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A kind of berberine ultrafine intestinal adhesion type sustained-release pellets and preparation method thereof

A technology of slow-release pellets and berberine, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, block delivery, etc., can solve the problems of short residence time and low effective bioavailability, and achieve simple preparation methods, Improve the effective bioavailability and the effect of taking convenience

Active Publication Date: 2016-01-27
SHENYANG NO 1 PHARMA FACTORY DONGBEI PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a kind of berberine superfine intestinal adhesion type sustained-release pellets and preparation method thereof, to overcome the rapid drug release, bitter taste, short retention time in the gastrointestinal tract, The effective bioavailability is low and cannot meet the defects of long-term medication requirements of patients. It is convenient to take, slow release of drugs reduces the number of times and doses of medication, improves the effective bioavailability of drugs and the compliance and compliance of patients, and has a simple preparation method, which is suitable for Industrial production

Method used

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  • A kind of berberine ultrafine intestinal adhesion type sustained-release pellets and preparation method thereof
  • A kind of berberine ultrafine intestinal adhesion type sustained-release pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] 1. Preparation of berberine homogeneous suspension

[0015] Prepare 2.5% (w / v) HPMC aqueous solution as the carrier during grinding, weigh 500g of 2.5% (w / v) HPMC aqueous solution and pour it into the grinding cup, turn on the mechanical stirring and grinding machine, and continuously add the pre-weighed 150g Berberine hydrochloride, until the berberine hydrochloride is all added to the grinding cup, start timing, the grinding speed is 3600rpm, after grinding for 1 hour, take out the ground material from the feeding port to obtain the berberine suspension, ready for use. The particle size measurement results of the suspension are shown in Table 1.

[0016] Table 1 Particle size measurement results of berberine suspension

[0017] Time (min)

Mean(μm)

SD(μm)

<1μm (%)

<10μm (%)

d. 90 .(μm)

60

1.034

0.844

72.5

100

1.904

[0018] 2. Preparation of blank core

[0019] Weigh 500g of microcrystalline cellulose ...

Embodiment 2

[0026] Stir and grind an appropriate amount of hydroxypropyl cellulose aqueous solution with berberine to prepare a small and uniform berberine drug suspension; take an appropriate amount of blank pellet cores prepared by centrifugal granulation or extrusion spheronization In the chemical bed, spray the berberine drug suspension to make berberine small particle size drug-loaded pellets, and screen the pellets with a particle size of 0.25-0.43mm; EudragitRL, EudragitRS, EudragitL100, castor oil and polyethylene glycol Alcohol-1500 is made into a coating liquid, and coated to obtain berberine ultrafine intestinal adhesion type sustained-release pellets.

Embodiment 3

[0028] Pharmacokinetic fitting of berberine ultramicroparticle intestinal adhesion sustained-release pellets

[0029] Take the berberine ultrafine intestinal adhesion type sustained-release pellets prepared in Example 1, measure its release curve, and fit it with a commonly used release model. The fitting results are shown in Table 2:

[0030] Table 2 Pharmacokinetic fitting results of berberine ultrafine-grained intestinal-adhesive sustained-release pellets

[0031] model

[0032]From the fitting results, it can be seen that when the berberine ultrafine-grained intestinal-adhesive sustained-release pellets are fitted by the Higuchi equation, r>0.99, which is better than the other two models, and the fitting degree of the in vitro release model is as follows: Higuchi model > Zero-order model > First-order model. The three models in the above table are all proposed based on Fick’s diffusion law, and they obtain the approximate solution of Fick’s diffusion law on the ...

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Abstract

The invention discloses berberine ultrafine-particle intestinal adhesion-type sustained-release pellets and a preparation method for the same, which are applied to the field of pharmaceutical preparations. The berberine ultrafine-particle intestinal adhesion-type sustained-release pellets are composed of berberine small-particle-size pellets and a coating material, wherein the berberine small-particle-size pellets are prepared by wrapping a medicine suspension on blank pellet cores; the medicine suspension is composed of berberine and a hydrophilic carrier material; the hydrophilic carrier material is selected from any one or more of hydroxy propyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone and polyvinyl alcohol; a plasticizer is selected from any one or more of triethyl citrate, polyethylene glycol-6000, castor oil and polyethylene glycol-1500. The ultrafine-particle sustained-release pellets disclosed by the invention can be retained in the upper section of an intestinal canal for a long time and continuously release medicines, and can effectively act on local targets for treating glucolipid metabolic syndrome, of the intestinal canal, so as to achieve a goal of continuously reducing absorption for glycolipid substances, and then achieve goals of reducing blood sugar and regulating blood lipid; the ultrafine-particle intestinal adhesion-type sustained-release pellets are convenient to take and suitable for industrialized production.

Description

technical field [0001] The invention relates to a berberine ultrafine intestinal adhesion type slow-release pellet and a preparation method thereof in the field of pharmaceutical preparations. Background technique [0002] Berberine Hydrochloride, also known as berberine hydrochloride, is widely distributed in traditional Chinese medicinal materials such as Ranunculaceae, Berberidaceae, and Poppyaceae. It was isolated and identified as early as 1910. And the use of drugs for the treatment of enterobacterial diarrhea. In recent years, with the in-depth study of the pharmacology of berberine, its clinical use has expanded from simple antibacterial and antidiarrheal effects to cardiovascular diseases such as arrhythmia, refractory heart failure and hypertension, as well as diabetes Treatment of lipid metabolism syndrome such as diabetes, hyperlipidemia and diabetic complications. [0003] According to current reports, an important pathway for berberine to treat glucose and li...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/4375A61P3/10A61P3/06
Inventor 汲涌周凯唐星张宇蔡翠芳徐晖
Owner SHENYANG NO 1 PHARMA FACTORY DONGBEI PHARMA GRP
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