An alkylpolyglucoside surfactant as a prospective pharmaceutical excipient for topical formulations: The influence of oil polarity on the colloidal structure and hydrocortisone in vitro/in vivo permeation

There is a growing need for research into new skin- and environment-friendly surfactants. This paper focuses on a natural surfactant of an alkylpolyglucoside type, which can form both thermotropic and lyotropic liquid-crystalline phases. The aim of this study was to relate some physicochemical properties (characterised by polarisation and transmission electron microscopy, thermal analysis and rheology) of the three formulations based on cetearyl glucoside and cetearyl alcohol, to the results of in vitro and in vivo bioavailability of hydrocortisone (HC). The three formulations contained oils of different polarity (medium chain triglycerides: MG, isopropyl myristate: IPM and light liquid paraffin: LP), respectively. In vitro permeation was followed through the artificial skin constructs (ASC), while the parameters measured in vivo were erythema index: EI (using instrumental human skin blanching assay), transepidermal water loss (TEWL) and stratum corneum hydration (SCH). The vehicles based on cetearyl glucoside and cetearyl alcohol showed a complex colloidal structure of lamellar liquid-crystalline and lamellar gel-crystalline type, depending on oil polarity. Rheological profile of the vehicle was directly related to the in vitro profile of the HC permeation. In vivo results suggested that the vehicle with MG retarded the HC permeation, whereas less polar IPM and non-polar LP enhanced it. It is suggested that the enhancement is achieved either by a direct interaction with lipid lamellae of the SC or indirectly by improving skin hydration.

There were no adverse effects during in vivo study, which indicates a good safety profile of this alkylpolyglucoside surfactant.     

反相高效液相色谱法测定莪术油注射液中莪术醇和牛儿酮的含量

目的利用反相高效液相色谱法同时测定莪术油注射液中莪术醇和牛儿酮含量。方法采用AgilentTC ODS色谱柱(4.6 mm×15 cm,5μm),流动相A:乙腈-甲醇-水-磷酸(550∶225∶225∶1);流动相B:甲醇,梯度洗脱,流速1.0 mL/min,柱温:35℃,检测波长:210 nm。结果在该条件下,莪术醇、牛儿酮浓度分别在0.940 6~94.06μg/mL和1.333~133.2μg/mL范围内与峰面积呈良好的线性关系;回收率分别为100.70%和100.37%,RSD分别为0.86%和0.92%。结论本法可用于同时测定莪术油注射液中莪术醇和牛儿酮的含量,方法简便、结果准确。     

胆舒片处方工艺研究

目的对胆舒片进行处方工艺的筛选。方法以薄荷脑损耗率为指标,筛选处方工艺,并对优化处方工艺制备的胆舒片进行稳定性考察。结果按筛选出的最佳处方工艺制得的胆舒片含量合格、稳定,对光、热、湿敏感。结论该工艺有效地解决了薄荷脑稳定性问题,且制备工艺简单可行,适合工业化生产。     

HPLC法测定莪术油微乳液中莪术醇和吉马酮的含量

目的:建立测定莪术油微乳液中莪术醇及吉马酮含量的HPLC方法。方法:采用RP-HPLC法。色谱柱:ODS色谱柱;流动相:甲醇-水(80:20);流速:0.8 mL.min-1;柱温:室温;进样量:20μL;检测波长分别为:205nm(莪术醇)和245 nm(吉马酮);室温测定,莪术醇和吉马酮的保留时间分别为13.6和14.7分钟。结果:莪术醇和吉马醇的的线性范围分别为1.016～16.256mg.L-1和0.468～29.928mg.L-1;最低检测限分别为0.30μg/ml和0.021μg/ml,日内和日间变异系数小于10%,精密度大于90%。结论:该方法灵敏、快速、准确,操作简便、线性范围宽,可适用于测定莪术油微乳液中莪术醇和吉马酮的含量。     

反相微乳制备的影响因素考察及处方优化

目的:考察油相、乳化剂和药物对反相微乳形成的影响。方法:采用伪三元相图法,考察乳化剂为司盘-80/吐温-80,模型药为胸腺五肽,油相为长链甘油酯、中链甘油酯、非甘油酯等各因素不同组成对反相微乳形成的影响,筛选最优处方。结果:以中链甘油酯为油相制得的反相微乳具有最大的W/O区域面积;确定最终处方为蒸馏水/司盘-80/吐温-80/辛癸酸三甘油酯(2∶3∶6∶9),胸腺五肽溶于水相中较宜。结论:乳化剂及油相组成、药物均对反相微乳的形成有影响,实际制备中应对各因素水平进行优化。     

复方紫草滴耳油治疗急性化脓性中耳炎临床研究

目的：观察复方紫草滴耳油治疗急性化脓性中耳炎的临床疗效。方法：治疗组198例用复方紫草滴耳油滴耳,对照组194例用2．5％氯霉素滴耳液滴耳。结果：治疗组治愈率75．3％、总有效率99．5％;对照组治愈率19．6％、总有效率89．2％,两组比较有极显著性差异（P〈0．01）。治疗组疗效明显优于对照组。结论：复方紫草滴耳油治疗急性化脓性中耳炎效果显著,且无毒副作用。     

药对陈皮—生姜与其单味药挥发油共有组分的比较分析

目的:利用气相色谱—质谱法分离检测药对陈皮—生姜及其单味药陈皮、生姜的挥发油成分。方法:采用交互移动窗口因子分析法(AMWFA)对药对与单味药挥发油成分的共有组分进行比较分析。用质谱库结合保留指数进行定性,并采用总体积积分法定量。结果:分别定性了陈皮、生姜、药对陈皮—生姜挥发油成分57、32和44种,分别占总含量的95.79%、82.80%、91.78%。结论:药对与陈皮、生姜的共有组分分别为28、21种,三者的共有组分为12种。     

当归油对痛经小鼠子宫组织中一氧化氮和钙离子的影响

目的探讨当归油治疗原发性痛经的作用机理。方法通过测定痛经模型小鼠子宫重量、子宫组织中一氧化氮和钙离子水平,研究当归油对子宫的作用。结果与阴性组比较,当归油能够减少催产素所致痛经小鼠的扭体次数(P<0.01),对痛经模型小鼠子宫重量无明显影响(P>0.05);给药组小鼠子宫组织中一氧化氮的含量显著升高(P<0.05);而钙离子含量显著降低(P<0 01)。结论当归油对催产素所致痛经小鼠扭体有显著抑制作用,并可升高子宫组织中一氧化氮水平,同时降低钙离子水平。这些作用可能是当归油治疗原发性痛经的部分机制。     

正交试验法优化超临界CO_2萃取蒙药肉豆蔻挥发油的工艺

采用正交试验法对超临界二氧化碳萃取蒙药肉豆蔻挥发油的工艺条件进行研究。考察了萃取温度、压力、时间对挥发油萃取率的影响。依据正交试验结果得出了超临界二氧化碳萃取蒙药肉豆蔻挥发油的较佳工艺条件:萃取是45℃、萃取压力是25MPa、萃取时间是1.5h。     

苦杏仁油的超声提取

目的：从苦杏仁中提取脂肪油。方法：运用超声技术提取，并对提取的苦杏仁油进行理化常数的检测。结果：用超声技术提取苦杏仁油的出油率为47．08％。结论：用超声技术从苦杏仁中提取苦杏仁油，可提高提取率，节省提取时间。