CN103356609A - Compound intravenous anesthetic - Google Patents

Compound intravenous anesthetic Download PDF

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Publication number
CN103356609A
CN103356609A CN2012100869569A CN201210086956A CN103356609A CN 103356609 A CN103356609 A CN 103356609A CN 2012100869569 A CN2012100869569 A CN 2012100869569A CN 201210086956 A CN201210086956 A CN 201210086956A CN 103356609 A CN103356609 A CN 103356609A
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etomidate
propofol
compound recipe
mass ratio
intravenous
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陈希雨
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Abstract

The invention discloses a compound intravenous anesthetic which comprises propofol and etomidate according to a mass ratio of (2.5-5.5):1. The compound intravenous anesthetic disclosed by the invention is high-efficiency, safe, high in controllability, slight in adverse reaction and convenient in clinical application.

Description

A kind of compound recipe intravenous anesthesia agent
Technical field
The present invention relates to field of medicaments, relate to particularly a kind of compound recipe intravenous anesthesia agent.
Background technology
Propofol (propofol), its chemistry 2,6-diisopropylphenol by name is to be used for generally clinically at present that induction of anesthesia, anesthesia are kept, a kind of novel quick, the fugitive intravenous anesthetic of ICU critical patient calmness.Propofol injection oozes intravenous fluid for white waits, and every milliliter contains 10 milligrams of Disoprivans, includes simultaneously refined soybean oil, refine yolk lecithin, glycerol and water for injection etc.This product is the fugitive intravenous anesthetic of induced by alkyl hydroxybenzene, by activating GABA receptor-chloride ion complex, the performance sedative-hypnotic effect.During clinical dosage, propofol increases the chloride ion conduction, makes the sense of GABA receptor desensitization when heavy dose of, thereby suppresses the central nervous system, produces calm, hypnotic effect, and it is 1.8 times of penthiobarbital that its anesthesia is tired.Rapid-action, action time is short, and during with the 2.5mg/kg intravenous injection, onset time is 30-60 second, holds time approximately about 10 minutes, revives rapidly.
Etomidate, other titles: Eto-lipuro, specification: Emulsion: 20mg/10mlx1 ampoule.Etomidate is a kind of hypnosis intravenous anesthetics, is imidazole derivative, and safety is large, is one of induction of anesthesia medicine commonly used, the history in existing 30 years of etomidate clinical practice.Etomidate is non-barbiturates intravenous sedation medicine, is the hydroxylation salt of imidazoles, molecular formula C14H16N2O2, molecular weight 244.29.Etomidate is water insoluble, and is unstable in the neutral solution.Mainly contain two kinds of dosage forms in clinical practice: 1. water preparation: etomidate is dissolved in the injection that is prepared from 35% propylene glycol; 2. lipomul: etomidate is dissolved in the injection that is prepared from the long-chain triglyceride in 20%.Two kinds of dosage forms are except main solvent difference, and topmost difference is that osmotic concentration is different.The osmotic concentration of water preparation is 4640mOsm/L, is higher than the physiology osmotic concentration far away; The osmotic concentration of Emulsion is 390mOsm/L, near physiology osmotic concentration scope.Therefore compare with water preparation, lipomul can significantly reduce the side effect such as injection pain and blood vessel injury.Etomidate does not precipitate when mixing with clinical anesthesia common drug such as muscle relaxant, vasoactive drug or lignocaine etc.
During clinical anesthesia is used at present, mostly be single choice the third pool sweet smell or the compound opium kind analgesics thing of etomidate and carry out balanced anesthesia, the third pool sweet smell has strong vasodilator and myocardiac inhibition and respiration inhibition effect, often cause comparatively serious circulation inhibition and respiration inhibition effect, respiration inhibition is more obvious during special 5 usefulness opioid drug.Etomidate then has myoclonus and higher incidence of vomiting.Cause anesthetic risks and untoward reaction to increase, clinical application range is limited.
Summary of the invention
The object of the present invention is to provide a kind of compound recipe intravenous anesthesia agent, to solve above-mentioned the topic that exists in the prior art.Compound recipe intravenous anesthesia agent highly effective and safe provided by the invention, controllability is strong, and untoward reaction is slight, and is clinical easy to use.Compound preparation of the present invention, the ingredient reasonable mixture ratio is given full play to the synergism between different pharmaceutical, reduces adverse reaction rate separately, and excellent performance is safe and efficient, easy to use, and production technology is ripe, uses low cost.
Technical scheme provided by the invention is as follows:
A kind of compound recipe intravenous anesthesia agent is characterized in that: in mass ratio, comprise propofol and etomidate 2.5-5.5: 1.Anesthetis in this ratio range, than any medicine of independent use, its untoward reaction has reduction.
More preferably, in mass ratio, comprise propofol and etomidate 4-5.5: 1.Anesthetis in this proportion, its respiration inhibition and circulation suppress lower.
More preferably, in mass ratio, comprise propofol and etomidate 2.5-4: 1.Myoclonus and postoperative nausea, vomiting, postoperative bellyache incidence rate be lower,
Best, in mass ratio, comprise propofol and etomidate 4: 1.The anesthetis of this proportioning has maximum cooperative effect and minimum adverse reaction rate.That its respiration inhibition and circulation inhibition, myoclonus and postoperative nausea, vomiting, postoperative bellyache incidence rate all reach is minimum,
Preferably, described etomidate is lipomul.
A kind of compound recipe intravenous anesthesia agent by aforesaid proportioning, is mixed in proportion into mixed solution with these two kinds of medicines, or is sub-packed in binding sale in the different vessels by proportioning.
Compound recipe intravenous anesthesia agent of the present invention in use, can be used with reference to the consumption of propofol dose,equivalent 2.5mg/kg.
The present invention is mixed into mixed solution by optimal proportion in advance with etomidate and the fragrant two kinds of medicines of the third pool, or be to be sub-packed in bundle sale in the different vessels in proportion, inject simultaneously during use and carry out Compound Intravenous Anesthesia, avoid drug ratios unreasonable, arbitrarily larger, and need calculate separately use amount, extract separately, complex operation, administration time and order are different, the defective of impact anesthesia quality.And avoided easily obscuring because these two kinds of medicinal liquid outward appearances are identical, the medication that leads to errors may wait weak point.
The present invention mainly is the defective of eliminating etomidate with propofol, through a large amount of clinical trial certificates of inventor, if dosage of propofol is excessive, for example surpasses 5.5: 1, and then the shortcoming of propofol self will embody more obvious; If dosage of propofol is very few, for example less than 2.5: 1, then eliminate the poor effect of etomidate shortcoming.
Compound preparation of the present invention is given full play to synergism between different pharmaceutical and the complementarity of pharmacological action, utilizes existing final drug in dosage form and drug solvent something in common, greatly simplifies pharmaceutical technology, reduces development cost.Have complementary advantages in pharmacological property, elimination the untoward reaction used of single medicine, have easy and simple to handle, easily control of depth of anesthesia control, safe and efficient, circulation suppresses, respiration inhibition, myoclonus, the advantage such as the adverse reaction rate of the common three intravenous anesthetics such as vomiting is low, and degree is slight.Can directly utilize existing finished product pharmaceutical technology; Need not to carry out great production technology and update, thereby the advantage such as reduce production costs.
The specific embodiment
1.1 case is selected: the outpatient service early pregnancy patient of obstetrics 600 examples, age 20-35 one full year of life, body weight 40-75kg; ASA scoring I level is previously without great internal organs illness history, medicine-less allergy history.Routine examination before the art: hemanalysis, coagulation function, EKG, nothing by mouth 8h before the art.At random case is divided into: fragrant (200mg/20ml)-etomidate (20mg/10ml) fat milk of the third pool mixture different proportion contrast groups.Every group of 200 examples.
The A group, dose ratio (mass ratio) 2.5: 1; The B group, dose ratio (mass ratio) 4: 1; The C group, dose ratio (mass ratio) 5.5: 1.
1.2 medicine dose,equivalent: propofol: etomidate dose,equivalent ratio is about 8.3: 1; A group mixed liquor propofol dose,equivalent concentration is 14.4mg/ml; B group mixed liquor propofol dose,equivalent concentration is 13.7mg/ml; C group mixed liquor propofol dose,equivalent 13.1mg/ml;
1.3 anesthesia: after patient enters the room, measure HR, MAP, SPO2, open veins of upper extremity passage, each is organized patient and all gives fentanyl 1ug/kg, the slow quiet propofol-Etomidate fatty emulsion mixed liquor dose,equivalent 2.5mg/kg that pushes away injects time>60s behind the 30s of interval.Move such as body, append 1/5~1/4 first dosage of first dosage.
1.4 monitoring index: the indexs such as the MAP of 1min, 2min, 3min, 5min, HR, SPO2 reach the drug use amount of respectively organizing, recovery time, reach the untoward reaction such as myoclonus in the art, postoperative nausea, vomiting, stomachache after the injection.
2 results
Referring to table 1 to table 3, three groups of corrective surgery modes are identical, age, body weight, pregnant time and operating time are all without significant difference, contrast every monitoring index and adverse reaction rate, myoclonus and postoperative nausea in the A group art, vomiting, postoperative bellyache incidence rate are higher, there is significant difference in drug use dosage greater than B group and C group; Respiration inhibition and circulation suppress significantly greater than two groups of A, B in the C group art, drug dose and B group no significant difference.
MAP before and after three groups of patient's medications of table 1, HR, SpO2 value ()
Figure BDA0000147958050000041
Compare p<0.05, p<0.01 with basic value
Figure BDA0000147958050000042
Figure BDA0000147958050000051
With B group ratio, P<0.05, △ △P<0.01; Compare P<005, P<001 with the A group

Claims (6)

1. compound recipe intravenous anesthesia agent is characterized in that: in mass ratio, comprise propofol and etomidate 2.5-5.5: 1.
2. a kind of compound recipe intravenous anesthesia agent as claimed in claim 1 is characterized in that: in mass ratio, comprise propofol and etomidate 4-5.5: 1.
3. a kind of compound recipe intravenous anesthesia agent as claimed in claim 1 is characterized in that: in mass ratio, comprise propofol and etomidate 2.5-4: 1.
4. a kind of compound recipe intravenous anesthesia agent as claimed in claim 1 is characterized in that: in mass ratio, comprise propofol and etomidate 4: 1.
5. such as each described a kind of compound recipe intravenous anesthesia agent of claim 1 to 4, it is characterized in that: described etomidate is lipomul.
6. compound recipe intravenous anesthesia agent is characterized in that: according to claim 1 to 4 each proportionings, sell after these two kinds of medicines are mixed in proportion into mixed solution, or being sub-packed in proportion in the different vessels binding sells.
CN2012100869569A 2012-03-28 2012-03-28 Compound intravenous anesthetic Pending CN103356609A (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104800396A (en) * 2015-04-29 2015-07-29 张如意 Anesthetic and preparation method and use method thereof
CN105395482A (en) * 2015-11-24 2016-03-16 四川百利药业有限责任公司 Propofol composition for injection and preparation method thereof
WO2018014770A1 (en) * 2016-07-22 2018-01-25 四川海思科制药有限公司 Phenol derivative and etomidate pharmaceutical composition, pharmaceutical preparation, and application thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101032467A (en) * 2007-04-13 2007-09-12 西安力邦制药有限公司 Superregulated long-cycled lipid emulsion carrying medicine reagent for mainline

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101032467A (en) * 2007-04-13 2007-09-12 西安力邦制药有限公司 Superregulated long-cycled lipid emulsion carrying medicine reagent for mainline

Non-Patent Citations (2)

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Title
李茂芳等: "丙泊酚与依托咪酯联合诱导用于老年人麻醉临床观察", 《吉林医学》, vol. 32, no. 35, 31 December 2011 (2011-12-31), pages 7483 - 7484 *
邓彩英等: "丙泊酚联合依托咪酯对全麻诱导气管插管期间血流动力学的影响", 《广东医学》, vol. 33, no. 3, 28 February 2012 (2012-02-28), pages 401 - 403 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104800396A (en) * 2015-04-29 2015-07-29 张如意 Anesthetic and preparation method and use method thereof
CN105395482A (en) * 2015-11-24 2016-03-16 四川百利药业有限责任公司 Propofol composition for injection and preparation method thereof
WO2018014770A1 (en) * 2016-07-22 2018-01-25 四川海思科制药有限公司 Phenol derivative and etomidate pharmaceutical composition, pharmaceutical preparation, and application thereof
CN109310676A (en) * 2016-07-22 2019-02-05 四川海思科制药有限公司 The pharmaceutical composition of a kind of phenol derivatives and Etomidate, pharmaceutical preparation and application thereof
CN112245426A (en) * 2016-07-22 2021-01-22 四川海思科制药有限公司 Pharmaceutical composition and pharmaceutical preparation of phenol derivative and etomidate and application of pharmaceutical composition and pharmaceutical preparation

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Application publication date: 20131023