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Slow release drop pills comprising toraesmide active ingredient and method for preparing same

A technology of torasemide and sustained-release pellets, which is applied in the direction of active ingredients of heterocyclic compounds, bulk delivery, blood diseases, etc., can solve problems such as major side effects, achieve easy industrialization, improve therapeutic effect, and increase safety Effect

Inactive Publication Date: 2009-10-14
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The elimination half-life of torasemide in the blood is 2.2 to 5 hours. In order to maintain the trough concentration and still be effective, the dosage must be increased, and long-term medication may bring greater side effects

Method used

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  • Slow release drop pills comprising toraesmide active ingredient and method for preparing same
  • Slow release drop pills comprising toraesmide active ingredient and method for preparing same
  • Slow release drop pills comprising toraesmide active ingredient and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1, the preparation of drug-containing pellets

[0046]

[0047] Mix the prescription amount of lactose (or microcrystalline cellulose) and starch evenly, add the binder prepared by sucrose or hypromellose, use a granulator (or coating pan) to start and roll the pellets to the required The mesh number is 15-30 mesh (lubricant and glidant are added while rolling the pellets), dried, and the best 18-25 mesh is screened out.

[0048]

[0049] Preparation:

[0050] Add torsemide, hypromellose (or polyvinylpyrrolidone) and talcum powder described in the prescription into water or 70% ethanol respectively, and stir for 20 minutes to form a uniform mixture. In the fluidized bed (or coating pan), keep the temperature of the pellets at 40°C-60°C, spray the mixed solution evenly on the outer layer of the blank pellets obtained in the previous step to prepare drug-containing pellets.

Embodiment 2

[0051] Embodiment 2, preparation of drug-containing pellets

[0052]

[0053]

[0054] Preparation

[0055] Mix the prescription amount of lactose (or microcrystalline cellulose), starch and medicine evenly, add sucrose and polyethylene glycol or (hypromellose and polyethylene glycol) prepared binder, and use a granulator ( or coating pan) and roll the balls to the required mesh number of 15-30 (adding lubricant and glidant while rolling the balls), sieve out the best 18-25 mesh, and dry to get.

Embodiment 3

[0056] Embodiment 3, the preparation of sustained-release pellets

[0057] prescription

[0058] The drug-containing pellet 150g of embodiment 1

[0059] Acrylic resin NE30D 20g

[0060] Talc powder 5g

[0061] water 150ml

[0062] Preparation:

[0063] The pellets obtained in Example 1 were put into a fluidized bed (or coating pan), and the temperature of the pellets was kept at 25°C. Add triethyl citrate and talcum powder to the acrylic resin NE30D aqueous dispersion, stir evenly, and spray on the outer layer of drug-containing pellets at a flow rate of 5ml / min to make sustained-release pellets.

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Abstract

The invention discloses a slow release micro-pill of tolasami active ingredient, which consists of drug micro-pill and release control layer. The preparing method comprises the following steps: filling hollow pill with tolasami or auxiliary material and drug, allocating retardant, porous agent, plasticizer or antisticking agent into dressing liquid, spraying the external layer of drug micro-pill in the dressing stove or ebullated bed to prepare the product.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and more specifically relates to a sustained-release pellet containing an active ingredient of torasemide and a preparation method thereof. Background technique [0002] According to relevant surveys, the sales of cardiovascular drugs in my country ranks third only after anti-infective drugs and gastrointestinal drugs, and hypertensive patients account for about 50% of cardiovascular cases in my country. Hypertension is a major risk factor for coronary heart disease. Long-term high blood pressure will increase the burden on the heart, leading to heart failure and concurrent renal failure, which in turn will aggravate high blood pressure and form a vicious circle. Hypertension cannot be completely cured, but strict control of blood pressure and attention to the selection of antihypertensive drugs that protect target organs can reduce the risk of cardiovascular and cere...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/44A61K9/16A61P9/12A61P7/10A61P9/04A61P13/12
Inventor 任晓文徐为人连潇嫣李洪起
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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