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Preparation method of water-insoluble drug microcapsule

A water-insoluble, microcapsule technology, applied in microcapsules, capsule delivery, pharmaceutical formulations, etc., can solve problems such as poor absorption, low bioavailability, adverse reactions, etc., to increase specific surface area, achieve drug targeting, The effect of improving solubility

Inactive Publication Date: 2010-07-14
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] There are serious problems in the application of poorly water-soluble drugs: first, poor water solubility will lead to poor absorption and low bioavailability, especially for oral administration
However, the use of surfactants in prescriptions is prone to toxicity or adverse reactions
Moreover, the solubilization capabilities of these carriers for different drugs often show great differences, which is not conducive to the practical application of drugs.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Step (1) Weigh 2g of gelatin microspheres with an average particle size of 300nm and pour them into a 500mL small beaker.

[0028] Step (2) Add 100 mL of an anionic polyelectrolyte poly-4-styrenesulfonate (PSS) (containing 0.5M NaCl) aqueous solution with a concentration of 1 g / L. Place on a shaker at room temperature for 20 min. Centrifuge at 5000 rpm for 15 min with a centrifuge. The supernatant was removed, and the resulting precipitate was washed / centrifuged / redispersed four times with deionized water to obtain microspheres with a layer of PSS adsorbed.

[0029] In step (3), 100 mL of an aqueous solution of cationic polyelectrolyte polyallylamine hydrochloride (PAH) (containing 0.5 M NaCl) with a concentration of 1 g / L was added. Place on a shaker at room temperature and shake for 20 minutes, then centrifuge to remove the supernatant, and the resulting precipitate is washed / centrifuged / redispersed 4 times with deionized water to obtain microspheres with PAH adsorb...

Embodiment 2

[0035] SiO with an average particle size of 2 μm 2 Microspheres replace the gelatin microspheres in Example 1, replace "poly-4-styrene sulfonate (PSS)" with anionic polyelectrolyte "sodium alginate", replace "polyallylic acid" with cationic polyelectrolyte "chitosan" Ammonium hydrochloride (PAH)", use acid (such as HF) to adjust the pH value to 12, and dissolve SiO at room temperature 2 Microspheres, centrifuged to remove dissolved SiO 2 , washed with water, and freeze-dried to obtain polyelectrolyte cavity capsules. All the other steps are the same as in Example 1, and finally the first, third, fifth, and seventh layers are chitosan adsorption layers, and the second, fourth, sixth, and eighth layers are insoluble drug capsules with sodium alginate adsorption layers. The encapsulation efficiency measured by the same method was 75.78%. After 2 minutes of sample injection, the dissolution rate of the drug reached 61%.

[0036] The above-mentioned template microspheres can al...

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Abstract

The invention relates to a preparation method of a water-insoluble drug microcapsule. The water-insoluble drug microcapsule is a capsule with a multi-layer shell structure, and the wall of the water-insoluble drug microcapsule consists of a water-insoluble drug and a membrane layer formed by alternating deposition of a plurality of layers of polyelectrolyte with opposite charges. The preparation steps are as follows: 1), at first, preparing a soluble template microsphere with the surface thereof absorbed with a plurality of polyelectrolyte membranes; 2) then, removing the soluble template microsphere to prepare a hollow polyelectrolyte capsule; and 3), finally, loading the water-insoluble drug in the hollow polyelectrolyte capsule. The insoluble drug microcapsule prepared in the method has the advantages of uniform size, high drug solubility, controllable drug releasing rate and good dispersibility in various kinds of aqueous solution, and can also be connected with biologically active substances, such as antibodies, antigens, enzymes, proteins or nucleic acid, in order to achieve drug targeting.

Description

technical field [0001] The invention relates to a method for preparing microcapsules of poorly water-soluble medicines, in particular to a method for preparing microcapsules with multi-layer shell structure and containing medicines with strong fat solubility and weak water solubility. Background technique [0002] There are serious problems in the application of poorly water-soluble drugs: First, poor water solubility will lead to poor absorption and low bioavailability, especially for oral administration. Second, intravenous administration of drugs with poor water solubility may cause serious adverse reactions such as pulmonary embolism and even respiratory failure, and may also deposit locally, resulting in excessive local drug concentration and side effects. Data in recent years have shown that nearly 40% of candidate compounds with good therapeutic potential that have been screened through high-throughput have terminated further research and development, including formul...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K45/00A61K47/32A61K47/36A61K47/42
Inventor 杨晓玲朱以华张振宗洁
Owner EAST CHINA UNIV OF SCI & TECH
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