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Felodipine film-controlled slow-release pellet capsule

A technology of slow-release pellets and horizontal membranes, which can be used in medical preparations with non-active ingredients, oil/fat/wax non-effective ingredients, cardiovascular system diseases, etc., and can solve the problems of membrane aging and release decline

Active Publication Date: 2013-07-24
北京天衡药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to solve the problem of release decline caused by film aging of felodipine film-controlled sustained-release pellets prepared by aqueous dispersion coating, the present invention provides a film-controlled film that can maintain stable release performance throughout the validity period. Felodipine slow-release pellet capsules are characterized in that the core of the pellets contains sodium carboxymethyl starch with high water-swellability, and the slow-release coating film is deformed by water swelling, thereby offsetting the aging of the film

Method used

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  • Felodipine film-controlled slow-release pellet capsule
  • Felodipine film-controlled slow-release pellet capsule
  • Felodipine film-controlled slow-release pellet capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The felodipine slow-release pellet capsule of embodiment 1 common ball core

[0030] 1. Prescription

[0031] 1. Pill core prescription (1000 capsules)

[0032]

[0033]

[0034] 2. Prescription of sustained-release film coating solution

[0035]

[0036] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0037] Second, the preparation process:

[0038] 1. Ball core preparation process:

[0039] (1) Pass Felodipine through an 80-mesh sieve.

[0040] (2) Felodipine, microcrystalline cellulose PH101, lactose are taken by weighing recipe quantity, put in the wet granulator and mix homogeneously;

[0041] (3) polyoxyethylene hydrogenated castor oil RH40 of recipe quantity is dissolved in a small amount of 2% sodium carboxymethylcellulose 10% ethanol solution;

[0042] (4) Pour 2% sodium carboxymethylcellulose 10% ethanol solution containing polyoxyethylene hydrogenated castor oil RH40 into a wet granulator to make soft materials, and then use an app...

Embodiment 2

[0066] Example 2 Felodipine Sustained-release Pellet Capsules Containing 5% Sodium Carboxymethyl Starch

[0067] 1. Prescription

[0068] 1. Pill core prescription (1000 capsules)

[0069]

[0070] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0071] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0072] Second, the preparation process:

[0073] 1. Ball core preparation process:

[0074] (1) Felodipine is passed through a 60 mesh sieve;

[0075] (2) Felodipine, microcrystalline cellulose PH101, lactose, carboxymethyl starch sodium of recipe quantity are taken by weighing, put in the wet granulator and mix homogeneously;

[0076] (3) polyoxyethylene hydrogenated castor oil RH40 of recipe quantity is dissolved in a small amount of 2% sodium carboxymethylcellulose 10% ethanol solution;

[0077] (4) All the 2% sodium carboxymethylcellulose 10% ethanol solution containing polyoxyethylene hydrogenated castor oil RH40 is po...

Embodiment 3

[0099] Embodiment 3 Felodipine slow-release pellet capsule containing 10% sodium carboxymethyl starch

[0100] 1. Prescription

[0101] 1. Pill core prescription (1000 capsules)

[0102]

[0103] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0104] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0105] Second, the preparation process:

[0106] 1. Ball core preparation process: the same as in Example 2

[0107] 2. Preparation process of sustained-release film coating solution:

[0108] Same as Example 1

[0109] 3. Coating (sustained release film):

[0110] The ball core is placed in a fluidized bed for coating, and the weight gain of the coating film is controlled, and the weight gain of the coating is 25.5% and 29.4%.

[0111] 4, heat treatment: with embodiment 1

[0112] 5. Filling capsules:

[0113] Same as Example 1

[0114] 3. Release, content determination and results

[0115] Measuring method: with embodime...

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Abstract

The invention relates to a felodipine film-controlled slow-release pellet capsule. A slow-release film of the felodipine film-controlled slow-release pellet utilizes Eurdragit RL 30D as a film-formation material. A pellet core of the felodipine film-controlled slow-release pellet contains sodium carboxymethyl starch having high expansibility, and also contains pharmaceutically acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose and lactose as fillers and polyoxyethylene hydrogenated castor oil RH40 as a solubilizer, and the pellet core comprises 5 to 20wt% of sodium carboxymethyl starch. The slow-release film comprises Eurdragit RL 30D, triethyl citrate as a plasticizer and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit RL 30D to triethyl citrate to talcum powder is 30: 3: 4 and a film weight increasing ratio is in a range of 20 to 36%. The felodipine film-controlled slow-release pellet comprises the pellet core containing sodium carboxymethyl starch having high water expansibility and thus after absorbing water, the felodipine film-controlled slow-release pellet expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the felodipine film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.

Description

technical field [0001] The invention relates to a felodipine membrane-controlled sustained-release pellet capsule, in particular to a felodipine membrane-controlled sustained-release pellet capsule with a pellet core containing sodium carboxymethyl starch, belonging to the field of pharmaceutical preparations. Background technique [0002] Felodipine is a calcium antagonist that selectively antagonizes the influx of calcium ions in vascular smooth muscle to produce a hypotensive effect and is used for the treatment of hypertension. [0003] Felodipine is almost insoluble in water, and the earliest common preparation on the market needs to be taken twice a day, the blood concentration fluctuates greatly, the peak concentration is too high, and the adverse reactions are serious. [0004] Felodipine Sustained-release Tablets (trade name: Plendine) listed by AstraZeneca is a gel matrix sustained-release tablet. Since the drug release area of ​​the matrix is ​​constantly changing...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/4422A61K47/36A61K47/44A61P9/12
Inventor 姜庆伟狄媛吕玉珠唐亚坤刘俊轶
Owner 北京天衡药物研究院有限公司
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