Metoprolol succinate sustained-release tablet and preparation method thereof

A technology of metoprolol succinate and sustained-release tablets, which can be applied to pharmaceutical formulations, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., and can solve the differences in drug release and release consistency defects, etc. problems, to achieve the effect of simplifying the production process, reducing the difficulty of process amplification, and reducing environmental pollution

Active Publication Date: 2022-01-14

北京联嘉医药科技开发有限公司

4 Cites 0 Cited by

AI-Extracted Technical Summary

Problems solved by technology

Our research found that the in vitro drug release of such sustained-release tablets will have significant differences before and after ...

Abstract

The present invention provides a metoprolol succinate sustained-release tablet and a preparation method thereof. Metoprolol succinate sustained-release particles are firstly prepared by adopting a hot melting process, and then the metoprolol succinate sustained-release tablet is prepared by granulating and tabletting the sustained-release particles, a disintegrating agent and other additional auxiliary materials. The metoprolol succinate sustained-release tablet provided by the invention has dissolution consistency before and after breaking under the condition that the metoprolol succinate sustained-release tablet is broken off by a patient according to the doctor's advice, can avoid the problem that a sustained-release particle coating layer in the existing sustained-release tablet is easy to break during tablet pressing, can significantly simplify the production process, and reduces the manufacturing cost of a unit preparation, and the clinical medication requirements under the condition of medical insurance cost control in China are met.

Application Domain

Organic active ingredientsPharmaceutical non-active ingredients +2

Technology Topic

Biomedical engineeringPharmaceutical Aids +7

Image

Examples

Experimental program(4)
Comparison scheme(3)

Example Embodiment

[0053] Example 1

[0054] Metoprolol succinate hot-melt particles with different compositions and their preparation

[0055] Weigh the components in the recipe quantities of F3-1 to F3-6, mix the components uniformly, and prepare the premix by hot-melt extrusion process at 100-110° C. to prepare slow-release granules. The compositions of the hot-melt particles F3-1 to F3-6 are shown in Table 5.

[0056]

[0057] Weigh a certain amount of metoprolol succinate hot-melt granules from F3-1 to F3-6 (equivalent to 47.5 mg of metoprolol succinate), and measure the release degree of each prescription hot-melt granule within 24 hours. . The results show that the hot-melt granules of metoprolol succinate prepared with the selected melting material can achieve sustained release effect in the 24-hour in vitro dissolution test. It can be used for the preparation of sustained-release solid preparations such as capsules or tablets.

[0058]

Example Embodiment

[0065] Example 2

[0066] Preparation of Metoprolol Succinate Sustained-Release Tablets by Direct Compression Process Using Hot Melt Granules

[0067] Using the metoprolol succinate hot-melt granules prepared in Example 1, take each component of F5-1 to F5-6 recipe quantities according to Table 9, mix each component except the lubricant in each recipe, then Mix again with the external lubricant, and use a punching tool with a score to directly compress the tablet after fully mixing to prepare the sustained-release metoprolol succinate tablets F5-1 to F5-6.

[0068]

[0069] Take metoprolol succinate sustained-release tablets F5-1 to F5-6, and measure the release degrees of the sustained-release tablets before and after being split along the direction of the score respectively. The measurement results are shown in Table 10. The results showed that Metoprolol Succinate Sustained-Release Tablets F5-1 to F5-6 exhibited sustained-release effect in the 24-hour in vitro dissolution test, and the release rate did not change significantly before and after the split, and the similar factor f 2 ≥50.

[0070]

Example Embodiment

[0071] Example 3

[0072] Preparation of Metoprolol Succinate Sustained-Release Tablets by Wet Granulation Process Using Hot Melt Granules

[0073] Weigh the hot-melt granules F3-4 prepared in Example 1, lactose, and pregelatinized starch according to the prescription in Table 11. After fully mixing, use PVP K29/32 aqueous solution for wet granulation. The obtained wet granulation granules are dried, passed through Sieve, then pulverize the particles on the screen, and finally mix the particles under the screen, the pulverized particles on the screen with the external lubricant stearic acid, and use a punch with a score to perform tablet compression to prepare metoprolol succinate. Sustained release tablet F6-1.

[0074]

[0075] Take metoprolol succinate sustained-release tablet F6-1, and measure the release degree of the sustained-release tablet before and after it is split along the notch direction, and the measurement results are shown in Table 12. The results showed that Metoprolol Succinate Sustained-Release Tablets F6-1 exhibited sustained-release effect in the 24-hour in vitro dissolution test, and the release rate did not change significantly before and after splitting, and the similar factor f 2 ≥50.

[0076]

PUM

Description & Claims & Application Information

We can also present the details of the Description, Claims and Application information to help users get a comprehensive understanding of the technical details of the patent, such as background art, summary of invention, brief description of drawings, description of embodiments, and other original content. On the other hand, users can also determine the specific scope of protection of the technology through the list of claims; as well as understand the changes in the life cycle of the technology with the presentation of the patent timeline. Login to view more.

Classification and recommendation of technical efficacy words

Simple production process

Metoprolol succinate sustained-release tablet and preparation method thereof

AI-Extracted Technical Summary

Problems solved by technology

Abstract

Image

Examples

Example Embodiment

Example Embodiment

Example Embodiment

PUM

Description & Claims & Application Information

Similar technology patents

Drag reducer and preparation method thereof

Method of recovering manganese sulfate from low-grade manganese carbonate and manganese oxide

Packaging method of LED (light-emitting diode) flexible lamp strip

Biaxially oriented nylon film (BOPA) matt film and manufacturing method thereof

Micro USB (universal serial bus) receptacle

Classification and recommendation of technical efficacy words

Waste rubber powder/styrene-butadiene-styrene (SBS) composite modified asphalt and production process thereof

Preparation method of NdFeB magnet with high coercivity

Method for synthesizing modified sodium alginate flocculating agent and application of flocculating agent

Production method of composite bimetal pipe

Method for producing outer bag paper of apple fruit growing bag by coating method