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Metoprolol Tartaric Acid and Felodipine slow-release double-layer tablet and preparation method thereof

A technology for a sustained-release layer of metoprolol tartrate and torolol, which is applied to sustained-release double-layer tablets and preparation thereof, and the sustained-release double-layer tablet comprising metoprolol tartrate and felodipine and the field of preparation thereof. Solve the problems of damaged coating film, difficult operation, long process, etc., to achieve the effect of being beneficial to industrial production, reliable slow release effect and cost saving

Active Publication Date: 2013-03-27
BEIJING RED SUN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The defect that this technology exists comprises: 1, need to make pellet and to pellet coating, equipment and production process are complicated, flow process is long
2. There is a difference in particle size between coated pellets and felodipine, which requires high mixing uniformity, while the uniformity of the slow-release material is directly related to the release uniformity of felodipine, and the operation is difficult
3. Coated granules are subjected to huge pressure during tablet compression, which will cause damage to the coating film and affect the sustained release effect of the drug
Therefore, it is necessary to accurately grasp the pressure during the pressing process, which further complicates the preparation process.

Method used

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  • Metoprolol Tartaric Acid and Felodipine slow-release double-layer tablet and preparation method thereof
  • Metoprolol Tartaric Acid and Felodipine slow-release double-layer tablet and preparation method thereof
  • Metoprolol Tartaric Acid and Felodipine slow-release double-layer tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1 sustained-release double-layer tablet prescription (1000 tablets amount)

[0045] Metoprolol tartrate layer:

[0046] Metoprolol Tartrate 50g

[0047] Ethylcellulose powder 150g

[0048] 30% (g / L) ethyl cellulose aqueous suspension 80g

[0049] Hydroxypropyl methylcellulose (viscosity 100000cp) 130g

[0050] Hydroxypropyl methylcellulose (viscosity 50cp) 50g

[0051] Magnesium Stearate 4.6g

[0052] Felodipine layer:

[0053] Felodipine 5g

[0054] Povidone k29 / 32 45g

[0055] Hydroxypropyl methylcellulose (viscosity 15000cp) 30g

[0056] Hydroxypropyl methylcellulose (viscosity 50cp) 30g

[0057] Lactose 190g

[0058] Magnesium Stearate 3g

[0059] Coating solution:

[0060] Hydroxypropyl methylcellulose (viscosity 50cp) 20g

[0061] Titanium dioxide 16g

[0062] Talc powder 20g

[0063] Polysorbate 80 8g

[0064] Ethanol 400g

[0065] 500ml of water.

Embodiment 2

[0066] Embodiment 2 Preparation of Metoprolol Felodipine Tartrate Sustained-release Double-Layer Tablet

[0067] According to the distribution ratio of each component shown in the prescription of Example 1, respectively prepare metoprolol tartrate sustained-release layer granules and felodipine sustained-release layer granules, and then use the mold to compress them into double-layer tablets, and take the double-layer tablets Place the formulation in a coating pan, blow hot air to 30-40°C, adjust the spray speed to coat, increase the weight of the double-layer tablet by 2%, and dry and solidify the coated tablet to obtain the finished product.

[0068] Concrete preparation process is as follows:

[0069] The preparation technology of metoprolol tartrate sustained-release layer granule comprises the following steps:

[0070] (1) Metoprolol tartrate is crossed 80 mesh sieves, for subsequent use;

[0071] (2) Metoprolol tartrate and ethyl cellulose powder of prescription quanti...

Embodiment 3

[0080] The selection of embodiment 3 metoprolol tartrate sustained-release layer formula

[0081] Considering the high solubility of metoprolol tartrate in water, first granulate metoprolol tartrate with water-insoluble material-ethyl cellulose, and then use high-viscosity hydroxypropyl methylcellulose to prepare slow release layer.

[0082] Make 5 grams of metoprolol tartrate and ethyl cellulose through a 80-100 mesh sieve to make a soft material, granulate, dry, and granulate, and then mix the obtained granules with hydroxypropyl methylcellulose evenly, and then add Magnesium stearate.

[0083] The influence of factors such as the addition forms of different ethyl cellulose, different viscosities of hydroxypropyl methylcellulose, and the amount of hydroxypropyl methylcellulose were investigated. The screening results are as follows:

[0084] Table 1 Screening of the prescription of metoprolol tartrate sustained-release layer

[0085]

[0086] Note: EC-ethyl cellulose; ...

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Abstract

The invention provides a Metoprolol Tartaric Acid and Felodipine slow-release double-layer tablet and its preparation method. The slow-release double-layer tablet comprises a Metoprolol Tartaric Acid slow-release layer containing, by weight, 50 parts of Metoprolol Tartaric Acid, 100-150 parts of an ethyl cellulose powder, 24-30 parts of ethyl cellulose in the form of an ethyl cellulose aqueous suspension and 130-230 parts of hydroxypropyl methyl cellulose; and a Felodipine slow-release layer containing 5 parts of Felodipine and 60 parts of hydroxypropyl methyl cellulose. By adjusting the ingredients and their ratio in the Metoprolol Tartaric Acid slow-release layer and the Felodipine slow-release layer, the release speeds of medicament layers can cooperate with each other and the slow-release effect is more reliable, thus reaching a good curative effect; in addition, it is ensured that the medicament layers can be smoothly compacted to form a double-layer tablet, and the hidden trouble of damaged coating particles can be avoided. The preparation method provided by the invention mainly employs the double-layer tablet compacting technology with simple equipment, can save cost and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a slow-release double-layer tablet and a preparation method thereof, in particular to a slow-release double-layer tablet containing metoprolol tartrate and felodipine and a preparation method thereof. Background technique [0002] Felodipine is a vasoselective calcium antagonist used in the treatment of hypertension and stable angina. Felodipine belongs to dihydropyridine derivatives, which inhibits the electrical behavior and contraction behavior of vascular smooth muscle by acting on calcium ion channels on the cell membrane, thereby reducing peripheral vascular resistance, especially arterial vascular resistance. [0003] Metoprolol is a selective beta 1 receptor blockers. beta below the effect on peripheral blood vessels and respiratory tract 2 At doses at which receptors function, metoprolol can only act on cardiac beta 1 receptor. Metoprolol has no β-receptor a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4422A61K31/205A61K9/24A61K9/36A61P9/12A61P9/10
Inventor 林德良
Owner BEIJING RED SUN PHARMA
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