、中医症状积分、28个关节疾病活动度(DAS28)-C反应蛋白(CRP)、关节炎生活质量量表2-短卷(AIMS2-SF)总分以及血浆D-二聚体(D-D)、纤维蛋白原(FIB)水平和血清CRP、Nod样受体蛋白3(NLRP3)、白细胞介素(IL)-1β、基质金属蛋白酶-3(MMP-3)水平。并统计两组不良反应情况。结果治疗后,治疗组总有效率是93.75%,较对照组的81.25%显著提高(P<0.05)。治疗后,两组关节压痛数、肿胀数、关节疼痛VAS评分均显著降低,晨僵时间显著缩短(P<0.05);治疗后,治疗组主要临床表现改善优于对照组(P<0.05)。治疗后,两组中医症状积分、DAS28-CRP均显著下降,而AIMS2-SF总分均显著升高(P<0.05);以治疗组改善更显著(P<0.05)。治疗后,两组血浆D-D、FIB水平均显著下降(P<0.05);治疗后治疗组D-D、FIB显著低于对照组(P<0.05)。治疗后,两组血清CRP、NLRP3、IL-1β、MMP-3水平均显著下降(P<0.05);且治疗后,治疗组血清CRP、NLRP3、IL-1β、MMP-3水平均显著低于对照组(P<0.05)。治疗组和对照组不良反应发生率分别是6.25%、4.69%,两组不良反应发生率比较差异无统计学意义。结论通痹胶囊联合酮洛芬治疗类风湿性关节炎有确切疗效,在改善患者主要临床表现、降低疾病活动度以及提高生活质量方面的效果满意,并可进一步纠正机体凝血功能障碍、减轻炎症损伤,且具有较好的安全性。

酮洛芬微丸缓释片的制备及体外释放度考察

目的:制备一种酮洛芬缓释片剂。方法:采用挤出-滚圆法制备酮洛芬微丸,用Eudragit?RS 30D和Eudragit?RL30D包衣。再将包衣微丸与酮洛芬原药压片,最终制成酮洛芬缓释片。结果:体外释放度实验显示,制备的酮洛芬缓释片在2h内能释药30%,剩余70%药物在随后的10 h内缓慢释放。结论:用本方法制备酮洛芬缓释片,工艺简便,易于操作。

酮洛芬脉冲控释片在家犬体内的药动学及生物利用度研究

目的:考察酮洛芬脉冲控释片在家犬体内的药动学及生物利用度。方法:将6只犬随机均分为2组,分别口服受试制剂酮洛芬脉冲控释片和参比制剂酮洛芬肠溶胶囊150mg,1周后2组交叉试验。给药后不同时间点取样,采用高效液相色谱法测定血样中酮洛芬浓度并计算药动学参数及比较体内、外相关性。结果:受试制剂与参比制剂的tmax分别为(5.00±0.41)、(3.75±0.00)h;Cmax分别为(15.40±1.94)、(20.73±1.72)μg·mL-1,AUC0～t分别为(101.33±17.49)、(93.21±25.03)μg.h.mL-1,受试制剂相对生物利用度为108.71%,体外释药与体内吸收数据r=0.987,具有较好的相关性。结论:酮洛芬脉冲控释片与酮洛芬肠溶胶囊具有生物等效性。

鹿川活络胶囊联合酮洛芬治疗膝骨关节炎的临床研究

目的探讨鹿川活络胶囊联合酮洛芬缓释片治疗膝骨关节炎的临床疗效。方法回顾性分析2020年2月—2021年2月在天津市宝坻区人民医院治疗的106例膝骨关节炎患者临床资料,根据用药差别分为对照组和治疗组,每组各53例。对照组患者口服酮洛芬缓释片,75 mg/次,2次/d;治疗组患者在对照组基础上口服鹿川活络胶囊,1.35 g/次,3次/d。两组均经4周治疗进行效果比较。观察两组的临床疗效,比较两组治疗前后相关评分、血清学指标、超声指标的变化情况。结果经治疗,治疗组患者总有效率是98.11%,显著高于对照组的81.13%(P<0.05)。经治疗,两组患者Lysholms评分显著升高,但VAS评分、WOMAC评分、ISOA评分及临床症状评分均显著降低(P<0.05),治疗后,治疗组相关评分改善优于对照组(P<0.05)。经治疗,两组患者髌上囊积液深度、腘窝囊肿范围、滑膜厚度均显著降低,但股骨内外侧髁软骨厚度均显著增加(P<0.05);治疗后,治疗组软骨病变情况及滑膜组织改善优于对照组(P<0.05)。经治疗,两组血清金属蛋白酶组织抑制因子1(TIMP-1)显著升高,但白细胞介素-1β(IL-1β)、血管内皮生长因子(VEGF)、基质金属蛋白酶-9(MMP-9)、白细胞介素-6(IL-6)均显著降低(P<0.05);且治疗后,治疗组炎症介质水平改善优于对照组(P<0.05)。结论鹿川活络胶囊联合酮洛芬缓释片治疗膝骨关节炎具有较好的临床疗效,可有效改善患者症状和关节功能,降低炎症介质水平和滑膜组织损伤,有着良好的临床应用价值。

酮基布洛芬分散片的制备及其体外溶出评价

目的:制备酮基布洛芬分散片,并考察其体外溶出度。方法:以微晶纤维素(MCC)为填充剂,采用湿法制粒法制备分散片;以MCC、羧甲基淀粉钠(CMS-Na)的处方用量及羟丙基甲基纤维素(HPMC)的浓度为因素,并采用正交试验设计优化处方;采用中国药典溶出度法第二法,以磷酸盐缓冲液为介质进行体外溶出度考察。结果:最佳处方为MCC30%、CMSNa3%、HPMC1%;所制片剂呈白色、片面光洁,崩解时限20s,含量、分散均匀性均符合中国药典2010年版相关要求,30min溶出度大于90%。结论:该分散片制备方法简单,分散均匀,溶出速度快且完全。