A kind of shikimic acid core-shell structure nano-preparation and preparation method thereof

A core-shell structure and nano-preparation technology, applied in antiviral agents, pharmaceutical formulations, active ingredients of anhydrides/acids/halides, etc., can solve problems such as sudden release and possible presence of carriers inside or on the surface

Active Publication Date: 2020-10-20
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the common uniaxial electrostatic spraying technology is not suitable for immiscible polymer solutions, and the drug may exist inside or on the surface of the carrier, the interaction between the drug and the carrier that acts on the surface of the carrier through physical adsorption, etc. The adhesion is relatively loose, which can easily lead to sudden release and other phenomena

Method used

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  • A kind of shikimic acid core-shell structure nano-preparation and preparation method thereof
  • A kind of shikimic acid core-shell structure nano-preparation and preparation method thereof
  • A kind of shikimic acid core-shell structure nano-preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 shikimic acid nano preparation

[0029] Accurately weigh 40 mg of shikimic acid and 40 mg of PLA, dissolve in 5 mL of acetone-methanol (volume ratio 4:1) mixed solvent, stir magnetically at room temperature for about 10 min, and obtain a clear and transparent solution, which is the nuclear layer solution to be sprayed. Another accurately weighed 20mg PLGA50 / 50 was dissolved in 5mL acetone solution, and magnetically stirred at room temperature for about 10min to obtain another clear and transparent solution, which was the shell solution to be sprayed. Draw up the prepared liquid to be sprayed with a syringe respectively, and fix it on the constant flow pump device, such as figure 1 shown. Connect the special coaxial injection needle with the positive pole of the high-voltage power supply, and connect the receiving device (aluminum foil) with the negative pole of the high-voltage power supply. Two constant-current pumps control the ejection speed of the nucl...

Embodiment 2

[0030] Embodiment 2 shikimic acid nano preparation

[0031] Accurately weigh 20 mg of shikimic acid and 60 mg of PLA, dissolve in 5 mL of acetone-methanol (volume ratio 4:1) mixed solvent, stir magnetically at room temperature for about 10 min, and obtain a clear and transparent solution, which is the nuclear layer solution to be sprayed. In addition, accurately weigh 50 mg of phospholipid and dissolve it in 5 mL of methanol solution, and stir magnetically at room temperature for about 10 minutes to obtain another clear and transparent solution, which is the shell solution to be sprayed. Draw up the prepared liquid to be sprayed with a syringe respectively, and fix it on the constant flow pump device. Connect the special coaxial injection needle with the positive pole of the high-voltage power supply, and connect the receiving device (aluminum foil) with the negative pole of the high-voltage power supply. Two constant-current pumps control the ejection speed of the nuclear lay...

Embodiment 3

[0032] Embodiment 3 shikimic acid nano preparations

[0033] Accurately weigh 10 mg of shikimic acid and 100 mg of PLA, dissolve in 5 mL of acetone-methanol solvent (volume ratio 4:1), and stir magnetically at room temperature for about 10 min to obtain a clear and transparent spinning solution, which is the core layer solution to be spun. Another accurately weighed 80mg of PLGA 85 / 15 was dissolved in acetone solution (5mL), and magnetically stirred at room temperature for about 10min to obtain another clear and transparent solution, which was the shell solution to be sprayed. Draw up the prepared solution with a 5mL syringe respectively, and fix it on the constant flow pump device respectively. Connect the special coaxial injection needle with the positive pole of the high-voltage power supply, and connect the receiving device (aluminum foil) with the negative pole of the high-voltage power supply. Two constant-current pumps control the ejection speed of the nuclear layer sol...

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Abstract

The invention discloses a shikimic acid core-shell structural nano-preparation and a preparation method thereof. The shikimic acid core-shell structural nano-preparation consists of shikimic acid, a core layer carrier and a shell layer carrier. The medicine (the shikimic acid) and the core layer carrier are dissolved in a core layer solvent and the shell layer carrier is dissolved in a shell layer solvent, and both the core layer solvent and the shell layer solvent are prepared by virtue of a coaxial electrostatic spraying method, wherein the mass ratio of the shikimic acid to the core layer carrier to the shell layer carrier is at 1 to (1-10) to (0.6-8); and the mass-volume ratio of the medicine to the core layer solvent to the shell layer solvent is at (10-40)mg to 5mL to 5mL. The nano-preparation can significantly relieve medicine burst release, and the in vivo bioavailability of the water-soluble medicine, namely the shikimic acid, is improved. Moreover, the process disclosed by the invention is simple and relatively low in cost; and the preparation method can be applied to sustained-release research of medicines relatively widely; therefore, the preparation method is relatively good in application prospect.

Description

technical field [0001] The invention relates to the field of nano drug preparations, in particular to shikimic acid core-shell nano preparations and a preparation method thereof. Background technique [0002] Shikimic acid (Shikimic Acid), white powder, easily soluble in water, insoluble in organic solvents such as chloroform, benzene and petroleum ether, is a kind of important organic acid existing in nature, first obtained from star anise by Eykmann et al in 1885 It is isolated from the fruits of the family plants (see: Bohm B A. Shikimic Acid (3,4,5-Trihydroxy-1-cyclohexene-1-carboxylic Acid)[J].Chemical Reviews,1965,65(4):435- 466.). Previously, shikimic acid was generally used as a chemical raw material, or transformed into other chemical substances or chemical agents. Since shikimic acid was discovered in 1997 as the raw material for the synthesis of specific anti-H5N1 avian influenza drugs, the Swiss company Roche has used shikimic acid as a raw material to synthesi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/19A61K47/24A61K47/34A61P31/16A61J3/07
CPCA61J3/07A61K9/5123A61K9/5146A61K31/19
Inventor 徐希明朱源王苗苗鲁双余江南
Owner JIANGSU UNIV
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