CN107412161A - A kind of methoxyestradiol intravenous injection of self-emulsifying 2 and preparation method thereof - Google Patents
A kind of methoxyestradiol intravenous injection of self-emulsifying 2 and preparation method thereof Download PDFInfo
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- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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Abstract
The present invention relates to a kind of methoxyestradiol intravenous injection of self-emulsifying 2 and preparation method thereof, belong to field of pharmaceutical preparations.The methoxyestradiol intravenous injection of self-emulsifying 2 of the present invention, is mainly made up of the raw material of following percentage by weight：2 methoxyestradiols 0.1 10%, oil for injection 4.9 30%, emulsifying agent 10 80%, assistant for emulsifying agent 0 85%.Gained self-emulsifying 2 methoxyestradiol intravenous injection drugloading rate of the invention is high, stability is good, has certain targeting, increases drug effect, reduce toxic side effect, security is good；And preparation technology is simple, cost is low, has good industrialization and Commercial Prospect.
Description
Technical field
The present invention relates to a kind of self-emulsifying 2ME2 intravenous injection and preparation method thereof, belong to pharmaceutical preparation
Field.
Background technology
2ME2 is a kind of steroid hormone class compound, is a kind of endogenous metabolites of estradiol, belongs to
Novel hormonal series antineoplastic medicament.Since the 1990s, numerous studies show, 2ME2 has induction swollen
Apoptosis of tumor and differentiation, antineoplastic vascular is newborn, suppresses the effect such as tumor cell proliferation, to kinds of tumors, including chronic grain
Chronic myeloid leukemia, breast cancer, liver cancer, stomach cancer etc., there is antitumor activity.
Clinical studies show, 2ME2 is orally active, and still, as other steroid hormones, 2-ME is molten
Solution property solubility poor, in water is about 2 μ g/mL, and oral rear bioavilability is relatively low, and its oral rear internal pharmacokinetics
Learn irregular, correlation is lacked between pharmacokinetics and dosage.Therefore, 2ME2 preparation used for intravenous injection is prepared
The defects of can avoiding being administered orally, there is certain practical significance.
At present, for the related improving dosage form of 2ME2 and patent application have nanoemulsion used for intravenous injection,
Nano suspension and its lyophilized formulations, solubilized formulation (including oral solid formulation and liposome) etc..
Publication No. CN 101249070A Chinese invention patent 2ME2 vena nano emulsions, by weight
It is the 2ME2 0.05%~0.5% of volume ratio, oil for injection 5%~50%, emulsifying agent 0.05%~5%, isotonic
Conditioning agent 2%~6%, pH adjusting agent and surplus are made up of water for injection, and its preparation technology is complicated.
The relevant report of self-emulsifying 2ME2 intravenous injection is there is no at present.
The content of the invention
It is an object of the invention to provide a kind of self-emulsifying 2ME2 intravenous injection, and 2- first is improved to reach
The purpose of the solubility of epoxide estradiol, high drug load and targeting.
Second purpose of the invention is to provide a kind of preparation method of self-emulsifying 2ME2 intravenous injection.
To achieve the above object, the technical scheme is that：
A kind of self-emulsifying 2ME2 intravenous injection, is mainly made up of the raw material of following percentage by weight：2-
Methoxyestradiol 0.1-10%, oil for injection 4.9-30%, emulsifying agent 10-80%, assistant for emulsifying agent 0-85%.
The oil for injection be crude vegetal, a length of C8-C10 of chain fatty glyceride in any one or it is several
Kind.
The crude vegetal is any one in soybean oil, corn oil, castor oil, safflower oil, cottonseed oil, olive oil
It is or several.
The fatty glyceride of a length of C8-C10 of chain be preferably saturation Trivent OCG or Triglyceride DDD or
The triglycerides of saturation caprylic-capric acid mixing.
The emulsifying agent be phosphatide, Tween 80, Pluronic F68, in Cremophor EL 35 any one or
It is several.
The phosphatide is any one or a few in natural phospholipid, semi-synthetic phosphatide, synthetic phospholipid.
The natural phospholipid is any one or two kinds in soybean lecithin, egg yolk lecithin；The semi-synthetic phosphatide
For hydrogenated soya phosphatide, hydrogenation yolk phospholipid；The synthetic phospholipid is DOPC, two myristoyl phosphatidyl second
Hydramine, DPPE, two myristoyl phosphatidylserines, DSPE,
Dilauroyl lecithin, two myristoyl lecithin, DPPC or distearyl acyl group lecithin and on
State any one or a few in the polyethyleneglycol derivative of synthetic phospholipid.
The assistant for emulsifying agent be docosahexaenoic acid, polyethylene glycol, TPGS, cholesterol,
One or more in ethanol, glycerine, ethyl acetate, propane diols.
Appropriate emulsifying agent may be such that formed emulsifying film is more firm with assistant for emulsifying agent collective effect, and increase forms breast
The stability of agent.
Above-mentioned self-emulsifying 2ME2 intravenous injection, in addition to pharmaceutically acceptable additives；It is described
Additives are any one or a few in bacteriostatic agent, antioxidant, pH adjusting agent, osmotic pressure regulator.
Above-mentioned osmotic pressure regulator is any one or a few in propane diols, glycerine, mannitol.
Above-mentioned antioxidant includes complexing of metal ion agent, preferably second two by tetraacethyl and its sodium salt, calcium salt, vitamin E,
One or more in vitamin C.
Above-mentioned self-emulsifying 2ME2 intravenous injection is the self-emulsifiable preparation of transparent clarification.Add during Clinical practice
Into physiological saline or 5% glucose solution, jog can form the emulsion of 10-10000nm particle diameters, for intravenously administrable.On
The particle diameter for stating emulsion is preferably 10nm~500nm.
The preparation method of above-mentioned self-emulsifying 2ME2 intravenous injection, comprises the following steps：
The one kind or two being first dissolved in 2ME2 by formula ratio in oil for injection, emulsifying agent, assistant for emulsifying agent
In the mixed liquor of kind, remaining dissolution of raw material is added, is produced.
Remaining above-mentioned raw material refers to the raw material for not adding reaction system.
The preparation method of above-mentioned self-emulsifying 2ME2 intravenous injection, comprises the following steps：
2ME2 is dissolved in the mixed liquor of oil for injection, emulsifying agent, assistant for emulsifying agent by formula ratio, i.e.,
.
Self-emulsifying 2ME2 intravenous injection of the present invention has advantages below：
1) drugloading rate is high, stability is good, is advantageous to the transport and storage of medicine；
2) there is certain targeting, increase drug effect, toxic side effect is small；
3) preparation technology is simple, and cost is low, has good industrialization and Commercial Prospect.
Embodiment
Embodiment 1
Self-emulsifying 2ME2 intravenous injection of the present invention, is made up of the raw material of following percentage by weight：2- first
Epoxide estradiol 10%, saturation Trivent OCG 10%, soybean lecithin 15%, ethanol 65%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
Saturation Trivent OCG, soybean lecithin, the ethanol of formula ratio are well mixed, dissolves, adds formula ratio
2ME2 dissolves, you can forms the 2ME2 self-emulsifiable preparation of clear.The injection is taken during use
Agent 1mL is added in 5mL physiological saline, and jog can form emulsion, uses its particle diameter of dynamic light scattering determination as 156nm,
PDI 0.152。
Embodiment 2
Self-emulsifying 2ME2 intravenous injection of the present invention, is made up of the raw material of following percentage by weight：2- first
Epoxide estradiol 5%, soybean oil 10%, Tween80 50%, propane diols 35%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The soybean oil, Tween80, mixed with propylene glycol of formula ratio is uniform, dissolve, add the 2- methoxyl groups female two of formula ratio
Alcohol dissolves, you can forms the 2ME2 self-emulsifiable preparation of clear.In use, injection 1mL is taken to be added to
In the glucose of 5mL 5%, jog can form the emulsion with light blue opalescence, use its particle diameter of dynamic light scattering determination for
56nm, PDI 0.152.
Embodiment 3
Self-emulsifying 2ME2 intravenous injection of the present invention, is made up of the raw material of following percentage by weight：2- first
Epoxide estradiol 1%, soybean oil 5%, Pluronic F68 40%, polyethylene glycol 400 54%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The soybean oil, Pluronic F68, polyethylene glycol 400 of formula ratio are well mixed, dissolved, adds the 2- of formula ratio
Methoxyestradiol dissolves, you can forms the 2ME2 self-emulsifiable preparation of clear.
Embodiment 4
Self-emulsifying 2ME2 intravenous injection of the present invention, is made up of the raw material of following percentage by weight：2- first
Epoxide estradiol 5%, Triglyceride DDD 20%, Cremophor EL 35 65%, glycerine 10%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The Triglyceride DDD of formula ratio, Cremophor EL 35, glycerine are well mixed, dissolves, adds formula ratio
2ME2 dissolves, you can forms the 2ME2 self-emulsifiable preparation of clear.In use, by said preparation
5ml is added in 5ml physiological saline, is gently shaken, you can the emulsion with light blue opalescence is formed, using dynamic light scattering method
It is 35nm, PDI 0.117 to determine its particle diameter.
Embodiment 5
Self-emulsifying 2ME2 intravenous injection of the present invention, is made up of the raw material of following percentage by weight：2- first
Epoxide estradiol 0.1%, castor oil 30%, DPPE 10%, docosahexaenoic acid 59.9%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The castor oil, DPPE, docosahexaenoic acid of formula ratio are well mixed, dissolved,
Add the 2ME2 dissolving of formula ratio, you can form the 2ME2 self-emulsifiable preparation of clear.
Embodiment 6
Self-emulsifying 2ME2 intravenous injection of the present invention, is made up of the raw material of following percentage by weight：2- first
Epoxide estradiol 0.1%, cottonseed oil 4.9%, dilauroyl lecithin 30%, TPGS 15%,
Ethanol 50%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The cottonseed oil of formula ratio, dilauroyl lecithin, TPGS, ethanol are mixed equal
It is even, dissolving, add the 2ME2 dissolving of formula ratio, you can form the 2ME2 self-emulsifying of clear
Preparation.
Embodiment 7
Self-emulsifying 2ME2 intravenous injection of the present invention is made up of the raw material of following percentage by weight：2- methoxies
Base estradiol 10%, safflower oil 10%, two myristoyl phosphatidyl-ethanolamines 80%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The 2ME2 of formula ratio is dissolved in safflower oil, two myristoyl phosphatidyl-ethanolamines and mixed
It is even, dissolving, you can form the 2ME2 self-emulsifiable preparation of clear.
Embodiment 8
Self-emulsifying 2ME2 intravenous injection of the present invention, is mainly made up of the raw material of following percentage by weight：
2ME2 8%, olive oil 20%, DOPC 50%, cholesterol 10%, propane diols 12%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The 2ME2 of formula ratio is dissolved in the mixed liquor of olive oil and propane diols, then adds formula
DOPC, the cholesterol of amount are well mixed, dissolving, you can form the 2ME2 self-emulsifying of clear
Preparation.
Embodiment 9
Self-emulsifying 2ME2 intravenous injection of the present invention, is made up of the raw material of following percentage by weight：2- first
Epoxide estradiol 8%, olive oil 20%, hydrogenate yolk phospholipid 50%, ethyl acetate 18%, 4% mannitol.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The 2ME2 of formula ratio is dissolved in olive oil, then adds the hydrogenation yolk phosphorus of formula ratio
Fat, ethyl acetate, mannitol are well mixed, dissolving, you can form the 2ME2 self-emulsifiable preparation of clear.
Embodiment 10
Self-emulsifying 2ME2 intravenous injection of the present invention, is made up of the raw material of following percentage by weight：2- first
Epoxide estradiol 0.1%, cottonseed oil 4.9%, DPPC 10%, ethyl acetate 85%.
The preparation method of self-emulsifying 2ME2 intravenous injection of the present invention, comprises the following steps：
The cottonseed oil, DPPC, ethyl acetate of formula ratio are well mixed, dissolves, adds formula ratio
2ME2 dissolves, you can forms the 2ME2 self-emulsifiable preparation of clear.
Experimental example
Physiological saline is added to carry out cavy after emulsifying gained self-emulsifying 2ME2 intravenous injection in embodiment 1
The allergic reaction of whole body initiative is tested, and vein low dose group 5mg/Kg, high dose group 30mg/Kg, measurement result is feminine gender；With
Red cell suspension determines its hemolytic, low dose group 5mg/mL, high dose group 30mg/mL, and test sample does not occur molten in 3h
Blood and red blood cell condensation phenomenon, illustrate that self-emulsifying 2ME2 intravenous injection administration security of the present invention is good, poison is secondary
Act on small.
Claims (10)
1. a kind of self-emulsifying 2ME2 intravenous injection, it is characterised in that mainly by the original of following percentage by weight
Material is made：2ME2 0.1-10%, oil for injection 4.9-30%, emulsifying agent 10-80%, assistant for emulsifying agent 0-85%.
2. self-emulsifying 2ME2 intravenous injection according to claim 1, it is characterised in that the injection
Oil is any one or a few in crude vegetal, a length of C8-C10 of chain fatty glyceride.
3. self-emulsifying 2ME2 intravenous injection according to claim 2, it is characterised in that the natural plant
Thing oil is soybean oil, the one or more in corn oil, castor oil, safflower oil, cottonseed oil, olive oil.
4. self-emulsifying 2ME2 intravenous injection according to claim 1, it is characterised in that the emulsifying agent
For the one or more in phosphatide, Tween 80, Pluronic F68, Cremophor EL 35.
5. self-emulsifying 2ME2 intravenous injection according to claim 4, it is characterised in that the phosphatide is
Any one or a few in natural phospholipid, semi-synthetic phosphatide, synthetic phospholipid.
6. self-emulsifying 2ME2 intravenous injection according to claim 5, it is characterised in that the natural phosphorus
Fat is any one or two kinds in soybean lecithin, egg yolk lecithin；The semi-synthetic phosphatide is hydrogenated soya phosphatide, hydrogenation
Yolk phospholipid；The synthetic phospholipid is DOPC, two myristoyl phosphatidyl-ethanolamines, two palmityl phosphatide
Acyl monoethanolamine, two myristoyl phosphatidylserines, DSPE, dilauroyl lecithin, two
Myristoyl lecithin, DPPC or the polyethylene glycol of distearyl acyl group lecithin and above-mentioned synthetic phospholipid
Any one or a few in derivative.
7. self-emulsifying 2ME2 intravenous injection according to claim 1, it is characterised in that described to help emulsification
Agent is docosahexaenoic acid, polyethylene glycol, TPGS, cholesterol, ethanol, glycerine, acetic acid second
Any one or a few in ester, propane diols.
8. self-emulsifying 2ME2 intravenous injection according to claim 1, it is characterised in that also include additional
Agent；The additives are any one or a few in bacteriostatic agent, antioxidant, pH adjusting agent, osmotic pressure regulator.
9. a kind of preparation method of self-emulsifying 2ME2 intravenous injection as claimed in claim 1, its feature exist
In comprising the following steps：
2ME2 is first dissolved in one or both of oil for injection, emulsifying agent, assistant for emulsifying agent by formula ratio
In mixed liquor, remaining dissolution of raw material is added, is produced.
10. a kind of preparation method of self-emulsifying 2ME2 intravenous injection as claimed in claim 1, its feature exist
In comprising the following steps：
2ME2 is dissolved in the mixed liquor of oil for injection, emulsifying agent, assistant for emulsifying agent by formula ratio, produced.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710364766.1A CN107412161A (en) | 2017-05-22 | 2017-05-22 | A kind of methoxyestradiol intravenous injection of self-emulsifying 2 and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201710364766.1A CN107412161A (en) | 2017-05-22 | 2017-05-22 | A kind of methoxyestradiol intravenous injection of self-emulsifying 2 and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108992403A (en) * | 2018-08-31 | 2018-12-14 | 田红卫 | A kind of long-acting slow-release ivermectin injection and preparation method thereof |
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| WO2002003979A2 (en) * | 2000-07-12 | 2002-01-17 | Board Of Regents, The University Of Texas System | Combination of 2-methoxyestradiol and an agent that increases intracellular superoxide anion |
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|---|---|---|---|---|
| CN1247741A (en) * | 1999-08-17 | 2000-03-22 | 刘进 | Emulsified inhalational anaesthetic for intravenous injection and its preparation |
| WO2002003979A2 (en) * | 2000-07-12 | 2002-01-17 | Board Of Regents, The University Of Texas System | Combination of 2-methoxyestradiol and an agent that increases intracellular superoxide anion |
| CN101249070A (en) * | 2008-04-02 | 2008-08-27 | 郑州大学 | 2-methoxy estradiol vena nano emulsions |
| CN101953774A (en) * | 2010-09-17 | 2011-01-26 | 郑州大学 | 2-methoxy estradiol injectable hydrogel implant |
| CN102793663A (en) * | 2012-09-12 | 2012-11-28 | 郑州大学 | Sustained-release microsphere injection containing antitumor drug (2-methoxyestradiol) |
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| Title |
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| SUNA HE等: "A Cremophor-Free Self-Microemulsified Delivery System for Intravenous Injection of Teniposide: Evaluation In Vitro and In Vivo", 《AAPS PHARMSCITECH》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108992403A (en) * | 2018-08-31 | 2018-12-14 | 田红卫 | A kind of long-acting slow-release ivermectin injection and preparation method thereof |
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Application publication date: 20171201 |