Nattokinase external transdermal absorbent and preparation method thereof

The technology of a transdermal absorbent and nattokinase is applied in the field of nattokinase external transdermal absorbent and its preparation, which can solve the problems of poor transdermal property, poor stability and low bioavailability of nattokinase

Active Publication Date: 2021-08-20
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention provides an external transdermal absorbent for nattokinase, which has good absorbability and strong stability, solves the problem of poor transdermal properties of nattokinase, and overcomes the low and stable bioavailability of nattokinase when it is taken as an oral preparation sex problem

Method used

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  • Nattokinase external transdermal absorbent and preparation method thereof
  • Nattokinase external transdermal absorbent and preparation method thereof
  • Nattokinase external transdermal absorbent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1 Preparation and Drug Release Test of Nattokinase External Transdermal Absorbent

[0048] 1. Preparation of Nattokinase External Transdermal Absorbent

[0049] (1) Preparation of Nattokinase Molecular Microcapsules

[0050] Prescription: nattokinase: soybean lecithin: sodium deoxycholate (w / w / w)=1:5:0.5;

[0051]Preparation steps: Dissolve 0.26g of nattokinase dry powder in 20mL of normal saline as the water phase; dissolve 1.3g of soybean lecithin and 0.13g of sodium deoxycholate in 30mL of absolute ethanol, dissolve evenly, and use it as the organic phase; Evaporate in a rotary evaporator to form a uniform film, add the water phase, continue to hydrate for 60 minutes, and form a suspension of microcapsules. Ultrasonic (ultrasonic power: 200W) is dispersed in an ice bath for 5 minutes, and refrigerated and centrifuged at 4°C (centrifugal speed (15000rpm) for 20min, discard the supernatant, collect the precipitate, freeze-dry to obtain nattokinase molecula...

Embodiment 2

[0066] The preparation (three batches) of embodiment 2 nattokinase external transdermal absorption agent pilot product

[0067] According to the method of Example 1, the prescription in Table 2 was prepared into three batches of pilot product of nattokinase external transdermal absorption agent, 100 parts / batch, and the dosage range of nattokinase was guaranteed to be 0.250g~0.283g / per part.

[0068] Table 2

[0069]

[0070] Pilot-scale product (three batches) nattokinase transdermal absorber release assay mode is the same as implementation example 1, and detection result is as shown in table 3, Figure 4 Nattokinase release curves are shown.

[0071] table 3

[0072]

[0073]

[0074] Depend on Figure 4 As can be seen from Table 3, the above-mentioned pilot product of nattokinase external transdermal absorption agent is consistent with the release rule of nattokinase described in Example 1. Nattokinase reaches the effective concentration in the body after 2 hou...

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Abstract

The invention discloses a nattokinase external transdermal absorbent and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The nattokinase external transdermal absorbent is prepared by the following steps of adding nattokinase molecular microcapsules into a blank matrix by an equivalent gradual increase method, uniformly dispersing, then adding a humectant, an emulsifier and a penetration enhancer, uniformly stirring, adding a pH regulator, and regulating the pH value to 6-7, thereby obtaining the nattokinase external transdermal absorbent. The nattokinase external transdermal absorbent provided by the invention can avoid low bioavailability and liver first-pass effect caused by oral administration, has the characteristics of good absorbability and strong stability, overcomes the defect that the nattokinase is difficult to transdermal absorption due to large molecular weight, and realizes the purpose of treating cardiovascular and cerebrovascular diseases by using the nattokinase external transdermal absorbent.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a nattokinase transdermal absorbent for external use and a preparation method thereof. Background technique [0002] The data show that the overall prevalence of dyslipidemia in Chinese adults is as high as 40.4%. At present, the commonly used lipid-lowering drugs in clinical practice include statins, vitamin B3, fibrates, bile acid chelating agents, polyene fatty acids, etc., among which statins are used The most common, its lipid-lowering effect is good, but long-term high-dose use will lead to dose-dependent, but also cause side effects such as headache, gastrointestinal symptoms and muscle adverse reactions (myositis, rhabdomyolysis), and the administration of these lipid-lowering drugs Most of the routes are oral or intravenous administration, and no external lipid-lowering preparation has been found in the application mode. [0003] Nattokinase (Na...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/38A61K47/18A61K47/32A61K38/48A61K9/50A61K47/24A61P3/06
CPCA61K38/482C12Y304/21062A61K9/7053A61K47/38A61K47/183A61K9/5015A61P3/06
Inventor 金青刘兴华李微微陈永根郝小惠赵文英谭心舜彭佳
Owner QINGDAO UNIV OF SCI & TECH
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