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Novel skeleton sustained release tablet containing metoprolol succinate

A technology of metoprolol succinate and toprolol succinate, which is applied in the field of novel matrix sustained-release tablets, can solve the problems of large residues, unachieved, inability to effectively control drug release, etc., and achieves low cost, large Economic benefits, suitable for industrialized large-scale production

Active Publication Date: 2011-04-13
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When using the USP30 method, the sampling time is 1h, 4h, 8h and 20h to measure its release. It can be seen from the release data that the 4h and 8h release exceeds the reasonable release limit, indicating that the technology used in this preparation cannot Effectively controlled drug release,
[0014] India's Emcure Company has launched S-metoprolol succinate sustained-release tablets in India, which are traditional matrix sustained-release tablets. The actual test results show that the release effect in the early stage (1-8h) is acceptable, but the middle and late stages are slow. At 20h, the residue is very large, and the 20h cumulative release of its 25mg and 50mg extended-release tablets has not even reached 80%

Method used

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  • Novel skeleton sustained release tablet containing metoprolol succinate
  • Novel skeleton sustained release tablet containing metoprolol succinate
  • Novel skeleton sustained release tablet containing metoprolol succinate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Example 1 S-metoprolol succinate double-layer matrix sustained-release tablet with auxiliary layer

[0081] 1. Prescription

[0082] 1. Tablet core prescription:

[0083] Slow release layer:

[0084]

[0085] Auxiliary layer:

[0086]

[0087]

[0088] 2. Prescription of film coating solution

[0089] Xiaolun Coating Powder 10g

[0090] water 100ml

[0091] Makes 100ml

[0092] 2. Detailed preparation process

[0093] 1. Preparation process of S-metoprolol succinate tablet core:

[0094] The tablet core is a double-layer tablet, one layer is a slow-release layer, and the other layer is an auxiliary layer. The preparation process is as follows:

[0095] Slow release layer:

[0096] (1) S-metoprolol succinate, hypromellose K4M, hypromellose K15M, and stearic acid are respectively passed through a 60-mesh sieve;

[0097] (2) take prescription amount) S-metoprolol succinate, hypromellose K4M, hypromellose K15M, micropowder silica gel,...

Embodiment 2

[0114] Example 2 S-metoprolol succinate double-layer matrix sustained-release tablet with auxiliary layer

[0115] 1. Prescription

[0116] 1. The prescriptions of the slow-release layer and the auxiliary layer are shown in Table 8 below

[0117] 2, the prescription of film coating coating liquid is the same as embodiment 1.

[0118] 2. Preparation process

[0119] With embodiment 1, difference is that the hypromellose of auxiliary layer is K4M and / or K100.

[0120] 3. Release test: according to the United States Pharmacopoeia USP30 Metoprolol Succinate Sustained Release Tablets standard, the results are shown in Table 9:

[0121] Table 8 Embodiment 2 prescription and release result

[0122]

[0123]

[0124] Table 9 embodiment 2 release test result

[0125]

[0126] 4

[0127] The above test results show that the S-metoprolol succinate double-layer matrix sustained-release tablets with an auxiliary layer have ideal release behaviors in all spec...

Embodiment 3

[0128] Example 3 Metoprolol succinate double-layer matrix sustained-release tablet with auxiliary layer

[0129] 1. Prescription

[0130] 1. See Table 10 below for the prescriptions of the slow-release layer and the auxiliary layer

[0131] 2, the prescription of film coating coating liquid is the same as embodiment 1.

[0132] 2. Preparation process

[0133] With embodiment 1, difference is that the hypromellose of auxiliary layer is K4M and K100.

[0134] 3. Release test: according to the United States Pharmacopoeia USP30 Metoprolol Succinate Sustained Release Tablets standard, the results are shown in Table 11:

[0135] Table 10 Example 3 tablet core prescription: (1000 tablet quantities, unit: g)

[0136]

[0137] Table 11 embodiment 3 release degree test result

[0138]

[0139] The metoprolol succinate described in this embodiment is R, the S-metoprolol succinate, and the above-mentioned test results show that the R with the auxiliary layer, the S-metoprolol s...

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Abstract

The invention provides a novel skeleton sustained release tablet containing metoprolol succinate, relating to a dual-layer skeleton sustained release tablet with metoprolol succinate of an auxiliary layer capable of assisting in adjusting the release speed. By using a novel skeleton sustained release tablet technology, the auxiliary layer for assisting in adjusting the release speed is added on the basis of the traditional skeleton piece and a long-acting sustained release tablet of the metoprolol butanedioic acid salt can be successfully prepared. The release speed of the obtained sustained release tablet containing metoprolol succinate amazingly represents favorable linearity and completely meets the United States Pharmacopoeia (USP30) standard. Compared with products of astrazeneca coming into market, the in vitro release behavior of the novel skeleton sustained release tablet is quite close; in addition, the novel skeleton sustained release tablet has simple process and low cost.

Description

technical field [0001] The present invention relates to a novel matrix sustained-release tablet containing metoprolol succinate, in particular to a metoprolol succinate matrix sustained-release tablet with an auxiliary layer that can adjust the release rate. Toprolol succinates include R,S-metoprolol succinate and S-metoprolol succinate. Background technique [0002] Metoprolol (metoprolol) is a selective beta-receptor blocker, the chemical name is 1-[4-(2-methylethyl)phenoxy]-3-isopropylaminopropanol, It is a chiral molecule with 1 chiral carbon atom, and the salts of R, S-metoprolol and S-metoprolol succinate are currently on the market. Clinically, it is mainly used to treat mild and moderate hypertension, stable angina pectoris and arrhythmia. [0003] The earliest metoprolol and its preparations on the market were metoprolol tartrate from AstraZeneca, which was a common tablet (trade name: Betaloc). After the patient takes the ordinary tablet, because of the short el...

Claims

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Application Information

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IPC IPC(8): A61K9/24A61K9/28A61K31/138A61K47/38A61K47/12A61P9/12A61P9/10A61P9/06
CPCA61K31/138A61K9/2086A61P9/06A61P9/10A61P9/12
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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