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Metoprolol sustained release capsule and preparation method thereof

A technology of torolol sustained-release capsules and sustained-release capsules is applied in the directions of capsule delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc., and can solve the problems of time-consuming and energy-consuming, complex process, and high technical difficulty of water-based coating. , to achieve the effect of easy operation, solving instability and good industrialization prospects

Active Publication Date: 2017-05-31
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing research on metoprolol sustained-release capsules is to prepare sustained-release pellets first, and then fill them into hollow hard capsule shells, and the process is relatively complicated.
The slow-release coating of hard capsules has always been a difficult point in the preparation, because the gelatin capsule shell is unstable in contact with water, and the water-based coating technology is difficult, and it is necessary to add an isolation layer or strictly control the coating conditions; while the organic solvent coating not only consumes energy and time, There are also problems such as explosion-proof and organic solvent pollution

Method used

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  • Metoprolol sustained release capsule and preparation method thereof
  • Metoprolol sustained release capsule and preparation method thereof
  • Metoprolol sustained release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Mix 100 g of metoprolol, 300 g of microcrystalline cellulose and 400 g of lactose uniformly, and use a No. 2 capsule plate to prepare the inner core of a gelatin hard capsule, and each capsule contains about 25 mg of metoprolol on average.

[0023] Mix 420g of Eudragit RS, 42g of Eudragit RL and 46.2g of triethyl citrate, hot-melt extrusion at 100°C, air pulverized, add 46.2g of talc and mix to prepare a pre-plastic with RS:RL=10:1 Mixed powder. Put the inner core of the hard capsule in a coating pan at 30 rpm and 70 °C, spray 4.6 g of wetting agent PEG 3350 with a liquid spray gun; Coated capsules with a coating weight gain of about 15% were prepared and aged in an oven at 65°C for 6 hours.

Embodiment 2

[0025] Mix 100 g of metoprolol, 300 g of microcrystalline cellulose and 400 g of lactose uniformly, and use a No. 2 capsule plate to prepare the inner core of a gelatin hard capsule, and each capsule contains about 25 mg of metoprolol on average.

[0026] Mix 385g Eudragit RS, 77g Eudragit RL and 46.2g triethyl citrate, hot melt extrusion at 100°C, jet pulverize, and mix 46.2g talc powder to prepare pre-plasticized RS:RL=5:1 Mix powder.

Embodiment 3

[0028] Mix 100 g of metoprolol, 300 g of microcrystalline cellulose and 400 g of lactose uniformly, and use a No. 2 capsule plate to prepare the inner core of a gelatin hard capsule, and each capsule contains about 25 mg of metoprolol on average.

[0029] Mix 231g Eudragit RS, 231g Eudragit RL and 46.2 g triethyl citrate, hot melt extrusion at 100°C, jet mill, and mix 46.2g talc powder to prepare pre-plasticized RS:RL=1:1 Mix powder.

[0030] Using 500 mL of purified water as the release medium, add the metoprolol sustained-release capsules obtained in Example 1-3 into water, rotate at 75 rpm, temperature 37 ± 0.5 ° C, sample 10 mL regularly, filter with a 0.45 μm filter membrane, and measure the absorbance at 274 nm. The concentration was calculated from the standard curve, and the in vitro release curve was drawn (see appendix). figure 1 ). The results showed that the ratio of RS and RL had a significant effect on the release curve in vitro. When RS:RL=10:1, the 24h sustai...

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Abstract

The invention provides a metoprolol sustained release capsule and a preparation method thereof. The sustained release capsule is composed of drug-containing filler, a gelatin capsule shell and sustained release coating. The preparation method of the sustained release capsule comprises the following steps: uniformly mixing metoprolol, microcrystalline cellulose and lactose, placing the mixture in a hollow gelatin capsule shell to prepare a drug-containing capsule inner core; and carrying out dry powder coating on the drug-containing capsule inner core by using an inner adding method or an outer adding method of a plasticizer, and carrying out aging at 60-70 DEG C for 2-12h to obtain the metoprolol sustained release capsule. The metoprolol sustained release capsule provided by the invention represents first-order drug release behavior in 24h drug release in vitro, and provides a product convenient to swallow for treating cardiovascular diseases. The metoprolol sustained release capsule is prepared by dry powder coating, no aqueous or organic solvent is used in the preparation process, so the operation is convenient, and the problems of instability, energy consumption, time consumption, environmental pollution and the like of hard capsules can be solved.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a metoprolol sustained-release capsule and a preparation method for dry powder coating thereof. Background technique [0002] Metoprolol is a β1-receptor blocker widely used in the treatment of cardiovascular diseases such as hypertension, angina pectoris and myocardial infarction. The development of metoprolol sustained-release capsules can reduce the number of administrations, smooth the blood concentration, facilitate patients' swallowing, and improve clinical efficacy and compliance. [0003] The research on the existing metoprolol sustained-release capsules is realized by first preparing the sustained-release pellets, and then loading them into the hollow hard capsule shell, and the process is relatively complicated. The sustained-release coating of hard capsules has always been a difficulty in formulation, because the gelatin capsule shell is unstable in water...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/138A61K47/32A61K47/38A61K47/26A61P9/12A61P9/10
CPCA61K9/0002A61K9/4825A61K9/4866A61K9/4891A61K31/138A61K47/32
Inventor 杨燕沈莲单伟光
Owner ZHEJIANG UNIV OF TECH
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