CN101120930B - Omeprazole composition and preparing process thereof - Google Patents
Omeprazole composition and preparing process thereof Download PDFInfo
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- CN101120930B CN101120930B CN2007101415774A CN200710141577A CN101120930B CN 101120930 B CN101120930 B CN 101120930B CN 2007101415774 A CN2007101415774 A CN 2007101415774A CN 200710141577 A CN200710141577 A CN 200710141577A CN 101120930 B CN101120930 B CN 101120930B
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Abstract
A compound of the omeprazole and the Sodium Bicarbonate comprise a plurality of enteric-coated pellets composed by the omeprazole and the Sodium Bicarbonate, the capsules composed by Sodium Bicarbonate of any mode. The enteric-coated pellets comprise a pellet core, an isolation layer and an enteric-coated layer. The present invention has the advantages that acid degradation of the omeprazole is resolved by the enteric-coated layer, which prolongs binding between the gastric wall and omeprazole. When Sodium Bicarbonate of any mode neutralizing the gastric acid reaches a certain PH value, the enteric-coated layer can disintegrate and omeprazole can be released. PH value in the stomach remains stable during the releasing process. Another advantage of the present invention is that the compound can be taken at any time when stomachache happens.
Description
Technical field
The present invention relates to the compositions of a kind of omeprazole and sodium bicarbonate, also relate to the preparation method of said composition.
Technical background
Digestive system disease is one of common frequently-occurring disease, and wherein based on Peptic Ulcers, total sickness rate accounts for 10～20% of population.U.S. peptic ulcer patient is about 10%, and Germany is 12.3%; China is according to the investigation of minority area, and the digestive tract disease sickness rate is 11.43%, and wherein the peptic ulcer rate is 4.54%.
Along with the Chinese society development, the change of circumstances, the variation of population structure and people life style, mainly because of smoking, drink, nervous, medicine irritation etc., the sickness rate of peptic ulcer increases gradually, become a kind of commonly encountered diseases and frequently-occurring disease, bring great misery, cause patients ' life quality to descend to the patient.Therefore for these reasons, the treatment of peptic ulcer more and more receives publicity clinically and payes attention to, and medicament for resisting peptic ulcer receives publicity safely and effectively, and becomes one of the emphasis of present drug development research and focus.
Proton pump inhibitor is than histamine H
2-receptor antagonist and the excretory medicine of other gastric acid inhibitory have obvious superiority, as selectivity height, good effect, few side effects, can eliminate helicobacter pylori (gastric ulcer pathogenic bacterium) etc. with the compound preparation of antibiotic compatibility.
Omeprazole is typical proton pump inhibitor, is usually used in treating gastric ulcer clinically.Its chemical name is: 5-methoxyl group-2-{[(4-methoxyl group-3,5-dimethyl-2-pyridine radicals)-methyl]-sulfoxide }-the 1H-benzimidazole.Take 1 omeprazole (omeprazole) 20mg every day, it presses down acid and acts in initial 3～5d and constantly add up, and the suppression ratio of the basic gastric acid in 1 week back can reach 100%.
Omeprazole is highly sour unsettled, is easy to the degeneration of degrading in acid and neutral medium, considers stability, and apparent omeprazole must not contact it by the enteric coat layer protection with acidic gastric juice, so oral formulations is enteric coated preparation or capsule.Because morning the gastric juice acidity whole day of comparing, PH is higher, instructions of taking also is confined to swallow morning every day, that is to say needs on an empty stomach just to advance to obey omeprazole in about 10 hours.
Pilbrant etc., the exploitation of omeprazole peroral dosage form, Scandinavia Gastroenterology (SCAND.J.GASTROENT.) 20 (supplementary issue 108): 113～120 (1985) have lectured the suspension of 60g micronization omeprazole in also containing the 50ml water of 8mmol sodium bicarbonate.By this suspension of following method afford: in fasting after at least 10 hours, give the 50ml aqueous solution of patient 8mmol sodium bicarbonate, after 5 minutes, the patient takes the omeprazole suspension with another part 50ml sodium bicarbonate solution, after 10,20 and 30 minutes, take the sodium bicarbonate solution of 50ml respectively, therefore then, this therapeutic process complexity, the omeprazole that the patient takes dose also needs to absorb the 48mmol sodium bicarbonate.
A large amount of taking of sodium bicarbonate can produce significant side effects, such as: the patient or the critical patient that are not suitable for must accepting repeatedly omeprazole dosage; Sodium bicarbonate is neutralized under one's belt or absorbs, so that the phenomenon of having the hiccups occurs, and the patient who suffers from gastroesophageal reflux may increase the weight of or worsen their reflux disease; Patient with a plurality of diseases of following critical illness should avoid the sodium bicarbonate of overdose; The buffering omeprazole solution of prior art need be taken sodium bicarbonate for a long time, makes the patient be difficult to comply with the therapeutic scheme of prior art.Therefore wish to have a kind of preparation of proton pump inhibitor, taking convenience can be provided, have good patient's compliance and offer the patient to alleviate their discomfort.
With Swedish patent SE9600071-6 is that the Chinese patent CN96193594.4 of priority has put down in writing the proton pump inhibitor that contains acid-sensitive sense and the solid preparation of one or more antacids or alginate, three kinds of forms can be arranged: the proton pump inhibitor piller of enteric coating and the mixing mutually that contains antacid and drug excipient, tabletting; One deck is the proton pump inhibitor piller of enteric coating, and another layer contains the mixture of drug excipient and antacid or alginic acid agent, separated tabletting arbitrarily by the antisticking layer; By the enteric coat layer coating, there is sealing coat in proton pump inhibitor at label between label and enteric coat layer, and has one deck and the blended antacid of drug excipient, tabletting on enteric coat layer.The tablet outside of above-mentioned three kinds of forms is all by any coating of film coating layer.In the tabletting process, enteric coating breaks easily, and simultaneously, its antacid is the mixture of aluminium hydroxide and calcium carbonate.
US6489346, US6645988, US6699885, US6780882 are with the patent of U.S. Pat 5840737 for the continuation application mandate of female case application, these patents have all been put down in writing the composition preparation of proton pump inhibitor and at least a buffer agent, wherein compounded plate, powder, the chewable tablet of disintegrate suspension sheet, standard film, effervescent tablet and effervescent granule, parietal cell activator (choco-base product), regularly release all are that sodium bicarbonate powder and omeprazole are mixed and made into corresponding dosage form fast, and omeprazole contacts with coat of the stomach simultaneously with sodium bicarbonate.It should be noted that:
1, omeprazole capsule: the omeprazole 20g of non-casing is inserted the #4 empty gelatin capsule be evenly dispersed in the 240g sodium bicarbonate powder and form capsule-core.Then this capsule-core is inserted the #00 empty gelatin capsule with 600g sodium bicarbonate and 110g pre-gelatinized starch.
2, omeprazole two parts sheet: (1), omeprazole is fully mixed with sodium bicarbonate, get 220g and be added to one 3/8 and " be pressed into small pieces in the mould of diameter; The sodium bicarbonate that takes by weighing 280g in addition is added to 1/2 " mould in, tabletting with 3/8 " small pieces are put into 1/2 " top and be placed on central authorities, adds the sodium bicarbonate of 380g, tabletting at the top.(2), getting the 220g omeprazole is added to one 3/8 and " is pressed into small pieces in the mould of diameter; The sodium bicarbonate that takes by weighing 280g in addition is added to 1/2 " mould in, tabletting with 3/8 " small pieces are put into 1/2 " top and be placed on central authorities, adds the sodium bicarbonate of 380g, tabletting at the top.
More than two kinds of dosage forms all do not have enteric coatedly, can not guarantee the stable absorption of omeprazole, in addition, these two dosage form dosage are big, the technological operation complexity is not suitable for big commercial production.
Based on above shortcoming, hope can provide a kind of and take easyly, can delay omeprazole and combine with coat of the stomach, and the sour environment in the stomach is alleviated gradually, and omeprazole is discharged, and is fit to the pharmaceutical composition of suitability for industrialized production simultaneously.
Summary of the invention
The shortcoming of the present invention in order to overcome above-mentioned dosage form and must (medicine) being taken before meal to use, a kind of omeprazole capsule that can take at any time when stomachache is provided, has comprised some enteric-coated pellets of 10g omeprazole, 100～200g sodium bicarbonate and the formation of molding adjuvant and the 350～450g sodium bicarbonate that exists in any way in this capsule.
This omeprazole capsule is characterized in that the some enteric-coated pellets that formed by the 10mg omeprazole that incapsulates shell, 100～200mg sodium bicarbonate and molding adjuvant and the 350～450mg sodium bicarbonate that exists in any way form.
Enteric-coated pellets is made up of ball core, sealing coat, enteric coat layer three parts, and wherein the ball core is made up of following ingredients by weight percent:
Omeprazole 1～8%
Sodium bicarbonate 40～79%
Filler 20～55%
Disintegrating agent 0～10%
Binding agent is an amount of
Sealing coat is made up of following ingredients by weight percent:
Coating materials 1～4%
Pulvis Talci 1～8%
Plasticizer 0.1～3%
70% ethanol 85～97%
Enteric coat layer is made up of the component of following weight percent:
Enteric coating agents 0.5～10%
Pulvis Talci 0.5～7%
Plasticizer 0.1～4%
70% ethanol 80～95%
The sodium bicarbonate that any-mode exists can be mixed with into forms such as granule, ball, powder with conventional adjuvant, be made up of following ingredients by weight percent:
Sodium bicarbonate 50～90%
Filler 10～40%
Disintegrating agent 0～8%
Lubricant 0～3%
Filler is selected from microcrystalline Cellulose, Icing Sugar, starch, lactose, erythrose, mannitol, sorbitol, more than the mixture of two or more material.
Disintegrating agent is selected cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, crosslinked carboxymethyl fecula sodium, low-substituted hydroxypropyl cellulose, microcrystalline Cellulose for use, or the mixture of above two or more material.
Coating materials is selected from hydroxypropyl emthylcellulose, hydroxypropyl cellulose, methylcellulose, polyvidone, or the mixture of above two or more material.
Enteric coating agents is selected from homemade II resin, homemade III resin, EUDRAGIT L 100, EUDRAGIT L 30 D-55, EUDRAGIT L 100-55, or the mixture of above two or more material.
Plasticizer is selected from propylene glycol, Polyethylene Glycol, glycerol, Fructus Citri Limoniae triethylenetetraminehexaacetic acid fat, dibutyl phthalate, phthalic acid dimethyl ester, or the mixture of above two or more material.
Binding agent is selected from starch slurry, polyvinylpyrrolidone, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose or various cellulose family, or the mixture of above two or more material.
Lubricant can be selected magnesium stearate, Pulvis Talci or its mixture for use.
The preparation method of omeprazole capsule:
Omeprazole, sodium bicarbonate and preparations shaping adjuvant are made enteric-coated pellets.Sodium bicarbonate is mixed and made into arbitrary form with the adjuvant of routine, and the sodium bicarbonate with enteric-coated pellets and arbitrary form existence incapsulates then, promptly.
The invention has the advantages that, delaying omeprazole by enteric coating combines with coat of the stomach, overcome the acid degradation of omeprazole, when in the sodium bicarbonate that arbitrary form exists and gastric acid when reaching certain pH value, the enteric coating disintegrate, discharge wherein omeprazole and sodium bicarbonate, in dispose procedure, can also guarantee that pH value is stable in the stomach.
Specific embodiment
Further set forth the present invention by the following example, but should not be construed as limiting the invention.
Omeprazole capsule is made up of the enteric-coated pellets of omeprazole and sodium bicarbonate and the sodium bicarbonate of arbitrary form, wherein the enteric-coated pellets in the omeprazole capsule is made up of ball core, sealing coat, enteric coat layer three parts, and the preferred following weight percentage of the ball core of enteric-coated pellets is formed:
Omeprazole 3～6%
Sodium bicarbonate 45～70%
Filler 25～45%
Disintegrating agent 0～6%
Binding agent is an amount of
Sealing coat is made up of following ingredients by weight percent:
Coating materials 1～2.5%
Lubricant 0～3%
Plasticizer 0～1%
70%～85% ethanol 93～96%
Enteric coat layer is made up of the component of following weight percent:
Enteric coating agents 1～8%
Lubricant 0～6%
Plasticizer 0～2%
70～95% ethanol 89～94%
The sodium bicarbonate that any-mode exists can be mixed with into forms such as granule, ball, powder with conventional adjuvant, be made up of following ingredients by weight percent:
Sodium bicarbonate 60～88%
Filler 10～35%
Disintegrating agent 0～4%
Lubricant 0～2%
Embodiment one
1, the preparation of enteric-coated pellets:
Ball core prescription:
Composition weight (g) weight percentage (%)
Omeprazole 10 4.8
Sodium bicarbonate 100 47.6
Microcrystalline Cellulose PH301 100 47.6
Add up to 210 100
Add behind the above-mentioned prescription mix homogeneously and become some ball cores in the centrifugal granulator machine, binding agent selects for use 2～4% hydroxypropyl emthylcellulose (HPMC) aqueous solution an amount of.
The sealing coat prescription:
Composition weight (g) weight percentage (%)
HPMC 2 1.9
Pulvis Talci 3 2.8
Propylene glycol 1 0.9
75% ethanol 100 94.4
Add up to 106 100
Above-mentioned sealing coat mixing of materials is even, adopt the centrifugal granulator machine that above-mentioned ball core is carried out coating.
The enteric coat layer prescription:
Composition weight (g) weight percentage (%)
Homemade II resin 4 3.7
Pulvis Talci 4 3.7
Propylene glycol 1 0.9
75% ethanol 100 91.7
Above-mentioned enteric coating mixing of materials is even, adopt the centrifugal granulator machine that the above-mentioned piller that has wrapped sealing coat is carried out coating.
2, sodium bicarbonate particle
Composition weight (g) weight percentage (%)
Sodium bicarbonate 450 68.5
Microcrystalline Cellulose PH101 200 30.4
Pulvis Talci 7 1.1
Add up to 657 100
With sodium bicarbonate and microcrystalline Cellulose PH101 mix homogeneously, granulate earlier with the 2%HPMC aqueous solution, encapsulated after mixing with enteric-coated pellets, Pulvis Talci then.
Embodiment two
1, the preparation of enteric-coated pellets:
Ball core prescription:
Composition weight (g) weight percentage (%)
Omeprazole 10 3.7
Sodium bicarbonate 150 55.6
Microcrystalline Cellulose 100 37.0
Carboxymethyl starch sodium 10 3.7
Add up to 270 100
Add behind the above-mentioned prescription mix homogeneously in the centrifugal granulator machine and make some ball cores, binding agent selects for use 2% hydroxypropyl emthylcellulose (HPMC) aqueous solution an amount of.
The sealing coat prescription:
Composition weight (g) weight percentage (%)
HPMC 2 1.9
Pulvis Talci 3 2.8
Propylene glycol 1 0.9
75% ethanol 100 94.4
Add up to 106 100
Above-mentioned sealing coat mixing of materials is even, adopt the centrifugal granulator machine that above-mentioned ball core is carried out coating.
The enteric coat layer prescription:
Composition weight (g) weight percentage (%)
Homemade II resin 4 3.7
Pulvis Talci 4 3.7
Fructus Citri Limoniae triethylenetetraminehexaacetic acid fat 1 0.9
75% ethanol 100 91.7
Add up to 109 100
Above-mentioned enteric coating mixing of materials is even, adopt the centrifugal granulator machine that the above-mentioned piller that has wrapped sealing coat is carried out coating.
2, sodium bicarbonate particle
Composition weight (g) weight percentage (%)
Sodium bicarbonate 400 65.6
Microcrystalline Cellulose 200 32.8
Pulvis Talci 5 0.8
Magnesium stearate 5 0.8
Add up to 610 100
With sodium bicarbonate and microcrystalline Cellulose mix homogeneously, granulate earlier with the 2%HPMC aqueous solution, encapsulated after mixing with enteric-coated pellets, Pulvis Talci, magnesium stearate then.
Embodiment three
1, the preparation of enteric-coated pellets:
Ball core prescription:
Composition weight (g) weight percentage (%)
Omeprazole 10 3.2
Sodium bicarbonate 200 64.5
Microcrystalline Cellulose 100 32.3
Add up to 310 100
Become ball in the adding centrifugal granulator machine behind the above-mentioned prescription mix homogeneously, binding agent selects for use 2～4% hydroxypropyl emthylcellulose aqueous solutions an amount of.
The sealing coat prescription:
Composition weight (g) weight percentage (%)
HPMC 2 1.9
Pulvis Talci 3 2.8
Propylene glycol 1 0.9
75% ethanol 100 94.4
Add up to 106 100
Above-mentioned sealing coat mixing of materials is even, adopt the centrifugal granulator machine to above-mentioned ball core by carrying out coating.
The enteric coat layer prescription:
Composition weight (g) weight percentage (%)
Homemade II resin 4 3.7
Pulvis Talci 4 3.7
Fructus Citri Limoniae triethylenetetraminehexaacetic acid fat 1 0.9
75% ethanol 100 91.7
Add up to 109 100
Above-mentioned enteric coating mixing of materials is even, become suspension, adopt the centrifugal granulator machine that the above-mentioned piller that has wrapped sealing coat is carried out coating.
2, sodium bicarbonate particle
Composition weight (g) weight percentage (%)
Sodium bicarbonate 350 63.0
Microcrystalline Cellulose 200 36.0
Pulvis Talci 3 0.5
Magnesium stearate 3 0.5
Add up to 556 100
With sodium bicarbonate and microcrystalline Cellulose mix homogeneously, granulate earlier with the 2%HPMC aqueous solution, encapsulated after mixing with enteric-coated pellets, Pulvis Talci, magnesium stearate then.
Embodiment four
1, the preparation of enteric-coated pellets:
Ball core prescription:
Composition weight (g) weight percentage (%)
Omeprazole 10 3.1
Sodium bicarbonate 200 61.5
Lactose 100 30.8
Icing Sugar 15 4.6
Add up to 325 100
Become ball in the adding centrifugal granulator machine behind the above-mentioned prescription mix homogeneously, binding agent selects for use 2～4% hydroxypropyl emthylcellulose aqueous solutions an amount of.
The sealing coat prescription:
Composition weight (g) weight percentage (%)
HPMC 2 1.9
Pulvis Talci 3 2.8
Propylene glycol 1 0.9
75% ethanol 100 94.4
Add up to 106 100
Above-mentioned sealing coat mixing of materials is even, adopt the centrifugal granulator machine that above-mentioned ball core is carried out coating.
The enteric coat layer prescription:
Composition weight (g) weight percentage (%)
EUDRAGIT?L?30?D-55 40 38.1
Pulvis Talci 4 3.8
Fructus Citri Limoniae triethylenetetraminehexaacetic acid fat 1 1.0
Pure water 60 57.1
Add up to 105 100
Above-mentioned enteric coating mixing of materials is even, adopt the centrifugal granulator machine that the above-mentioned piller that has wrapped sealing coat is carried out coating.
2, capsular preparation
Composition weight (g) weight percentage (%)
Sodium bicarbonate 350 62.8
Microcrystalline Cellulose 200 35.9
Magnesium stearate 7 1.3
Add up to 557 100
With sodium bicarbonate and microcrystalline Cellulose mix homogeneously, granulate earlier with the 2%HPMC aqueous solution, encapsulated after mixing with enteric-coated pellets, magnesium stearate then.
Embodiment five
1, the preparation of enteric-coated pellets:
Ball core prescription:
Composition weight (g) weight percentage (%)
Omeprazole 10 3.8
Sodium bicarbonate 150 57.7
Starch 50 19.2
Lactose 50 19.2
Add up to 260 100
Become ball in the adding centrifugal granulator machine behind the above-mentioned prescription mix homogeneously, binding agent selects for use 10% polyvinylpyrrolidone aqueous solution an amount of.
The sealing coat prescription:
Composition weight (g) weight percentage (%)
HPMC 2 1.9
Pulvis Talci 3 2.8
Propylene glycol 1 0.9
75% ethanol 100 94.4
Add up to 106 100
Above-mentioned sealing coat mixing of materials is even, adopt the centrifugal granulator machine that above-mentioned ball core is carried out coating.
The enteric coat layer prescription:
Composition weight (g) weight percentage (%)
EUDRAGIT?L?100 5 4.6
Pulvis Talci 4 3.6
Fructus Citri Limoniae triethylenetetraminehexaacetic acid fat 1 0.9
70% ethanol 100 90.9
Add up to 110 100
Above-mentioned enteric coating mixing of materials is even, adopt the centrifugal granulator machine that the above-mentioned piller that has wrapped sealing coat is carried out coating.
2, sodium bicarbonate powder
Composition weight (g) weight percentage (%)
Sodium bicarbonate 400 87.4
Microcrystalline Cellulose 50 10.9
Pulvis Talci 8 1.7
Add up to 458 100
With sodium bicarbonate and microcrystalline Cellulose mix homogeneously, granulate earlier with the 2%HPMC aqueous solution, encapsulated after mixing with enteric-coated pellets, Pulvis Talci then.
Embodiment six
1, the preparation of enteric-coated pellets:
Ball core prescription:
Composition weight (g) weight percentage (%)
Omeprazole 10 3.3
Sodium bicarbonate 200 66.7
Microcrystalline Cellulose 40 13.3
Sorbitol 40 13.3
Low-substituted hydroxypropyl cellulose 10 3.3
Become ball in the adding centrifugal granulator machine behind the above-mentioned prescription mix homogeneously, binding agent selects for use 10% polyvinylpyrrolidone aqueous solution an amount of.
The sealing coat prescription:
Composition weight (g) weight percentage (%)
HPMC 2 1.9
Pulvis Talci 3 2.8
Propylene glycol 1 0.9
75% ethanol 100 94.4
Add up to 106 100
Above-mentioned sealing coat mixing of materials is even, adopt the centrifugal granulator machine that above-mentioned ball core is carried out coating.
The enteric coat layer prescription:
Composition weight (g) weight percentage (%)
Homemade III resin 4 4.6
Pulvis Talci 4 3.6
Propylene glycol 1 0.9
75% ethanol 100 90.9
Add up to 110 100
Above-mentioned enteric coating mixing of materials is even, become suspension, adopt the centrifugal granulator machine that the above-mentioned piller that has wrapped sealing coat is carried out coating.
2, sodium bicarbonate particle:
Composition weight (g) weight percentage (%)
Sodium bicarbonate 350 86.3
Microcrystalline Cellulose 50 12.3
Pulvis Talci 3 0.7
Magnesium stearate 3 0.7
Add up to 406 100
With sodium bicarbonate and microcrystalline Cellulose mix homogeneously, granulate earlier with the 2%HPMC aqueous solution, encapsulated after mixing with enteric-coated pellets, Pulvis Talci, magnesium stearate then.
Embodiment seven
1, omeprazole piller
Composition weight (g) weight percentage (%)
Omeprazole 10 4.5
Sodium bicarbonate 100 45.5
Lactose 50 22.7
Starch 60 27.3
3% hypromellose aqueous solution is an amount of
Add up to 220 100
Sealing coat:
Hydroxypropyl emthylcellulose 1.5
75% ethanol 75ml
Coatings:
Eudragit 4.2
95% ethanol 70ml
Operation: with omeprazole, sodium bicarbonate, lactose, starch mix homogeneously, use 3% HPMC aqueous solution pelletize then, with the screen cloth of wet feed by diameter 0.8mm, be squeezed into cylinder bar shaped extrudate, heap is discharged on the rotation frictional disk of spheronizator afterwards, is rolled into spheroidal gradually through rolling friction ceaselessly, 40 ± 2 ℃ of dryings, get 18～24 order micropills and put fluidized bed coating, the ethanol liquid bag contagion gown of hydroxypropyl emthylcellulose, the Eudragit enteric is enteric coated again.
2, omeprazole granules
With embodiment 1.
Claims (6)
1. omeprazole capsule, it is characterized in that some enteric-coated pellets of forming by the 10mg omeprazole that incapsulates shell, 100～200mg sodium bicarbonate and molding adjuvant and form with 350～450mg sodium bicarbonate that granule, ball or powder mode exist, wherein enteric-coated pellets is made up of ball core, sealing coat, enteric coat layer, wherein
The ball core of enteric-coated pellets is made up of following ingredients by weight percent:
Omeprazole 1～8%
Sodium bicarbonate 40～79%
Filler 20～55%
Disintegrating agent 0～10%
Binding agent is an amount of
Sealing coat is made up of following ingredients by weight percent:
Coating materials 1～4%
Pulvis Talci 1～8%
Plasticizer 0.1～3%
70% ethanol 85～97%
Wherein coating materials is selected from hydroxypropyl emthylcellulose, hydroxypropyl cellulose, methylcellulose, polyvidone, or the mixture of above two or more material,
Enteric coat layer is made up of following ingredients by weight percent:
Enteric coating agents 0.5～10%
Pulvis Talci 0.5～7%
Plasticizer 0.1～4%
70% ethanol 80～95%
Wherein enteric coating agents is selected from homemade II resin, EUDRAGIT L 30 D-55, EUDRAGIT L 100 or homemade III resin,
Wherein the sodium bicarbonate that exists with granule, ball, powder type can be mixed with conventional adjuvant by sodium bicarbonate, is made up of following ingredients by weight percent:
Sodium bicarbonate 50～90%
Filler 10～40%
Disintegrating agent 0～8%
Lubricant 0～3%.
2. omeprazole capsule according to claim 1 wherein can be mixed with conventional adjuvant with the sodium bicarbonate that granule, ball, powder type exist by sodium bicarbonate, is made up of following ingredients by weight percent:
Sodium bicarbonate 60～88%
Filler 10～35%
Disintegrating agent 0～4%
Lubricant 0～2%.
3. omeprazole capsule, it is characterized in that some enteric-coated pellets of forming by the 10mg omeprazole that incapsulates shell, 100～200mg sodium bicarbonate and molding adjuvant and form with 350～450mg sodium bicarbonate that granule, ball or powder mode exist, wherein enteric-coated pellets is made up of ball core, sealing coat, enteric coat layer, wherein
The ball core of enteric-coated pellets is made up of following weight percentage:
Omeprazole 3～6%
Sodium bicarbonate 45～70%
Filler 25～45%
Disintegrating agent 0～6%
Binding agent is an amount of
Sealing coat is made up of following ingredients by weight percent:
Coating materials 1～2.5%
Lubricant 0～3%
Plasticizer 0～1%
70%～85% ethanol 93～96%
Wherein coating materials is selected from hydroxypropyl emthylcellulose, hydroxypropyl cellulose, methylcellulose, polyvidone, or the mixture of above two or more material,
Enteric coat layer is made up of following ingredients by weight percent:
Enteric coating agents 1～8%
Lubricant 0～6%
Plasticizer 0～2%
70～95% ethanol 89～94%
Wherein enteric coating agents is selected from homemade II resin, EUDRAGIT L 30 D-55, EUDRAGIT L100 or homemade III resin,
Wherein the sodium bicarbonate that exists with granule, ball, powder type can be mixed with conventional adjuvant by sodium bicarbonate, is made up of following ingredients by weight percent:
Sodium bicarbonate 60～88%
Filler 10～35%
Disintegrating agent 0～4%
Lubricant 0～2%.
4. according to claim 1 or 3 described omeprazole capsules, plasticizer is selected from propylene glycol, Polyethylene Glycol, glycerol, Fructus Citri Limoniae triethylenetetraminehexaacetic acid fat, dibutyl phthalate, phthalic acid dimethyl ester, or the mixture of above two or more material.
5. according to claim 1 or 3 described omeprazole capsules, filler is selected from microcrystalline Cellulose, Icing Sugar, starch, lactose, erythrose, mannitol, sorbitol, more than the mixture of two or more material.
6. according to claim 1 or 2 or 3 described omeprazole capsules, its preparation method is: omeprazole, sodium bicarbonate and preparations shaping adjuvant are mixed and made into enteric-coated pellets, sodium bicarbonate is mixed and made into granule, ball or powder type with the adjuvant of routine, sodium bicarbonate with enteric-coated pellets and granule, ball or powder type existence incapsulates then, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2007101415774A CN101120930B (en) | 2006-08-11 | 2007-08-08 | Omeprazole composition and preparing process thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200610048129 | 2006-08-11 | ||
| CN200610048129.5 | 2006-08-11 | ||
| CN2007101415774A CN101120930B (en) | 2006-08-11 | 2007-08-08 | Omeprazole composition and preparing process thereof |
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| CN101120930A CN101120930A (en) | 2008-02-13 |
| CN101120930B true CN101120930B (en) | 2010-09-29 |
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| CN102119927B (en) * | 2010-01-11 | 2012-12-26 | 石药集团中奇制药技术（石家庄）有限公司 | Enteric-coated pellet preparation of proton pump inhibitor and preparation method thereof |
| CN101816641B (en) * | 2010-03-11 | 2012-04-04 | 沈阳亿灵医药科技有限公司 | Omeprazole quick-release solid preparation and preparation method thereof |
| CN102764237A (en) * | 2012-07-06 | 2012-11-07 | 华润赛科药业有限责任公司 | Oral enteric-coated pellet medicinal preparation |
| CN103006691B (en) * | 2013-01-05 | 2014-10-08 | 青岛大学 | Compound capsule preparation containing omeprazole and sodium bicarbonate |
| CN115708812A (en) * | 2022-11-29 | 2023-02-24 | 江苏四环生物制药有限公司 | Ranolazine sustained release tablet and preparation method thereof |
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| US6489346B1 (en) * | 1996-01-04 | 2002-12-03 | The Curators Of The University Of Missouri | Substituted benzimidazole dosage forms and method of using same |
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| US6489346B1 (en) * | 1996-01-04 | 2002-12-03 | The Curators Of The University Of Missouri | Substituted benzimidazole dosage forms and method of using same |
| CN1183047A (en) * | 1996-01-08 | 1998-05-27 | 阿斯特拉公司 | Oral Pharmaceutical dosage forms comprising a proton pump inhibitor and an antacid agent or alginate |
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| CN101120930A (en) | 2008-02-13 |
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