CN102688480A - 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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- CN102688480A CN102688480A CN2011100684267A CN201110068426A CN102688480A CN 102688480 A CN102688480 A CN 102688480A CN 2011100684267 A CN2011100684267 A CN 2011100684267A CN 201110068426 A CN201110068426 A CN 201110068426A CN 102688480 A CN102688480 A CN 102688480A
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Abstract
A sustained-release preparation of a polypeptide drug for treating diabetes and a production method thereof relate to the technical field of diabetes prevention medicines. The sustained-release preparation provided by the invention is composed of phosphatide, PLGA, sesame oil, glycerin, exenatide and ethanol. According to the invention, the drug is uniformly wrapped in a biodegradation material. Due to hydrophobicity and viscosity of a packing material, the drug will not be rapidly released after subcutaneous injection, so as to greatly reduce stimulation of an injected position, slowly release the drug and obviously decrease toxic and side effect. 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. As there exist no solid particles, 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 that overcomes the insufficient diabetes polypeptide drugs of prior art.
The present invention is mainly by phospholipid, PLGA, Oleum sesami, glycerol, form according to gloomy Taide 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, PLGA, Oleum sesami and glycerol mixing back are added ethanol, and heating also uses the ultrasonic stirring mixing to form oil phase; To add in the entry according to gloomy Taide and dissolve, and regulate pH value, forming pH value is the water of 4.0-5.0; Said oil phase and water are mixed, use the ultrasound probe of Ultrasonic Cell Disruptor to carry out emulsifying, form water in oil emulsion, re-use rotary evaporator moisture in the water in oil emulsion and ethanol are removed, add ethanol again and form single phase soln; Carry out aseptic filtration then.
Production technology of the present invention is simple, reasonable, is easy to production control, and product stability is good.
The specific embodiment
45g phospholipid, 1gPLGA, 30g Oleum sesami and 9g glycerol mixing back are added an amount of ethanol, and heating also uses the ultrasonic stirring mixing to produce homogeneous liquid, forms oil phase.
5g according to dissolving in the gloomy Taide adding 10g water, is produced transparent clear liquid, regulate PH, be called water to 4.0-5.0.
Oil phase and water are mixed, use the ultrasound probe of Ultrasonic Cell Disruptor to carry out emulsifying, form water in oil emulsion.
Use rotary evaporator that moisture in the water in oil emulsion and ethanol are removed, produce complex.
In complex, add an amount of 10g ethanol and form single phase soln, carry out aseptic filtration then.
Claims (2)
1. the slow releasing preparation of diabetes polypeptide drugs is characterized in that mainly by phospholipid, PLGA, Oleum sesami, glycerol, forms according to gloomy Taide and ethanol.
2. the production method of the slow releasing preparation of diabetes polypeptide drugs according to claim 1 is characterized in that phospholipid, PLGA, Oleum sesami and glycerol are mixed the back adds ethanol, and heating is also used ultrasonic stirring to mix and formed oil phase; To add in the entry according to gloomy Taide and dissolve, and regulate pH value, forming pH value is the water of 4.0-5.0; Said oil phase and water are mixed, use the ultrasound probe of Ultrasonic Cell Disruptor to carry out emulsifying, form water in oil emulsion, re-use rotary evaporator moisture in the water in oil emulsion and ethanol are removed, add ethanol again and form single phase soln; Carry out aseptic filtration then.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011100684267A CN102688480A (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 |
|---|---|---|---|
| CN2011100684267A CN102688480A (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 |
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| CN102688480A true CN102688480A (en) | 2012-09-26 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN2011100684267A Pending CN102688480A (en) | 2011-03-22 | 2011-03-22 | Sustained-release preparation of polypeptide drug for treating diabetes and production method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107156533A (en) * | 2017-05-08 | 2017-09-15 | 张银花 | A kind of lobster cultivation selenium element high-efficiency sustained-release high protein feed |
-
2011
- 2011-03-22 CN CN2011100684267A patent/CN102688480A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107156533A (en) * | 2017-05-08 | 2017-09-15 | 张银花 | A kind of lobster cultivation selenium element high-efficiency sustained-release high protein feed |
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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 |