CN101134033A - Famotidine oral cavity disintegrating lyophilized tablets and method for preparing the same - Google Patents
Famotidine oral cavity disintegrating lyophilized tablets and method for preparing the same Download PDFInfo
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- CN101134033A CN101134033A CNA2006101519158A CN200610151915A CN101134033A CN 101134033 A CN101134033 A CN 101134033A CN A2006101519158 A CNA2006101519158 A CN A2006101519158A CN 200610151915 A CN200610151915 A CN 200610151915A CN 101134033 A CN101134033 A CN 101134033A
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- famotidine
- oral cavity
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- lyophilized tablets
- cavity disintegrating
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Abstract
The present invention relates to one kind of antiacid and antiulcer medicine capable of being disintegrated and absorbed fast in oral cavity. The antiacid and antiulcer medicine is oral disintegrated tablet is prepared with famotidine as main medicine component, and through preparing solution while adding proper amount of stuffing, adhesive and corrective, freeze drying and tabletting. The antiacid and antiulcer medicine has the advantages of no need of water for taking, fast disintegrating within 30 sec in oral cavity and fast acting.
Description
[technical field]
The present invention relates to a kind of can be in the oral cavity antacid and the Mucosta of disintegrate and absorption rapidly, mainly be principal agent with the famotidine, add suitable filler, binding agent and correctives and make solution, make oral cavity disintegration tablet after the lyophilization.The invention still further relates to the preparation method of famotidine oral cavity disintegrating lyophilized tablets.
[background technology]
Digestive system disease is one of at present common frequently-occurring disease, according to statistics, and the average attack rate 11.43% of China, and big city sickness rate such as Shanghai are higher, reach about 30%, second of morbidity in the majority.In digestive system disease, the sickness rate of Peptic Ulcers is higher, has accounted for significant proportion.In China, the peptic ulcer prevalence still reaches more than 1 ‰ at present.In addition, age of onset that in recent years should disease is rising.Show that according to the Zhongshan affiliated hospital of shanghai medical university statistics nineties in 20th century, old man's peptic ulcer patient number ratio rose before 30 years one times more than 60 years old.For the domestic market that begins to enter aged society, person in middle and old age group of people at high risk supports constantly one of basis of development, digestive ulcer medicament market.
At present in the antiulcer medicine, based on bisfentidine and proton pump inhibitor two big verieties.The proton pump inhibitor medicine is representative with the omeprazole, and bisfentidine is representative at present with the famotidine.Famotidine all has curative effect preferably to gastric and duodenal ulcers, reflux esophagitis, upper gastrointestinal hemorrhage, a tall and erect Chinese mugwort syndrome etc.Compare with like product, its action intensity is than the big 30-100 of cimetidine times, than the big 6-10 of ranitidine doubly.Be about 30% than cimetidine and ranitidine action time.Oral 20mg famotidine can be kept more than 12 hours the inhibitory action of gastric acid secretion amount.Quiet injection famotidine 20mg, hemostatic efficiency reaches 91%.In addition, the famotidine untoward reaction is less, can not change gastric emptying rate, does not disturb pancreatic function, and the cardiovascular system renal function of unifying is also had no adverse effects.
According to prescription that provides in the national drug standards and preparation technology, the famotidine sheet is the histamine H2-receptor blocade.Gastric acid secretion is had the obvious suppression effect, also can suppress pepsic secretion, the zoopery ulcer is had certain protective role.
Famotidine sheet English name: Famotidine Tablets
This product contains famotidine (C8H15N7O2S3) and should be 90.0%～110.0% of labelled amount.
[character] this product is white tablets, coated tablet or Film coated tablets, remove sugar-coat or film-coat after, whitening color or off-white color.
The solution under the uniformity of dosage units item is got in [discriminating] (1), measures according to spectrophotography (appendix IV A), at 265nm ± 2nm wavelength place absorption maximum is arranged.
(2) in the chromatogram that writes down under the assay item, the retention time at test sample peak should be consistent with the retention time at famotidine reference substance peak.
[inspection] uniformity of dosage units is got 1 of this product (10mg specification), puts in the 100ml measuring bottle, adds the PH4.5 potassium phosphate buffer and (gets potassium dihydrogen phosphate 13.6g, add the suitable quantity of water dissolving and be diluted to 1000ml, shake up, regulate PH4.5) 40ml, jolting makes dissolving, be diluted to scale with the PH4.5 potassium phosphate buffer, shake up, filter, it is an amount of that precision is measured subsequent filtrate, add the quantitative dilution of PH4.5 potassium phosphate buffer and make the solution that contains famotidine 10 μ g among every 1ml, as need testing solution; Other precision takes by weighing through 4 hours famotidine reference substance of 80 ℃ of C drying under reduced pressure of phosphorus pentoxide an amount of, adds the dissolving of PH4.5 potassium phosphate buffer, and quantitatively the solution that contains 10 μ g among every 1ml, product solution are in contrast made in dilution.Get above-mentioned two kinds of solution, measure trap at the wavelength place of 265nm ± 2nm and calculate content according to spectrophotography (appendix IVA), should (appendix XE) up to specification.
Dissolution is got this product, according to dissolution method (appendix XC first method), with PH4.5 potassium phosphate buffer 900ml is solvent, and rotating speed is that per minute 100 changes, operation in accordance with the law, in the time of 30 minutes, get solution 10ml, filter, it is an amount of that precision is measured subsequent filtrate, make the solution that contains 10 μ g among every 1ml with the homogeneous solvent dilution, as need testing solution.Measure according to the method under the uniformity of dosage units item, calculate every stripping quantity.Limit is 80% of a labelled amount, should be up to specification.
Other should meet every regulation relevant under the tablet item (appendix IA).
[assay] measured according to high performance liquid chromatography (appendix VD).
Chromatographic condition and system suitability test are filler with octadecylsilane chemically bonded silica, (get sodium heptanesulfonate 2.0g with the heptanesulfonic acid sodium solution, after adding water 900ml dissolving, regulate pH value to 3.9, add water to 1000ml with glacial acetic acid)-acetonitrile-methanol (25: 6: 1) is mobile phase; The detection wavelength is 254nm.Number of theoretical plate calculates by the famotidine peak should be not less than 1400.Algoscopy is got 20 of this product, and accurate the title decided porphyrize, precision takes by weighing in right amount (being equivalent to famotidine 50mg approximately), puts in the 50ml measuring bottle, and it is an amount of to add methanol, jolting makes the famotidine dissolving, and is diluted to scale with methanol, shakes up, filter, precision is measured subsequent filtrate 5ml, puts in the 50ml measuring bottle, is diluted to scale with mobile phase, shake up, as need testing solution; 4 hours the famotidine reference substance 50ml of 80 ℃ of phosphorus pentoxides decompression that learn from else's experience accurately claim surely, put in the 50ml measuring bottle, add methanol and dissolve in right amount and be diluted to scale, shake up, precision is measured 5ml, puts in the 50ml measuring bottle, be diluted to scale with mobile phase, shake up, in contrast product solution.Precision is measured each 20 μ l of above-mentioned two kinds of solution, injects chromatograph of liquid respectively, the record chromatogram.Press external standard method with calculated by peak area, promptly.
[classification] same famotidine.
[specification] (1) 10mg (2) 20mg
[storage] shading, sealing is preserved.
The same veriety of present domestic listing has famotidine conventional tablet, granule, injection, capsule, dispersible tablet.Oral cavity disintegrating lyophilized tablets is the open network structure substrate that is loaded with medicine, can be in a spot of water disintegrate and homodisperse rapidly, thereby improve the dissolution rate and the bioavailability of medicine, more effective performance therapeutical effect and avoid the excessive concentration of topical remedy and reduce the generation of untoward reaction also makes gerontal patient, dysphagia patients and taking medicine in water-stressed conditions become more convenient simultaneously.
[summary of the invention]
The objective of the invention is to remedy the deficiencies in the prior art, to extensive patients and medical personnel provide a kind of can be in the oral cavity antacid and the Mucosta of disintegrate and absorption rapidly, it mainly is principal agent with the famotidine, add suitable filler, binding agent and correctives and make solution, make oral cavity disintegration tablet after the lyophilization.The invention still further relates to the preparation method of famotidine oral cavity disintegrating lyophilized tablets.Take following preparation method can make famotidine oral cavity disintegrating lyophilized tablets involved in the present invention.
[preparation method]
1. obtain solution: famotidine and solubilizing agent is soluble in water, form solution A; Filler, correctives, binding agent are added the water mixed dissolution, form solution B; Solution A and solution B are mixed, and add the suitable quantity of water dilution, fully stir.
2. freeze: above-mentioned mixed solution is put into the mould of required specification, put into fridge quick freezing under-20 ℃～-30 ℃ temperature then.
3. sublimation drying: the charging mould that will freeze is put into freezer dryer, distils under the vacuum and low temperature condition, removes moisture.
4. press mold is packed: with the tablet press mold packing that obtains after the lyophilizing.
[beneficial effect]
Famotidine is the 3rd generation H2-receptor antagonist, and its gastric acid inhibitory secretion capacity is strong 7.5 times than ranitidine, and strong 40 times than cimetidine, be about 30% than cimetidine and ranitidine action time.Famotidine all has the same veriety of the present domestic listing of curative effect preferably that the famotidine conventional tablet is arranged to gastric and duodenal ulcers, reflux esophagitis, upper gastrointestinal hemorrhage, a tall and erect Chinese mugwort syndrome etc., capsule, dispersible tablet, slow releasing capsule, slow releasing tablet.
Oral cavity disintegrating lyophilized tablets is the open network structure substrate that is loaded with medicine, can be in a spot of water disintegrate and homodisperse rapidly, absorb fast, bioavailability is high.Oral cavity disintegrating lyophilized tablets can influence the rate of dissolution of medicine, particularly to the influence of insoluble medicine rate of dissolution, so make oral cavity disintegration tablet and can improve bioavailability of medicament, oral cavity disintegration tablet needn't be used water delivery service, saliva can make its disintegrate or dissolving, can swallow by common dose, can be placed in the water again and take after the disintegrate, can also not need to take medicine with water swallow.Being particularly useful for the patient of old man, children's's dysphagia and the inconvenient person that fetches water takes medicine convenience is provided.The oral cavity disintegrating lyophilized tablets intestinal is residual few, and side effect was hanged down before medicine arrives gastrointestinal tract disintegrate rapidly and is dispersed into trickle granule, caused medicine to distribute in the gastrointestinal tract large tracts of land, and absorption point increases, thereby has reduced medicine to the gastrointestinal local excitation.In addition because oral cavity disintegration tablet rapidly disintegrate in mouth except that major part enters the gastrointestinal tract with swallowing act, also has considerable part to absorb through the oral cavity, thus rapid-action, first pass effect is little.
Utilize famotidine oral cavity disintegrating lyophilized tablets that the oral cavity disintegrating lyophilized tablets technology makes can be in a spot of water disintegrate and homodisperse rapidly, more effective performance therapeutical effect and avoid the excessive concentration of topical remedy also makes gerontal patient, dysphagia patients and taking medicine in water-stressed conditions become more convenient simultaneously.
[specific embodiment]
1. fill a prescription: by weight, principal agent famotidine: filler: binding agent: correctives=20: 20: 12: 1.Wherein filler is one or more the mixture in mannitol, lactose, sorbitol, xylitol, glucose, maltose, the glycine soluble dextrins; Binding agent is one or more the mixture in xanthan gum, gelatin, gelatin hydrolysate, arabic gum, pectin, guar gum, Resina persicae, pectin, tragacanth, acacin, hydroxymethyl cellulose sodium, polyethylene, ketopyrrolidine, carbomer, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, polyethylene glycol oxide, polyvinyl alcohol and the alginate; Correctives is that sucrose, A Siba are sweet, one or more the mixture in the steviosin, chocolate essence, wintergreen oil, menthol, NHDC.
2. obtain solution: famotidine and solubilizing agent is soluble in water, form solution A; Filler, correctives, binding agent are added the water mixed dissolution, form solution B; Solution A and solution B are mixed, and add the suitable quantity of water dilution, fully stir.
3. freeze: above-mentioned mixed solution is put into the mould of required specification, put into fridge quick freezing under-20 ℃～-30 ℃ temperature then.
4. sublimation drying: the charging mould that will freeze is put into freezer dryer, distils under the vacuum and low temperature condition, removes moisture.
5. press mold is packed: with the tablet press mold packing that obtains after the lyophilizing.
Example one: specification: every contains famotidine 20mg
With 4 gram famotidines, the 1.5g aspartic acid adds the 20ml water dissolution, forms solution A; With the 2g gelatin, the 0.4g gelatin hydrolysate, 4g mannitol, 0.2g A Siba is sweet, and the 0.1g NHDC is dissolved in the 50ml water, forms solution B; Solution A and solution B are mixed, and add suitable quantity of water and be diluted to 100ml, fully stir.Above-mentioned mixed solution is put into the mould of required specification, put into fridge quick freezing under-20 ℃～-30 ℃ temperature then.In the charging mould defence freezer dryer that will freeze, under the vacuum and low temperature condition, distil, remove moisture.The press mold packing: with 200 that obtain after the lyophilizing, the press mold packing.
Example two: specification: every contains famotidine 10mg
With 2 gram famotidines, the 0.8g aspartic acid adds the 20ml water dissolution, forms solution A; With the 2g gelatin, the 0.4g gelatin hydrolysate, 4g mannitol, 0.2g A Siba is sweet, and the 0.1g NHDC is dissolved in the 50ml water, forms solution B; Solution A and solution B are mixed, and add suitable quantity of water and be diluted to 100ml, fully stir.Above-mentioned mixed solution is put into the mould of required specification, put into fridge quick freezing under-20 ℃～-30 ℃ temperature then.In the charging mould defence freezer dryer that will freeze, under the vacuum and low temperature condition, distil, remove moisture.The press mold packing: with 200 that obtain after the lyophilizing, the press mold packing.
Claims (8)
1. antacid and Mucosta famotidine oral cavity disintegrating lyophilized tablets, be characterised in that it be with famotidine as principal agent, add suitable filler, binding agent and correctives and make solution, lyophilization forms.
2. famotidine oral cavity disintegrating lyophilized tablets according to claim 1 is characterized in that described filler is one or more the mixture in mannitol, lactose, sorbitol, xylitol, glucose, maltose, the glycine soluble dextrins.
3. famotidine oral cavity disintegrating lyophilized tablets according to claim 1 is characterized in that described binding agent is one or more the mixture in xanthan gum, gelatin, gelatin hydrolysate, arabic gum, pectin, guar gum, Resina persicae, pectin, tragacanth, acacin, hydroxymethyl cellulose sodium, polyethylene, ketopyrrolidine, carbomer, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, polyethylene glycol oxide, polyvinyl alcohol and the alginate.
4. famotidine oral cavity disintegrating lyophilized tablets according to claim 1 is characterized in that described correctives is that sucrose, A Siba are sweet, one or more the mixture in the steviosin, chocolate essence, wintergreen oil, menthol, NHDC.
5. famotidine oral cavity disintegrating lyophilized tablets according to claim 1 is characterized in that by weight, principal agent famotidine: filler: binding agent: correctives=15～30: 15～30: 8～15: 1～3.
6. famotidine oral cavity disintegrating lyophilized tablets according to claim 5 is characterized in that by weight, principal agent famotidine: filler: binding agent: correctives=20: 20: 12: 1.
7. famotidine oral cavity disintegrating lyophilized tablets according to claim 1, its feature also is to contain a certain amount of solubilizing agent, comprises one or more mixture and various derivants of Polyethylene Glycol of lactic acid, aspartic acid, tartaric acid, malic acid, citric acid.
8. the preparation method of famotidine oral cavity disintegrating lyophilized tablets according to claim 1 is characterized in that according to formula ratio, and famotidine and solubilizing agent is soluble in water, forms solution A; Filler, correctives, binding agent are added the water mixed dissolution, form solution B; Solution A and solution B are mixed, and add the suitable quantity of water dilution, fully stir, join in the mould, freezing, sublimation drying, the press seal packing obtains the lyophilizing sheet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101519158A CN101134033A (en) | 2006-08-31 | 2006-08-31 | Famotidine oral cavity disintegrating lyophilized tablets and method for preparing the same |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101519158A CN101134033A (en) | 2006-08-31 | 2006-08-31 | Famotidine oral cavity disintegrating lyophilized tablets and method for preparing the same |
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| CN101134033A true CN101134033A (en) | 2008-03-05 |
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| CNA2006101519158A Pending CN101134033A (en) | 2006-08-31 | 2006-08-31 | Famotidine oral cavity disintegrating lyophilized tablets and method for preparing the same |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103536570A (en) * | 2013-10-15 | 2014-01-29 | 海南卫康制药(潜山)有限公司 | Cimetidine composition lyophilized oral-disintegration tablets |
| CN104546684A (en) * | 2014-12-25 | 2015-04-29 | 海南卫康制药(潜山)有限公司 | Famotidine composition lyophilization tablet and preparation method thereof |
| CN107843668A (en) * | 2017-12-05 | 2018-03-27 | 上海信谊万象药业股份有限公司 | The assay method of drug content in a kind of omeprazole solid preparation |
| CN113384556A (en) * | 2021-06-29 | 2021-09-14 | 烟台荣昌制药股份有限公司 | Gel-forming oral solid preparation for treating hyperacidity and preparation method thereof |
| CN114028342A (en) * | 2021-12-08 | 2022-02-11 | 广东彼迪药业有限公司 | Famotidine rapidly disintegrating particles, famotidine tablets and preparation method |
-
2006
- 2006-08-31 CN CNA2006101519158A patent/CN101134033A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103536570A (en) * | 2013-10-15 | 2014-01-29 | 海南卫康制药(潜山)有限公司 | Cimetidine composition lyophilized oral-disintegration tablets |
| CN104546684A (en) * | 2014-12-25 | 2015-04-29 | 海南卫康制药(潜山)有限公司 | Famotidine composition lyophilization tablet and preparation method thereof |
| CN107843668A (en) * | 2017-12-05 | 2018-03-27 | 上海信谊万象药业股份有限公司 | The assay method of drug content in a kind of omeprazole solid preparation |
| CN113384556A (en) * | 2021-06-29 | 2021-09-14 | 烟台荣昌制药股份有限公司 | Gel-forming oral solid preparation for treating hyperacidity and preparation method thereof |
| CN114028342A (en) * | 2021-12-08 | 2022-02-11 | 广东彼迪药业有限公司 | Famotidine rapidly disintegrating particles, famotidine tablets and preparation method |
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Open date: 20080305 |