Comparison of Pharmaceutical Characterization and Tissue Distribution Between Chuanqi Ophthalmic Microemulsion in situ Gel and Normal in situ Gel

Mao-bo DU; Shu-zhi LIU; Li-na LIANG; Shuo SHEN; Kai XU

doi:10.13422/j.cnki.syfjx.20182313

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Comparison of Pharmaceutical Characterization and Tissue Distribution Between Chuanqi Ophthalmic Microemulsion in situ Gel and Normal in situ Gel

Pharmacy and Processing | 更新时间：2021-02-09

- Comparison of Pharmaceutical Characterization and Tissue Distribution Between Chuanqi Ophthalmic Microemulsion in situ Gel and Normal in situ Gel
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 25, Issue 5, Pages: 151-155(2019)
- 作者机构：
  
  1.中国中医科学院　中药研究所，北京　 100700；
  2.中国中医科学院　眼科医院，北京　 100040
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.20182313
  CLC： R22;O657.6;R285.5;R283.6
- Received：04 May 2018，
  
  Published Online：12 September 2018，
  
  Published：05 March 2019
- 稿件说明：
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Mao-bo DU, Shu-zhi LIU, Li-na LIANG, et al. Comparison of Pharmaceutical Characterization and Tissue Distribution Between Chuanqi Ophthalmic Microemulsion in situ Gel and Normal in situ Gel[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(5): 151-155.
DOI：

Mao-bo DU, Shu-zhi LIU, Li-na LIANG, et al. Comparison of Pharmaceutical Characterization and Tissue Distribution Between Chuanqi Ophthalmic Microemulsion in situ Gel and Normal in situ Gel[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(5): 151-155. DOI： 10.13422/j.cnki.syfjx.20182313.

摘要

目的：

考察微乳在川芪微乳原位凝胶中的作用，为相关眼用制剂的研发提供参考。

方法：

通过川芪微乳原位凝胶与川芪普通原位凝胶的平行比较确定微乳的作用，包括制剂学表征及组织分布研究。

结果：

川芪微乳原位凝胶、普通原位凝胶的平均粒径分别为(38.20±0.13)，(985±37) nm。微乳在微乳原位凝胶复合体系中仍能保持其纳米载体的特性。在大鼠眼组织中，3个指标成分川芎嗪、藁本内酯及黄芪甲苷只有藁本内酯可被检测到；川芪微乳原位凝胶中藁本内酯在角膜、玻璃体及视网膜上均能检测到，而川芪普通原位凝胶的藁本内酯只能在角膜中被检测到，且含量极低。3个指标成分中藁本内酯的油水分配系数常用对数(lg

)2.87，在理想的眼用药物油水分配系数范围内(lg

＝2.0～3.0)，同时微乳提高了该成分在角膜各组织的分配浓度。

结论：

微乳纳米载体的特性可增加藁本内酯类成分的溶解性，使其在角膜外的泪液中有更好的分配，到达角膜时具有较高的浓度，形成角膜浓度梯度，从而通过跨眼屏障将药物由前眼部位输送到到后眼部位。

Abstract

Objective:

In this paper

the effect of microemulsion in Chuanqi ophthalmic microemulsion

in situ

gel was investigated.

Method:

The effect of microemulsion was confirmed by the parallel comparison between the Chuanqi microemulsion

in situ

gel and normal

in situ

gel

including study of pharmaceutical characterization and tissue distribution.

Result:

The average particle sizes of Chuanqi microemulsion

in situ

gel and normal

in situ

gel were (38.20±0.13) nm and (985±37) nm

respectively.Microemulsion could maintain the properties of nanocarrier in a microemulsion

in situ

gel composite system.The result of tissue distribution study showed that only ligustilide could be detected.This was related to the nature of these three indicator components(ligustrazine

ligustilide and astragaloside A). The common logarithm of oil and water partition coefficient of ligustilide(lg

) was 2.87

which was consistent with the range of lg

of ideal ophthalmic drugs(lg

=2.0-3.0). The ligustilide from Chuanqi microemulsion

in situ

gel could be detected in the cornea

vitreous body and retina

and this compound from normal

in situ

gel could only be detected in the cornea with low content.At the same time

microemulsion could increase the content of ligustilide in corneal tissues.

Conclusion:

The characteristics of microemulsion nanocarriers can increase the solubility of ligustilide

compared with normal

in situ

gel

it can be better distributed in the tears outside the corneal

it reaches the cornea with a higher concentration

and forms a corneal concentration gradient

and ligustilide is transported from the anterior ocular region to the posterior ocular region through the transocular barrier.

关键词

Keywords

references

唐忠庆，吴坚，郑赓唐，等．多囊卵巢综合征与卵巢颗粒细胞凋亡基因蛋白Bcl-2、Bax、P53的相关性研究 [J]. 世界最新医学信息文摘， 2016 , 16 ( A5 ): 98 - 99 .

易红，杨华，高进，等． O/W型微乳凝胶粒度分布特性的研究 [J]. 中国实验方剂学杂志， 2011 , 17 ( 17 ): 1 - 4 .

Chastain J E , Sanders M E , Curtis M A , et al . Distribution of topical ocular nepafenac and its active metabolite amfenac to the posterior segment of the eye [J]. Exp Eye Res , 2016 , 145 : 58 - 67 .

Di Tommaso C , Bourges J L , Valamanesh F , et al . Novel micelle carriers for cyclosporin A topical ocular delivery：in vivo cornea penetration，ocular distribution and efficacy studies [J]. Eur J Pharm Biopharm , 2012 , 81 ( 2 ): 257 - 264 .

Tajika T , Isowaki A , Sakaki H. Ocular distribution of difluprednate ophthalmic emulsion 0.05% in rabbits [J]. J Ocul Pharmacol Ther , 2011 , 27 ( 1 ): 43 - 49 .

SHEN J , DENG Y , JIN X , et al . Thiolated nanostructured lipid carriers as a potential ocular drug delivery system for cyclosporine A：improving in vivo ocular distribution [J]. Int J Pharm , 2010 , 402 ( 1/2 ): 248 - 253 .

孙考祥，彭绍民，孙大卫，等．双氯酚酸钠滴眼液的眼内组织分布及药代动力学 [J]. 中国临床药理学杂志， 2001 , 17 ( 2 ): 118 - 120 .

汤成泳，李卿，周远大，等．麝香滴眼液在家兔眼内组织中的分布及药代动力学研究 [J]. 中成药， 2010 , 32 ( 4 ): 581 - 585 .

李彬．与年龄有关的黄斑变性 [J]. 国外医学·眼科学分册， 1994 , 18 ( 1 ): 8 - 21 .

王玉国，高宇．年龄相关性黄斑变性的研究进展 [J]. 航空航天医学杂志， 2007 , 18 ( 1 ): 57 - 59 .

刘家琦，李凤鸣．实用眼科学 [M]. 3版．北京：人民卫生出版社， 2010 ： 164 - 165 .

杜茂波，沈硕，陈强，等．粒径法筛选微乳固体型表面活性剂 [J]. 中国实验方剂学杂志， 2015 , 21 ( 22 ): 137 - 139 .

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