Isosorbide dinitrate oral administration impulse pellet preparations

A technology of pulsed pellets and isosorbide, which is used in medical preparations with non-active ingredients, cardiovascular system diseases, non-active ingredients of oil/fat/wax, etc. Effect

Active Publication Date: 2008-09-24
TIANJIN INSTITUTE OF PHARMA RESEARCH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As long as the patient takes the medicine before going to bed, the medicine will not be released for a period of time (the person is in a period of low physiological level), and the medicine will be released quickly before the peak of angina pectoris at 6-10 in the morning, and the blood drug concentration will quickly reach the therapeutic value, achieving prevention and treatment. The purpose of treatment, while solving the problem of patients' difficulty in taking medicine at night

Method used

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  • Isosorbide dinitrate oral administration impulse pellet preparations
  • Isosorbide dinitrate oral administration impulse pellet preparations
  • Isosorbide dinitrate oral administration impulse pellet preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Drug-containing immediate-release pill core prescription:

[0030] Starch sucrose blank core 400g

[0031] Isosorbide Dinitrate 100g

[0032] 95% ethanol 1kg

[0033] Preparation process: Dissolve isosorbide dinitrate in 95% ethanol, apply fluidized bed coating, temperature 32±1°C, flow rate 8mL / min, wrap isosorbide dinitrate on the blank core to obtain Drug immediate release pill core. The average cumulative dissolution rate was 90% in 45 minutes.

[0034] Alkaline Layer Recipe: Sodium Bicarbonate 10% (w / v), add water to 100%

[0035] Preparation process: Dissolve sodium bicarbonate in water, apply fluidized bed coating, temperature 50±1°C, flow rate 3mL / min, wrap sodium bicarbonate on drug-containing immediate-release pellet core, coating weight gain 20%, A pellet core containing an alkaline layer is prepared.

[0036] Hysteresis layer prescription w / v(%)

[0037] Polyacrylic resin III (Eudragit S100) 6.5

[0038] Magnesium stearate 1.2

[0039] Add 95% ethan...

Embodiment 2

[0042] Drug-containing immediate-release pill core prescription:

[0043] Starch sucrose blank core 600g

[0044] Isosorbide Mononitrate 100g

[0045] 95% ethanol 1kg

[0046] The coating process is the same as in Example 1. Get the drug-containing immediate-release pellet core. The average cumulative dissolution rate was 90% in 45 minutes.

[0047] Basic layer: Potassium dihydrogen phosphate 10% (w / v), add water to 100%, the coating process is the same as in Example 1. The weight of the coating increased by 12%, and the ball core containing the basic layer was obtained.

[0048] Hysteresis layer prescription w / v(%)

[0049] Polyacrylic resin III (Eudragit S100) 6

[0050] Micronized silica gel 1.4

[0051] Add 95% ethanol to 100%,

[0052] The coating process is the same as in Example 1. Coating weight gain of 120%. The obtained pulse pellet release curve is shown in the appendix figure 2 : Lags for about 3.5 hours, then releases completely within 2 hours.

Embodiment 3

[0054] Whole medicated immediate-release pellet core formulation w / w(%)

[0055] Isosorbide dinitrate 30

[0056] Low-substituted hydroxypropyl cellulose 40

[0057] Microcrystalline Cellulose 30

[0058] Preparation process: add 5% HPMC in 70% ethanol solution to make soft material, extrude the soft material through the sieve plate of the extruder (aperture 0.8mm), put the strip-shaped particles in the spheronizer and spheronize, and dry the pellet core at 50°C After 5 hours, sieve the 18-24 mesh drug core to obtain the drug-containing immediate-release pellet core. The average cumulative dissolution rate was 5% in 45 minutes.

[0059] Basic layer: sodium carbonate 10% (w / v), add water to 100%, the coating process is the same as in Example 1. Coating weight gain 25%;

[0060] Hysteresis layer prescription w / v(%)

[0061] Polyacrylic resin III (Eudragit S100) 8

[0062] Dibutyl sebacate 1

[0063] Glycerin 0.2

[0064] Talc 1.5

[0065] Add 95% ethanol to 100%, the c...

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Abstract

The invention discloses an oral pulse pellet pharmaceutical preparation of isosorbide esters, which consists of an immediate-release pellet core, an alkaline layer and a retardation layer containing isosorbide esters of 10 to 50 mg, wherein, the retardation layer contains polyacrylic resin 3, the weight increment of which is 80 to 200 percent of the immediate-release pellet core; the alkaline layer is a medicinal water-soluble alkaline adjuvant, the weight of which is 10 to 30 percent of the immediate-release pellet core. The pharmaceutical preparation has the characteristics that the drug does not release immediately after being taken orally, releases immediately from the pellet after 3 to 4 hours time lagging and the plasma concentration presents a pulse peak value. The pharmaceutical preparation can achieve the goal of preventing angina pectoris and other diseases from being triggered due to the rise of blood pressure and heart rate within a few hours after a patient awakens and wakes up in the early morning.

Description

technical field [0001] The invention relates to an oral preparation of isosorbide dinitrate, in particular to a dosage form composition of an oral pulse pellet preparation of isosorbide dinitrate and a preparation method of the preparation. Background technique [0002] With the development of chronopharmacology research, it has been found that the onset of many diseases shows obvious circadian rhythm changes, especially cardiovascular diseases such as angina pectoris and myocardial infarction. The morbidity and mortality of these diseases are highest in the early morning. If the optimal administration time is selected according to the biological rhythm of the onset of these diseases, the drug can exert the greatest therapeutic effect with the smallest therapeutic dose when it is most needed, while minimizing toxic and side effects. Pulse drug delivery system, also known as intelligent drug delivery system, is a new dosage form that releases effective doses of drugs at regul...

Claims

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Application Information

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IPC IPC(8): A61K31/34A61K9/16A61K47/04A61K47/10A61K47/12A61K47/14A61K47/34A61K47/44A61P9/10A61P9/12A61K47/32
Inventor 刘衡马滔王春龙
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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