Choline fenofibrate film-controlled enteric slow-release pellet capsule

Abstract

The invention relates to a choline fenofibrate film-controlled enteric slow-release pellet capsule. A slow-release film of the choline fenofibrate film-controlled enteric slow-release pellet utilizes Eurdragit RS 30D as a film-formation material. A pellet core of the choline fenofibrate film-controlled enteric slow-release pellet contains low-substituted hydroxypropyl cellulose 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 10 to 40wt% of the low-substituted hydroxypropyl cellulose. 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 urdragit RS 30D to triethyl citrate to talcum powder is 30: 3: 4 and a film weight increasing ratio is in a range of 20 to 38%. The choline fenofibrate film-controlled enteric slow-release pellet comprises the pellet core containing low-substituted hydroxypropyl cellulose having high water expansibility and thus after absorbing water, the choline fenofibrate film-controlled enteric 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 choline fenofibrate film-controlled enteric 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 choline fenofibrate membrane-controlled enteric-coated sustained-release pellet capsule, in particular to a choline fenofibrate membrane-controlled enteric-coated sustained-release capsule containing low-substituted hydroxypropyl cellulose The micropill capsule belongs to the field of pharmaceutical preparations. Background technique

[0002] Choline fenofibrate is a lipid-lowering drug that degrades fat and triglycerides in plasma by activating peroxisome proliferator-activated receptor α (PPAR-α), activating lipolytic enzymes and reducing the synthesis of apolipoprotein CIII The clearance is significantly increased, thereby exerting a lipid-lowering effect. It is used in combination with statins to treat mixed dyslipidemia; single drug is used to treat severe hypertriglyceridemia, etc. The basic clinical requirement for this type of drug is that it can control symptoms for a long time.

[0003] The solubility of choline ...

Examples

Embodiment 1

[0035] Example 1 Choline fenofibrate enteric-coated sustained-release pellet capsules with common ball core

[0036] 1. Prescription

[0037] 1. Pill core prescription (1000 capsules)

[0038]

[0039] 2. Prescription of sustained-release film coating solution

[0040]

[0041]

[0042] 3. Prescription of enteric coating solution

[0043]

[0044] 4. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0045] Second, the preparation process:

[0046] 1. Ball core preparation process:

[0047] (1) Choline fenofibrate is passed through a 60 mesh sieve;

[0048] (2) Take choline fenofibrate and microcrystalline cellulose PH101 of prescription quantity, put in wet granulator and mix uniformly;

[0049] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft materials;

[0050] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0051] (5) spheronization, the spheronization speed is 900~1000rpm,...

Embodiment 2

[0079] Example 2 Choline fenofibrate enteric-coated sustained-release pellet capsule containing 10% low-substituted hydroxypropyl cellulose

[0080] 1. Prescription

[0081] 1. Pill core prescription (1000 capsules)

[0082]

[0083] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0084] 3. Prescription of enteric coating film coating solution: same as Example 1

[0085] 4. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0086] Second, the preparation process:

[0087] 1. Ball core preparation process:

[0088] (1) Choline fenofibrate is passed through a 60 mesh sieve;

[0089] (2) Choline fenofibrate, microcrystalline cellulose PH101, and low-substituted hydroxypropyl cellulose are taken by weighing the prescription amount, and mixed uniformly in a wet granulator;

[0090] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft materials;

[0091] (4) Extrude on the extruder, the screen aperture is 1.0mm,...

Embodiment 3

[0113] Example 3 Choline fenofibrate enteric-coated sustained-release pellet capsules containing 20% ​​low-substituted hydroxypropyl cellulose

[0114] 1. Prescription

[0115] 1. Pill core prescription (1000 capsules)

[0116]

[0117] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0118] 3. Prescription of enteric coating film coating solution: same as Example 1

[0119] 4. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0120] Second, the preparation process:

[0121] 1. Ball core preparation process:

[0122] (1) Choline fenofibrate is passed through a 60 mesh sieve;

[0123] (2) Choline fenofibrate, microcrystalline cellulose PH101, and low-substituted hydroxypropyl cellulose are taken by weighing the prescription amount, and mixed uniformly in a wet granulator;

[0124] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft materials;

[0125] (4) Extrude on the extruder, the screen aperture is 1.0...

technical field

[0001] The invention relates to a choline fenofibrate membrane-controlled enteric-coated sustained-release pellet capsule, in particular to a choline fenofibrate membrane-controlled enteric-coated sustained-release capsule containing low-substituted hydroxypropyl cellulose The micropill capsule belongs to the field of pharmaceutical preparations. Background technique

[0002] Choline fenofibrate is a lipid-lowering drug that degrades fat and triglycerides in plasma by activating peroxisome proliferator-activated receptor α (PPAR-α), activating lipolytic enzymes and reducing the synthesis of apolipoprotein CIII The clearance is significantly increased, thereby exerting a lipid-lowering effect. It is used in combination with statins to treat mixed dyslipidemia; single drug is used to treat severe hypertriglyceridemia, etc. The basic clinical requirement for this type of drug is that it can control symptoms for a long time.

[0003] The solubility of choline ...

Examples

Embodiment 1

[0035] Example 1 Choline fenofibrate enteric-coated sustained-release pellet capsules with common ball core

[0036] 1. Prescription

[0037] 1. Pill core prescription (1000 capsules)

[0038]

[0039] 2. Prescription of sustained-release film coating solution

[0040]

[0041]

[0042] 3. Prescription of enteric coating solution

[0043]

[0044] 4. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0045] Second, the preparation process:

[0046] 1. Ball core preparation process:

[0047] (1) Choline fenofibrate is passed through a 60 mesh sieve;

[0048] (2) Take choline fenofibrate and microcrystalline cellulose PH101 of prescription quantity, put in wet granulator and mix uniformly;

[0049] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft materials;

[0050] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0051] (5) spheronization, the spheronization speed is 900~1000rpm,...

Embodiment 2

[0079] Example 2 Choline fenofibrate enteric-coated sustained-release pellet capsule containing 10% low-substituted hydroxypropyl cellulose

[0080] 1. Prescription

[0081] 1. Pill core prescription (1000 capsules)

[0082]

[0083] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0084] 3. Prescription of enteric coating film coating solution: same as Example 1

[0085] 4. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0086] Second, the preparation process:

[0087] 1. Ball core preparation process:

[0088] (1) Choline fenofibrate is passed through a 60 mesh sieve;

[0089] (2) Choline fenofibrate, microcrystalline cellulose PH101, and low-substituted hydroxypropyl cellulose are taken by weighing the prescription amount, and mixed uniformly in a wet granulator;

[0090] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft materials;

[0091] (4) Extrude on the extruder, the screen aperture is 1.0mm,...

Embodiment 3

[0113] Example 3 Choline fenofibrate enteric-coated sustained-release pellet capsules containing 20% ​​low-substituted hydroxypropyl cellulose

[0114] 1. Prescription

[0115] 1. Pill core prescription (1000 capsules)

[0116]

[0117] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0118] 3. Prescription of enteric coating film coating solution: same as Example 1

[0119] 4. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0120] Second, the preparation process:

[0121] 1. Ball core preparation process:

[0122] (1) Choline fenofibrate is passed through a 60 mesh sieve;

[0123] (2) Choline fenofibrate, microcrystalline cellulose PH101, and low-substituted hydroxypropyl cellulose are taken by weighing the prescription amount, and mixed uniformly in a wet granulator;

[0124] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft materials;

[0125] (4) Extrude on the extruder, the screen aperture is 1.0...

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