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Statin-related drug composition as well as capsule preparation and preparation method thereof

A composition and drug technology, applied in the field of medicine, can solve the problems of narrow therapeutic index of colchicine, adverse reactions, enhanced colchicine muscle toxicity, etc.

Inactive Publication Date: 2015-07-01
ZHAOKE PHARMA GUANGZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the combination of colchicine and statins can enhance the effect of treating stable coronary heart disease, the therapeutic index of colchicine is narrow, and the distance between the effective concentration (0.3~4ng / mL) and the toxic concentration (>5ng / mL) is narrow. Small, moreover, colchicine itself is a substrate of P-glycoprotein, and when used in combination with P-glycoprotein inhibitory drugs (including erythromycin, cyclosporin A, verapamil, etc.), it can significantly increase its concentration in the blood Concentrations in , reach toxic concentrations, induce serious adverse reactions, and even some foods (such as grapefruit juice) also have this effect
More importantly, amiodarone, simvastatin, and atorvastatin calcium can all inhibit P-glycoprotein, and can significantly increase the concentration of colchicine in the body, thereby significantly enhancing the muscle toxicity of colchicine

Method used

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  • Statin-related drug composition as well as capsule preparation and preparation method thereof
  • Statin-related drug composition as well as capsule preparation and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0034] The present invention also provides a kind of preparation method of capsule preparation, comprises the following steps:

[0035] A) In terms of mass fraction, mix 80-90% polyethylene glycol 1000 vitamin E succinate and 5-19% auxiliary materials to obtain mixed auxiliary materials,

[0036] The excipients include macrogol glyceride laurate, macrogol 200, macrogol 300, macrogol 400, macrogol 600, ethanol, propylene glycol and caprylic capric macrogol glyceride one or more of them;

[0037] B) by mass fraction, mixing 0.1-10% of statins and 0.01-5% of colchicine with the mixed auxiliary materials obtained in step A) to obtain the content;

[0038] C) filling the content obtained in the step B) into a capsule to obtain a capsule preparation.

[0039] In terms of mass fraction, the present invention mixes 80-90% polyethylene glycol 1000 vitamin E succinate and 5-19% auxiliary materials to obtain mixed auxiliary materials, and the present invention preferably mixes the poly...

Embodiment 1

[0049] Embodiment 1 Pharmacokinetic experiment 1

[0050] The pharmacokinetic experiment on female rats was carried out according to the formula in Table 1, and Table 1 shows the ratio of raw materials and dosage of Example 1 of the present invention. The experimental animals were female rats (180g-200g), 6 in each group, 0.3ml blood samples were collected respectively at 15min, 30min, 45min, 1h, 1.5h, 3h, 4h, 6h and 24h time points after administration of the test product solution ( Anticoagulant), the colchicine concentration in plasma was measured by HPLC, and the pharmacokinetic parameters were calculated. The experimental results are shown in Table 2. Table 2 is the pharmacokinetic experimental results of Example 1 of the present invention. The data recorded in Table 2 are the mean values ​​± standard deviations of the experimental data of each group.

[0051] Table 1 Raw material proportioning and dosage of the embodiment of the present invention 1

[0052]

[0053]...

Embodiment 2

[0057] Embodiment 2 pharmacokinetic experiment 2

[0058] The experimental animals were 350g~400g male rats, 5 in each group, all underwent bile duct intubation and carotid artery intubation under anesthesia (maintaining the anesthesia state during the experiment), using 4 groups of drugs as shown in Table 3, respectively. Tail vein injection. The specific administration method is: first inject polyethylene glycol 1000 vitamin E succinate (using normal saline containing 50% concentration of propylene glycol as vehicle), and then give colchicine (using normal saline containing 50% concentration of propylene glycol) after 30 minutes. as the solvent). After colchicine was administered, bile and blood were collected every 10 minutes (12 times in total), the colchicine concentration in bile and plasma was measured, and the pharmacokinetic parameters were calculated. The results are shown in Table 4, which is the pharmacokinetic parameters of colchicine in rat bile and plasma in E...

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Abstract

The invention provides a statin-related drug composition comprising the following components in percentage by mass: 0.1-10% of a statin-related drug, 0.01-5% of colchicine and 85-98% of polyethylene glycol 1000 vitamin E succinate. In the statin-related drug composition provided by the invention, the polyethylene glycol 1000 vitamin E succinate can inhibit P-glucoprotein in advance and can avoid the statin-related drug from interacting with colchicine by influencing P-glucoprotein, thereby reducing the gastrointestinal toxicity and other toxicities of colchicine. Meanwhile, the polyethylene glycol 1000 vitamin E succinate improves the bioavailability of colchicine and reduces the treatment effective dose of colchicine, thereby further reducing the toxicity of colchicine.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a statin pharmaceutical composition, a capsule preparation and a preparation method thereof. Background technique [0002] Cardiovascular disease generally refers to ischemic or hemorrhagic diseases in the heart and systemic tissues caused by hyperlipidemia, blood viscosity, atherosclerosis, and hypertension. It is a common disease that seriously threatens the health of human beings, especially middle-aged and elderly people over 50 years old. The number of people who die from cardiovascular and cerebrovascular diseases in the world is as high as 15 million every year, ranking first among various causes of death. [0003] Statins are commonly used drugs for the treatment of cardiovascular diseases, but the existing statins cannot specifically correct the occurrence and development of inflammation in cardiovascular diseases. Atherosclerotic plaques are susceptible to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/765A61K31/366A61K31/40A61K31/22A61K31/505A61K47/34A61K9/48A61P9/10A61K31/165
CPCA61K9/48A61K31/165A61K31/366A61K31/765
Inventor 李小羿戴向荣叶文锐
Owner ZHAOKE PHARMA GUANGZHOU
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