CN105496953A - Compound propofol water-based injection for dogs, preparing method thereof and application - Google Patents
Compound propofol water-based injection for dogs, preparing method thereof and application Download PDFInfo
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- CN105496953A CN105496953A CN201610044954.1A CN201610044954A CN105496953A CN 105496953 A CN105496953 A CN 105496953A CN 201610044954 A CN201610044954 A CN 201610044954A CN 105496953 A CN105496953 A CN 105496953A
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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
- A61K9/08—Solutions
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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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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Abstract
本发明涉及一种犬用复方丙泊酚水性注射液及其制备方法与应用，属于兽药制备技术领域，适用于犬的制动、麻醉。所述注射液以丙泊酚、盐酸赛拉嗪为活性组分，加入药学上可接受的载体。本发明犬用复方丙泊酚水性注射液兼具催眠、镇静、镇痛作用，能够通过一次给药，达到麻醉诱导或麻醉维持的效果，使麻醉过程更加便捷；降低了各单药的使用剂量，达到较好的麻醉效果，最低的副作用；本发明注射液性质稳定，适用于皮下、肌肉和静脉注射，注射时无疼痛；本发明制剂舍弃了应用最为广泛的脂肪乳载体，制成水性溶液，能限制微生物生长，可多次抽吸，避免了丙泊酚脂肪乳制剂的药物浪费问题。
The invention relates to a compound propofol aqueous injection for dogs and a preparation method and application thereof, which belong to the technical field of veterinary drug preparation and are suitable for immobilization and anesthesia of dogs. The injection contains propofol and xylazine hydrochloride as active components, and a pharmaceutically acceptable carrier is added. The compound propofol aqueous injection for dogs of the present invention has both hypnotic, sedative and analgesic effects, and can achieve the effect of anesthesia induction or anesthesia maintenance through one administration, making the anesthesia process more convenient; reducing the dosage of each single drug , to achieve better anesthesia effect and the lowest side effects; the injection of the present invention is stable in properties, suitable for subcutaneous, intramuscular and intravenous injection, and has no pain during injection; the preparation of the present invention abandons the most widely used fat emulsion carrier and makes an aqueous solution , can limit the growth of microorganisms, can be pumped repeatedly, and avoids the problem of drug waste of propofol fat emulsion preparations.
Description
Technical field
The invention discloses a kind of dog compounded propofol water type injection, belong to technical field of animal remedy preparation.Be applicable to the braking of dog, anesthesia.
Background technology
Propofol (2,6-Bis(1-methylethyl)phenol) is a kind of induced by alkyl hydroxybenzene vein GENERAL ANESTHETICS, and current veterinary clinic is commonly used to induction of anesthesia, anesthesia maintenance, calmness etc.After conventional administration, onset rapidly, through steady, animal is without side effect such as muscle involuntary movement, cough, singultuss.Persistent period is very short, revives completely, does not have excited phenomenon, be comparatively ideal hypnotic general intravenous anesthesia medicine, but do not have analgesic activity, therefore can not reach the object of anesthesia maintenance by alone propofol.
" Diprivan " of listing in 1986 is that research is the most ripe at present, most widely used a kind of propofol fat emulsion-type, said preparation is O/W type, containing soybean oil 100g/L, and glycerol 22.5g/L, refined lecithin 1.2g/L, very stable under this dosage form room temperature, see that light should not decompose.But lipid is the good culture medium of growth of microorganism, and therefore multiple producer adds the antibacterial such as disodiumedetate, sodium metabisulfite in the formulation, to prevent the growth of microorganism under portion's pollution condition outside.However, still can not avoid the generation of growth of microorganism, therefore, relevant manufacturers explicitly points out all in the description, extracts medicine and strictly should follow sterile working, and the medicine of Kaifeng after 6 hours, should discard.
Therefore, in the urgent need to the stable propofol dosage form of a kind of energy restricting bacterial growth.
Xylazine hydrochloride is a kind of α
2-3 adrenergic receptor agonists, is widely used in veterinary clinic, animal can be made to be in the different conditions such as peace and quiet, drowsiness, anesthesia according to dosage difference.Under general using dosage, the general anesthesia effect that animal reaches good can not be made, and only can make that animal muscle is lax, spirit is depressed, drowsiness or in the state of sleeping soundly.But when heavy dose, animal also can be made to enter dark narcotism, now then often occur untoward reaction.Common adverse effect has vomiting, and breath cycle suppresses.
Induction of anesthesia in current veterinary clinic and maintenance general employing combined anesthesia mode, i.e. conbined usage two kinds and two or more medicines, to produce addition between medicine or synergism, thus reduce the using dosage of single anesthetics, reduce untoward reaction, reach a kind of ideal anaesthetic effect.
Therefore, veterinary clinic needs a kind of pharmaceutical composition, can single administration be passed through, reach the effect of induction of anesthesia or anesthesia maintenance.
Summary of the invention
The object of the invention is to propofol and xylazine hydrochloride two kinds of medicines to carry out reasonable compatibility, select suitable carrier, make aqueous solution.Make pharmaceutical composition have hypnosis, calmness, analgesic activity concurrently, by single administration, reach the effect of induction of anesthesia or anesthesia maintenance, make induction of anesthesia and maintenance process more convenient; Reduce the using dosage of each single medicine, reach good anaesthetic effect, minimum side effect; Dog of the present invention compounded propofol water type injection has given up fat milk carrier, avoids the defect that it encourages growth of microorganism, repeatedly can aspirate, greatly can reduce the incidence rate of microbial contamination.
The object of the invention is to realize in the following manner:
A kind of dog compounded propofol water type injection, with propofol, xylazine hydrochloride for active component, adds pharmaceutically acceptable carrier.
Described dog 100mL injection every in compounded propofol water type injection contains 0.8-1.2g propofol, 0.12-0.18g xylazine hydrochloride.
Most preferably every 100mL preparation contains propofol 1.0g, xylazine hydrochloride 0.16g.
Above-mentioned carrier comprises buffer agent, cosolvent and chelating agen.
Above-mentioned dog compounded propofol water type injection, every 100mL injection consists of: buffer agent 0.3-0.4g, cosolvent 25-35g, chelating agen 0.005-0.01g, propofol 0.8-1.2g, xylazine hydrochloride 0.12-0.18g, and surplus is water for injection.
Most preferably dog compounded propofol water type injection, every 100mL injection consists of: buffer agent 0.36g, cosolvent 30g, chelating agen 0.005g, propofol 1.0g, xylazine hydrochloride 0.16g, and surplus is water for injection.
Above-mentioned buffer agent is the compositions of citric acid and sodium citrate, and ratio is 1:5.
Above-mentioned cosolvent is 2-HP-BETA-CD.
Above-mentioned chelating agen is disodiumedetate.
The above-mentioned dog preparation method of compounded propofol water type injection, comprises following steps:
Buffer agent, cosolvent, chelating agen, propofol, xylazine hydrochloride are dissolved in appropriate water for injection successively, standardize solution, filter, subpackage, sterilizing obtains.
Above-mentioned dog compounded propofol water type injection can be applied in the calmness of preparation dog, hypnosis, analgesia, flesh pine, convulsion and anaesthetic.
The present invention is by propofol, xylazine hydrochloride two kinds of compatibility of drugss, preferred by orthogonal test, determines best prescription.By the best prescription that optimizes by intravenous administration, be applied to dog.Observe its induction of anesthesia time, hold time, stage of surgical anesthesia, recovery time, the change of every physiological parameter and anaesthetic effect, find that this dog compounded propofol water type injection combines the advantage of each single medicine, greatly reduce the side effect of appearance of each prescription used time, anaesthesia process, wakeup process are steady; Complete induced anesthesia by single administration, improve the convenience of medication; Preparation energy restriction micro-organisms grows, and repeatedly can extract use, avoid the drug waste problem of propofol fat emulsion formulation.
Accompanying drawing explanation
Fig. 1 anaesthetizes every physiological parameter variation tendency of rear dog;
Fig. 2 anaesthetize rear dog analgesia, calmness, flesh pine scoring.
Detailed description of the invention
Now by the mode of embodiment, the present invention is described, experimental example only for illustration of, be never to limit to scope of the present invention.
Experimental dog, 6 (female 4 heros 2), 2.76 ± 0.39kg, 4 monthly ages.Experimental dog fasting 4 hours, prohibits water 2 hours.By the best prescription optimized, (namely every 100mL injection contains buffer agent 0.36g, cosolvent 30g, chelating agen 0.005g, propofol 1.0g, xylazine hydrochloride 0.16g, and surplus is water for injection.Wherein buffer agent is the compositions of citric acid and sodium citrate, and ratio is 1:5; Cosolvent is 2-HP-BETA-CD; Chelating agen is disodiumedetate) by intravenous administration (dosage is 0.3mL/kg), is applied to dog, observes postanesthetic induction time, hold time, recovery time, the results are shown in Table 1.
Change (the table 2 of every physiological parameter, Fig. 1), anaesthetic effect scoring (table 3, Fig. 2) is [before observation injecting anesthetic medicine (0 minute), injection rear 1,5,10,15,20,25,30 minutes following indexs are also averaged: 1. analgesic effect: acupuncture parts of body skin, and clamp lip, ear, pawl, nose, tail 5 positions judge analgesic effect.Criterion: analgesis is judged to " +++ ", hypalgesia is judged to " ++ ", and the pain sensation is obviously judged to "+", and the pain sensation is judged to "-" with before medication.2. flesh pine effect: observe stomach wall, masseter, lingualis, tail force situation.Criterion: carry and pinch abdominal wall muscle ungauged regions, tractive tongue, the upper lower jaw that swings, tail non-resistance are respectively judged to " +++ "; Carry and pinch abdominal wall muscle and shrink slight, tractive tongue, swing upper lower jaw, tail slightly resistance, is judged to " ++ "; Carry and pinch abdominal wall muscle contraction obviously, tractive tongue, the upper lower jaw that swings, tail resistance are obvious, are respectively judged to "+"; Press stomach wall and then shrink slivering shuttle shape, shortened tongue returns, opening can not, freely wag the tail and be respectively judged to "-".3. calming effects: call, beat Baoding table top, observes the reaction of dog in anaesthesia process.To audio response without, be judged to " +++ "; Performance is opened eyes, ear is dynamic is judged to " ++ "; Performance ear is dynamic, eye opening, instantaneously limbs are twitched and be judged to "+"; The struggle of performance new line is judged to "-".Above judged result is marked: each "+" meter 1 point, "-" meter 0 point].
Table 1 anesthesia duration
The every physiological parameter variation tendency of rear dog anaesthetized by table 2
Table 3 anaesthetizes the analgesia of rear dog, calmness, the scoring of flesh pine
Result shows, after the present invention is applied to dog, its major physiological parameter heart rate is obvious decline compared with before anesthesia 1 minute time, tends towards stability afterwards; Obvious decline compared with before anesthesia when Mean Arterial is pressed in 5 minutes, afterwards in slow downward trend, and is stabilized in more than 70.40mmHg; Respiration Rate after being anesthetized 1 minute time with anesthesia before obvious decline, be slowly increased to preanaesthesic level afterwards, slowly reduce again afterwards, and be stabilized in more than 19.33 beats/min; Anesthesia after animal heat slowly decline, but with anesthesia before be more or less the same; Blood oxygen saturation slowly declines after being anesthetized, but remains at more than 95%.Every physiological parameter is all in normal physiologic range.
Claims (10)
1. a dog compounded propofol water type injection, is characterized in that: injection for active component, adds pharmaceutically acceptable carrier with propofol, xylazine hydrochloride.
2. dog according to claim 1 compounded propofol water type injection, is characterized in that: every 100mL injection contains 0.8-1.2g propofol, 0.12-0.18g xylazine hydrochloride.
3. dog according to claim 1 compounded propofol water type injection, is characterized in that: described carrier comprises buffer agent, cosolvent and chelating agen.
4. dog according to claim 3 compounded propofol water type injection, is characterized in that: every 100mL injection consists of: buffer agent 0.3-0.4g, cosolvent 25-35g, chelating agen 0.005-0.01g, propofol 0.8-1.2g, xylazine hydrochloride 0.12-0.18g, surplus is water for injection.
5. dog according to claim 4 compounded propofol water type injection, is characterized in that: every 100mL injection consists of: buffer agent 0.36g, cosolvent 30g, chelating agen 0.005g, propofol 1.0g, xylazine hydrochloride 0.16g, surplus is water for injection.
6. the compounded propofol water type injection of the dog according to claim 3-5 any one, is characterized in that: described buffer agent is the compositions of citric acid and sodium citrate, and ratio is 1:5.
7. the compounded propofol water type injection of the dog according to claim 3-5 any one, is characterized in that: described cosolvent is 2-HP-BETA-CD.
8. the compounded propofol water type injection of the dog according to claim 3-5 any one, is characterized in that: described chelating agen is disodiumedetate.
9. the preparation method of compounded propofol water type injection of the dog according to claim 4 or 5, comprises following steps:
Buffer agent, cosolvent, chelating agen, propofol, xylazine hydrochloride are dissolved in appropriate water for injection successively, standardize solution, filter, subpackage, sterilizing obtains.
10. the application of compounded propofol water type injection in the calmness of preparation dog, hypnosis, analgesia, flesh pine, convulsion and anaesthetic of the dog according to claim 1-5 any one.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201610044954.1A CN105496953A (en) | 2016-01-25 | 2016-01-25 | Compound propofol water-based injection for dogs, preparing method thereof and application |
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| CN201610044954.1A CN105496953A (en) | 2016-01-25 | 2016-01-25 | Compound propofol water-based injection for dogs, preparing method thereof and application |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110638755A (en) * | 2019-10-29 | 2020-01-03 | 江苏盈科生物制药有限公司 | Propofol medium-long chain fat emulsion and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1957918A (en) * | 2006-11-15 | 2007-05-09 | 闫章年 | Compound injection of Xylazine, and preparation technique |
| CN101287447A (en) * | 2005-08-12 | 2008-10-15 | 印度血清及疫苗有限公司 | Aqueous anesthetic composition comprising propofol |
| CN101658524A (en) * | 2009-09-25 | 2010-03-03 | 南京农业大学 | A compound anesthetic for dogs |
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2016
- 2016-01-25 CN CN201610044954.1A patent/CN105496953A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101287447A (en) * | 2005-08-12 | 2008-10-15 | 印度血清及疫苗有限公司 | Aqueous anesthetic composition comprising propofol |
| CN1957918A (en) * | 2006-11-15 | 2007-05-09 | 闫章年 | Compound injection of Xylazine, and preparation technique |
| CN101658524A (en) * | 2009-09-25 | 2010-03-03 | 南京农业大学 | A compound anesthetic for dogs |
Non-Patent Citations (1)
| Title |
|---|
| S.SOORYADAS ET AL: "Electrocardiogram changes during xylazine-propofol anaesthesia in dogs: a clinical study", 《 INDIAN J. VET. SURG.》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110638755A (en) * | 2019-10-29 | 2020-01-03 | 江苏盈科生物制药有限公司 | Propofol medium-long chain fat emulsion and preparation method thereof |
| CN110638755B (en) * | 2019-10-29 | 2021-05-11 | 江苏盈科生物制药有限公司 | Propofol medium-long chain fat emulsion and preparation method thereof |
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Application publication date: 20160420 |