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Metformin/ursolic acid nano oral preparation and preparation method thereof

A technology for metformin and oral preparations, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve problems such as increased liver burden, increased nephrotoxicity, increased lactic acid, etc. Availability, reduce gastrointestinal irritation, release long-lasting effects

Active Publication Date: 2018-07-13
FUZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the most common side effect of metformin is that it will irritate the digestive tract when it first enters the human body, causing nausea, vomiting, bloating and other discomfort symptoms. At the same time, taking metformin will lead to increased lactic acid and increase the burden on the liver
In addition, metformin can only be eliminated by the kidneys in the body, which also increases nephrotoxicity

Method used

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  • Metformin/ursolic acid nano oral preparation and preparation method thereof
  • Metformin/ursolic acid nano oral preparation and preparation method thereof
  • Metformin/ursolic acid nano oral preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1) Weigh 33 mg of metformin hydrochloride, dissolve it in 20 mL of distilled water, and make it into an aqueous solution of metformin hydrochloride; weigh 46.5 mg of ursolic acid powder, dissolve it in 5 mL of methanol, and make it into an ursolic acid solution;

[0034] 2) Add 20mL of metformin hydrochloride aqueous solution into a 100mL small beaker, then slowly add 1mL of ursolic acid solution dropwise to it, and stir at room temperature for 1 hour to make it self-assemble to form a metformin / ursolic acid nanoparticle solution;

[0035] 3) Take polyethylene glycol and water to prepare 150ml of 0.1mg / ml polyethylene glycol aqueous solution; mix the obtained metformin / ursolic acid nanoparticle solution with polyethylene glycol aqueous solution and freeze-dry to obtain the drug-containing powder ;

[0036] 4) Add 60 mg of lactose, 15 mg of croscarmellose sodium, 5 mg of silicon dioxide, 5 mg of magnesium stearate and 5 mg of talc into the obtained drug-containing powder...

Embodiment 2

[0038] 1) Weigh 33 mg of metformin hydrochloride, dissolve it in 20 mL of distilled water, and make it into an aqueous solution of metformin hydrochloride; weigh 46.5 mg of ursolic acid powder, dissolve it in 5 mL of methanol, and make it into an ursolic acid solution;

[0039] 2) Add 20mL of metformin hydrochloride aqueous solution into a 100mL small beaker, then slowly add 1mL of ursolic acid solution dropwise to it, and stir at room temperature for 1 hour to make it self-assemble to form a metformin / ursolic acid nanoparticle solution;

[0040] 3) Take polyvinylpyrrolidone and water to form 150ml of 0.1mg / ml polyvinylpyrrolidone aqueous solution; mix the obtained metformin / ursolic acid nanoparticle solution with polyvinylpyrrolidone aqueous solution and freeze-dry to obtain the drug-containing powder;

[0041] 4) Add 60 mg of lactose, 15 mg of crospovidone, 10 mg of silicon dioxide and 5 mg of talc to the obtained drug-containing powder, and mix evenly to obtain the metformin...

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Abstract

The invention discloses a metformin / ursolic acid nano oral preparation and a preparation method thereof. The preparation method is characterized by self-assembling metformin and a pentacyclic triterpene natural product-ursolic acid into nanoparticles of which the particle size is 180 to 220 nm through a self-assembly nano technology, and preparing the nanoparticles together with main accessories,additional accessories and a stabilizing agent into the nano oral preparation. The obtained nano oral preparation prepared by the invention has a slow release function and is capable of relieving sideeffects brought by a common oral metformin hydrochloride preparation.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a metformin / ursolic acid nanometer oral preparation and a preparation method thereof. Background technique [0002] Ursolic acid is a pentacyclic triterpenoid compound that exists in natural plants. It has various biological effects such as sedation, anti-inflammatory, antibacterial, anti-diabetic, anti-ulcer, and lowering blood sugar. Ursolic acid also has obvious anti-inflammatory effects. Oxidative function, thus widely used as medicine and cosmetic raw materials. [0003] Metformin is a biguanide oral hypoglycemic agent, and it is the first choice for type 2 diabetes that is ineffective in simple diet control and physical exercise, especially obese type 2 diabetes. Metformin has a variety of hypoglycemic mechanisms, including delaying the uptake of glucose from the gastrointestinal tract, increasing the utilization of peripheral glucose by imp...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/10A61K47/32A61K47/38A61K47/36A61K47/02A61K31/56A61K31/155A61P3/10
CPCA61K9/0053A61K31/155A61K31/56A61K47/02A61K47/10A61K47/32A61K47/36A61K47/38A61K2300/00
Inventor 邵敬伟林娟芳郭燕
Owner FUZHOU UNIVERSITY
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