CN106031711A - Preparation method and applications of ilaprazole sodium liposome - Google Patents
Preparation method and applications of ilaprazole sodium liposome Download PDFInfo
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- CN106031711A CN106031711A CN201510116690.1A CN201510116690A CN106031711A CN 106031711 A CN106031711 A CN 106031711A CN 201510116690 A CN201510116690 A CN 201510116690A CN 106031711 A CN106031711 A CN 106031711A
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Abstract
The present invention provides a preparation method and applications of ilaprazole sodium liposome, wherein the method is characterized in that lecithin and cholesterol are adopted as film materials and an ethanol injection method is adopted to encapsulate an ilaprazole sodium composition into the ilaprazole sodium liposome. According to the present invention, the ilaprazole sodium liposome has characteristics of targeting property, slow releasing property, cell affinity, histocompatibility, no toxicity, and drug stability increasing; the obtained preparation has characteristics of high stability, low side effect and long drug acting time, and further has effects of gastric acid secretion inhibiting, gastric mucosa protecting, and Helicobacter pylori killing; and with the application of the ethanol injection method to prepare the ilaprazole sodium liposome, the continuous production can be achieved, and the industrialized requirement can be well met, such that the broad application prospects are provided in the field of medicine.
Description
Technical field
The present invention relates to pharmaceutical technology field, be specifically related to the preparation method and applications of a kind of ilaprazole sodium lipidosome.
Background technology
Peptic ulcer (peptic ulcer) is one of commonly encountered diseases frequently-occurring disease clinically.China is the hotspot of ulcer, and the crowd of the most about about 10% suffered from primary disease the most once.Duodenal ulcer is common compared with gastric ulcer clinically, both ratios about 1.56～5.6: 1.The sick kind that gastric ulcer, duodenal ulcer are a kind of chronic diseases, recurrence coefficient is bigger, needs gastric ulcer, the patient of duodenal ulcer that the treatment of long period, particularly helicobacter pylori infections cause.From the point of view of patient, the price factor of medicine is particularly significant.Therefore, extensive patients in the urgent need to good effect, safety is high, price is low, ill effect is little, ruggedness is good, to treatment gastric ulcer, the product of duodenal ulcer determined curative effect.
Ilaprazole Sodium (Ilaprazole) is the latest generation proton pump inhibitor that ocean Pharmaceutical Co., Ltd of Korea S one develops, and is widely used for the digestive tract disease relevant to various acid, such as duodenal ulcer, gastric ulcer, reflux esophagitis etc..Compared with other PPI, Ilaprazole Sodium has that anti-acid activity is the strongest, treatment without controlling the advantages such as sour ability is higher at individual variation, night, be expected to become core product in PPI market.
Liposome (liposome) refers to medicine etc. is encapsulated in lipoids bilayer the micro-shape vesicle formed, and is also called lipoid bead or liquid crystal microcapsules.Liposome is owing to having the features such as the stability of targeting, slow-releasing, cellular affinity and histocompatibility, the toxicity of reduction medicine, raising medicine, thus extensively applies at medicine and cosmetic field.
Ilaprazole (Ilaprazole) structure belongs to benzimidazole, unstable to acid, is the proton pump inhibitor of irreversible.It is selectively entered parietal cell after ilaprazole oral administration, is converted into sulfenamide active metabolite, with the sulfydryl effect on H+, K+-ATP enzyme, form the covalent bond of disulfide bond, irreversible suppression H+, K+-ATP enzyme, produce the effect of gastric acid secretion inhibiting.First generation PPI is because gastric acid secretion bounce-back after delayed gastric emptying, parietal cell swelling and obvious drug withdrawal can be caused, so clinical practice has limitation.Ilaprazole is as one of proton pump inhibitor (PPI) of new generation, overcome some defect of original like product the most to varying degrees, can strengthen dyskinesis sample functional dyspepsia (GERD) and the curative effect of other acid-related diseases simultaneously.The main feature of ilaprazole includes: 1. clinical acid suppression is effective；2. Acidinhibitor is rapid-action；The most all can maintain higher acid suppression level；4. determined curative effect, individual variation is little；5. without influencing each other and between other drug；6. untoward reaction is few.
The most domestic Ilaprazole Sodium enteric coated tablet, Metronidazole Tablet, three kinds of drug combinations of clarithromycin tablet treatment peptic ulcers the most just it are respectively adopted.Weak point is erious adverse reaction, and onset is slow.Not having the preparation of ilaprazole sodium lipidosome on market, the application of this patent can overcome the disadvantages that the blank of this part.
In order to overcome existing technological deficiency, it is provided that a kind of alcohol injection prepares ilaprazole sodium lipidosome, is possible not only to realize continuous prodution, moreover it is possible to preferably adapt to industrialization demand, the prospect being therefore widely used at field of medicaments.
Summary of the invention
In order to overcome the defect of prior art, the invention provides the preparation method and applications of a kind of ilaprazole sodium lipidosome.The preparation method and applications of a kind of ilaprazole sodium lipidosome of the present invention, ilaprazole composition of sodium is made up of following ingredient: Ilaprazole Sodium 10-20mg, metronidazole 0.5-1mg, sodium bicarbonate 50-100mg mix.The method of the ilaprazole sodium lipidosome described in preparation, step is as follows: weigh lecithin, cholesterol and ilaprazole composition of sodium in proportion, add 4mL dehydrated alcohol in 55 DEG C of water-baths to molten, inject in the aqueous vehicles of the phosphate buffer filling 20mLpH6.0-8.0 while stirring with syringe, stirring aquation 30min, rotary evaporation removes ethanol (55 DEG C, vacuum 0.1MPa), cooling rapidly, extra high pressure homogenize (pressure 25000PSI, circulate 2-4 time), then lyophilization or spray drying, to obtain final product.
The advantage of a kind of ilaprazole sodium lipidosome of the present invention has: 1. this ilaprazole sodium lipidosome has targeting, slow-releasing, cellular affinity and histocompatibility, and nontoxic, improves the stability of medicine simultaneously.
2. the preparation not only stability that prepared by this ilaprazole sodium lipidosome is high, side effect is little, and drug treating time is long, and has gastric acid secretion inhibiting, protects gastric mucosa, kills the effect of helicobacter pylori simultaneously.
3. use alcohol injection to prepare ilaprazole sodium lipidosome, be possible not only to realize continuous prodution, moreover it is possible to preferably adapt to industrialization demand, the prospect being therefore widely used at field of medicaments.
4. pair treatment peptic ulcer has obvious action, has drug effect fast, and effect is strong, it is possible to increase bioavailability, the advantage thoroughly killing helicobacter pylori.
Detailed description of the invention embodiment 1 weighs lecithin, cholesterol for 2:1 in molar ratio, ilaprazole composition of sodium is added 4mL dehydrated alcohol in 55 DEG C of water-baths to molten, injecting with syringe while stirring in the aqueous vehicles of the phosphate buffer filling 20mLpH6.0-8.0, stir aquation 30min, rotary evaporation removes ethanol (55 DEG C, vacuum 0.1MPa), cooling, extra high pressure homogenize (pressure 25000PSI circulates 2-4 time) rapidly, then lyophilization, to obtain final product.
Embodiment 2 Ilaprazole Sodium sheet 10mg(is in terms of Ilaprazole Sodium) prescription: ilaprazole sodium lipidosome 500 parts, lactose 500g, polyvinylpolypyrrolidone 1000g, magnesium stearate 1000g, make 1000.
Preparation method: weighing ilaprazole sodium lipidosome, lactose, polyvinylpolypyrrolidone, magnesium stearate, mix homogeneously by recipe quantity, direct compression forms, prepares tablet.
Embodiment 3 ilaprazole natrium capsule 20mg(is in terms of Ilaprazole Sodium) prescription: ilaprazole sodium lipidosome 1000 parts, microcrystalline Cellulose 2000g, carboxymethyl starch sodium 1000g, magnesium stearate 1000g, make 1000.
Preparation method: weighing ilaprazole sodium lipidosome by recipe quantity and mix homogeneously with microcrystalline Cellulose, carboxymethyl starch sodium, magnesium stearate, capsule machine filling forms, prepares capsule.
Embodiment 4 ilaprazole sodium injection (every 5mL) prescription: ilaprazole sodium lipidosome 500 parts, Calcium Disodium Versenate 5g, water for injection is appropriate, makes 1000.
Preparation method: weigh ilaprazole sodium lipidosome 500 parts by recipe quantity, Calcium Disodium Versenate 5g adds the water for injection of 80%, stir, with the sodium hydroxide solution regulation pH value of 0.1mol/L to 10.0-12.5, treating that supplementary material is completely dissolved, benefit adds to the full amount of water for injection, again through the membrane filtration mistake of 0.22 μm, embedding, sterilizing, to obtain final product.
Embodiment 5 ilaprazole sodium injection (every 10mL) prescription: ilaprazole sodium lipidosome 1000 parts, Calcium Disodium Versenate 10g, water for injection is appropriate, makes 1000.
Preparation method: weigh ilaprazole sodium lipidosome 1000 parts by recipe quantity, Calcium Disodium Versenate 10g adds the water for injection of 80%, stir, with the sodium hydroxide solution regulation pH value of 0.1mol/L to 10.0-12.5, treating that supplementary material is completely dissolved, benefit adds to the full amount of water for injection, again through the membrane filtration mistake of 0.22 μm, embedding, sterilizing, to obtain final product.
Embodiment 6 injection Ilaprazole Sodium (every bottle of 10mg is in terms of Ilaprazole Sodium)
Prescription: ilaprazole sodium lipidosome 500 parts, mannitol 150g, Calcium Disodium Versenate 2.5g, water for injection is appropriate, makes 1000 bottles.
Preparation method: weigh ilaprazole sodium lipidosome, mannitol, Calcium Disodium Versenate by recipe quantity, injects and is thoroughly mixed in right amount to being completely dissolved with water, adds the water for injection of 90%, stir, benefit adds to the full amount of water for injection, then regulates pH value between 10.0-12.5 with the sodium hydroxide solution of 1mol/L, stirring and evenly mixing, filtering with microporous membrane through 0.22 μm, aseptic subpackaged in cillin bottle, partly jump a queue, lyophilization, evacuation tamponade, roll lid, to obtain final product.
Embodiment 7 injection Ilaprazole Sodium (every bottle of 20mg is in terms of Ilaprazole Sodium)
Prescription: ilaprazole sodium lipidosome 1000 parts, mannitol 300g, Calcium Disodium Versenate 5g, water for injection is appropriate, makes 1000 bottles.
Preparation method: weigh ilaprazole sodium lipidosome, mannitol, Calcium Disodium Versenate by recipe quantity, injects and is thoroughly mixed in right amount to being completely dissolved with water, adds the water for injection of 90%, stir, benefit adds to the full amount of water for injection, then regulates pH value between 10.0-12.5 with the sodium hydroxide solution of 1mol/L, stirring and evenly mixing, filtering with microporous membrane through 0.22 μm, aseptic subpackaged in cillin bottle, partly jump a queue, lyophilization, evacuation tamponade, roll lid, to obtain final product.
Claims (6)
1. the preparation method and applications of an ilaprazole sodium lipidosome, it is characterised in that ilaprazole sodium lipidosome, with lecithin, cholesterol for film material, uses alcohol injection, are prepared from the encapsulating of ilaprazole composition of sodium.
The preparation method and applications of a kind of ilaprazole sodium lipidosome, it is characterised in that ilaprazole composition of sodium is mixed by Ilaprazole Sodium 10-20mg, metronidazole 0.5-1mg, sodium bicarbonate 50-100mg.
3. the method for the ilaprazole sodium lipidosome described in preparation, step is as follows: weigh lecithin, cholesterol and ilaprazole composition of sodium in proportion, add 4mL dehydrated alcohol in 55 DEG C of water-baths to molten, inject in the aqueous vehicles of the phosphate buffer filling 20mLpH6.0-8.0 while stirring with syringe, stirring aquation 30min, rotary evaporation removes ethanol (55 DEG C, vacuum 0.1MPa), cooling rapidly, extra high pressure homogenize (pressure 25000PSI, circulate 2-4 time), then lyophilization or spray drying, to obtain final product.
The preparation method and applications of a kind of ilaprazole sodium lipidosome, it is characterised in that C/PL is the basic substance collectively forming cell membrane and liposome, lecithin and cholesterol mol ratio are 2:1.
5., according to the preparation method and applications of a kind of ilaprazole sodium lipidosome described in claim 1 and 2, it is characterised in that the ilaprazole sodium lipidosome made by alcohol injection, can be applicable to the pharmaceutical preparation of the dosage forms such as tablet, capsule, injection.
6. according to the preparation method and applications of a kind of ilaprazole sodium lipidosome described in claim 1,2 and 3; it is characterized in that gained preparation not only stability is high, side effect is little, drug treating time is long, and has gastric acid secretion inhibiting; protection gastric mucosa, kills the effect of helicobacter pylori simultaneously.
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| CN201510116690.1A CN106031711A (en) | 2015-03-18 | 2015-03-18 | Preparation method and applications of ilaprazole sodium liposome |
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| CN201510116690.1A CN106031711A (en) | 2015-03-18 | 2015-03-18 | Preparation method and applications of ilaprazole sodium liposome |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101502326A (en) * | 2009-02-23 | 2009-08-12 | 江南大学 | Method for preparing vitamin E nano liposome |
| CN102120030A (en) * | 2010-01-08 | 2011-07-13 | 丽珠医药集团股份有限公司 | Medicament of ilaprazole chemical structure and application thereof |
| CN103405471A (en) * | 2013-07-27 | 2013-11-27 | 珠海保税区丽珠合成制药有限公司 | Compound preparation containing ilaprazole sodium |
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- 2015-03-18 CN CN201510116690.1A patent/CN106031711A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101502326A (en) * | 2009-02-23 | 2009-08-12 | 江南大学 | Method for preparing vitamin E nano liposome |
| CN102120030A (en) * | 2010-01-08 | 2011-07-13 | 丽珠医药集团股份有限公司 | Medicament of ilaprazole chemical structure and application thereof |
| CN103405471A (en) * | 2013-07-27 | 2013-11-27 | 珠海保税区丽珠合成制药有限公司 | Compound preparation containing ilaprazole sodium |
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Application publication date: 20161019 |