RP-HPLC法测定无极膏中丙酸倍氯米松的含量

目的应用高效液相色谱法测定无极膏中丙酸倍氯米松的含量。方法色谱柱为A lltim a C18(5μm,4.6 mm×150 mm),流动相为甲醇-水(75∶25),检测波长为240 nm,流速为1.0 m l.m in-1。结果丙酸倍氯米松在2.38~23.80 mg.L-1范围内进样量与峰面积呈良好线性关系(r=0.999 9);回收率为99.06%,RSD=0.72%(n=5)。结论该法测定结果准确、灵敏、重现性好。     

Stepping-across controlled asthmatic patients to extrafine beclometasone/formoterol combination

BackgroundAsthma management focuses on achieving and maintaining asthma control. Few studies have assessed whether complete and sustained asthma control is maintained in clinical practice after stepping-across ICS/LABA fixed combinations. Aim of this double-blind, double-dummy, randomized, parallel group, controlled study was to demonstrate clinical equivalence between equipotent doses of extrafine beclometasone/formoterol (BDP/F) pMDI and fluticasone/salmeterol (FP/S) Diskus^® in maintaining lung function and asthma control.MethodsA total of 416 asthmatic patients already controlled with FP/S 500/100 μg/day (Diskus^®, pMDI or separate inhalers) were randomized to a 12-week treatment with extrafine BDP/F 400/24 μg/day pMDI or FP/S 500/100 μg/day Diskus^®. Pre-dose 1-s forced expiratory volume (FEV₁) was the primary efficacy variable; secondary variables included asthma control questionnaire (ACQ-7) and FEV₁0-1 h area under the curve (FEV₁AUC_0–1h). Safety was assessed through adverse events monitoring and vital signs.ResultsAfter 12 weeks of treatment, pre-dose FEV₁ did not differ between treatments (difference between means 0.01 L; 95% CI –0.03–0.06 L) with no significant changes from baseline in both groups (p = 0.726 and p = 0.783 in BDF/F arm and FP/S, respectively). ACQ-7 score showed that control was maintained after stepping-across to extrafine BDP/F. FEV₁AUC_0–1h was significantly higher in BDP/F arm at the beginning (p = 0.004) and at the end of the 12-week treatment period (p = 0.019). No safety issues were reported in both groups.ConclusionsPatients previously controlled with FP/S in any device formulation can effectively step-across to extrafine BDP/F pMDI, maintaining lung function and asthma control with a 5-min onset of action.     

HPLC测定无极膏中丙酸倍氯米松的含量

目的:采用高效液相色谱法(HPLC)测定无极膏中丙酸倍氯米松的含量。方法:色谱柱为Hypersil ODS2(150 mm×4.6 mm.5μm),流动相为甲醇-水(70:30),流速为1.0 ml/min,检测波长为240 nm。结果:丙酸倍氯米松在5.94～13.86μg/ml范围内与峰面积呈良好的线性关系,回归方程为A=29 747.475C-1 300(r=0.999 9),平均回收率为99.87％.CT为0.665％,结论:本法简便、快速、准确,重现性好,可作为无极膏中丙酸倍氯米松的含量测定标准。     

Effect of AeroChamber Plus™ on the lung and systemic bioavailability of beclometasone dipropionate/formoterol pMDI

AIM

To assess the effect of AeroChamber Plus™ on lung deposition and systemic exposure to extra-fine beclometasone dipropionate (BDP)/formoterol (100/6 µg) pMDI (Foster®). The lung deposition of the components of the combination given with the pMDI was also evaluated using the charcoal block technique.

METHODS

Twelve healthy male volunteers received four inhalations of extra-fine BDP/formoterol (100/6 µg) using (i) pMDI alone, (ii) pMDI and AeroChamber Plus™ and (iii) pMDI and charcoal ingestion.

RESULTS

Compared with pMDI alone, use of AeroChamber Plus™ increased the peak plasma concentrations (C_max) of BDP (2822.3 ± 1449.9 vs. 5454.9 ± 3197.1 pg ml⁻¹), its active metabolite beclometasone 17-monopropionate (17-BMP) (771.6 ± 288.7 vs. 1138.9 ± 495.6 pg ml⁻¹) and formoterol (38.4 ± 17.8 vs. 54.7 ± 20.0 pg ml⁻¹). For 17-BMP and formoterol, the AUC(0,30 min), indicative of lung deposition, was increased in the AeroChamber Plus™ group by 41% and 45%, respectively. This increase was mainly observed in subjects with inadequate inhalation technique. However, use of AeroChamber Plus™ did not increase the total systemic exposure to 17-BMP and formoterol. Results after ingestion of charcoal confirmed that AUC(0,30 min) can be taken as an index of lung bioavailability and that more than 30% of the inhaled dose of extra-fine BDP/formoterol 100/6 µg was delivered to the lung using the pMDI alone.

CONCLUSIONS

The use of AeroChamber Plus™ optimizes the delivery of BDP and formoterol to the lung in subjects with inadequate inhalation technique. The total systemic exposure was not increased, supporting the safety of extra-fine BDP/formoterol pMDI with AeroChamber Plus™.     

氟替卡松与培氯米松治疗成人哮喘的疗效比较

目的：比较氟替卡松与培氯米松治疗成人哮喘的疗效。方法：采用随机双盲对照方法，氟替卡松组２１例（男性１１例，女性１０例，年龄４６±ｓ１２ａ），用氟替卡松干粉剂２００μｇ，吸入，ｂｉｄ，６ｗｋ为一个疗程。培氯米松组１９例（男性１２例，女性７例，年龄４３±１１ａ），用培氯米松干粉剂４００μｇ，吸入，ｂｉｄ，６ｗｋ为一个疗程。结果：氟替卡松组和培氯米松组的早晨最大呼气流量（ＰＥＦ）均增加，症状评分及沙丁胺醇气雾剂用量均减少，肺功能明显改善，但２组间比较无明显差异（Ｐ＞０．０５）。治疗前后２组血浆氢化可的松均在正常范围内，２组间比较Ｐ＜０．０５。结论：２组治疗哮喘皆有效。     

无极膏中丙酸倍氯米松薄层鉴别的改进

目的改进无极膏中丙酸倍氯米松薄层鉴别的方法.方法增加软膏的取样量和滤除基质干扰后进行试验.结果提高了样品中主药检出的准确性.结论本改进方法优于原标准.     

超细颗粒丙酸倍氯米松对哮喘患者小气道异常疗效的 Meta 分析

目的:系统评价超细颗粒倍氯米松(BDP)与普通吸入性糖皮质激素(ICS)对哮喘患者小气道异常的疗效,为小气道功能障碍哮喘患者的治疗提供参考。 方法:计算机检索 the Cochrane Library、PubMed、EMBase、Clinical Trials. gov、中国知网、万方数据库、中国生物医学文献数据库(CBM)、维普数据库,收集关于超细颗粒 BDP 与普通 ICS 对哮喘患者小气道影响的随机对照试验(RCT),检索时限均为建库至 2021 年 11 月。 两位研究人员独立筛选文献、提取资料及评估方法学质量后,采用 Cochrane 风险偏倚评估工具,RevMan 5. 4 软件进行 Meta 分析。 结果:最终纳入 12 篇 RCT。 超细颗粒 BDP 与普通 ICS 在改善最大呼气中段流速(MMEF,SMD= 0. 55,95%CI 0. 08~1. 03,P<0. 05)、闭合容量(CC,MD= -0. 33,95%CI -0. 39~ -0. 27,P<0. 01)、小气道阻力(MD= -0. 03,95%CI -0. 05~ -0. 01,P<0. 01)方面比较差异均有统计学意义。 超细颗粒 BDP 与普通 ICS 在剩余 50%肺活量时的用力呼气流量(MEF50 ,MD= 2. 36,95%CI -5. 09~9. 80,P>0. 05)、剩余 25%肺活量时的用力呼气流量(MEF25 ,MD = 4. 81,95%CI -1. 60~11. 22,P>0. 05)、残气量(RV,SMD = -0. 21,95%CI -0. 81 ~ -0. 38,P>0. 05)、残气量/ 肺总量(RV/ TLC,SMD = -0. 36,95%CI -1. 06~0. 33,P>0. 05)、闭合容量(CV,SMD = -1. 14,95%CI -3. 23 ~ 0. 94,P>0. 05)、肺泡一氧化氮(CaNO,MD = -0. 35,95%CI -1. 29~0. 60,P>0. 05)方面比较差异均无统计学意义。 结论:超细颗粒 BDP 与普通 ICS 治疗哮喘患者小气道异常比较,在改善 MMEF、CC 和小气道阻力上具有优势。 受样本量及小气道参数不同的影响,此结论尚需更多高质量研究进一步验证。     

快速高效液相色谱法测定丙酸倍氯米松喷雾液的含量

本文建立了快速高效液相色谱法测定喷雾液中的丙酸倍氯米松含量的方法。以地西泮为内标，甲醇∶水（７０∶３０）为流动相，检测波长为２４０ｎｍ，其浓度在５～３５μｇ／ｍｌ范围内呈良好的线性关系，ｒ＝０．９９９８，平均回收率（ｎ＝６）为１００．２％，ＲＳＤ为１．４６％。方法快速，灵敏，准确，简便。