β-细辛醚鼻用微乳凝胶的制备及其释放度考察
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摘要
目的:制备β-细辛醚微乳凝胶,并考察其质量和释放度。方法:以微乳区域大小为指标,并且以油相种类和混合乳化剂比例为因素,通过溶解度和伪三元相图筛选和制备微乳,选择合适凝胶基质制成微乳凝胶,并考察β-细辛醚微乳凝胶中β-细辛醚的含量、理化性质、稳定性和释放度。结果:选用Capryol-90为油相、吐温-80为乳化剂、丙三醇为助乳化剂,添加适量泊洛沙姆和卡波姆制成β-细辛醚微乳凝胶,各项考察指标均符合鼻腔给药要求,大鼠体内血药浓度(c_(max))为0.65μg/mL。结论:所制备的β-细辛醚微乳凝胶具有稳定性高,释药快速持久的特点,可作为鼻腔内给药用剂型的制备及其使用。
Objective: To study the preparation of micro-emulsion-based gel of β-asarone and its release in Vitro.Methods: The microemulsion area size was indicators, the types of oil phase and mixed emulsifier ratio were factor,the microemulsion prescription was screened using solubility and the pseudo-ternary phase diagram; the microemulsionbased gel was made from the suitable gel-base; the content determination, the physicochemical property, stability and pharmacokinetic of microemulsion-based gel were investigated. Results: The oil phase was Capryol-90, emulgator was Tween-80, co-emulsifier was glycerol, microemulsion-based gel was made from Poloxamer and Carbopol; the inspection indexes conformed to the requirements of the nasal drug delivery, and the cmaxwas 0.65 μg/mL in rat Vivo. Conclusion: The preparation of β-asarone microemulsion-based gels have characteristics of quality stabilization and the drug release rapid and everlasting. It can be used as the preparation and application of intranasal drug dosage form.
Objective: To study the preparation of micro-emulsion-based gel of β-asarone and its release in Vitro.Methods: The microemulsion area size was indicators, the types of oil phase and mixed emulsifier ratio were factor,the microemulsion prescription was screened using solubility and the pseudo-ternary phase diagram; the microemulsionbased gel was made from the suitable gel-base; the content determination, the physicochemical property, stability and pharmacokinetic of microemulsion-based gel were investigated. Results: The oil phase was Capryol-90, emulgator was Tween-80, co-emulsifier was glycerol, microemulsion-based gel was made from Poloxamer and Carbopol; the inspection indexes conformed to the requirements of the nasal drug delivery, and the cmaxwas 0.65 μg/mL in rat Vivo. Conclusion: The preparation of β-asarone microemulsion-based gels have characteristics of quality stabilization and the drug release rapid and everlasting. It can be used as the preparation and application of intranasal drug dosage form.
引文
[1]兰烨荣,刘素香,张铁军,等.细辛醚的研究进展[J].现代药物与临床,2013,28(2):252-257.
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[9]柯雪红,魏刚,方永奇. HPLC测定石菖蒲药材中β-细辛醚、α-细辛醚的含量[J].中成药,2002,24(10):791-792.
[10]张友智,杨晓艳,崔颖.特比萘芬乳凝胶的制备及质量评价[J].中国药房,2014,25(13):1204-1207.
[11]吴宏斌,方永奇.β-细辛醚在大鼠体内的药代动力学[J].药学学报,2004,39(10):836-838.
[12]蒋学林.效应面法优化壳聚糖温敏凝胶的制备及缓释性研究[J].临床合理用药,2014,7(7下):100-102.
[13]王莉,杨晓艳.奥硝唑温敏微乳凝胶的制备与性质考察[J].中国医院用药评价与分析,2018,18(8):1078-1081.
[14]李晓云,窦金凤,王爽,等.姜黄素微乳温敏原位凝胶剂的制备及其理化性质研究[J].药物生物技术,2013,20(3):225-228.
[2]张龙开,许日鑫,蒋梅,等.β-细辛醚微乳鼻腔给药脑内靶向性评价[J].中草药,2014,45(1):86-89.
[3]许日鑫,石添香,廖娴,等.β-细辛醚微乳的制备及其性质考察[J].中草药,2013,44(1):31-35.
[4]赵宇,王晓波,张治然,等.温敏凝胶的研究与进展[J].中国药房,2015,26(1):132-135.
[5]陈充抒,梁艳,梁莉.氧氟沙星凝胶的制备及质量控制[J].中国医院用药评价与分析,2012,12(5):434-435.
[6]范永春,戴薇,李步阳.蟾蜍毒素微乳的制备及体外透皮吸收考察[J].中国实验方剂学杂志,2013,19(21):49-53.
[7]宋艳红,崔颖.盐酸文拉法辛温敏型原位凝胶的研制[J].西北药学杂志,2015,30(2):165-168.
[8]易蕾,程德珍.氯雷他定温敏型鼻用凝胶的制备及质量研究[J].解放军药学学报,2016,32(1):5-9.
[9]柯雪红,魏刚,方永奇. HPLC测定石菖蒲药材中β-细辛醚、α-细辛醚的含量[J].中成药,2002,24(10):791-792.
[10]张友智,杨晓艳,崔颖.特比萘芬乳凝胶的制备及质量评价[J].中国药房,2014,25(13):1204-1207.
[11]吴宏斌,方永奇.β-细辛醚在大鼠体内的药代动力学[J].药学学报,2004,39(10):836-838.
[12]蒋学林.效应面法优化壳聚糖温敏凝胶的制备及缓释性研究[J].临床合理用药,2014,7(7下):100-102.
[13]王莉,杨晓艳.奥硝唑温敏微乳凝胶的制备与性质考察[J].中国医院用药评价与分析,2018,18(8):1078-1081.
[14]李晓云,窦金凤,王爽,等.姜黄素微乳温敏原位凝胶剂的制备及其理化性质研究[J].药物生物技术,2013,20(3):225-228.