双氯芬酸钠滴眼液稳定性研究

采用高效液相色谱法测定双氯芬酸钠滴眼液的含量，方法简便，准确，能将药与杂质峰完全分离。应用化学动力学原理以恒温加试验预测双氯芬酸钠滴眼液稳定性及有效期，室温下有效期ｔ＾２５℃０．９约为２．５７年，与留样观察结果相符。     

水合氯醛胶浆剂的制备及稳定性预测

目的：研究水合氯醛胶浆剂的制备方法及稳定性。方法：采用β－环糊精包裹制成水合氯醛的胶浆剂，通过初匀速法测定室温下的有效期。结果：胶浆剂掩盖了水合氯醛的气味，在室温测得有效期为46．63日。结论：确定了制剂的有效期，减少了水合氯醛的刺激性。     

双氯芬酸赖氨酸盐缓释片的初步稳定性研究

目的：在双氯芬酸赖氨酸盐缓释片体外研究的基础上，对其初步稳定性进行了考察，以确定双氯芬酸赖氨酸盐缓释片有效期。方法：考察双氯芬酸赖氨酸盐缓释片在高温光照和高湿条件下的变化，进行加速实验3个月并进行室温留样观察，考察双氯芬酸赖氨盐缓释片的各项指标。结果：双氯芬酸赖氨酸盐缓释片在高温下，释放加快，在高温条件下，易吸湿，在强光下，第10天释放加快，所以双氯芬酸赖氨酸盐缓释片应避免高温高湿，强光保存。结论：暂定有效期2年。     

双氯芬酸赖氨酸盐缓释片的初步稳定性研究

目的 在双氯芬酸赖氨酸盐缓释片体外研究的基础上 ,对其初步稳定性进行了考察 ,以确定双氯芬酸赖氨酸盐缓释片有效期。 方法 考察双氯芬酸赖氨酸盐缓释片在高温光照和高湿条件下的变化 ,进行加速实验 3个月并进行室温留样观察 ,考察双氯芬酸赖氨酸盐缓释片的各项指标。 结果 双氯芬酸赖氨酸盐缓释片在高温下 ,释放加快 :在高湿条件下 ,易吸湿 ;在强光下 ,第 10天释放加快 ,所以双氯芬酸赖氨酸盐缓释片应避免高温 ,高湿 ,强光保存。 结论 暂定有效期 2年     

双氯芬酸赖氨酸盐缓释片的制备及初步稳定性研究

目的 :在双氯芬酸赖氨酸盐缓释片体外研究的基础上 ,对其初步稳定性进行了考察 ,以确定双氯芬酸赖氨酸盐缓释片有效期。方法 :考察双氯芬酸赖氨酸盐缓释片在高温、光照和高湿条件下的变化 ,进行加速实验3mo ,并进行室温留样观察 ,考察双氯芬酸赖氨酸盐缓释片的各项指标。结果 :双氯芬酸赖氨酸盐缓释片在高温下 ,释放加快 ;在高湿条件下 ,由于为亲水凝胶骨架片 ,易吸湿 ;在强光下 ,d10释放加快。所以 ,双氯芬酸赖氨酸盐缓释片应避免高温、高湿、强光保存。结论 :暂定有效期2y。     

双氯芬酸钠胶浆剂家兔直肠给药的药动学特征

目的 研究双氯芬酸钠胶浆剂直肠给药在家兔体内的药动学.方法 24只家兔随机分为2组,每组12只(♀♂各半),分别直肠给予双氯芬酸钠胶浆剂和栓剂(3 mg·ks-1),按试验方案采血,采用HPLC法测定血药浓度.结果 双氯芬酸钠胶浆剂组tmax为12.60 min,ρmax为8.39 mg·L-1(P＜0.001);双氯芬酸钠栓剂组tmax为94.46 min,ρmax为5.62 mg·L-1(P＜0.001).结论 双氯芬酸钠胶浆剂直肠给药后血药峰浓度高,且达峰时间短,优于双氯芬酸钠栓剂直肠给药.     

复乐乳膏的稳定性考察

［摘要］目的研究复乐乳膏的稳定性，并预测其室温贮存有效期。方法以高效液相色谱法测定哈西奈德的含量，采用初匀速法预测其有效期。结果复乐乳膏在室温下密闭保存，有效期为1 a。结论初匀速法预测药品有效期简便、省时、适用于医院制剂稳定性研究。     

双氯芬酸凝胶剂的稳定性研究

以经典恒温加速试验法测试双氯芬酸凝胶剂的稳定性，并考察了光照等的影响，结果表明，该制剂双氯芬酸的降解反应是一级反应，室温贮存有效期长达２６年。     

枸橼酸阿奇霉素注射液稳定性及有效期预测

目的：考察枸橼酸阿奇霉素注射液的稳定性，并预测其室温贮存有效期。方法：用分光光度法测定枸橼酸阿奇霉素注射液含量；用初均速法预测其有效期。结果：本品在室温、高温条件下稳定；在光照下色泽变深，含量及pH有较明显变化。室温贮存有效期为11个月。结论：枸橼酸阿奇霉素注射液应闭光保存。     

美洛西林钠皮试液稳定性考察及有效期预测

目的 考察美洛西林钠皮试液的稳定性及有效贮存期。方法 采用经典恒温试验法及留样观察法考察外观及pH值变化，紫外分光光度法测定其中美洛西林钠含量。结果 皮试液室温（25℃）有效期为20d，夏季（37℃）有效期为6d，与留样观察结果基本一致。结论 美洛西林钠皮试液在室温下20d内稳定。     

Physicochemical characterization and in vivo evaluation of poloxamer-based solid suppository containing diclofenac sodium in rats

To develop a poloxamer-based solid suppository with poloxamer mixtures, the melting point of various formulations composed of poloxamer 124 (P 124) and poloxamer 188 (P 188) were investigated. The dissolution and pharmacokinetic study of diclofenac sodium delivered by the poloxamer-based suppository were performed. Furthermore, the identification test in the rectum and morphology test of rectal tissues were carried out after its rectal administration in rats. The poloxamer mixtures composed of P 124 and P 188 were homogeneous phases. Very small amounts of P 188 affected the melting point of poloxamer mixtures. In particular, the poloxamer mixture [P 124/P 188 (97/3%)] with the melting point of about 32 degrees C was a solid form at room temperature and instantly melted at physiological temperature. Very small amounts of P 188 hardly affected the dissolution rates of diclofenac sodium from the suppository. Dissolution mechanism analysis showed the dissolution of diclofenac sodium was proportional to the time. The poloxamer-based suppository gave significantly higher initial plasma concentrations and faster T(max) of diclofenac sodium than did conventional PEG-based suppository, indicating that the drug from poloxamer-based suppository could be absorbed faster than that from PEG-based one in rats. It retained in the rectum for at least 4 h and could not irritate or damage the rectal tissues of rats. Thus, the poloxamer-based solid suppository with P 124 and P 188 was a mucoadhesive, safe and effective rectal dosage form for diclofenac sodium.     

Effect of sodium chloride on the gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium

Liquid suppository systems composed of poloxamers and bioadhesive polymers were easy to administer to the anus and mucoadhesive to the rectal tissues without leakage after the dose. However, a liquid suppository system containing diclofenac sodium could not be developed using bioadhesive polymers, since the drug was precipitated in this preparation. To develop a liquid suppository system using sodium chloride instead of bioadhesive polymers, the physicochemical properties such as gelation temperature, gel strength and bioadhesive force of various formulations composed of diclofenac sodium, poloxamers and sodium chloride were investigated. The mixtures of P 407 (15%) and P 188 (15-20%) existed as a liquid at room temperature, but gelled at physiological temperature. Diclofenac sodium significantly increased the gelation temperature and weakened the gel strength and bioadhesive force, while sodium chloride did the opposite. Furthermore, the poloxamer gels with less than 1.0% of sodium chloride, in which the drug was not precipitated, were inserted into the rectum of rabbits without difficulty and leakage, and retained in the rectum of rats for at least 6 h. Our results suggested that a thermosensitive liquid suppository system with sodium chloride and poloxamers was a more physically stable and convenient rectal dosage form for diclofenac sodium.     

Single intramuscular injection of diclofenac sodium in febrile pediatric patients

Objectives:There are few reports on the effectiveness and safety of intramuscular (IM) antipyretic injections in pediatric patients. This study reports the efficacy and adverse effects of a single IM injection of diclofenac sodium in pediatric patients.Results:The dose of diclofenac sodium injected was approximately 2 mg/kg. The average time elapsed until antipyresis was 69.1 ± 23.8 min. The average temperature reduction after 1 h was 1.1 ± 0.6°C. The average proportion of temperature change after 1 h was 40.6 ± 22.2%. During the period at the emergency department, there were no reported serious side effects.Conclusions:A single dose of diclofenac sodium provided effective antipyresis in pediatric patients. Serious side effects were not observed.KEY WORDS: Antipyretics, diclofenac sodium, intramuscular, pediatric, side effects     

双氯芬酸钠药物树脂复合物的体外释放特性

目的:制备双氯芬酸钠药物树脂复合物,对其体外释药动力学进行考察。方法:采用不同交联度的离子交换树脂以静态法制备双氯芬酸钠药物树脂复合物并对双氯芬酸钠药物树脂复合物释放的影响因素进行考察。结果:随着树脂交联度的减小,树脂对双氯芬酸钠的载药速率变快,载药量增加。体外释药动力学研究表明,双氯芬酸钠药物树脂的释药速率随着温度的升高和溶出介质中离子强度的增大而加快;而且与树脂本身性质也有关,释药速率随着树脂交联度和粒径的减小而增大;双氯芬酸钠药物树脂的释放为pH依赖型。结论:双氯芬酸钠药物树脂的释药速率与释放温度、溶出介质的离子强度和pH值及树脂交联度和粒径有关。     

综合康复治疗腰椎间盘突出症332例

目的观察综合康复治疗腰椎间盘突出症的疗效。方法腰椎间盘突出症患者332例随机分为观察组和对照组各116例,观察组采用手法牵引加中药热敷等康复治疗方法,对照组采用口服双氯芬酸钠肠溶片治疗。结果治疗15 d后,观察组治愈74例、好转84例、未愈8例,总有效率95.8%。对照组治愈56例、好转50例、未愈60例,总有效率63.9%。两组比较,差异有统计学意义(P<0.05)。结论手法与中草药热敷治疗腰椎间盘突出疗效显著,值得推广。     

A multi-centre comparative study of diclofenac sodium and a dipyrone/spasmolytic combination, and a single-centre comparative study of diclofenac sodium and pethidine in renal colic patients in India

A single-blind, randomized clinical trial was carried out to compare the analgesic effectiveness in patients with renal colic of single intramuscular doses of diclofenac sodium (75 mg) versus a dipyrone (1 g)/spasmolytics combination, and diclofenac sodium (75 mg) versus pethidine (75 mg). The first study involved three centres, the second study one centre. In total, 107 patients were treated with diclofenac sodium, 85 with dipyrone/spasmolytics, and 25 with pethidine. Assessments were made during the first hour after drug administration of the degree of pain relief, the severity of pain using a visual analogue scale, and the duration of analgesia. A global assessment of treatment efficacy was made by the participating physicians at the end of the study period. Patients treated with diclofenac sodium showed an earlier onset of analgesia and a higher incidence of total pain relief compared to those treated with dipyrone/spasmolytics or pethidine. Although the mean duration of analgesia was only slightly greater in the diclofenac sodium group than in the dipyrone/spasmolytics group, a significantly longer effect was seen when diclofenac sodium was compared with pethidine (p less than 0.01). Pain severity assessments revealed that diclofenac sodium caused a significantly greater improvement in pain after 60 minutes compared to dipyrone/spasmolytics (p less than 0.05) and after 30 minutes compared to pethidine (p less than 0.05). Global efficacy assessments by the physician rated diclofenac sodium as significantly superior to dipyrone/spasmolytics (p less than 0.01) and pethidine (p less than 0.001). Moreover, diclofenac sodium was better tolerated than either of the comparative treatments. The results indicate that intramuscular diclofenac sodium is a useful alternative to the drugs commonly used in India in the treatment of renal colic.     

Physicochemical characterization and<Emphasis Type="Italic">in vivo</Emphasis> evaluation of thermosensitive diclofenac liquid suppository

Liquid suppository systems composed of poloxamers and bioadhesive polymers were easy to administer to the anus and mucoadhesive to the rectal tissues without leakage after the dose. However, a liquid suppository containing diclofenac sodium could not be developed using bioadhesive polymers, since the drug was precipitated in this preparation. To develop a liquid suppository system using sodium chloride instead of bioadhesive polymers, the physicochemical properties such as gelation temperature, gel strength and bioadhesive force of various formulations composed of diclofenac sodium, poloxamers and sodium chloride were investigated. Furthermore, the pharmacokinetic study of diclofenac sodium delivered by the liquid suppository was performed. Diclofenac sodium significantly increased the gelation temperature and weakened the gel strength and bioadhesive force, while sodium chloride did the opposite. The liquid suppositories with less than 1.0% of sodium chloride, in which the drug was not precipitated, were inserted into the rectum without difficulty and leakage. Furthermore, liquid suppository gave significantly higher initial plasma concentrations and faster Tmax of diclofenac sodium than did solid suppository, indicating that drug from liquid suppository could be absorbed faster than that from solid one in rats. Our results suggested that a thermosensitive liquid suppository system with sodium chloride and poloxamers was a more physically stable, convenient and effective rectal dosage form for diclofenac sodium.     

传递体作为双氯芬酸钠经皮渗透载体的研究

目的:研制双氯芬酸钠传递体,进行初步临床研究.方法:通过实验筛选该传递体的处方工艺,对其性状、包封率、稳定性、体外透皮及初步临床进行实验.结果:制得的传递体为乳白色混悬液,平均粒径81.50 nm ;平均包封率73.12% ;24 h时药物累积透皮吸收百分率58.62%,药物滞留在皮内的百分率22.61% ;临床应用中实验组与对照组双氯芬酸凝胶的疗效相当,不良反应发生率低.结论:双氯芬酸钠传递体有望成为适于临床给药的一种新剂型.