CN101991543A - Omeprazole enteric dried suspension agent and preparation method thereof - Google Patents
Omeprazole enteric dried suspension agent and preparation method thereof Download PDFInfo
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- CN101991543A CN101991543A CN2009101009553A CN200910100955A CN101991543A CN 101991543 A CN101991543 A CN 101991543A CN 2009101009553 A CN2009101009553 A CN 2009101009553A CN 200910100955 A CN200910100955 A CN 200910100955A CN 101991543 A CN101991543 A CN 101991543A
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- omeprazole
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Abstract
The invention relates to an omeprazole enteric dried suspension agent and a preparation method thereof. The omeprazole enteric dried suspension agent comprises 5 to 20 weight percent of omeprazole pellet or granule, 1 to 10 weight percent of suspending agent and 70 to 90 weight percent of flavoring agent. The omeprazole enteric dried suspension agent has stable quality, quick response and good suspension effect and it is convenient for old people, children and dysphagia patients to use the suspension agent.
Description
Technical field
The present invention relates to field of medicine preparations, relate in particular to the preparation of omeprazole, particularly a kind of omeprazole enteric-coated dry suspension and preparation method thereof.
Background technology
Omeprazole (chemical name 5-methoxyl group-2[[(4-methoxyl group-3; 5-dimethyl-2-pyridine radicals) methyl] sulfinyl]-the 1-benzimidazole) be the excretory potent inhibitor of acidic gastric juice, can be used for treating gastric ulcer, duodenal ulcer, anti-sharp ulcer, reflux esophagitis and Zhuo-Emhorn syndrome.European patent EP 0005129 discloses the reactive compound of proton pump inhibitor omeprazole.Omeprazole and salt thereof see among the EP0005129 and EP0124495 in.WO94/27988 discloses some salt and the preparation thereof of omeprazole single enantiomer.
Omeprazole is easy to degraded and conversion in acidity or neutral medium.The degradation half life of omeprazole was 10min at PH less than 4 o'clock, and equaling at 6.5 o'clock at PH is 18 hours, equaled to be approximately 300 days at 11 o'clock at PH.Omeprazole in acid and neutral medium to degraded, transform responsive, and with mixture of alkaline compounds in stable, in addition, above-claimed cpd stability also wet, the influence of hot, organic solvent and light.Because omeprazole is unstable in sour environment, the oral formulations that contains omeprazole requires to avoid to contact with tart gastric juice, must transfer in the intestinal of meta-alkalescence with original shape, therefore, what use clinically all is enteric coated preparation of omeprazole, the main dosage form of omeprazole in the market is omeprazole enteric-coated capsules, omeprazole enteric-coated, but these dosage forms and the patient that is not suitable for child, old man and dysphagia use.
Summary of the invention
The object of the present invention is to provide that a kind of compliance is good, steady quality, rapid-action omeprazole enteric-coated dry suspension so that the patient of child, old man and dysphagia uses.
In order to realize the foregoing invention purpose, the present invention adopts following technical scheme:
A kind of omeprazole enteric-coated dry suspension comprises Omeprazole Pellets or granule 5%～20%, suspending agent 1%～10%, correctives 70%～90%, and described percentage ratio is weight percentage.
Described Omeprazole Pellets or granule comprise pharmaceutically active layer, sealing coat, enteric layer, sealing coat weightening finish 5%～25%, enteric layer weightening finish 15%～30%.
Described pharmaceutically active layer comprises omeprazole, filler, alkaline stabiliser, surfactant, disintegrating agent and binding agent.
Described alkaline stabiliser is the faintly acid sodium of the organic or inorganic of phosphoric acid, carbonic acid, citric acid, malic acid, fumaric acid, potassium, calcium, magnesium, aluminum salt, aluminium hydroxide/sodium bicarbonate coprecipitate.
Filler can be selected from starch, pregelatinized Starch, lactose, sucrose, sucrose ball core, microcrystalline Cellulose, mannitol.
Surfactant can be selected from sodium lauryl sulphate or Tween 80.
Disintegrating agent can be selected from sodium carboxymethyl cellulose, carboxymethyl starch sodium, polyvinylpolypyrrolidone, low-substituted hydroxypropyl level cellulose etc.
Binding agent can be selected from polyvidone, hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, carboxymethyl cellulose, ethyl cellulose, acid polyethylene, Polyethylene Glycol etc.
Active layer can also add fluidizer and improves liquidity in addition, as micropowder silica gel etc.
Described sealing coat coating material is one or more mixing in starch, lactose, sucrose, microcrystalline Cellulose, mannitol, hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, carboxymethyl cellulose, the ethyl cellulose.
Described enteric layer coating material is one or more mixing in acrylic resin, hydroxypropyl methylcellulose acetic acid succinate (HPMCPCAS), hydroxypropyl methylcellulose dimethyl phthalate (HPMCP), the cellulose acetate dimethyl phthalate (CAP).
Described suspending agent is one or more mixing in xanthan gum, carrageenan, arabic gum, gelatin, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, polyvidone, pectin, guar gum, sodium alginate, the carboxymethyl cellulose.
The prescription of 1000 bags of enteric dry suspension of preparation is: omeprazole 10g, sucrose ball core 60, mannitol 10g, carboxymethyl starch sodium 2g, sodium dihydrogen phosphate 2g, tween 80 1g, HPMC5g, acrylic resin aqueous dispersion 60g, triethyl citrate 1.8g, titanium dioxide 1.8g, Pulvis Talci 2.7g, xanthan gum 8g, sucrose 669.7g, micropowder silica gel 8g, Herba Menthae essence are an amount of.
The prescription of 1000 bags of enteric dry suspension of preparation is: omeprazole 20g, Icing Sugar 60g, mannitol 20g, carboxymethyl starch sodium 4g, sodium dihydrogen phosphate 4g, tween 80 2g, HPMC6g, acrylic resin aqueous dispersion 80g, triethyl citrate 2.4g, titanium dioxide 2.4g, Pulvis Talci 6g, xanthan gum 10g, sucrose 849.2g, micropowder silica gel 10g, Herba Menthae essence are an amount of.
The invention also discloses a kind of preparation method of omeprazole enteric-coated dry suspension, this preparation method comprises the steps:
(1) preparation omeprazole pastille micropill or granule;
(2) bag sealing coat;
(3) bag enteric layer;
(4) be mixed with and obtain omeprazole enteric-coated dry suspension with the residue adjuvant.
The omeprazole enteric-coated dry suspension steady quality that the present invention obtains, rapid-action, suspendible is effective, makes things convenient for the patient of old people, child and dysphagia to use.
The specific embodiment
Embodiment 1: 1000 bags of omeprazole enteric-coated dry suspension of present embodiment preparation, adopt following prescription:
Omeprazole 10g sucrose ball core 60g
Mannitol 10g carboxymethyl starch sodium 2g
Sodium dihydrogen phosphate 2g Tween 80 1g
HPMC 5g acrylic resin aqueous dispersion 60g
Triethyl citrate 1.8g titanium dioxide 1.8g
Pulvis Talci 2.7g xanthan gum 8g
Sucrose 669.7g micropowder silica gel 8g
Herba Menthae essence is an amount of
Preparation technology:
(1), omeprazole and mannitol, carboxymethyl starch sodium, sodium dihydrogen phosphate cross 120 mesh sieve mix homogeneously, and be standby; Preparation 2%HPMC solution, the Tween 80 of adding recipe quantity, standby; Sucrose ball core is placed centrifugal granulator, add medicine to as binding agent, the rearmounted 40 ℃ of oven for drying that finish of adding medicine to above-mentioned 2%HPMC solution;
(2), Omeprazole Pellets that step 1 is obtained places centrifugal granulator, with 5%HPMC solution bag sealing coat, coating is finished rearmounted 40 ℃ of oven for drying;
(3), with exsiccant above-mentioned micropill, place fluid bed, with acrylic resin aqueous dispersion coating solution coating, after coating is finished, take out and to place 40 ℃ of oven for drying;
(4), with omeprazole enteric-coated micro-pill and sucrose, xanthan gum mix homogeneously, again with micropowder silica gel, Herba Menthae essence mix homogeneously promptly.
The omeprazole enteric-coated dry suspension that present embodiment makes is compared with dosage form in the past, possesses good stability, advantage such as rapid-action, and the patient who is fit to old people, child and dysphagia more takes.
Embodiment 2: 1000 bags of omeprazole enteric-coated dry suspension of present embodiment preparation, adopt following prescription:
Omeprazole 20g microcrystalline Cellulose ball core 60g
Mannitol 20g carboxymethyl starch sodium 4g
Sodium dihydrogen phosphate 4g Tween 80 2g
HPMC 6g acrylic resin aqueous dispersion 80g
Triethyl citrate 2.4g titanium dioxide 2.4g
Pulvis Talci 6g xanthan gum 10g
Icing Sugar 849.2g micropowder silica gel 10g
Herba Menthae essence is an amount of
Preparation method is identical with embodiment 1.
Embodiment 3: 1000 bags of omeprazole enteric-coated dry suspension of present embodiment preparation, adopt following prescription:
Omeprazole 20g Icing Sugar 60g
Ethyl cellulose 20g carboxymethyl starch sodium 4g
Calcium hydrogen phosphate 4g Tween 80 2g
HPMC 4.5g HPMCPCAS 78g
Triethyl citrate 2.4g titanium dioxide 2.4g
Pulvis Talci 5g arabic gum 9.5g
Icing Sugar 900g micropowder silica gel 10g
Herba Menthae essence is an amount of
Preparation method is identical with embodiment 1.
Claims (10)
1. an omeprazole enteric-coated dry suspension is characterized in that comprising Omeprazole Pellets or granule 5%～20%, suspending agent 1%～10%, correctives 70%～90%, and described percentage ratio is weight percentage.
2. a kind of omeprazole enteric-coated dry suspension according to claim 1 is characterized in that described Omeprazole Pellets or granule comprise pharmaceutically active layer, sealing coat, enteric layer, sealing coat weightening finish 5%～25%, enteric layer weightening finish 15%～30%.
3. a kind of omeprazole enteric-coated dry suspension according to claim 2 is characterized in that described pharmaceutically active layer comprises omeprazole, filler, alkaline stabiliser, surfactant, disintegrating agent and binding agent.
4. a kind of omeprazole enteric-coated dry suspension according to claim 3, it is characterized in that described alkaline stabiliser is the faintly acid sodium of organic or inorganic, potassium, calcium, magnesium, the aluminum salt of phosphoric acid, carbonic acid, citric acid, malic acid, fumaric acid, aluminium hydroxide/sodium bicarbonate coprecipitate.
5. a kind of omeprazole enteric-coated dry suspension according to claim 2 is characterized in that described sealing coat coating material is one or more mixing in starch, lactose, sucrose, microcrystalline Cellulose, mannitol, hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, carboxymethyl cellulose, the ethyl cellulose.
6. a kind of omeprazole enteric-coated dry suspension according to claim 2 is characterized in that described enteric layer coating material is one or more mixing in acrylic resin, hydroxypropyl methylcellulose acetic acid succinate (HPMCPCAS), hydroxypropyl methylcellulose dimethyl phthalate (HPMCP), the cellulose acetate dimethyl phthalate (CAP).
7. a kind of omeprazole enteric-coated dry suspension according to claim 1 is characterized in that described suspending agent is one or more mixing in xanthan gum, carrageenan, arabic gum, gelatin, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, polyvidone, pectin, guar gum, sodium alginate, the carboxymethyl cellulose.
8. a kind of omeprazole enteric-coated dry suspension according to claim 1 is characterized in that the prescription for preparing 1000 bags of enteric dry suspension is: omeprazole 10g, sucrose ball core 60, mannitol 10g, carboxymethyl starch sodium 2g, sodium dihydrogen phosphate 2g, tween 80 1g, HPMC5g, acrylic resin aqueous dispersion 60g, triethyl citrate 1.8g, titanium dioxide 1.8g, Pulvis Talci 2.7g, xanthan gum 8g, sucrose 669.7g, micropowder silica gel 8g, Herba Menthae essence are an amount of.
9. a kind of omeprazole enteric-coated dry suspension according to claim 1 is characterized in that the prescription for preparing 1000 bags of enteric dry suspension is: omeprazole 20g, Icing Sugar 60g, mannitol 20g, carboxymethyl starch sodium 4g, sodium dihydrogen phosphate 4g, tween 80 2g, HPMC6g, acrylic resin aqueous dispersion 80g, triethyl citrate 2.4g, titanium dioxide 2.4g, Pulvis Talci 6g, xanthan gum 10g, sucrose 849.2g, micropowder silica gel 10g, Herba Menthae essence are an amount of.
10. according to the preparation method of the described a kind of omeprazole enteric-coated dry suspension of claim 1～9, it is characterized in that this preparation method comprises the steps:
(1) preparation omeprazole pastille micropill or granule;
(2) bag sealing coat;
(3) bag enteric layer;
(4) be mixed with and obtain omeprazole enteric-coated dry suspension with the residue adjuvant.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2009101009553A CN101991543A (en) | 2009-08-10 | 2009-08-10 | Omeprazole enteric dried suspension agent and preparation method thereof |
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| CN2009101009553A CN101991543A (en) | 2009-08-10 | 2009-08-10 | Omeprazole enteric dried suspension agent and preparation method thereof |
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| CN101991543A true CN101991543A (en) | 2011-03-30 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102641286A (en) * | 2012-03-12 | 2012-08-22 | 南京海纳医药科技有限公司 | Compound omeprazole dry suspension and preparation method thereof |
| CN106798750A (en) * | 2017-03-23 | 2017-06-06 | 济宁华能制药厂有限公司 | A kind of preparation method of compound omeprazole dry suspension |
| EP3523288A4 (en) * | 2016-10-06 | 2020-05-27 | Jubilant Generics Limited | Pharmaceutical suspension dosage form of benzimidazole compounds and process of preparation thereof |
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| CN1025151C (en) * | 1986-04-30 | 1994-06-29 | 哈斯莱股份公司 | Pharmaceutical formulations of acid labile substances for oral use |
| CN1827089A (en) * | 2005-02-28 | 2006-09-06 | 上海艾力斯医药科技有限公司 | Fine granules containing acid-labile medicine and preparation thereof |
| CN1935139A (en) * | 2006-09-30 | 2007-03-28 | 邢为藩 | Substituted benzimidazole proton pump inhibitor composition, and its preparing method |
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2009
- 2009-08-10 CN CN2009101009553A patent/CN101991543A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1025151C (en) * | 1986-04-30 | 1994-06-29 | 哈斯莱股份公司 | Pharmaceutical formulations of acid labile substances for oral use |
| CN1827089A (en) * | 2005-02-28 | 2006-09-06 | 上海艾力斯医药科技有限公司 | Fine granules containing acid-labile medicine and preparation thereof |
| CN1935139A (en) * | 2006-09-30 | 2007-03-28 | 邢为藩 | Substituted benzimidazole proton pump inhibitor composition, and its preparing method |
Non-Patent Citations (1)
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| 黄惠芳等: "奥美拉哇肠溶胶囊的制备及其工艺评价", 《广东药学》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102641286A (en) * | 2012-03-12 | 2012-08-22 | 南京海纳医药科技有限公司 | Compound omeprazole dry suspension and preparation method thereof |
| EP3523288A4 (en) * | 2016-10-06 | 2020-05-27 | Jubilant Generics Limited | Pharmaceutical suspension dosage form of benzimidazole compounds and process of preparation thereof |
| CN106798750A (en) * | 2017-03-23 | 2017-06-06 | 济宁华能制药厂有限公司 | A kind of preparation method of compound omeprazole dry suspension |
| CN106798750B (en) * | 2017-03-23 | 2019-08-20 | 济宁华能制药厂有限公司 | A kind of preparation method of compound omeprazole dry suspension |
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Application publication date: 20110330 |