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Time-controlled release MT (metoprolol tartrate) pellets and preparation method thereof

A technology of metoprolol tartrate and tartaric acid, which is applied in directions such as pharmaceutical formulations, microcapsules, and drug combinations, can solve problems such as unsatisfactory drug release speed and limited pore-forming ability.

Inactive Publication Date: 2016-06-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ethyl cellulose forms a dense film and has certain toughness, while conventional water-soluble porogens have limited pore-forming ability, so the drug release rate with time lag is not ideal.

Method used

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  • Time-controlled release MT (metoprolol tartrate) pellets and preparation method thereof
  • Time-controlled release MT (metoprolol tartrate) pellets and preparation method thereof
  • Time-controlled release MT (metoprolol tartrate) pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] a. Prescription and preparation of metoprolol tartrate drug-loaded pellets (1000 grains):

[0050]

[0051] Preparation process: HPMC is added to 80% ethanol solution of metoprolol tartrate, and talcum powder is added under continuous stirring. A fluidized bed is used to apply the drug in the way of bottom spraying, and after the drug application is completed, the fluidized drying is continued at 39° C. for 2 hours to prepare the drug-loaded pellets.

[0052] B, prescription and preparation of metoprolol tartrate swelling layer pellets (1000 grains):

[0053] CC-Na: 56.875g

[0054] PVPK90: 8.125g

[0055] Preparation process: disperse croscarmellose sodium in water, dissolve polyvinylpyrrolidone K90 in ethanol, and mix the two solutions to obtain a swelling layer coating solution. Fluidized bed coating is adopted, and the swelling layer is coated on the drug-loaded pellet core by bottom spraying technology.

[0056] C, prescription and preparation of metoprolol ...

Embodiment 2

[0060] a. Prescription and preparation of metoprolol tartrate drug-loaded pellets (1000 grains):

[0061]

[0062] B, prescription and preparation of metoprolol tartrate swelling layer pellets (1000 grains):

[0063] CC-Na: 56.875g

[0064] PVPK90: 8.125g

[0065] C, prescription and preparation of metoprolol tartrate time-released pellets (1000 grains):

[0066]

[0067] The preparation method is the same as in Example 1.

Embodiment 3

[0069] a. Prescription and preparation of metoprolol tartrate drug-loaded pellets (1000 grains):

[0070]

[0071] B, prescription and preparation of metoprolol tartrate swelling layer pellets (1000 grains):

[0072] CC-Na: 56.875g

[0073] PVPK90: 8.125g

[0074] C, prescription and preparation of metoprolol tartrate time-released pellets (1000 grains):

[0075]

[0076] The preparation method is the same as in Example 1.

[0077] Table 1 Embodiment 1~3 cumulative release (%)

[0078] time (h)

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PUM

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Abstract

The present invention relates to a kind of metoprolol tartrate time-selected drug release pellet and preparation method thereof, the preparation is a multi-layer coated pellet preparation, the basic structure from inside to outside is respectively a blank pellet core, a drug layer, a swelling layer, Lag layer. Wherein, the drug layer contains metoprolol tartrate, adhesive and anti-sticking agent. The swelling layer consists of a disintegrant and a binder. A non-water-soluble pore-forming agent and a water-soluble pore-forming agent are added to an ethylcellulose organic solvent as a lagging layer coating liquid. Time-selective drug release pellets were prepared by fluidized bed coating technology. The metoprolol tartrate timed-release pills provided by the invention have obvious timed-release characteristics, can guarantee a 4-hour time lag and a faster drug release rate after the time lag, and the drug release amount is greater than 2 hours after the immediate lag. 90%. The auxiliary materials used in the invention are easy to obtain and low in cost, the production process is simple and easy to operate, and the curing time for film formation of the lag layer is saved, which is suitable for industrial production.

Description

technical field [0001] The invention relates to a metoprolol tartrate time-selected drug release pellet and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] With the development of chronopharmacology, it has been found that the onset of many diseases shows obvious circadian rhythm changes, especially cardiovascular diseases such as hypertension, angina pectoris, myocardial infarction, and the morbidity and mortality of these diseases are highest in the early morning. In order to effectively prevent and treat these diseases, if it can be administered in the early morning, the therapeutic effect will be better. However, the patient is in a deep sleep state in the early morning, and the compliance of the patient to take the medicine is poor at this time. For some conventional immediate-release preparations or sustained-release preparations, the drug in the preparation is released immediately after administration...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/138A61K47/38A61K47/32A61P9/12A61P9/10
CPCA61K9/5078A61K9/0002A61K9/5026A61K9/5042A61K31/138
Inventor 吴琼珠张歆宗莉戴爽薛夏林王佳佳
Owner CHINA PHARM UNIV
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