Preparation and <i>in Vitro</i>Drug Release Evaluation of Once-Daily Metformin Hydrochloride Sustained-Release Tablets

The objective of this study was to develop once-daily metformin hydrochloride sustained-release tablets (MHSRT) and evaluate their in vitro release behavior. MHSRT were prepared by the film coating method. The in vitro drug release rate of MHSRT and the commercial tablets Fortamet? made in the United States of America in water was fitted with zero order kinetic equation, and Ritger-Peppas kinetic equation in 0.1 M HCl and pH 6.8-phosphate buffer, respectively. The similarity factor f2 values of MHSRT in three different dissolution medium were 82, 80 and 74, respectively in comparison with imported Fortamet?, which were all greater than 50. The results of storage-stability showed that MHSRT were stable for at least 6 months under stress condition (40℃ ± 2℃, RH 75% ± 5%). Therefore, in this study, MHSRT were successfully prepared using optimized formulation technologies that meet mass produce. The in vitro release behavior of MHSRT was almost similar to that of imported Fortamet?.

Preparation and evaluation of sustained-release azithromycin tablets in vitro and in vivo

The objective of this study was to prepare azithromycin(AZI)sustained-release products in order to allow for a high dose to be administered,reduce gastrointestinal side-effects and increase the compliance of patients.AZI sustained-release tablets with different release performance(F-I:T_(100%)=3 h and F-II:T_(100%)=8 h in pH 6.0 phosphate buffer)were successfully prepared by wet granulation.The in vitro release rate and drug release mechanism were studied.The release rate of F-Iwas affected by dissolutionmedia with different pH,but not for F-II.HixsoneCrowellmodel was the best regression fitting model for F-I and F-II.Additionally,F-I and F-II both belonged to non-Fick diffusion.Oral pharmacokinetics of the two tablets and one AZI dispersible tablet as reference were studied in six healthy beagle dogs after oral administration.Compared with the reference,the C_(max) of F-I and F-II were decreased,and the T_(max) were prolonged,in that case which meet the requirement of sustained-release tablets.The relative bioavailability of F-I and F-II were 79.12%and 64.09%.T-test ofAUC_(0-144),and AUC_(0-∞) for F-I and F-II indicated there was no significant difference between F-I and F-II.These mean that the extended release rate did not induce different pharmacokinetics in vivo.

Clinical observation of Baitou Weng Decoction combined with mesalazine sustained-release tablets in treating heat-toxic and smoldering ulcerative colitis

Objective:To observe the clinical efficacy of Baitou Weng Decoction combined with mesalazine sustained-release tablets in the treatment of ulcerative colitis with febrile heat and its effect on immune function and serum inflammatory factors.Methods: A total of 84 patients with ulcerative colitis were randomly divided into control group and treatment group, with 42 cases in each group. The control group was given mesalazine sustained-release tablets orally, while the treatment group was given Baitou Weng Decoction and mesalazine sustained-release tablets orally. The treatment period was 30 days and the patients were followed up for 3 months. After treatment, the clinical efficacy, quality of life, immune function and serum inflammatory factors of the two groups were observed.Results: The effective rate of treatment group (90.47%) was higher than that of control group (73.81%) (P<0.05);compared with before treatment, the scores of inflammatory bowel disease quality of life questionnaire scale in both groups were significantly improved (P<0.05), and the difference between the two groups was significant (P<0.05);after treatment, the plasma CD4+/CD8+ ratio and NK+ levels in both groups were significantly higher than those before treatment (P<0.05), and the treatment group was changed. The serum levels of tumor necrosis factor-α, interleukin-17 and interleukin-23 were significantly decreased in both groups after treatment (P<0.05), and the improvement was more significant in the treatment group (P<0.05). No significant adverse reactions were observed in the treatment group.Conclusions: Modified Baitou Weng Decoction combined with mesalazine in the treatment of heat-toxic and incandescent ulcerative colitis can significantly improve the clinical efficacy, improve the quality of life of patients, effectively regulate the expression level of serum inflammatory factors in ulcerative colitis patients, promote the recovery of patients' immune function, and have high drug safety.

Simultaneous Analysis of Indapamide and Related Impurities in Sustained-Release Tablets by a Single-Run HPLC-PDA Method

The contents of indapamide and related impurities in generic indapamide sustained-release tablets were simultaneously detected by a single-run high performance liquid chromatography equipped with photodiode array detector(HPLC-PDA)method for the quality control in this paper.The results showed the method had a good selectivity and was validated through linearity,limits of detection and quantification,recovery,and precision.The linear ranges of indapamide,2-methyl-1-nitroso-2,3-dihydro-1H-indole(impurity A,ImA),4-chloro-N-(2-methyl-1H-indol-1-yl)-3-sulphamoyl-benzamide(impurity B,ImB)and 4-chloro-3-sulfamoylbenzoic acid(impurity 1,Im1)were 0.028-1.80μg/mL(R=0.99995),0.060-1.20μg/mL(R=0.9996),0.0324-1.20μg/mL(R=0.99985)and 0.060-1.20μg/mL(R=0.9997)with detection limits of 0.0093,0.012,0.012 and 0.006μg/mL,respectively.ImA and Im1 were not detectable in the generic drug.The content of indapamide was 96.7%of the labeled amount with a relative standard deviation(RSD)of 1.30%,and the percentage of ImB relative to the labeled amounts of indapamide was 0.106%with an RSD of 1.82%.The content of other unspecified impurities all met the reference quality standards.The results provided references for the quality control and the quality standard study of generic indapamide sustained-release tablets.

非洛地平缓释片联合氢氯噻嗪治疗对高血压患者血压水平的影响分析

目的分析非洛地平缓释片联合氢氯噻嗪治疗对高血压患者血压水平的影响。方法100例高血压患者,根据治疗方法不同分为对照组与观察组,各50例。对照组服用非洛地平缓释片治疗,观察组在对照组治疗基础上加用氢氯噻嗪治疗。比较两组患者治疗前后的血压水平(24 h平均收缩压、24 h平均舒张压)、生活质量以及三餐后血压下降幅度、餐后低血压(PPH)发生情况。结果治疗8周后,两组患者24 h平均收缩压、24 h平均舒张压均低于治疗前,且观察组患者24 h平均收缩压(134.15±10.22)mm Hg(1 mm Hg=0.133 kPa)、24 h平均舒张压(83.49±8.59)mm Hg均低于对照组的(146.69±12.36)、(87.69±9.66)mm Hg,差异具有统计学意义(P<0.05)。治疗8周后,两组患者早餐、午餐、晚餐后血压下降幅度均小于治疗前,且观察组患者早餐后血压下降幅度(21.19±4.15)mm Hg、午餐后血压下降幅度(25.36±5.06)mm Hg、晚餐后血压下降幅度(24.32±5.03)mm Hg均低于对照组的(25.36±5.16)、(27.89±5.29)、(27.39±6.95)mm Hg,差异具有统计学意义(P<0.05)。治疗8周后,观察患者组早餐后PPH发生率30.00%、新增发病率4.00%均低于对照组的60.00%、16.00%,差异具有统计学意义(P<0.05);两组患者午餐、晚餐后PPH发生率以及新增发病率比较,差异均无统计学意义(P>0.05)。治疗8周后,两组患者躯体评分、认知评分、情绪评分、角色评分、社会功能评分均高于治疗前,且观察组患者躯体评分(81.11±8.57)分、认知评分(86.95±8.45)分、情绪评分(85.69±9.44)分、角色评分(81.48±7.28)分、社会功能评分(78.29±5.44)分高于对照组的(70.22±9.52)、(75.65±8.52)、(75.98±8.56)、(71.42±7.48)、(70.18±5.56)分,差异具有统计学意义(P<0.05)。结论针对高血压患者,应用非洛地平联合氢氯噻嗪治疗更能有效控制患者的血压水平,且不会明显增加患者临床治疗期间PPH发生率,帮助患者获得较高的生活质量,具有理想的应用价值。

非洛地平缓释片治疗社区原发性高血压的效果观察

目的:观察非洛地平缓释片治疗社区原发性高血压的效果。方法:选取2020年10月—2022年10月北京市丰台区北宫镇社区卫生服务中心收治的原发性高血压患者60例作为研究对象,采用随机数字表法分为两组,各30例。对照组给予硝苯地平控释片治疗,观察组给予非洛地平缓释片治疗。比较两组治疗效果。结果:观察组治疗总有效率高于对照组,差异有统计学意义(P=0.0195)。治疗后,两组收缩压、舒张压水平低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05)。观察组不良反应总发生率低于对照组,差异有统计学意义(P=0.0195)。治疗后,两组生理状况、社会功能、自理行为、情感状况、精神状况、生命活力、总健康评分高于治疗前,且观察组高于对照组,差异有统计学意义(P<0.05)。结论:非洛地平缓释片治疗社区原发性高血压的效果显著,可改善患者血压水平,降低不良反应发生率,提升生活质量。

非洛地平缓释片治疗高血压的作用评估分析

目的 讨论高血压患者采取降压药物疗法时非洛地平缓释片的功效。方法 本研究选取2021年5月—2023年5月青岛市城阳区人民医院治疗的138例高血压患者为研究对象,按照随机数表法分为两组,每组69例。对比组采取常规疗法,研究组采取非洛地平缓释片疗法,比较两组患者临床疗效、血压水平、药物不良反应发生率。结果 研究组患者治疗总有效率为94.20%,高于对比组,差异有统计学意义(χ^(2)=5.434,P<0.05);研究组患者治疗8周后的舒张压(83.58±4.62)mmHg、收缩压(132.41±6.59)mmHg低于对比组,差异有统计学意义(t=6.264、7.339,P<0.05);研究组不良反应总发生率为1.45%,低于对比组,差异有统计学意义(χ^(2)=5.824,P<0.05)。结论 高血压患者控制饮食与运动期间,再予以非洛地平缓释片治疗方案,有提高疗效、改善血压作用,药物不良反应发生率很低,临床应用价值很高。

非洛地平缓释片治疗社区高血压的效果及病人依从性观察

目的探讨非洛地平缓释片治疗社区高血压的效果及病人依从性。方法择2018年10月-2021年10月本社区收治的150例高血压患者为研究对象,依据随机抽签法分为治疗组和对照组,每组各75例。治疗组予以非洛地平缓释片治疗,对照组采用厄贝沙坦治疗。比较两组患者治疗前后SBP、DBP指数以及治疗依从度。结果两组治疗前SBP、DBP指数比较差异无统计学意义(P>0.05);两组治疗后,治疗组SBP、DBP指数均低于对照组(P<0.05)。治疗组患者治疗总依从度92.00%高于对照组80.00%(P<0.05)。结论非洛地平缓释片治疗社区高血压的效果显著,改善舒张压以及收缩压指数,提升治疗依从度,利于病情恢复,值得推广和运用。

不同产品非洛地平缓释片药物动力学比较

目的:比较几种国产非洛地平缓释片在体内的药物动力学和生物利用度。方法:用高效液相色谱测定口服药物后血浆药物浓度,以普通非洛地平片作为参照,计算药物动力学和生物利用度。结果:在0.5～10μg·L-1范围内,非洛地平血浆药物浓度与色谱峰高呈现良好线性相关。单剂量人血浆中非洛地平缓释片动力学参数在不同产品存在差别,相对于普通制剂的生物利用度分别为168%、177%和125%。结论:不同产品非洛地平缓释片药物动力学和生物利用度存在差别。

非洛地平口腔粘附片的研究

目的 :研制非洛地平口腔粘附片 ,考察其体外膨胀率、粘附力及释药性能。方法 :采用不同粘度规格的羟丙基甲基纤维素 ( HPMC)和卡波母 ( Carbopol 934 P)为生物粘附材料 ,以不同配比制备非洛地平口腔粘附片 ,桨板法测定其释放度。结果 :以低粘度规格的 HPMC和 Carbopol934 P( 3∶ 1 )为生物粘附材料 ,制得的口腔粘附片较好。结论 :非洛地平口腔给药是可行的。

非洛地平缓释制剂体外释放度比较

目的:对不同厂家非洛地平缓释制剂的体外释放度进行比较。方法:按照非洛地平的部颁标准,采用桨法测定非洛地平缓释制剂的释放度,通过选用数学模型线性拟合,求出参数,进行方差分析。结果:B样品释放度的均一性和重现性均好于A样品,A样品同一样品不同批号间释放度差异极具显著性(P<0.01),B样品有2个批号间差异具显著性(P<0.05)。结论:两个厂家的产品的释放度均符合部颁标准规定,B样品释放度好于A样品。

非洛地平口腔粘膜粘附片的制备及其性质评价(英文)

目的 :制备非洛地平口腔粘膜粘附片 ,并对其进行性能评价。方法 :以HPMCK4M和Carbopol 974P为生物粘附聚合物 ,加入碳酸氢钠采用直接压片法制备非洛地平口腔粘膜粘附片。以鸡嗉囊为模型测定其粘附力 ,采用改进的桨法测定粘附片的体外释放行为 ,并测定了粘附片的表面pH值 ,对粘附片的体内粘附行为和刺激性也进行了评价。结果 :粘附片的表面pH值为 7 0 1± 0 11。非洛地平从粘附片中以SuperCase Ⅱ机制释放 ,表观释放速率常数k为 3 3 %h-1 。粘附片与鸡嗉囊接触后产生的粘附力平均为 181 3 5± 3 1 0 8g ,经体内验证与口腔粘附性较为合适 ,且对口腔粘膜刺激性较小。结论

硝苯地平缓释片与非洛地平缓释片治疗不同高血压患者疗效观察

目的观察硝苯地平缓释片与非洛地平缓释片对不同高血压患者的临床疗效。方法266例患者根据血压水平分为高血压1、2级组和高血压3级组。每组患者随机再分成两组,分别服用硝苯地平缓释片(伲福达)与非洛地平缓释片(波依定),观察疗效。结果高血压1、2级组中,硝苯地平缓释片组(伲福达组)与非洛地平缓释片组(波依定组)的降压总有效率相似(P>0.05)。高血压3级组中,硝苯地平缓释片组降压总有效率高于非洛地平缓释片组(P<0.05)。结论对于轻、中度高血压患者,两种药物降压效果相似,均可选择。对于重度高血压患者,硝苯地平缓释片较非洛地平缓释片更为有效。

通心络胶囊联合非洛地平缓释片治疗高血压伴糖尿病患者的效果

目的 观察通心络胶囊联合非洛地平缓释片对高血压伴糖尿病患者的治疗效果。方法选取2014年4月至2015年4月江西省人民医院收治的高血压伴糖尿病患者82例,按照随机数字表法分为观察组和对照组,各41例。对照组采用非洛地平缓释片,5 mg/次,每日1次,观察组患者在此基础上加以通心络胶囊,2~4粒/次,每日3次。两组患者的治疗疗程均为1个月。比较两组患者的血糖、血压、血脂、治疗效果、不良反应发生情况。结果 观察组患者餐后2 h血糖、空腹血糖、收缩压、舒张压水平显著低于对照组[（11.0±2.5）mmol/L比（12.5±2.9）mmol/L、（6.4±1.4）mmol/L比（8.4±1.4）mmol/L、（118.0±9.3）mmHg（1 mmHg=0.133 k Pa）比（128.4±10.4）mmHg、（79.9±1.2）mmHg比（96.0±2.3）mmHg],差异有统计学意义（P〈0.05）。观察组低密度脂蛋白胆固醇、三酰甘油、总胆固醇显著低于对照组[（1.3±0.4）mmol/L比（2.4±0.5）mmol/L、（1.5±0.3）mmol/L比（2.4±0.4）mmol/L、（1.7±0.3）mmol/L比（2.6±0.7）mmol/L],高密度脂蛋白胆固醇显著高于对照组[（1.7±0.5）mmol/L比（1.3±0.3）mmol/L],差异有统计学意义（P〈0.01）。观察组患者的临床总有效率显著高于对照组[92.68%（38/41）比73.17%（30/41）],不良反应发生率显著低于对照组[12.20%（5/41）31.71%（13/41）],差异有统计学意义（P〈0.05）。结论 高血压伴糖尿病患者采用通心络胶囊联合非洛地平缓释片进行治疗,能明显降低患者的血压和血糖水平,有利于患者血脂水平的改善,临床疗效良好,安全性高。

三种治疗高血压药物的成本-效果分析

目的对3种治疗高血压药物进行经济学评价。方法运用成本-效果分析法对氨氯地平、非洛地平、缓释硝本地平的疗效及成本进行比较。结果3组成本-效果比分别为1.14、0.81、0.78。结论缓释硝本地平为最佳方案。

控释制剂释放动力学评价理论研究

目的:建立控释制剂释放动力学的评价新理论和模型。方法:针对控释制剂具有零级释放动力学基本特征,结合控释制剂释放度及其变化速率的曲线特征,阐明控释制剂释放动力学评价的原理。采用新建立的模型,评价市售非洛地平渗透泵片在不同转速下的控释特征。结果:依据控释制剂释放动力学原理,提出控释度(ICR)、早期释放差异指数(IR-Di)、末端释放差异指数(IRDt)等指标。非洛地平渗透泵片在75,100,150r/min时的体外ICR分别为70.8%,74.8%和64.2%;IRDi和IRDt定量反映了测定因素转速对非洛地平渗透泵片的控释特征的影响。结论:本文提出的控释制剂释放动力学评价理论,可以对控释制剂的不同释放阶段及整体的控释动力学进行定量评价,相关参数为剂型定量设计和优化提供了方法学基础。

互聚物复合形成对口腔粘膜粘附片释放的影响(英文)

通过测量 HPMC和 Carbopol974 P在不同 p H值的缓冲液中的混合溶液浊度变化的方法证实了互聚物复合形成。复合的程度在酸性 p H条件下高 ,当两者比例为 1∶ 1时最强 ,然后随着 p H值的升高而减弱。以非洛地平为模型药物 ,采用直接压片工艺制备了口腔粘膜粘附片。体外释放实验表明 ,互聚物复合形成对药物的释放有很大影响 ,能够有效控制药物释放。粘附片中加入不同酸碱度的物质可调节药物的释放速率。聚合物间的这种特殊的互聚物复合形成现象可用于设计具有不同释药行为的药物释放系统。

非洛地平缓释片释放度比较

目的观察非洛地平缓释片体外释放度和治疗效果分析。方法照中国药典2000版二部和卫生部有关非洛地平质量控制标准的有关规定,采用转篮法,十六烷基三甲基溴化胺-磷酸盐缓冲液为介质,紫外分光光度法测定。结果非洛地平缓释片累积释放百分率符合H iguch i方程,释放速度符合零级模型。结论不同产品药物释放情况与临床治疗结论一致。

非洛地平缓释片的释放度研究

目的 :考察与比较国产缓释片和进口缓释片的释药行为。方法 :采用中国药典的转篮法 ,研究国产片及进口片的释放度。结果 :前者释药较快 ,6h释药达 98%以上 ,但后者释药缓慢平稳 ,释药时间长达 10h ,两者释药行为均符合零级动力学。结论

4种不同的包衣材料对非洛地平释药性能的影响

[目的]考察4种不同的包衣材料对非洛地平释药性能的影响。[方法]对不同包衣材料缓释片的硬度、脆碎度、吸湿性进行测定,结合电镜扫描图谱,采用非洛地平缓释片质量标准的释放度测定法,以相似因子f2值为指标,筛选包衣材料的种类和增重量。[结果]f2值为56.01,确定欧巴代Ⅱ型为非洛地平缓释片的包衣材料,包衣增重量为2%,硬度为109.11 N,脆碎度为0.46%和吸湿增重百分率为0.16%,均符合要求。并且结果可以满足中国药典对缓控释制剂的体外溶出要求,释放动力学特征以Ritger-Peppas模型拟合较好,根据Peppas方程,其释放机制是药物扩散和骨架溶蚀的共同作用。[结论]欧巴代Ⅱ型包衣片与原研药的释药特性最为相似,可用于非洛地平的包衣材料。