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A menthol-camphor eutectic nanoemulsion in situ gel preparation

An in-situ gel, eutectic technology, applied in the directions of drug combination, aerosol delivery, emulsion delivery, etc., can solve the problem of transmucosal absorption of menthol and camphor, no oil phase nanoemulsion preparation in situ coagulation. Glue, affecting the stability of active ingredients or preparations, etc., to achieve good mucosal penetration promotion function, conducive to absorption through nasal mucosa, and improve the effect of drug absorption

Inactive Publication Date: 2020-07-14
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, making nanoemulsions into in-situ gels is still rare in this field, especially in the process of gel preparation, the gel components are likely to have various interactions with active ingredients or excipients, thus affecting the active ingredients. Or the stability of preparation, therefore, the situation that nanoemulsion is prepared as in-situ gel in this field is less, and there is no oil phase nanoemulsion based on menthol and camphor eutectic to prepare in-situ gel
[0006] In addition, although the compound menthol nasal drops has a good therapeutic effect on dry and atrophic rhinitis, the original recipe is backward in technology, and the current administration method is still in the form of nasal drops. The main problems are as follows: 1) There is a large amount of liquid paraffin (98%) in the original preparation, which affects the transmucosal absorption of menthol and camphor; 2) A large amount of liquid paraffin in the original preparation shifts and changes the peak shape of the drug during the determination process, which interferes to a large extent Drug content determination
3) The original preparation is a fluid liquid with a short residence time in the nasal cavity, resulting in low bioavailability and poor patient compliance due to frequent use, which limits the development of this prescription to a certain extent; 4) Camphor in the original preparation and menthol are volatile and have unstable properties

Method used

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  • A menthol-camphor eutectic nanoemulsion in situ gel preparation
  • A menthol-camphor eutectic nanoemulsion in situ gel preparation
  • A menthol-camphor eutectic nanoemulsion in situ gel preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0050] Weigh 2.00 g eutectic product as the oil phase, add 4.00 g Tween-80 and 2.00 g glycerin and mix well; gradually add 20 mL water into the above mixture and mix well to make a nanoemulsion; add 0.50 g deacetylated Add cold gelatin to 50 mL of deionized water, and then add 0.20 g of sodium alginate to make a gel solution; add nanoemulsion to the gel solution, mix well, and add water to 100 mL. The measured nanoemulsion in the above system is recorded as sample 1, and the specific parameters are shown in Table 1.

Embodiment 2

[0052] Weigh 1.00 g of eutectic product as the oil phase, add 5.00 g of polyethylene glycol octylphenyl ether and 5.00 g of propylene glycol and mix well; gradually add 20 mL of water into the above mixture and mix well to make a nanoemulsion; Add 22 g of poloxamer 407 to 50 mL of deionized water, and then add 0.10 g of sodium carboxymethylcellulose to make a gel solution; add the nanoemulsion to the gel solution, mix well, add water to 100 mL have to. The measured nanoemulsion in the above system is recorded as sample 2, and the specific parameters are shown in Table 1.

Embodiment 3

[0054] Weigh 4.00 g of eutectic product as the oil phase, add 5.00 g of polyoxyethylene castor oil and 5.00 g of polyethylene glycol 400 and mix well; gradually add 20 mL of water into the above mixture, and mix well to make a nanoemulsion; Add 0.4g of Carbomer 974 to 50 mL of deionized water, and then add 0.10 g of sodium carboxymethylcellulose; add the nanoemulsion to the gel solution, mix well, add water to 100 mL, and obtain. The measured nanoemulsion in the above system is recorded as sample 3, and the specific parameters are shown in Table 1.

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Abstract

The present invention relates to a nasal nano-emulsion in situ gel using a menthol-camphor eutectic mixture as an oil phase, and a preparation method thereof, wherein the preparation is prepared from an oil phase, an emulsifier, a co-emulsifier, a gelling agent, a thickener, water and the like, is a low-viscosity liquid having good fluidity in vitro, and is rapidly converted into the gel state after being mixed with blenna narium under a physiological condition (in nasal cavity). According to the present invention, with the menthol-camphor eutectic mixture nano-emulsion in situ gel preparation, the residence time of the drug in the nasal cavity part can be significantly prolonged, the drug absorption across nasal mucosa can be promoted, and the bioavailability can be increased; and the preparation has no obvious irritation and side effect on the nasal mucosa, and has advantages of stable and controllable quality, easy treatment effect improving, and patient medication compliance improving.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations. More specifically, the invention relates to a nasal nanoemulsion in-situ gel of menthol-camphor eutectic and a preparation method thereof. Background technique [0002] Compound Menthol Nasal Drops is a common preparation for treating dry and atrophic rhinitis. The main active ingredients are menthol and camphor of equal quality, and the solvent is liquid paraffin. Menthol selectively acts on the cold receptors of the mucous membrane to produce a cold sensation. Due to the emission of the receptors, the blood vessels are constricted, the edema is reduced, and the discomfort of inflammation is relieved. Camphor also has the effect of stimulating cold receptors similar to menthol, and at the same time, it also has analgesic and antipruritic effects. [0003] There have been records in the prior art that menthol and camphor are made into eutectics, but only menthol and camphor are made in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K9/107A61K31/125A61K47/36A61K47/26A61K47/10A61K47/38A61K47/44A61K47/22A61K47/32A61K47/24A61P11/02A61K31/045
Inventor 王文苹刘晨杨魏静隋宏胡进张秋菊张立成
Owner NINGXIA MEDICAL UNIV