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Liquid-state lipid micro-particles used for delivering cerebric medicine through olfactory pathway, preparation method thereof, and preparation thereof

A technology of liquid lipids and microparticles, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problem of unfavorable processing conditions for hormones, peptides, proteins, genes or vaccines, drug stability, long freeze-drying process, and inability to guarantee high quality. Encapsulation efficiency and other issues to achieve the effect of promoting drug absorption, avoiding first-pass effect, and prolonging drug action time

Inactive Publication Date: 2012-03-14
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] There are many liposome preparation methods, but most of the liposome preparation methods including the reverse phase evaporation method are more complicated, and the treatment conditions are not conducive to maintaining the stability of hormones, polypeptides, proteins, genes or vaccine drugs, and the liposomes obtained are also Does not guarantee high encapsulation efficiency and is prone to leakage
Freeze-drying can improve the stability of this type of drug, but the freeze-drying process is longer, and the liposome particle size after freeze-drying will increase several times, and it cannot be effectively controlled, reducing the risk of drugs entering the brain through the nasal olfactory area. efficiency

Method used

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  • Liquid-state lipid micro-particles used for delivering cerebric medicine through olfactory pathway, preparation method thereof, and preparation thereof
  • Liquid-state lipid micro-particles used for delivering cerebric medicine through olfactory pathway, preparation method thereof, and preparation thereof
  • Liquid-state lipid micro-particles used for delivering cerebric medicine through olfactory pathway, preparation method thereof, and preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Many traditional Chinese medicine plants such as Melaleuca pagoda, Yizhiren, Polygala, ginseng, celery seed, safflower, etc. contain active ingredients for treating stroke and senile dementia. However, due to the lack of brain selectivity of common Chinese medicine preparations such as decoctions, tablets, capsules, and injections, the toxicity and side effects are large during application, and the therapeutic effect is poor. In the first embodiment of the present invention, Huperzine A, the active ingredient of Melaleuca plant alkaloids, is used as the main drug, ethanol and Tween 80 are used as penetration enhancers, and the natural phospholipid material soybean phospholipid and cholesterol are used as the main lipid materials to prepare liquid Lipid particles.

[0025] Labeling of huperzine A: reference [Shi Senlin, Xu Lianying, Wu Jinjin, etc. Comparison of drug distribution of breviscapine in different routes of administration in the brain. Acta Pharmaceutica Sinic...

Embodiment 2

[0034] The second embodiment of the present invention utilizes two kinds of lipid particles loaded with huperzine A prepared in Example 1 to carry out animal experiments, and compares the ordinary liposomes and liquid lipid particles loaded with huperzine A to promote drug entry. brain delivery efficiency.

[0035] Experimental method: SD rats were anesthetized by intraperitoneal injection of 20% urethane (5ml / kg), fixed in supine position, the head was slightly elevated, the neck was opened, the trachea and esophagus were exposed, the trachea was intubated to maintain the normal breathing of the rat, and acrylic acid was applied. Resin seals the pharynx. Insert rat nostril about 5mm with micro-injector, slowly push into each 0.5ml of the lipid particle solution of two kinds of encapsulating huperzine A prepared in embodiment 1, after administration, at 0.5, 1, 2 and 4h (each time Point 3 rats) to collect cerebrospinal fluid and brain tissue samples to determine the drug cont...

Embodiment 3

[0043] Biomacromolecular drugs such as hormones, peptides, genes or vaccines have the characteristics of large molecular weight, poor thermal stability, and easy to be rapidly degraded in the body. The nasal olfactory pathway enters the brain. In the third embodiment of the present invention, synthetic phospholipids are used as materials, insulin is used as a model drug, combined with solid dispersion technology to improve the dissolving ability of insulin in propylene glycol, and filtered through a 0.2 μm filter membrane to prepare insulin liquid lipid particles below 250 nm.

[0044] Labeling of Insulin: Reference [Zhou Wenli, Yan Chaoying, Zhang Jiantao, Zhao Jing. Exogenous nerve growth factor on blood-brain barrier permeability and brain tissue distribution of neonatal rats with hypoxic brain injury. Chinese Journal of Biological Products. 2010, 23(3): 261-263], using chloramine T method to label insulin, made 125 I - Insulin.

[0045] package 125 The preparation of th...

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Abstract

The invention relates to liquid-state lipid micro-particles used for delivering a cerebric medicine through a nose olfactory pathway, a preparation method thereof, and a preparation thereof. The liquid-state lipid micro-particles at least comprise a medicine, a lipid material, a penetrating agent, hydroxyethyl starch, propylene glycol and water. The mass ratio of the medicine to the lipid material is 1:1 to 1:10. The volume ratio of propylene glycol to water is 2:1 to 1:10. The liquid-state lipid micro-particles are advantaged in large drug load, high deformation capacity, simple preparation method, and high entrapment rate. The micro-particles are beneficial for the medicine to be delivered into the brain through the nose olfactory pathway and to provide curative effects. The range of appropriate medicines of the liquid-state lipid micro-particles is large, and the liquid-state lipid micro-particles are especially suitable for hormone, polypeptide, gene or vaccine medicines. With the liquid-state lipid micro-particles, preparations such as aerosols, nasal drops, and gels can be produced, such that requirements of cerebric disease medication can be satisfied.

Description

【Technical field】 [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically, the invention relates to a liquid lipid microparticle for intracerebral drug delivery through the nasal olfactory pathway, a preparation method and a preparation thereof. 【Background technique】 [0002] The blood-brain barrier is the most important bottleneck for the treatment of central diseases through peripheral administration of drugs into the brain, especially for hormones, peptides, proteins, genes or vaccines for the treatment of brain diseases. At present, drugs break through the blood-brain barrier mainly through structural or dosage form modification. Due to the special connection between the nasal cavity and brain tissue, peptide or protein drugs can directly enter the brain and cerebrospinal fluid through the olfactory area, so nasal administration is a convenient way for drugs to enter the brain. [0003] Studies have found that single or continuou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/127A61K9/72A61K47/36A61K47/10A61K49/18A61K51/12A61K9/12A61P25/28
Inventor 赵应征鲁翠涛赵子逸
Owner ZHEJIANG HISUN PHARMA CO LTD
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