CN1259901C - Musk liposome injection and its preparation method - Google Patents
Musk liposome injection and its preparation method Download PDFInfo
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- CN1259901C CN1259901C CNB031428886A CN03142888A CN1259901C CN 1259901 C CN1259901 C CN 1259901C CN B031428886 A CNB031428886 A CN B031428886A CN 03142888 A CN03142888 A CN 03142888A CN 1259901 C CN1259901 C CN 1259901C
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- moschus
- musk
- liposome injection
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Abstract
The present invention provides a musk liposome injection which is prepared by modern liposome injection preparation technology. When the musk liposome injection is injected to the part behind eyeballs or the part around the eyeballs, pigmentary degeneration of retina and optic atrophy can be treated. When the musk liposome injection is injected into veins, central nervous system diseases of cerebral seizure, coma hepaticum, pulmonary encephalopathy, cerebral edema, stupor and cerebral anoxia caused by craniocerebral trauma, consciousness disturbance caused by poisoning of various medicines and toxic substances, etc. When the musk liposome injection is injected into acupoints of human bodies, the acupoint slow release pharmacodynamics effect is generated, and various intractable diseases can be treated according to an acupoint effect principle.
Description
Technical field
The present invention relates to a kind of Moschus lipidosome injection.
Background technology
Retinitis pigmentosa and optic atrophy are ophthalmology common diseases, and previously not having has the specific treatment measure.Acupuncture point medicine injection treatment is that medicine is injected in the acupuncture point, treats disease by acupuncture and drug influence stimulating acupoint, and the medicine that in the past is applied to acupoint injection therapy is the normal injection agent, no slow release pharmacodynamics effect.Motherland's medical science record, Moschus has causing resuscitation with aromatic drugs, refreshment analepsia, tranquilizing mind, blood stasis dispelling spasmolytic effect, modern medicine study confirms: muscone or Moschus have anti-cerebral ischemia anoxia, encephaledema and microcirculation improvement effect, XINGNAOJING ZHUSHEYE is to be the first aid medicine of the diseases such as treatment apoplexy of principal agent with the Moschus, and also the someone uses musk injection and makes acupoint injection therapy.At present still do not have to have and contain the lipidosome injection that Moschus is a principal agent.
Summary of the invention
The purpose of this invention is to provide a kind of lipidosome injection with Moschus slow release pharmacodynamics effect, this Moschus lipidosome injection can be treated diseases such as retinitis pigmentosa, optic atrophy, apoplexy, this Moschus lipidosome injection is injected in the human acupoint, according to the acupuncture point effect, can treat multiple disease.
This Moschus lipidosome injection is made up of Moschus, liposome substrate, its technical characterictic is that Moschus can be muscone or natural Moschus's extract, liposome substrate is phospholipid and cholesterol, phospholipid can be lecithin, cephalin, fabaceous lecithin, and multiphasic liposomes substrate also can add efficient non-ionic surface active agent such as span, tween; Add high-performance solid dispersant such as polyvinylpyrrolidone, Polyethylene Glycol, gelatin; Add unsaturated fatty acid such as oleic acid, linoleic acid, arachidonic acid, linolenic acid, palmitic acid etc. as stabilizing agent, every milliliter of Moschus lipidosome injection includes muscone 1-10mg or Moschus 10-40mg.
Common Moschus lipidosome injection prescription is as follows, by weight ratio: Moschus 20-70 part; Phosphatidase 13 00-500 part; Cholesterol 50-200 part.
Heterogeneous Moschus lipidosome injection prescription is as follows, by weight ratio: Moschus 20-70 part; Phosphatidase 13 00-500 part; Cholesterol 50-200 part; Arlacel-80 2-6 part; Polyvinylpyrrolidone 5-9 part; Oleic acid 2-6 part.
Liposome is a kind of slow release, delay the new drug carrier of drug metabolism.The present invention utilizes the pharmaceutical carrier of liposome as Moschus, the lipidosome injection that preparation has Moschus slow release pharmacodynamics effect.Do this Moschus lipidosome injection behind the ball or the injection of ball week, can treat retinitis pigmentosa and optic atrophy; With this Moschus lipidosome injection intravenously administrable, can treat apoplexy, hepatic coma, pulmonary encephalopathy, the central nervous system disease such as disturbance of consciousness due to the mould thing of cerebral edema, stupor, cerebral anoxia and the various medicine due to the craniocerebral trauma is poisoned; This Moschus lipidosome injection is injected in the human acupoint, produces acupuncture point slow release pharmacodynamics effect,, can treat multiple refractory disease according to the acupuncture point effect principle.This Moschus lipidosome injection has biodegradation, reduces advantages such as medication number of times and dosage, has no side effect.
The specific embodiment
Preparation to Moschus lipidosome injection of the present invention describes in further detail below.
The technology of preparing of lipidosome injection is the existing medicament technology of preparing of a kind of maturation, prepares simple usually.The technology of preparing of at present existing lipidosome injection has film dispersion method, ultrasonic dispersing method, injection method, freeze-drying, freeze-thaw method, reverse phase evaporation, multi-emulsion method, fusion method, high pressure homogenize method, the solvent breast sedimentation method, micropore cooling method, surfactant facture, centrifuging, pH gradient method, pro-liposome method, calcium fusion method, pressurization extrusion molding, spray drying method etc.In preparation process, two or more technology of preparing combination, can form a kind of new technology of preparing, be combined into thin film-ultrasonic dispersing method as film dispersion method and ultrasonic dispersing method, injection method and ultrasonic dispersing method are combined into injection-ultrasonic dispersing method, and film dispersion method and freeze-drying are combined into thin film-freeze-drying.The preparation of Moschus lipidosome injection can be selected the technology of preparing of above-mentioned any or two kinds of lipidosome injections.
Used Moschus in the Moschus lipidosome injection, can be the muscone that synthetic muscone or natural Moschus extract, also can select steam distillation or the alcohol reflux method of purification of natural Moschus through modern pharmaceutical technology for use, the refining removal foreign material of purifying get Moschus extract.
The film dispersion method technology of preparing: this technology of preparing is that Moschus, phospholipid and cholesterol are dissolved in the chloroform (or other organic solvents), rotary evaporation under nitrogen current then, remove chloroform, on the inwall of vial, form thin film, phosphate buffer is added constantly stirring in the vial, promptly get Moschus liposome turbid liquor injection.Concrete preparation method is as follows: the smart muscone 50mg that claims, phosphatidase 14 00mg, cholesterol 100mg, place the pyriform glass flask, dissolve with chloroform 20ml, on thin film rotary evaporator, make film, chloroform is removed in decompression in 30-50 ℃ of water-bath, to the vial wall, form thin film, with pH6.6 sodium hydrogen phosphate 10ml, also available 0.9% sodium chloride solution 10ml, place the phospholipid membrane that contains Moschus in the vial on the aquation vial wall, and put fragmentation in the tissue mashing machine, and adding the injection water to 50ml, filter filters, inflated with nitrogen packing ampoule, 100 ℃ of sterilizations in 30 minutes of flowing steam promptly get milky or faint yellow Moschus lipidosome injection, contain muscone 1mg in every milliliter of Moschus lipidosome injection.
Ultrasonic dispersing method technology of preparing: this technology is to be dissolved in Moschus, phospholipid and cholesterol in the organic solvent altogether, remove organic solvent through stirring evaporation, debris continuous ultrasound concussion in 50 ℃ of water liquid formula ultrasonic generators is handled, and isolates lipidosome injection then.
The freeze-drying technology of preparing: the Moschus lipidosome injection of liquid condition phenomenons such as coalescent, layering and particle diameter increase can occur in storage process.The Moschus liposome of using the freeze-drying preparation is freezing powder product, after adding the injection water during application and dissolving, and the very fast liposome that forms liquid condition again.In the freeze-drying preparation process, also can add antioxidant, chelating agen and cryoprotective agent.Concrete technology of preparing is that Moschus, phospholipid and cholesterol are dissolved in chloroform or other organic solvents, is suspended in then in the phosphate buffer, and the cold cut supersound process, vacuum freezing drying dehydration is prepared into the cold-dry powder product.
Spray drying method for preparation technology: muscone is added pH7.0 sodium hydrogen phosphate buffer, get phospholipid and add fusion cholesterol mixing, muscone is added in fused phospholipid and the cholesterol fused mass, stir, add phosphoric acid disodium hydrogen buffer, put tissue mashing machine, high-speed stirred, put spray dryer decompression spray drying, inlet temperature 130-140 ℃, outlet temperature 50-60 ℃, air pressure 1.2Atm, charging rate 60ml/min gets milky or flaxen Moschus pro-liposome.
Injection method technology of preparing: Moschus, phospholipid and cholesterol are dissolved in the organic solvent, this solution slowly injects the phosphate buffer that is heated to 50 ℃ (and using magnetic agitation) through syringe, till constantly being stirred to organic solvent and eliminating, promptly get macrovesicle, its suspension is passed through high pressure dispersing emulsification machine twice, gained lipidosome injection.
Reverse phase evaporation technology of preparing: phospholipid, cholesterol are dissolved in organic solvent such as the chloroform, add muscone and carry out ultrasonic concussion processing, reduction vaporization is removed organic solvent then, reach colloidal state after, drip buffer, rotation helps the gel on the wall to come off, under reduced pressure continue evaporation then, make suspension, pass through ultracentrifugation, remove non-encapsulated medicine, promptly obtain lipidosome injection.
The fusion method technology of preparing: with phospholipid, use an amount of dissolve with ethanol, mix with it after the fusion of adding cholesterol, fusion under the temperature about 65 ℃ adds the phosphate buffer that contains muscone, puts the high speed bruisher and smashs to pieces, and this method can prepare liposome in a large number.
Claims (3)
1. a Moschus lipidosome injection is made up of Moschus, liposome substrate, and its technical characterictic is: Moschus is muscone or Moschus extract, and liposome substrate is phospholipid and cholesterol, and wherein the weight portion ratio of each raw material is: Moschus 20-70 part; Phosphatidase 13 00-500 part; Cholesterol 50-200 part.
2. by the described Moschus lipidosome injection of claim 1, its technical characterictic is: contain muscone 1-10mg or Moschus 10-40mg in every milliliter of lipidosome injection.
3. by the described Moschus lipidosome injection of claim 1, its technical characterictic is: wherein the weight portion ratio of each raw material is: Moschus 20-70 part; Phosphatidase 13 00-500 part; Cholesterol 50-200 part; Arlacel-80 2-6 part; Polyvinylpyrrolidone 5-9 part; Oleic acid 2-6 part.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB031428886A CN1259901C (en) | 2003-06-16 | 2003-06-16 | Musk liposome injection and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB031428886A CN1259901C (en) | 2003-06-16 | 2003-06-16 | Musk liposome injection and its preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1565479A CN1565479A (en) | 2005-01-19 |
| CN1259901C true CN1259901C (en) | 2006-06-21 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNB031428886A Expired - Fee Related CN1259901C (en) | 2003-06-16 | 2003-06-16 | Musk liposome injection and its preparation method |
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Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101664452B (en) * | 2006-03-27 | 2011-04-06 | 深圳市金沙江投资有限公司 | Drug combination containing musk |
| CN102327237B (en) * | 2011-07-14 | 2012-09-26 | 海南灵康制药有限公司 | Azasetron hydrochloride lipidosome injection |
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2003
- 2003-06-16 CN CNB031428886A patent/CN1259901C/en not_active Expired - Fee Related
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| Publication number | Publication date |
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| CN1565479A (en) | 2005-01-19 |
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