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Rutin nanocrystal, rutin nanocrystal transdermal drug delivery gel and preparation method thereof

A technology of nanocrystals and gels, applied in pharmaceutical formulations, skin diseases, liquid delivery, etc., can solve problems such as reducing capillary wall fragility and permeability, low water solubility and skin permeability, and restricting application, and achieve prevention. and treatment of skin photoaging and photodamage, good particle size distribution, increased skin retention

Pending Publication Date: 2020-06-02
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It mainly exists in plants and has the functions of antibacterial and anti-inflammatory, reducing the fragility and permeability of capillary walls, and hemostasis. It is mainly used in the adjuvant treatment of hypertension, cerebral hemorrhage, traumatic pulmonary hemorrhage and other diseases. A natural strong oxidizing agent for scavenging free radicals can terminate the chain reaction of free radicals, inhibit the peroxidation of polyunsaturated fatty acids on biofilms, and remove lipid peroxidation products. It plays an important role in the body, but due to its Very low water solubility and skin permeability limit the application in this area
Currently on the market, there are only oral rutin tablets and compound rutin tablets, and their pharmacokinetics show that they are hardly absorbed in the body, and the two are rarely used clinically

Method used

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  • Rutin nanocrystal, rutin nanocrystal transdermal drug delivery gel and preparation method thereof
  • Rutin nanocrystal, rutin nanocrystal transdermal drug delivery gel and preparation method thereof
  • Rutin nanocrystal, rutin nanocrystal transdermal drug delivery gel and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Preparation of rutin nanocrystal suspension

[0034] Accurately weigh a certain amount of rutin API and poloxamer 188 respectively, so that the mass ratio of rutin API and poloxamer 188 is 1:0.06, put poloxamer 188 into 20mL pure water for use It is completely dissolved, then slowly pour the weighed rutin raw material into the aqueous dispersion medium containing poloxamer 188, and stir magnetically for 10 minutes to disperse the rutin in the stabilizer aqueous dispersion medium. Cut for 1 min to obtain a coarse suspension. Pour the obtained coarse suspension into a high-pressure homogenizer, circulate 2 times at 200 bar, and circulate 5 times at 1000 bar to obtain a rutin nanosuspension. The average particle size of the rutin nanosuspension prepared by this method is 797.1nm, and the PDI value is 0.279.

Embodiment 2

[0036] Preparation of rutin nanocrystal suspension

[0037] Accurately weigh a certain amount of rutin raw material and sodium lauryl sulfate respectively, so that the mass ratio of rutin raw material and sodium lauryl sulfate is 1:3, put sodium lauryl sulfate into 20mL pure Dissolve it completely in water, then slowly pour the weighed rutin raw material into the aqueous dispersion medium containing sodium lauryl sulfate, and stir magnetically for 10 minutes to disperse the rutin in the stabilizer aqueous dispersion medium, Shearing machine 8000rpm shears 15min, obtains coarse suspension. Pour the resulting coarse suspension into a high-pressure homogenizer, and circulate 10 times at 1000 bar and 40 times at 2500 bar to obtain a rutin nanosuspension. The average particle diameter of the rutin nanosuspension prepared by this method is 685.4nm, and the PDI value is 0.250.

Embodiment 3

[0039] Preparation of rutin nanocrystal suspension

[0040] Accurately weigh a certain amount of rutin raw material and sodium lauryl sulfate respectively, so that the mass ratio of rutin raw material and sodium lauryl sulfate is 1:3, put sodium lauryl sulfate into 20mL pure Dissolve it completely in water, then slowly pour the weighed rutin raw material into the aqueous dispersion medium containing sodium lauryl sulfate, and stir magnetically for 10 minutes to disperse the rutin in the stabilizer aqueous dispersion medium, Shearing machine 8000rpm shears 15min, obtains coarse suspension. Pour the resulting coarse suspension into a high-pressure homogenizer, and circulate 10 times at 800 bar and 40 times at 2200 bar to obtain a rutin nanosuspension. The average particle size of the rutin nanosuspension prepared by this method is 535.4nm, and the PDI value is 0.221.

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Abstract

The invention discloses a rutin nanocrystal, rutin nanocrystal transdermal drug delivery gel and a preparation method thereof. The rutin nanocrystal contains a drug rutin and a stabilizer in the massratio being (1:0.06)-(1:3). The rutin nanocrystal transdermal drug delivery gel is prepared from 0.01%-5% of the rutin nanocrystal, 0.1%-5% of substrate gel, 1%-30% of a moisturizer and the balance ofwater. The rutin nanocrystal has the advantages of uniform particle size distribution, good stability, high saturation solubility, high dissolution rate and the like, the transdermal drug delivery gel is applied to transdermal drug delivery, can effectively overcome keratoderma barrier and notably improve the in-vitro transdermal permeation performance and the bioavailability of rutin, a preparation has a good treatment effect, besides, and damage to the keratoderma structure to a certain extent due to a physical means such as a common microneedle and the like for overcoming the keratoderma barrier is avoided.

Description

technical field [0001] The invention relates to compound crystals and dosage forms, in particular to a rutin nanocrystal, a rutin nanocrystal gel for transdermal administration and a preparation method thereof. Background technique [0002] Transdermal drug delivery systems (TDDS) refers to a drug delivery route through the skin or mucosal surface to achieve local or systemic therapeutic effects. It has the advantages of avoiding the first-pass effect of the liver and the destruction of the drug by the gastrointestinal tract during oral administration, and can improve the bioavailability and therapeutic effect of the drug. Therefore, transdermal preparations occupy an important position in the drug delivery system. The skin is our body's first line of defense in contact with the external environment, and it is a natural barrier to prevent the loss of water in the body and the entry of foreign substances into the body. However, due to the dense "brick wall structure" of the ...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K9/06A61K47/10A61K47/20A61K47/26A61K47/38A61K47/32A61P17/18A61P17/16
CPCA61K31/7048A61K9/06A61K47/10A61K47/20A61K47/26A61K47/38A61K47/32A61P17/18A61P17/16
Inventor 孙敏捷倪维龙玛依努尔·艾沙
Owner CHINA PHARM UNIV
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