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Preparation method of Anhydroicaritin oral micelle preparation

A technology of icariin and micelles, which is applied in anti-inflammatory agents, pharmaceutical formulas, non-central analgesics, etc., can solve the problem of poor dissolution of icariin, difficulties in meeting the requirements of oral micelles, biological Problems such as low utilization can achieve the effects of improving drug safety, eliminating conventional hydration and freeze-drying processes, and simple preparation process

Pending Publication Date: 2020-01-24
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] CN101485630A discloses an icariin liposome, which uses soybean lecithin and cholesterol to carry icariin, which improves the problems of poor in vitro dissolution and low bioavailability of icariin
However, the particle size of micelles is too large to meet the requirements of oral micelles, and the preparation process takes a long time, the process is cumbersome, and the technical cost is high
[0009] CN102755298A discloses the preparation method and application of resveratrol freeze-dried polymer micelles. The preparation has good stability, high bioavailability, and can be taken orally or injected, but it also has cumbersome process, high technical threshold, and long time consumption. question

Method used

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  • Preparation method of Anhydroicaritin oral micelle preparation
  • Preparation method of Anhydroicaritin oral micelle preparation
  • Preparation method of Anhydroicaritin oral micelle preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1) Prescription

[0034] 1 part icariin

[0035] PEG 3000 -PLA 3000 5 copies

[0036] Lactose 60 parts

[0037] 2) Preparation steps:

[0038] a) Weighing the prescription amount of icariin and mPEG-PLA, adding 12 parts of acetonitrile, stirring to dissolve;

[0039] b) adding the prescription amount of lactose to the mixed solution in step a), and preparing the soft material through a wet mixing granulator;

[0040] c) Make wet granules through a 18-mesh sieve, transfer the wet granules into a fluidized granulator, and dry at 40°C;

[0041] d) The dried granules are sieved through a 12-mesh sieve, and packed separately.

Embodiment 2

[0043] 1) Prescription

[0044] 1 part icariin

[0045] PEG 2400 -PLA 5600 2 copies

[0046] 50 parts of sucrose

[0047] 2) Preparation steps:

[0048] a) Weigh the prescription amount of icariin and mPEG-PLA, add 10 parts of tetrahydrofuran, and stir to dissolve it;

[0049] b) adding the prescription amount of sucrose to the mixed solution of step a), and preparing the soft material through a wet mixing granulator;

[0050] c) Make wet granules through a 18-mesh sieve, transfer the wet granules into a fluidized granulator, and dry at 40°C;

[0051] d) The dried granules are sieved through a 12-mesh sieve, and packed separately.

Embodiment 3

[0053] 1) Prescription

[0054] Arctigenin 1 part

[0055] PEG 7000 -PLA 3000 10 copies

[0056] Dextrin 70 parts

[0057] 2) Preparation steps:

[0058] a) Weigh arctigenin and mPEG-PLA of the prescribed amount, add 14 parts of acetone, and stir to dissolve it;

[0059] b) Add the prescription amount of dextrin to the mixed solution in step a), and prepare the soft material through a wet mixing granulator;

[0060] c) Make wet granules through a 18-mesh sieve, transfer the wet granules into a fluidized granulator, and dry at 40°C;

[0061] d) The dried granules are sieved through a 12-mesh sieve, and packed separately.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a preparation method of an Anhydroicaritin micelle preparation for oral administration. The preparation method comprises the following steps: dissolving anhydroicaritin and an amphiphilic polymer in an organic solvent, adding pharmaceutically acceptable water-soluble auxiliary materials to prepare a soft material, drying the material, sub-packaging the material, and adding water to dissolve during taking, thereby obtaining the oral micelle preparation. Compared with the prior art, conventional hydration and freeze-drying processes are omitted, time and production cost are greatly saved, the preparation process is simple, operability is high, and wide application prospects are achieved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a preparation method of an oral icarigenin micelle preparation. Background technique [0002] Icaritin (IT) is a polyhydroxy flavonoid monomer component extracted from Epimedium genus Epimedium of Berberidaceae, which has the functions of promoting regeneration and differentiation of myocardial cells, anti-inflammation, aphrodisiac, regulating immunity , promote bone protection, anti-tumor and lower blood sugar and other pharmacological effects, its structural formula is as follows: [0003] [0004] Icarigenin is extremely fat-soluble, almost insoluble in water, and almost insoluble or insoluble in different pH buffers. Its extremely low solubility leads to poor oral absorption and low bioavailability, which seriously restricts the efficacy of the drug. [0005] The polymer micellar drug delivery system can effectively improve the solubility ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K47/26A61K47/36A61K47/10A61K31/352A61K31/365A61K31/58A61P9/00A61P29/00A61P15/00A61P37/02A61P19/00A61P35/00A61P3/10
CPCA61K9/0056A61K9/1075A61K31/352A61K31/365A61K31/58A61K47/10A61K47/26A61K47/34A61K47/36A61P3/10A61P9/00A61P15/00A61P19/00A61P29/00A61P35/00A61P37/02
Inventor 张贵民尚萍萍郑华
Owner LUNAN PHARMA GROUP CORPORATION
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