Oral chronopharmacologic drug delivery mini-pill preparation of propranolol and its salts

A technology for propranolol hydrochloride and preparations is applied in the field of propranolol and its salt oral preparations, which can solve problems such as difficulty in taking medicine by patients, and achieve the effects of simple preparation process and improved compliance.

Inactive Publication Date: 2013-10-23
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 (when the person is in a period of low physiological level), and the medicine will be released slowly and steadily when the blood pressure starts to rise from 6 to 10 in the morning, so as to effectively control the blood pressure during the day; At night, because the drug is basically not released, the blood drug concentration reaches a low point, which effectively avoids the thrombus problem caused by excessively lowering blood pressure at night, and also reduces the occurrence of toxic side effects and tolerance, and solves the problem of patients taking medicine at night difficult question

Method used

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  • Oral chronopharmacologic drug delivery mini-pill preparation of propranolol and its salts
  • Oral chronopharmacologic drug delivery mini-pill preparation of propranolol and its salts
  • Oral chronopharmacologic drug delivery mini-pill preparation of propranolol and its salts

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 The method for measuring the release of samples in different pH media is the same except that the replacement media is different from the previous one.

[0041] Example 1

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

[0043] Starch sucrose blank core 200g

[0044] Propranolol Hydrochloride 240g

[0045] 80% ethanol 1kg

[0046] Preparation process: Dissolve isosorbide dinitrate in 95% ethanol, apply fluidized bed coating, temperature 32±1°C, flow rate 8mL / min, wrap propranolol hydrochloride on the blank core, and obtain Drug immediate release pill core. The average cumulative dissolution rate was 90% in 45 minutes.

[0047] Sustained-release layer prescription: Ethylcellulose 4% (w / v) 80% ethanol solution.

[0048] Preparation process: dissolve ethyl cellulose in 80% ethanol, apply fluidized bed coating, temperature 35±2°C, flow rate 8mL / min, wrap ethyl cellulose on drug-containing immediate-release pellet core, coating increases W...

Embodiment 2

[0057] Drug-containing sustained-release pill core prescription:

[0058] Starch sucrose blank core 200g

[0059] Propranolol Hydrochloride 240g

[0060] 95% ethanol 1kg

[0061] The coating process is the same as in Example 1. The drug-containing immediate-release pellet core is obtained. The average cumulative dissolution rate was 90% in 45 minutes.

[0062] Sustained-release layer prescription: NE 30D is diluted with water to a solid content of 10%, and talcum powder accounting for 10% of the solid content is added as an anti-sticking agent, and stirred to make the mixture even.

[0063] Preparation process: Dilute a certain amount of NE 30D with water to a solid content of 10%, add talcum powder accounting for 10% of the solid content as an anti-adhesive agent, stir to mix evenly, and use a fluidized bed to coat at a temperature of 20±2°C. At a flow rate of 6 mL / min, NE 30D was coated on the drug-containing immediate-release pellet core, and the weight of the coating ...

Embodiment 3

[0072] Whole medicated immediate-release pellet core formulation w / w(%)

[0073] Propranolol Hydrochloride 240g

[0074] Low-substituted hydroxypropyl cellulose 100g

[0075] Microcrystalline Cellulose 100g

[0076] 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.

[0077] Sustained-release layer prescription: Ethylcellulose 4% (w / v) 80% ethanol solution.

[0078] Preparation process: dissolve ethyl cellulose in 80% ethanol, apply fluidized bed coating, temperature 35±2°C, flow rate 8mL / min, wrap ethyl cellulose on drug-containing immediate-release pellet core, coating increases Weight 8%, prepare...

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Abstract

The invention discloses an oral chronopharmacologic drug delivery mini-pill preparation of propranolol and its salts. The preparation comprises a quick release pill core containing 40-120mg of propranolol and its salts, a slow release layer, an alkaline layer, and a retardation layer, or comprises a slow release pill core containing 40-120mg of propranolol and its salts, the alkaline layer, and the retardation layer, wherein the retardation layer which contains polyacrylic resin III has a weight of 80-200% of the pill core, and the alkaline layer which is a medicinal water-soluble alkaline accessory has a weight of 10-30% of the pill core. The preparation has a characteristic that a medicament which is not immediately released after being orally taken is slowly released from the mini-pill when going through a time lag for 3-4h, and the slow release time can achieve 12-16h, so the daytime blood pressure can be stably controlled, and a purpose that the blood pressure in ten hours or so of early-morning wakefulness and daytime are stably controlled can be achieved.

Description

technical field [0001] The invention relates to propranolol and its salt oral preparations, in particular to the dosage form composition of propranolol salt oral time-selected controlled-release pellet preparations and the preparation method of the preparation. technical background [0002] With the research and development of chronopharmacology and chronotherapy, 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. Time-selected controlled-release drug delivery system, also known as intelligent drug delivery system...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/138A61K47/38A61K47/32A61P9/12
Inventor 郭红王成港王春龙刘衡
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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