油包油型辣椒素乳剂的制备与体外透皮研究

摘要
图/表
参考文献(20)
相关文章 (0)

全文: PDF (827 KB) HTML (1 KB)
输出: BibTeX | EndNote (RIS)

摘要目的制备油包油型辣椒素乳剂，以控制辣椒素释放速率，并延长瘙痒潜伏时间。方法采用正交试验，通过高压均质法制备油包油型辣椒素乳剂，采用改良Franz 扩散池进行体外透皮试验，以稳态扩散速率（Js）和离心稳定性为指标筛选最优处方。并以右旋糖酐致小鼠瘙痒模型测定其药效，其中受试组（n=8）、市售组小鼠（n=8）背部皮肤分别给予油包油型辣椒素乳剂与市售辣椒素软膏，空白对照组小鼠（n=8）给予等容积生理盐水，比较各组的潜伏时间和瘙痒次数。结果油包油型辣椒素乳剂的最佳处方是相体积比为0.5，硅油黏度为500 mPa·s，Triton X100 用量为2%。油包油型辣椒素乳剂的透皮速率低于亲水性辣椒乳膏。受试组的潜伏时间长于空白对照组和市售组，瘙痒次数少于空白对照组和市售组，差异有统计学意义（P<0.05）。结论制备的油包油型辣椒素乳剂具有良好的缓释效果，可用于治疗慢性瘙痒。

	服务

	把本文推荐给朋友
	加入我的书架
	加入引用管理器
	E-mail Alert
	RSS
	作者相关文章

关键词 ：辣椒素, 油包油型乳剂, 体外透皮

Abstract：Objective To prepare oil-in-oil capsaicin emulsion to control the release rate of capsaicin and prolong the latent itching time. Methods The oil-in-oil capsaicin emulsion was prepared by high pressure homogenization using orthogonal test, and transdermal test was conducted in vitro using modified Franz diffusion cell. The optimal formulation was selected by using the steady-state diffusion rate (Js) and centrifugal stability as indexes. The effect of dextran induced pruritus in mice was determined. The experimental group (n=8) and the commercial sale group (n=8) were given oil-in-oil capsaicin emulsion and commercial capsaicin ointment, respectively, and the blank control group (n=8) were given equal volume of normal saline. The latency time and itching times of each group were compared. Results The optimal formula of oil-in-oil capsaicin emulsion was 0.5 phase volume ratio, 500 mPa·s viscosity of silicone oil and 2%dosage of Triton X100. The transdermal rate of oil-in-oil capsaicin emulsion was lower than that of hydrophilic pepper cream. The latency time of the experimental group was longer than that of the blank control group and the commercial sale group, and the itching frequency was less than that of the blank control group and the commercial sale group, the differences were statistically significant (P<0.05). Conclusion The oil-in-oil capsaicin emulsion have good sustained release effect, high drug loading and little irritation. It is hopeful to be used in the treatment of chronic pruritus.

Key words： apsaicin Oil-in-oil-emulsions In vitro transdermal penetration

基金资助:广东省佛山市科技创新项目（医学类科技攻关）（1920001000634）

作者简介: 钟仲（1984-），男，汉族，硕士，副主任中药师，研究方向：中药学

引用本文:

钟仲；杨棣华；麦蕴华. 油包油型辣椒素乳剂的制备与体外透皮研究[J]. 中国当代医药, 2022, 29(8): 15-20.
ZHONG Zhong1 Yang Dihua2 MAI Yunhua1. Preparation and in vitro transdermal penetration of oil-in-oil capsaicin emulsion. 中国当代医药, 2022, 29(8): 15-20.

链接本文:

https://www.dangdaiyiyao.com/CN/ 或 https://www.dangdaiyiyao.com/CN/Y2022/V29/I8/15

[19]	朱溶月，李博莉，王文苹，等.“薄荷脑-樟脑”低共熔物载甘草次酸纳米乳的制备与初步评价[J].时珍国医国药，2019，30（12）：2898-2900.
[20]	李明杰，孙芮芮，李慧峰，等.四逆软膏剂基质处方优化与体外渗透性研究[J].辽宁中医药大学学报，2020，22（11）：43-49.
[1]	Wang F，Xue Y，Fu L，et al.Extraction，purification，bioactivity and pharmacological effects of capsaicin：a review[J].Crit Rev Food Sci Nutr，2021，16：1-29.
[2]	黄贤威，李戈，姚梦玮，等.辣椒碱通过TRPV1 诱导结肠癌SW480 细胞凋亡[J].中国实验方剂学杂志，2021，27（17）：75-82.
[3]	高爱琴，柏春玲，李秀英.辣椒碱对小鼠Lewis 肺癌细胞LL/2 的抗肿瘤作用研究[J].中国临床药理学杂志，2019，35（32）：2679-2681，2686.
[4]	Zhang S，Wang D，Huang J，et al.Application of capsaicin as a potential new therapeutic drug in human cancers[J].J Clin Pharm Ther，2020，45（1）：16-28.
[5]	Li R，Lan Y，Chen C，et al.Anti-obesity effects of capsaicin and the underlying mechanisms：a review[J].Food Funct，2020，11（9）：7356-7370.
[6]	Nava-Ochoa AE，Antunes-Ricardo M，Guajardo-Flores D.Nano-sized carriers for capsaicinoids with topic analgesic and anti-inflammatory effects[J].J Biotechnol，2021，333：77-85.
[7]	Anand P，Bley K.Topical capsaicin for pain management：therapeuticpotentialandmechanismsofactionofthenewhighconcentration capsaicin 8% patch[J].Br J Anaesth，2011，107（4）：490-502.
[8]	王荣雁，陈朝军，武世奎，等.辣椒碱药理作用的分子机制研究进展[J].西北药学杂志，2016，31（1）：108-110.
[9]	陈丹，艾云智，谭功军，等.梅花针刺联合辣椒素、积雪苷软膏对烧伤瘢痕患者瘙痒、睡眠及抑郁的影响[J].中医药导报，2019，25（8）：105-107，113.
[16]	Hakansson A.Emulsion Formation by Homogenization：Current Understanding and Future Perspectives[J].Annu Rev Food Sci Technol，2019，10：239-258.
[17]	李柯，陈丹，戚建中，等.HPLC 法测定复方感冒灵颗粒中9 种成分的含量[J].中药材，2019，42（6）：1347-1351.
[18]	钟钰，胡鹏翼，郑琴，等.紫苏精油纳米乳的处方工艺研究与初步质量评价[J].中草药，2020，51（22）：5714-5722.
[10]	Goncalves D，Rebelo V，Barbosa P，et al.8% Capsaicin Patch in Treatment of Peripheral Neuropathic Pain[J].Pain Physician，2020，23（5）：E541-E548.
[11]	Rottke M，Lunter DJ，Daniels R.In vitro studies on release and skin permeation of nonivamide from novel oil-in-oilemulsions[J].Eur J Pharm Biopharm，2014，86（2）：260-266.
[12]	Carvalho VF，de Lemos DP，Vieira CS，et al.Potential of Non-aqueous Microemulsions to Improve the Delivery of Lipophilic Drugs to the Skin[J].AAPS Pharm Sci Tech，2017，18（5）：1739-1749.
[13]	Jaitely V，Sakthivel T，Magee G，et al.Formulation of oil in oil emulsions：potential drug reservoirs for slow release[J].J Drug Del Sci Tech，2004，14（2）：113-117.
[14]	Lunter DJ，Rottke M，Daniels R.Oil-in-oil-emulsions with enhanced substantivity for the treatment of chronic skin diseases[J].J Pharm Sci，2014，103（5）：1515-1519.
[15]	Zia A，Pentzer E，Thickett S，et al.Advances and Opp-ortunities of Oil-in-Oil Emulsions[J].ACS Appl Mater Interfaces，2020，12（35）：38 845-38 861.