Resveratrol injection solution and intravenous injection

A technology of resveratrol and solution, applied in the field of medicine, can solve the problems of easy in vitro agglomeration of reticuloendothelial cells, long operation time, low inclusion rate, etc., and achieves the advantages of no toxic and side effects, good safety and simple preparation process. Effect

Inactive Publication Date: 2011-09-21
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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Problems solved by technology

[0007] 3. Inclusion compound of resveratrol, An Weijuan et al. (Preparation and identification of resveratrol-hydroxypropyl-β-cyclodextrin inclusion compound [J]. Journal of Hebei Agricultural University, 2009, 32( 1): 103-106), the average inclusion rate of the inclusion compound of resveratrol is only 63.29%, the inclusion rate is very low, the druggability is poor, it also needs freezing treatment, vacuum freeze-drying, long operation time, and preparation process Hydroxypropyl-β-cyclodextrin used in has strong hemolytic properties, especially nephrotoxicity;
[0008] 4. Resveratrol Albumin Nanoparticles, Guo Liyuan et al. (Preparation of Resveratrol Albumin Nanoparticles and its Anti-proliferation Effect on Ovarian Cancer Cells [J]. Chemical Journal of Chinese Universities, 2009, 30(3) : 474-477), the particle size of resveratrol albumin nanoparticles is 400-500nm, the particle size is relatively large, easy to aggregate in vitro and easy to be phagocytized by reticuloendothelial cells in vivo, resulting in poor stability in vivo and in vitro. In addition, the encapsulation efficiency Relatively low, only 33.97%, poor druggability
[0009] Due to the various deficiencies in the above-mentioned injections, so far no resveratrol injections have been used in clinical practice.

Method used

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  • Resveratrol injection solution and intravenous injection
  • Resveratrol injection solution and intravenous injection
  • Resveratrol injection solution and intravenous injection

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Embodiment 1 prepares resveratrol intravenous injection

[0044] 1. Preparation of resveratrol injection solution:

[0045] Take 5 grams of resveratrol, add it to 90 ml of polyethylene glycol 400 solvent, stir and dissolve at 75 ° C, then use polyethylene glycol 400 to adjust the pH to 4.5, add 0.48 Activated carbon for gram needles, adsorbed at 70°C for 25 minutes, then filtered with a 0.45 μm microporous membrane, divided the filtrate into 2 ml per bottle, pressed the cap, and then sterilized with high-pressure steam at 105°C for 60 minutes to obtain white Veratrol solution for injection.

[0046] 2. Prepare the emulsion:

[0047] (1) Prepare the oil phase: put 100 grams of soybean oil for injection and 100 grams of caprylic triglyceride in a water bath, heat to 80° C., stir to dissolve, and obtain the oil phase;

[0048] (2) Prepare the water phase: take 650 ml of water for injection, add 12 grams of soybean lecithin for injection, and 22.5 grams of glycerin, plac...

Embodiment 2

[0052] Embodiment 2 prepares resveratrol intravenous injection

[0053] 1. Preparation of resveratrol injection solution:

[0054] Take 5 grams of resveratrol, add it to 90 ml of polyethylene glycol 300, stir and dissolve at 80°C, then use polyethylene glycol 300 to make the volume to 100 ml, add 0.02 g of disodium edetate, Use acetic acid to adjust the pH to 4.5, add 0.35 g of activated carbon for needles, absorb for 30 minutes at 65 ° C, then filter with a 0.45 μm microporous membrane, divide the filtrate into 2 ml per bottle, press the cap, and then use high-pressure steam Sterilize at 115°C for 45 minutes to obtain the resveratrol injection solution.

[0055] 2. Preparation of Emulsion

[0056] (1) Preparation of the oil phase: 100 grams of caprylic triglyceride for injection, 50 grams of soybean oil, 10 grams of lanmenene oil, 10 grams of linseed oil, 15 grams of seabuckthorn oil, 5 grams of zedoary oil, and oyster oil 10 grams, mixed, placed in a water bath, heated to...

Embodiment 3

[0060] Embodiment 3 prepares resveratrol intravenous injection

[0061] 1. Preparation of resveratrol injection solution:

[0062] Take 0.1 g of resveratrol, add it to a mixed solution of 58 ml of polyethylene glycol 400, 2 ml of absolute ethanol and 25 ml of dimethylacetamide, add 0.05 g of tocopherol, stir and dissolve at 20°C , then dilute to 100 ml with polyethylene glycol 400, adjust the pH to 5.5 with hydrochloric acid and sodium hydroxide, add 0.26 g of activated carbon for needles, adsorb for 15 minutes at 100 ° C, and then filter with a 0.45 μm microporous membrane , the filtrate was divided into 5 ml bottles, capped, and then sterilized with high-pressure steam at 105° C. for 60 minutes to obtain the resveratrol injection solution.

[0063] 2. Preparation of emulsion:

[0064] (1) Prepare the oil phase: put 100 grams of soybean oil for injection and 100 grams of caprylic triglyceride in a water bath and heat to 85° C., add 10 grams of soybean lecithin for injection...

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Abstract

The invention relates to the technical field of medicament, in particular relates to a resveratrol injection solution and an intravenous injection thereof, wherein the resveratrol injection solution mainly comprises resveratrol, an injection solvent and a small amount of pH conditioning agent. The resveratrol intravenous injection is prepared by evenly mixing the resveratrol injection solution and the emulsion according to the volume ratio being 1:5 to 1:250 when in use. After the resveratrol injection solution and the emulsion are mixed, the drug loading rate of the resveratrol in the intravenous injection can achieve 1.5mg / ml, and the resveratrol can not be crystallized and separated out within 18 hours. The preparation method of the resveratrol injection solution is simple and safe, the solution has good stability and is convenient to store and transport, the resveratrol intravenous injection has good stability and no toxic and side effects by taking the emulsion as a carrier solution medium. According to the invention, the problem that the resveratrol can not be prepared into the intravenous injection and applied clinically for a long term is solved.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a resveratrol injection solution and an intravenous injection thereof. Background technique [0002] Resveratrol is an anthraquinone terpenoid compound, formerly known as 3,5,4″-trihydroxystilbene; Organic solvents such as ethanol and acetone. [0003] Resveratrol has strong pharmacological effects such as anti-cancer, anti-bacterial, anti-oxidation, anti-inflammatory, anti-allergic, and hypolipidemic. Widely used in medicine, health products, food and cosmetics and other fields. In 1998, when American Al Mindell compiled the "Anti-aging Holy Book", resveratrol was listed as one of the "100 most popular and effective anti-aging substances". In the 1990s, Chinese scientific and technological workers continued to deepen their research on resveratrol, and revealed its pharmacological effects: inhibiting abnormal aggregation of platelets, preventing myocardial infarction and cerebr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/107A61K31/05A61P3/06A61P29/00A61P31/04A61P35/00A61P37/08A61P39/06
Inventor 陈建明揭继龙张莹莹岳力群赵强高保安马露露
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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