Preparation and Evaluation of Orodispersible Tablets of Pheniramine Maleate by Effervescent Method

In the present work, orodispersible tablets of pheniramine maleate were designed with a view to enhance patient compliance by effervescent method. In the effervescent method, mixture of sodium bicarbonate and tartaric acid (each of 12% w/w concentration) were used along with super disintegrants, i.e., pregelatinized starch, sodium starch glycolate, croscarmellose sodium and crospovidone. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 60 s), three formulations were tested for in vitro drug release pattern (in pH 6.8 phosphate buffer), short-term stability (at 40±2°/75±5% RH for 3 mo) and drug-excipient interaction (IR spectroscopy). Among three promising formulations, formulation ECP₄ containing 4% w/w crospovidone and mixture of sodium bicarbonate and tartaric acid (each of 12% w/w) emerged as the overall best formulation (t_70% = 1.65 min) based on the in vitro drug release characteristics compared to commercial conventional tablet formulation. Short-term stability studies on the formulations indicated no significant changes in the drug content and in vitro dispersion time (P < 0.05).     

Design and evaluation of fast dissolving tablets of clonazepam

In the present work, fast dissolving tablets of clonazepam were prepared by direct compression method with a view to enhance patient compliance. Three super-disintegrants, viz., crospovidone, croscarmellose sodium and sodium starch glycolate in different ratios with microcrystalline cellulose (Avicel PH-102) along with directly compressible mannitol (Pearlitol SD 200) to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water absorption ratio and in vitro dispersion time. Based on in vitro dispersion time (approximately 13 s), three formulations were tested for the in vitro drug release pattern (in pH 6.8 phosphate buffer), short-term stability (at 40°/75% relative humidity for 6 mo) and drug-excipient interaction (IR spectroscopy). Among the three promising formulations, the formulation prepared by using 10% w/w of crospovidone and 35% w/w of microcrystalline cellulose emerged as the overall best formulation (t(50%) 1.8 min) based on the in vitro drug release characteristics compared to conventional commercial tablet formulation (t(50%) 16.4 min). Short-term stability studies on the formulations indicated that there were no significant changes in drug content and in vitro dispersion time (P<0.05).     

Development of Fast Dispersible Aceclofenac Tablets: Effect of Functionality of Superdisintegrants

Aceclofenac, a non-steroidal antiinflammatory drug, is used for posttraumatic pain and rheumatoid arthritis. Aceclofenac fast-dispersible tablets have been prepared by direct compression method. Effect of superdisintegrants (such as, croscarmellose sodium, sodium starch glycolate and crospovidone) on wetting time, disintegration time, drug content, in vitro release and stability parameters has been studied. Disintegration time and dissolution parameters (t_50% and t_80%) decreased with increase in the level of croscarmellose sodium. Where as, disintegration time and dissolution parameters increased with increase in the level of sodium starch glycolate in tablets. However, the disintegration time values did not reflect in the dissolution parameter values of crospovidone tablets and release was dependent on the aggregate size in the dissolution medium. Stability studies indicated that tablets containing superdisintegrants were sensitive to high humidity conditions. It is concluded that fast-dispersible aceclofenac tablets could be prepared by direct compression using superdisintegrants.     

盐酸非索非那定盐酸伪麻黄碱缓释片处方工艺研究

目的对盐酸非索非那定盐酸伪麻黄碱缓释片的处方及工艺进行研究。方法采用单因素和正交设计法分别考察盐酸非索非那定层和盐酸伪麻黄碱层处方。结果确定盐酸非索非那定层中崩解剂的量,盐酸伪麻黄碱层中羟丙甲纤维素,卡波姆的量为影响片剂质量的关键因素,筛选出最佳处方。结论采用本工艺进行放大生产的产品质量符合要求。     

Formulation Design of Fast Disintegrating Tablets Using Disintegrant Blends

In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by direct compression method. In this method, crospovidone (up to 3% w/w) and croscarmellose sodium (up to 5% w/w) in combination were used as superdisintegrants. Since disintegrants complement each other, accelerating the disintegration process when used together. Estimation of prochlorperazine maleate in the prepared tablet formulations was carried out by extracting the drug with methanol and measuring the absorbance at 254.5nm. The prepared formulations were further evaluated for hardness, friability, drug content uniformity, in vitro dispersion time, wetting time and water absorption ratio. Based on in vitro dispersion time (approximately 12 s), one promising formulation was tested for in vitro drug release pattern in phosphate buffer pH 6.8 and short-term stability (at 40°/70% RH for 3 mo), drug-excipient interaction (IR spectroscopy) were studied. Among the formulations tested, formulation DCPC₄ containing 5% w/w of croscarmellose sodium and 3% w/w of crospovidone as superdisintegrant emerged as the overall best (t_50% 7.0 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t_50% 17.4 min). Short-term stability studies on the promising formulation indicated that there were no significant changes in drug content and in vitro dispersion time (p<0.05).     

HPLC法测定赤牡泡腾片中芍药苷的含量

目的:建立高效液相色谱法测定赤牡泡腾片中芍药苷含量的方法.方法:采用Zobax Eclipse XDB-C18(250 mm×4.6 mm,5μm)色谱柱,乙腈-水(11:89)为流动相,流速:1.0 ml·min-1,柱温:30℃,检测波长230 nm.结果:芍药苷的线性范围为5.06~80.96 μg·ml-1(r=0.999 9).平均回收率为98.30%(RSD=0.91%,n=6).结论:本方法准确、简便、快速,能用于测定赤牡泡腾片中芍药苷的含量.     

Box-Behnken设计-效应面法优选四逆泡腾片干法制粒工艺

目的:优选四逆泡腾片干法制粒工艺。方法:以颗粒得率和颗粒脆碎度为评价指标,以轧轮压力、轧轮转速、浸膏粉含水量为考察因素,采用单因素试验考察各因素对指标的影响程度;采用Box-Behnken设计考察各因素对评价指标总评OD值的影响,并采用效应面法预测、分析、选取最佳工艺。结果:最佳干法制粒工艺为浸膏粉含水量为2.1%,轧轮转速为8.8 Hz,轧轮压力为2.3 MPa。结论:所选工艺稳定、可行、重现性好,可用于四逆泡腾片的制粒。     

咽舒饮泡腾片的质量标准

目的：建立咽舒饮泡腾片的质量标准。方法：采用薄层色谱（TLC）法对其中绿原酸、麦冬进行鉴别;高效液相色谱（HPLC）法测定其中绿原酸的含量。结果：TLC法可以鉴别其中绿原酸、麦冬。绿原酸线性范围为6．48～207．52μg·ml^-1（r=0．9999）,平均回收率为98．9％（RSD=0．74％）。结论：所建立的鉴别方法专属性强,定量方法简便,准确,可用于咽舒饮泡腾片的质量控制。     

莫西沙星阴道泡腾片的毒理学研究

目的研究莫西沙星阴道泡腾片（MVET）对豚鼠的毒性作用。方法对豚鼠分别采用单次及多次阴道给药，进行急性毒性和刺激性试验，观察其全身状态有无异常及阴道组织有无红斑和水肿等。结果豚鼠给药前、后全身状态无明显变化，刺激反应评分为0分。结论MVET对豚鼠安全，未见明显毒性。     

HPLC法测定清开灵泡腾片中栀子苷的含量

目的:建立测定清开灵泡腾片中栀子苷含量的方法。方法:采用高效液相色谱法。色谱柱为Agilent C18(150mm×4.6mm,5μm),流动相为乙腈-水(11:89),检测波长为238nm,流速为1.0mL·min-1。结果:栀子苷进样量在0.03012～0.90360μg之间与峰面积积分值呈良好的线性关系(r=0.9999);平均回收率为97.02%,RSD=1.0%(n=6)。结论:本方法简便、准确、分离效果好,可用于清开灵泡腾片的质量控制。     

法莫替丁泡腾片的制备与质量考察

目的研制法莫替丁泡腾片并建立质量控制方法。方法单因素筛选处方,粉末直接压片制备法莫替丁泡腾片,并对其性状、重量差异、崩解时限、酸度、含量等进行检查。结果确定了泡腾片的处方,即酒石酸-碳酸氢钠=1∶1,崩解剂用量为60%,乳糖为填充剂,润滑剂为PEG6000 3%,硬脂酸镁0.3%,本品在5 min内可完全崩解。结论本品处方合理,制备工艺简单,可进行推广开发。     

硼砂泡腾片的制备与临床应用

目的：将传统的硼砂漱口液改为泡腾片,提高制剂的稳定性。方法：设计制剂处方及其制备工艺,建立质量控制方法。结果：泡腾片在1 min内崩解生成澄明溶液。经加热试验和光加速试验表明稳定性良好。临床应用表明该制剂对慢性咽炎、牙龈炎、扁桃体炎、龋齿有效率均为100.0%,对口腔溃疡有效率75.0%。结论：硼砂泡腾片质量可靠,可以代替硼砂漱口液。     

替硝唑阴道泡腾片生产工艺研究

目的:简化、改进替硝唑阴道泡腾片生产工艺,提高产品质量。方法:采用非水制粒法,酸碱分别制粒、再混和法制备,并按照(中国药典)2000年版稳定性实验指导原则进行稳定性考察。结果:制备工艺稳定,重现性好,质量可控,通过稳定性加速实验后符合《中国药典》2000年版的质量要求。结论:替硝唑阴道泡腾片制备工艺方便、可行。     

In vitro evaluation of domperidone mouth dissolving tablets

In the present research work mouth dissolving tablets of domperidone were developed with superdisintegrants like crospovidone, croscarmellose sodium and sodium starch glycollate in various concentrations like 3%, 4% and 6% w/w by direct compression method. All formulations were evaluated for physical characteristics of compressed tablets such as weight variation, hardness, friability, content uniformity, in vitro disintegration time, wetting time and in vitro dissolution study. Among all, the formulation F3 (containing 6% w/w concentration of crospovidone) was considered to be the best formulation, having disintegration time of 9 s, wetting time of 15 s and in vitro drug release of 99.22% in 15 min.     

HPLC法测定复方氯霉素阴道泡腾片中己烯雌酚的含量

目的:建立高效液相色谱法测定复方氯霉素阴道泡腾片中己烯雌酚的含量。方法:色谱柱为DIONEX C₁₈（250mm×4.6mm,5μm）;流动相为甲醇-水（75:25）;流速为1.0 ml·min^-1;检测波长为239nm;进样量为50μl。结果:己烯雌酚的线性范围为1.1～8.6μg·ml^-1（r=0.9999）;平均回收率为100.8%（RSD=1.9%）。结论:本方法结果准确可靠,可作为复方氯霉素阴道泡腾片中己烯雌酚的含量测定方法。     

塞克硝唑阴道泡腾片的制剂工艺和质量研究

目的 :对塞克硝唑阴道泡腾片的制剂工艺和质量进行研究。方法 :采用紫外分光光度法测定主药塞克硝唑的含量。结果 :线性范围为 5 1 5～ 36 0 5μg/ml,相关系数为 0 9999,线性关系良好 ,平均回收率为 1 0 0 3 % ,RSD为 0 36 % (n =9)。结论 :本制剂设计合理 ,稳定性好 ,可满足临床需要     

绿茶泡腾片的制备及质量评价简

目的优选绿茶泡腾片的处方及制备方法,并对其进行质量评价。方法以泡腾片的溶解性、崩解性、泡腾效果和外观为综合评价指标,对泡腾剂、稀释剂、润滑剂及泡腾片制备工艺进行筛选,并对所制备的泡腾片的质量差异、崩解时限进行评价。结果按所筛选方法制备的泡腾片泡腾迅速,溶液澄清,无沉淀,不挂壁,外观好。结论采用优选出的处方及制备方法制备的绿茶泡腾片质量符合药典规定。     

匹多莫德联合非索非那定治疗慢性特发性荨麻疹50例疗效观察

目的观察非索非那定联合匹多莫德治疗慢性特发性荨麻疹的疗效。方法 100例患者随机分成两组,治疗组50例采用口服盐酸非索非那定片60mg,2次/d,连续治疗4周,同时口服匹多莫德分散片0.8g,1次/d,连续治疗4周;对照组50例单独口服盐酸非索非那定片,方法疗程同治疗组。结果治疗组总有效率为92.00%,对照组为76.00%,两组比较有统计学意义(χ2=5.26,P<0.05)。结论盐酸非索非那定片联合匹多莫德分散片治疗慢性特发性荨麻疹疗效确切。     

塞克硝唑阴道泡腾片的制剂工艺和质量研究

目的：对塞克硝唑阴道泡腾片的制剂工艺和质量进行研究。方法：采用紫外分光光度法测定主药塞克硝唑的含量。结果：线性范围为5.15-36.05μg/ml，相关系数为0.9999。线性关系良好，平均回收率为100.3%,RSD为0.36%(n=9)。结论：本制剂设计合理，稳定性好。可满足临床需要。     

HPLC法测定妇宁阴道泡腾片中苦参碱和氧化苦参碱的总量

目的：建立妇宁阴道泡腾片中苦参碱和氧化苦参碱的总量测定方法。方法：色谱柱：Agilent氨基柱（250mm×4．6mm,5μm）,流动相：乙腈-无水乙醇-3％磷酸溶液（85：7．5：7．5）,流速：1．0ml·min^-1,检测波长：220nm,柱温：30℃,外标法测定。结果：苦参碱、氧化苦参碱与其他杂质之间能够达到很好分离;苦参碱在19．68～157．40μg·ml^-1浓度范围内线性关系良好（r=0．9999）;氧化苦参碱在25．25—202．00μg·ml^-1浓度范围内线性关系良好（r=0．9999）;苦参碱的加样回收率为99．10％,RSD为1．11％;氧化苦参碱加样回收率为99．01％,RSD为1．54％。结论：该法能够同时准确测定两组分的总量,而且简便、准确、快速,可用于批次样品的含量测定及质量控制。