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Nitroglycerin micro-tablet as well as preparation method and preparation thereof

A technology of nitroglycerin and microtablets, which is applied in the fields of pill delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc. It can solve problems such as content uniformity, poor dissolution rate and stability, and decreased bioavailability of disintegration and dissolution time , to achieve good content uniformity and dissolution rate, to avoid the decline of bioavailability, and to improve the effect of utilization

Active Publication Date: 2022-04-29
BEIJING VAGARY PHARM TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It will also avoid the problem of decreased bioavailability caused by direct swallowing of conventional sublingual tablets due to long disintegration and dissolution time
At the same time, it overcomes the problems of content uniformity, dissolution rate and poor stability.

Method used

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  • Nitroglycerin micro-tablet as well as preparation method and preparation thereof
  • Nitroglycerin micro-tablet as well as preparation method and preparation thereof
  • Nitroglycerin micro-tablet as well as preparation method and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] A preparation method of nitroglycerin microchips, the composition of the microchips is as follows:

[0054] The composition of table 1 embodiment 1

[0055]

[0056] The preparation method of described microchip, comprises the steps:

[0057] (1) Polyethylene glycol is dissolved in 10% nitroglycerin ethanol solution; Prepare the solution for subsequent use;

[0058] (2) Mix mannitol, microcrystalline cellulose, dextran and sodium starch glycolate, and use the solution obtained in (1) to carry out fluidized bed granulation. The outlet temperature of the fluidized bed is set at 40° C. to obtain granules containing The amount of water is 2.3%;

[0059] (3) mixing the granules obtained in (2) with silicon dioxide and glyceryl monostearate;

[0060] (4) Use a tablet machine to make microtablets with a diameter of 2 mm, a tablet weight of 5 mg, and 0.25 mg of nitroglycerin.

Embodiment 2

[0062] A preparation method of nitroglycerin microchips, the composition of the microchips is as follows:

[0063] The composition of table 2 embodiment 2

[0064]

[0065] The preparation method of described microchip, comprises the steps:

[0066] (1) hydroxypropyl cellulose is dissolved in 10% nitroglycerin ethanol solution; the prepared solution is for subsequent use;

[0067] (2) Sorbitol, pregelatinized starch, sucrose and sodium starch glycolate are mixed, and fluidized bed granulation is carried out with the solution obtained in (1), and the outlet temperature of the fluidized bed is set at 40° C., and the water content of the obtained granules is 1.0%;

[0068] (3) mixing the granules obtained in (2) with silicon dioxide sodium stearyl fumarate;

[0069] (4) Use a tablet machine to make microtablets with a diameter of 2 mm, a tablet weight of 5 mg, and 0.2 mg of nitroglycerin.

Embodiment 3

[0071] A preparation method of nitroglycerin microchips, the composition of the microchips is as follows:

[0072] The composition of table 3 embodiment 3

[0073]

[0074]

[0075] The preparation method of described microchip, comprises the steps:

[0076] (1) Carbomer 940 is dissolved in 10% nitroglycerin ethanol solution; the prepared solution is for subsequent use;

[0077] (2) Sorbitol, lactose, fructose and povidone K30 are mixed, and the solution obtained in (1) is used for fluidized bed granulation, and the outlet temperature of the fluidized bed is set at 40° C., and the water content of the obtained granules is 3.0%;

[0078] (3) mixing the granules obtained in (2) with silicon dioxide and stearic acid;

[0079] (4) Use a tablet machine to make microtablets with a diameter of 2 mm, a tablet weight of 5 mg, and 0.1 mg of nitroglycerin.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a nitroglycerin micro-tablet as well as a preparation method and a preparation thereof. The diameter of the micro-tablet is 1-4 mm, the weight of the micro-tablet is 2-50 mg, and each micro-tablet contains 0.1-2.5 mg of nitroglycerin. The invention also provides a preparation method of the micro-tablet. The compound used by the micro-tablet can obviously improve the stability of the preparation and accelerate the disintegration time limit; and the micro-tablet is rapidly disintegrated and dissolved and is absorbed by sublingual mucosa at a higher speed, so that the first-pass effect of the liver on the medicine can be avoided, and the onset time of first aid is accelerated. And the problem that the bioavailability is reduced due to the fact that the conventional sublingual tablet is directly swallowed after being taken due to overlong disintegration and dissolution time can also be avoided.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a nitroglycerin microchip, a preparation method and a preparation thereof. Background technique [0002] Nitroglycerin, also known as glyceryl trinitrate, is the trinitrate ester of glycerin and is a highly explosive explosive. It can be used as a vasodilator in medicine to treat angina pectoris caused by coronary artery stenosis. [0003] [0004] Nitroglycerin is an organic nitrate and a short-acting vasodilator with rapid action (1 to 2 minutes). The duration after one administration is about 3 to 5 minutes. The elimination half-life in plasma is relatively short. About 1.5 minutes, and the metabolites are non-toxic. Nitroglycerin undergoes biotransformation in vascular endothelial cells, produces and releases exogenous nitric oxide (NO), relaxes vascular smooth muscle by activating soluble guanylate cyclase (cGMP), and has a vasodilation effect. ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/21A61K47/26A61K47/38A61K47/36A61P9/10
CPCA61K9/2018A61K9/2054A61K9/2059A61K9/006A61K31/21A61P9/10
Inventor 宁宗超郭全禄郭明亮
Owner BEIJING VAGARY PHARM TECH LTD
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