塞克硝唑栓的研制和质量控制

目的 建立塞克硝唑栓的制备方法及质量控制标准.方法筛选基质,确定栓剂中的主要成分和基质的组成与比例,并采用高效液相色谱法测定栓剂中塞克硝唑的含量.结果以塞克硝唑为主药,使用水溶性基质制备栓剂;塞克硝唑浓度在0.1～60μg·mL-1内呈良好的线性关系(r=0.999 9),平均回收率为98.93%,RSD为1.7%.结论 该制剂制备工艺简单,质量稳定质量控制方法简便、准确、精密度好.     

复方奥硝唑泡腾栓的制备与质量控制

目的 制备复方奥硝唑泡腾栓并建立其质量控制方法. 方法 以奥硝唑,硝酸咪康唑为主药制成泡腾栓,采用高效液相色谱法测定栓剂中奥硝唑及硝酸咪康唑的含量,并考查该制剂稳定性. 结果 制剂稳定性较好. 含量测定方法 准确,奥硝唑及硝酸咪康唑均在40~200 μg.mL^-1浓度范围内线性关系良好,平均回收率分别为100.09%(RSD=0.15%),100.02%(RSD=0.35%). 结论 复方奥硝唑泡腾栓处方及制备工艺合理,质量稳定可控.     

反相高效液相色谱法测定水溶性奥硝唑栓含量

目的建立反相高效液相色谱法测定栓剂中奥硝唑含量的方法。方法色谱柱为Zobarx C18柱,流动相为乙腈-0.1%磷酸(30∶70),流速为1 mL.min-1,检测波长为305 nm。结果奥硝唑在43~430μg.mL-1浓度范围内线性关系良好(r=0.999 6),平均回收率(99.65±1.20)%。结论该方法操作简便,结果准确,可用于奥硝唑栓的质量控制。     

紫外分光光度法测定奥硝唑栓的含量

目的建立奥硝唑栓剂中奥硝唑的含量测定方法。 方法采用紫外分光光度法，样品不经分离直接测定奥硝唑栓剂中奥硝唑的含量，检测波长为312 nm。结果奥硝唑浓度为4.0～20.0 μg·mL-1时，线性关系良好，线性回归方程为A＝0.039 89C＋0.009 593，r＝0.999 9，平均回收率为100.23%，RSD＝0.90%。结论该法简便、快速、准确，可作为奥硝唑栓剂的质量控制方法。     

奥硝唑含漱液的制备及质量控制

目的制备奥硝唑含漱液并建立其含量测定方法。方法以高效液相色谱法测定制剂中奥硝唑的含量。结果奥硝唑在20~200μg.mL-1峰面积与浓度呈良好线性关系,r=0.999 9,平均回收率为100.13%,RSD为0.31%。结论本制剂制备和含量测定方法简便、快速、准确、质量可控。     

复方奥硝唑口腔溃疡涂膜的制备及质量控制

目的制备复方奥硝唑口腔溃疡涂膜并建立高效液相色谱法测定其中奥硝唑的含量.方法采用正交试验设计法优选奥硝唑口腔溃疡涂膜的基质组成及制备工艺.HPLC色谱条件色谱柱ZORBAX SB-C18(150 mm×4.6 mm),流动相为甲醇-水(5050),检测波长310 nm,流速0.8 mL·min-1,柱温40℃.结果最优的基质组成为壳聚糖1.8%,明胶1%,甘油15%.HPLC法中奥硝唑在40～200 mg·L-1范围内浓度与峰面积线性关系良好,r=0.999 8,加样回收率为99.54%,RSD为0.49%.结论制备复方奥硝唑口腔溃疡涂膜可用高效液相色谱法对主药奥硝唑进行质量控制,方法简便、快速、灵敏、可靠.     

奥硝唑凝胶剂的制备及质量控制

目的:制备奥硝唑凝胶剂并建立其质量控制方法.方法:以卡波姆-940为基质制备奥硝唑凝胶剂,采用一阶导数光谱法测定凝胶剂中奥硝唑的含量.结果:奥硝唑在8～80μg·ml-1范围内与峰谷间振幅值(D)呈良好的线性关系,回归方程为:D=1.33×10-3C 1.44×10-3,r=0.999 9(n=3),平均回收率为100.71%,RSD为0.89%(n=7).结论:该制剂制备工艺简单,性质稳定,质量可控.     

紫外分光光度法测定奥硝唑氯化钠注射液中奥硝唑含量

目的:建立奥硝唑氯化钠注射液中奥硝唑的含量测定方法.方法:采用紫外分光光度法,以318 m为测定波长.结果:奥硝唑在5.62～16.86mg·L-1浓度范围内呈现良好线性关系,r=0.999 9,平均回收率为100.44%,RSD为0.59%(n=5).结论:本法操作简便准确,可作为该制剂的质量控制方法.     

复方奥硝唑乳剂的制备与质量控制

目的探讨复方奥硝唑乳剂的制备方法并对其进行质量控制。方法羧甲基纤维素钠加适量注射用水，溶胀完全，加入亚硫酸氢钠，研磨混匀，再依次加入鱼肝油、吐温-80、奥硝唑、酮康唑研磨使混匀，最后加入水继续研磨制成复方奥硝唑乳剂，并采用双波长-系数倍率法测定其含量。结果奥硝唑的浓度在7.04～14.08 μg·mL^-1范围内与△A线性关系良好，r＝0.999 5(n＝7)，平均回收率100.10%，RSD＝0.58%(n＝4)。酮康唑的浓度在9.984～19.968 μg·mL^-1范围内与△A线性关系良好，r＝0.999 9(n＝7)，平均回收率100.10%，RSD＝0.90%(n＝4)。结论该制剂稳定、制备简便，质控方法准确。     

复方奥硝唑含漱液的制备及质量控制

目的 :制备复方奥硝唑含漱液 ,并建立其含量测定方法。方法 :以紫外分光光度法测定制剂中奥硝唑含量 ,以双波长等吸收点法测定醋酸氯己定含量。结果 :奥硝唑检测浓度在5 5～16 6μg/ml范围内线性关系良好 ,醋酸氯己定检测浓度在5 6～16 8μg/ml范围内线性关系良好 ,2组分的平均回收率分别为100 23 %、99 77 % ,相对标准差分别为0 47 %、0 31 %。结论 :本制剂制备和含量测定方法简便、快速、准确 ,质量可控。     

氟甲栓的制备及质量控制

目的:制备氟甲栓并建立其质量控制方法。方法:以聚乙二醇为基质,甲硝唑、诺氟沙星为主药制备栓剂;采用高效液相色谱法同时测定其中主药的含量;并考察该制剂室温放置12个月的稳定性。结果:所制制剂为乳白色至淡黄色的圆锥形栓,鉴别、检查均符合2005年版《中国药典》中的相关规定;甲硝唑、诺氟沙星检测浓度的线性范围分别为8.32～41.60、2.08～10.40μg·mL-(1r=0.9999),平均回收率分别为98.23%、98.69%,日内、日间平均RSD分别为0.70%、0.62%,0.76%、0.65%;制剂12个月时各项指标未见明显变化。结论:该制剂制备工艺简便可行,质量稳定可控。     

水溶性基质奥硝唑栓的制备及质量控制

目的建立奥硝唑栓剂的制备方法及质量控制标准。方法以PEG400,PEG6000为基质,熔融法制备奥硝唑栓剂,采用紫外分光光度法测定其含量。结果本品为淡黄色鱼雷型栓剂;重量差异及熔变时限符合药典要求;含量测定方法方便、准确、精密度好。结论所得制剂工艺简便易行,质量可控,有望用于临床。     

替硝唑泡腾栓基质的筛选

目的：控制替硝唑泡腾栓的质量,方法：以碳酸氢钠和柠檬酸为泡腾剂,分别以聚乙二醇（PEG）,半合成脂肪酸酯,乌桕脂为基质,制备替硝唑泡腾栓,并进行体外深出度测定,结果：3种泡腾栓的释药性差 有显著性,以聚乙二醇为基质泡腾栓最好,结论：以聚乙二醇为替硝唑泡腾栓的基质较合适。     

奥硝唑栓的制备及临床应用

目的建立奥硝唑栓栓剂的制备方法及质量控制标准。方法以PEG400,PEG6000为基质,用熔融法制备,采用紫外分光光度法测定其含量,并对其进行临床疗效观察。结果含量测定方法简便,质量可控,稳定性好,疗效满意。结论所得制剂工艺简便易行,值得临床推广应用。     

奥硝唑生物粘附性缓释栓的制备及质量控制

目的：制备治疗滴虫感染的奥硝唑生物粘附性缓释栓，并制定其质量控制标准。方法：以PEG—600，PEG—6000，CMC—Na为栓剂基质，奥硝唑为主药制成栓剂，并用紫外分光光度法测定主药的含量。结果：低、中、高3种浓度的平均回收率分别为99.92％，98．76％，100．61％，RSD分别为0．08％，1．24％，0．61％。结论：奥硝唑生物粘附性缓释栓制备工艺简单，栓剂成型性好，含量剩定方法可行，结果可靠。     

Rectal absorption of omeprazole from suppositories in rabbits

Rectal absorption of omeprazole, a proton pump inhibitor, from suppositories was studied in rabbits. The suppositories were prepared by the conventional melting method with two types of bases, water-soluble polyethylene glycol (PEG) 4000 and oil-soluble Witepsol H15 bases, and administered intrarectally (ir) to rabbits at a dose of 10 mg omeprazole/kg. The plasma omeprazole concentration-time profiles of the two suppositories were compared with those following intravenous (iv) administration of the same dose. There were no significant differences between the two suppositories in bioavailabilities and peak plasma concentrations (C_max). Bioavailabilities and C_max of PEG- and Witepsol suppositories were 30.3 and 33.9%, and 7.0 and 5.6 μg/ml, respectively. However, PEG suppository showed significantly (P<0.05) shorter time to reach peak plasma concentration (T_max), mean absorption time (MAT) and mean residence time in the plasma (MRT) than Witepsol suppository. The T_max MRT and MAT were 25.0, 83.0 and 38.5 min for PEG suppository, but were 90.0, 122.5 and 78.0 min for Witepsol suppository, respectively. These differences between the two suppositories could be explained by the difference in the in vitro dissolution rates between the suppositories. The dissolution of omeprazole from PEG suppository was reportedly much faster than that from Witepsol suppository. It suggests that plasma profiles of omeprazole, especially C_max, MAT and MRT, could be controlled by modifying thein vitro dissolution rate of the drug from the suppositories. Above results suggest that rectal suppository is worth developing as an alternative dosage form of omeprazole to the conventional oral preparations which need sophisticated treatments, such as enteric coating, to prevent acid degradation of the drug in the stomach fluid.     

The Release of Isoconazole Nitrate from Different Suppository Bases: In-vivo Release of Drug Labelled with 99mTc in Rabbits

The influence of the suppository bases on the in-vivo release of ^99mTc-labelled isoconazole nitrate was investigated. The single-dose vaginal suppository formulations for local treatment of vaginitis were prepared by a fusion method using polyethylene glycols, Witepsol H15, Novata BD and Cremao. Prepared vaginal suppositories containing solid-labelled substance were applied to the vagina of rabbits and at 0, 2 and 24 h after administration, the amounts of radioactivity in the vagina were detected by the SPECT Gamma Camera and the release rates of the drug were calculated. The percent released was found to be in the following order; polyethylene glycol (PEG) 6000 > PEG 4000 > Witepsol > PEG 1500 > Novata BD > Cremao. The results obtained in both in-vitro and in-vivo studies indicated that the vaginal suppository of isoconazole nitrate prepared with polyethylene glycols could confidently be used in therapy.     

醋氯芬酸栓的制备及质量控制

目的:制备醋氯芬酸栓并建立其质量控制方法。方法:以醋氯芬酸为主药,半合成脂肪酸甘油酯为基质制备栓剂;采用高效液相色谱法测定其中主药的含量,同时经强光、加速、长期试验考察制剂稳定性。结果:所制制剂为类白色至淡黄色栓,鉴别、检查项均符合相关规定。醋氯芬酸检测浓度的线性范围为5.08～30.48μg·mL-1(r=0.9998),平均回收率为99.3%,日内平均RSD=1.23%,日间平均RSD=1.88%。稳定性试验考察显示各项指标无变化。结论:该制剂制备工艺简单可行,质量稳定可控。     

Preparation and investigation of acetyl salicylic acid-caffeine complex for rectal administration

An acetyl salicylic acid-caffeine complex was prepared and evaluated for the potential use in rectal administration. The results revealed the formation of a complex between acetyl salicylic acid and caffeine in a 1:1 molar ratio by a charge transfer mechanism. The effects of acetyl salicylic acid and complex on the rectal tissues showed destruction in the mucosal epithelium in case of acetyl salicylic acid; however, no change in the rectal tissues was noticed upon the administration of the complex. The effect of suppository bases on the release of the complex was studied using Witepsol H15 as fatty base and polyethylene glycols (PEG) 1000 and 4000 as a water soluble suppository base. The release profiles of acetyl salicylic acid and the complex were faster from PEG than from that of Witepsol H15. The percent release for the complex and acetyl salicylic acid from PEG base were 45.8, and 34.9%, respectively. However, it was 8.7 and 7.8%, respectively, from Witepsol H15 fatty base. The release kinetic was found to follow the non-Fickian diffusion model for complex from the suppository bases. It was concluded that acetyl salicylic acid caffeine complex can be used safely for rectal administration.     

茶碱脉冲栓剂的制备及体外释药性考察

目的:制备茶碱脉冲栓剂并评价其体外释药性质。方法:以处方基质中泊洛沙姆、羧甲基纤维素钠(CMC-Na)、聚乙二醇6000(PEG6000)、PEG400的不同用量为因素,以释药时滞及累积释药率为指标采用单因素法筛选栓剂处方组成,并考察填充不同内容物(茶碱原料、茶碱-PVP物理混合物和茶碱-PVP固体分散体)的栓剂的累积释药率。结果:较优基质处方组成为70%泊洛沙姆、6%CMC-Na、12%PEG6000、12%PEG400,其体外释药时滞为4h,90min累积释药率为85%以上;3种填充不同内容物的栓剂累积释药率分别为58.8%、65.8%、91%。结论:所制茶碱脉冲栓剂具有较好的脉冲释药作用。