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Isosorbide mononitrate microporous osmotic pump controlled-release preparation and preparation method thereof

A technology of isosorbide dinitrate and controlled-release preparations, which is applied in the direction of pharmaceutical formulas, medical preparations of non-active ingredients, drug combinations, etc., can solve the problems of incomplete drug release and decreased drug release kinetics, and improve patient compliance , reduced terminal residues, and stable blood drug concentration

Inactive Publication Date: 2018-10-30
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation of single-chamber osmotic pump tablets is simple, but there is a problem: with the advancement of the drug release process, the osmotic pressure difference between the inside and outside of the semipermeable membrane gradually decreases, and the drug release kinetics gradually decreases, resulting in incomplete drug release in the chamber, and about 10 Drugs around %

Method used

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  • Isosorbide mononitrate microporous osmotic pump controlled-release preparation and preparation method thereof
  • Isosorbide mononitrate microporous osmotic pump controlled-release preparation and preparation method thereof
  • Isosorbide mononitrate microporous osmotic pump controlled-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Prescription of osmotically active substance delayed-release pellet core (1000 tablets):

[0047] Glucose 10.27g

[0048] Microcrystalline Cellulose 4.40g

[0049] Preparation process of ball core: Glucose and microcrystalline cellulose are passed through 80-mesh sieve respectively, and then mixed evenly through 60-mesh sieve, water is used as a binder to make soft material, extruded and spheronized, dried at 40°C for 24 hours, sieved Pellets between 24-30 mesh.

[0050] The prescription composition (coating weight gain 10.0%) of pellet isolation layer coating liquid:

[0051] HPMC 2g

[0052] Ethanol 36ml

[0053] water 4ml

[0054] Coating process of isolation gown: take the pellet core and place it in a fluidized bed, adjust the air inlet temperature to 35°C, and the blast frequency to 30.50HZ, slowly add HPMC to the ethanol water solvent, and use it as an isolation layer coating after being clarified and transparent Use a peristaltic pump to pump the coating s...

Embodiment 2

[0066] The prescription and preparation process of the osmotically active substance delayed-release pellets are the same as in Example 1, the weight gain of the coating of the isolation layer is 9.5%, and the weight gain of the coating of the controlled release layer is 14.5%.

[0067] Tablet core prescription composition (1000 tablets):

[0068]

[0069] The prescription composition of semi-permeable membrane coating liquid (coating weight gain 4.45%):

[0070]

[0071] The tablet core of the present embodiment is prepared according to the tablet core preparation method of the isosorbide mononitrate of Example 1, and according to the coating solution prescription, the tablet core of the present embodiment is coated by the coating process of Example 1, and solidified to obtain the present embodiment. Novel Isosorbide Mononitrate Microporous Osmotic Pump Formulations of the Examples.

Embodiment 3

[0073] The prescription and preparation process of the osmotically active substance delayed-release pellets are the same as in Example 1, the weight gain of the coating of the isolation layer is 10.5%, and the weight of the coating of the controlled release layer is 15.5%.

[0074] Tablet core prescription composition (1000 tablets):

[0075]

[0076] The prescription composition of semi-permeable membrane coating liquid (coating weight gain 4.55%):

[0077]

[0078] The tablet core of the present embodiment is prepared according to the tablet core preparation method of the isosorbide mononitrate of Example 1, and according to the coating solution prescription, the tablet core of the present embodiment is coated by the coating process of Example 1, and solidified to obtain the present embodiment. Novel Isosorbide Mononitrate Microporous Osmotic Pump Formulations of the Examples.

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Abstract

The invention relates to a novel isosorbide mononitrate micro-porous osmotic pump controlled-release preparation and a preparation method thereof. The preparation comprises a medicated tablet core, and a semipermeable controlled-release membrane coating the tablet core. The tablet core contains isosorbide mononitrate, general osmotic pressure active substance, delayed-release micro pills permeating the active substance and filler; the semipermeable membrane comprises cellulose acetate and a pore-foaming agent. The invention further relates to a preparation method of the controlled-release preparation. The most important characteristic of the invention is that the delayed-release micro pill having certain time lag and permeating the active substance is added into the table core, so as to supplement osmotic pressure in a pump chamber at late period of release and promote further release of the drug, thus, the pharmaceutics requirement that end release residue in the pump chamber is not more than 5% is fulfilled, meanwhile, zero-order release of drug is guaranteed, plasma drug concentration is steady, frequency of use is reduced for the patient, and safety of medication, effectiveness and patient compliance are all improved.

Description

technical field [0001] The invention relates to a controlled-release preparation of isosorbide mononitrate used for treating angina pectoris, in particular to a preparation method of delayed-release pellets of osmotic active substances and the controlled-release tablet. Background technique [0002] Isosorbide mononitrate is a new generation of nitrate anti-angina drugs, it can dilate veins stronger than arteries, reduce myocardial oxygen consumption, relax arterial blood pressure and dilate coronary vessels, thereby reducing cardiac ejection resistance, It can improve myocardial ischemia, and is especially suitable for the prevention and treatment of patients with coronary heart disease and angina pectoris. It is one of the more promising varieties of nitrate drugs at present. [0003] Oral absorption of isosorbide mononitrate is fast, reaching the peak of blood concentration after 30 minutes, no liver first-pass effect, bioavailability as high as 100%, long elimination hal...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/36A61K9/30A61K31/34A61K47/38A61K47/32A61P9/10
Inventor 王柏吴作敏
Owner CHINA PHARM UNIV
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