A kind of isradipine controlled-release tablet and preparation method thereof

Abstract

The invention provides an isradipine controlled-release tablet and a preparation method thereof, which comprises a double-layer tablet composed of a drug layer and a booster layer, a controlled-release semi-permeable membrane, a drug-release hole and a moisture-proof coat. The drug layer is composed of the main drug isradipine and the carrier, and the carrier mainly includes vinylpyrrolidone and / or vinylpyrrolidone copolymer; the booster layer is mainly composed of permeation enhancers, insoluble polymers and osmotic pressure enhancers, and the controlled-release semi-permeable membrane is mainly composed of Consists of cellulose acetate, plasticizer and porogen. In the invention, the application of the polymer material enables isradipine to be released at a controlled rate after oral administration, so that the preparation achieves the purpose of maintaining the drug release for 24 hours after administration once a day, stabilizes the blood drug concentration, and improves the clinical therapeutic effect of the drug.

Description

technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to a single-chamber double-layer osmotic pump-type controlled-release preparation containing the active drug isradipine and a preparation method thereof, which enables isradipine to release the drug at a controlled rate in the gastrointestinal tract, Realize stable blood drug concentration in the body and improve clinical treatment effect. Background technique

[0002] Isradipine (also known as: Isradipine), chemical name: isopropylmethyl (±)-4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl -3,6-Pyridinedicarboxylate. Isradipine is a new type of dihydropyridine calcium channel blocker, like other dihydropyridine drugs, by blocking the influx of transmembrane calcium ions, it can effectively and selectively inhibit the contraction caused by depolarization in the It plays a role in cardiac muscle and vascular smooth muscle, has high selectivity of blood vessels, and can relax...

Examples

example 1

[0012] The preparation of example 1. isradipine controlled release tablet

[0013] (1) Preparation of double-layer core

[0014] ① drug layer

[0015] Isradipine 5g

[0016] Carbomer 70g

[0017] Povidone 30g

[0018] Silica 1g

[0019] Magnesium Stearate 1g

[0020] Mix the isradipine, carbomer and povidone in the above prescription amount evenly, prepare a soft material with an appropriate amount of 60-80% ethanol, granulate it with a 18-mesh nylon net, and ventilate and dry the prepared granules at 50°C. Then add silicon dioxide and magnesium stearate, mix well, and set aside.

[0021] ② Booster layer

[0022] Low-substituted hydroxypropyl cellulose 30g

[0023] Cross-linked sodium carboxymethyl starch 60g

[0024] Sodium chloride 20g

[0025] Red Iron Oxide 2g

[0026] Silica 1g

[0027] Magnesium Stearate 1g

[0028] Mix the low-substituted hydroxypropyl cellulose, cross-linked carboxymethyl starch sodium, sodium chloride, and red iron oxide in the above pres...

example 2

[0046] The preparation of example 2. isradipine controlled-release tablets

[0047] (1) Preparation of double-layer core

[0048] ① drug layer

[0049] Isradipine 10g

[0050] Carbomer 90g

[0051] Povidone 45g

[0052] Silica 1g

[0053] Magnesium Stearate 1g

[0054] Mix the isradipine, carbomer and povidone in the above prescription amount evenly, prepare a soft material with an appropriate amount of 60-80% ethanol, granulate it with a 18-mesh nylon net, and ventilate and dry the prepared granules at 50°C. Then add silicon dioxide and magnesium stearate, mix well, and set aside.

[0055] ② Booster layer

[0056] Cross-linked sodium carboxymethyl starch 70g

[0057] Hypromellose 40g

[0058] Sodium chloride 22g

[0059] Red Iron Oxide 2g

[0060] Silica 1g

[0061] Magnesium Stearate 1g

[0062] Mix the hydroxypropylmethyl cellulose, cross-linked sodium carboxymethyl starch, sodium chloride, and red iron oxide in the above prescription amount evenly, prepare sof...

technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to a single-chamber double-layer osmotic pump-type controlled-release preparation containing the active drug isradipine and a preparation method thereof, which enables isradipine to release the drug at a controlled rate in the gastrointestinal tract, Realize stable blood drug concentration in the body and improve clinical treatment effect. Background technique

[0002] Isradipine (also known as: Isradipine), chemical name: isopropylmethyl (±)-4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl -3,6-Pyridinedicarboxylate. Isradipine is a new type of dihydropyridine calcium channel blocker, like other dihydropyridine drugs, by blocking the influx of transmembrane calcium ions, it can effectively and selectively inhibit the contraction caused by depolarization in the It plays a role in cardiac muscle and vascular smooth muscle, has high selectivity of blood vessels, and can relax...

Examples

example 1

[0012] The preparation of example 1. isradipine controlled release tablet

[0013] (1) Preparation of double-layer core

[0014] ① drug layer

[0015] Isradipine 5g

[0016] Carbomer 70g

[0017] Povidone 30g

[0018] Silica 1g

[0019] Magnesium Stearate 1g

[0020] Mix the isradipine, carbomer and povidone in the above prescription amount evenly, prepare a soft material with an appropriate amount of 60-80% ethanol, granulate it with a 18-mesh nylon net, and ventilate and dry the prepared granules at 50°C. Then add silicon dioxide and magnesium stearate, mix well, and set aside.

[0021] ② Booster layer

[0022] Low-substituted hydroxypropyl cellulose 30g

[0023] Cross-linked sodium carboxymethyl starch 60g

[0024] Sodium chloride 20g

[0025] Red Iron Oxide 2g

[0026] Silica 1g

[0027] Magnesium Stearate 1g

[0028] Mix the low-substituted hydroxypropyl cellulose, cross-linked carboxymethyl starch sodium, sodium chloride, and red iron oxide in the above pres...

example 2

[0046] The preparation of example 2. isradipine controlled-release tablets

[0047] (1) Preparation of double-layer core

[0048] ① drug layer

[0049] Isradipine 10g

[0050] Carbomer 90g

[0051] Povidone 45g

[0052] Silica 1g

[0053] Magnesium Stearate 1g

[0054] Mix the isradipine, carbomer and povidone in the above prescription amount evenly, prepare a soft material with an appropriate amount of 60-80% ethanol, granulate it with a 18-mesh nylon net, and ventilate and dry the prepared granules at 50°C. Then add silicon dioxide and magnesium stearate, mix well, and set aside.

[0055] ② Booster layer

[0056] Cross-linked sodium carboxymethyl starch 70g

[0057] Hypromellose 40g

[0058] Sodium chloride 22g

[0059] Red Iron Oxide 2g

[0060] Silica 1g

[0061] Magnesium Stearate 1g

[0062] Mix the hydroxypropylmethyl cellulose, cross-linked sodium carboxymethyl starch, sodium chloride, and red iron oxide in the above prescription amount evenly, prepare sof...

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