Losartan potassium membrane controlled-release pellet capsule

Abstract

The invention relates to a losartan potassium membrane controlled-release pellet capsule. The controlled-release film of the pellet adopts Eurdragit NE 30D as a film forming material, the core of the controlled-release pellet contains high-expansibility low-substituted hydroxypropylcellulose and a pharmaceutically-acceptable excipient commonly used for controlled-release pellets, and optimally, the excipient is microcrystalline cellulose, wherein the weight percentage of the low-substituted hydroxypropylcellulose in the core of the controlled-release pellet is 10-40%. The controlled-release film of the controlled-release pellet includes the Eurdragit NE 30D and an anti-adherent talcum powder, the optimal ratio of the Eurdragit NE 30D to the talcum powder is 30:6, and the optimal coating weight gain is 19-36%. The core will obviously expand after absorbing water because of the containment of the low-substituted hydroxypropylcellulose highly expanding after contacting with water, so the controlled-release film is stretched, the thickness of the film is thinned, the apertures of water-pervious micro-pores are increased, the permeability is good, and the permeability decrease caused by film ageing is compensated, thereby the middle and later stage release speed is basically constant, the last stage residue is small, and a stable release performance is always maintained prior to the expiration date.

Description

technical field

[0001] The invention relates to a losartan potassium membrane-controlled sustained-release pellet capsule, in particular to a losartan potassium membrane-controlled sustained-release pellet capsule containing low-substituted hydroxypropyl cellulose in the pellet core, belonging to the field of pharmaceutical preparations . Background technique

[0002] Losartan potassium is an angiotensin II receptor (AT1 type) antagonist, which can block various pharmacological effects of endogenous and exogenous angiotensin II by selectively acting on AT1 receptors (Including promoting vasoconstriction, aldosterone release, etc.), for the treatment of high blood pressure. The basic clinical requirement for this type of drug is that it can control symptoms for a long time.

[0003] Losartan Potassium is dissolved in water, and Merck & Co. has launched Losartan Potassium Common Tablets (trade name: Cozaar) administered once a day. Losartan potassium is a prodrug with a sho...

Examples

Embodiment 1

[0028] The losartan potassium slow-release pellet capsule of embodiment 1 common ball core

[0029] 1. Prescription

[0030] 1. Pill core prescription (1000 capsules)

[0031]

[0032] 2. Prescription of sustained-release film coating solution

[0033]

[0034]

[0035] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0036] Second, the preparation process:

[0037] 1. Ball core preparation process:

[0038] (1) Losartan potassium is passed through a 60 mesh sieve;

[0039](2) Losartan Potassium and Microcrystalline Cellulose PH101 are taken by weighing recipe quantity, put in wet granulator and mix homogeneously;

[0040] (3) soft material made of 1% sodium carboxymethyl cellulose aqueous solution;

[0041] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0042] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the fluidized bed;

[0043] (6) Sieve, and take ball cores between...

Embodiment 2

[0069] Example 2 Losartan Potassium Sustained-release Pellet Capsules Containing 10% Low-substituted Hypromellose

[0070] 1. Prescription

[0071] 1. Pill core prescription (1000 capsules)

[0072]

[0073] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0074] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0075] Second, the preparation process:

[0076] 1. Ball core preparation process:

[0077] (1) Losartan potassium is passed through a 60 mesh sieve;

[0078] (2) Losartan Potassium, microcrystalline cellulose PH101, low-substituted hydroxypropyl cellulose are taken by weighing recipe quantity, put in wet granulator and mix homogeneously;

[0079] (3) soft material made of 1% sodium carboxymethyl cellulose aqueous solution;

[0080] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0081] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the flu...

Embodiment 3

[0100] Example 3 Losartan Potassium Sustained-release Pellet Capsules Containing 20% ​​Low-substituted Hypromellose

[0101] 1. Prescription

[0102] 1. Pill core prescription (1000 capsules)

[0103]

[0104] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0105] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0106] Second, the preparation process:

[0107] 1. Ball core preparation process: the same as in Example 2

[0108] 2. Preparation process of sustained-release film coating solution:

[0109] Same as Example 1

[0110]3. Coating (sustained release film):

[0111] 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 21.3% and 27.5%.

[0112] 4, heat treatment: with embodiment 1

[0113] 5. Fill capsules

[0114] The coated micropills are filled into capsules to obtain losartan potassium sustained-release micropill ...

technical field

[0001] The invention relates to a losartan potassium membrane-controlled sustained-release pellet capsule, in particular to a losartan potassium membrane-controlled sustained-release pellet capsule containing low-substituted hydroxypropyl cellulose in the pellet core, belonging to the field of pharmaceutical preparations . Background technique

[0002] Losartan potassium is an angiotensin II receptor (AT1 type) antagonist, which can block various pharmacological effects of endogenous and exogenous angiotensin II by selectively acting on AT1 receptors (Including promoting vasoconstriction, aldosterone release, etc.), for the treatment of high blood pressure. The basic clinical requirement for this type of drug is that it can control symptoms for a long time.

[0003] Losartan Potassium is dissolved in water, and Merck & Co. has launched Losartan Potassium Common Tablets (trade name: Cozaar) administered once a day. Losartan potassium is a prodrug with a sho...

Examples

Embodiment 1

[0028] The losartan potassium slow-release pellet capsule of embodiment 1 common ball core

[0029] 1. Prescription

[0030] 1. Pill core prescription (1000 capsules)

[0031]

[0032] 2. Prescription of sustained-release film coating solution

[0033]

[0034]

[0035] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0036] Second, the preparation process:

[0037] 1. Ball core preparation process:

[0038] (1) Losartan potassium is passed through a 60 mesh sieve;

[0039](2) Losartan Potassium and Microcrystalline Cellulose PH101 are taken by weighing recipe quantity, put in wet granulator and mix homogeneously;

[0040] (3) soft material made of 1% sodium carboxymethyl cellulose aqueous solution;

[0041] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0042] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the fluidized bed;

[0043] (6) Sieve, and take ball cores between...

Embodiment 2

[0069] Example 2 Losartan Potassium Sustained-release Pellet Capsules Containing 10% Low-substituted Hypromellose

[0070] 1. Prescription

[0071] 1. Pill core prescription (1000 capsules)

[0072]

[0073] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0074] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0075] Second, the preparation process:

[0076] 1. Ball core preparation process:

[0077] (1) Losartan potassium is passed through a 60 mesh sieve;

[0078] (2) Losartan Potassium, microcrystalline cellulose PH101, low-substituted hydroxypropyl cellulose are taken by weighing recipe quantity, put in wet granulator and mix homogeneously;

[0079] (3) soft material made of 1% sodium carboxymethyl cellulose aqueous solution;

[0080] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0081] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the flu...

Embodiment 3

[0100] Example 3 Losartan Potassium Sustained-release Pellet Capsules Containing 20% ​​Low-substituted Hypromellose

[0101] 1. Prescription

[0102] 1. Pill core prescription (1000 capsules)

[0103]

[0104] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0105] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0106] Second, the preparation process:

[0107] 1. Ball core preparation process: the same as in Example 2

[0108] 2. Preparation process of sustained-release film coating solution:

[0109] Same as Example 1

[0110]3. Coating (sustained release film):

[0111] 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 21.3% and 27.5%.

[0112] 4, heat treatment: with embodiment 1

[0113] 5. Fill capsules

[0114] The coated micropills are filled into capsules to obtain losartan potassium sustained-release micropill ...

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