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Oleanolic acid nanometer oral system with inhibiting effect on insulin resistance

A technology for insulin resistance and oleanolic acid, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problem of large insulin loss and poor oral bioavailability of insulin resistance substances. , easy to be digested, etc.

Active Publication Date: 2017-10-27
SOUTH CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In any case, the loss of insulin during transportation is too large, so that insulin cannot be fully utilized, and exogenous insulin is an antigen for the body itself, and the immune system in the body has a certain rejection of exogenous insulin
Despite great efforts by researchers, there are still no oral products on the market for the natural treatment of insulin resistance
The oral bioavailability of natural insulin resistance substances is very poor, mainly because they are easily digested in the stomach or not easily absorbed in the intestine, which makes researchers have to solve this problem in other ways

Method used

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  • Oleanolic acid nanometer oral system with inhibiting effect on insulin resistance
  • Oleanolic acid nanometer oral system with inhibiting effect on insulin resistance
  • Oleanolic acid nanometer oral system with inhibiting effect on insulin resistance

Examples

Experimental program
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Effect test

Embodiment 1

[0071] The preparation of embodiment 1 OA-PGA micelle particle

[0072] 1. Schematic diagram of the synthesis of OA-PGA micellar particles figure 1 As shown, the carboxyl group on polygalacturonic acid (PGA) and the hydroxyl group on oleanolic acid (OA) undergo esterification reaction under alkaline conditions to form OA-PGA polymer, because polygalacturonic acid has affinity Oleanolic acid is water-based, and oleanolic acid is hydrophobic. Under the action of different hydrophilic properties at both ends, the OA-PGA polymer self-assembles to form nano-sized micellar particles.

[0073] 2. Specifically, the synthesis method of OA-PGA micellar particles is as follows:

[0074] (1) Dissolve 0.05-0.2g of polygalacturonic acid (pectin can be used instead) in 5mL of double distilled water at 55°C, adjust the pH value to 8.0 with NaOH, and then magnetically stir at 600rpm for 0.5h.

[0075] (2) Dissolve 0.05-0.2 g of oleanolic acid in 5 mL of dimethylformamide (DMF) solvent and st...

Embodiment 2

[0078] The characterization of embodiment 2 OA-PGA micelle particle

[0079] 1. Infrared spectrum and Raman spectrum detection of OA-PGA micellar particles

[0080] Dry the OA-PGA micellar particles, then put them into a mortar, add a certain amount of KBr, and grind the mixture evenly to make the particle size less than 2 μm, so as to avoid the influence of scattered light, and then put them into a dryer for drying. Press the mixture into a transparent sheet with a pressure of about 10 MPa on the hydraulic press, and measure it on the machine.

[0081] In order to understand the changes in the stage of forming OA-PGA micelles, we performed infrared spectroscopy experiments on OA-PGA micelles, as shown in figure 2As shown, in the process of synthesizing OA-PGA micellar particles, the reaction between substances caused the change of the corresponding characteristic peaks in the infrared spectrum, in OA at 1666.4cm -1 The absorption peak is the C=O stretching fluctuation on t...

Embodiment 3

[0090] Example 3 Experiment of long-term oral delivery of OA-PGA micellar particles in rat model

[0091] 1. Establishment of type 2 diabetes rat model

[0092] Purchasing rats, the incidence rate in the male and female rats of type 2 diabetes according to literature is respectively 92% and 43%, so use STZ (70mg / kg, configure with citric acid buffer) to induce male rats and High-fat feed (feeding for two weeks) was carried out to establish a type 2 diabetes model, and the fasting blood glucose value of rats ≥ 200 mg / dl was considered as a type 2 diabetes rat, which could be used for subsequent experiments.

[0093] 2. Detection of long-term drug feeding signs and oral hypoglycemic experiment in rats

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Abstract

The invention discloses an oleanolic acid nanometer oral system with an inhibiting effect on insulin resistance. A hydrophilic substance polygalacturonic acid (PGA) and a hydrophobic substance oleanolic acid (OA) are connected together via esterification reaction and then are self-assembled to form nano-scale micelle particles OA-PGA. The micelle particles increase the utilization rate of medicines while maintaining the characteristics of the two substances; serving as an insulin resistance nanometer targeted oral delivery system, the micelle particles can realize targeted transportation of the medicines and can convey the medicines into a body well, and the nanoparticles have high stability, so the sensitivity of the insulin can be improved, the activity of islet cells can be improved, and effects of inhibiting and relieving insulin resistance and organ damage are obvious; the OA-PGA micelle particles transfer natural insulin sensitizers harmless to a body by taking natural substances as carriers, do not have toxicity on cells, and have great potential and application prospect in the aspect of treating type II diabetes.

Description

technical field [0001] The invention belongs to the technical field of medical materials. More specifically, it relates to an oleanolic acid nano oral system capable of inhibiting insulin resistance and its preparation method and application. Background technique [0002] Diabetes Mellitus (DM) is a metabolic disease with multiple etiologies, characterized by chronic hyperglycemia, accompanied by disorders of sugar, fat and protein metabolism caused by defects in insulin secretion or action, and it can also cause many terrible complications. Diabetes has now become a worldwide disease, and the mortality rate continues to rise. It is considered to be one of the three major diseases that threaten human health. Diabetes is mainly divided into two types: type 1 diabetes is manifested by the patient's own immune cells attacking pancreatic β cells, making pancreatic β cells unable to secrete insulin, resulting in elevated blood sugar; type 2 diabetes is related to age, personal l...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K31/56A61K9/107A61P5/50
CPCA61K9/0053A61K9/1075A61K31/56
Inventor 关燕清李健
Owner SOUTH CHINA NORMAL UNIVERSITY
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