Pharmacokinetics of nifedipine sustained-release tablets in healthy Chinese volunteers

Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 （5 μm, 4.6 mm ×150 mm） column and a mobile phase of methanol： 0.01 mol·L^-1ammonium acetate （60：40, V/V） were used to separate nifedipine, the detections was accuracy under atmosperic pressure electronic spray ionization （AP-ESI） mode and ion mass spectrum （m/z） of 314.9 [M＋H]^＋ for nifedipine, and 320.8 [M＋H]^＋ for lorazepam （Internal Standard, IS）. Results The linear range of nifedipine was 0.3 - 80 ng·mL^-1 （ r = 0.9997）, and the limit of quantitation （LOQ） was 0.3 ng·mL^-1. The nifedipine pharmacokinetic parameters after a single dose of 20 mg nifedipine sustained-release tablets test （T） or reference （R） were as the followings, t1/2 （6.73 ± 2.00） h and （7.04 ± 2.18） h, Tmax （4.28 ± 0.70） h and （4.48 ± 0.70） h, Cmax（39.66 ± 10.58） ng·mL^-1 and （40.19 ± 10.97） ng·mL^-1, AUC0-36 （391.63 ± 108.55） ng·mL^-1·h and （387.57 ± 121.51） ng·mL^-1·h, and AUC0-∞ （408.28 ± 121.16） ng·mL^-1·h and （406.15 ± 133.13） ng·mL^-1·h. The relative bioavailability of nifedipine sustained-release tablets （test） was （103.02 ± 13.93） %. Conclusion LC-MS method for the determination of concentrations of nifedipine in human plasma was sensitive and accurate, and could be used in nifedipine bioavailability and pharmacokinetic studies.

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.

Clinical observation on treatment of cancer pain with TCM oriented drugs combined with oxycodone sustained-release tablets and nimesulide sustained-release tablets

Objective： To study the effect of the transdermal preparation of traditional Chinese medicine in treating cancer pain. Methods： From October 2016 to January 2018, 126 patients with cancer pain were enrolled and divided into 4 groups, 39 patients in group A （directed TCM permeation）, 26 patients in group B （oxycodone sustained-release tablets）, 32 patients in group C （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets）, and 29 patients group D （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets ＋ nimesulide sustained release tablets）, according to KPS scores. Results： Transdermal preparations of traditional Chinese medicine can significantly alleviate cancer pain. For the treatment of moderate to severe cancer pain, the Chinese medicine transdermal preparation can reduce the dosage of oxycodone sustained-release tablets. At the same time, the patient＇s KPS and NRS scores were significantly reduced. Moreover, the transdermal preparation of traditional Chinese medicine has a better therapeutic effect on visceral pain. Conclusion： The traditional Chinese medicine tra_nsdermal preparation combined with western medicine for the treatment of cancer pain may be a new method for the treatment of cancer pain.

Pharmacokinetic Study on Lovastatin Sustained-release Tablet and Sustained-release Capsule in Begal Dogs

This study pharmacokinetically examined the lovastatin sustained-release tablet and sustained-release capsule in Beagle dogs. An reversed-phase HPLC method was established for the determination of lovastatin in Beagle dog plasma. Pharmacokinetic findings were compared among three preparation(lovastatin sustained-release tablet,T p; sustained-release capsule,T J and conventional capsule). Our results showed that the pharmacokinetic parameters in 6 dogs after single-dose oral administration of three perparations were calculated. T max, C max and MRT revealed significant difference (P<0.05). Relative bioavailability was 111.5±16.9 % (T P) and 110.4%±9.6 % (T J). The pharmacokinetic parameters in the 6 dogs after multiple-dose oral administration of three perparations, T max, C max MRT and DF had significant difference (P<0.05); C av , C min and AUC 0-24 h displayed no significant difference (P>0.05). It is concluded that the lovastatin sustained-release tablet and sustained-release capsule are able to maintain a sustained-release for 24 h.

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.

Qualitative and quantitative analysis of HPLC fingerprint of Wuji gastric floating sustained-release tablets

A qualitative and quantitative test method of fingerprint of Wuji gastric floating sustained-release tablets was established. High performance liquid chromatography （HPLC） was adopted, using Agilent ZORBAX SB-C18 column （250 mm×4.6 mm, 5 μm） as the chromatographic column, and acetonitrile-0.05 mol/L potassium dihydrogen phosphate solution as the mobile phase in a gradient elution with the flow rate of 1.0 mL/min. Sample solution （10 μL） was injected and was tested at the wavelength of 225 nm for 75 min at the column temperature of 30 ℃, Fingerprint similarity software （2004A version） was used to conduct data analysis. A total of 11 batches of Wuji gastric floating sustained-release tablets were tested and analyzed with HPLC fingerprint. Seventeen common peaks were found and the similarity of the 11 batches of agents was greater than 0.9, indicating that the production process of the agent is stable and feasible. The method is operable and could effectively control the quality of Wuji gastric floating sustained-release tablets.

天麻钩藤汤联合非洛地平缓释片治疗肝阳上亢型原发性高血压患者的效果

目的:观察天麻钩藤汤联合非洛地平缓释片治疗肝阳上亢型原发性高血压(EH)的效果。方法:选取2021年6月至2023年6月该院收治的100例肝阳上亢型EH患者进行前瞻性研究,按随机数字表法将其分为观察组与对照组各50例。对照组采用非洛地平缓释片治疗,观察组在对照组基础上联合天麻钩藤汤治疗。比较两组临床疗效,治疗前后血压水平、中医证候积分、血管内皮功能指标[内皮素-1(ET-1)、一氧化氮(NO)]水平,以及不良反应发生率。结果:观察组治疗总有效率为94.00%(47/50),高于对照组的80.00%(40/50),差异有统计学意义(P<0.05);治疗后,两组收缩压、舒张压水平均低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05);治疗后,两组头晕头痛、烦躁易怒、少寐多梦、口苦口干、便秘等中医证候积分均低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05);治疗后,两组ET-1水平均低于治疗前,且观察组低于对照组,两组NO水平均高于治疗前,且观察组高于对照组,差异有统计学意义(P<0.05);两组不良反应发生率比较,差异无统计学意义(P>0.05)。结论:天麻钩藤汤联合非洛地平缓释片治疗肝阳上亢型EH患者可提高治疗总有效率,改善血管内皮功能指标水平,降低血压水平和中医证候积分,其效果优于单纯非洛地平缓释片治疗。

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。