Metoprolol fumarate film-controlled slow-release pellet capsule

A technology of slow-release pellets and torol film, which is applied in the direction of medical preparations of non-active ingredients, cardiovascular system diseases, organic active ingredients, etc., and can solve the problem of 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

[0007] In order to solve the problem of release decline caused by membrane aging of metoprolol fumarate film-controlled sustained-release pellets prepared by aqueous dispersion coating, the present invention provides a release performance that can always maintain stability during the validity period The film-controlled metoprolol fumarate sustained-release pellet capsules are characterized in that the core of the pellets contains croscarmellose sodium with high water swelling, and the sustained-release coating is swollen by absorbing water. Membrane deformation, which counteracts membrane aging

Method used

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  • Metoprolol fumarate film-controlled slow-release pellet capsule
  • Metoprolol fumarate film-controlled slow-release pellet capsule
  • Metoprolol fumarate film-controlled slow-release pellet capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The metoprolol fumarate sustained-release pellet capsule of embodiment 1 common ball core

[0042] 1. Prescription

[0043] 1. Pill core prescription (1000 capsules)

[0044]

[0045] 2. Prescription of sustained-release film coating solution

[0046]

[0047] 3. Capsule shell size 0 is 1000 capsules.

[0048] Second, the preparation process:

[0049] 1. Ball core preparation process:

[0050] (1) Metoprolol fumarate is passed through a 60 mesh sieve;

[0051] (2) Take by weighing metoprolol fumarate and microcrystalline cellulose PH101 of prescription quantity, put in the wet granulator and mix uniformly;

[0052] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft material;

[0053] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0054] (5) spheronization, the spheronization speed is 800~1000rpm, drying in the fluidized bed;

[0055] (6) Sieve, and take ball cores between 16 and 30 mesh...

Embodiment 2

[0078] Example 2 Metoprolol Fumarate Sustained-release Pellet Capsules Containing 5% Croscarmellose Sodium

[0079] 1. Prescription

[0080] 1. Pill core prescription (1000 capsules)

[0081]

[0082] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0083] 3. Capsule shell size 0 is 1000 capsules.

[0084] Second, the preparation process:

[0085] 1. Ball core preparation process:

[0086] (1) Metoprolol fumarate is passed through a 60 mesh sieve;

[0087] (2) Take by weighing metoprolol fumarate, microcrystalline cellulose PH101, croscarmellose sodium of recipe quantity, put in the wet granulator and mix uniformly;

[0088] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft material;

[0089] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0090] (5) spheronization, the spheronization speed is 800~1000rpm, drying in the fluidized bed;

[0091] (6) Sieve, and take...

Embodiment 3

[0109] Example 3 Metoprolol Fumarate Sustained-release Pellet Capsules Containing 10% Croscarmellose Sodium

[0110] 1. Prescription

[0111] 1. Pill core prescription (1000 capsules)

[0112]

[0113] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0114] 3. Capsule shell size 0 is 1000 capsules.

[0115] Second, the preparation process:

[0116] 1. Ball core preparation process: the same as in Example 2

[0117] 2. Preparation process of sustained-release film coating solution:

[0118] Same as Example 1

[0119] 3. Coating (sustained release film):

[0120] 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 20.3%.

[0121] 4, heat treatment: with embodiment 1

[0122] 5. Fill capsules

[0123] It is obtained by filling the coated pellets into capsules.

[0124] 3. Release, content determination and results

[0125] Measuring meth...

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Abstract

The invention relates to a metoprolol fumarate film-controlled slow-release pellet capsule. A slow-release film of the metoprolol fumarate film-controlled slow-release pellet utilizes Eurdragit RS 30D as a film-formation material. A pellet core of the metoprolol fumarate film-controlled slow-release pellet contains croscarmellose sodium having high expansibility, and also contains a pharmaceutically-acceptable common excipient for the slow-release pellet, wherein preferably, the excipient comprises microcrystalline cellulose, and the pellet core comprises 5 to 20wt% of croscarmellose sodium. The slow-release film comprises Eurdragit RS 30D, triethyl citrate as a plasticizer, and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit RS 30D to triethyl citrate to talcum powder is 30: 3: 4 and a film weight increasing ratio is in a range of 18 to 33%. The metoprolol fumarate film-controlled slow-release pellet comprises the pellet core containing croscarmellose sodium having high water expansibility and thus after absorbing water, the metoprolol fumarate film-controlled slow-release pellet obviously 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 metoprolol fumarate 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 metoprolol fumarate film-controlled sustained-release pellet capsule, in particular to a metoprolol fumarate film-controlled sustained-release pellet core containing croscarmellose sodium The micropill capsule belongs to the field of pharmaceutical preparations. Background technique [0002] Metoprolol fumarate is beta 1 Beta-blockers, by selectively blocking beta 1 Receptors produce therapeutic effects. Combined with statins, it is used to treat hypertension, angina pectoris, myocardial infarction, migraine, etc. The basic clinical requirement for this type of drug is that it can control symptoms for a long time. [0003] Metoprolol fumarate dissolves in water. Novartis has launched metoprolol fumarate osmotic pump controlled-release tablets, which can achieve zero-order release and uniform drug release. The disadvantage is that it uses a semi-permeable membrane composed of polymer materials. Easy aging and large drug r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/16A61K31/205A61K31/138A61K47/38A61P9/12A61P9/10A61P25/06
Inventor 姜庆伟衣伟锋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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