阿立哌唑口腔崩解片与阿立哌唑片治疗精神分裂症对照研究

目的:比较阿立哌唑口腔崩解片与阿立哌唑片治疗精神分裂症的疗效和安全性.方法:将120例精神分裂症患者随机分为研究组(阿立哌唑口腔崩解片治疗组)60例和对照组(阿立哌唑片治疗组)60例.研究组阿立哌唑口腔崩解片10-30mg/d,对照组阿立哌唑片10-30ms/d,疗程均为8周.在治疗前及治疗后第2、4、8周末使用PANSS评定临床疗效、使用TESS评定药物不良反应,进行比较分析.结果:阿立哌唑口腔崩解片的治疗有效率为68.3%.阿立哌唑片的治疗有效率为70.0%,两组疗效无显著性差异,不良反应无显著性差异(P>0.05).结论:阿立哌唑口腔崩解片与阿立哌唑片治疗精神分裂症均有良好的疗效与耐受性,两药差异不显著.     

口腔崩解片的研究进展

综述了近年来国内外口腔崩解片申报和研究进展，讨论了口腔崩解片所应用的技术如直接压片法、喷雾干燥、冷冻干燥及预处理等方法及辅料的应用情况，指出了该剂型的发展前景和尚待解决的问题．     

米氮平口腔崩解片治疗抑郁症患者的临床研究概述

除了研发新药以外,现有药物新剂型的研发和应用也是治疗抑郁症的新思路。口崩剂型抗抑郁药米氮平口腔崩解片凭借其便于携带、口感良好及易于吞服等优点,作为能较好改善抑郁症患者依从性的一种剂型在临床广泛应用。本文从疾病本身的特点,结合抗抑郁药物的药理特征和不良反应,介绍米氮平口腔崩解片在抑郁症患者的临床研究情况。     

葛根素口腔崩解片的研制

目的：以葛根素为模型药物制备口腔崩解片。方法该研制把崩解时间及沉降容积比为指标,单因素法筛选片剂的处方组成及工艺,并优化制备工艺。结果葛根素口腔崩解片的辅料为甘露醇、明胶、阿司帕坦与薄荷香精,经过冷冻干燥方法制备,口感良好,4s的崩解时间,在4min内体外溶出度达96．46％。结论葛根素口腔崩解片可迅速崩解于口腔内,制备工艺可行。     

氯诺昔康口腔崩解片的制备

目的:对氯诺昔康口腔崩解片的处方及制备工艺进行研究,并评价其质量。方法:以片剂崩解时限、口感为指标,采用正交试验设计优化处方。通过直接压片法制备氯诺昔康口腔崩解片,并测定了其体外崩解时间、溶出度等质量指标。结果:所得片剂完整光洁、口感良好,能在20 s内崩解完全,5 min内体外溶出度超过85%。结论:氯诺昔康口腔崩解片达到了设计要求,方便患者服药。     

刺五加脑灵口腔崩解片的制备

目的：刺五加脑灵口腔崩解片是由我国中药部颁标准第18册收载的刺五加脑灵液改变剂型而得。方法：采用微晶纤维素、甘露醇、低取代羟丙基纤维素为辅料，直接压片法制备，确定了测定口崩时限方法，用高效液相色谱（HPLC）法测定五味子甲素含量。结果：刺五加脑灵口腔崩解片，口崩时限符合要求，崩解时限短，口崩时限小于1min。结论：筛选的处方合理，质量控制用薄层扫描法鉴别和HPLC法测定五味子甲素的含量。测定方法简单、方便、准确。     

Dissolution testing of orally disintegrating tablets

For industrially manufactured pharmaceutical dosage forms, product quality tests and performance tests are required to ascertain the quality of the final product. Current compendial requirements specify a disintegration and/or a dissolution test to check the quality of oral solid dosage forms. These requirements led to a number of compendial monographs for individual products and, at times, the results obtained may not be reflective of the dosage form performance. Although a general product performance test is desirable for orally disintegrating tablets (ODTs), the complexity of the release controlling mechanisms and short time-frame of release make such tests difficult to establish. For conventional oral solid dosage forms (COSDFs), disintegration is often considered to be the prerequisite for subsequent dissolution. Hence, disintegration testing is usually insufficient to judge product performance of COSDFs. Given the very fast disintegration of ODTs, the relationship between disintegration and dissolution is worthy of closer scrutiny. This article reviews the current status of dissolution testing of ODTs to establish the product quality standards. Based on experimental results, it appears that it may be feasible to rely on the dissolution test without a need for disintegration studies for selected ODTs on the market.     

阿司匹林口腔崩解片的研制

目的:研究阿司匹林口腔崩解片的最佳处方和制备工艺.方法:选用微晶纤维素和低取代羟丙基纤维素作为崩解剂,通过湿法制粒压片制备,以体外崩解时间为指标,正交试验优化处方,并测定体外和人体口腔内的崩解时间及体外溶出度等质量评价指标.结果:优选处方的口腔崩解片的体外崩解时间为(9.26±0.06)s,口腔内的崩解时间为(31.82±2.17)s,体外释放非常迅速,2min之内释放76.9%.结论:本研究所得的处方和工艺可以制备性能优良的阿司匹林口腔崩解片.     

利培酮口腔崩解片的研制

目的研究利培酮口腔崩解片的最佳处方和制备工艺。方法选用微晶纤维素和交联羧甲基纤维素钠作为崩解剂,通过湿法制粒压片制备,以体外崩解时间为指标,正交试验优化处方,并测定体外崩解时间及口感等质量评价指标。结果优选处方的口腔崩解片的体外崩解时间为(18.26±0.1)s,口感佳。结论本研究所得的处方可以制备性能优良的利培酮口腔崩解片。     

Bioequivalence of clozapine orally disintegrating 100-mg tablets compared with clozapine solid oral 100-mg tablets after multiple doses in patients with schizophrenia

BACKGROUND: This study compared the bioequivalence of FazaClo (clozapine orally disintegrating tablets) 100 mg to Clozaril (clozapine standard oral tablets) 100 mg after multiple doses in patients with schizophrenia. METHODS: This was a randomized, open-label, multiple-dose study in which patients with schizophrenia received FazaClo or Clozaril 100 mg twice daily for 5 days before crossing over to the alternate therapy. Blood samples were obtained at regular intervals during and after the completion of treatment, and standard pharmacokinetic parameters were calculated. Safety and patient satisfaction with FazaClo were also assessed. RESULTS: Thirty-six patients were enrolled, of whom 33 completed the study and 30 were included in the steady-state analyses. All pharmacokinetic parameters for clozapine and desmethylclozapine (the major metabolite of clozapine) were similar between FazaClo and Clozaril in both the completer and steady-state populations. Geometric mean values for steady-state maximum and minimum concentrations and area under the plasma concentration-time curve for FazaClo were all within 95-105% of those for Clozarilwell within the range considered by the US FDA as acceptable for bioequivalence (80-125%). Patients also expressed a high level of satisfaction with the FazaClo orally disintegrating tablet formulation. CONCLUSIONS: FazaClo produced pharmacokinetic profiles almost identical to those of Clozaril. This should provide clinicians with reassurance that patients who receive FazaClo will achieve plasma drug concentrations similar to those produced by the same daily dose of Clozaril, and that no cross-titration is necessary when switching from one of these clozapine formulations to the other.     

盐酸曲马多口腔崩解片的研制

目的：利用固体分散体技术，制备盐酸曲马多口腔崩解片。方法：以水不溶性材料为载体，用溶剂挥发法制备盐酸曲马多固体分散体，采用粉末直接压片法制备口腔崩解片。结果：以水不溶性材料作载体制得的盐酸曲马多口腔崩解片在体外崩解时间不超过40s，在水中的体外溶出度试验表明药物在10min内完全溶出。结论：该口腔崩解片工艺简单，适合于工业大生产。     

盐酸左旋沙丁胺醇口腔速崩片的研制

目的:研制盐酸左旋沙丁胺醇口腔速崩片。方法:采用正交设计法对盐酸左旋沙丁胺醇口腔速崩片处方进行筛选。结果:确定最佳处方为:微晶纤维素和低取代羟丙甲纤维素最佳配比为4:1的混合物用量为40%,交联聚乙烯吡咯烷酮用量10%,阿斯巴甜用量4%,柠檬酸用量6%。结论:盐酸左旋沙丁胺醇口腔速崩片能快速崩解,且释放迅速,口感舒适。     

头孢克肟口崩片在健康人体内的相对生物利用度研究

目的研究头孢克肟口崩片与胶囊在中国健康成年男性志愿者体内的相对生物利用度,评价两者的生物等效性。方法采用随机、开放、双周期交叉试验设计,20名男性健康受试者分别单剂量口服试验制剂头孢克肟口崩片200 mg或参比制剂胶囊200 mg。采用HPLC-UV法测定给药后不同时间采集的血样中头孢克肟的血药浓度。结果受试者单次口服200 mg头孢克肟后,头孢克肟口崩片与胶囊的Cmax分别为（2.922±1.161）、（2.725±1.042）mg.L-1 tmax分别为（3.42±0.94）、（3.50±0.61）h AUC0~t分别为（21.32±9.87）、（19.54±9.51）mg.h.L-1 t1/2分别为（3.68±1.69）、（3.86±1.73）h。方差分析结果表明2种制剂的参数之间没有显著性差异,头孢克肟口崩片与胶囊的相对生物利用度为（110.2%±12.7%）。结论受试制剂头孢克肟口崩片与参比制剂头孢克肟胶囊为生物等效制剂。     

多潘立酮口腔崩解片的人体生物等效性

目的研究多潘立酮口腔崩解片与普通片口服给药后的人体药动学及相对生物利用度。方法采用2制剂双周期交叉试验设计,22名健康男性受试者分别单剂量口服(10mg)2种制剂,采用高效液相色谱-串联质谱法测定血浆药物浓度。DAS程序进行药动学参数计算及生物等效性评价。结果口腔崩解片与普通片的主要药动学参数:c_(max)分别为(6.2±s 2.0)和(6.5±2.9)μg·L~(-1);t_(max)分别为(0.67±0.18)和(0.8±0.4)h;A UC_(0-24h)分别为(20±9)和(21±9)μg·h·L~(-1);AUC_(0-∞)分别为(24±10)和(24±10)μg·h·L~(-1);t_(1/2)分别为(6±3)和(5.9±2.7)h。2剂型的AUC_(0-24h),AUC_(0-∞)和c_(max)对数转换后进行方差分析和双单侧t检验,结果表明2制剂生物等效,口腔崩解片的相对生物利用度为(102±34)%。结论口腔崩解片与普通片生物等效。     

盐酸昂丹司琼口腔崩解片的研制

OBJECTIVETo develop the optimal formula and preparation for ondansetron hydrochloride orally disintegrating tablets. METHODMicrocrystaline cellulose and low-substituted hydroxypropylcellulose are employed as disintegrants. The tablets are prepared by wet     

盐酸异丙嗪口崩片的制备

目的 制备盐酸异丙嗪口崩片并评价其质量.方法 以片剂崩解时限为指标,采用正交试验筛选盐酸异丙嗪口腔崩解片的处方,同时考虑其口感,确定最优处方.通过粉末直接压片法制备,并测定体外崩解时限及溶出度等质量评价指标.结果 优选处方的体外崩解时限为28 s,口腔崩解时间为26 s,3 min的体外溶出度可达85％以上.结论 该处方和工艺可制备质量优良的盐酸异丙嗪口腔崩解片,方便患者服用.     

盐酸托烷司琼口腔崩解片的制备

目的 制备并评价盐酸托烷司琼口腔崩解片.方法 选择辅料,以口腔中崩解时间为考察指标,综合运用效应面图和等高线图对口腔崩解片处方进行优化,直接压片法压片后,考察盐酸托烷司琼口腔崩解片的溶出度.结果 所用处方为5 mg盐酸托烷司琼、78 mg微晶纤维素、95 mg甘露醇、20 mg交联羧甲基纤维素钠、1.6 mg草莓香精、0.4 mg硬脂酸镁.口腔中崩解时间为22.8 s,溶出度为97.4%.结论 采用直接压片法制备的盐酸托烷司琼口腔崩解片崩解时间短、溶出速度快.     

利培酮口腔崩解片治疗首发精神分裂症的临床疗效

目的探讨利培酮口腔崩解片治疗首发精神分裂症的效果与不良反应。方法将首发精神分裂症患者60例随机分治疗组和对照组,每组30例,分别给予利培酮口腔崩解片（商品名：可同）和利培酮片（商品名：维思通）进行临床对比研究,疗程均为8周。于治疗前及治疗第2、4、8周末采用阳性与阴性症状量表评价临床疗效、副反应量表评价不良反应。结果2组PANSS评分治疗前后均有显著下降,可同治疗组有效率为83.3％,维思通治疗有效率为80.0％,2组比较疗效差异无统计学意义。2组不良反应相似,程度较轻,以锥体外系反应为主,差异无统计学意义。结论利培酮口腔崩解片治疗精神分裂症疗效肯定,不良反应少,依从性好。     

盐酸氨溴索口腔崩解片的研制

目的:设计制备氨溴索口腔崩解片.方法:采用正交设计,根据口腔崩解片的特点选用不同辅料,考察各处方制备崩解片的溶出度和崩解时限.结果:最佳处方为:甘露醇10克,微晶纤维素 30 g,羟丙纤维素 8 g 和碳酸氢钠 1 g.结论:制备的氨溴索口腔崩解片崩解时限符合规定,口感良好,溶出速度明显优于普通片.     

多潘立酮口腔崩解片在健康人体的生物等效性

目的观察多潘立酮口腔崩解片(胃动力药)在健康人体的生物等效性。方法22名健康受试者随机交叉单剂口服多潘立酮口腔崩解片剂及多潘立酮片剂后,用HPLC法测定多潘立酮血药浓度。结果2种制剂的Cmax分别为(40.43±12.89),(42.31±20.32)μg·mL-1;tmax分别为(0.84±0.29),(0.91±0.48)h;t1/2(ke)分别为(11.23±5.06),(10.13±4.02)h;AUC0-tn分别为(187.61±81.20),(189.07±97.69)μg·h·mL-1;AUC0-∞分别为(220.18±106.93)和(215.57±102.13)μg·h·mL-1;F0-tn、F0-∞分别为(102.61±16.41)%和(101.96±16.06)%。结论试验制剂和参比制剂具有生物等效性。