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Betulinic acid nanometer suspension and preparation method thereof

A nano-suspension, betulinic acid technology, applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of reducing drug safety, low encapsulation rate, and increased heart rate. Nephrotoxicity and neurotoxicity and other problems, to achieve the effect of increasing saturation solubility and dissolution rate, solubility and dissolution rate improvement, and green non-toxic drug loading

Active Publication Date: 2019-05-03
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Betulinic acid also has certain defects, such as poor water solubility, the solubility in water is only 21 μg / mL, low bioavailability, and poor targeting, which limits its clinical application
[0006] At present, the existing betulinic acid preparations include: betulinic acid sustained-release tablets, but due to the poor water solubility of betulinic acid itself, the release rate of the sustained-release tablets is greatly reduced, which will directly affect its bioavailability; Liposome, due to the addition of PEG to attach to the surface of the drug, greatly avoids the recognition of the liposome by the immune system, poor targeting, and low encapsulation efficiency; betulinic acid nanoemulsion, because the oil phase solvent is polyoxyethylene Castor oil, significantly increased cardiorenal toxicity and neurotoxicity, reduced drug safety

Method used

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  • Betulinic acid nanometer suspension and preparation method thereof
  • Betulinic acid nanometer suspension and preparation method thereof
  • Betulinic acid nanometer suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Weigh 2 mg of poloxamer 188 (P188) or 2 mg of egg yolk lecithin into 20 ml of deionized water, stir magnetically at 600 rpm for 30 minutes to fully saturate the stabilizer in the water; weigh 40 mg of betulinic acid and add it to the aqueous solution of the stabilizer, Stir for 30 minutes; place the above liquid in an ultrasonic cell disruptor for 5 minutes to obtain a coarse suspension; media grind the above coarse suspension at 1500 rpm for 95 minutes to obtain betulinic acid nanosuspension. The measured particle diameter was 946±105.9 nm, and the polydispersity index (PDI) was 0.51±0.13.

Embodiment 2

[0040] Weigh 4mg of poloxamer 188 (P188) or 4mg of egg yolk lecithin into 20ml of deionized water, stir magnetically at 600rpm for 30min to fully saturate the stabilizer in the water; Stir for 30 minutes; place the above liquid in an ultrasonic cell disruptor for 5 minutes to obtain a coarse suspension; media grind the above coarse suspension at 1500 rpm for 95 minutes to obtain betulinic acid nanosuspension. The measured particle diameter was 918±39.7 nm, and the polydispersity index (PDI) was 0.31±0.17.

Embodiment 3

[0042] Weigh 3mg of poloxamer 188 (P188) and 3mg of egg yolk lecithin into 20ml of deionized water, and stir magnetically at 600rpm for 30min to fully saturate the stabilizer in the water; weigh 40mg of betulinic acid and add it to the aqueous stabilizer solution, Stir for 30 minutes; place the above liquid in an ultrasonic cell disruptor for 5 minutes to obtain a coarse suspension; media grind the above coarse suspension at 1500 rpm for 95 minutes to obtain betulinic acid nanosuspension. The measured particle size is 909±22.8 nm, and the polydispersity index (PDI) is 0.27±0.05.

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Abstract

The invention discloses a betulinic acid nanometer suspension and a preparation method thereof. The betulinic acid nanometer suspension is mainly prepared from betulinic acid and a stabilizing agent,wherein the stabilizing agent comprises poloxamer 188 and egg yolk lecithin. Compared with betulinic acid self-assembled nanoparticles or betulinic acid nanoemulsion and the like in the prior art, theobtained betulinic acid nanometer suspension is lower in consumption of auxiliary materials, the saturation solubility and the dissolving out rate of medicines are notably increased, restraining of accumulation of particles is facilitated, and the betulinic acid nanometer suspension has long-term physical stability. Organic solvents are not added, and an environment-friendly idea is merged, so that a nanometer preparation being green, non-toxic and high in medicine carrying amount is creatively obtained. In vivo pharmacokinetics research shows that Cmax and AUC<0-t> are notably increased, andthe trend that the smaller the particle diameters are, the larger the AUC is, and the higher the biological availability is presented. The AUC of the betulinic acid nanometer suspension of which theparticle diameter is about 160nm is the highest, the biological availability is notably improved, and the betulinic acid nanometer suspension is favorable for natural products having various bioactivity to be used as a medicine for clinical application further.

Description

technical field [0001] The invention belongs to the technical field of betulinic acid preparations, and in particular relates to a betulinic acid nanosuspension and a preparation method thereof. Background technique [0002] Betulinic acid (C 30 h 48 o 3 , Betulinic acid) is a pentacyclic triterpene acid, mainly extracted from birch bark. Its chemical structural formula is as follows: [0003] [0004] Studies in recent years have shown that BA, as a natural compound, has outstanding performance in anti-tumor. Betulinic acid has inhibitory effects on more than 20 different tumor cells to a certain extent, and induces cell death through various mechanisms, such as: inducing apoptosis, inhibiting angiogenesis, hindering cell cycle, inhibiting invasion and migration, reversing Multidrug resistance, immune regulation, autophagy, etc. Secondly, betulinic acid can also indirectly inhibit the ATP-dependent P-gp efflux pump by destroying the mitochondria of tumor cells, and...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/19A61K47/10A61K47/24A61K31/56A61P35/00
Inventor 李俊松王若宁王鑫
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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