CN110420180A - A kind of nanoemulsion medicine and preparation method thereof containing vitamin E - Google Patents
A kind of nanoemulsion medicine and preparation method thereof containing vitamin E Download PDFInfo
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- CN110420180A CN110420180A CN201910669573.6A CN201910669573A CN110420180A CN 110420180 A CN110420180 A CN 110420180A CN 201910669573 A CN201910669573 A CN 201910669573A CN 110420180 A CN110420180 A CN 110420180A
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- ezetimibe
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
- A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
- A61K31/355—Tocopherols, e.g. vitamin E
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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Abstract
The invention discloses one kind to contain vitamin E nano-emulsion drug, by vitamin E 1g, Ezetimibe 1g, 9 g of polysorbas20,2 g of ethyl alcohol and 17 g of distilled water composition.Preparation method includes the following steps: 1) to weigh vitamin E, Ezetimibe, surfactant, cosurfactant and distilled water spare；2) Ezetimibe is added in vitamin E and is stirred evenly, added cosurfactant and stir to being completely dissolved；3) surfactant is added in the solution of step 2 preparation and is stirred evenly；4) rapid whipping step 3 at room temperature) preparation solution, stirring while is added dropwise distilled water, is stirred continuously the transparent clear liquid of system.Nanoemulsion medicine object of the invention is significant in efficacy, safe ready, has no toxic side effect and low in cost.
Description
Technical field
The invention belongs to pharmaceutical technology fields, and in particular to one kind contains vitamin E nano-emulsion drug and preparation method thereof.
Background technique
With the rapid development of modern society, people's living standard gradually improves, and Pet feeding also tends to high fat diet, suffers from
The probability of upper hyperlipidaemic conditions is higher, and in addition pet does not move for a long time, easily causes obesity, and fat pet mostly blood lipid is high,
It is serious to cause the diseases such as pulse atherosclerosis, coronary heart disease, pancreatitis.Illness pet show as spirit it is depressed, without appetite eat
It is intended to decline, laziness is unwilling activity etc..Therefore can be by reducing plasma blood-fat level, the especially horizontal stretcher of cholesterol is high
Blood lipid.Ezetimibe (Ezetimibe) is cholesterol absorption inhibitor, mainly passes through the absorption for reducing enteron aisle to cholesterol
The level of the cholesterol in diet and bile is reduced, above-mentioned cholesterol accounts for about the 75% of total cholesterol.It is main small by inhibition
A kind of specific transport protein, that is, NPC1L1 (niemann-pick c1 like1) reduces the absorption of cholesterol in intestinal mucosa,
The cholesterol levels stored in blood and in liver can be reduced simultaneously.Vitamin E can inhibit internal cholesterol biosynthesis rate-limiting enzyme, i.e. 3-
The activity of -3 methyl glutaryl coenzyme A reductase of hydroxyl, to reduce blood plasma cholesterol level.
Summary of the invention
For above-mentioned problems of the prior art and deficiency, the purpose of the present invention is to provide one kind to contain vitamin
E nanoemulsion medicine, the drug can effectively reduce the cholesterol level stored in blood and in liver.
Realizing technical solution used by foregoing invention purpose is: one kind exists containing vitamin E nano-emulsion drug, feature
In by vitamin E 1g, Ezetimibe 1g, 9 g of polysorbas20,2 g of ethyl alcohol and 17 g of distilled water composition.
The present invention, which a further object is, provides a kind of preparation method containing vitamin E nano-emulsion drug, specifically includes down
Column step:
(1) vitamin E is weighed, Ezetimibe, surfactant, cosurfactant and distilled water are spare；
(2) Ezetimibe is added in vitamin E and is stirred evenly, added cosurfactant and stir to being completely dissolved；
(3) surfactant is added in the solution of step (2) preparation and is stirred evenly；
(4) distilled water is added dropwise in the solution of rapid whipping step (3) preparation at room temperature, stirring while, and the system of being stirred continuously is in
Transparent clear liquid.
Compared with prior art, the present invention contains vitamin E nano-emulsion drug tool following advantages:
1) vitamin E and Ezetimibe are used in mixed way, and effectively reduce the cholesterol level stored in blood and in liver.
2) nanoemulsion medicine stable structure of the invention is not in phenomena such as drug is precipitated, is layered.
3) nanoemulsion medicine of the invention is significant in efficacy, safe ready, has no toxic side effect and low in cost.
Detailed description of the invention
Fig. 1 is the grain-size graph of nanoemulsion medicine of the present invention.
Specific embodiment
Embodiment 1
(1) vitamin E 1g is taken, Ezetimibe 1g, 9 g of polysorbas20, ethyl alcohol 2 g and 17 g of distilled water are spare；
(2) Ezetimibe is added in vitamin E and is stirred evenly, then plus ethyl alcohol stir to being completely dissolved；
(3) polysorbas20 is added in the solution of step (2) preparation and is stirred evenly；
(4) distilled water is added dropwise in the solution of rapid whipping step (3) preparation at room temperature, stirring while, and the system of being stirred continuously is in
Transparent clear liquid.
Experimental example 1
1) particle size and morphological observation
With the particle size of laser granulometry measurement vitamin E nano-emulsion.Pass through its form of transmission electron microscope observation.
2) study on the stability
Vitamin E nano-emulsion is subjected to accelerated test with 13000r/min centrifugation 30min, respectively in room temperature, 4 DEG C and 37 DEG C of items
30d is investigated under part, is observed 1 time every 5d, is placed under daylight and irradiates 10d, in 1,3,5,10d sampling observation；Respectively more than observation
Whether there is or not significant changes for medicament appearance and partial size in test.
3) Animal Model
The 6 week old health male Wistar rats of selection activity freely, animal feeding environment sound insulation is good, and room temperature is suitable
In (22 ± 2) DEG C, humidity is suitable for 40%-50%, and preferably, daylighting is good for ventilation, it then follows animal normal activity rule, illumination and black
Dark alternately padding clean dried, gives enough water and normal diet is fed, and adapts to animal environment 1 week, complete high lipid food
It feeds, and gives vitamine D3 simultaneously and pour into that (total amount is 5 × 10 through stomach5 U/kg is poured into 3 days).Complete high lipid food
It is continuous to feed 8 weeks, it extracts 2 out at random from hyperlipidemia model group, is anaesthetized execution, be fixed on mouse plate, take out aorta,
Blood or clot are cleaned, conventional dehydration is carried out, is embedded and be sliced with paraffin mass, HE dyeing, the micro- sem observation section are carried out to it
Blood vessel whether there is atherosclerosis and its severity, to determine whether hyperlipidemia model is established.From microscopically observation to
When vascellum endometrial hyperplasia and prominent obvious fatty streaks, it may be determined that atherosclerosis animal model modeling success.It presses
It is treated 4 weeks according to the therapeutic modality of different disposal group, in progress blood parameters detection in the 12nd week.
4) it is grouped and treats
Blank nano-emulsion group (A group): according to the volume stomach-filling blank nano-emulsion of vitamin E nano-emulsion group stomach-filling rat nano-emulsion, 1
Times/day；Model group (B group): according to the volume stomach-filling distilled water of vitamin E nano-emulsion group stomach-filling rat nano-emulsion, 1 times/day；
Ezetimibe+vitamin E group (C group): according to 5 mg/kg of rat dosage, by the Ezetimibe for being dissolved in vitamin E, (ratio is same to be received
Ratio both in rice milk) stomach-filling, 1 times/day of；Vitamin E nano-emulsion group (D group): according to 5 mg/kg Ezetimibe of rat dosage
By the vitamin E nano-emulsion stomach-filling containing Ezetimibe, 1 times/day.
5) detection of Serum Indexes
Respectively at 8 weekend vena ophthalmica clumps blood sampling and 12 weekend femoral artery blood sampling, measure TC(total cholesterol), TG(glycerol three
Ester), HDL-C(high-density lipoprotein cholesterol), LDL-C(low density lipoprotein cholesterol) it is horizontal.
6) result
Nano-emulsion average grain diameter is 28.76 ± 12.68 nm.The result is shown in Figure 1.
Nano-emulsion is still in clear without precipitating after stability result shows high speed centrifugation, when being placed at room temperature for for a long time and is long
Between solar radiation nano-emulsion system stablize.
The variation of rat TG, TC, LDL-C, HDL-C level and comparison among groups, 8 weekends are through detection discovery, model group rats
With healthy rat comparison TG, TC and LDL-C level increase, HDL-C level reduce, and there are statistical difference (P <
0.05), illustrate that long term high-fat diet can cause rat fat to increase, HDL-C is reduced, from illustrating hyperlipidemia model on the other hand
Success is moulded, the experimental study of next stage can be gone on smoothly.
When 12 weekend, Serum Lipids in Experimental HypercholesterolemicRats variation: (1) TG level compares: C, D group obvious drop horizontal compared with B group TG
Low (P < 0.05), there are statistical difference (P < 0.05) between C, D group and B group, there are statistical difference (P between C group and D group
< 0.05).(2) comparison of TC: C, D group are substantially reduced (P < 0.05) (3) LDL-C level compared with B group TC level and compare: C, D
Group is substantially reduced (P < 0.05) compared with B group LDL-C level.(4) C, D group it is horizontal compared with B group HDL-C it is significantly raised (P <
0.05), between C, D group and B group there are statistical difference (P<0.05), no difference of science of statistics between C group and D group (P>
0.05).(as shown in table 1).
The result (mean+SD) (unit mmol/L) of rat fat when 1 12 weekend of table
| Group | n | TG | TC | HDL-C | LDL-C |
| A | 10 | 5.10±0.28 | 2.65±0.12 | 0.36±0.037 | 0.71±0.074 |
| B | 10 | 5.12±0.40 | 2.68±0.15 | 0.31±0.028 | 0.72±0.055 |
| C | 10 | 4.17±0.19#▲ | 2.03±0.15#▲ | 0.46±0.032#▲ | 0.68±0.061#▲ |
| D | 10 | 3.29±0.11#*▲ | 1.18±0.05#*▲ | 0.92±0.029#*▲ | 0.23±0.033#*▲ |
Note: there are statistical difference, P < 0.05 with B group for # each group；* there are statistical difference, P < 0.05 with C group for each group.
There are statistical difference, P < 0.05 with A group for ▲ each group.
Claims (2)
1. one kind contains vitamin E nano-emulsion drug, which is characterized in that by vitamin E 1g, Ezetimibe 1g, polysorbas20 9
G, 2 g of ethyl alcohol and 17 g of distilled water composition.
2. preparing the preparation method containing vitamin E nano-emulsion drug described in claim 1, which is characterized in that including following step
It is rapid:
(1) it is spare that vitamin E, Ezetimibe, surfactant, cosurfactant and distilled water are weighed；
(2) Ezetimibe is added in vitamin E and is stirred evenly, added cosurfactant and stir to being completely dissolved；
(3) surfactant is added in the solution of step (2) preparation and is stirred evenly；
(4) distilled water is added dropwise in the solution of rapid whipping step (3) preparation at room temperature, stirring while, and the system of being stirred continuously is in
Transparent clear liquid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910669573.6A CN110420180A (en) | 2019-07-24 | 2019-07-24 | A kind of nanoemulsion medicine and preparation method thereof containing vitamin E |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201910669573.6A CN110420180A (en) | 2019-07-24 | 2019-07-24 | A kind of nanoemulsion medicine and preparation method thereof containing vitamin E |
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| Publication Number | Publication Date |
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| CN110420180A true CN110420180A (en) | 2019-11-08 |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005007111A2 (en) * | 2003-07-11 | 2005-01-27 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives as cannabinoid receptor modulators |
| CN101102768A (en) * | 2004-09-17 | 2008-01-09 | 中国医学科学院医药生物技术研究所 | Method and composition for the treatment of hyperlipidemia |
| CN101679236A (en) * | 2007-01-24 | 2010-03-24 | 克尔克公司 | Process for the preparation of ezetimibe and derivatives thereof |
| US20130210794A1 (en) * | 2010-06-18 | 2013-08-15 | Genovéva Filipcsei | Nanostructured ezetimibe compositions, process for the preparation thereof and pharmaceutical compositions containing them |
| CN103520103A (en) * | 2013-10-14 | 2014-01-22 | 陕西科技大学 | Vitamin E nano-emulsion and preparation method thereof |
-
2019
- 2019-07-24 CN CN201910669573.6A patent/CN110420180A/en not_active Withdrawn
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005007111A2 (en) * | 2003-07-11 | 2005-01-27 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives as cannabinoid receptor modulators |
| CN101102768A (en) * | 2004-09-17 | 2008-01-09 | 中国医学科学院医药生物技术研究所 | Method and composition for the treatment of hyperlipidemia |
| CN101679236A (en) * | 2007-01-24 | 2010-03-24 | 克尔克公司 | Process for the preparation of ezetimibe and derivatives thereof |
| US20130210794A1 (en) * | 2010-06-18 | 2013-08-15 | Genovéva Filipcsei | Nanostructured ezetimibe compositions, process for the preparation thereof and pharmaceutical compositions containing them |
| CN103520103A (en) * | 2013-10-14 | 2014-01-22 | 陕西科技大学 | Vitamin E nano-emulsion and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| VIKAS BALI等: "Study of surfactant combinations and development of a novel nanoemulsion for", 《COLLOIDS AND SURFACES B: BIOINTERFACES》 * |
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Application publication date: 20191108 |