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.

Tablets of paliperidone using compression-coated technology for controlled ascending release

The aim of this work was to prepare ascending release compression-coated(CC) tablets with paliperidone(PAL) using a simple manufacturing technique and short manufacturing process.The release behavior and mechanisms in vitro of the final tablets was investigated and evaluated. The PAL CC tablets were comprised of a core layer of high viscosity hydroxypropyl cellulose(HPC-H) and a coating layer of high viscosity hydroxypropyl methylcellulose(HPMCK100 M). Several factors such as materials and core tablet compositions were studied for their influence in the formulation procedure. The drug release mechanism was studied using gravimetric analysis. The data could be fitted to the Peppas model. The ascending drug release results were expressed in terms of the slope of the release curve at different time points.Results showed that the formulation could achieve a good ascending drug release when the weight ratio of PAL was 5:1(core:layer). The fraction of HPC and HPMC was 33 %, and the combination of Eudragit RL-PO was 10%. The ascending release mechanism was due to solvent penetration into the PAL CC tablets, and subsequent drug dissolution from the gelatinous HPC and HPMC matrix erosion. The release mechanism was therefore a combination of diffusion and erosion. This work demonstrated that the compression-coated tablets could achieve controlled ascending release over 24 h for the oral administration systems.

Potential of RP-UHPLC-DAD-MS for the qualitative and quantitative analysis of sofosbuvir in film coated tablets and profiling degradants

Sofosbuvir is one of the new direct-acting antiviral drugs against hepatitis C virus(HCV) infection. This drug has recently been launched into the market, and generic versions of the medication are expected to be produced by local drug producers in some countries. Therefore, new methods are required to control sofosbuvir in pharmaceuticals. In the present study, a new method based on reversed phase(RP)-ultra-high performance liquid chromatography(UHPLC) coupled to diode array detection(DAD) and mass spectrometry(MS) was developed to facilitate the qualitative and quantitative analysis of sofosbuvir in film coated tablets. A wavelength of 260 nm was selected to perform a cost-effective quantification and the method showed adequate linearity,with an R^2 value of 0.9998, and acceptable values of accuracy(75%–102%) and precision(residual standard deviation < 5%). The detection and quantification limits were 0.07 μg/mL and 0.36 μg/mL, respectively.Furthermore, the use of high-resolution MS enabled us to ensure the specificity, check impurities and better sensitivity. Therefore, this methodology promises to be suitable not only for the routine analysis of sofosbuvir in pharmaceutical dosage forms, but also for potential degradants.

Film coated floating tablets using sublimable substances

During the past few decades floating drug delivery systems(FDDSs)have been developed to prolong gastric retention time and obtain sufficient drug bioavailability[1].To avoid unpredictable time to float due to variable pH of the gastric fluid in each subject and food in the stomach[2],sublimation technique is the new interesting approach to prepare noneffervescent FDDSs[3].The objective of the present study was to develop the low-density film coated floating tablets using sublimable substances.

Formulation Development of Generic Omeprazole 20 mg Enteric Coated Tablets

Omeprazole is a potent proton pump inhibitor with powerful inhibition of secretion of gastric juice. Oral site-specific drug delivery systems have recently attracted a great interest for the local treatment of bowel disease and for improving systemic absorption of drugs which are unstable in the stomach. However, microenvironment in the gastrointestinal tract and varying absorption mechanisms cause hindrance for the formulation and optimization of oral drug delivery. The objective of the study was to develop and optimize enteric coating process for omeprazole tablets. Different batches of core tablets were sub coated, one set sub coated with opadry and another with a mixture of light magnesium oxide, magnesium stearate and absolute alcohol omeprazole magnesium. Seal coating was applied by using opadry to achieve certain weight gain and to protect omeprazole from acidic coating polymers. A comparative dissolution test was performed. The variation of thickness and diameter were observed to be minimal with a weight gain of 3% - 4% of enteric polymer. Disintegration test showed that in each tested batch the enteric coated layer remained intact in 0.1N HCl for 2 hours and when exposed to alkaline media of phosphate buffer pH 6.8, it dissolved within few minutes. Dissolution release was 98.8% to 102.4% within two hours when the product was exposed to phosphate buffer pH 6.8 after 2 hours. The similarity and dis-similarity factors were calculated and observed to be 54 to 61 and 4 to 5 respectively. Therefore a simple and good enteric coating process was developed and tested with potential for transfer this technology into local pharmaceutical industries using cheap and easily available materials.

Sample Size Determination and Statistical Hypothesis Testing for Core Centration in Press Coated Tablets

A novel statistical approach to evaluate the manufacturing quality of press coated tablets in terms of the centering of their core is presented. We also provide a formula to determine the necessary sample size. This approach is applied to real data.

Study the effect of formulation variables in the development of timed-release press-coated tablets by Taguchi design

In this investigation, the effect of formulation variables on the release properties of timed- release press-coated tablets was studied using the Taguchi method of experimental design. Formulations were prepared based on Taguchi orthogonal array design with different types of hydrophilic polymers (X1), varying hydrophilic polymer/ethyl cellulose ratio (X2), and addition of magnesium stearate (X3) as independent variables. The design was quantitatively evalu-ated by best fit mathematical model. The results from the statistical analysis revealed that factor X1, X3 and interaction factors between X1X2 and X1X3 were found to be significant on the re-sponse lag time (Y1), where as only factor X1 was found to be significant on the response percent drug release at 8 hrs (Y2). A numerical optimization technique by desirability function was used to optimize the response variables, each having a different target. Based on the re-sults of optimization study, HPC was identified as the most suitable hydrophilic polymer and incorporation of hydrophobic agent magnesium stearate, could significantly improve the lag time of the timed-release press-coated tablet.

Determination of drug,excipients and coating distribution in pharmaceutical tablets using NIR-CI

The growing interest of the pharmaceutical industry in Near Infrared-Chemical Imaging (NIR-CI) is a result of its high usefulness for quality control analyses of drugs throughout their production process (particularly of its non-destructive nature and expeditious data acquisition).In this work,the concentration and distribution of the major and minor components of pharmaceutical tablets are determined and the spatial distribution from the internal and external sides has been obtained.In addition,the same NIR-CI allowed the coating thickness and its surface distribution to be quantified.Images were processed to extract the target data and calibration models constructed using the Partial Least Squares (PLS) algorithms.The concentrations of Active Pharmaceutical Ingredient (API) and excipients obtained for uncoated cores were essentially identical to the nominal values of the pharmaceutical formulation.But the predictive ability of the calibration models applied to the coated tablets decreased as the coating thickness increased.

Formulation Development, in Vitro Evaluation and Stability Study of Aceclofenac Tablet

The objective of the study was to develop film coated tablets of aceclofenac using wet granulation technique. Possible drug-excipient interaction was evaluated by HPLC （high performance liquid chromatography） and FTIR （fourier infrared spectroscopy）. The tablets prepared were assessed for their physicochemical, in vitro dissolution at pH 1.2, 4.5, 6.8 and 7.5 and stability characteristics. Comparison with a commercial aceclofenac product was made in vitro and in vitro studies. There was no interaction between aceclofenac and used excipients. Furthermore, the physicochemical properties of the tablets were satisfactory. The dissolution profile of one of the formulated aceclofenac tablets （D07） was statistically similar （p 〈 0.05） to that of the commercial aceclofenac brand in all the dissolution media. The formulated products ware stable and showed no changes in physical appearance, drug content, or dissolution pattern after storage at 40 ℃/75% RH for 6 months. The results indicate that it is feasible to achieve a stable aceclofenac tablet formulation by using wet granulation technique.

脉血康胶囊(肠溶片)治疗心脑血管疾病临床应用专家共识

脉血康胶囊(肠溶片)治疗心脑血管疾病具有良好的临床疗效及安全性。在临床医生问卷调查和脉血康胶囊(肠溶片)研究文献系统回顾的基础上,采用国际临床医学专家共识研制方法,基于现有最佳证据,充分结合专家经验,遵循“循证为主,共识为辅,经验为鉴”的原则,国内26位中西医临床、药学、方法学等多学科专家共同研制该共识,旨在进一步提高临床医生对该药的认识,更好地指导其临床合理用药。共识采用国际公认的证据分级推荐标准即评估、发展和评价建议的分级(Grading of Recommendations Assessment,Development and Evaluation,GRADE分级),如果证据充分则形成“推荐意见”,采用GRADE网格计票规则;如果证据不充分,则形成“共识建议”,采用多数计票规则。共识对脉血康胶囊(肠溶片)用于心脑血管疾病的适应证、用法用量、疗程、禁忌证、合并用药进行了推荐或建议,并完善了安全性信息,为其临床的合理使用提供参考。

乌蔹莓灌肠对远端溃疡性结肠炎患者的临床疗效

目的探讨乌蔹莓灌肠对远端溃疡性结肠炎患者的临床疗效。方法60例患者随机分为对照组和观察组,每组30例,对照组给予美沙拉嗪肠溶片,观察组在对照组基础上加用乌蔹莓灌肠,疗程8周。检测临床疗效、生活质量评分、DAI评分、Mayo活动指数、肠黏膜屏障功能指标(DAO、ET、D-乳酸)、肠道菌群(双歧杆菌、乳酸杆菌、大肠杆菌、肠球菌)、炎症因子(IL-10、IL-6、TNF-α)、安全性指标变化。结果观察组总有效率高于对照组(P<0.05)。治疗后,观察组生活质量评分、IL-10升高(P<0.05),DAI评分、Mayo活动指数、肠黏膜屏障功能指标、IL-6、TNF-α降低(P<0.05),双歧杆菌、乳酸杆菌增加(P<0.05),大肠杆菌、肠球菌减少(P<0.05),并比对照组更明显(肠球菌除外)(P<0.05)。2组未发现不良反应。结论乌蔹莓灌肠可安全有效地改善远端溃疡性结肠炎患者DAI评分和Mayo活动指数,其机制可能与调节菌群稳态、修复肠黏膜屏障、抑制炎症因子释放有关。

氨糖美辛肠溶片中盐酸氨基葡萄糖有关物质研究

目的 建立测定氨糖美辛肠溶片中盐酸氨基葡萄糖有关物质的高效液相色谱法,并分析其影响因素。方法 色谱柱为纳谱ChromCore AQ C18柱(250 mm×4.6 mm,3μm),流动相为水-乙腈(梯度洗脱),流速为1.0 mL/min,检测波长为280 nm,柱温为30℃,进样量为20μL。采用加速稳定性试验和辅料相容性试验,结合生产工艺分析有关物质的影响因素。结果 已知杂质果糖嗪、2,5-脱氧果糖嗪、吡嗪、5-羟甲基糠醛、糠醛、2-甲基吡嗪、吡咯-2-甲醛、5-甲基糠醛质量浓度分别在0.20~3.30μg/mL、0.20~3.00μg/mL、0.25~7.54μg/mL、0.18~7.04μg/mL、0.25~10.10μg/mL、0.25~10.18μg/mL、0.25~10.17μg/mL、0.26~10.50μg/mL范围内与峰面积线性关系良好(R2≥0.999);检测限为0.3~5.0μg/mL,定量限为0.7~20.1μg/mL;精密度、稳定性、重复性试验结果的RSD均小于2.0%;平均加样回收率为98.24%~101.20%,RSD为0.33%~2.19%(n=9)。影响制剂有关物质产生的因素为工艺、温度和时间,影响有关物质含量增长速率的因素除工艺外,还有辅料(主要为羟甲基淀粉钠)和水分。结论 该方法简便、准确、专属性好,可用于氨糖美辛肠溶制剂中盐酸氨基葡萄糖有关物质的检测。建议优化工艺中干燥温度及时间,考察添加辅料的合理性,并控制片剂中的水分,进一步提高制剂质量的均一性和稳定性。

双联抗血小板治疗非轻型缺血性脑卒中的临床效果

目的:探究双联抗血小板治疗非轻型缺血性脑卒中的临床效果。方法:选取2021年1月—2023年3月萍乡市人民医院神经内科就诊的91例非轻型缺血性脑卒中患者,中途脱落研究的患者共7例,最终84例患者进入研究。根据随机数字表法将患者分为对照组和研究组,各42例。对照组予以阿司匹林肠溶片治疗,研究组予以阿司匹林联合氯吡格雷治疗,并在21 d后改为阿司匹林单抗治疗。观察两组患者的临床效果及治疗前后的神经功能情况、不良事件及卒中复发情况。结果:治疗3个月后,研究组患者的临床有效率为85.71%,显著高于对照组(66.67%),差异有统计学意义(P<0.05)。研究组患者在治疗第7天、第21天、3个月的美国国立卫生研究院卒中量表(NIHSS)评分均低于对照组,差异均有统计学意义(P<0.05)。研究组卒中复发率(2.38%)显著低于对照组(14.29%),差异有统计学意义(P<0.05)。两组不良事件发生率比较,差异无统计学意义(P>0.05)。结论:双联抗血小板治疗非轻型缺血性脑卒中能较好地改善临床症状,降低卒中复发率,恢复神经功能且并未增加不良事件发生率,疗效及安全性良好。

泊沙康唑肠溶片在中国健康受试者中的生物等效性研究

目的研究泊沙康唑肠溶片在中国健康受试者体内的生物等效性。方法受试者空腹或餐后条件下口服受试或参比制剂100 mg后,用LC-MS/MS法检测泊沙康唑的血药浓度,用Phoenix WinNonlin 8.3计算药代动力学参数,并评价两制剂的生物等效性。结果两制剂主要药代动力学参数C_(max)、AUC_(0-t)、AUC_(0-∞)几何均值比90%置信区间均落在80.00%~125.00%。在试验过程中,未发生严重不良事件和非预期可疑不良事件。结论在空腹和餐后条件下,两种泊沙康唑肠溶片在中国健康受试者中具有生物等效性,且两制剂的安全性相当。

五味苦参肠溶胶囊联合沙利度胺片治疗难治性溃疡性结肠炎的疗效观察及对炎症因子、免疫功能和氧化应激的影响

目的:探究五味苦参肠溶胶囊联合沙利度胺片治疗难治性溃疡性结肠炎(UC)的疗效及对炎症因子、免疫功能和氧化应激的影响。方法:选取2018年6月~2022年6月于某院就诊的86例难治性UC患者为研究对象,采用随机数字表法分为对照组及观察组,每组43例。对照组患者仅给予沙利度胺片治疗,观察组给予沙利度胺片联合五味苦参肠溶胶囊治疗,两组均连续治疗4周。观察并比较两组患者治疗前后的外周血T淋巴细胞亚群(CD3^(+)、CD4^(+)、CD8^(+)及CD4^(+)/CD8^(+))水平、炎症因子水平[超敏C反应蛋白(hs-CRP)、肿瘤坏死因子-α(TNF-α)、细胞间黏附分子-1(ICAM-1)、血管细胞黏附分子1(VCAM-1)及白介素-10(IL-10)]及氧化应激指标[超氧化物歧化酶(SOD)、丙二醛(MDA)]水平、改良Mayo内镜评分、临床疗效及临床症状(腹痛、腹泻、脓血便、肛门灼热)改善时间。结果:治疗后,两组患者CD3^(+)、CD4^(+)及CD4^(+)/CD8^(+)均较治疗前升高,且观察组高于对照组(P<0.05);CD8^(+)水平较治疗前降低,且观察组低于对照组(P<0.05);hs-CRP、TNF-α、ICAM-1及VCAM-1水平均较治疗前降低,且观察组低于对照组(P<0.05);IL-10水平较治疗前升高,且观察组高于对照组(P<0.05);SOD水平较治疗前升高,MDA水平较治疗前降低(P<0.05),且观察组的改善程度优于对照组(P<0.05)。两组患者改良Mayo内镜评分较治疗前降低,且观察组低于对照组(P<0.05)。观察组的临床治疗总有效率(93.02%)高于对照组(79.07%,P<0.05);腹痛、腹泻、脓血便以及肛门灼热等临床症状改善时间均短于对照组(P<0.05)。结论:与单用沙利度胺片相比,五味苦参肠溶胶囊联合沙利度胺片可进一步改善难治性UC患者的临床症状,缩短症状改善时间,调节患者体内外周血T淋巴细胞水平,改善炎症因子水平以及氧化应激水平,具有较好的治疗前景,值得临床推广。

化湿解毒方治疗湿热内蕴型溃疡性结肠炎临床研究

目的:观察化湿解毒方治疗湿热内蕴型溃疡性结肠炎的临床疗效及对患者大肠杆菌、乳酸菌和双岐杆菌等肠道菌群的影响。方法:将60例湿热内蕴型溃疡性结肠炎患者按照随机数字表法分为对照组和治疗组,每组各30例。对照组口服美沙拉嗪肠溶片,治疗组给予化湿解毒方。比较两组患者的临床疗效及治疗前后腹胀、腹痛、黏液脓血便及里急后重等临床症状积分变化情况,检测两组患者治疗前后大肠杆菌、双歧杆菌及乳酸菌等肠道菌群数量,统计两组患者治疗前后疾病活动指数(isease activity index,DAI)及内镜评分。结果:治疗组有效率为93%,对照组有效率为80%,两组患者有效率比较,差异具有统计学意义(P<0.05)。两组患者治疗后临床症状积分低于本组治疗前,且治疗后治疗组低于对照组(P<0.05)。两组患者治疗后肠道菌群中大肠杆菌数量低于本组治疗前,乳酸杆菌和双歧杆菌数量高于本组治疗前,且治疗后组间比较,差异具有统计学意义(P<0.05)。两组患者治疗后DAI及内镜评分低于本组治疗前,且治疗后治疗组低于对照组(P<0.05)。结论:化湿解毒方治疗湿热内蕴型溃疡性结肠炎,疗效确切,可调节患者肠道菌群数量,有效改善临床症状。

阿司匹林肠溶片药物利用评价标准的建立与应用

目的建立阿司匹林肠溶片药物利用评价(DUE)标准,为临床合理应用阿司匹林肠溶片提供参考。方法参考阿司匹林肠溶片药品说明书、相关指南、专家共识和文献,并通过德尔菲法,在用药指征、用药过程和用药结果3个方面建立阿司匹林肠溶片DUE标准。采用回顾性研究方法,对福建医科大学附属福清市医院2021年1月—2022年6月使用阿司匹林肠溶片的住院患者病历进行用药合理性评价。结果共纳入1071份病历,完全符合评价标准的有683例,用药合理率为63.77%。不合理用药情况主要为适应证不适宜(6.26%)、超说明书用药未备案(28.48%)、用药禁忌(1.03%)、用法用量不适宜(1.68%)、有潜在临床意义的药物相互作用(0.65%)和其他不适宜(2.71%)。结论本研究建立的阿司匹林肠溶片DUE标准有较强的科学性、实用性和可行性。该院阿司匹林肠溶片用药不合理率较高,应制订相应的干预措施,保证临床用药安全。

白屈菜总生物碱缓释片制备工艺研究

目的:以羟丙基甲基纤维素为缓释材料制备白屈菜总生物碱缓释薄膜衣片解决白屈菜有效成分药物浓度不稳定的缺点,并建立可靠的含量测定方法。方法:采用单因素实验对白屈菜总碱缓释薄膜衣片制备工艺进行筛选,以释放度为依据;采用高效液相色谱法(HPLC)建立了白屈菜总碱缓释薄膜衣片中血根碱的含量测定方法。结果:优化的缓释片工艺处方:30%白屈菜总碱提取物、30%HPMC、20%可压性淀粉、10%乳糖、10%微晶纤维素,挤压制粒,加1%硬脂酸镁,压片,即得。结论:该工艺制得白屈菜总碱缓释片释药曲线平缓,缓释效果良好,方法简单易行,所得薄膜衣片外观和可压性良好。

实炎方对湿热蕴肠型溃疡性结肠炎患者的临床疗效

目的探讨实炎方对湿热蕴肠型溃疡性结肠炎患者的临床疗效。方法82例患者随机分为对照组和观察组,每组41例,对照组给予美沙拉嗪肠溶片,观察组在对照组基础上加用实炎方,疗程8周。检测临床疗效、中医证候评分、炎症因子(白细胞介素-6、白细胞介素-22、白细胞介素-33)、肠黏膜屏障功能指标(二胺氧化酶、D-乳酸、内毒素)、肠道菌群(大肠杆菌、肠球菌、双歧杆菌、乳酸杆菌)、GQOLI-74评分变化。结果观察组总有效率高于对照组(P<0.05)。治疗后,2组中医证候评分、血清炎症因子、肠黏膜屏障功能指标降低(P<0.05),GQOLI-74升高(P<0.05),肠球菌减少(P<0.05),双歧杆菌、乳酸杆菌增加(P<0.05),以观察组更明显(P<0.05)。结论实炎方可提高溃疡性结肠炎患者生活质量,临床疗效明显。

富马酸伏诺拉生片治疗非糜烂性反流病的临床研究

目的研究富马酸伏诺拉生片与艾司奥美拉唑镁肠溶片在治疗非糜烂性反流病(non-erosive reflux disease,NERD)中的效果及不良反应对比。方法选取124例NERD患者,采用随机数字表法分为观察组62例和对照组62例。观察组给予富马酸伏诺拉生片,对照组给予艾司奥美拉唑镁肠溶片,疗程均为4周。对幽门螺旋杆菌(helicobacter pylori,HP)阳性的患者进一步根除HP。比较2组患者的临床疗效、反流性疾病问卷量表(reflux disease questionnaire,RDQ)评分、匹兹堡睡眠质量指数(pittsburgh sleep quality index,PSQI)评分、治疗前后食管pH值变化、HP根除率及不良反应发生率。结果观察组总有效率高于对照组(P<0.05),观察组治疗后RDQ评分低于对照组(P<0.05),观察组治疗后PSQI评分低于对照组(P<0.05),观察组治疗后pH<4反流次数、>5 min反流次数和pH<4总时间低于对照组(P<0.05),观察组HP根除率高于对照组(P<0.05)。观察组和对照组比较,总不良反应率无明显差异(P>0.05)。结论在治疗非糜烂性反流病方面,富马酸伏诺拉生片与艾司奥美拉唑镁肠溶片对比,疗效显著,可改善睡眠质量,抑酸更强,提高HP根除率,并不增加不良反应。