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Spray-drying method for preparing metoprolol succinate sustained-release capsules

A technology of metoprolol succinate and spray drying method, which is applied in the field of preparing metoprolol succinate microcapsules, can solve the problems of short drug release time, large amount of organic solvent, easy aggregation of microcapsules, etc. The volume of oily substances and a large amount of volatile solvents can be washed, the effect of reducing the residue of organic solvents and rounding the shape

Inactive Publication Date: 2012-07-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solvent evaporation method has the following disadvantages: the prepared microcapsules are easy to agglomerate; the amount of organic solvent used in the preparation process is large; the process is complex and the operating parameters need to be strictly controlled; the encapsulation efficiency of hydrophilic drugs is very low
However, the microcapsule preparation obtained by the traditional spray drying method not only has obvious burst release, but also has a short release time of the drug.

Method used

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  • Spray-drying method for preparing metoprolol succinate sustained-release capsules
  • Spray-drying method for preparing metoprolol succinate sustained-release capsules
  • Spray-drying method for preparing metoprolol succinate sustained-release capsules

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Utilize spray-drying method to prepare the method for metoprolol succinate microcapsule, prescription is as follows:

[0037]

[0038] The preparation process is as follows:

[0039] (1) Primary encapsulation of raw materials (oil phase)

[0040] Evenly disperse metoprolol succinate in oleic acid containing Span80, and ultrasonicate for 600s to form an oil phase.

[0041] (2) Configure the spray liquid (outer water phase)

[0042] Dissolving ethyl cellulose in ethanol solution, adding micropowder silica gel, glycerin and polyisobutylene, stirring evenly, filtering to obtain the outer water phase.

[0043] (3) Homogeneous emulsification of spray liquid

[0044] Add the oil phase to the external water phase for homogeneous emulsification, the homogenization temperature is 50°C, the high-pressure homogenization speed is 14000rpm, and the time is 6min, to obtain the S / O / W type double emulsion spray liquid.

[0045] (4) spray drying

[0046] Spray-dry the above-mention...

Embodiment 2

[0050] Embodiment 2 release experiment

[0051] Refer to the detection method of metoprolol succinate sustained-release tablets in the United States Pharmacopoeia USP32, adopt the rotating basket method, use 900ml of distilled water as the release medium, and the speed is 100 revolutions per minute, operate according to the law, at 0.5, 1, 2, 4, 6, Take 5ml of the solution at 8, 10, 12, 15, and 24 hours respectively, filter, and immediately supplement the release medium at the same temperature and volume, take the subsequent filtrate, and measure it at a wavelength of 274nm according to ultraviolet-visible spectrophotometry. Absorbance. Calculate the cumulative drug release percentage at each time point, see the release curve figure 2 As shown, the burst release amount is less than 15%, and its release can last for 24 hours, and the drug release performance in vitro conforms to the characteristics of sustained-release preparations.

Embodiment 3

[0053] Utilize spray-drying method to prepare the method for metoprolol succinate microcapsule, prescription is as follows:

[0054]

[0055] The preparation process is as follows:

[0056] (1) Primary encapsulation of raw materials (oil phase)

[0057] Evenly disperse metoprolol succinate in peanut oil containing Span80, and ultrasonicate for 600s to form an oil phase.

[0058] (2) Configure the spray liquid (outer water phase)

[0059] Dissolve ethyl cellulose (5 cps) and ethyl cellulose (10 cps) in ethanol solution, then add micropowdered silica gel, glycerin and polyisobutylene, stir evenly, and filter to obtain the external water phase.

[0060] (3) Homogeneous emulsification of spray liquid

[0061] The oil phase was added to the external water phase for homogeneous emulsification, the homogenization temperature was 55°C, the high-pressure homogenization speed was 12000 rpm, and the time was 9 minutes to obtain the S / O / W type double emulsion spray liquid.

[0062]...

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Abstract

The invention provides a spray-drying method for preparing metoprolol succinate sustained-release capsules. The method comprises the following steps of: (1) dispersing metoprolol succinate in an oil phase uniformly, and emitting ultrasound to obtain a suspension, wherein the oil phase contains 1 to 10 percent of surfactant; (2) dissolving a macromolecular capsule material in an aqueous solution of ethanol, adding an antisticking agent, a plasticizer and a dispersing agent, stirring uniformly, filtering and preparing an external water phase for later use; and (3) adding the suspension obtainedin the step (1) into the ethanol solution obtained in the step (2), homogenizing and emulsifying to obtain a metoprolol succinate suspension / oil / water (S / O / W) multi-emulsion spray liquid, and spray-drying. The metoprolol succinate sustained-release capsules are rounded in appearance, smooth and clean in surfaces, high in flowability and encapsulation rate, lasting in medicinal effect and high in stability, have the grain diameter of between 30 and 300 micrometers, can control burst release effectively, have an obvious sustained-release effect, and are suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a method for preparing metoprolol succinate microcapsules by a spray drying method. Background technique [0002] Metoprolol is a selective beta 1 Receptor blockers are one of the commonly used drugs for the treatment of hypertension, coronary heart disease, chronic heart failure and arrhythmia. The earliest metoprolol preparation on the market is metoprolol tartrate, which has a short elimination half-life of about 3 to 4 hours, so the plasma drug concentration fluctuates greatly, and it needs to be taken 2 to 4 times a day. In response to these shortcomings, several metoprolol tartrate slow-release preparations have appeared on the market, but because the solubility of metoprolol tartrate is very large (> 700mg / ml), in order to obtain more slow and sustained release metoprolol, use Succinate was used instead of tartrate, so that its solubility in water (270mg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/138B01J13/04A61P9/04A61P9/06A61P9/10A61P9/12
Inventor 平其能宋力何盛江
Owner CHINA PHARM UNIV
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