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Double-layer tablet containing ezetimibe and rosuvastatin and preparation method thereof

A technology of rosuvastatin and ezetimibe, which is applied in the field of compound double-layer tablets, can solve problems such as difficulty in in vitro dissolution, difficult release of ezetimibe, and poor dissolution of ezetimibe. The effect of reducing adverse drug reactions, increasing drug safety, and improving compliance

Active Publication Date: 2014-02-19
WUHAN WUYAO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dosage forms such as soft capsules and powders described in this patent are difficult to meet the requirements technically.
[0006] CN102451161A discloses an example in which ezetimibe and rosuvastatin are prepared into dispersible tablets. Ezetimibe and rosuvastatin are not granulated separately, resulting in ezetimibe affecting rosuvastatin, and related substances increase
And without the use of antioxidants, its stability cannot be guaranteed
[0007] CN103229725A discloses a slow-release double-layer tablet prepared from ezetimibe, statins (including rosuvastatin) and a calcium ion antagonist. Mixing ezetimibe and statins into granulated tablets causes mutual interference, and cannot ensure its stability
In addition, the amlodipine layer is an immediate-release tablet without adding a matrix material. When this layer is released, it will affect the release of the sustained-release layer where ezetimibe and statins are located, making it difficult to reach a consensus on in vitro dissolution.
[0008] CN102357096A discloses a compound tablet of ezetimibe and rosuvastatin, which is characterized in that rosuvastatin granules are prepared first, then ezetimibe is added, and finally compressed into tablets uniformly, although the former can effectively control ezetimibe Interference with rosuvastatin, but after tableting together, a part of rosuvastatin enters the ezetimibe layer under strong pressure, and the internal environment of the ezetimibe layer, such as pH value, excipient ingredients and rosuvastatin The suvastatin layer is different, so that the related substances of rosuvastatin in this part increase greatly. At the same time, ezetimibe is not micronized, so it is difficult to release ezetimibe, which makes the in vitro dissolution rate poor.
[0009] Therefore, inventing a compound tablet of ezetimibe and rosuvastatin, which can not only ensure the stability of rosuvastatin, but also solve the problem of poor dissolution of ezetimibe, is our urgent need to be solved. question

Method used

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  • Double-layer tablet containing ezetimibe and rosuvastatin and preparation method thereof
  • Double-layer tablet containing ezetimibe and rosuvastatin and preparation method thereof
  • Double-layer tablet containing ezetimibe and rosuvastatin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1: A bilayer tablet containing ezetimibe and rosuvastatin and one of its preparations (prescription quantity: 1000 tablets)

[0048]

[0049] Preparation method: Ezetimibe is micronized in advance (see Example 6 for the specific implementation process), passed through a 200-mesh sieve, and the remaining raw and auxiliary materials are respectively passed through an 80-mesh sieve for later use. Ezetimibe layer: put ezetimibe, lactose, microcrystalline cellulose, croscarmellose sodium, and sodium lauryl sulfate into the wet granulator according to the composition ratio of the prescription and mix evenly, add 8 The solution of povidone K30 of % recipe is granulated, dried, granulated with a 20 mesh sieve, added with magnesium stearate and mixed evenly. Rosuvastatin layer: put rosuvastatin, lactose, microcrystalline cellulose, croscarmellose sodium, tert-butyl-4-hydroxyanisole, and meglumine into the wet process according to the composition ratio of the prescript...

Embodiment 2

[0050] Example 2: A bilayer tablet containing ezetimibe and rosuvastatin and its preparation 2 (prescription quantity: 1000 tablets)

[0051]

[0052] Preparation method: Ezetimibe is micronized in advance (see Example 6 for the specific implementation process), and passed through a 200-mesh sieve, and the remaining raw and auxiliary materials are respectively passed through an 80-mesh sieve for later use. Ezetimibe layer: Put ezetimibe, lactose, pregelatinized starch, carboxymethyl starch sodium, and Tween-80 into the wet granulator according to the composition ratio of the prescription and mix them evenly, and add 8% of the prescription amount of polysaccharide The vitamin K90 solution is granulated, dried, sized with a 20-mesh sieve, added with silicon dioxide and mixed evenly. Rosuvastatin layer: put rosuvastatin, lactose, pregelatinized starch, sodium carboxymethyl starch, propyl gallate, and disodium hydrogen phosphate into a wet granulator according to the compositio...

Embodiment 3

[0053] Example 3: A bilayer tablet containing ezetimibe and rosuvastatin and its preparation 3 (prescription quantity: 1000 tablets)

[0054]

[0055] Preparation method: Ezetimibe is micronized in advance (see Example 6 for the specific implementation process), and passed through a 200-mesh sieve, and the remaining raw and auxiliary materials are respectively passed through an 80-mesh sieve for later use. Ezetimibe layer: put ezetimibe, microcrystalline cellulose, pregelatinized starch, crospovidone, and Tween-80 into the wet granulator according to the composition ratio of the prescription and mix evenly, add 10% of the prescription A certain amount of ethyl cellulose solution is granulated, dried, granulated with a 20-mesh sieve, added with glyceryl behenate and mixed evenly to obtain the product. Rosuvastatin layer: granulate rosuvastatin, microcrystalline cellulose, pregelatinized starch, crospovidone, citric acid, sodium hydroxide, and 10% prescription ethylcellulose ...

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Abstract

The invention relates to a double-layer tablet which contains ezetimibe and rosuvastatin serving as effective components and has a lipid-lowering effect and a preparation method thereof. Aiming at the problems poor water solubility of ezetimibe, instability of rosuvastatin to acid and oxygen and the like, the method adopts a micronization technology to improve the dissolution rate of ezetimibe and adopts an anti-oxidizing agent and a double-layer tabletting technology to improve the stability of rosuvastatin in a human body, further, ingredients of a medicine is enabled to take effect sufficiently, and the best synergistic effect is achieved; and a compound preparation agent is mainly applied to treatment of diseases relative to hypercholesteremia.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a compound bilayer tablet with lipid-lowering effect, which uses ezetimibe and rosuvastatin as active components. technical background [0002] Hyperlipidemia is one of the main causes of coronary heart disease and stroke. With the aging of my country's population and the improvement of living standards, patients with hyperlipidemia are also increasing. Clinical studies have shown that elevated levels of total cholesterol, low-density lipoprotein (LDL), and apolipoprotein (Apo) B (the main component of LDL) can lead to atherosclerosis in humans. In addition, decreased levels of high-density lipoprotein (HDL) can also lead to atherosclerosis. Plasma cholesterol is mainly derived from intestinal absorption or endogenous synthesis. The two lipid-lowering compositions, rosuvastatin and ezetimibe, form a complementary mechanism that can reduce the levels of enriched total ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61K9/20A61P3/06A61K31/397
Inventor 杨科冯小路耿海明杨波
Owner WUHAN WUYAO SCI & TECH
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