Study of Sustained Release Phenylpropanolamine Hydrochloride Hydrophilic Matrix Tablets Containing Hydroxypropylmethylcellulose K100M and Carbopol 971P

选用HPMC K100M和卡波普971P为骨架材料，粉末直接压片法制备骨架片，考察释放度，反相高效液相色谱法检测盐酸苯丙醇胺（PPA·HCl）的浓度。释药曲线均符合Higuchi方程（R＞0．98，P＜0．01）。运用正交设计法，以美国市场的PPA·HCl缓释片Acutrim^R为对照，相似因子f2值为指标，筛选获得了最优处方。其工艺重现性合格。研制片在0．1mol·L^-1 HCl,H2O(pH6.5)，磷酸盐缓冲液（PBS）pH5.0,6.8和7.4的介质中，以及在0.1mol·L^-1HCl中释放2h，转移至PBS6．8中释放10h，相对于对照品的f2值为63－74，表明在各介质中两制剂的释药曲线相似。释药影响因素的考察结果表明：在本实验考察的范围内，骨架片在水中的释药速率与HPMC K100M和卡波普971P的用量呈负相关。HPMC K100M和卡波普971P的比例（保持聚合物总用量相同），硬脂酸镁量和骨架片硬度对释药速率无显著性影响。

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?.

Pharmacokinetics of Moclobemide Sustained Release Tablets after Multiple Oral Dose Administration in Healthy Volunteers

To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg oncedaily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide inplasma were determined by reversed-phase high performance liquid chromatography. The partialpharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results Theconcentration-time profile fitted an one-compartment model best. The steady-state pharmacokineticparameters of moclobemide sustained release tablets after multiple oral doses were as follows:C_(max) was (1 950 +- 156) μg· L^(-1), T_(max) was (6.00 +-1.55) h, T_(1/2(kel)) was (3.14 +-0.12)h, AUC_(ss 0-24) was (22 836 +- 1 842) μg·h· L^(-1), MRT was (7.68+-0.36) h, CL/F_((s)) was(20.2+-2.1) L·h^(-1), and V/F_((c)) was (91.4+-9.4) L, respectively. No marked adverse events werenoted during this study. Conclusion The formulation has a sustained-release effect and goodtolerance in the healthy volunteers, which provides useful information for clinical practice.

Preparation and Pharmacokinetic Characterization of Sustained Release Melatonin Tablet

Aim To prepare the sustained release melatonin tablet with HPMC matrix and study its pharmacokinetics and bioavailatility. Methods HPMC was used as matrix to formulate the sustained release tablet. The influences of the size of melatonin, type and amount of HPMC, drug loading, type and amount of additives, and compressing pressure were investigated. Plasma concentration of melatonin in dogs after intravenous injection of two doses and oral administration of sustained release tablets and unmodified release capsules was detected by HPLC using fluorescence detector. Results The drug release from sustained release tablets was influenced by the size of melatonin, type and amount of HPMC, drug loading, and type and amount of additives. Melatonin was found to fit two compartment model after intravenous injection, AUC was proportional to doses, and t(1/2β) of two doses has no significant difference. Relative bioavailability of melatonin sustained release tablet to normal capsule was 83.8%, and absolute bioavailability was 3.75% for sustained release tablet and 4.49% for capsule. Conclusion The melatonin sustained release tablet was well formulated. The absolute bioavilability for oral administration of either sustained release tablet or unmodified release capsule of melatonin was less than 5%. The bioavailability of melatonin sustained release tablet was lower than that of unmodified release capsule, but MRT of sustained release tablet was significantly longer than that of capsule.

HPLC Method for the Determination of Tamsulosin Hydrochloride in Sustained Release Tablets

The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0 5% phosphoric acid solution (20∶30∶50, V/V/V ) at a flow rate of 1 0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0 81-8 10 μg/mL. The mean recovery was 99 8% ( S R=0 7%, n =9), and the precision was found to be 0 45% ( n =9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.

Efficacy of Metoprolol Succinate Sustained Release Tablets Combined with Wenxin Granules in the Treatment of Coronary Heart Disease Arrhythmia

Objective:To explore the effect of metoprolol succinate sustained-release tablets combined with Wenxin Granules in the treatment of coronary heart disease patients with arrhythmia.Methods:The research objects were 50 patients with arrhythmia who were treated in our hospital from September 2019 to September 2020.According to different treatment methods,they were divided into observation group(Wenxin Granule+metoprolol succinate treatment)and control group(metoprolol succinate treatment),25 cases in each group.The curative effects of the two groups were compared.Results:After treatment,there was no significant difference in rnn50,RMSSD,sdnni and SDANN between the two groups(P>0.05).Compared with the control group,the SDNN in the observation group was higher than that in the control group(P<0.05);Before treatment,there was no significant difference in the above indexes between the two groups(P>0.05);The effective rates of the observation group and the control group were 92.00%and 68.00%respectively,and the curative effect of the observation group was higher than that of the control group(P<0.05);There was no significant difference in the incidence of adverse reactions between the two groups(P>0.05).Conclusion:In the treatment of patients with coronary heart disease and arrhythmia,Wenxin Granule Combined with metoprolol succinate sustained-release tablets has significant effect,which can effectively improve the dynamic electrocardiogram indexes of patients,improve the clinical efficacy,and has high safety.

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.

Evaluation of gum mastic(Pistacia lentiscus) as a microencapsulating and matrix forming material for sustained drug release

In this study, a natural gum mastic was evaluated as a microencapsulating and matrixforming material for sustained drug release. Mastic was characterized for its physicochemical properties. Microparticles were prepared by oil-in-oil solvent evaporation method. Matrix tablets were prepared by wet and melt granulation techniques. Diclofenac sodium(DFS) and diltiazem hydrochloride(DLTZ) were used as model drugs. Mastic produced discrete and spherical microspheres with DLTZ and microcapsules with DFS. Particle size and drug loading of microparticles was in the range of 22–62 μm and 50–87%, respectively. Increase in mastic:drug ratio increased microparticle size, improved drug loading and decreased the drug release rate. Microparticles with gum: drug ratio of 2:1 could sustain DLTZ release up to 12 h and released 57% DFS in 12 h. Mastic produced tablets with acceptable pharmacotechnical properties. A 30% w/w of mastic in tablet could sustain DLTZ release for 5 h from wet granulation,and DFS release for 8 h and 11 h from wet and melt granulation, respectively. Results revealed that a natural gum mastic can be used successfully to formulate matrix tablets and microparticles for sustained drug release.

Blue emitting CsPbBr3 perovskite quantum dot inks obtained from sustained release tablets

Blue emitting perovskite ink obtained from cesium lead halide quantum dots bearing chlorine(CsPbClxBr3-x,0<x<3)suffers from the low photoluminescence quantum yield and poor stability.Cesium lead bromine(CsPbBr3)quantum dots free of chlori ne have more stable crystalstructure and fewer crystal defects.Precise control of crystal sizes and surface passivation comporients of CsPbBr3 quantum dots is crucial for the best use of quantum confinement effect and blueshift of emission wavelength to blue region.Here,by polymerizing acrylamide under UV-light irradiation to form polymer gel networks in dimethyl sulfoxide(DMSO)with CsPbBr3 precursors and passivating agents trapped,wesuccessfully prepared novel sustained release tablets with different shapes and sizes.Thanks to the limitation of the polymer networks onsolve nt releasi ng,the resulting CsPbBr3 qua ntum dots have the average size of 1.1±0.2 nm.On the basis of the excelle nt quantum confin eme nteffect and optimized surface passivation,the obtained PQD ink can emit high quality blue light for more than 6 weeks.This work elucidates anew and convenient technique to prepare blue emission perovskite quantum dots ink with high stability and photoluminescence qua ntumyield and provides a great potential technology for the preparation of perovskite optoelectronic devices.

Development of curcumin floating tablets based on low density foam powder

The floating drug delivery system (FDDS) has become increasingly attractive system for gastroretentive dosage forms because it can prolong gastric retention time and improve drug bioavailability (1)Using low density material of polypropylene foam powder is one of the interesting approaches for FDDS development. This floating system has initial low density so it can float immediately without lag time.

宫腔镜手术分别联合屈螺酮炔雌醇片(Ⅱ)与LNG-IUS治疗子宫内膜息肉的疗效分析

目的对比分析宫腔镜下子宫内膜息肉切除术分别联合屈螺酮炔雌醇片(Ⅱ)和左炔诺孕酮宫内缓释系统(levonorgestrel intrauterine sustained release system,LNG-IUS)的有效性及安全性,评估其在预防术后子宫内膜息肉复发的效果,为临床应用提供依据。方法对2018年5月—2020年5月间我院确诊的563例子宫内膜息肉病例进行回顾性研究,全部病例经宫腔镜下手术摘除子宫内膜息肉,包括182例(LNGIUS组)、203例(药物组)和178例(对照组),其中203例药物组接受屈螺酮炔雌醇片(Ⅱ)3个月的疗程。三组分别于术后3、6、12个月进行随访,对比不同干预措施在月经模式、预防息肉复发的疗效及不良反应发生的情况。结果所有患者的手术均顺利完成,术后经病理明确诊断为子宫内膜息肉。术后三组月经模式均较术前改善,经期时长缩短,血红蛋白水平上升,尤其是药物组与LNG-IUS组(P<0.05)。术后3月,三组均无息肉复发;但在术后6月、12月,药物组和LNG-IUS组息肉复发率明显低于对照组(P<0.05)。不良反应方面,药物组阴道点滴出血率低于LNG-IUS组和对照组(P<0.05),全程治疗和随访过程中,均未出现严重不良反应。结论宫腔镜分别联合应用屈螺酮炔雌醇和左炔诺孕酮宫内缓释系统,安全可行,能较好地防止息肉复发,且疗效相近。

阿利沙坦酯联合硝苯地平缓释片对中重度原发性高血压伴心绞痛疗效和安全性的研究

目的观察阿利沙坦酯联合硝苯地平缓释片对中重度原发性高血压伴心绞痛疗效和安全性。方法选取2021年1月至2022年1月佛山市中医院禅城高新区医院老年医学科收治的符合纳入标准的120例中重度原发性高血压伴心绞痛患者,根据随机数表法分为研究组和对照组,每组各60例。对照组使用硝苯地平缓释片Ⅰ治疗,研究组在对照组基础上联合阿利沙坦酯片治疗,疗程为12周。治疗前后测量诊室血压并进行动态血压监测,评估降压效果,计算血压达标率。记录治疗期间两组心绞痛发作持续时间、发作频率、硝酸甘油用量,评估心绞痛改善情况。测量治疗前后患者生命体征,并行血尿常规、血糖、胆固醇、三酰甘油、尿素氮、肌酐、尿酸、血电解质、转氨酶、血清肌酐等实验室检查,记录治疗期间不良反应发生情况。结果治疗后,两组诊室收缩压(SBP)和舒张压(DBP)均较治疗前降低,且研究组低于对照组(P<0.05)。治疗后,两组24 h SBP、24 h DBP、白昼SBP(dSBP)、白昼DBP(dDBP)、夜间SBP(nSBP)和夜间DBP(nDBP)均降低,且研究组低于对照组(P<0.05)。研究组降压总有效率高于对照组(P<0.05)。两组与同组治疗2周后和治疗4周后比较,治疗8周后和治疗12周后两组血压达标率均增加(P<0.05)。治疗后,两组心绞痛发作持续时间、发作频率、硝酸甘油用量均较治疗前减少,且研究组低于对照组(P<0.05)。研究组心绞痛改善总有效率高于对照组(P<0.05)。两组不良反应总发生率比较,差异无统计学意义(P>0.05)。结论阿利沙坦酯联合硝苯地平缓释片治疗中重度原发性高血压伴心绞痛疗效显著,有效降压并维持血压稳定的同时,还可改善心绞痛症状,且安全性较高,具有临床应用价值。

硫酸沙丁胺醇气雾剂与茶碱缓释片治疗急诊老年哮喘的临床效果

目的 探讨硫酸沙丁胺醇气雾剂与茶碱缓释片治疗急诊老年哮喘的临床效果。方法 80例急诊老年哮喘患者,应用计算机随机数字表法将所有患者分成常规组与联合组,每组40例。常规组患者使用硫酸沙丁胺醇气雾剂吸入治疗,联合组患者采用硫酸沙丁胺醇气雾剂吸入治疗联合茶碱缓释片口服治疗。比较两组患者治疗前后第1秒用力呼气容积、炎性因子[白细胞介素(IL)-4、IL-13、γ-干扰素(IFN-γ)]水平以及临床疗效、不良反应发生率。结果 治疗4、8周,两组组患者第1秒用力呼气容积均高于治疗前,联合组第1秒用力呼气容积分别为(2.47±0.21)、(2.62±0.17)L,均高于常规组的(2.03±0.23)、(2.16±0.11)L(P<0.05)。联合组临床总有效率90.00%高于常规组的67.50%(P<0.05)。治疗2、8周,两组患者IL-4、IL-13、IFN-γ水平均低于治疗前,联合组患者IL-4分别为(12.03±1.52)、(10.47±1.61)pg/ml,低于常规组的(15.98±1.47)、(12.69±1.63)pg/ml, IL-13分别为(195.26±21.69)、(182.36±27.98)pg/ml,低于常规组的(213.98±21.66)、(200.48±26.39)pg/ml, IFN-γ分别为(8.36±0.62)、(5.17±0.32)pg/ml,低于常规组的(10.47±0.69)、(7.69±0.36)pg/ml(P<0.05)。联合组不良反应发生率22.50%与常规组的17.50%比较,差异无统计学意义(P>0.05)。结论 硫酸沙丁胺醇气雾剂联合茶碱缓释片用于治疗急诊老年哮喘既有较好的安全性,还能提升抑制炎症反应、提升呼吸功能的作用。

盐酸曲美他嗪缓释片治疗扩张型心肌病的用药效果及用药安全性分析

目的探讨扩张型心肌病用药治疗期间应用盐酸曲美他嗪缓释片的总体效果。方法目的选取2023年3月—2024年3月临朐县人民医院选取扩张型心肌病患者72例为研究对象。以具体治疗方式划分组别,每组均36例。患者均给予常规药物进行干预。参照组在常规治疗基础上,联合应用沙库巴曲缬沙坦钠片。研究组以参照组治疗方案为前提,结合盐酸曲美他嗪缓释片。对两组心功能、心率变异性、治疗效果、不良反应进行评定。结果与参照组相比,研究组左室射血分数较高,左心室舒张末内径、左室收缩末期容积降低,差异有统计学意义(P均<0.05);对比两组不良反应发生率,差异无统计学意义(P>0.05);研究组治疗效果为94.4%(34/36),高于参照组的77.8%(28/36),差异有统计学意义(χ^(2)=4.181,P=0.041);研究组相邻RR间期差值均方根、窦性RR间期总体标准差等心率变异性指标在治疗后高于参照组,差异有统计学意义(P均<0.05)。结论予以患者盐酸曲美他嗪缓释片,具有良好的用药效果,可改善患者心功能,降低心率变异风险,且用药安全性。

使用盐酸羟考酮缓释片治疗晚期癌痛的药学作用探讨

目的探讨使用盐酸羟考酮缓释片治疗晚期癌痛药学作用。方法选取2020年8月—2023年7月如皋博爱医院收治的156例晚期癌痛患者作为研究对象,通过随机数表法,将患者分为观察组和对照组,每组78例。观察组实行盐酸羟考酮缓释片治疗,对照组实行盐酸吗啡缓释片治疗,对比两组疼痛缓解情况、用药相关指标以及不良反应发生情况。结果观察组癌痛缓解有效率与对照组相比,差异无统计学意义(P>0.05)。观察组患者疼痛控制稳定时间,疼痛爆发次数与解救药物使用记录均低于对照组,差异有统计学意义(P均<0.05)。观察组的不良反应发生率(7.69%)低于对照组(19.23%),差异有统计学意义(χ^(2)=4.457,P<0.05)。结论给予晚期癌痛患者盐酸羟考酮缓释片作为镇痛措施,效果显著,且镇痛稳定、起效迅速,不良反应作用少。

基于体外溶出评价方法对硝苯地平缓释片(Ι)一致性评价研究

建立硝苯地平缓释片(Ⅰ)体外溶出评价方法,以原研制剂为参比,评价本公司一致性研究前后的自研制剂(以下简称自制1、自制2),为质量一致性提供依据。选取0.3%吐温80的不同pH值(pH值1.0,pH值4.0,pH值6.8,水)溶液为溶出介质,采用高效液相色谱法考察0.25,0.5,1,2,3,10,12 h的释放度,从而建立体外溶出曲线方法,并进行了方法学验证,最后采用相似因子法(f_(2))将自研制剂与参比进行比较。结果表明,建立的本品体外溶出曲线方法的专属性、线性、精密度、准确度、滤膜吸附、溶液稳定性各项指标均符合要求;自制1与参比溶出行为不一致且f_(2)小于50,调整处方工艺后,自制2与参比体外溶出行为一致,且f_(2)均大于50。本品建立的体外溶出评价方法准确可靠,自制1与参比体外溶出不一致;自制2与参比溶出曲线相似,体外溶出一致。

凉血十味片联合硝苯地平缓释片治疗原发性高血压性视网膜病变临床观察

目的探究凉血十味片联合硝苯地平缓释片治疗原发性高血压性视网膜病变(HR)的疗效及安全性。方法选取HR患者100例,按照随机数字表法分为治疗组(凉血十味片+硝苯地平缓释片)及对照组(硝苯地平缓释片),各50例,对比2组临床疗效。结果治疗组总有效率高于对照组(P<0.05);治疗后,治疗组血压、视力、眼底改变情况、眼底荧光素血管造影情况、中医证候积分均优于对照组(P<0.05)。结论凉血十味片联合硝苯地平缓释片治疗HR疗效确切,能有效提升患者视力,提高患者视觉质量,且无不良反应,安全有效。

达格列净在血糖控制不佳肥胖2型糖尿病患者临床治疗中的效果观察

目的探讨达格列净在血糖控制不佳肥胖2型糖尿病患者临床治疗中的效果。方法选择2022年10月—2023年10月该院收治的104例肥胖2型糖尿病患者为研究对象,按随机数字表法将其分为对照组与观察组,各52例。对照组采用二甲双胍缓释片治疗,观察组采用二甲双胍缓释片联合达格列净治疗。比较两组血糖指标、血脂指标、胰岛功能指标、身体质量指数、腹围指标及不良反应发生情况。结果治疗前,两组血糖指标、血脂指标、胰岛功能指标、身体质量指数及腹围指标比较,组间差异无统计学意义(P>0.05):治疗后,观察组空腹血糖、糖化血红蛋白、总胆固醇、甘油三酯、低密度脂蛋白胆固醇、胰岛素抵抗指数、身体质量指数及腰围指标水平均低于对照组,胰岛β细胞功能指数、空腹胰岛素、空腹C肽水平均高于对照组,组间差异有统计学意义(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)。结论达格列净治疗效果优于利格列汀,其降血糖、血脂及改善胰岛功能、减轻患者体重及缩小腹围的作用更佳,且安全性良好。

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。

Box-Behnken中心组合设计优化甘草酸二铵缓释片的处方

目的考察甘草酸二铵缓释片的制备工艺,并对其体外释药机制进行研究。方法采用羟丙基甲基纤维素(HPM Ck4m)、山菕酸甘油酯为骨架材料,制备甘草酸二铵缓释片;使用Box-Behnken中心组合设计试验方案,借助试验设计软件Design Expert绘制响应面曲线图,筛选适合的处方;并通过方程拟合探讨释药机制。结果按预测处方制备的缓释片,在2、4、8、12 h的体外累积释放率均值分别为32.55%、49.94%、73.88%、97.89%。对其体外释药曲线进行模型拟合,结果表明药物的释放机制为扩散和骨架溶蚀二者的协同作用。结论验证试验证实了预测处方与实际处方之间具有较好的拟合度,Box-Behnken中心组合设计可以应用于甘草酸二铵缓释片处方的筛选。