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Drug composition containing acetylshikonin and application thereof in drugs for pulmonary artery hypertension

An acetylshikonin and pulmonary arterial hypertension technology, applied in the field of medicine, can solve the problems of not being included in the basic medical insurance drug catalogue, unsatisfactory treatment effect, and no research reports have been found, so as to improve pulmonary vascular remodeling, Efficacy of alleviating pulmonary arteriolar remodeling and reducing right heart failure

Inactive Publication Date: 2018-01-12
WUXI PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The development and application of the three types of targeted drugs have played an important role in the current treatment of PAH, but due to insurmountable side effects and the therapeutic effect are not satisfactory; most of the targeted drugs for PAH are imported drugs, which are expensive. Not included in the basic medical insurance drug list, resulting in huge economic pressure for PAH patients to take long-term combined drugs
Modern pharmacological studies have shown that acetylshikonin has various pharmacological activities, including scavenging oxygen free radicals, preventing the reduction of superoxide dismutase (SOD), and exerting antioxidant effects; inhibiting the activity of acyl-CoA, reducing cholesterol levels, Protect the cardiovascular system; reduce blood pressure, antithrombotic and inhibit platelet aggregation; enhance protein kinase B (PKB) activity, exert insulin-like biological activity, prevent diabetes and its complications; in addition, acetylshikonin inhibits new microvascular The production of acetylshikonin plays a tumor suppressor role, but so far, we have not found any relevant research reports on the treatment of pulmonary arterial hypertension with acetylshikonin

Method used

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  • Drug composition containing acetylshikonin and application thereof in drugs for pulmonary artery hypertension
  • Drug composition containing acetylshikonin and application thereof in drugs for pulmonary artery hypertension
  • Drug composition containing acetylshikonin and application thereof in drugs for pulmonary artery hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The preparation method of the pharmaceutical composition containing acetylshikonin, the steps are as follows:

[0043] (1) Preparation of medicinal solution: Stir the acetylshikonin compound, sorbitol and citric acid with water for injection at a weight ratio of 10:3:1 until completely dissolved, adjust the pH to 6.8-7.6 with sodium bicarbonate, and then inject Water until the total volume of the solution is 200-250 times the mass of acetylshikonin;

[0044] (2) Decolorization of medicinal liquid: use medical activated carbon to decolorize the prepared medicinal liquid at room temperature, filter and decarbonize, and filter the obtained filtrate to sterilize with microporous membrane filtrate of 0.22 μm pore size, and divide it with sterilized ampoule or vial Pack;

[0045] (3) Preparation: according to the needs, the sub-package solution obtained in step (2) is made into a required dosage form, and a pharmaceutical composition containing acetylshikonin is obtained.

...

Embodiment 2

[0048] The establishment of embodiment 2 pulmonary hypertension rat model

[0049] SU5416 is a fat-soluble small molecule vascular endothelial growth factor (vascular endothelial growthfactor, VEGF) receptor signal transduction inhibitor. The study found that SU5416 combined with chronic persistent hypoxia (10%O 2 ) induced pulmonary hypertension model in rats can better simulate pulmonary vascular plexus-like lesions when human pulmonary hypertension occurs. SU5416 combined with chronic continuous hypoxia for 3 weeks can improve the mean pulmonary arterial pressure (mPAP), RVSP, right ven-tricular hypertrophy index (right ven-tricular hypertrophy index, RVHI), pulmonary arteriole WT% and muscularization degree in rats Significantly higher, narrow lumen, showing obvious pulmonary vascular remodeling, indicating that SU5416 combined with chronic hypoxia can more effectively induce and establish a reliable model of pulmonary hypertension than simple normal pressure chronic hypo...

Embodiment 3

[0053] Example 3 Effect of acetylshikonin on hemodynamic indexes in rats with pulmonary arterial hypertension

[0054] After calculating the survival rate, the rats were anesthetized with 0.2 mL / kg of 10% chloral hydrate, and the right external jugular vein was bluntly dissected. The pressure of the right ventricle of the rats was detected by classical right heart catheterization, and the average systolic blood pressure of each group was recorded and counted. Systemic circulation results display (such as figure 1 ), there were no significant differences in heart rate, systolic and diastolic blood pressure among the groups. It shows that the drug has no obvious effect on the systemic circulation. Right ventricular pressure results (eg figure 1 ) showed that the right ventricular pressure in the model group was significantly higher than that in the normal group, indicating that the modeling was successful. Compared with the model group, the positive drug and acetylshikonin dos...

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Abstract

The invention relates to a new pharmacological action of a traditional Chinese medicine simplex component-acetylshikonin, belonging to the technical field of medicines. The drug composition containingacetylshikonin comprises an effective dosage of acetylshikonin required for treatment and a carrier or an auxiliary material pharmaceutically acceptable, and further comprises a drug composition prepared together with other substances in any proportion and used in drugs preventing and relieving pulmonary artery hypertension and complications thereof. The acetylshikonin of the invention is a monomeric compound extracted from the wide raw material resource radix arnebiae, has low toxicity, has great application and development prospect, is an ideal, new traditional Chinese medicine monomer fortreating hypoxic pulmonary artery hypertension, and can be applied to preparation of products for preventing and treating pulmonary artery hypertension.

Description

technical field [0001] The invention relates to a novel pharmacological effect of acetylshikonin, a monomer component of traditional Chinese medicine, in particular to a pharmaceutical composition containing acetylshikonin and its application in pulmonary arterial hypertension medicine, belonging to the technical field of medicine. Background technique [0002] Pulmonary Artery Hypertension (PAH) is a malignant disease between malignant tumors and chronic diseases. It is a clinical syndrome characterized by progressive increase in pulmonary vascular resistance. Vascular proliferation and remodeling lead to increased pulmonary vascular resistance, resulting in right ventricular hypertrophy, and eventually death of the patient from right heart failure. Data show that the average age of diagnosis of this disease is only 36 years old. If it is not treated in time, the average survival time of patients is only 2.8 years, which is only better than liver cancer and worse than other...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/222A61P9/12A61P11/00
Inventor 聂晓伟秦国伟王谦戴友爱谈建新陈员沈忱悠叶书高杨旭生陈静瑜
Owner WUXI PEOPLES HOSPITAL
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