Levamlodipine besylate tablet, preparation process thereof and control method for relevant materials

Abstract

The invention relates to a levamlodipine besylate tablet, a preparation process thereof and a control method for relevant materials. Each 1000 levamlodipine besylate tablets provided by the invention comprise the following compositions: 2.5g of levamlodipine besylate (measured in besylate), 30 to 50g of lactose (as a filler), 20 to 40g of beta-cyclodextrin (as an inclusion agent), 25 to 45g of microcrystalline cellulose (as a disintegrating agent), 5 to 15g of cross-linked polyvinylpyrrolidone (as a disintegrating agent), 1 to 2g of magnesium stearate (as lubricant), and 50 to 80g of 2.5% HPMC (hydroxypropyl methylcellulose) and 50% ethanol (as an adhesive). The levamlodipine besylate tablet provided by the invention has the advantages of making multi-item improvements on the properties of the levamlodipine besylate, increasing the solubility and apparent dissolution rate of the tablet, improving the stability of the tablet, reducing the excitability of the tablet, significantly reducing the limit of the relevant material, and having better clinical treatment effect, so that the blood pressure lowering of the patient with hypertension is more stable.

Description

technical field

[0001] The invention belongs to the field of western medicine preparations, and relates to a new dosage form of levamlodipine, in particular to a levamlodipine besylate tablet, its preparation and a control method for related substances. Background technique

[0002] Levoamlodipine besylate is the left-handed form of amlodipine besylate, which is currently a commonly used drug for the treatment of hypertension. Levoamlodipine Besylate Tablets have two clinical effects: (1) hypertension, for mild and moderate hypertensive patients (used alone or in combination with other drugs); (2) angina pectoris, especially spontaneous angina pectoris (alone or in combination with other drugs). Levoamlodipine besylate is well tolerated, and the side effects caused by the combination with other cardiovascular drugs are small, long-acting, slowly absorbed, and gradually produce vasodilator effects.

[0003] Chiral pharmaceuticals are at the forefront of the pharmaceutical i...

Examples

Embodiment 1

[0036] Embodiment one: levamlodipine besylate tablet

[0037] A kind of levamlodipine besylate tablet described in the present embodiment, every 1000 contains following components:

[0038] Levoamlodipine besylate 2.5g, calculated as levamlodipine;

[0039] Lactose 45.5g as filler;

[0040] β-cyclodextrin 20g, as inclusion agent;

[0041] Microcrystalline cellulose 45g, as a disintegrant;

[0042]Cross-linked polyvinylpyrrolidone 5g, as a disintegrant;

[0043] Magnesium stearate 1g, as a lubricant;

[0044] 2.5% hypromellose-50% ethanol 50g, as a binder.

[0045] The preparation method of the levamlodipine besylate sheet described in the present embodiment may further comprise the steps:

[0046] A) Weigh levamlodipine besylate and β-cyclodextrin according to the component content of 1000 tablets, add 2 to 5 times the amount of purified water to β-cyclodextrin and grind evenly, and mix levamlodipine besylate Soluble in 95% ethanol, fully mix the dissolved β-cyclodextri...

Embodiment 2

[0054] Embodiment two: levamlodipine besylate tablet

[0055] A kind of levamlodipine besylate tablet described in the present embodiment, every 1000 contains following components:

[0056] Levoamlodipine besylate 2.5g, calculated as levamlodipine;

[0057] Lactose 30g, as filler;

[0058] β-cyclodextrin 40g, as inclusion agent;

[0059] Microcrystalline cellulose 30g, as a disintegrant;

[0060] Cross-linked polyvinylpyrrolidone 15g, as a disintegrant;

[0061] Magnesium stearate 1.5g, as a lubricant;

[0062] 2.5% hypromellose-50% ethanol 60g, as a binder.

[0063] The preparation method of this embodiment is the same as that of Embodiment 1.

Embodiment 3

[0064] Embodiment Three: Levoamlodipine Besylate Tablets

[0065] A kind of levamlodipine besylate tablet described in the present embodiment, every 1000 contains following components:

[0066] Levoamlodipine besylate 2.5g, calculated as levamlodipine;

[0067] Lactose 50g, as filler;

[0068] β-cyclodextrin 29.5g, as inclusion agent;

[0069] Microcrystalline cellulose 25g, as a disintegrant;

[0070] Cross-linked polyvinylpyrrolidone 10g, as a disintegrant;

[0071] Magnesium stearate 2g, as a lubricant;

[0072] 2.5% hypromellose-50% ethanol 80g, as a binder.

[0073] The preparation method of this embodiment is the same as that of Embodiment 1.

technical field

[0001] The invention belongs to the field of western medicine preparations, and relates to a new dosage form of levamlodipine, in particular to a levamlodipine besylate tablet, its preparation and a control method for related substances. Background technique

[0002] Levoamlodipine besylate is the left-handed form of amlodipine besylate, which is currently a commonly used drug for the treatment of hypertension. Levoamlodipine Besylate Tablets have two clinical effects: (1) hypertension, for mild and moderate hypertensive patients (used alone or in combination with other drugs); (2) angina pectoris, especially spontaneous angina pectoris (alone or in combination with other drugs). Levoamlodipine besylate is well tolerated, and the side effects caused by the combination with other cardiovascular drugs are small, long-acting, slowly absorbed, and gradually produce vasodilator effects.

[0003] Chiral pharmaceuticals are at the forefront of the pharmaceutical i...

Examples

Embodiment 1

[0036] Embodiment one: levamlodipine besylate tablet

[0037] A kind of levamlodipine besylate tablet described in the present embodiment, every 1000 contains following components:

[0038] Levoamlodipine besylate 2.5g, calculated as levamlodipine;

[0039] Lactose 45.5g as filler;

[0040] β-cyclodextrin 20g, as inclusion agent;

[0041] Microcrystalline cellulose 45g, as a disintegrant;

[0042]Cross-linked polyvinylpyrrolidone 5g, as a disintegrant;

[0043] Magnesium stearate 1g, as a lubricant;

[0044] 2.5% hypromellose-50% ethanol 50g, as a binder.

[0045] The preparation method of the levamlodipine besylate sheet described in the present embodiment may further comprise the steps:

[0046] A) Weigh levamlodipine besylate and β-cyclodextrin according to the component content of 1000 tablets, add 2 to 5 times the amount of purified water to β-cyclodextrin and grind evenly, and mix levamlodipine besylate Soluble in 95% ethanol, fully mix the dissolved β-cyclodextri...

Embodiment 2

[0054] Embodiment two: levamlodipine besylate tablet

[0055] A kind of levamlodipine besylate tablet described in the present embodiment, every 1000 contains following components:

[0056] Levoamlodipine besylate 2.5g, calculated as levamlodipine;

[0057] Lactose 30g, as filler;

[0058] β-cyclodextrin 40g, as inclusion agent;

[0059] Microcrystalline cellulose 30g, as a disintegrant;

[0060] Cross-linked polyvinylpyrrolidone 15g, as a disintegrant;

[0061] Magnesium stearate 1.5g, as a lubricant;

[0062] 2.5% hypromellose-50% ethanol 60g, as a binder.

[0063] The preparation method of this embodiment is the same as that of Embodiment 1.

Embodiment 3

[0064] Embodiment Three: Levoamlodipine Besylate Tablets

[0065] A kind of levamlodipine besylate tablet described in the present embodiment, every 1000 contains following components:

[0066] Levoamlodipine besylate 2.5g, calculated as levamlodipine;

[0067] Lactose 50g, as filler;

[0068] β-cyclodextrin 29.5g, as inclusion agent;

[0069] Microcrystalline cellulose 25g, as a disintegrant;

[0070] Cross-linked polyvinylpyrrolidone 10g, as a disintegrant;

[0071] Magnesium stearate 2g, as a lubricant;

[0072] 2.5% hypromellose-50% ethanol 80g, as a binder.

[0073] The preparation method of this embodiment is the same as that of Embodiment 1.

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