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Isosorbide mononitrate sustained-release tablet and preparation method thereof

A technology of isosorbide dinitrate and sustained-release tablets, which is applied in the fields of medical formula, drug delivery, and cardiovascular system diseases, and can solve the problems of patients with coronary heart disease who miss the drug action time, increase drug residues, and drugs cannot take effect quickly , to achieve the effect of avoiding multi-dose resistance, delaying multi-dose resistance, and rapid onset of effect

Inactive Publication Date: 2012-04-18
NANJING CHENGONG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The half-life of isosorbide mononitrate is about 5 hours, and the gastrointestinal absorption is rapid and complete. It is mainly metabolized by the kidneys as the original drug. The common tablets used cannot achieve long-term effective sustained release of blood drugs, and need to be administered twice a day. Although the release preparation formulation achieves once-a-day administration, because the drug cannot take effect quickly during the initial period of administration, the optimal drug action time may be missed for patients with coronary heart disease
In addition, since the slow release of the drug increases the residual amount of the drug when administered the next day, it is easy to induce drug resistance in the body

Method used

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  • Isosorbide mononitrate sustained-release tablet and preparation method thereof
  • Isosorbide mononitrate sustained-release tablet and preparation method thereof
  • Isosorbide mononitrate sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Formulation of Isosorbide Mononitrate Extended Release Tablets

[0027]

[0028] A total of 1000 tablets were pressed.

[0029] Preparation process: 1. Transfer 100g of blank microcrystalline cellulose ball cores to the fluidized bed system, add 60g of isosorbide mononitrate into the aqueous solution to dissolve, and spray 45g of isosorbide mononitrate solution into the blank microcrystalline Isosorbide mononitrate drug-loaded microspheres were prepared in a fluidized bed of cellulose spheres. In the process of preparing drug-loaded microspheres, the inlet temperature is 40°C, the outlet temperature is 35°C, and the product temperature is 35°C. In the drying process, the inlet temperature is 45°C, the output temperature is 35°C, and the product temperature is 35°C. The spray speed is 5mL / min, and the spray pressure is 2bar.

[0030] 2. Dissolve 16g of coating material in purified water. The weight ratio of hypromellose, triacetin, and talcum powder in the coating ...

Embodiment 2

[0033] Formulation of Isosorbide Mononitrate Extended Release Tablets

[0034]

[0035] A total of 1000 tablets were pressed.

[0036] Preparation process: 1. Transfer 95g of blank microcrystalline cellulose ball cores to the fluidized bed system, add 60g of isosorbide mononitrate into the aqueous solution to dissolve, and spray 45g of isosorbide mononitrate solution into the blank microcrystalline Isosorbide mononitrate drug-loaded microspheres were prepared in a fluidized bed of cellulose spheres. Process parameter is with embodiment 1.

[0037] 2. Dissolve 12g of coating material in purified water. The weight ratio of hypromellose, triacetin, and talcum powder in the coating material is 1:0.3:0.3, and it is prepared into a coating solution. Perform coating. Process parameter is with embodiment 1.

[0038] 3. Mix the coated drug-loaded microspheres with 15 g of isosorbide mononitrate, hydroxypropyl cellulose, povidone, starch, and magnesium stearate, and then compress...

Embodiment 3

[0040] Formulation of Isosorbide Mononitrate Extended Release Tablets

[0041]

[0042] A total of 1000 tablets were pressed.

[0043] Preparation process: 1. Transfer 98g of blank microcrystalline cellulose ball cores to the fluidized bed system, add 60g of isosorbide mononitrate into the aqueous solution to dissolve, and spray 45g of isosorbide mononitrate solution into the blank microcrystalline Isosorbide mononitrate drug-loaded microspheres were prepared in a fluidized bed of cellulose spheres. Process parameter is with embodiment 1.

[0044] 2. Dissolve 17g of coating material in purified water, the weight ratio of hypromellose, triacetin, and talc in the coating material is 1:0.3:0.2, and prepare a coating solution. Perform coating. Process parameter is with embodiment 1.

[0045] 3. Mix the coated drug-loaded microspheres with 15 g of isosorbide mononitrate, hydroxypropyl cellulose, lactose, and magnesium stearate, and then compress into tablets.

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Abstract

The invention relates to an isosorbide mononitrate sustained-release tablet and a preparation method thereof, belonging to the technical field of medicinal preparations. The sustained-release tablet comprises a coating of isosorbide mononitrate drug loaded microballoons which account for 48% to 55% of the total weight of the tablet and a quick-release layer which accounts for 45% to 52% and comprises isosorbide mononitrate, a binder, a filler and a lubricant. According to the invention, isosorbide mononitrate is divided into two parts, i.e., the part of quick release and the part of sustained release, which enables the tablet to take effect rapidly at an initial stage of administration, maintain an effective plasma concentration after the effective plasma concentration is reached and retain the effective plasma concentration at a low level so as to reduce residual quantity of the tablet at administration time of the tablet the next day, thereby effectively avoiding generation of drug resistance.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to an isosorbide mononitrate sustained-release tablet and a preparation method thereof. Background technique [0002] Nitrate drugs are the most effective drugs for the treatment of myocardial ischemic diseases. Their main pharmacological effect is to relax vascular smooth muscle, thereby leading to vasodilation, reducing cardiac preload and postload, improving myocardial blood supply, and reducing oxygen consumption. Myocardial ischemia, angina pectoris. Nitrate drugs include nitroglycerin, isosorbide mononitrate, isosorbide dinitrate, pentyl tetranitrate, etc. These drugs are still the most commonly used clinically for the treatment of myocardial ischemic diseases. Isosorbide mononitrate is a typical representative of nitrate drugs. It is one of the metabolites of isosorbide dinitrate. It is characterized by no liver first-pass effect, complete and rapid absorp...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/34A61P9/10
Inventor 郭昭
Owner NANJING CHENGONG PHARM CO LTD
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