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Curcuma zedoary oil solid lipid nano-particle and its preparation method

A solid lipid nanometer, solid lipid technology, applied in liposome delivery, liquid delivery, pharmaceutical formulations, etc., can solve problems such as easy generation of fever, hemolysis, irritation, shock, etc., to reduce leakage and volatilization, physiological Good compatibility and improved stability

Inactive Publication Date: 2006-08-30
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the prescriptions of Zedoary Oil Injection and Zedoary Oil Glucose Injection contain a large amount of co-solvent Tween-80, which is prone to hemolysis and stimulation, causing severe toxic and side effects such as hypotension and shock, and bringing many unsafe factors to clinical application.
Therefore, the Adverse Reaction Monitoring Center of the State Food and Drug Administration has released information that reminds people to pay attention to the adverse reactions of Zedoary Oil Injection, which limits the application of the drug.
Although the zedoary oil preparations in Chinese Patent No. 200410022045.5, No. 200410100424.1 and No. 200510020215.0 do not contain Tween-80, they all use soybean oil as a carrier, which is prone to side effects such as heating, chills, palpitations, shortness of breath, headaches, and long-term Input is likely to cause adverse reactions such as elevated alanine aminotransferase
However, turmeric oil is highly volatile, and microemulsions and liposomes are prone to leakage, which affects the stability of volatile oil drugs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Prescription: Curcuma Oil 80-600mg

[0015] dynasan118 60-800mg

[0016] Phospholipids 100-600mg

[0017] Solutol HS 15 60-500mg

[0018] Vitamin E 10-50mg

[0019] TPGS 10-50mg

[0020] water 20mL

[0021] Preparation method: Heat dynasan118 in a water bath at 65-75°C until it melts, add vitamin E and zedoary oil under nitrogen, mix well as the oil phase; fully disperse Solutol HS 15, phospholipids, and TPGS in 20mL of water, and heat to The same temperature is used as the water phase; under the conditions of stirring and nitrogen, add the water phase dropwise to the oil phase at the same temperature, and continue stirring for a certain period of time to form colostrum; ultrasonic probe for 3-8 minutes or high-pressure milk homogenizer for 3-3 minutes 10 times; airtight stirring at 0-2°C for 1-2 hours; filtration with a 0.22 μm microporous membrane to obtain the solid lipid nanoparticle suspension of ...

Embodiment 2

[0023] Prescription: Curcuma Oil 80-600mg

[0024] dynasan118 100-600mg

[0025] Miglyol812N 20-300mg

[0026] Phospholipids 100-600mg

[0027] Solutol HS 15 60-500mg

[0028] Vitamin E 10-50mg

[0029] TPGS 10-50mg

[0030] water 20mL

[0031] Preparation method: Heat dynasan118 and Miglyol812N in a water bath at 45-60°C until melting, add vitamin E and zedoary oil under nitrogen, and mix well as the oil phase; fully disperse Solutol HS 15, phospholipids, and TPGS in 20mL of water, Heat to the same temperature as the water phase; add the water phase dropwise to the oil phase at the same temperature under the condition of stirring and nitrogen gas, and continue to stir for a certain period of time to form colostrum; ultrasonically probe for 3-8 minutes or use a high-pressure milk homogenizer to homogenize the milk 3 to 10 times; airtight stirring at 0 to 2°C for 1 to 2 hours; filtration through a 0...

Embodiment 3

[0033] Prescription: Curcuma Oil 80-600mg

[0034] Dynasan 160-800mg

[0035] Phospholipids 100-600mg

[0036] Solutol HS 15 60-500mg

[0037] Vitamin E 10-50mg

[0038] TPGS 10-50mg

[0039] water 20mL

[0040] Preparation method: Heat dynasan118 in a water bath at 65-75°C until it melts, add vitamin E and zedoary oil under nitrogen, mix well to make the oil phase; cool the oil phase, take it out after solidification, and cool it under liquid nitrogen or dry ice Use a ball mill to crush into a powder with a particle size of 50-100 μm; fully disperse Solutol HS 15, phospholipids, and TPGS in 20 mL of water as the water phase; disperse the drug-containing powder into the water phase, and then ultrasonically probe at 2-30 °C for 5 ~10min or 35~15 times with a high-pressure milk homogenizer; filter through a 0.22 μm microporous membrane to obtain a suspension of zedoary oil solid lipid nanoparticles. Store in a s...

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Abstract

A lipid nanoparticle of zedoary oil used for preparing solid, liquid, injection, ointment, suppository, film, aerosol, etc is prepared from zedoary oil, medicinal phosphatide, emulsifier, solid lipid, liquid lipid and deoxidant through multiple methods.

Description

technical field [0001] The invention relates to a solid lipid nanoparticle of zedoary oil and a preparation method thereof. The medicine can be used for the treatment of diseases such as anti-tumor, anti-virus and anti-thrombosis, and the route of administration is injection, oral administration, external application and the like. Background technique [0002] Zedoary oil is the volatile oil extracted from the dried rhizomes of Curcuma phaeocaulis Valeton, Curcuma kwangsiensis S.G.Lee et C.F.Liang or Curcuma wenyujin Y.H.Chen et C.Ling. It contains β-olium Various active ingredients such as sarcene, curcumol, curcumone, and gemmacone have antitumor, antiviral, and antithrombotic effects. Injections, suppositories, and ointments made from zedoary oil have been widely used in clinical practice. [0003] The second part of the 2005 edition of "Chinese Pharmacopoeia" contains Zedoary Oil Injection and Zedoary Oil Glucose Injection, which are mainly used as anti-virus. However,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/9066A61K9/127A61K9/14A61K9/02A61K9/06A61K9/12A61K9/70A61K9/08A61P31/12A61P35/00A61P7/02
Inventor 杨凯亮陈大为
Owner SHENYANG PHARMA UNIVERSITY
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