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Matrine magnetic slow-releasing capsule and preparation method

A technology of sustained-release capsules and matrine, applied in the direction of pharmaceutical formulations, organic active ingredients, medical preparations of non-effective ingredients, etc., can solve the problem of ineffective reduction of drug side effects and adverse drug reactions, drug side effects and adverse effects Increased response, lack of targeted drug delivery characteristics, etc., to achieve improved bioavailability, high saturation magnetization, and sustained release

Inactive Publication Date: 2012-01-04
LANZHOU UNIV SECOND HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the defects and deficiencies in the design of the above-mentioned matrine pharmaceutical preparations, in clinical use, doctors increase the dosage of the drug to increase the concentration of the drug in order to obtain a good clinical treatment effect, which will lead to increased toxic and side effects and adverse reactions of the drug. Poor compliance, low drug bioavailability, unable to achieve the expected therapeutic purpose
In order to overcome the above shortcomings, Chinese invention patent application 03100896.8 and Chinese invention patent application 03100897.6 disclose the sustained-release preparation of matrine. The sustained-release preparations disclosed in the above-mentioned patent documents are capsules and enteric-coated tablets. Effect time, but does not have the characteristics of targeted drug delivery, still can not effectively reduce drug side effects and adverse drug reactions, effectively improve drug bioavailability, and enhance clinical treatment effect
Chinese invention patent application 200610019300.X discloses a matrine magnetic microsphere, which is a preparation composed of magnetic targeting and slow-release dual drug release mechanisms. However, the preparation is administered in the form of intravenous infusion. Not only is the medication method complicated, it is very inconvenient for patients, and the compliance is poor, and there are many fatal problems that cannot be overcome, such as how to eliminate or remove the magnetic fluid remaining in the blood vessel (because this kind of substance itself cannot be degraded and metabolized), and how to solve it. It adheres and accumulates on the inner wall of blood vessels, causing granulation tissue hyperplasia, blocking blood vessels, reducing blood flow, and damaging body tissues and organs, etc.

Method used

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  • Matrine magnetic slow-releasing capsule and preparation method
  • Matrine magnetic slow-releasing capsule and preparation method
  • Matrine magnetic slow-releasing capsule and preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0030] (1) dissolving chitosan in an aqueous acetic acid solution with a volume ratio of 0.2% to 1%, and the concentration of chitosan in the aqueous acetic acid solution is 0.005 to 0.04g / mL to obtain an acetic acid solution of chitosan. The preparation method of chitosan in other embodiments of the present invention is the same as this.

[0031] (2) Preparation of matrine drug-loaded magnetic particles: Weigh microcrystalline cellulose (the cellulose content is 97.0% to 102%, and the colloid viscosity can reach 3000 to 5000mPa·s when the concentration is 3%, used in the following examples Each of the microcrystalline cellulose is the same) 0.4g, Fe 3 o 4 Magnetic nanoparticles (20nm, the magnetic nanoparticles particle size used in the following examples are the same) 0.12g and matrine 0.1g, after mixing, add 0.02g / mL chitosan in 1% acetic acid solution 2mL, stir well , Soft materials. Pass through a 65-mesh sieve to granulate, dry at a constant temperature of 50°C, sieve...

Embodiment 2

[0035] (1) Preparation of matrine drug-loaded magnetic particles: weigh 0.4 g of microcrystalline cellulose, Fe 3 o 4 After mixing 0.1 g of magnetic nanoparticles and 0.1 g of matrine, add 0.02 g / mL chitosan into 3 mL of 1% acetic acid solution, stir evenly, and make a soft material. Pass through a 65-mesh sieve to granulate, dry at a constant temperature of 50°C, sieve through a 65-mesh sieve, and granulate to obtain matrine drug-loaded magnetic particles.

[0036] (2) Preparation of matrine magnetic slow-release granules: prepare 12 mL of 1% acetic acid aqueous solution, add 0.24 g of chitosan to make it naturally peptized, and repeatedly spray or wrap the above-mentioned chitosan acetic acid solution in Sophora flavescens for 13 times The surface of the alkali-loaded magnetic granules is sieved with a 50-mesh sieve, sized, and dried at a constant temperature of 50°C to obtain the matrine magnetic sustained-release granules.

[0037] (3) Preparation of matrine magnetic sus...

Embodiment 3

[0039] (1) Preparation of matrine drug-loaded magnetic particles: weigh 0.4 g of microcrystalline cellulose, Fe 3 o 4 After mixing 0.12g of magnetic nanoparticles and 0.1g of matrine, add 0.025g / mL chitosan in 2mL of 1% acetic acid solution, stir evenly, and make a soft material. Pass through a 65-mesh sieve to granulate, dry at a constant temperature of 50°C, sieve through a 65-mesh sieve, and granulate to obtain matrine drug-loaded magnetic particles.

[0040] (2) Preparation of matrine magnetic slow-release granules: prepare 6 mL of 1% acetic acid aqueous solution, add 0.15 g of chitosan to make it naturally peptized, and repeatedly spray or wrap the above-mentioned chitosan acetic acid solution in Sophora flavescens for 13 times The surface of the alkali-loaded magnetic granules is sieved with a 50-mesh sieve, sized, and dried at a constant temperature of 50°C to obtain the matrine magnetic sustained-release granules.

[0041] (3) Preparation of matrine magnetic sustaine...

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Abstract

The invention discloses a matrine magnetic slow-releasing capsule for treating gastrointestinal tumors through oral administration, and a preparation method of the matrine magnetic slow-releasing capsule. The content of the matrine magnetic slow-releasing capsule is matrine magnetic slow-releasing particles; the matrine magnetic slow-releasing capsule comprises drug carried magnetic particles and a slow-releasing coating film; the drug carried magnetic particles of the content include matrine, magnetic substance (ferroferric oxide) nanoparticles, microcrystalline cellulose and chitosan in the slow-releasing coating film; and the mass ratio of the matrine, the magnetic substance (ferroferric oxide) nanoparticles, the microcrystalline cellulose and the chitosan is 1 : 0.5-2 : 1-8: 0.1-3 . Through oral administration and being guided by the magnetic field, the matrine magnetic slow-releasing capsule not only can target the gastrointestinal tumor cells, but also can delay the release speed of the main drug; the adverse effects, complications and adverse reactions of the drug can be expected to be reduced; the drug administration frequency is reduced; the compliance of the patients is increased; and the clinical treatment effect of the drug is enhanced.

Description

Technical field: [0001] The invention relates to a pharmaceutical preparation, in particular to a new matrine sustained-release magnetic capsule for treating digestive tract tumors and a preparation method. Background technique: [0002] Matrine is an alkaloid extracted and isolated from leguminous plants Sophora flavescens, Sophora flavescens, and broad bean root. It belongs to the tetracyclic quinolizidine class and has significant antitumor activity. See "Jiang H, et al. al. Matrine upregulates the cell cycle protein E2F-1 and triggers apoptosis via the mitochondrial pathway in K562 cells. European Journal of Pharmacology, 2007, 559: 98.". Studies have shown that the mechanism of its anti-tumor activity includes: inhibiting tumor proliferation, inducing tumor differentiation and apoptosis, inhibiting tumor invasion and distant metastasis, alleviating tumor-induced cachexia and inhibiting tumor drug resistance, inhibiting telomerase activity, etc. [0003] In addition, ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/4375A61K47/38A61K47/02A61P35/00A61P1/16A61P31/20A61P7/00
Inventor 李平李玉民张玲玲王晓飞焦海胜
Owner LANZHOU UNIV SECOND HOSPITAL
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