骨伤康复外洗颗粒质量标准研究

目的建立骨伤康复外洗颗粒的质量标准,为骨伤康复外洗颗粒的质量控制提供可行、可靠的分析方法。方法采用薄层色谱法对制剂中的黄柏进行定性鉴别;采用紫外分光光度法对制剂中君药大黄中的大黄总蒽醌进行含量测定。结果在薄层鉴别中,黄柏在供试品色谱中在与对照药材和对照品色谱相应的位置上,显相同颜色的斑点,且薄层色谱斑点清晰,而阴性对照无干扰;在含量测定中,大黄素含量在0.072～0.720mg范围内与吸光度呈良好的线性关系（r=0.9993）,平均加样回收率分别为99.40%,RSD为1.91%（n=5）,并确定本品中每1g含大黄以大黄总蒽醌计不得少于5.0mg。结论本方法专属性强、快速、准确、重现性好,可作为骨伤康复外洗颗粒的质量控制标准。     

癌痛栓质量标准的研究

目的：癌痛栓质量标准的研究。方法：用薄层色谱法对其中的冰片、灵猫香进行了定性鉴别;用薄层分光光度法对延胡索中有效成分延胡索乙素进行了含量测定。结果：本品定性鉴别薄层色谱特征明显,易于区别;本品中延胡索乙素含量测定线性范围为0．5－25μg,平均回收率102．11％,RSD为1．12％。结论：鉴别与含量测定方法简便可靠,可做为该制剂的质量标准。     

薄层色谱法鉴别胃康乐颗粒

目的建立胃康乐颗粒的薄层色谱鉴别方法。方法采用薄层色谱法对处方中的枳壳、延胡索、黄连等进行定性鉴别。结果在薄层色谱图中检出了枳壳、延胡索、黄连等药材的特征斑点。结论该法专属性强、重现性好、可作为该制剂质量控制的参考。     

双金胃疡灵胶囊质量标准的研究

目的:对双金胃疡灵胶囊进行质量标准研究。方法:采用薄层色谱法对制剂中的延胡索、青木香进行定性鉴别;其中延胡索的薄层色谱鉴别采用延胡索乙素为对照品,以正己烷-氯仿-甲醇-二乙胺(10:6:1:0.1)为展开剂;青木香的薄层色谱鉴别采用青木香为对照药材,以苯-甲醇-冰醋酸(5:0.8:0.1)为展开剂。采用高效液相色谱法对延胡索中延胡索乙素进行含量测定,采用YWG-C_(18)(5μm,4.6 mm×250 mm)色谱柱。流动相为:甲醇-水-磷酸盐缓冲液(58:42:1.8),检测波长为283nm,流速1.0 mL·min~(-1)。结果:10批双金胃疡灵胶囊中含延胡索乙素(C_()21H_(25)NO_4)为 0.016％～0.029％。平均加样回收率为98.72％,RSD为1.8％。结论:本法可作为该产品的质量控制方法。     

复方益母草颗粒的薄层色谱鉴别

目的 建立复方益母草颗粒中主要成分的薄层色谱鉴别方法,为研究该复方制剂的质量标准奠定基础.方法 采用薄层色谱分析方法对该制剂中的益母草、黄芪、延胡索等药材进行定性鉴别.结果 各供试品色谱中,在与各自对照品色谱相同的位置上,显相同颜色的斑点,阴性对照无干扰.结论 该鉴别方法专属性强、重现性好、灵敏度高.可作为该复方制剂的质量控制方法之一.关键调:复方益母草颗粒;益母草;黄芪;延胡索;薄层色谱法     

阿昔洛韦胃漂浮片的制备

目的研制阿昔洛韦胃漂浮片。方法采用粉末直接压片法制备阿昔洛韦胃漂浮片,以漂浮性能和阿昔洛韦的释放度为考察指标进行处方筛选。结果以羟丙基甲基纤维素(HPMC K4M)和聚氧乙烯(PEO WSR N-205)为亲水凝胶骨架,十六醇为助漂剂,碳酸氢钠为产气剂,制备了12 h缓释胃漂浮片。该制剂在胃酸中立即起漂,2 h释放30%,6 h释放60%,12 h释放大于90%。结论所制备的阿昔洛韦胃漂浮片具有良好的漂浮性和缓释特性。     

二氢杨梅素胃内漂浮片处方研究

目的为了延长二氢杨梅素在胃内停留的时间,延缓药物的释放,将其制备成胃内漂浮片。方法采用粉末直接压片法制片,运用单因素的平行实验和L9（3^4）正交设计,以起漂时间、漂浮持续时间及释放度为指标选择最佳处方。结果最佳处方：片剂重量为300mg,其他各成分的含量分别为：HPMCK4M75mg,PVPK3040mg,NaHC0340mg,主药80mg,乳糖65mg,该制剂在37℃的人工胃液中立即起漂,12h释放〉90％,持漂时N〉10h。结论制备的胃漂浮片具有优良的漂浮能力和释药行为,可增加二氢杨梅素在胃部的滞留时间,提高药物的稳定性,增强保肝作用。     

安中片质量标准研究

目的:建立安中片的质量标准.方法:采用薄层色谱法对原质量标准中桂枝、延胡索、砂仁进行定性鉴别,采用高效液相色谱法对甘草酸铵进行含量测定.结果:在薄层色谱中可检出桂枝、延胡索的特征斑点;甘草酸单铵盐峰面积与选样量在0.218 2～7.637 0μg范围内线性关系良好,r=0.999 9.结论:所建立的方法稳定可靠,可用于该制剂的质量控制.     

冠脉宁片的质控标准拟定

目的提高冠脉宁片的质量标准,更有效地控制该中成药的质量。方法采用薄层色谱法进行药材鉴别,利用高效液相色谱法测定其中葛根素的含量。结果鉴定处方中的两味药材,并对葛根素的含量测定进行方法学考察。结论该方法适用于冠脉宁片的鉴别和含量测定,能有效地控制成品质量。     

四方胃片质量标准研究

目的:建立四方胃片的质量控制方法。方法:采用薄层色谱法对制剂中的延胡索和浙贝母进行定性鉴别,采用高效液相色谱法测定四方胃片中盐酸小檗碱的含量。结果:定性鉴别专属性强;盐酸小檗碱进样量在0.06～1.8μg范围内与峰面积积分值呈良好线性关系(r=0.9999),平均回收率为97.1%,RSD=1.6%(n=6)。结论:所建标准能有效控制该制剂的质量。     

阿魏酸钠胃内漂浮片的制备及体外释放机制考察

目的优化阿魏酸钠胃内漂浮片的制备工艺,并对其体外释药机理进行研究。方法以HPMC K4M为亲水性凝胶骨架,十六醇为助漂剂,NaHCO3为产气剂,采用星点设计-效应面法对处方进行优化,并通过方程拟合探讨释药机制。结果优化得到最优处方,所制得胃内漂浮片均能在1 min内起漂,持续漂浮10 h。结论采用星点设计-效应面法优化的处方预测性良好,并且所制得的胃内漂浮片具有良好的漂浮和控释能力。     

Optimisation of floating matrix tablets and evaluation of their gastric residence time

The present investigation concerns the development of the floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. The importance of the composition optimisation, the technological process development for the preparation of the floating tablets with a high dose of freely soluble drug and characterisation of those tablets (crushing force, floating properties in vitro and in vivo, drug release) was examined. Tablets containing hydroxypropyl methylcellulose (HPMC), drug and different additives were compressed. The investigation shows that tablet composition and mechanical strength have the greatest influence on the floating properties and drug release. With the incorporation of a gas-generating agent together with microcrystalline cellulose, besides optimum floating (floating lag time, 30 s; duration of floating, >8 h), the drug content was also increased. The drug release from those tablets was sufficiently sustained (more than 8 h) and non-Fickian transport of the drug from tablets was confirmed. Radiological evidence suggests that, that the formulated tablets did not adhere to the stomach mucus and that the mean gastric residence time was prolonged (>4 h).     

格列喹酮片的分剂量评价

目的 评价单面带刻痕的格列喹酮片的分剂量药学特性。方法 分别采用切药器和手工对自研品和参比制剂进行分割,以分割前后质量损失为评价指标,考察自研品和参比制剂的可分割性;取在硬度上限（8 kg）和下限（4 kg）处的自研格列喹酮片分别用切药器分割后,考察分割质量损失;按照《中国药典》2020年版片剂脆碎度检查法研究分割后的片剂脆碎度;参考《欧洲药典》,随机取30片,分割后检测单一半片占半片平均片质量百分比;高效液相色谱法测定格列喹酮整片、半片在pH 8.5磷酸盐缓冲液中的溶出曲线;参照《中国药典》含量均匀度检查法（通则0941）,对切药器分割后的30片自研品进行含量均匀度测定。结果 质量损失结果表明手工分割和切药器分割无显著性差异;硬度上限与下限时片剂分割后的脆碎度和质量损失均符合要求;分割后片剂质量差异、脆碎度和含量均匀度均符合药典要求;自研品与参比制剂的半片溶出行为一致;与整片溶出量相比,分割后的自研品60 min溶出量为51.46%,参比制剂为49.12%。结论 自研品和参比制剂分割后的药学特性相同。     

元胡止痛分散片的制备及质量标准研究

目的:制备元胡止痛分散片并制订制剂的质量标准。方法:用二氧化碳超临界流体萃取法(CO2-SFE)提取元胡和白芷药材的有效成分,加入适当辅料制备元胡止痛分散片;以薄层色谱鉴别元胡和白芷药材,以高效液相色谱法测定有效成分的含量。结果:确立了CO2-SFE提取药材的工艺指标及分散片的制备方法,建立了药材鉴别的薄层色谱条件及延胡素乙素和欧前胡素含量测定的高效液相色谱方法。结论:药材提取方法先进,分散片制备工艺稳定、可控,质量标准可行。     

左卡尼汀胃漂浮缓释片的制备及体外评价

目的:应用Box-behnken效应面法优化左卡尼汀胃漂浮缓释片处方,并评价其体外漂浮和释放特性.方法:以粉末直接压片法制备片剂.采用单因素法筛选出主要影响因素,即硬度、HPMC用量及碳酸氢钠用量,以漂浮性能和不同时间点释药性能为评价指标,通过Boxbehnken设计实验优化处方,对体外释药数据进行方程拟合,并结合扫描电子显微镜对溶出前后片剂表面形态的观察,探讨其释药机理.结果:优选处方为每片含HPMCK100M 29.7％,碳酸氢钠5.0％,十八烷醇15.0％,硬度为4 kg· mm-2.体外释药符合Makoid-Banakar模型,药物的释药机制为骨架溶蚀与药物扩散双重作用.结论:Box-behnken效应面法可用于左卡尼汀胃漂浮缓释片处方优化,且制备工艺简单,优化处方具漂浮缓释作用.     

Design and in vitro testing of a floatable gastroretentive tablet of metformin hydrochloride

Metformin hydrochloride, which is better absorbed in the upper intestine, was formulated as a floating (buoyant) matrix tablet using a gas generating agent (sodium bicarbonate) and a gel forming hydrophilic polymer (hydroxypropyl methylcellulose). The formulation was optimized on the basis of floating ability and in vitro drug release. The resulting formulation produced robust tablets with optimum hardness, consistent weight uniformity and low tablet friability. All tablets but one exhibited satisfactory (gradual and near complete) drug release and buoyancy. In vitro drug release tests of these tablets indicated controlled sustained release of metformin hydrochloride and 96-99% released at the end of 8 h. Two formulations of fabricated tablets containing metformin hydrochloride (500 mg), sodium bicarbonate (75 mg), hydroxypropyl methylcellulose-K 4M (170-180 mg), citric acid (between 15 and 20 mg) and polyvinyl pyrrolidone K90 (32-40 mg) with hardness between 6.8 to 7.5 kg/cm2 showed a floating time of more than 8 h and promising drug release results. The release followed the Higuchi kinetic model, indicating diffusion dominated drug release.     

Floating matrix dosage form for dextromethorphan hydrobromide based on gas forming technique: In vitro and in vivo evaluation in healthy volunteers

The objective of this study was to develop the dextromethorphan hydrobromide sustained-release (DMB-SR) tablets using floating technique to prolong the gastric residence time and compared their pharmacokinetic behavior with conventional sustained release tablets. DMB-SR floating tablets were prepared employing hydroxypropyl methylcellulose (HPMC) as hydrophilic gel material, sodium bicarbonate as gas-generating agent and hexadecanol as floating assistant agent. An orthogonal experiment design method was used to select the optimized formulation. The floating tablets were evaluated for uniformity of weight, hardness, friability, drug content, floating characteristics, in vitro release and in vivo bioavailability. The optimized tablets were prepared with HPMC K4M 25 mg, sodium bicarbonate 20 mg and hexadecanol 18 mg. The prepared tablets could float within 3 min and maintain for more than 24 h. The data of physical parameters were all lie within the limits. Drug release at 12 h was more than 85%. The comparative pharmacokinetic study was performed by administration of the DMB-SR floating tablets and conventional DMB-SR tablets. The area under curve of plasma concentration–time (AUC) of floating tablets was slightly higher than that of reference tablets, T_max was prolonged apparently. The results showed the floating tablets are a feasible approach for the sustained-release preparation of drugs, which have limited absorption sites in the stomach.     

An approach to formulating an oral floating drug delivery system for dexchlorpheniramine maleate using factorial design

The purpose of this research was to formulate and evaluate a floating tablet formulation of dexchlorpheniramine maleate (DCPM) using full factorial design. A 32 factorial design (nine runs) was utilized to optimize the formulation, the contents of hydroxypropyl methyl cellulose (HPMC) (X1) and Carbopol 934P (X2) being taken as independent variables and t50% (Y1), % drug release after 6 h (Y2), % drug release after 12 h (Y3), and floating lag time (FLT) (Y4) as the dependent variables. The tablets showed 99.2635 to 102.4709 of the labeled amount of dexchlorpheniramine maleate indicating uniformity of content. The tablets containing DCPM released 72.28 to 99.461% of drug at the end of 12 h by an in vitro release study. Hardness, friability, floating capacity, weight variation and content uniformity were also examined. In addition,the tablets were evaluated for in vitro release characteristics for 24 h. The optimal batch (F9) was selected by regression analysis and followed Higuchi kinetics. The drug release mechanism was found to be a complex mixture of diffusion, swelling and erosion. The floating tablets of DCPM developed may be used clinically for prolonged drug release for at least 16 hrs, thereby improving bioavailability and patient compliance.     

Formulation and evaluation of famotidine floating tablets

The purpose of this investigation was to prepare a gastroretentive drug delivery system of famotidine. Floating tablets of famotidine were prepared employing two different grades of methocel K100 and methocel K15M by effervescent technique; these grades of methocel were evaluated for their gel forming properties. Sodium bicarbonate was incorporated as a gas-generating agent. The floating tablets were evaluated for uniformity of weight, hardness, friability, drug content, in vitro buoyancy and dissolution studies. The effect of citric acid on drug release profile and floating properties was investigated. The prepared tablets exhibited satisfactory physico-chemical characteristics. All the prepared batches showed good in vitro buoyancy. The tablet swelled radially and axially during in vitro buoyancy studies. It was observed that the tablet remained buoyant for 6-10 hours. Decrease in the citric acid level increased the floating lag time but tablets floated for longer duration. A combination of sodium bicarbonate (130mg) and citric acid (10mg) was found to achieve optimum in vitro buoyancy. The tablets with methocel K100 were found to float for longer duration as compared with formulations containing methocel K15M. The drug release from the tablets was sufficiently sustained and non-Fickian transport of the drug from tablets was confirmed.     

Studies on Formulation and In Vitro Evaluation of Floating Matrix Tablets of Domperidone

Floating matrix tablets of domperidone were developed to prolong gastric residence time and thereby increased drug bioavailability. Domperidone was chosen as a model drug because it is poorly absorbed from the lower gastrointestinal tract. The tablets were prepared by wet granulation technique, using polymers such as hydroxypropylmethylcellulose K4M, carbopol 934P, and sodium alginate, either alone or in combination, and other standard excipients. Tablets were evaluated for physical characteristics viz. hardness, % friability, floating capacity, weight variation and content uniformity. Further, tablets were evaluated for in vitro release characteristics for 24 h. In vitro release mechanism was evaluated by linear regression analysis. Floating matrix tablets based on combination of three polymers namely; hydroxypropylmethylcellulose K4M, carbopol 934P and sodium alginate exhibited desired floating and prolonged drug release for 24 h. Carbopol loading showed negative effect on floating properties but were found helpful to control the release rate of drug.