Background:To assess efficacy and safety of oxcarbazepine (OXC) oral suspension in pediatric patients aged 2-16 years with partial seizures (PS) and/or generalized tonic-clonic seizures (GTCS) in real-world clinical p...Background:To assess efficacy and safety of oxcarbazepine (OXC) oral suspension in pediatric patients aged 2-16 years with partial seizures (PS) and/or generalized tonic-clonic seizures (GTCS) in real-world clinical practice in China.Methods:This 26-week,single arm,multicenter and observational study recruited patients aged 2-16 years with PS or GTCS suitable for OXC oral suspension treatment.Enrolled patients received OXC oral suspension treatment for 26 weeks.Primary endpoints included mean seizure frequency at the end of the treatment and mean seizure frequency reduction at the end of the treatment vs.baseline.Secondary efficacy-related endpoints and safety parameters were also assessed.Results:Nine hundred and eighty-seven pediatric patients were enrolled and 912 (92.4%) completed the study.The mean seizure frequencies at baseline and the end of week 26 were 13.40±64.92 and 1.62±19.47 times/month,respectively.The mean seizure frequency reduction was 10.03±63.67 times/month and the mean seizure frequency reduction percentage was 90.02%±5127.0% (P<0.0001).After 26 weeks of treatment,82.36%,7.24% and 3.86% of the patients became controlled,significantly improved and improved,respectively.Adverse events (AEs) were reported in 74 (7.65%) patients.Rash was the most common AE.The efficacy of OXC was not affected by seizure types,age or gender.Conclusion:This study confirms the efficacy and good safety profile of OXC oral suspension in Chinese pediatric patients aged 2-16 years with PS and/or GTCS.展开更多
Background This study aimed to assess efficacy and safety of oxcarbazepine (OXC) oral suspension in pediatric patients aged 2-5 years with partial seizures (PS) and/or generalized tonic-clonic seizures (GTCS) in real-...Background This study aimed to assess efficacy and safety of oxcarbazepine (OXC) oral suspension in pediatric patients aged 2-5 years with partial seizures (PS) and/or generalized tonic-clonic seizures (GTCS) in real-world clinical practice in China. Methods This 26-week, prospective, single-arm, multicenter, observational study recruited pediatric patients aged 2-5 years with PS or GTCS suitable for OXC oral suspension treatment based on physicians' judgments from 11 medical centers in China. Enrolled subjects started OXC oral suspension treatment as monotherapy or in combination with other antiepileptic drugs. Primary efficacy outcome was the percentage of pediatric subjects achieving ≥ 50% seizure frequency reduction at the end of the 26-week treatment. Secondary efficacy-related parameters and safety parameters such as adverse events (AEs) and serious AEs (SAEs) were also monitored during the 26-week treatment period. Results Six hundred and six pediatric patients were enrolled and 531 (87.6%) completed the study. After 26 weeks of treat-ment, 93.3% subjects achieved ≥ 50% seizure frequency reduction, and 81.8% achieved 100% seizure frequency reduction compared to baseline. Among diff erent seizure types, OXC was eff ective in all subjects with simple PS and in > 90% of subject with other type of seizure present in the study. AEs were observed in 49 (8.1%) subjects. Only three subjects expe-rienced SAE. Rash (n = 18, 2.97%) was the most common AE. Only 17 subjects discontinued due to AEs. Conclusion This study, reporting the real-world data, further confi rms the efficacy and good safety profi le of OXC oral suspension in Chinese pediatric patients aged 2-5 years with PS and/or GTCS.展开更多
目的进行阿奇霉素缓释干混悬剂体外释放度的测定及比格犬体内外相关性评价。方法按2010版中国药典释放度测定法测定阿奇霉素缓释干混悬剂体外释放度,用液相色谱-串联质谱(LC/MS/MS)法测定阿奇霉素在比格犬体内的血药浓度,并用WinNonlin ...目的进行阿奇霉素缓释干混悬剂体外释放度的测定及比格犬体内外相关性评价。方法按2010版中国药典释放度测定法测定阿奇霉素缓释干混悬剂体外释放度,用液相色谱-串联质谱(LC/MS/MS)法测定阿奇霉素在比格犬体内的血药浓度,并用WinNonlin Professional v5.2进行数据处理。结果以体内吸收分数(fa)对体外累积释放度(F)进行线性回归,得方程fa=1.1553F-52.931(r=0.9475)。结论体内吸收分数与体外累积释放度具有良好的相关性,阿奇霉素缓释干混悬剂所采用的释放度测定方法合理,可以较好反映体内吸收情况。展开更多
以黄原胶为增稠剂,采用不同的剪切工艺参数制备康唑类药物(BKZ)的口服混悬液,测定了所得混悬液的溶出度、粒径及黏度,并考察黄原胶及其与果葡糖浆和甘油的组合物的水分散液在溶出介质中的分散状态及溶解速度,以确定剪切工艺对含黄原胶...以黄原胶为增稠剂,采用不同的剪切工艺参数制备康唑类药物(BKZ)的口服混悬液,测定了所得混悬液的溶出度、粒径及黏度,并考察黄原胶及其与果葡糖浆和甘油的组合物的水分散液在溶出介质中的分散状态及溶解速度,以确定剪切工艺对含黄原胶口服混悬液的溶出速度的影响,并探讨其中的机制。结果表明,在BKZ口服混悬液中,黄原胶与果葡糖浆和甘油可形成稳定的凝胶结构,该凝胶结构的稳定性是影响混悬液溶出速度的关键因素。高剪切工艺对凝胶结构有不可逆的破坏作用,从而会加快主药的溶出速度和降低制剂的黏度;且随着剪切速率和剪切时间的增加,主药的溶出速度增加,混悬液的黏度下降并在停止剪切后不会恢复。根据QbD(quality by design)原则,在以黄原胶为增稠剂的口服混悬液的研发过程中,应充分重视黄原胶的流变学性质,以及剪切工艺对关键质量属性(溶出性能)的影响;并通过制剂溶出速度的变化,确定剪切工艺参数的操作范围,优化工艺设计,增强制备过程的工艺稳定性。展开更多
Eosinophilic esophagitis(EoE)is an emerging chronic local immune-mediated disease of the esophagus.Beside proton pump inhibitors and food-restrictiondiets swallowed topical corticosteroids(STC)can be offered as a firs...Eosinophilic esophagitis(EoE)is an emerging chronic local immune-mediated disease of the esophagus.Beside proton pump inhibitors and food-restrictiondiets swallowed topical corticosteroids(STC)can be offered as a first line therapy according to current guidelines.This review describes the background and practical management of STCs in EoE.So far,mainly asthma inhalers containing either budesonide or fluticasone have been administered to the esophagus by swallowing these medications“off label”.Recently esophagus-targeted formulations of topical steroids have been developed showing clinicopathological response rates up to 85%-an orodispersible tablet of budesonide has been approved as the first“in label”medication for EoE in Europe in June 2018.Whereas it was shown that disease remission induction of EoE by STCs is highly effective,there is still a lack of data regarding long-term and maintenance therapy.However,current studies on STC maintenance therapy add some movement into the game.展开更多
提供了一种即溶型阿奇霉素口服混悬液的制备方法。该制剂分为两部分,即阿奇霉素混悬用粉末和空白混悬液,临用前将二者混合,能配制成均匀分散的口服混悬液。采用高效液相色谱法对所得制剂的稳定性进行考察。结果显示,阿奇霉素混悬用粉末...提供了一种即溶型阿奇霉素口服混悬液的制备方法。该制剂分为两部分,即阿奇霉素混悬用粉末和空白混悬液,临用前将二者混合,能配制成均匀分散的口服混悬液。采用高效液相色谱法对所得制剂的稳定性进行考察。结果显示,阿奇霉素混悬用粉末在常温(10~30℃)、常湿(相对湿度45%~75%)下保存12个月,含量没有明显变化;配制的阿奇霉素口服混悬液在振摇后静置1 h期间含量均匀,在2~8℃下保存1个月,含量也没有明显改变。以市售阿奇霉素干混悬剂(希舒美)为对照,比较自制阿奇霉素口服混悬液在p H 6.8磷酸盐缓冲液中的溶出行为。结果显示,自制口服混悬液和市售干混悬剂5 min时的溶出率为(95.3±0.7)%和(87.6±0.6)%。展开更多
文摘Background:To assess efficacy and safety of oxcarbazepine (OXC) oral suspension in pediatric patients aged 2-16 years with partial seizures (PS) and/or generalized tonic-clonic seizures (GTCS) in real-world clinical practice in China.Methods:This 26-week,single arm,multicenter and observational study recruited patients aged 2-16 years with PS or GTCS suitable for OXC oral suspension treatment.Enrolled patients received OXC oral suspension treatment for 26 weeks.Primary endpoints included mean seizure frequency at the end of the treatment and mean seizure frequency reduction at the end of the treatment vs.baseline.Secondary efficacy-related endpoints and safety parameters were also assessed.Results:Nine hundred and eighty-seven pediatric patients were enrolled and 912 (92.4%) completed the study.The mean seizure frequencies at baseline and the end of week 26 were 13.40±64.92 and 1.62±19.47 times/month,respectively.The mean seizure frequency reduction was 10.03±63.67 times/month and the mean seizure frequency reduction percentage was 90.02%±5127.0% (P<0.0001).After 26 weeks of treatment,82.36%,7.24% and 3.86% of the patients became controlled,significantly improved and improved,respectively.Adverse events (AEs) were reported in 74 (7.65%) patients.Rash was the most common AE.The efficacy of OXC was not affected by seizure types,age or gender.Conclusion:This study confirms the efficacy and good safety profile of OXC oral suspension in Chinese pediatric patients aged 2-16 years with PS and/or GTCS.
文摘Background This study aimed to assess efficacy and safety of oxcarbazepine (OXC) oral suspension in pediatric patients aged 2-5 years with partial seizures (PS) and/or generalized tonic-clonic seizures (GTCS) in real-world clinical practice in China. Methods This 26-week, prospective, single-arm, multicenter, observational study recruited pediatric patients aged 2-5 years with PS or GTCS suitable for OXC oral suspension treatment based on physicians' judgments from 11 medical centers in China. Enrolled subjects started OXC oral suspension treatment as monotherapy or in combination with other antiepileptic drugs. Primary efficacy outcome was the percentage of pediatric subjects achieving ≥ 50% seizure frequency reduction at the end of the 26-week treatment. Secondary efficacy-related parameters and safety parameters such as adverse events (AEs) and serious AEs (SAEs) were also monitored during the 26-week treatment period. Results Six hundred and six pediatric patients were enrolled and 531 (87.6%) completed the study. After 26 weeks of treat-ment, 93.3% subjects achieved ≥ 50% seizure frequency reduction, and 81.8% achieved 100% seizure frequency reduction compared to baseline. Among diff erent seizure types, OXC was eff ective in all subjects with simple PS and in > 90% of subject with other type of seizure present in the study. AEs were observed in 49 (8.1%) subjects. Only three subjects expe-rienced SAE. Rash (n = 18, 2.97%) was the most common AE. Only 17 subjects discontinued due to AEs. Conclusion This study, reporting the real-world data, further confi rms the efficacy and good safety profi le of OXC oral suspension in Chinese pediatric patients aged 2-5 years with PS and/or GTCS.
文摘目的进行阿奇霉素缓释干混悬剂体外释放度的测定及比格犬体内外相关性评价。方法按2010版中国药典释放度测定法测定阿奇霉素缓释干混悬剂体外释放度,用液相色谱-串联质谱(LC/MS/MS)法测定阿奇霉素在比格犬体内的血药浓度,并用WinNonlin Professional v5.2进行数据处理。结果以体内吸收分数(fa)对体外累积释放度(F)进行线性回归,得方程fa=1.1553F-52.931(r=0.9475)。结论体内吸收分数与体外累积释放度具有良好的相关性,阿奇霉素缓释干混悬剂所采用的释放度测定方法合理,可以较好反映体内吸收情况。
文摘以黄原胶为增稠剂,采用不同的剪切工艺参数制备康唑类药物(BKZ)的口服混悬液,测定了所得混悬液的溶出度、粒径及黏度,并考察黄原胶及其与果葡糖浆和甘油的组合物的水分散液在溶出介质中的分散状态及溶解速度,以确定剪切工艺对含黄原胶口服混悬液的溶出速度的影响,并探讨其中的机制。结果表明,在BKZ口服混悬液中,黄原胶与果葡糖浆和甘油可形成稳定的凝胶结构,该凝胶结构的稳定性是影响混悬液溶出速度的关键因素。高剪切工艺对凝胶结构有不可逆的破坏作用,从而会加快主药的溶出速度和降低制剂的黏度;且随着剪切速率和剪切时间的增加,主药的溶出速度增加,混悬液的黏度下降并在停止剪切后不会恢复。根据QbD(quality by design)原则,在以黄原胶为增稠剂的口服混悬液的研发过程中,应充分重视黄原胶的流变学性质,以及剪切工艺对关键质量属性(溶出性能)的影响;并通过制剂溶出速度的变化,确定剪切工艺参数的操作范围,优化工艺设计,增强制备过程的工艺稳定性。
文摘Eosinophilic esophagitis(EoE)is an emerging chronic local immune-mediated disease of the esophagus.Beside proton pump inhibitors and food-restrictiondiets swallowed topical corticosteroids(STC)can be offered as a first line therapy according to current guidelines.This review describes the background and practical management of STCs in EoE.So far,mainly asthma inhalers containing either budesonide or fluticasone have been administered to the esophagus by swallowing these medications“off label”.Recently esophagus-targeted formulations of topical steroids have been developed showing clinicopathological response rates up to 85%-an orodispersible tablet of budesonide has been approved as the first“in label”medication for EoE in Europe in June 2018.Whereas it was shown that disease remission induction of EoE by STCs is highly effective,there is still a lack of data regarding long-term and maintenance therapy.However,current studies on STC maintenance therapy add some movement into the game.
文摘提供了一种即溶型阿奇霉素口服混悬液的制备方法。该制剂分为两部分,即阿奇霉素混悬用粉末和空白混悬液,临用前将二者混合,能配制成均匀分散的口服混悬液。采用高效液相色谱法对所得制剂的稳定性进行考察。结果显示,阿奇霉素混悬用粉末在常温(10~30℃)、常湿(相对湿度45%~75%)下保存12个月,含量没有明显变化;配制的阿奇霉素口服混悬液在振摇后静置1 h期间含量均匀,在2~8℃下保存1个月,含量也没有明显改变。以市售阿奇霉素干混悬剂(希舒美)为对照,比较自制阿奇霉素口服混悬液在p H 6.8磷酸盐缓冲液中的溶出行为。结果显示,自制口服混悬液和市售干混悬剂5 min时的溶出率为(95.3±0.7)%和(87.6±0.6)%。
