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Controlled-release pharmaceutical composition for treating thyroid dysfunction

A technology for thyroid function and controlled release of drugs, which is applied in the field of composition of new preparations, and can solve problems such as deterioration of cardiac function, induction, and unfixed T4/T3 ratio

Pending Publication Date: 2019-02-22
FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the existing drugs cannot meet the treatment needs of cardiovascular patients. In the previous research of the applicant, it was found that T3 decreased most obviously in cardiovascular emergencies. This phenomenon is different from the hypothyroid patients we usually see. Low T3 It is an important risk factor affecting the prognosis of patients with acute myocardial infarction, but the current treatment methods are still limited to supplementing conventional LT4 drugs, and the level of the active ingredient T3 cannot be guaranteed
[0007] After using T4 instead, it still needs to be converted into T3 under the action of deiodinase, and the poor response of myocardial infarction patients to L-T4 treatment is mainly due to the change of deiodinase activity in the body. In order to solve this clinical problem, the development The key is to make a reasonable ratio of T3 / T4 mixed drugs. In the treatment of T4 and T3 mixture, animal thyroid extracts were widely used in the early stage, but animal thyroid dry preparations contain many impurities, and the ratio of T4 / T3 is not fixed. The application in patients with myocardial infarction may lead to further cardiovascular risks induced by excessive hormones, and it cannot be safely applied to high-risk cardiovascular patients. What ratio of T3 / T4 should be applied has become the key to solving the suffering of patients.
[0008] Acute myocardial infarction and heart failure are one of the most important causes of death from cardiovascular diseases. Although existing treatments can delay the progression of the disease, myocardial infarction and heart failure can induce a series of neuroendocrine system abnormalities, which eventually lead to cardiac dysfunction. deterioration

Method used

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  • Controlled-release pharmaceutical composition for treating thyroid dysfunction
  • Controlled-release pharmaceutical composition for treating thyroid dysfunction
  • Controlled-release pharmaceutical composition for treating thyroid dysfunction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037]

[0038] In a 3000ml flask, add ethylcellulose in 500ml of water, and add a solution of liothyronine in 1000ml of water with continuous stirring, after mixing well, add sodium lauryl sulfate, disodium hydrogen phosphate and magnesium stearate , keep stirring at room temperature until the suspension is completely homogeneous. Put 750g of blank ball cores into the fluidized bed, and spray with the pre-prepared suspension under the following conditions: air flow: 200 cubic meters per hour, nozzle diameter: 1.0mm , Injection pressure: 0.85bar, injection of suspension: 35g / min, fluidized bed temperature: 50°C.

[0039] In a 3000 ml flask, prepare an aqueous homogeneous dispersion of Tween-80, triethyl citrate, natural carotene and Eudragit-L in purified water, and add sodium lauryl sulfate and talc, and keep stirring at room temperature until mixed The suspension is completely homogeneous. Put the single-layer coated drug-loaded pellets into the fluidized bed, and spray ...

Embodiment 2

[0042]

[0043]In a 3000ml flask, add ethylcellulose in 500ml of water, and add a solution of liothyronine in 1000ml of water with continuous stirring, after mixing well, add sodium lauryl sulfate, disodium hydrogen phosphate and magnesium stearate , keep stirring at room temperature until the suspension is completely homogeneous. Put 750g of blank ball cores into the fluidized bed, and spray with the pre-prepared suspension under the following conditions: air flow: 200 cubic meters per hour, nozzle diameter: 1.0mm , injection pressure: 0.85 bar, injection of suspension: 35 g / min, fluidized bed temperature: 60°C.

[0044] In a 3000 ml flask, prepare an aqueous solution of Tween-80, triethyl citrate, cochineal and Eudragit-L uniformly dispersed in purified water, and add sodium lauryl sulfate and talc, and keep stirring at room temperature until mixed. The suspension is completely homogeneous. Put the single-layer coated drug-loaded pellets into the fluidized bed, and spray...

Embodiment 3

[0047]

[0048] In a 1500 ml flask, add ethyl cellulose in 500 ml of water, and add a solution of liothyronine in 500 ml of water with continuous stirring, after mixing well, add sodium lauryl sulfate, disodium hydrogen phosphate and magnesium stearate , keep stirring at room temperature until the suspension is completely homogeneous. Put 750g of blank ball cores into the fluidized bed, and spray with the pre-prepared suspension under the following conditions: air flow: 200 cubic meters per hour, nozzle diameter: 1.0mm , injection pressure: 0.85 bar, injection of the suspension: 25 g / min, fluidized bed temperature: 50°C.

[0049] In a 1500 ml flask, prepare a 95% ethanol homogeneous dispersion of Tween-80, triethyl citrate, natural carotene, and shellac, and add sodium lauryl sulfate and talc, and keep stirring at room temperature until suspended The liquid is completely uniform. Put the single-layer coated drug-loaded pellets into the fluidized bed, and spray with the pre-...

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Abstract

The invention belongs to the field of medicines, and particularly relates to a pharmaceutical composition, in particular to a controlled-release pharmaceutical composition for treating thyroid dysfunction. The controlled-release pharmaceutical composition is made into pellets or pellet capsules. As for 10%-20% of thyroid hypofunction of 10%-20%, the pharmaceutical composition can promote content stability of free thyroxine and liothyronine in animals and human bodies, and the normal physiological functions of all target organs under the hormone effect are ensured.

Description

Technical field: [0001] The present invention relates to a composition of a new preparation, especially relates to the preparation of a sustained and controlled release pharmaceutical composition for treating abnormal thyroid function, which has good drug stability and content stability in the body. Background technique: [0002] The thyroid gland is an important endocrine organ of the human body. It can produce two hormones, T4 (thyroxine) and T3 (liothyronine), among which T4 accounts for the majority (about 80%) in quantity, but in tissues and cells The level of physiological activity is T3. [0003] An estimated 17 percent of women and 8 percent of men age 60 or older experience hypothyroidism. The most common cause of low thyroid production is an autoimmune disease called Hashimoto's thyroiditis, when lymphocytes produce hormones that make the thyroid gland The disease occurs when cells that produce antibodies slowly and gradually lose function. Hypothyroidism can also...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/38A61K47/32A61K9/48A61K9/20A61K31/195A61K31/198A61P5/14
CPCA61K9/2027A61K9/2054A61K9/4866A61K9/5026A61K9/5047A61K9/5078A61K31/195A61K31/198A61P5/14A61K2300/00
Inventor 唐熠达王文尧程宇镳王恺皓田间
Owner FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE