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Metoprolol oral pulsatile tablet and preparation method and application of metoprolol oral pulsatile tablet

A technology of pulsating and immediate-release tablets, which is applied in the direction of pharmaceutical formulas, medical preparations containing active ingredients, and medical preparations containing active ingredients. It is convenient and feasible to take medicine, improve the treatment effect, and improve the effect of medication compliance

Active Publication Date: 2013-01-16
JINAN UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The time lag of the pulse drug delivery system mentioned in the above related documents and patents is evenly distributed in 3 to 4.5 hours. It is said that patients can only take the above-mentioned pulse preparations at around 12 o'clock in the middle of the night to be clinically effective, and to avoid the rhythm period (2:00~3:00A.M.) of patients' blood pressure lowering at night without causing side effects of hypotension. It is very inconvenient for patients to take medication, resulting in poor medication compliance
[0012] (2) Most of the pulse drug delivery systems mentioned in the above-mentioned relevant documents and patents have complicated prescription designs, such as the reported metoprolol pulse-release pellets, which are usually composed of the main drug immediate-release pellet core, swelling layer and controlled-release layer or by The main drug is composed of immediate-release pellet core, basic layer and hysteresis layer, and the preparation process is cumbersome

Method used

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  • Metoprolol oral pulsatile tablet and preparation method and application of metoprolol oral pulsatile tablet
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  • Metoprolol oral pulsatile tablet and preparation method and application of metoprolol oral pulsatile tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Tablet prescription:

[0053]

[0054]

[0055] Preparation process: After the above-mentioned metoprolol tartrate and auxiliary materials are fully mixed, the powder is directly compressed into tablets to obtain immediate-release tablet cores.

[0056] Controlled release film coating layer coating solution prescription (g / ml):

[0057]

[0058] Preparation process: Prepare the coating liquid according to the coating liquid prescription, and use the pan coating method to coat the prepared tablet cores. The coating temperature is 50° C., the flow rate of the coating liquid is 3.0 ml / min, the rotation speed of the coating pan is 35 rpm, and the coating weight gain rate is 20%. The drug release time lag of the prepared pulse tablet is about 7h, and the time lag is reached, and the average cumulative dissolution percentage of the drug is greater than 90% in 10 minutes. The drug release curve in vitro is shown in figure 1 .

Embodiment 2

[0060] Tablet prescription:

[0061]

[0062] Preparation process: After the above-mentioned metoprolol tartrate and auxiliary materials are fully mixed, the powder is directly compressed into tablets to obtain immediate-release tablet cores.

[0063] Controlled release film coating layer coating solution prescription (g / ml):

[0064]

[0065] Preparation process: the tablet core is coated according to the coating process of Example 1, and the coating weight gain rate is 15%. The drug release time lag of the prepared pulse tablet is about 7h, and the time lag is reached, and the average cumulative dissolution percentage of the drug is greater than 90% in 10 minutes, and the drug release curve in vitro is similar to that of figure 1 The drug release curve is similar, no longer attached drawings.

Embodiment 3

[0067] Tablet prescription:

[0068]

[0069] Preparation process: After the above-mentioned metoprolol tartrate and auxiliary materials are fully mixed, the powder is directly compressed into tablets to obtain immediate-release tablet cores.

[0070] Controlled release film coating layer coating solution prescription (g / ml):

[0071]

[0072] Preparation process: the tablet core is coated according to the coating process of Example 1, and the coating weight gain rate is 12%. The drug release time lag of the prepared pulse tablet is about 7h, the time lag is reached, and the average cumulative dissolution percentage of the drug is greater than 91% in 10 minutes. The drug release curve in vitro is similar to that of figure 1 The drug release curve is similar, no longer attached drawings.

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PUM

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Abstract

The invention discloses a metoprolol oral pulsatile tablet and a preparation method and an application of the metoprolol oral pulsatile tablet. The oral pulsatile tablet comprises a quick release tablet core and a release controlling thin film coating layer. The rate of body weight gain of the release controlling thin film coating layer to the weight of the quick release table core is 1-50%; the quick release table core consists of the basic remedy and the inner accessories, wherein the basic remedy is metoprolol salt, and the dosage form of the basic remedy is 15-100 mg per table based on the metoprolol; and the release controlling thin film coating layer consists of the thin film coating material and the external accessories, wherein the thin film coating material is water-insoluble andalways insoluble under different pH. The lag time of the pulsatile tablet can be controlled to fluctuate within 1.3-9.5 hours through changing the formula and preparation technique, and correspondinglag time can be selected with preference according to the rhythmicity of the outbreak of diseases, namely, the specific requirements of clinical time therapeutics on diseases. The formulation of the metoprolol oral pulsatile tablet is not complex, and the metoprolol oral pulsatile tablet is prepared by the simple and easy direct powder tabletting method and normal thin film coating method, so that the metoprolol oral pulsatile tablet is suitable for large-scale industrialized production.

Description

technical field [0001] The invention belongs to the field of drug preparations for pulse administration, and in particular relates to a metoprolol oral pulse tablet for treating hypertension and angina pectoris and its preparation method and application, that is, a drug release agent that can be selected according to the needs of disease timing and treatment. The prescription composition, preparation method and application of pulse preparations with time lag and rapid and complete drug release after time lag. Background technique [0002] In recent years, studies of chronobiology and chronopharmacology have shown that the physiological functions of the human body and the onset of certain diseases have obvious rhythmic changes, and the therapeutic effects, adverse reactions and internal processes of drugs all have time rhythms. The traditional sustained and controlled release preparations that release drugs at a zero-order or first-order rate process cannot meet the needs of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K9/32A61K31/138A61K47/38A61P9/10A61P9/12
Inventor 李沙李财福王兴立陈新民张绪文蒋杰
Owner JINAN UNIVERSITY