CN1263450C - Disintegration piece of omeprazole and ramification taken through oral cavity and jpreparing technique - Google Patents

Disintegration piece of omeprazole and ramification taken through oral cavity and jpreparing technique Download PDF

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Publication number
CN1263450C
CN1263450C CN 200510002276 CN200510002276A CN1263450C CN 1263450 C CN1263450 C CN 1263450C CN 200510002276 CN200510002276 CN 200510002276 CN 200510002276 A CN200510002276 A CN 200510002276A CN 1263450 C CN1263450 C CN 1263450C
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China
Prior art keywords
omeprazole
oral cavity
cavity disintegration
coating
tablet
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CN1660093A (en
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蒋海松
王红喜
王锦刚
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Beijing Kexin Bicheng Medicine Technology Development Co Ltd
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Beijing Kexin Bicheng Medicine Technology Development Co Ltd
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Abstract

The present invention provides an oral disintegration tablet of a proton pump inhibitor, which comprises omeprazole or derivatives of omeprazole as the active components of the medicine. The oral disintegration tablet is prepared by using omeprazole (5-methoxy group-2-{[(4-methoxy group-3, 5-dimethyl-2-pyridyl)-methyl]-sulfoxide}-1H-benzimidazole) or derivatives of omeprazole as raw materials by various pharmacy methods, coating a protective coating layer, and adding a filling agent, a disintegrating agent, a corrigent, a flow aid, a lubricator, etc. as auxiliary materials by a specific preparation method. Different types of plasticizing agents can be added into the protective coating layer according to different conditions. The oral disintegration tablet of the present invention has the characteristics of good friability, quick disintegration, good taste, no sand feeling, portability, convenience for storage, transport and taking, etc. Particularly, the oral disintegration tablet can be taken under a condition without water and can quickly take effects. Thus, the compliance of patients is improved, and the therapeutic effect of medicines is enhanced.

Description

The oral cavity disintegration tablet of omeprazole and derivant thereof and preparation technology thereof
Technical field
The present invention relates to a kind of omeprazole (5-methoxyl group-2-{[(4-methoxyl group-3,5-dimethyl-2-pyridine radicals)-methyl that is applicable to treatment gastric ulcer, duodenal ulcer, stress ulcer, reflux esophagitis and Zollinger-Ellison Syndrome diseases such as (gastrinomas)]-sulfoxide }-the 1H-benzimidazole) and the oral cavity disintegration tablet of omeprazole derivant.The present invention also designs the preparation method of said preparation.
Background technology
Omeprazole is that the mechanism of action of Recent study exploitation is different from H 2The brand-new antiulcer drug of receptor antagonism.It acts on the gastric mucosa parietal cell specifically, reduces the H in the parietal cell +-K +The activity of-ATP enzyme, thus suppress basic gastric acid and stimulate the gastric acid secretion that causes.Because H +-K +-ATP enzyme is called " proton pump " again, so this class medicine is called " proton pump inhibitor " again.
The omeprazole derivant of being addressed in the present invention refers to various salts, hydrate, single enantiomer and their the various crystal formations thereof of pharmaceutically acceptable omeprazole.
Omeprazole and derivant thereof are easy to degraded in sour environment.Because tart gastric environment, the oral administration form of above-mentioned active substance must prevent that omeprazole and derivant thereof from contacting too early with gastric juice, and above-mentioned active substance must intactly be delivered to the intestinal part that pH is closely neutral and active matter mass-energy is absorbed rapidly.
From the stability characteristic of omeprazole and derivant thereof, must advise that usually omeprazole and basic matterial mix to produce higher pH environment in order to overcome omeprazole problem of unstable and its storage stability of prolongation in sour environment as can be seen.For example:
United States Patent (USP) 4,738,974 have described the alkali salt of omeprazole, and it comprises Li +, K +, Mg 2+, Ca 2+, Ti 4+, N +(R 1) 4Or guanidinesalt.
United States Patent (USP) 4,786,505 have described the omeprazole of oral form, and wherein omeprazole mixes with alkaline matter to produce suitable alkaline environment, makes the pH of omeprazole granules be not less than 7, and preferred pH is not less than 8.Described alkaline matter comprises phosphoric acid, carbonic acid, citric acid or other suitable weak inorganic or organic acid sodium, potassium, calcium, magnesium and aluminum salt.The preparation method of omeprazole nuclear has been described simultaneously: omeprazole is mixed with alkaline material to form mixture of powders, then with mixture of powders corning, sheet, capsule.
United States Patent (USP) 5,232,706 have described the omeprazole of oral form, and it mixes the basic salt of omeprazole or omeprazole and alkali compounds and coating material.Wherein coating material contains a kind of excipient and another kind of alkali compounds and enteric coating at least.Alkali compounds in the described coating material refers to sodium, potassium, magnesium, calcium, aluminum or the dihydroxy aluminum salt of aminoacid (for example glycine, glutamic acid or lysine), picolinic acid (for example nicotinic acid) or organic base (for example guanidine).
Simultaneously, can prevent the peroral dosage form of omeprazole and derivant thereof and contacting of acidic gastric juice preferably by a kind of enteric coat layer.But enteric coating commonly used has acidic-group mostly, if directly with enteric coating parcel omeprazole and derivant thereof, cause omeprazole and derivant variable color and degraded easily.Therefore, it is necessary wrapping up one deck sealing coat coating earlier before the parcel enteric coating layer.
United States Patent (USP) 4,786,505 have described enteric-coated omeprazole preparation.Described omeprazole preparation comprises the core of the alkalescence that contains omeprazole, sealing coat and enteric coating layer.Can make tablet although mentioned prepared piller in the explanation of this patent under the final dosage form of subhead, not have embodiment to describe this tablet or prepare the technology of this tablet.
In fact, variety of issue can appear during as the piller of the enteric coating coating of active substance and granule tabletting when the medicine that will contain acid-sensitive sense.Main difficulty is that enteric coating is unable to undergo to push and the cracked phenomenon of coating membrane takes place, and causes the acidic gastric juice that acid responsive active substance is penetrated into is destroyed.After being tabletting, the acid resistance of preparation descends.
Chinese patent 95190815.4 has been described and has been contained omeprazole or the unitary repressed made tablet of its single enantiomer enteric coating, finds that pressing process does not make significant difference to the character of enteric coating.And describe this tablet and can be dispersed in wet suit and use.
Chinese patent 95194038.4 has been described the oral pharmaceutical formulation that contains magnesium salt of omeprazole.This patent has been emphasized to use the application of the enteric material of aqueous dispersion form, and has made conventional tablet, and the result is good.
Chinese patent 96193763.7 has been described the effervescent dosage form of the multiple units that contains proton pump inhibitor, it is characterized in that proton pump inhibitor is used celphere medicine-feeding method or extrude-be coated with sealing coat behind the piller of round as a ball legal system, after bag is with enteric coating, make effervescent tablet; Its purpose is to be suitable for the patient of dysphagia.
Chinese patent 96197132.0 has been described new containing unsettled omeprazole composition of acid and preparation method thereof, it is characterized in that and to the unsettled active matter dissolving of acid or to be suspended in the suitable adhesive solution, above-mentioned substance is being sprayed in fluid bed on the lactose kernel, dry back adds disintegrating agent and lubricant is pressed into microplate, wrap enteric layer behind the bag sealing coat, last fill is in capsule.Its characteristics are behind the tabletting coating again, do not relate to the destruction of tabletting process to coatings.
Chinese patent 01800081.9 has been described the pharmaceutical preparation and preparation method thereof of the oral administration of benzimidizole derivatives, and its preparation method is characterised in that by wrapping up to make granule or piller behind the protective coating again after the inert core medicine-feeding again; Making capsule or tablet then.Can granule or the piller tabletting according to the method preparation that it provided do not further not specified in invention description though it is mentioned in the claims, do not have embodiment that relevant example and data are provided yet.
Because dosage form needs a large amount of water to send down when most of oral formulations are taken, this makes the patient of many old peoples, infant or dysphagia, water intaking inconvenience be difficult to take.Injection often is easy to generate anaphylaxis or untoward reaction etc. again, and it is big that the while injection also exists operation easier, and the patient suffering is also big, makes and medical treatment cost high the shortcoming that patient economy burden is heavy.Therefore, be necessary to prepare and take convenient dosage form to satisfy the multiple needs that clinical treatment and family use.
Chinese patent 98805424.8 has been described a kind of have excellent Orally disintegrating and deliquescent solid pharmaceutical preparation, and having it is characterized in that selecting water miscible sorbitol, maltose alcohol, reduced form starch sugar, xylitol, reduced form BATANG, erythritol and hydroxypropyl content is the low-substituted hydroxypropyl cellulose of 7.0-9.0% (quality).This patent is to protecting according to the prepared lansoprazole oral cavity disintegration tablet of its described method.
Oral cavity disintegration tablet is a kind of dosage form of new development in recent years, has characteristics such as the taking convenience of carrying, and is very suitable for the patient of dysphagia, as old people and infant etc.Existing list of references does not have the preparation prescription and the preparation method of the oral cavity disintegration tablet of a kind of identical with the present invention or similar omeprazole of full disclosure and derivant thereof.
The orally disintegrating tablet preparation that the object of the present invention is to provide omeprazole and derivant thereof just and preparation method.This oral cavity disintegration tablet has excellent Orally disintegrating characteristic and suitable intensity; and adopt the proper drug method to make and protect for the active substance of acidic gastric juice sensitivity; make product be able to take the influence of tablet forming technique, guarantee by the oral cavity disintegration tablet of prepared omeprazole of prescription provided by the invention and technology and derivant thereof can in gastric juice, not be damaged and behind the neutral intestinal rapidly stripping absorb.
Summary of the invention
The objective of the invention is to improve existing omeprazole and the deficiency of derivant aspect peroral dosage form thereof, provide a kind of taking convenience, absorption is rapid-action, bioavailability is high omeprazole and derivative oral disintegrating tablet preparation thereof to extensive patients and medical personnel.Needn't drink water when the present invention relates to take, in the oral cavity, only need tens seconds can rapid disintegrate or dissolving, the omeprazole that can finish to take medicine with saliva hypopharynx and oral cavity disintegration tablet of derivant thereof and preparation method thereof.
The feature of oral cavity disintegration tablet that contains omeprazole and derivant thereof is as follows: with active substance or make the granule or the piller of appropriate particle size separately or with other acceptable accessories, wrap then with sealing coat, wrap again with enteric coating, can also be at other protective layer of enteric coating outer coatings; Again with the granule behind the above-mentioned coating or piller and specific adjuvant lyophilizing or be pressed into oral cavity disintegration tablet.
In order to the prescription of preparation oral cavity disintegration tablet and the acid resistance that technology can not reduce the enteric coating layer of granule or piller significantly.That is to say, the engineering properties of enteric coating, thickness etc. must guarantee the requirement of Chinese Pharmacopoeia to enteric coating goods defined, guarantee that the granule and the piller of parcel enteric coating is no more than 10% at active matter behind the tabletting at the medium of regulation and the stripping quantity in the time behind the tabletting.
The omeprazole that reaches of the present invention and the oral cavity disintegration tablet of derivant thereof, its preparation method is direct compression process or freeze-drying, the manufacturer with working condition all can adopt.
The omeprazole derivant of one of described active matter in the present invention, available sodium, potassium, calcium and the magnesium salt that omeprazole is arranged; Preferably (-)-omeprazole, Omeprazole Sodium and magnesium omeprazole; More preferably adopt degree of crystallinity greater than 70% magnesium omeprazole.
The poor stability in sour environment in view of omeprazole and derivant thereof, therefore protect omeprazole and derivant thereof is not the problem that overriding concern solves by gastric environment with being damaged, method commonly used is at active component outer wrapping enteric coating.Before the parcel enteric coating layer, the present invention can adopt two kinds of different preprocess methods: 1. omeprazole or omeprazole derivant and specific acceptable accessories are made granule or piller; 2. omeprazole or omeprazole derivant are directly carried out powder coating.
Concrete preparation method is as follows:
The pretreatment of first step omeprazole or omeprazole derivant:
1. piller---omeprazole or omeprazole derivant and specific acceptable accessories are made granule or piller for granulation or system.
Being used for coated granules or piller can be made up of different materials.Active matter can be mixed with other composition.These compositions other acceptable accessories such as filler, surfactant, antacid, binding agent, lubricant and disintegrating agent that can wet, these compositions can add separately, but also combination in any is used.For example, filler can be selected mannitol, starch, pregelatinized Starch, Icing Sugar, dextrin, lactose and microcrystalline Cellulose etc.; Binding agent can be selected methylcellulose, carboxymethyl cellulose, ethyl cellulose, polyvinyl alcohol, Polyethylene Glycol, polyvinylpyrrolidone (PVP), alginic acid and alginate, xanthan gum, hydroxypropyl cellulose and hydroxypropyl emthylcellulose (HPMC).Relatively poor in view of the omeprazole water solublity, can add suitable surfactant, as sodium lauryl sulphate (sodium lauryl sulfate) and polyoxyethylene sorbitan monoleate (Tween 80) etc.Also can add suitable disintegrants to increase the disintegrating property of finished product, as using carboxymethyl starch sodium (CMS-Na), sodium carboxymethyl cellulose (CCNa), crospolyvinylpyrrolidone (PVPP) and low substituted hydroxy-propyl methylcellulose (L-HPC) etc.
Further mixing omeprazole or omeprazole derivant and antacid with the stability that improves these active component is of great use method.Described in the present invention antacid refers to pharmaceutically acceptable alkaline matter.Antacid can be selected from but be not limited only to following material, as phosphoric acid, carbonic acid, citric acid, malic acid, fumaric acid or the faintly acid sodium of other suitable organic or inorganic, potassium, calcium, magnesium and aluminum salt, aluminium hydroxide/sodium bicarbonate coprecipitate; The oxide of calcium, magnesium and aluminum, hydroxide or their complex are as Al 2O 36MgOCO 212H 2O, Mg 6Al 2(OH) 16CO 34H 2O, MgOAl 2O 32SiO 2NH 2O or similar compounds; Basic amino acid and their salt are as arginine, lysine, histidine and L-Tryptophan sodium.
Granulating or making in the process of piller, also can add proper amount of lubricating agent to reach specific pharmacy purpose.Used lubricant can be selected from micropowder silica gel, liquid paraffin; Stearic acid, magnesium stearate, calcium stearate, zinc stearate, glyceryl monostearate, Polyethylene Glycol, hydrogenated vegetable oil, sodium stearyl fumarate, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium laurylsulfate, magnesium laurylsulfate, Stepanol MG and Pulvis Talci etc., can use use also capable of being combined separately.
In the present invention, the facility for granulating that is adopted can be selected for use but be not limited only to fluid bed one-step-granulating method, centrifugal granulating coating machine, High Speed Stirring Machine, extrude-round as a ball comminutor and wave granulator.
In the present invention, the pill method that is adopted can be selected for use but be not limited only to celphere medicine-feeding method, extruding-round as a ball one-tenth ball method, spray drying method or congealing spray, preferably adopts celphere medicine-feeding method and extrudes-spheronization; The equipment that is adopted has coating pan (traditional and heavy duty detergent), fluid bed, centrifugal granulating coating machine and extrudes round as a ball comminutor.
2. directly carry out powder coating
In the present invention, also can adopt the powder coating technology.Can carry out powder coating separately to active substance, also can will carry out coating after active substance and other mixing acceptable accessories.These acceptable accessories with above-mentioned 1. granulate or the pill method in selected adjuvant scope identical.
In the method, the coating solution that is adopted mainly contains pharmaceutically acceptable macromolecule coating material, also can add plasticizer, antacid, pigment, color lake, antitack agent, antistatic agent as the case may be.Selected macromolecule coating material mainly is selected from Polyethylene Glycol, polyvinylpyrrolidone, polyvinyl alcohol, polyvinyl acetate, hydroxypropyl cellulose, methylcellulose, ethyl cellulose, hydroxypropyl emthylcellulose and sodium carboxymethyl cellulose etc., can select use also capable of being combined separately for use; The preferred cellulose family macromolecule material that uses is as hydroxypropyl cellulose, methylcellulose, ethyl cellulose, hydroxypropyl emthylcellulose.Above-mentioned coating material can be selected the organic solvent dissolving for use, also can select its corresponding aqueous dispersion form for use, and specifically adopting the sort of mode is not emphasis of the present invention.Selected antacid is identical with the scope of selected antacid in above-mentioned 1. granulation or the pill method.Selected antitack agent and antistatic agent mainly contain tristerin, dimethicone, silicone oil, methyl-silicone oil, Pulvis Talci, titanium dioxide (titanium dioxide), micropowder silica gel (silicon dioxide) and magnesium stearate etc., can use use also capable of being combined separately.In this step, selecting for use of plasticizer, pigment and color lake is not emphasis.
Can adopt suitable device to finish this processing step, preferably use fluid bed to carry out powder coating in the methods of the invention.
The second step parcel sealing coat (directly powder coating technology need not this step):
The main purpose of parcel sealing coat is to form the pH relief area between active matter and enteric coating, with the enteric-coating material of the acid crylic acid resin that prevents to use always the destruction to active matter.The composition of sealing coat and first step method 2. in the composition of coating solution identical, be not described in detail in this.
The available equipment of this step has granulating and coating machine, fluid bed or coating pan (traditional or heavy duty detergent); Preferred high-efficiency coating pot and the fluid bed of using more preferably adopts fluid bed.
The 3rd step enteric-coating layer:
Adopt suitable packaging technique that 2. first step method is wrapped up one or more layers enteric coating with second granule or the piller that goes on foot gained.Enteric coating material can be dissolved in the organic solvent, also can adopt the aqueous dispersion form.Enteric coating material can be selected from Lac, Cellacefate, HPMC-AS, poly-acetic acid O-phthalic vinyl acetate, acetic acid benzenetricarboxylic acid cellulose, carboxymethylethylcellulose, cellulose acetate phthalate ester (CAP), Hydroxypropyl Methylcellulose Phathalate (HPMCP), crylic acid resin (enteric solubility II number, enteric solubility III number, EudragitL series, EudragitS series, EudragitRL series, EudragitRS series, EudragitFS, EudragitNE) etc., can use use also capable of being combined separately.
In this enteric coating layer, it is necessary adding plasticizer, so that obtain the enteric coating layer of enough mechanical strengths.Selected plasticizer has but is not limited only to polyethylene glycols (PEG), diethyl phthalate (DEP), phthalic acid dibutyl ester (DBP), dibutyl sebacate (DBS), triethyl citrate (triethyl citrate, TEC), triglycerin acetate and Semen Ricini wet goods, preferably use polyethylene glycols and triethyl citrate.
According to selected enteric coating coating material and plasticizer, the content of described plasticizer in enteric coating must be optimized to obtain to have the enteric coating film of enough mechanical properties, and above-mentioned granule or the piller acid resistance after standing tablet forming technique is not significantly descended.The amount that plasticizer dosage accounts for enteric coated polymers generally is no less than 10%, and preferred amounts is 15%-50%, more preferably 20%-50%.
In enteric coating layer, also can add pigment, color lake, antitack agent, antistatic agent etc.Selected antitack agent and antistatic agent mainly contain silicone oil, methyl-silicone oil, Pulvis Talci, titanium dioxide (titanium dioxide), micropowder silica gel (silicon dioxide) and magnesium stearate etc., can use use also capable of being combined separately.In this step, selecting for use of plasticizer, pigment and color lake is not emphasis.
Enteric coating layer can be one deck, also can be multilamellar.The thickness of enteric coating layer is at least 10 μ m, is preferably greater than 20 μ m.In the present invention, selected enteric coating layer is characterised in that outermost enteric coating layer do not select the not good plasticizer of mouthfeel for use, as ETHYL CTTRATE etc.; So that final finished product has good mouthfeel.
As mentioned above, therefore some enteric coating can consider to wrap up one deck mouthfeel better protect layer because of the mouthfeel of indivedual coating materials or plasticizer etc. again outside enteric coating layer, and sealing coat is basic identical among selected coating material and the present invention, no longer repeats at this.In this protective layer, other adding ingredient is not an emphasis of the present invention.
The coating equipment that is adopted preferably uses high-efficiency coating pot and fluid bed.
The 4th step mixing of materials:
Filler, correctives, disintegrating agent and fluidizer are taken by weighing and mix homogeneously according to quantity, and the mixing of materials with above-mentioned gained makes evenly again, and adding lubricant mixing is standby.
In the present invention, it is characterized in that mannitol (granular or powdery), microcrystalline Cellulose, PROSOLV SMCC, polymerization sugar (EMDEX), coupling sugar, glucose, lactose, sucrose, dextrin and starch etc. that filler is selected from, can use separately, also can applied in any combination, consumption is generally (10-80) %.
98805424.8 pairs of water miscible sorbitol of Chinese patent, maltose alcohol, reduced form starch sugar, xylitol, reduced form BATANG, erythritol and hydroxypropyl content are that the application that the low-substituted hydroxypropyl cellulose of 7.0-9.0% (quality) is combined and used in the oral cavity disintegration tablet is protected, so one of feature of the present invention makes not relate to and uses these adjuvants.
In the present invention, it is characterized in that selected correctives includes but are not limited to mannitol, stevioside, lactose, fructose, sucrose, protein sugar, glycyrrhizin, Sodium Cyclamate, gelatin, aspartame, flavoring banana essence, flavoring pineapple essence, vanillin, fragrant citrus essence, flavoring orange essence, Herba Menthae essence, ginseng essence, strawberry essence, citric acid, citric acid etc., can use use also capable of being combined separately.
In the present invention, it is characterized in that selected disintegrating agent includes but are not limited to crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), cross-linking sodium carboxymethyl cellulose (CCNa) and soybean polysaccharide (EMCOSOY) etc., can use use also capable of being combined separately.
In the present invention, it is characterized in that selected fluidizer includes but are not limited to micropowder silica gel, Pulvis Talci, Cab-O-sil , Aerosil , hydrated sodium aluminosilicate etc., can use use also capable of being combined separately.
In the present invention, it is characterized in that selected lubricant includes but are not limited to stearic acid, magnesium stearate, calcium stearate, zinc stearate, glyceryl monostearate, Polyethylene Glycol, hydrogenated vegetable oil, sodium stearyl fumarate, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium laurylsulfate, magnesium laurylsulfate, Stepanol MG and Pulvis Talci etc., can use use also capable of being combined separately.
In the present invention, according to circumstances also can add the adjuvant effervescent.Effervescent can be selected from the mixture of malic acid, citric acid (citric acid) or tartaric acid and sodium bicarbonate or sodium carbonate.
The 5th step tabletting or lyophilization:
Above-mentioned material detects through intermediate, determine that sheet is heavy after, send into the tablet machine tabletting.It is characterized in that adopting direct compression process technology, the hardness of the tablet of acquisition is between 10 to 100 newton, and preferred tablet hardness is 15 to 45 newton, and disintegration time is at 1-60 in second.
Or above-mentioned prepared coating powder, granule or piller be suspended in the solution A of cellulose family macromolecule material; then gelatin, the pure and mild correctives of water-soluble sugar are mixed the back dissolving and form solution B; again with freezing in an amount of pure water dilution and the rearmounted mould of abundant mixing; again in the method freeze dryer lyophilizing to the material bone dry; press seal is used blister package.
Beneficial effect
Tablet is a kind of conventional dosage forms, because of its steady quality, dosage accurately, take, easy to carry, mechanization degree is high, low one of the at present the most frequently used dosage form that becomes of production cost, but because of the tablet extrusion forming, disintegrate is slow, bioavailability is lower, and part patient swallows comparatively difficult, thereby promoting the use of to a certain extent of tablet is restricted.The oral administration solid quick releasing formulation becomes a focus, particularly oral cavity disintegration tablet of new drug development in recent years for this reason, because of its taking convenience, rapid-action, bioavailability is high, the good emphasis that becomes tablet exploitation of mouthfeel.
Oral cavity disintegration tablet is meant not to be needed water or only needs low amounts of water, need not to chew, and tablet places lingual surface, disintegrate rapidly after the chance saliva, or borrow and swallow power, medicine can be gone into the tablet of stomach onset.The characteristics of oral cavity disintegration tablet are that absorption is fast, bioavailability is high, and intestinal is residual few, and side effect is low, avoids liver first-pass effect etc.
According to the requirement of " formulation characteristic of oral cavity disintegration tablet and quality control meeting summary ", oral cavity disintegration tablet has essential leap than the disintegration rate of drop pill and ordinary tablet, and the disintegrate of oral cavity disintegration tablet generally in 30 seconds, is no more than 1 minute at most.
Specific embodiment
The preparation method of omeprazole of the present invention and derivative oral disintegrating tablet thereof is described by following embodiment; For embodiment be for the present invention is described better, rather than limit the invention.
Embodiment one
One. prescription
Supplementary material title consumption (g)
Core layer magnesium omeprazole 200.00
Magnesium hydroxide 50.00
Lactose 50.00
Powder coating layer hydroxypropyl emthylcellulose 30.00
Sodium lauryl sulphate 3.00
Pulvis Talci 6.00
50% alcoholic solution 561.00
Add up to 600.00
Protectiveness coatings hydroxypropyl emthylcellulose 33.90
Mannitol 20.00
Dimethicone Emulsion (dry measure) 2.00
Pure water 622.10
Add up to 678.00
Enteric layer Eudragit L100-55 552.86
Triethyl citrate 71.08
Pulvis Talci 12.47
95% alcoholic solution 2363.59
Add up to 3000.00
External protection hydroxypropyl cellulose 32.22
Stearoyl polyglycerin ester 3.00
Mannitol 120.47
Pure water 544.31
Add up to 700.00
The above-mentioned coating powder 800.00 of tablet
Mannitol 970.00
Methylcellulose 160.00
Gelatin 50.00
Stevioside 20.00
Be pressed into 10000 altogether, amount to 2000.00
Two. preparation method
1) get the hydroxypropyl emthylcellulose of powder coating layer, the dissolve with ethanol solution with 50%, sodium lauryl sulphate, sodium hydroxide and Pulvis Talci adding recipe quantity stir, and be standby;
2) omeprazole is put fluidisation in the fluid bed, sprayed into above-mentioned material then;
The hydroxypropyl emthylcellulose of 3) fetch protection coatings, pure water dissolving adds mannitol and dimethicone again, stirs, and treats step 2) continue to spray into the coating solution that this step is prepared after spray;
4) get the Eudragit of enteric layer L30D-55, triethyl citrate and Pulvis Talci are prepared with pure water, stir, and treat to continue after step 3) has been sprayed to spray into the coating solution of this step preparation;
5) get the Eudragit of external protection L30D-55, PEG6000, stearoyl polyglycerin ester and mannitol are prepared with pure water, stir, and treat to continue after step 4) has been sprayed to spray into the coating solution of this step preparation;
6) dry (dry in fluid bed or the baking oven), temperature is controlled at below 50 ℃;
7) methylcellulose is suspended in above-mentioned coating powder wherein with after the suitable quantity of water dissolving, mannitol, gelatin and stevioside is soluble in water, mix with aforementioned suspension then, put lyophilizing in the mould then, press seal is used blister package, promptly.
Embodiment two
One. prescription
Supplementary material title consumption (g)
Core layer omeprazole 200.00
Magnesium hydroxide 70.00
Microcrystalline Cellulose 75.00
Lactose 45.00
Hydroxypropyl emthylcellulose 8.00
Sodium lauryl sulphate 2.00
Pure water Q.S.
Add up to 400.00
Sealing coat hydroxypropyl emthylcellulose 40.00
Dimethicone Emulsion (dry measure) 2.00
Pulvis Talci 2.00
Pure water 756.00
Add up to 800.00
Enteric layer Eudragit L30D-55 (dry measure) 87.02
Eudragit NE30D (dry measure) 21.76
Triethyl citrate 46.42
Pulvis Talci 7.77
95% alcoholic solution 1837.03
Add up to 2000.00
External protection hydroxypropyl cellulose 30.35
Stearoyl polyglycerin ester 3.00
Mannitol 159.68
Pure water 1406.97
Add up to 1600.00
The above-mentioned coated pill core 800.00 of tablet
Mannitol 1130.00
Microcrystalline Cellulose 250.00
Stevioside 20.00
Crospolyvinylpyrrolidone 150.00
Low-substituted hydroxypropyl cellulose 100.00
Micropowder silica gel 25.00
Sodium stearyl fumarate 25.00
Be pressed into 10000 altogether, amount to 2500.00
Two. preparation method
1) sodium lauryl sulphate of getting recipe quantity in the core layer is with an amount of pure water dissolving, and is standby;
2) get omeprazole, magnesium hydroxide, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose and the hydroxypropyl emthylcellulose of recipe quantity in the core layer, put fully to stir in the high-speed stirring mixer and make mix homogeneously;
3) solution with step 1) adds step 2) in, high-speed stirred is mixed cutting and is granulated;
4) material of step 3) is put in the extruder, crossed the screen cloth of 0.5 mm dia;
5) material of step 4) is put in the spheronizator round as a ball, become piller;
6) piller of step 5) is put 50 ℃ of drying under reduced pressure in the baking oven, standby;
7) press the coating solution of the prescription preparation sealing coat of sealing coat, standby;
8) piller of step 6) is put be preheated to 35 ℃ in the high-efficiency coating pot, spray into the sealing coat coating solution then;
9) press the coating solution of the prescription preparation enteric layer of enteric layer, treat to continue to spray into the enteric layer coating solution after step 8) has been sprayed;
10) press the coating solution of the prescription preparation external protection of external protection, treat to continue to spray into the external protection coating solution after step 9) has been sprayed;
11) treat that step 10) sprays into the after drying 12 hours of finishing, temperature is controlled at below 45 ℃;
12) get the additive of tablet and the above-mentioned coated pellets mix homogeneously of recipe quantity, after intermediate detects, determine that sheet is heavy, tabletting, the slice, thin piece Hardness Control is in 15～55 newton, promptly.
Embodiment three
One. prescription
Layer title supplementary material title consumption (g)
Ball core sugar ball ball core (80 order) 100.00
Medicine layer Omeprazole Sodium 200.00
Arginine 10.00
Hydroxypropyl cellulose 50.00
Pure water 440.00
Add up to 700.00
Sealing coat hydroxypropyl emthylcellulose 36.00
Pulvis Talci 1.85
Magnesium stearate 0.15
Pure water 682.00
Add up to 720.00
Enteric layer Eudragit L100-55 78.01
Eudragit NE30D (dry weight) 19.50
Triethyl citrate 41.79
Pulvis Talci 7.33
95% alcoholic solution 1843.37
Add up to 1990.00
External protection hydroxypropyl emthylcellulose 49.02
PEG6000 5.45
Dimethicone Emulsion (dry measure) 1.20
Mannitol 159.71
Pure water 1084.63
Add up to 1300.00
The above-mentioned coated pill core 760.00 of tablet
Mannitol 1539.00
Microcrystalline Cellulose 300.00
Aspartame 21.00
Liquorice essence 20.00
Crospolyvinylpyrrolidone 150.00
Cross-linking sodium carboxymethyl cellulose 150.00
Micropowder silica gel 30.00
Sodium stearyl fumarate 30.00
Be pressed into 10000 altogether, amount to 3000.00
Two. preparation method
1) press medicine layer prescription preparation coating solution, standby;
2) sugared ball ball core is put fluidisation in the fluid bed, spray into the material of step 1) then;
3) press the coating solution of the prescription preparation sealing coat of sealing coat, treat step 2) continue to spray into the sealing coat coating solution after having sprayed;
4) press the coating solution of the prescription preparation enteric layer of enteric layer, treat to continue to spray into the enteric layer coating solution after step 3) has been sprayed;
5) press the coating solution of the prescription preparation external protection of external protection, treat to continue to spray into the external protection coating solution after step 4) has been sprayed;
6) treating that step 5) sprays into carries out drying (dry in fluid bed or the baking oven) after finishing, and temperature is controlled at below 50 ℃;
7) get the additive of tablet and the above-mentioned coated pellets mix homogeneously of recipe quantity, after intermediate detects, determine that sheet is heavy, tabletting, the slice, thin piece Hardness Control is in 15～55 newton, promptly.
Embodiment four
One. prescription
Supplementary material title consumption (g)
Ball core sugar ball ball core (60 order) 100.00
Medicine layer (-)-omeprazole 200.00
Arginine 40.00
Sodium lauryl sulphate 10.00
Hydroxypropyl cellulose 50.00
Pure water 600.00
Add up to 900.00
Sealing coat hydroxypropyl emthylcellulose 40.00
Pulvis Talci 1.85
Magnesium stearate 0.15
Pure water 758.00
Add up to 800.00
Enteric layer HPMC-AS 204.00
Triethyl citrate 61.20
Pulvis Talci 13.96
70% alcoholic solution 1930.84
Add up to 2210.00
External protection hydroxypropyl emthylcellulose 36.06
Dimethicone Emulsion (dry measure) 1.20
Mannitol 141.58
Pure water 521.16
Add up to 700.00
The above-mentioned coated pill core 900.00 of tablet
Mannitol 1419.00
Microcrystalline Cellulose 280.00
Aspartame 21.00
Strawberry essence 20.00
Crospolyvinylpyrrolidone 300.00
Micropowder silica gel 30.00
Sodium stearyl fumarate 30.00
Be pressed into 10000 altogether, amount to 3000.00
Two. preparation method
1) press medicine layer prescription preparation coating solution, standby;
2) sugared ball ball core is put fluidisation in the fluid bed, spray into the material of step 1) then;
3) press the coating solution of the prescription preparation sealing coat of sealing coat, treat step 2) continue to spray into the sealing coat coating solution after having sprayed;
4) press the coating solution of the prescription preparation enteric layer of enteric layer, treat to continue to spray into the enteric layer coating solution after step 3) has been sprayed;
5) press the coating solution of the prescription preparation external protection of external protection, treat to continue to spray into the external protection coating solution after step 4) has been sprayed;
6) treating that step 5) sprays into carries out drying after finishing, and product temperature is controlled at 45 ℃ to below 50 ℃;
7) get the additive of tablet and the above-mentioned coated pellets mix homogeneously of recipe quantity, after intermediate detects, determine that sheet is heavy, tabletting, the slice, thin piece Hardness Control is in 15～55 newton, promptly.
Embodiment five
One. prescription
Layer title supplementary material title consumption (g)
Ball core sugar ball ball core (80 order) 100.00
Medicine layer (-)-magnesium omeprazole 200.00
Arginine 10.00
Hydroxypropyl cellulose 50.00
Pure water 440.00
Add up to 700.00
Sealing coat hydroxypropyl emthylcellulose 38.00
Pulvis Talci 1.85
Magnesium stearate 0.15
Pure water 662.00
Add up to 702.00
Enteric layer Eudragit L30D-55 (dry weight) 89.60
Eudragit NE30D (dry weight) 22.40
Triethyl citrate 48.00
Titanium dioxide 20.00
Pure water 1820.00
Add up to 2000.00
External protection hydroxypropyl emthylcellulose 29.00
Mannitol 121.D0
Pure water 600.00
Add up to 750.00
The above-mentioned coated pill core 730.00 of tablet
Mannitol 1180.00
Microcrystalline Cellulose 250.00
Aspartame 20.00
Fructus Citri Limoniae essence 20.00
Crospolyvinylpyrrolidone 100.00
Cross-linking sodium carboxymethyl cellulose 150.00
Micropowder silica gel 25.00
Magnesium stearate 25.00
Be pressed into 10000 altogether, amount to 2500.00
Two. preparation method
1) press medicine layer prescription preparation coating solution, standby;
2) sugared ball ball core is put fluidisation in the fluid bed, spray into the material of step 1) then;
3) press the coating solution of the prescription preparation sealing coat of sealing coat, treat step 2) continue to spray into the sealing coat coating solution after having sprayed;
4) press the coating solution of the prescription preparation enteric layer of enteric layer, treat to continue to spray into the enteric layer coating solution after step 3) has been sprayed;
5) press the coating solution of the prescription preparation external protection of external protection, treat to continue to spray into the external protection coating solution after step 4) has been sprayed;
6) treating that step 5) sprays into carries out drying after finishing, and product temperature is controlled at 45 ℃ to below 50 ℃;
7) get the additive of tablet and the above-mentioned coated pellets mix homogeneously of recipe quantity, after intermediate detects, determine that sheet is heavy, tabletting, the slice, thin piece Hardness Control is in 15～55 newton, promptly.
Embodiment six
One. prescription
Supplementary material title consumption (g)
Core layer omeprazole 200.00
Magnesium hydroxide 50.00
Lactose 50.00
Powder coating layer hydroxypropyl emthylcellulose 30.00
Sodium lauryl sulphate 3.00
Pulvis Talci 6.00
50% alcoholic solution 561.00
Add up to 600.00
Protectiveness coatings hydroxypropyl emthylcellulose 33.90
Mannitol 20.00
Dimethicone Emulsion (dry measure) 2.00
Pure water 622.10
Add up to 678.00
Enteric layer Eudragit L100-55 552.86
Triethyl citrate 71.08
Pulvis Talci 12.47
95% alcoholic solution 2363.59
Add up to 3000.00
External protection hydroxypropyl cellulose 32.22
Stearoyl polyglycerin ester 3.00
Mannitol 120.47
Pure water 544.31
Add up to 700.00
The above-mentioned coating powder 800.00 of tablet
Mannitol 1130.00
Microcrystalline Cellulose 250.00
Aspartame 20.00
Crospolyvinylpyrrolidone 150.00
Carboxymethyl starch sodium 100.00
Micropowder silica gel 25.00
Sodium stearyl fumarate 25.00
Be pressed into 10000 altogether, amount to 2500.00
Two. preparation method
1) press the preparation coating solution of powder coating layer, standby;
2) with fluidisation in the rearmounted fluid bed of the abundant mixing of the powder of core layer, spray into above-mentioned material then;
3) by the prescription of protectiveness coatings preparation coating solution, treat step 2) continue to spray into the coating solution that this step is prepared after spray;
4) prescription of pressing enteric layer is prepared coating solution, treats to continue after step 3) has been sprayed to spray into the coating solution of this step preparation;
5) prescription of pressing external protection is prepared coating solution, treats to continue after step 4) has been sprayed to spray into the coating solution of this step preparation;
6) drying, product temperature are controlled at below 50 ℃;
7) get the additive of tablet and the above-mentioned coating powder mix homogeneously of recipe quantity, after intermediate detects, determine that sheet is heavy, tabletting, the slice, thin piece Hardness Control is in 15～55 newton, promptly.
Embodiment seven
One. prescription
Supplementary material title consumption (g)
Ball core microcrystalline Cellulose ball core (80 order) 100.00
Medicine layer (-)-omeprazole 200.00
Arginine 40.00
Sodium lauryl sulphate 10.00
Hydroxypropyl cellulose 50.00
Pure water Q.S.
Add up to
Sealing coat hydroxypropyl emthylcellulose 40.00
Pulvis Talci 1.85
Magnesium stearate 0.15
Pure water 758.00
Add up to 800.00
Enteric layer Eudragit L30D-55 (dry weight) 74.26
Eudragit NE30D (dry weight) 18.56
Triethyl citrate 39.78
Pulvis Talci 6.60
Pure water 1860.80
Add up to 2000.00
External protection Eudragit L30D-55 (dry weight) 32.54
Eudragit NE30D (dry weight) 8.14
PEG6000 17.44
Dimethicone Emulsion (dry measure) 1.20
Mannitol 159.48
Pure water 1281.20
Add up to 1500.00
The above-mentioned coated pill core 800.00 of tablet
Mannitol 1519.00
Microcrystalline Cellulose 300.00
Aspartame 21.00
Cross-linking sodium carboxymethyl cellulose 150.00
Carboxymethyl starch sodium 150.00
Micropowder silica gel 30.00
Sodium stearyl fumarate 30.00
Be pressed into 10000 altogether, amount to 3000.00
Two. preparation method
1) press the preparating liquid of medicine layer, standby;
2) microcrystalline Cellulose ball core (80 order) is put in the centrifugal granulating coating machine, sprayed into above-mentioned material then;
3) press the prescription preparation coating solution of sealing coat, treat step 2) spray after with step 2) the piller transfer put in the fluid bed, continue to spray into the coating solution that this step is prepared;
4) prescription of pressing enteric layer is prepared coating solution, treats to continue after step 3) has been sprayed to spray into the coating solution of this step preparation;
5) prescription of pressing external protection is prepared coating solution, treats to continue after step 4) has been sprayed to spray into the coating solution of this step preparation;
6) drying, product temperature are controlled at below 50 ℃;
7) get the additive of tablet and the above-mentioned coating powder mix homogeneously of recipe quantity, after intermediate detects, determine that sheet is heavy, tabletting, the slice, thin piece Hardness Control is in 15～55 newton, promptly.
Embodiment eight
One. prescription
Supplementary material title consumption (g)
Core layer (-)-magnesium omeprazole 400.00
Microcrystalline Cellulose 85.00
Carboxymethyl starch sodium P5000 13.00
Sodium lauryl sulphate 2.00
Pure water Q.S.
Add up to 500.00
Sealing coat hydroxypropyl emthylcellulose 50.00
Methyl-silicone oil 2.50
Pulvis Talci 2.50
Pure water 745.00
Add up to 800.00
Enteric layer Eudragit L100-55 108.78
Eudragit NE30D (dry measure) 46.62
Triethyl citrate 66.60
Pulvis Talci 10.22
95% alcoholic solution 2267.78
Add up to 2500.00
External protection hydroxypropyl emthylcellulose 50.00
Stearoyl polyglycerin ester 3.00
Mannitol 159.78
Pure water 887.22
Add up to 1100.00
The above-mentioned coated pill core 1000.00 of tablet
Mannitol 1320.00
Microcrystalline Cellulose 300.00
Aspartame 20.00
Crospolyvinylpyrrolidone 200.00
Low-substituted hydroxypropyl cellulose 100.00
Micropowder silica gel 30.00
Sodium stearyl fumarate 30.00
Be pressed into 10000 altogether, amount to 3000.00
Two. preparation method
1) sodium lauryl sulphate of getting recipe quantity in the core layer is with an amount of pure water dissolving, and is standby;
2) get (-)-magnesium omeprazole, microcrystalline Cellulose and the carboxymethyl starch sodium P5000 of recipe quantity in the core layer, put fully to stir in the high-speed stirring mixer and make mix homogeneously;
3) solution with step 1) adds step 2) in, high-speed stirred is mixed cutting and is granulated;
4) material of step 3) is put in the extruder, crossed the screen cloth of 0.5 mm dia;
5) material of step 4) is put in the spheronizator round as a ball, become piller;
6) piller of step 5) is put 50 ℃ of drying under reduced pressure in the baking oven, standby;
7) press the coating solution of the prescription preparation sealing coat of sealing coat, standby;
8) piller of step 6) is put be preheated to 35 ℃ in the high-efficiency coating pot, spray into the sealing coat coating solution then;
9) press the coating solution of the prescription preparation enteric layer of enteric layer, treat to continue to spray into the enteric layer coating solution after step 8) has been sprayed;
10) press the coating solution of the prescription preparation external protection of external protection, treat to continue to spray into the external protection coating solution after step 9) has been sprayed;
11) treat that step 10) sprays into the after drying 12 hours of finishing, temperature is controlled at below 45 ℃;
12) get the additive of tablet and the above-mentioned coated pellets mix homogeneously of recipe quantity, after intermediate detects, determine that sheet is heavy, tabletting, the slice, thin piece Hardness Control is in 15～55 newton, promptly.
Embodiment nine
One. prescription
Supplementary material title consumption (g)
Ball core silicon dioxide ball core (80 order) 100.00
Medicine layer magnesium omeprazole 200.00
Low-substituted hydroxypropyl cellulose 50.00
Hydroxypropyl cellulose 50.00
Pure water Q.S.
Add up to
Sealing coat hydroxypropyl emthylcellulose 38.00
Pulvis Talci 1.00
Dimethicone Emulsion (dry measure) 1.00
Pure water 760.00
Add up to 800.00
Enteric layer Eudragit L100-55 98.56
Eudragit NE30D (dry weight) 24.64
PEG6000 52.80
Pulvis Talci 9.26
95% alcoholic solution 2314.74
Add up to 2500.00
The above-mentioned coated pill core 625.26 of tablet
Mannitol 1230.74
Microcrystalline Cellulose 300.00
Aspartame 20.00
Flavoring banana essence 24.00
Crospolyvinylpyrrolidone 125.00
Low-substituted hydroxypropyl cellulose 125.00
Micropowder silica gel 25.00
Sodium stearyl fumarate 25.00
Be pressed into 10000 altogether, amount to 2500.00
Two. preparation method
1) press the preparating liquid of medicine layer, standby;
2) silicon dioxide ball core (80 order) is put in the centrifugal granulating coating machine, sprayed into above-mentioned material then;
3) press the prescription preparation coating solution of sealing coat, treat step 2) spray after with step 2) the piller transfer put in the fluid bed, continue to spray into the coating solution that this step is prepared;
4) prescription of pressing enteric layer is prepared coating solution, treats to continue after step 3) has been sprayed to spray into the coating solution of this step preparation;
5) drying, product temperature are controlled at below 50 ℃;
6) get the additive of tablet and the above-mentioned coating powder mix homogeneously of recipe quantity, after intermediate detects, determine that sheet is heavy, tabletting, the slice, thin piece Hardness Control is in 15～55 newton, promptly.
Enteric-coated pellets sees Table 1 with the acid resistance experimental result of the tablet that is pressed into.
Table 1
Embodiment Piller acid resistance (%) The acid resistance of tablet (%)
1 93 93
2 99 96
3 96 94
4 91 90
5 97 94
6 93 91
7 99 97
8 96 95
9 98 94
Annotate: the acid resistance experiment is to carry out according to the method for 2000 editions defineds of Chinese Pharmacopoeia.

Claims (20)

1 one kinds of omeprazole oral cavity disintegration tablets, it is characterized in that: after omeprazole process powder coating or the granule coating, be pressed into oral cavity disintegration tablet with filler, correctives, disintegrating agent, fluidizer, lubricant, wherein each components by weight is that omeprazole coating powder or coated pill core 1～50%, disintegrating agent 2～35%, filler 10-80%, correctives 1～40%, fluidizer 0.01～5%, lubricant 0.3～3% are formed.
2 omeprazole oral cavity disintegration tablets as claimed in claim 1, wherein omeprazole wraps with sealing coat, enteric layer more successively with after pharmaceutically acceptable carrier carries out powder coating, makes omeprazole coating powder.
3 omeprazole oral cavity disintegration tablets as claimed in claim 1 after wherein omeprazole and pharmaceutically acceptable carrier are made granule, carry out granule coating, wrap successively with sealing coat, enteric layer again, make the omeprazole coated granule.
4 as claim 2 or 3 described omeprazole oral cavity disintegration tablets, wherein also can be at other protective layer of enteric layer outer coatings.
5 as the described omeprazole oral cavity disintegration tablet of claim 1-4, and wherein omeprazole is selected from omeprazole pharmaceutically acceptable salt, hydrate, optical isomer, pharmaceutically acceptable crystal formation and their mixture.
The 6 omeprazole oral cavity disintegration tablets any as claim 1-5, wherein filler is selected from one or more in mannitol, microcrystalline Cellulose, dextrin, lactose, starch, maltodextrin and the pregelatinized Starch.
7 omeprazole oral cavity disintegration tablets as claimed in claim 6, wherein filler is that mannitol closes/or microcrystalline Cellulose.
The 8 omeprazole oral cavity disintegration tablets any as claim 1-5, wherein correctives is selected from one or more in mannitol, lactose, stevioside, gelatin, aspartame, cyclamate, glycyrrhizin, fragrant citrus essence, flavoring orange essence, Herba Menthae essence, ginseng essence, strawberry essence, citric acid, the citric acid.
9 omeprazole oral cavity disintegration tablets as claimed in claim 8, wherein correctives is an aspartame.
The 10 omeprazole oral cavity disintegration tablets any as claim 1-5, wherein lubricant is selected from one or more in magnesium stearate, glyceryl monostearate, Stepanol MG, the Pulvis Talci, in the sodium stearyl fumarate.
The 11 omeprazole oral cavity disintegration tablets as claim 10, wherein lubricant is a sodium stearyl fumarate.
The 12 omeprazole oral cavity disintegration tablets any as claim 1-5, wherein fluidizer is selected from one or more in micropowder silica gel, Pulvis Talci, Cab-O-sil, Arosil, the hydrated sodium aluminosilicate.
The 13 omeprazole oral cavity disintegration tablets as claim 12, wherein fluidizer is micropowder silica gel.
The 14 omeprazole oral cavity disintegration tablets any as claim 1-14, wherein disintegrating agent is selected from one or more in crospolyvinylpyrrolidone, carboxymethyl starch sodium, low-substituted hydroxypropyl methylcellulose, cross-linking sodium carboxymethyl cellulose and the soybean polysaccharide.
The 15 omeprazole oral cavity disintegration tablets as claim 14, wherein disintegrating agent is selected from crospolyvinylpyrrolidone and/or carboxymethyl starch sodium and/or cross-linking sodium carboxymethyl cellulose.
The 16 omeprazole oral cavity disintegration tablets as claim 1-15, wherein the coating material of the granule coating of omeprazole or powder coating use is selected from one or more in Polyethylene Glycol, polyvinyl alcohol, polyvinyl acetate, polyvinylpyrrolidone, methylcellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxy methocel, the polyacrylic resin.
The 17 omeprazole oral cavity disintegration tablets as claim 17, wherein the coating material of the granule coating of omeprazole or powder coating use is a polyacrylic resin.
18 preparation methoies as any one the omeprazole oral cavity disintegration tablet of claim 1-17 is characterized in that being made up of following steps:
The first step is carried out powder coating or granule coating with omeprazole and proper supplementary material; Second step took by weighing correctives and Carthamus yellow granule or the feed particles after first step taste masking processing according to quantity, and mix homogeneously is standby;
The 3rd step took by weighing filler, disintegrating agent, fluidizer and mix homogeneously according to quantity, made evenly again with through second mixing of materials that goes on foot gained, added the lubricant mixing, and is standby;
The 4th step gained material detects through intermediate, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
19 as any one the omeprazole oral cavity disintegration tablet of claim 1-17 in as the treatment humans and animals with the medicine of the relevant disease of gastroxia in purposes.
20 purposes as claimed in claim 19, wherein disease is stomach and/or duodenal ulcer.
CN 200510002276 2005-01-20 2005-01-20 Disintegration piece of omeprazole and ramification taken through oral cavity and jpreparing technique Expired - Fee Related CN1263450C (en)

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CN103143025A (en) * 2013-04-07 2013-06-12 贵州圣济堂制药有限公司 Water-soluble enteric coating powder as well as preparation method and use method thereof
CN104546737A (en) * 2015-01-08 2015-04-29 浙江长典医药有限公司 Pellet type omeprazole enteric capsule and preparation method thereof
CN104586804B (en) * 2015-02-13 2017-06-23 沙莎 A kind of preparation method of the Letrozole piece of good stability
EP3277267B1 (en) * 2015-03-31 2021-01-06 Laboratorios Bagó S.A. Enteric-coated pellets containing a proton pump inhibitor
CN107913255A (en) * 2016-10-10 2018-04-17 北京阜康仁生物制药科技有限公司 A kind of tablet containing Omeprazole and preparation method thereof
JP7064683B2 (en) * 2017-01-27 2022-05-11 日本ケミファ株式会社 Composition for preventing damage to the enteric layer
CN109125282B (en) * 2018-09-05 2020-07-14 珠海润都制药股份有限公司 Omeprazole enteric capsule and preparation method thereof

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Granted publication date: 20060712