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Isosorbide dinitrate drops and preparation thereof

A technology of isosorbide dinitrate and dropping pills, which is applied in the direction of pill delivery, active ingredients of heterocyclic compounds, cardiovascular system diseases, etc., and can solve the problem of long disintegration time of isosorbide mononitrate tablets or capsules and the impact of isosorbide mononitrate Solve the problems of ester therapeutic effect, low dissolution rate and dissolution rate, etc., to achieve the effect of convenient carrying and taking, small pill size, and improved dissolution rate and dissolution rate

Inactive Publication Date: 2004-04-21
HONGYI SCI & TECH CO LTD NANCHANG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the disintegration time of isosorbide mononitrate tablets or capsules is long, the dissolution rate and dissolution rate are low, the absorption is poor, the bioavailability is low, the proportion of excipients is large, and it is inconvenient to take for children, the elderly, bedridden patients and patients with dysphagia. , poor compliance, affecting the therapeutic effect of isosorbide mononitrate

Method used

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  • Isosorbide dinitrate drops and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0051] prescription:

[0052] Isosorbide Mononitrate 5g

[0053] Macrogol 6000 15g

[0054] Makes 1000 capsules

[0055] Preparation method: Take the fine powder of isosorbide mononitrate that has been ultrafinely pulverized and passed through a 200-mesh sieve, add it to the molten polyethylene glycol 6000 matrix, stir well, use simethicone as coolant, make pellets by drop method, dry, Instantly.

example 2

[0057] prescription:

[0058] Isosorbide Mononitrate 5g

[0059] Macrogol 4000 15g

[0060] Makes 1000 capsules

[0061]Preparation method: Take the fine powder of isosorbide mononitrate that has been ultrafinely pulverized and passed through a 200-mesh sieve, add it to the molten polyethylene glycol 4000 matrix, stir well, use simethicone as coolant, make pellets by drop method, dry, Instantly.

example 3

[0063] prescription:

[0064] Isosorbide Mononitrate 5g

[0065] Macrogol 6000 5g

[0066] Macrogol 4000 10g

[0067] Makes 1000 capsules

[0068] Preparation method: Take the fine powder of isosorbide mononitrate that has been ultrafinely pulverized and passed through a 200-mesh sieve, add it to the molten mixed matrix of polyethylene glycol 4000 and polyethylene glycol 6000, stir well, and use simethicone oil as the coolant. Drop system into legal pills, dry, and get it.

[0069] 4. Example 4

[0070] prescription:

[0071] Isosorbide Mononitrate 5g

[0072] Glyceryl monostearate 15g

[0073] Makes 1000 capsules

[0074] Preparation method: Take isosorbide mononitrate fine powder that has been ultrafinely pulverized and passed through a 200-mesh sieve, add it to the molten glyceryl monostearate base, mix well, use ice water as a coolant, make pellets by dropping, dry, and have to.

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PUM

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Abstract

A dripping pill of isosorbide mononitrate is prepared through superfine pulverizing and conventional steps for preparing dripping pill. Its advantages are high disintegration speed, high stripping rate, quickly taking its effect, and low cost.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to isosorbide mononitrate dripping pills and a preparation method thereof. Background technique [0002] Isosorbide mononitrate is the main biologically active metabolite of isosorbide dinitrate. Like other organic nitrates, the main pharmacological effect is to relax vascular smooth muscle. Isosorbide mononitrate releases nitric oxide (NO). NO is the same as endothelial relaxation factor, activates guanylate cyclase, increases cyclic guanylate (cGMP) in smooth muscle cells, relaxes vascular smooth muscle, and makes peripheral arteries And venous expansion, the expansion of the veins is stronger. Venous dilation causes blood to remain in the periphery, reducing blood return to the heart, and reducing right ventricular end-diastolic pressure and pulmonary capillary wedge pressure (preload). Arterial dilation reduces peripheral vascular resistance, sys...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/34A61P9/10
Inventor 钱进许军彭红李平刘孝乐
Owner HONGYI SCI & TECH CO LTD NANCHANG
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