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Isosorbide mononitrate timing quick-release and slow-release preparation

A slow-release and preparation technology, applied in the field of isosorbide mononitrate time-release sustained-release preparations, to achieve the effects of improving stability, avoiding drug resistance, and preventing drug resistance

Active Publication Date: 2010-01-20
SHANGAI PHARMA GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the technical schemes of these single-release preparations or secondary-release preparations are still difficult to fully cover the maintenance time limit of effective blood drug concentration in patients with coronary heart disease during the daily attack-prone period or the formation of low 5-ISMN blood drug concentration intervals for a considerable period of time.

Method used

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  • Isosorbide mononitrate timing quick-release and slow-release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Isosorbide Mononitrate 7.7g

[0052] Microcrystalline shot core (25 / 30m) 200g

[0053] HPMC E5 0.77g

[0054] Talc powder 0.2g

[0055] EC 9.6g

[0056] 80% ethanol 120g

[0057] Eudragit RS30D 235.1g (acrylic resin accounts for 70.53g)

[0058] Eudragit RL30D 57.6g (acrylic resin accounted for 17.28g)

[0059] Triethyl citrate 8.8g

[0060] Glyceryl monostearate 4.3g

[0061] Isosorbide Mononitrate 3.4g

[0062] Low-substituted hydroxypropyl cellulose 52.5g

[0063] HPMC E5 26.2g

[0064] Surelease (water dispersion of ethyl cellulose) 1070g (ethyl cellulose accounts for 267.5g)

[0065] Talc powder 1.41g

[0066] Preparation:

[0067] Add 0.77g of HPMC (E5) into 200g of warm water at 90°C under stirring. After swelling, slowly add 7.7g of isosorbide mononitrate, stir, and the solution becomes clear, then add 0.2g of talc, stir until completely dispersed, and set aside. Weigh 9.6 g of EC and add it to 120 g of 80% ethanol, stir for 45 minutes to obtain a c...

Embodiment 2

[0070] Isosorbide Mononitrate 158g

[0071] Microcrystalline shot core (25 / 30m) 200g

[0072] PVP K30 19.8g

[0073] Talc powder 0.2g

[0074] HPMC E5 9.6g

[0075] Eudragit NE30D 186.6g (acrylic resin accounted for 55.98g)

[0076] Eudragit RS30D 8.3g (acrylic resin accounted for 2.49g)

[0077] Polyethylene glycol 0.83g

[0078] Talc powder 33.2g

[0079] Isosorbide Mononitrate 67g

[0080] Crospovidone xL-10 57.7g

[0081] PVP K30 144.3g

[0082] Glyceryl monostearate 342.9g

[0083] Talc powder 1.41g

[0084] Preparation:

[0085] Add 19.8g of PVP K30 into 200g of warm water under stirring, after swelling, slowly add 158g of isosorbide mononitrate, stir, the solution becomes clear, then add 0.2g of talc, stir until completely dispersed, set aside. Weigh 9.6g of HPMC E5 and add it into 120g of water, and wait for swelling to prepare a coating solution for subsequent use. Eudragit NE30D 186.6g, Eudragit RL30D 8.3g are fully stirred, add polyethylene glycol 0.83g...

Embodiment 3

[0088] Isosorbide Mononitrate 35g

[0089] Sucrose core (40 / 50m) 200g

[0090] HPMC E5 87.5g

[0091] Talc powder 0.2g

[0092] Hydroxypropyl Cellulose 56g

[0093] Methylcellulose 22.4g

[0094] EC 344g

[0095] 80% ethanol 425g

[0096] Diethyl phthalate 68g

[0097] Isosorbide Mononitrate 15g

[0098] Croscarmellose Sodium 373g

[0099] Methylcellulose 37.3g

[0100] Eudragit RS30D 345.6g (acrylic resin accounted for 103.68g)

[0101] Eudragit RL30D 84.7g (acrylic resin accounted for 25.41g)

[0102] Triethyl citrate 12.7g

[0103] Glyceryl monostearate 6.36g

[0104] Tween 80 3.5g

[0105] Preparation:

[0106] Add 87.5g of HPMC (E5) into 200g of warm water at 90°C under stirring. After swelling, slowly add 35g of isosorbide mononitrate, stir, and the solution becomes clear, then add 0.2g of talc, stir until completely dispersed, and set aside. Weigh 56 g of hydroxypropyl cellulose and add it into 120 g of 95% alcohol water, and stir for 45 minutes to obtain...

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Abstract

The invention discloses a time quick-release and slow-release preparation of isosorbide mononitrate. The technical problem for the invention to solve is to provide a time quick-release and slow-release preparation, which is provided with long time of retaining the effective plasma-drug concentration and a low interval of 5-ISMN plasma-drug concentration. Each structure layer of the invention is orderly arranged from the inside to the outside as a parent nuclear of a pill core, a drug layer of a second dosage, an insulating layer, a slow-release coating layer, a drug layer of a first dosage, an expanding layer and a release controlling layer. The weight percentages of each layer are 15 to 40 percent of the parent nuclear of the pill core, 0.3 to 5.7 percent of the drug layer of the second dosage, 0 to 20 percent of the insulating layer, 5 to 40 percent of the slow-release coating layer, 0.7 to 13.4 percent of the drug layer of the first dosage, 5 to 30 percent of the expanding layer and 5 to 40 percent of the release controlling layer. The invention combines the characteristics of a time quick-release and slow-release medication system to avoid the drug resistance as well as accurately meet the clinical requirement of the angina treatment of the patient of the coronary heart disease.

Description

technical field [0001] The invention relates to a timed, quick-release and sustained-release preparation, in particular to a timed, quick-release and sustained-release preparation of isosorbide mononitrate. Background technique [0002] Isosorbide mononitrate (5-ISMN) is a commonly used drug for treating angina pectoris of coronary heart disease. It has been clinically used for many years and has a definite curative effect. The drug is rapidly distributed after oral absorption, directly acts without first-pass metabolism, has a half-life of 4-5 hours, and has an absolute bioavailability of nearly 100%. [0003] During the continuous treatment of 5-ISMN in patients with coronary heart disease, there will be drug resistance problems, which manifests as the need to continuously increase the original drug dose to maintain the original therapeutic effect. Studies have found that although the human body is prone to drug resistance to 5-ISMN, the drug resistance can be quickly rev...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/34A61K47/38A61K47/34A61K9/16A61K9/52A61P9/10A61K47/10
Inventor 甘勇谢慧军
Owner SHANGAI PHARMA GRP CO LTD
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