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Berberine ultrafine-particle intestinal adhesion-type sustained-release pellet and preparation method thereof

A technology for sustained-release pellets and berberine, which is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, and bulk delivery, etc., can solve the problems of low effective bioavailability and short residence time, and achieves improved effective bioavailability. degree, the preparation method is simple, and the effect of reducing the absorption

Active Publication Date: 2013-11-20
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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  • Berberine ultrafine-particle intestinal adhesion-type sustained-release pellet and preparation method thereof
  • Berberine ultrafine-particle intestinal adhesion-type sustained-release pellet 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 out 500g of 2.5% (w / v) HPMC aqueous solution and pour into the grinding cup, turn on the mechanical stirring and grinder, and continuously add the pre-weighed 150g Berberine hydrochloride, until all the berberine hydrochloride is added to the grinding cup, start timing, the grinding speed is 3600 rpm, after grinding for 1 hour, the ground material is taken out from the receiving port to obtain the berberine suspension, which is ready for use. See Table 1 for the measurement results of the particle size of the suspension.

[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 pellet core

[0019] Weigh 500g of microcrystalline cellulose and place it in a centrifugal coating granulato...

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 pellets prepared by centrifugal granulation or extrusion spheronization starch to flow In the fluidized 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; Eudragit RL, Eudragit RS, Eudragit L100, castor oil and Polyethylene glycol-1500 is made into a coating solution and coated to obtain berberine ultrafine intestinal adhesion type sustained-release pellets.

Embodiment 3

[0028] Pharmacokinetics fitting of berberine ultrafine intestinal adhesion sustained-release pellets

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

[0030] Table 2 pharmacokinetics fitting results of berberine ultrafine intestinal adhesion sustained-release pellets

[0031] Model

[0032] It can be seen from the fitting results that when the berberine ultrafine intestinal adhesion sustained-release pellets are fitted with Higuchi equation, r> 0.99, better than the other two models, and the closeness 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 based on Fick’s diffusion law. They are based on some boundary conditions and assumptions to obtain approximate solutions to Fick’s diffusion law. Therefore, the drug in...

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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 sustained-release pellet in the field of pharmaceutical preparations and a preparation method thereof. Background technique [0002] Berberine Hydrochloride, also known as berberine hydrochloride, is widely distributed in Chinese medicinal materials such as Ranunculaceae, Berberineaceae, Papaveraceae, etc. It was isolated and identified as early as 1910, and has long been used clinically as a heat-clearing agent. Detoxification and treatment of intestinal diarrhea drugs. 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 sugar Treatment of lipid metabolism syndrome such as diabetes, hyperlipidemia and diabetic complications. [0003] According to the currently reported berberine trea...

Claims

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Application Information

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Patent Type & Authority Applications(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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