CN103110950A - Application of medicinal composition - Google Patents
Application of medicinal composition Download PDFInfo
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- CN103110950A CN103110950A CN2011103638646A CN201110363864A CN103110950A CN 103110950 A CN103110950 A CN 103110950A CN 2011103638646 A CN2011103638646 A CN 2011103638646A CN 201110363864 A CN201110363864 A CN 201110363864A CN 103110950 A CN103110950 A CN 103110950A
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- pharmaceutical composition
- anisodamine
- cholinesterase inhibitor
- neostigmine
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Abstract
The invention discloses an application of a medicinal composition in the preparation of crush injury treatment medicines, wherein the medicinal compositions contains a muscarinic acceptor blocker and a cholinesterase inhibitor. The medicinal composition has the advantages of effect enhancement, substantial effect, small toxic side effects, and overcoming of the side effects commonly caused by present medicines when the medicinal composition is used for treating crush injuries.
Description
Technical field
The present invention relates to a kind of application of pharmaceutical composition.
Background technology
In prior art, the clinical application of M-ChR blocker is as follows: 1, remove smooth muscle spasm: be applicable to various internal organs angor, to gastrointestinal angor, the curative effects such as irritation sign of bladder such as frequent micturition, urgent micturition are better, but relatively poor to biliary colic or Renal Colic, often need to share with opium kind analgesics.2, suppress glandular secretion: be used for the front administration of general anesthesia, to reduce respiratory tract body of gland and salivary gland secretion, prevent the generation of block of secretion respiratory tract and aspiration pneumonitis, also can be used for serious night sweat and ptyalism.3, ophthalmology: 1) iridocyclitis: 0.5%～1% atropine solution eye drip, can relax iris sphincter muscle and ciliary muscle make it abundant rest, help inflammation to disappear; Also can prevent iris and lenticular adhesion, still can with the miotic alternate application; 2) optometry gets the right lensses for one's eyeglasses: ophthalmic drips with atropine and has the effect of the paralysis of adjusting, and this moment is because crystalline lens is fixed, but the lenticular diopter of Accurate Determining; But the atropine acting duration is longer, can keep 2～3 days, therefore now use less; When only having child's optometry, still use it, because child's ciliary muscle regulatory function is stronger, needs to bring into play it with atropine and regulate fully the paralysis effect; 3) examination of ocular fundus: utilize its platycoria effect, can carry out examination of ocular fundus; 4) slow arrhythmia: atropine can be used for treating vagus nerve be overexcited due to the slow arrhythmia such as sino atrial block, auriculoventricular block; 5) shock: to patients with septic shock, available large-dose of atropine treatment can be removed vasospasm, and the diastole peripheral blood vessel improves microcirculation; 6) the rescue organophosphorus compounds is poisoning.
The clinical application of cholinesterase inhibitor is as follows: 1, myasthenia gravis; 2, postoperative abdomen flatulence and urine retention: the neostigmine excited gastrointestinal smooth muscle of energy and detrusor of bladder promote aerofluxus and urinate; 3, the excessive poisoning rescue of muscle relaxant: the rescue when as excessive in tubocurarine for the nondepolarizing type skeletal muscle relaxant; 4, other application: paroxysmal supraventricular tachycardia, glaucoma.
But the use of uniting of M-ChR blocker and cholinesterase inhibitor pharmaceutical composition there is not yet report.
Summary of the invention
Technical problem to be solved by this invention is when having overcome existing M-ChR blocker use, the dosage of medicine is large and side effect is many, perhaps cholinesterase inhibitor can cause that acetylcholine is accumulated and causes the unify defective of untoward reaction etc. of digestive system of cardiovascular system, and the application of a kind of pharmaceutical composition in the anti-extrusion vulnerary thing of preparation is provided.
The invention provides the application of a kind of pharmaceutical composition in the anti-extrusion vulnerary thing of preparation, wherein, described pharmaceutical composition contains M-ChR blocker and cholinesterase inhibitor.
When the present invention finds that through research uniting of M-ChR blocker and cholinesterase inhibitor used the treatment crush injury, action effect is remarkable, and the drug dose that uses is little, effect is strengthened greatly, and overcome the M-ChR blocker xerostomia, flushing, slight platycoria, look the side effect such as nearly thing is fuzzy, and use m receptor excitement that cholinesterase inhibitor can cause to the unify untoward reaction of digestive system of cardiovascular system.
What wherein, the quality ratio of described M-ChR blocker and cholinesterase inhibitor was better is 2.5 * 10
2-4.0 * 10
3
Wherein, described M-ChR blocker is the conventional M-ChR blocker that uses in this area, better is selected from Anisodamine, contains the plant extract of Anisodamine and one or more in atropine, commercially available getting.
The structural formula of described Anisodamine as shown in Equation 1, it is the esters that is formed by tropic acid and organic base, structure and atropine are similar, on 6 carbon atoms of tropyl, asymmetric hydroxyl are arranged.
Described atropinic structural formula as shown in Equation 2.
Wherein, described cholinesterase inhibitor is the conventional cholinesterase inhibitor that uses in this area, one or more that better is in neostigmine, pyridostigmine bromide and physostigmine, commercially available getting.
The structural formula of described neostigmine as shown in Equation 3.
The structural formula of described physostigmine as shown in Equation 4.
The structural formula of described pyridostigmine bromide as shown in Equation 5.
In the present invention, described Anisodamine can also extract from plant.Described Anisodamine can extract from the plant Radix Anisodi Tangutici, but extracting method list of references " Simultaneous analysis ofhyoscyamine, scopolamine, 6 β-hydroxyhyoscyamine and apoatropine inSolanaceous hairy roots by reversed-phase high-performance liquidchromatography " (Journal of Chromatography A, 2005,1091 (1-2): 32-39).
A preferred embodiments in the present invention, described M-ChR blocker is Anisodamine, described cholinesterase inhibitor is neostigmine.
In the present invention, what described pharmaceutical composition was better is one of the following:
Neostigmine: the mass ratio of Anisodamine is 1: 500-1: 4000, and better is 1: 500-1: 1000;
Neostigmine: atropinic mass ratio is 1: 2000-1: 4000;
Pyridostigmine bromide: the mass ratio of Anisodamine is 1: 250-1: 500;
Pyridostigmine bromide: atropinic mass ratio is 1: 450-1: 550, and better is 1: 500;
Each raw material of addressing in the present invention or reagent is commercially available getting all.
The preparation method of pharmaceutical composition of the present invention can be with existing commercially available above-claimed cpd, or the extract that contains above-claimed cpd that extracts from plant, by proportioning, adopts the conventional method of this area to mix, and gets final product.
Pharmaceutical composition of the present invention also can comprise the medicine of the treatment crush injury that has other now as active constituents of medicine, as long as its not appreciable impact pharmaceutical composition effect of the present invention.
As required, pharmaceutical composition of the present invention also can comprise pharmaceutically acceptable carrier.Described pharmaceutically acceptable carrier refers to the pharmaceutical carrier of pharmaceutical field routine, wherein, and diluent such as starch, Icing Sugar, dextrin, microcrystalline Cellulose, mannitol, lactose and Semen sojae atricolor wet goods; Binding agent such as polyvinylpyrrolidone or hydroxypropyl cellulose etc.; Disintegrating agent such as sodium carboxymethyl cellulose or low-substituted hydroxypropyl cellulose etc.; Lubricant such as magnesium stearate or Pulvis Talci etc.; Stabilizing agent such as sodium carboxymethyl cellulose or cyclodextrin etc.; Antiseptic such as ethylparaben or sodium benzoate etc.In addition, can also add other adjuvant such as flavouring agent and/or sweeting agent such as sucrose, fructose and aspartame etc. in this pharmaceutical composition.The active component of this pharmaceutical composition is the M-ChR blocker of the present invention for the treatment of effective dose and the pharmaceutical composition of cholinesterase inhibitor.This pharmaceutical composition can adopt the method for medical domain routine, and described active component and pharmaceutically acceptable carrier are made various dosage forms.When being used for it can being prepared into conventional solid preparation such as tablet, capsule, soft capsule, liquid preparation, granule, soft extract, pill, drop pill, suspending agent, dispersant, syrup or suppository etc. when oral; When being used for injection, it can be prepared into injection.Each pharmaceutical composition of the present invention can put on by dosage form the patient who needs this treatment by intravenous injection, subcutaneous injection or oral form.The general dosage that imposes on the patient who needs treatment is that the M-ChR blocker is 1-100mg/kg, and cholinesterase inhibitor is 6.25-100ug/kg; Better dosage M-ChR blocker is 12.5-50mg/kg, and cholinesterase inhibitor is 12.5-50ug/kg; Best dosage is Anisodamine 12.5mg/kg, neostigmine 50ug/kg.In concrete use procedure, also can take the circumstances into consideration to change according to age of patient, the state of an illness etc.
Agents useful for same of the present invention and raw material be commercially available getting all.
Positive progressive effect of the present invention is: the invention provides the application of a kind of pharmaceutical composition in the anti-extrusion vulnerary thing of preparation, wherein, described pharmaceutical composition contains M-ChR blocker and cholinesterase inhibitor.Pharmaceutical composition of the present invention is used for the treatment of crush injury, and it acts on enhancing, and effect is remarkable, and toxic and side effects is little, has overcome the side effect that existing medicine often causes.
The specific embodiment
Mode below by embodiment further illustrates the present invention, but does not therefore limit the present invention among described scope of embodiments.
Effect embodiment
The preparation of crush injury model: the rat numbering of weighing, then use ketamine 100mg/kg and diazepam 10mg/kg intraperitoneal injection of anesthesia (for ease of calculating, all using dosage calculates), after anesthesia, lower limb were placed under the iron block of 20kg extruding 6 hours, give respectively Drug therapy withdrawing each group of front 30 minutes of weight, the medication that specifically sees the following form gives 5ml normal saline lumbar injection simultaneously.
The therapeutic effect of table 1 medicine composite for curing crush injury of the present invention
Claims (8)
1. the application of pharmaceutical composition in the anti-extrusion vulnerary thing of preparation, wherein, described pharmaceutical composition contains M-ChR blocker and cholinesterase inhibitor.
2. application as claimed in claim 1 is characterized in that: described M-ChR blocker is selected from Anisodamine, contain the plant extract of Anisodamine and one or more in atropine.
3. application as claimed in claim 1 is characterized in that: described cholinesterase inhibitor is one or more in neostigmine, pyridostigmine bromide and physostigmine.
4. application as claimed in claim 1 is characterized in that: the quality ratio of described M-ChR blocker and cholinesterase inhibitor is 2.5 * 10
2-4.0 * 10
3
5. application as claimed in claim 1 is characterized in that: described M-ChR blocker is Anisodamine; Described cholinesterase inhibitor is neostigmine.
6. application as claimed in claim 1 is characterized in that: described pharmaceutical composition is one of the following:
Neostigmine: the mass ratio of Anisodamine is 1: 500-1: 4000;
Neostigmine: atropinic mass ratio is 1: 2000-1: 4000;
Pyridostigmine bromide: the mass ratio of Anisodamine is 1: 250-1: 500;
Pyridostigmine bromide: atropinic mass ratio is 1: 450-1: 550.
7. application as claimed in claim 6 is characterized in that: described pharmaceutical composition is one of the following:
Neostigmine: the mass ratio of Anisodamine is 1: 500-1: 1000;
Pyridostigmine bromide: atropinic mass ratio is 1: 500.
8. application as claimed in claim 1 is characterized in that: described pharmaceutical composition also comprises pharmaceutically acceptable carrier.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110363864.6A CN103110950B (en) | 2011-11-16 | 2011-11-16 | A kind of application of pharmaceutical composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110363864.6A CN103110950B (en) | 2011-11-16 | 2011-11-16 | A kind of application of pharmaceutical composition |
Publications (2)
| Publication Number | Publication Date |
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| CN103110950A true CN103110950A (en) | 2013-05-22 |
| CN103110950B CN103110950B (en) | 2016-11-23 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201110363864.6A Expired - Fee Related CN103110950B (en) | 2011-11-16 | 2011-11-16 | A kind of application of pharmaceutical composition |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993018768A1 (en) * | 1992-03-16 | 1993-09-30 | The Regents Of The University Of California | Combinations of parasympathomimetic agents with muscarinic antagonists for treating nicotine craving in smoking cessation |
| CN101002802A (en) * | 2007-01-05 | 2007-07-25 | 于瑞花 | Medicine for treating wound and ulcer, and its preparing method |
| CN101856498A (en) * | 2009-04-10 | 2010-10-13 | 中国人民解放军第二军医大学 | Anti-septic shock medicine compound and application thereof |
-
2011
- 2011-11-16 CN CN201110363864.6A patent/CN103110950B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993018768A1 (en) * | 1992-03-16 | 1993-09-30 | The Regents Of The University Of California | Combinations of parasympathomimetic agents with muscarinic antagonists for treating nicotine craving in smoking cessation |
| CN101002802A (en) * | 2007-01-05 | 2007-07-25 | 于瑞花 | Medicine for treating wound and ulcer, and its preparing method |
| CN101856498A (en) * | 2009-04-10 | 2010-10-13 | 中国人民解放军第二军医大学 | Anti-septic shock medicine compound and application thereof |
Non-Patent Citations (1)
| Title |
|---|
| 张海鹏等: "手指大部分离断伤非显微外科治疗效果观察", 《中国修复重建外科杂志》, vol. 17, no. 4, 31 December 2003 (2003-12-31), pages 331 - 332 * |
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| Publication number | Publication date |
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| CN103110950B (en) | 2016-11-23 |
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Granted publication date: 20161123 Termination date: 20191116 |