CN102688192A - Sustained-release preparation of polypeptide drug for treating diabetes and production method thereof - Google Patents
Sustained-release preparation of polypeptide drug for treating diabetes and production method thereof Download PDFInfo
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- CN102688192A CN102688192A CN2011100684248A CN201110068424A CN102688192A CN 102688192 A CN102688192 A CN 102688192A CN 2011100684248 A CN2011100684248 A CN 2011100684248A CN 201110068424 A CN201110068424 A CN 201110068424A CN 102688192 A CN102688192 A CN 102688192A
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Abstract
A sustained-release preparation of polypeptide drug for treating diabetes and a production method thereof relate to the technical field of diabetes prevention drugs. The sustained-release preparation is mainly composed of phosphatide, sesame oil, glycerin, liraglutide, salt and ethanol. According to the invention, the drug is uniformly wrapped in a biodegradable material. Due to hydrophobicity and viscosity of the packing material, the drug will not be rapidly released after subcutaneous injection, so as to greatly reduce stimulation of an injected position, and the slow release of the drug ensures that the toxic and side effect is obviously decreased. Injection can be carried out once a week even once a month by controlling selection and proportion of the material. Above all, the production technology is simpler than traditional microsphere and liposome technologies. By the adoption of the production method, product quality is not only guaranteed, but cost is also remarkably reduced. 26/27G syringe needles can be adopted and are easily accepted by patients.
Description
Technical field
The present invention relates to diabetes and prevent technical field of pharmaceuticals.
Background technology
Diabetes have become the killer who threatens human health.Present Chinese diabetics number ranks first in the world, and the whole nation in 2010 is 9,240 ten thousand people, and through estimation, the direct medical expenses that China's diabetes cause accounts for 13% of national medical total expenses, has reached 173,400,000,000 RMB.In the U.S., the diabetes number will reach 1/3rd of population according to estimates.
GLP-1 is a great achievement of diabetes study in recent years.First GLP-1 medicine Ai Saina peptide in 2005 is used to treat type ii diabetes, for patient brings great convenience by FDA approval listing.The function of GLP-1 is the level through the endocrine insulin of control agent, and blood sugar control is in normal scope.The hypoglycemia phenomenon that generation can not occur because insulin injection is excessive.Simultaneously, GLP-1 can make patient produce feeling of repletion, lowers appetite, thereby reaches fat-reducing effect.
In the world to injectable drug carry out the method for slow release nearly below several kinds:
The subcutaneous embedding of microsphere: be method classical with the most commonly used, pharmaceutical pack is rolled in the macromolecule, process microsphere,, be degraded gradually, drug slow is discharged through macromolecule in subcutaneous embedding.Usually use the PLGA copolymerized macromolecule to do carrier because biodegradation, and safety be studied at most, be received method; Come sustained release time length through changing two kinds of high molecular ratios and molecular weight.The eighties, ATP company released product at first, and slow-release time reaches one month, and the later stage product can reach 4 months through improving.Shortcoming is a complex process, and cost is very high; Drug loading is on the low side (5%), only is applicable to efficient low amount medicine; Granule is big (about 20 microns of average diameters), need injection needle more than 25G, and the obstruction possibility is arranged; Technical patent is a lot, and is by the monopolization of several companies, more difficult to get access.
Liposome technology: pharmaceutical pack is rolled in the liposome that phospholipid bilayer forms,, medicine is played the effect of slow release, protective effect is also arranged through different formulations and concentric multilamellar of prepared or disloyalty multilamelar liposome (DEPOFOAM).Usually be no more than a week release time, be usually used in targeting and discharge.Shortcoming is a complex process, and cost is very high; Drug loading is on the low side (5%), and stability is not high, and repeatability is bad; Technical patent is a lot, and is by the monopolization of several companies, more difficult to get access.Seldom use should technology for product in the market.
A kind of in addition method is to reduce water solublity through the molecular structure that changes medicine, salt kind or formation complex, reaches the purpose of slow release.Most typical product is a trypsin class medicine, and different types of salt is arranged in the market, or zincification forms a flat iron plate for making cakes compound.Extended to one day release time from several hours, and stability strengthens.Shortcoming is that some medicine salify or a flat iron plate for making cakes compound artifact availability reduce.
Other technologies comprise the infiltration press pump, Transdermal absorption, and pulmonary absorbs and waits because various restrictions are not promoted.At some novel carriers of conceptual phase, it is early stage that nano material or the like also is in research and development.
Summary of the invention
The object of the invention is to propose a kind of slow releasing preparation of injection diabetes polypeptide drugs.
The present invention mainly is made up of phospholipid, Oleum sesami, glycerol, Li Lalu peptide, salt and ethanol.
The present invention evenly is wrapped in medicine in the biodegradation material, because the hydrophobicity and the viscosity of packaging material, is injected at and can discharge medicine rapidly after subcutaneous, has significantly reduced the stimulation to the injection site, and medicine is discharged gently, obviously reduces toxic and side effects.Through selecting for use and ratio of control material, can reach the injection of jede Woche even every month once, the most important thing is that production technology is simply more a lot of than traditional microsphere and liposome technology, not only guarantee product quality more, and cost reduces significantly.Owing to there is not the existence of solid particle, the syringe needle of use is less than microsphere and liposome simultaneously.Adopt the 26G/27G syringe needle, accepted by patient more easily.The subcutaneous depot ejection preparation is applicable to the various macromole that need injection, comprises albumen, polypeptide, nucleic acid drug, particularly to needing the chronic disease of life-time service, such as diabetes.
Another purpose of the present invention is to propose the production method of the slow releasing preparation of above injection diabetes polypeptide drugs:
Phospholipid, Oleum sesami and glycerol are mixed the back add ethanol, heating also uses ultrasonic stirring to mix, and forms oil phase; Sucrose and salt are dissolved in water, form water; Water is mixed back emulsifying with oil phase, form emulsifying agent; After the pH value of the aqueous solution of Li Lalu peptide transferred to 9-10, add in the emulsifying agent,, use vacuum to remove moisture then through aseptic filtration.
Production technology of the present invention is simple, reasonable, is easy to production control, and product stability is good.
The specific embodiment
30g phospholipid, 8g Oleum sesami and 5g glycerol mixing back are added 60g ethanol, and heating also uses the ultrasonic stirring mixing to produce homogeneous liquid, is called oil phase.
1g sucrose and 1g salt are dissolved in water, form the aqueous solution of sucrose and salt.
Aqueous solution is added oil phase, use mulser to carry out emulsifying, form emulsifying agent.
Jolting in the 5g Li Lalu peptide adding 10g water is made it dissolving, PH is heightened to 9-10, again this solution is added in the emulsifying agent that produces.
Through aseptic filtration.Use vacuum to remove moisture then.
Claims (2)
1. the slow releasing preparation of diabetes polypeptide drugs is characterized in that mainly being made up of phospholipid, Oleum sesami, glycerol, Li Lalu peptide, salt and ethanol.
2. the production method of the slow releasing preparation of diabetes polypeptide drugs according to claim 1 is characterized in that phospholipid, Oleum sesami and glycerol are mixed the back adds ethanol, and heating also uses ultrasonic stirring to mix, and forms oil phase; Sucrose and salt are dissolved in water, form water; Water is mixed back emulsifying with oil phase, form emulsifying agent; After the pH value of the aqueous solution of Li Lalu peptide transferred to 9-10, add in the emulsifying agent,, use vacuum to remove moisture then through aseptic filtration.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011100684248A CN102688192A (en) | 2011-03-22 | 2011-03-22 | Sustained-release preparation of polypeptide drug for treating diabetes and production method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011100684248A CN102688192A (en) | 2011-03-22 | 2011-03-22 | Sustained-release preparation of polypeptide drug for treating diabetes and production method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102688192A true CN102688192A (en) | 2012-09-26 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011100684248A Pending CN102688192A (en) | 2011-03-22 | 2011-03-22 | Sustained-release preparation of polypeptide drug for treating diabetes and production method thereof |
Country Status (1)
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| CN (1) | CN102688192A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104055735A (en) * | 2013-03-22 | 2014-09-24 | 深圳翰宇药业股份有限公司 | Semaglutide liposome and preparation method thereof |
| WO2023041588A1 (en) | 2021-09-14 | 2023-03-23 | Advapharm Gmbh | Novel lipopeptide formulation |
-
2011
- 2011-03-22 CN CN2011100684248A patent/CN102688192A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104055735A (en) * | 2013-03-22 | 2014-09-24 | 深圳翰宇药业股份有限公司 | Semaglutide liposome and preparation method thereof |
| CN104055735B (en) * | 2013-03-22 | 2016-08-03 | 深圳翰宇药业股份有限公司 | A kind of liposome of Sa Molutai and preparation method thereof |
| WO2023041588A1 (en) | 2021-09-14 | 2023-03-23 | Advapharm Gmbh | Novel lipopeptide formulation |
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| Date | Code | Title | Description |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20120926 |