CN103933041B - A kind of local anesthetic composition and application thereof comprising bupivacaine - Google Patents
A kind of local anesthetic composition and application thereof comprising bupivacaine Download PDFInfo
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- CN103933041B CN103933041B CN201410159883.0A CN201410159883A CN103933041B CN 103933041 B CN103933041 B CN 103933041B CN 201410159883 A CN201410159883 A CN 201410159883A CN 103933041 B CN103933041 B CN 103933041B
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- local anesthetic
- bupivacaine
- anesthetic composition
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Abstract
The present invention relates to drug world, particularly relate to a kind of pharmaceutical composition with anesthetic action in operation.It is made up of the tetrahydropalmatine of the sufentanil of the bupivacaine of 1.0-3.0mg, 1-5<b> μ </b>g, 15-30<b> μ </b>g, the indomethacin of 15-30<b> μ </b>g and the ropivacaine of 0.1-0.5mg.Described anaesthetic composition is preferably made up of the tetrahydropalmatine of the sufentanil of the bupivacaine of 3.0mg, 3<b> μ </b>g, 20<b> μ </b>g, the indomethacin of 20<b> μ </b>g and the ropivacaine of 0.3mg.
Description
Technical field
The present invention relates to drug world, particularly relate to a kind of pharmaceutical composition with anesthetic action in operation.
Background technology
Along with growth in the living standard, China has stepped into aging society gradually, and the ratio of elderly patients in the middle of surgical patient raises gradually.At home, most of hypogastric region and lower extremity surgery complete under lumbar anesthesia, and lumbar anesthesia is used for the success rate that elderly patients can improve anesthesia, reduces the incidence rate that retardance is incomplete.
But gerontal patient fails due to organ dysfunction, stress ability is poor, part is in nervous anxiety state, the intense stimulus Chang Buneng brought for operation wound bears, its autonomic regulatory function declines, can not effective stabilizing blood pressure, bring out complication and worsen suddenly and even cause accident.So under lumbar anesthesia and epidural block, during Body Position Change can there is obvious fluctuation in hematodinamics, hypotension and heart rate is slack-off etc. that change can cause low-pressure injection and ischemia injury to brain, heart, kidney and other vitals after lumbar anesthesia, because autonomic nervous system hyporeactive is then to hemodynamic habituation, increase cardiovascular and cerebrovascular vessel risk.
Bupivacaine is long-acting local anesthetics of amide derivatives, is applicable to peripheral blockade, epidural block and subarachnoid block.But during application routine dose (15mg) Bupivacaine, although satisfied paroxysmal pain effect can be produced, also have disadvantageous one side simultaneously, namely cause hemodynamic instability and the retardance of complete nervus motorius and recovery time long.Because the metabolism of old people's cardiovascular system is limited, serious hypotension and bradycardia may be there is and cause serious consequence.
Summary of the invention
In view of the technical problem existed in prior art, the invention provides a kind of local anesthetic composition comprising bupivacaine, it is applicable to the lumbar anesthesia in gerontal patient's operation.
An object of the present invention is to provide a kind of local anesthetic composition comprising bupivacaine, it is by bupivacaine, the 1-5 of 1.0-3.0mg
μthe sufentanil of g, 15-30
μthe tetrahydropalmatine of g, 15-30
μthe indomethacin of g and the ropivacaine composition of 0.1-0.5mg.
In one embodiment of the invention, described anaesthetic composition is preferably by the bupivacaine, 3 of 3.0mg
μthe sufentanil, 20 of g
μthe tetrahydropalmatine, 20 of g
μthe indomethacin of g and the ropivacaine composition of 0.3mg.
Anaesthetic composition of the present invention conveniently technique adds the dosage form that pharmaceutically customary adjuvant makes clinical acceptance, and described dosage form is injection, lyophilized injectable powder.
Another object of the present invention is to provide a kind of method preparing the lyophilized injectable powder of described anaesthetic composition, and concrete steps are as follows:
By recipe quantity, corresponding anaesthetic composition component and 100mg glucose are dissolved in water for injection, add activated carbon adsorption, decarbonization filtering, 0.22
μm filtering with microporous membrane, is aseptically sub-packed in gained filtrate in aseptic cillin bottle by aforementioned dose specification again, obtains lyophilized powder through vacuum lyophilization; Then adopt the sealing of plastic cement aluminium lid cillin bottle by ampule sealing, labeling, obtains described lyophilized injectable powder.
Described vacuum freeze-drying method is:
1, first under-40 DEG C ~-60 DEG C ultralow temperature, quick-freeze pre-freeze becomes fine crystalline in 2 hours;
2 ,-20 DEG C of constant temperature sublimation dryings 12 hours are warming up to again under vacuo;
3,20 DEG C of continuation vacuum dryings 12 hours are then warming up to.
Another object of the present invention is to provide described anaesthetic composition and preparation thereof for the preparation of the application in anaesthetic; Described anesthesia is preferably lumbar anesthesia.
Advantage of the present invention:
The present invention adopts other components of bupivacaine compound of small amount for lumbar anesthesia, better can improve safety and the accuracy of anesthesia, be particularly useful for elderly patients.In prior art, common employing bupivacaine and sufentanil compound carry out lumbar anesthesia, but wherein bupivacaine large usage quantity, and still there are nervus motorius retardance, respiration inhibition, sensation retardance and other side effect, anaesthetic composition of the present invention and preparation thereof are then unexpected overcomes above-mentioned technical problem.
Detailed description of the invention
Further will describe the present invention in detail below.It is pointed out that following explanation is only illustrating the technical scheme that application claims is protected, any restriction not to these technical schemes.The content that protection scope of the present invention is recorded with appended claims is as the criterion.
the lyophilized injectable powder preparation of embodiment 1 anaesthetic composition
Bupivacaine: 3.0mg,
Sufentanil: 1
μg;
Tetrahydropalmatine: 30
μg;
Indomethacin: 15
μg;
Ropivacaine: 0.1mg
By recipe quantity, corresponding anaesthetic composition component and 100mg glucose are dissolved in water for injection, add activated carbon adsorption, decarbonization filtering, 0.22
μm filtering with microporous membrane, is aseptically sub-packed in gained filtrate in aseptic cillin bottle by aforementioned dose specification again, obtains lyophilized powder through vacuum lyophilization; Then adopt the sealing of plastic cement aluminium lid cillin bottle by ampule sealing, labeling, oxirane disinfection, obtains described lyophilized injectable powder.
Described vacuum freeze-drying method is: 1. first under-40 DEG C ~-60 DEG C ultralow temperature, quick-freeze pre-freeze becomes fine crystalline in 2 hours; 2. be warming up to-20 DEG C of constant temperature sublimation dryings 12 hours more under vacuo; 3. be then warming up to 20 DEG C of continuation vacuum dryings 12 hours.
the lyophilized injectable powder preparation of embodiment 2 anaesthetic composition
Bupivacaine: 3.0mg,
Sufentanil: 3
μg;
Tetrahydropalmatine: 20
μg;
Indomethacin: 20
μg;
Ropivacaine: 0.3mg
By recipe quantity, corresponding anaesthetic composition component and 100mg glucose are dissolved in water for injection, add activated carbon adsorption, decarbonization filtering, 0.22
μm filtering with microporous membrane, is aseptically sub-packed in gained filtrate in aseptic cillin bottle by aforementioned dose specification again, obtains lyophilized powder through vacuum lyophilization; Then adopt the sealing of plastic cement aluminium lid cillin bottle by ampule sealing, labeling, obtains described lyophilized injectable powder.
Described vacuum freeze-drying method is: 1. first under-40 DEG C ~-60 DEG C ultralow temperature, quick-freeze pre-freeze becomes fine crystalline in 2 hours; 2. be warming up to-20 DEG C of constant temperature sublimation dryings 12 hours more under vacuo; 3. be then warming up to 20 DEG C of continuation vacuum dryings 12 hours.
the anaesthetic effect research of lyophilized injectable powder prepared by embodiment 3 embodiment 1 and 2
Gerontal patient 160 example of collect row hypogastric region and lower extremity surgery, mean random is divided into 4 groups, age 61-83 year, body weight 49-75kg, ASAI-II level, without coagulation disorders, without medical histories such as lower extremity motor function obstacle and vomitings, operation kind: urethra TURP or bladder tumors electric resection, fracture of the lower limb internal fixation etc. (all operations all complete in 75min).
The preoperative 8h fasting of patient, puts down and crouches and connect monitoring equipment, record basic value.Patient gets lateral position row L3-4 gap, and hard-ridge combines puncture, injects anaesthetic, main about speed 20s after success in subarachnoid space.Equal conventional inhalation of low concentration flow oxygen after anesthesia of patient.
Record injection after-contraction pressure (SP), diastolic pressure (DP), heart rate (HR), blood oxygen saturation (SpO
2) and respiratory frequency (RR).
Close observation sensation residence time (for injection time point is to feeling that retardance reaches the time of T12) after anesthesia, sensation retardance persistent period (for injection time point is to sensory recovery to the time of L2 level) and nervus motorius retardance persistent period (for the time that injection time point to lower limb exercise recovers completely)
Record nervus motorius retarding degree: adopt improvement Bromage scoring: 0 ~ 3 grade, 0 grade without motion retardance; 1 grade of thigh can not on lift, knee joint and toes active; 2 grades of knee joints can not bend, active toes; 3 grades of toes are inactive;
Anaesthetic effect is evaluated: excellent, patient is without discomfort, and flesh pine is good, and operation smoothly; Good: patient has the slight pull-out performance of slight uncomfortable companion, but can coordinate hands art; Difference, has obvious tractive pain.Flesh pine is poor, and Anti-Ten thing need be assisted just to complete operation.
Untoward reaction detects and comprises nausea and vomiting, skin pruritus, hypotension, respiration inhibition, headache etc.
concrete outcome:
1.injection after-contraction pressure (SP), diastolic pressure (DP), heart rate (HR), blood oxygen saturation (SpO
2) and respiratory frequency (RR), before the injection of each group and after injection 30min and 60min, heart rate and blood oxygen saturation are without significant change, and other the results are shown in following table:
2.sensation retardance onset time, sensation retardance persistent period and nervus motorius retardance persistent period
| 1. divide into groups | 2. sensation retardance onset time (min) | 3. sensation retardance persistent period (min) | 4. nervus motorius retardance persistent period (min) |
| 5. embodiment 1 | 6. 1.1±0.3 | 7. 103±9 | 8. 104±11 |
| 9. embodiment 2 | 10. 0.9±0.2 | 11. 101±7 | 12. 103±9 |
| 13. comparative examples 1 | 14. 1.9±0.4 | 15. 67±5 | 16. 97±10 |
| 17. comparative examples 2 | 18. 1.7±0.3 | 19. 82±6 | 20. 110±12 |
in addition, each group motion blockage effect is without significant change.
Anaesthetic effect
| 21. groupings | 22. excellent (examples) | 23. good (examples) | 24. poor (examples) |
| 25. embodiments 1 | 26. 35 | 27. 3 | 28. 2 |
| 29. embodiments 2 | 30. 38 | 31. 2 | 32. 0 |
| 33. comparative examples 1 | 34. 11 | 35. 15 | 36. 14 |
| 37. comparative examples 2 | 38. 21 | 39. 12 | 40. 7 |
4.untoward reaction
| 41. groupings | 42. vomitings (example) | 43. prurituss (example) | 44. headaches (example) |
| 45. embodiments 1 | 46. 0 | 47. 0 | 48. 0 |
| 49. embodiments 2 | 50. 0 | 51. 0 | 52. 0 |
| 53. comparative examples 1 | 54. 3 | 55. 2 | 56. 4 |
| 57. comparative examples 2 | 58. 1 | 59. 5 | 60. 1 |
Content of the present invention merely illustrates some claimed specific embodiments; one of them or more described technical characteristic can be combined with arbitrary one or more technical scheme in technical scheme; these technical schemes obtained through combination also in the application's protection domain, just as these technical schemes obtained through combination in the disclosure of invention concrete record.
Claims (7)
1. comprise a local anesthetic composition for bupivacaine, it is characterized in that, it is made up of the tetrahydropalmatine of the sufentanil of the bupivacaine of 1.0-3.0mg, 1-5 μ g, 15-30 μ g, the indomethacin of 15-30 μ g and the ropivacaine of 0.1-0.5mg.
2. local anesthetic composition according to claim 1, is characterized in that, described local anesthetic composition is made up of the tetrahydropalmatine of the sufentanil of the bupivacaine of 3.0mg, 3 μ g, 20 μ g, the indomethacin of 20 μ g and the ropivacaine of 0.3mg.
3. local anesthetic composition according to claim 1, is characterized in that, described local anesthetic composition conveniently technique adds the dosage form that pharmaceutically customary adjuvant makes clinical acceptance.
4. prepare a method for the lyophilized injectable powder of local anesthetic composition according to claim 3, it is characterized in that, concrete steps are as follows:
By recipe quantity, corresponding topical anaesthetic composition component and 100mg glucose are dissolved in water for injection, add activated carbon adsorption, decarbonization filtering, 0.22 μm of filtering with microporous membrane;
Gained filtrate is aseptically sub-packed in aseptic cillin bottle by aforementioned dose specification again, obtains lyophilized powder through vacuum lyophilization;
Then adopt the sealing of plastic cement aluminium lid cillin bottle by ampule sealing, labeling, obtains described lyophilized injectable powder.
5. method according to claim 4, is characterized in that, described vacuum freeze-drying method is:
(1) first under-40 DEG C ~-60 DEG C ultralow temperature, quick-freeze pre-freeze becomes fine crystalline in 2 hours;
(2)-20 DEG C of constant temperature sublimation dryings 12 hours are warming up to again under vacuo;
(3) 20 DEG C of continuation vacuum dryings 12 hours are then warming up to.
6. the arbitrary described local anesthetic composition of claim 1-3 is for the preparation of the application in anaesthetic.
7. application according to claim 6, is characterized in that, described anesthesia is lumbar anesthesia.
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| CN201410159883.0A CN103933041B (en) | 2014-04-21 | 2014-04-21 | A kind of local anesthetic composition and application thereof comprising bupivacaine |
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| CN103933041B true CN103933041B (en) | 2016-03-16 |
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| US20190365730A1 (en) * | 2017-02-09 | 2019-12-05 | Med Solutions Sweden Aktiebolag | Anaesthetic composition comprising ropivacaine, prilocaine and lidocaine |
| CN109260202B (en) * | 2017-07-17 | 2020-06-19 | 北京泰德制药股份有限公司 | Topical preparation of local anesthetic and method for improving stability of topical preparation of local anesthetic |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101190184A (en) * | 2006-11-24 | 2008-06-04 | 天津药业研究院有限公司 | Micronizing solid external application local anesthetic and preparation method thereof |
| CN101842099A (en) * | 2008-04-18 | 2010-09-22 | 华沙整形外科股份有限公司 | Methods and compositions for treating post-operative pain comprising a local anesthetic |
| CN103142458A (en) * | 2013-01-22 | 2013-06-12 | 莱普德制药有限公司 | Component and preparation method of non-addition analgesia slow release medicine delivering system |
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| US20070253994A1 (en) * | 2006-04-28 | 2007-11-01 | Medtronic, Inc. | Intraspinal Drug Delivery Methods and Devices To Alleviate Chronic Pelvic Pain |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101190184A (en) * | 2006-11-24 | 2008-06-04 | 天津药业研究院有限公司 | Micronizing solid external application local anesthetic and preparation method thereof |
| CN101842099A (en) * | 2008-04-18 | 2010-09-22 | 华沙整形外科股份有限公司 | Methods and compositions for treating post-operative pain comprising a local anesthetic |
| CN103142458A (en) * | 2013-01-22 | 2013-06-12 | 莱普德制药有限公司 | Component and preparation method of non-addition analgesia slow release medicine delivering system |
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| CB03 | Change of inventor or designer information |
Inventor after: Wang Shoushi Inventor after: Feng Mei Inventor after: Diao Yujing Inventor before: Wang Shoushi Inventor before: Song Tingting Inventor before: Yang Cheng |
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Effective date of registration: 20160216 Address after: Qingdao City, Shandong province 266000 four Road No. 127 Applicant after: Zhongxin Hospital, Qingdao Address before: 266041, building 14, No. seven, 228 Jinsong Road, Laoshan District, Shandong, Qingdao, 1-601 Applicant before: Wang Shoushi |
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