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?.

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.

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.

阿片类联合激素及抗惊厥药治疗晚期癌痛的临床观察

目的探讨晚期癌痛应用阿片类药物的合理用药方案。方法选择伴有中、重度疼痛的晚期肿瘤患者,分3组,第一组36例,采用盐酸羟考酮控释片(奥施康定)单药治疗;第二组19例,用奥施康定和甲强龙联合治疗;第三组25例,用奥施康定联合加巴喷丁。观察3组患者治疗后的疼痛缓解情况和生活质量。结果单用奥施康定组完全缓解率为63.9%,奥施康定联合甲强龙组为68.4%,奥施康定和加巴喷丁联用组为48.0%。主要毒副反应为便秘,其次为恶心、呕吐。第二组毒副反应最轻,第三组部分患者出现头晕和嗜睡。结论阿片类药物奥施康定治疗晚期癌痛具有较好的疗效,其中奥施康定联合甲强龙尤其适合肺癌伴脑转移或骨转移患者,且安全性高,值得临床推广。

盐酸羟考酮缓释片治疗中重度癌痛疗效观察

目的:观察盐酸羟考酮缓释片治疗中重度癌痛患者临床疗效及不良反应。方法:166例中重度癌痛患者随机分为对照组(n=83)和观察组(n=83);对照组口服硫酸吗啡控释片,观察组在对照组基础上加服羟考酮缓释片。治疗10 d后观察比较两组患者镇痛疗效、生活质量评分及治疗过程中药品不良反应发生情况。结果:观察组治疗后总有效率(91.57%)显著高于对照组(P<0.05);生活质量评分(41.07±12.17分)也显著高于对照组(P<0.05)。两组患者不良反应发生率比较,差异无统计学意义(P>0.05)。结论:盐酸羟考酮控释片治疗中重度癌痛患者疗效显著,安全性高,值得推广应用。

缓控释强阿片类药物在老年癌痛患者中的应用分析

目的了解缓控释强阿片类药物在老年癌痛患者中的应用情况及用药趋势。方法对2008年1月至2010年12月在镇痛科就诊的776例年龄≥65岁的老年癌症患者使用缓控释强阿片类药物的情况进行统计和分析。结果缓控释强阿片类药物在老年癌痛患者的用量逐年增加,在硫酸吗啡缓释片、芬太尼透皮贴剂以及盐酸羟考酮控释片这三类缓控释强阿片类药物中,芬太尼透皮贴剂的用药频度位居第一,盐酸羟考酮控释片的用量增长迅速。结论本院老年癌症止痛治疗中用药是合理的。

羟考酮缓释片与即释吗啡片联合治疗对癌痛患者疼痛程度及疗效的影响

目的探讨羟考酮缓释片与即释吗啡片联合给药治疗对癌痛患者疼痛程度及疗效的影响。方法选择2016年1月—2018年4月该院肿瘤科癌痛患者112例,按照随机数字表法分成两组,每组56例。对照组患者采用羟考酮缓释片治疗,观察组在对照组患者的治疗基础上联合即释吗啡片治疗。通过疼痛视觉评分(VAS)评价两组患者治疗前、治疗10 d后疼痛程度,及两组患者治疗10 d后临床疗效。结果治疗后,观察组患者临床治疗总有效率明显高于对照组(82.14%vs 50.00%),差异有统计学意义(χ~2=13.47,P<0.05);两组患者VAS疼痛评分均较治疗前降低,且治疗后对比,观察组VAS疼痛评分明显低于对照组,差异有统计学意义(组内:t观察组=19.78,t对照组=4.07;组间:t治疗后=15.12;P<0.05)。结论羟考酮缓释片联合即释吗啡片可以更有效地缓解癌痛患疼痛程度和临床症状,临床疗效显著,在癌痛患者中的应用价值较高。

盐酸羟考酮缓释片在中重度成人癌痛门诊治疗中的疗效及安全性

目的观察盐酸羟考酮缓释片在中重度成人癌痛门诊治疗中的疗效和安全性。方法回顾分析49例中重度成人癌痛门诊就诊期间应用盐酸羟考酮缓释片的有效率、疼痛缓解效果及不良反应。比较性别、教育水平、首诊疼痛程度、疼痛类型及转移情况对有效率、疼痛缓解效果的影响。VAS评分下降25.0%及以上为治疗有效,其中疼痛完全消失为完全缓解,VAS评分下降75.0%及以上为明显缓解,VAS评分下降50.0%-74.9%为中度缓解,VAS评分下降25.0%-49.9%为轻度缓解,VAS评分下降小于25.0%为未缓解。结果盐酸羟考酮缓释片的总有效率为81.6%,其中完全缓解0例,明显缓解3例(6.1%),中度缓解25例(51.0%),轻度缓解12例(24.5%),未缓解9例(18.4%)。末次就诊时VAS评分(3.4±1.6)较首次就诊时(6.0±1.4)显著下降(P<0.01)。有效率影响因素分析显示,疼痛类型对有效率有影响,其中内脏痛患者治疗有效率显著优于混合性疼痛患者(94.1%vs 62.5%,P<0.05),性别、教育水平、疼痛程度和转移情况对治疗有效率无影响。疼痛缓解效果影响因素分析显示,首诊疼痛程度对疼痛缓解效果有影响,中度疼痛患者末次就诊VAS评分显著低于重度疼痛患者(2.8±0.9 vs 4.5±2.1,P<0.01),性别、教育水平、疼痛类型和转移情况对疼痛缓解效果无影响。药物用量影响因素分析显示,49例患者末次就诊时盐酸羟考酮缓释片用量为(89.5±45.6)mg/d,性别、教育水平、疼痛程度、疼痛类型和转移情况对药物用量无影响。呕吐发生率38.8%(19/49),便秘发生率55.1%(27/49),头晕、嗜睡、排尿困难发生率均为2%(1/49),不良反应均可通过调整剂量及对症治疗后逐渐减轻,未出现其他严重不良反应。结论盐酸羟考酮缓释片在中重度成人癌痛门诊治疗中效果显著,安全性良好,且对疼痛程度为中度癌痛患者和疼痛类型为内脏痛患者疼痛控制效果更好,值得进一步应用和推广。

氨酚羟考酮片对开胸术后镇痛疗效的临床对比研究

目的:以盐酸曲马多为对照,观察开胸术后氨酚羟考酮的镇痛疗效及安全性。方法:50例开胸术后患者,随机分为氨酚羟考酮组(n=25)和曲马多组(n=25)。分别服用氨酚羟考酮及盐酸曲马多片进行镇痛治疗。应用视觉模拟评分法(Visual analogue scale,VAS)观察治疗前后疼痛强度(PI)变化、疼痛缓解率及不良反应。结果:服氨酚羟考酮的患者首次服药后30min至1hPI下降明显,组内PI值即可出现显著性统计学差异(P<0.05),服药1d后,即能达到满意稳定的镇痛效果,相较于曲马多组,氨酚羟考酮组的PI值在5d的时间基本能维持在较低的水平上,但在统计学上没有显著差异性。服药5d后,两组疼痛缓解有效率均为100%,但疼痛缓解显效率分别为100%和76%,有显著性统计学差异(P<0.05)。各组间不良反应发生率差异无显著性意义。结论:氨酚羟考酮用于开胸术后镇痛安全有效。