Isosorbide mononitrate osmotic pump type controlled release formulation and preparation method thereof

A controlled-release technology of isosorbide dinitrate and osmotic pumps, which is applied in the fields of pharmaceutical formulations, drug combinations, cardiovascular system diseases, etc., can solve problems such as difficulty in controlling the onset of angina pectoris in the morning, great influence of individual differences, and poor patient compliance, etc., to achieve Avoid peaks and valleys, easy to take, and long-lasting effect

Inactive Publication Date: 2009-01-14
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After oral administration of common preparations, the blood drug concentration rises rapidly to 400ng / mL, which greatly exceeds the minimum effective dose of 100ng / mL, causing severe headache, nausea, vomiting, circulatory collapse and other side effects in patients, with an incidence rate of about 14%.
In addition, the effective action time of the drug can only last for 6 hours, and it needs to be taken three times a day. Not only is it difficult to control the onset of angina pectoris in the morning, but patients often have poor compliance due to frequent medication or severe side effects
Although sustained-release preparations have solved the above-mentioned common preparations that require frequent medication (only need to take medicine once a day), side effects are reduced to a certain extent; The rate is also affected by factors such as the gastrointestinal fluid in the patient's body, which is difficult to control and predict. Therefore, the blood drug concentration may still fluctuate greatly and have certain instability. The effective duration and side effects also vary from person to person. , the influence of individual differences is relatively large, and it is uncontrollable

Method used

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  • Isosorbide mononitrate osmotic pump type controlled release formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Prescription composition (based on 1000 tablets)

[0035] Chip:

[0036] Isosorbide Mononitrate 60g

[0037] Sodium chloride 67.5g

[0038] Lactose 135g

[0039] Povidone K 30 30g

[0040] Magnesium Stearate 3g

[0041] Talc powder 4g

[0042] Coating solution:

[0043] Ethylcellulose 50mg / ml

[0044] Hypromellose 4.5mg / ml

[0045] PEG4000 4.5mg / ml

[0046] Dichloromethane: ethanol 3:1 (V / V)

[0047] Isosorbide mononitrate, lactose, sodium chloride and povidone K 30 Sift and mix thoroughly. The soft material is prepared from a mixed solution of ethanol and water (95:5, volume ratio), granulated to 20 mesh, and dried in a 40°C oven. Sieve the dry granules with 18 meshes, add magnesium stearate and talcum powder, and press into tablet cores. Place in a coating pan for coating. Dry at 40°C for 16 hours to solidify the coating film. It is sufficient to prepare one or more small holes with a diameter of 0.1-1.0 mm on one side of the core b...

Embodiment 2

[0049] Prescription composition (based on 1000 tablets)

[0050] Chip:

[0051] Isosorbide Mononitrate 60g

[0052] Microcrystalline Cellulose 50g

[0053]Lactose 135g

[0054] Talc powder 6g

[0055] Coating solution:

[0056] Cellulose acetate 40mg / ml

[0057] Diethyl phthalate 4.5mg / ml

[0058] PEG4000 8.0mg / ml

[0059] Acetone: water 95:5 (V / V)

[0060] Sieve isosorbide mononitrate, microcrystalline cellulose, and lactose, and mix thoroughly and evenly. The soft material is prepared from a mixed solution of ethanol and water (70:30, volume ratio), granulated with 20 mesh, and dried in a drying oven at 40°C. Sieve the dry granules with 18 mesh, add talcum powder and press into tablet cores. Place in a coating pan for coating. Dry at 40°C for 16 hours to solidify the coating film. It is sufficient to prepare one or more small holes with a diameter of 0.1-1.0mm on one side of the core by using a laser drilling machine.

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Abstract

The invention relates to an isosorbide mononitrate osmotic pump type controlled release preparation and a preparation method thereof. The osmotic pump type controlled release preparation is composed of a tablet core and semipermeable film coating with medicine releasing holes; wherein, the tablet core is composed of isosorbide mononitrate, penetration enhancer, bond and other excipient, and the semipermeable film includes coating material and plasticizer; the punching mode includes mechanical drilling and laser drilling. The preparation of the invention can effectively control the constant speed release rate of medicine and has the advantages of few administration times, less side effect, long efficacy lasting time, avoidance of medicine tolerance, etc.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a novel osmotic pump controlled-release tablet preparation of isosorbide mononitrate for treating coronary heart disease and angina pectoris, and to a preparation method of the osmotic pump controlled-release tablet preparation. Background technique [0002] Isosorbide mononitrate is a commonly used drug for treating coronary heart disease and angina pectoris. It was first developed by Boehringer Mannheim GmbH in Germany and launched in the market in 1981. It has been clinically used for many years and has a definite curative effect. Its main mechanism of action is to expand venous volume vessels and peripheral resistance vessels, reduce cardiac preload and postload, and reduce myocardial oxygen consumption. The drug has the characteristics of high bioavailability, small individual differences, short half-life and remarkable curative effect, and is better than indigesti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/34A61P9/10
Inventor 梅兴国秦玮
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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