CN1857260A - Oral alpha-lipoic acid disintegrant tablet and its preparing method - Google Patents
Oral alpha-lipoic acid disintegrant tablet and its preparing method Download PDFInfo
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- CN1857260A CN1857260A CN 200610024746 CN200610024746A CN1857260A CN 1857260 A CN1857260 A CN 1857260A CN 200610024746 CN200610024746 CN 200610024746 CN 200610024746 A CN200610024746 A CN 200610024746A CN 1857260 A CN1857260 A CN 1857260A
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- lipoic acid
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Abstract
The present invention relates to a kind of oral alpha-lipoic acid disintegrant tablet with fast disintegration and its preparation process. The oral alpha-lipoic acid disintegrant tablet includes alpha-lipoic acid as main medicine component, stuffing, disintegrating agent, corrective, masking agent, lubricant, effervesce agent and other medicinal excipient. It is prepared through a specific preparation process. It has fast disintegration and good taste, and is suitable for taking without water and for patient with dysphagia. It is used for delaying senility, treating diabetic polyneuropathy, and preventing and treating noise, senility and drug caused deafness.
Description
Technical field
The present invention relates to a kind of newtype drug dosage form, be specially a kind of delaying senility that can be used for, treatment diabetic polyneuropathy, and prevention and treatment are because oral alpha-lipoic acid disintegrant tablet of the deafness of noise, aging and medicine source property and preparation method thereof.
Background technology
Alpha-lipoic acid (α-lipoic acid LA), also claims thioctic acid, is a kind of vitamin, and its chemical name is 1,2-dithiolane-3-valeric acid, and it was not only water-soluble but also be dissolved in fat.Alpha-lipoic acid is the strongest a kind of of effect in the known natural inhibitor, the endogenous antioxidant of can regenerating, and as vitamin E, vitamin C, coenzyme Q10, glutathion and alpha-lipoic acid itself is called as " antioxidant of antioxidant ".The epsilon-amino covalent bond of lysine residue in the normal and protein molecule of alpha-lipoic acid in the animal vegetable tissue exists with the form of amido link.The plant that alpha-lipoic acid content is the highest is a Herba Spinaciae, secondly is Fructus Lycopersici esculenti and Caulis et Folium Brassicae capitatae; Alpha-lipoic acid content is the highest in liver and the renal tissue in animal body.Alpha-lipoic acid is the cofactor of pyruvic dehydrogenase, and it changes S-acetyl-coenzyme-A at acetone acid, generates flavin adenine dinucleotide reduced form (FADH), and participating in the tricarboxylic acid cycle process is indispensable material.It is a metabolic antioxidant, can be converted into the dihydrolipoic acid (DHLA) of reduced form in vivo.In recent years, alpha-lipoic acid and DHLA have been subjected to showing great attention in the important function aspect antioxidation, carbohydrate metabolism, diabetic complication and other the multiple disease treatment.
At present, alpha-lipoic acid is approved for the curative of diabetic polyneuropathy in Germany; Be mainly used in the detoxifcation of hepatic insufficiency, subacute necrosis encephalopathy and poisonous mushroom in other American-European countries; In Asian countries, be used for the treatment of the inner ear dysfunction that hepatopathy, subacute necrotizing encephalopathy, streptomycin and poisoning by kanamycin and noise cause.Alpha-lipoic acid has caused common concern both domestic and external as antioxidant, and the experimental study of its protection audition also is in full swing.
Alpha-lipoic acid only has injection and capsule dosage form to use to some extent at present, finds no the relevant report of closing oral alpha-lipoic acid disintegrant tablet.Alpha-lipoic acid is made the oral cavity disintegration tablet dosage form, help the patient and carry and take.
Summary of the invention
The object of the present invention is to provide a kind of can be in the oral cavity oral alpha-lipoic acid disintegrant tablet of discharging of disintegrate and preparation method thereof rapidly.This oral cavity disintegration tablet disintegrate is rapid, fast Absorption, and mouthfeel is good, no sand type; It is convenient to have medication, characteristics such as is convenient to carry, and is specially adapted to take under dysphagia patients and the anhydrous condition.The present invention can be used for delaying senility, treatment diabetic polyneuropathy, and prevent and treat the deafness that causes owing to noise, aging and drug use.
The present invention relates to a kind of oral alpha-lipoic acid disintegrant tablet, comprising the principal agent alpha-lipoic acid and help the medicine medicinal excipient that rapid disintegrate discharges in the oral cavity.
The prescription of this oral alpha-lipoic acid disintegrant tablet is composed as follows: alpha-lipoic acid (5-50) %, filler (10-60) %, disintegrating agent (10-50) %, correctives (10-40) %, odor mask (0-30) %, lubricant (0.5-5) %, effervescent (0-30) %.Wherein:
Described filler includes but are not limited to lactose, sucrose, glucose, mannitol, sorbitol, xylitol, starch, microcrystalline Cellulose etc., can use alone or in combination.
Described disintegrating agent includes but are not limited to low-substituted hydroxypropyl cellulose (L-HPC), microcrystalline Cellulose (MCC), cross-linking sodium carboxymethyl cellulose (CCNa), crospolyvinylpyrrolidone (PVPP), crosslinked carboxymethyl fecula sodium (CCMS-Na) and handles agar (TAG) etc., can use alone or in combination.
Described correctives includes but are not limited to the sweet acid of gland, lactose, xylose, fructose, malt extract, glucose, Mel, sucrose, sorbitol, xylitol, maltose alcohol, glycyrrhizin, phyllodulcin, sweetleaf centautin, aspartame, glucide, saccharin sodium, mannitol, gelatin, citric acid, Herba Menthae essence, Fructus Citri tangerinae flavor essence etc., can use alone or in combination.
Described odor mask includes but are not limited to gelatin, arabic gum, chitosan, alginic acid and its esters, carboxymethyl cellulose salt, ethyl cellulose, methylcellulose, hypromellose, crylic acid resin, polyvinyl alcohol, polyvinylpyrrolidone etc., can use alone or in combination.
Described lubricant includes but are not limited to calcium stearate, magnesium stearate, zinc stearate, Pulvis Talci, Macrogol 4000, sodium benzoate etc., can use alone or in combination.
Described effervescent includes but are not limited to sodium carbonate, citric acid, tartaric acid, boric acid etc., can, use alone or in combination.
This dosage form adopts direct compression technology, can use conventional tablet pharmaceutical equipment production.
Concrete preparation method is as described below:
The first step takes by weighing alpha-lipoic acid and odor mask according to quantity, and the granule that alpha-lipoic acid is rolled into the about 1000 μ m of particle diameter with odor mask is to reach the purpose of covering the sand type that granule causes behind the disintegration of tablet;
Second step sieved filler and above-mentioned granule behind the mixing, added disintegrating agent, correctives and effervescent mix homogeneously, then added lubricant, and further mix homogeneously is standby;
The 3rd step gained material detects through intermediate, determines the heavy back of sheet with less pressure direct compression promptly.
The present invention runs in the oral cavity after the saliva rapidly that disintegrate becomes fine particle, and for disintegrate effect of the present invention is investigated, we have set corresponding in vitro disintegration time mensuration method, and method is as follows:
Get 6 of this product, put internal diameter respectively and be about 2.3cm, height is about in the container of 3.5cm, is medium with water 2ml, and temperature is 37 ± 1 ℃, tablet is immersed in the water fully, and disintegrate fully in 60 seconds, and should be fully by No. 1 sieve.
As stated above the present invention and alpha-lipoic acid ordinary tablet reference substance are checked that the present invention is all can disintegrate in 60 seconds molten to loose and by screen cloth, and ordinary tablet does not all reach this requirement.
Compare with conventional tablet, capsule and injection, oral alpha-lipoic acid disintegrant tablet has the advantage of significantly taking, it is taken does not need water, for old people, child, gulp down for the cancer chemotherapy patient that water promptly vomits very convenient, particularly at some special environment, when anhydrous, can take the deafness that causes with pre-antinoise as wartime temporarily.Simultaneously said preparation has also that other advantages of oral cavity disintegration tablet are fast as absorbing, bioavailability is high.
The specific embodiment
Oral alpha-lipoic acid disintegrant tablet of the present invention comprises principal agent alpha-lipoic acid and medicinal excipient such as filler, disintegrating agent, correctives, odor mask, lubricant and effervescent, through specific preparation method preparation, adopts tablet machine to suppress and get.Be the preparation method of better explanation oral alpha-lipoic acid disintegrant tablet of the present invention, as follows especially exemplified by example:
Embodiment 1. preparation oral alpha-lipoic acid disintegrant tablets
Prescription:
1. principal agent---alpha-lipoic acid 100.0g
2. odor mask---gelatin 20.0g
3. filler---lactose 55.0g
4. correctives---aspartame 3.0g
5. disintegrating agent---crospolyvinylpyrrolidone 10.0g
Microcrystalline Cellulose 90.0g
6. lubricant---magnesium stearate 3.0g
7. effervescent---sodium bicarbonate 69.0g
Preparation method:
1. 60 mesh sieves are standby excessively respectively to get alpha-lipoic acid, gelatin, lactose, aspartame, sodium bicarbonate.
2. get an amount of dissolved in distilled water gelatin, stir adding alpha-lipoic acid, lactose, aspartame and sodium bicarbonate down, 70 ℃ of stirring in water bath evaporates to dryness are pulverized, and it is standby to cross 60 mesh sieves.
3. get crospolyvinylpyrrolidone, microcrystalline Cellulose and cross 60 mesh sieves and mix homogeneously respectively, standby with the made granule of the previous step mixing that sieves again.
4. get magnesium stearate and add in the said mixture, the mixing that sieves gets intermediate.
5. the intermediate content detection is determined the heavy back of sheet direct compression promptly.
Gross weight 350g makes 1000 altogether, the heavy 350mg/ sheet of designation card.
6. measure disintegration, all in 15~30 seconds.
Embodiment 2. preparation oral alpha-lipoic acid disintegrant tablets
Prescription:
1. principal agent---alpha-lipoic acid 100.0g
2. odor mask---gelatin 25.0g
3. filler---mannitol 90.0g
4. correctives---aspartame 5.0g
The sweet sour 5.0g of gland
5. disintegrating agent---crospolyvinylpyrrolidone 20.0g
Microcrystalline Cellulose 90.0g
Low-substituted hydroxypropyl cellulose 10.0g
6. lubricant---magnesium stearate 5.0g
Preparation method:
1. 60 mesh sieves are standby excessively respectively to get alpha-lipoic acid, gelatin, mannitol, aspartame, the sweet acid of gland.
2. get an amount of dissolved in distilled water gelatin, stir adding alpha-lipoic acid down, 70 ℃ of stirring in water bath evaporates to dryness are pulverized, and it is standby to cross 60 mesh sieves.
3. it is standby to get mannitol, aspartame, the sweet sour mix homogeneously of gland and made granule of the 2nd step mixing that sieves.
4. get crospolyvinylpyrrolidone, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose and cross 60 mesh sieves and mix homogeneously respectively, standby with the 3rd step gained powder mixing that sieves again.
5. get magnesium stearate and add in the said mixture, the mixing that sieves gets intermediate.
6. the intermediate content detection is determined the heavy back of sheet direct compression promptly.
Gross weight 350g makes 1000 altogether, the heavy 350mg/ sheet of designation card.
7. measure disintegration, all in 15~40 seconds.
Embodiment 3. preparation oral alpha-lipoic acid disintegrant tablets
Prescription:
1. principal agent---alpha-lipoic acid 100.0g
2. odor mask---polyvinylpyrrolidone 10.0g
2. filler---xylitol 110.0g
3. correctives---aspartame 4.0g
Fructus Citri tangerinae flavor essence 3.0g
4. disintegrating agent---crospolyvinylpyrrolidone 15.0g
Low-substituted hydroxypropyl cellulose 25.0g
5. lubricant---magnesium stearate 3.0g
6. effervescent---sodium bicarbonate 80.0g
Preparation method:
1. 60 mesh sieves are standby excessively respectively to get alpha-lipoic acid, xylitol, aspartame, Fructus Citri tangerinae flavor essence and sodium bicarbonate.
2. get alpha-lipoic acid, aspartame, Fructus Citri tangerinae flavor essence and sodium bicarbonate, granulate with polyvinylpyrrolidone, pulverize, it is standby to cross 60 mesh sieves.
3. get xylitol, crospolyvinylpyrrolidone, low-substituted hydroxypropyl cellulose and cross 60 mesh sieves and mix homogeneously respectively, standby with the made granule of the previous step mixing that sieves again.
4. get magnesium stearate and add in the said mixture, the mixing that sieves gets intermediate.
5. the intermediate content detection is determined the heavy back of sheet direct compression promptly.
Gross weight 350g makes 1000 altogether, the heavy 350mg/ sheet of designation card.
6. measure disintegration, all in 15~40 seconds.
Claims (4)
1. an oral alpha-lipoic acid disintegrant tablet is formed prescription and is comprised alpha-lipoic acid, filler, disintegrating agent, correctives, odor mask, lubricant and effervescent, and it is composed as follows to it is characterized in that writing out a prescription:
Alpha-lipoic acid 5~50%
Filler 10~60%
Disintegrating agent 10~50%
Correctives 10~40%
Odor mask 0~30%
Lubricant 0.5~5%
Effervescent 0~30%.
2. according to the described a kind of oral alpha-lipoic acid disintegrant tablet of claim 1, it is characterized in that:
Described filler comprises lactose, sucrose, glucose, mannitol, sorbitol, xylitol, starch, microcrystalline Cellulose, can use alone or in combination;
Described disintegrating agent comprises low-substituted hydroxypropyl cellulose (L-HPC), microcrystalline Cellulose (MCC), cross-linking sodium carboxymethyl cellulose (CCNa), crospolyvinylpyrrolidone (PVPP), crosslinked carboxymethyl fecula sodium (CCMS-Na) and handles agar (TAG), can use alone or in combination;
Described correctives comprises the sweet acid of gland, lactose, xylose, fructose, malt extract, glucose, Mel, sucrose, sorbitol, xylitol, maltose alcohol, glycyrrhizin, phyllodulcin, sweetleaf centautin, aspartame, glucide, saccharin sodium, mannitol, gelatin, citric acid, Herba Menthae essence, Fructus Citri tangerinae flavor essence, can use alone or in combination;
Described odor mask comprises gelatin, arabic gum, chitosan, alginic acid and its esters, carboxymethyl cellulose salt, ethyl cellulose, methylcellulose, hypromellose, crylic acid resin, polyvinyl alcohol, polyvinylpyrrolidone, can use alone or in combination;
Described lubricant comprises calcium stearate, magnesium stearate, zinc stearate, Pulvis Talci, Macrogol 4000, sodium benzoate, can use alone or in combination;
Described effervescent comprises sodium carbonate, citric acid, tartaric acid, boric acid, can use alone or in combination, also can.
3. according to the preparation method of the described a kind of oral alpha-lipoic acid disintegrant tablet of claim 1, it is characterized in that forming by following steps:
The first step takes by weighing odor mask and alpha-lipoic acid according to quantity, alpha-lipoic acid is rolled into the granule of the about 1000 μ m of particle diameter with odor mask;
Second step sieved filler and above-mentioned granule behind the mixing, added disintegrating agent, correctives and effervescent mix homogeneously, then added lubricant, and further mix homogeneously is standby;
The 3rd step gained material detects through intermediate, determines the heavy back of sheet with less pressure direct compression promptly.
According to the described a kind of oral alpha-lipoic acid disintegrant tablet of claim 1 in delaying senility, treatment diabetic polyneuropathy and prevention and treatment because the application that noise, aging and drug use cause aspect deaf.
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CN 200610024746 CN1857260A (en) | 2006-03-16 | 2006-03-16 | Oral alpha-lipoic acid disintegrant tablet and its preparing method |
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102008470A (en) * | 2010-05-24 | 2011-04-13 | 中国人民解放军第二军医大学 | Compound preparation and use thereof for preventing and treating noise induced hearing damage |
CN105267164A (en) * | 2014-07-04 | 2016-01-27 | 江苏神龙药业有限公司 | Thioctic acid dispersible tablet and preparation method thereof |
GB2586745B (en) * | 2018-03-13 | 2023-04-05 | Nuchido Ltd | Compositions |
-
2006
- 2006-03-16 CN CN 200610024746 patent/CN1857260A/en active Pending
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102008470A (en) * | 2010-05-24 | 2011-04-13 | 中国人民解放军第二军医大学 | Compound preparation and use thereof for preventing and treating noise induced hearing damage |
CN102008470B (en) * | 2010-05-24 | 2012-08-29 | 中国人民解放军第二军医大学 | Compound preparation and use thereof for preventing and treating noise induced hearing damage |
CN105267164A (en) * | 2014-07-04 | 2016-01-27 | 江苏神龙药业有限公司 | Thioctic acid dispersible tablet and preparation method thereof |
CN105267164B (en) * | 2014-07-04 | 2019-11-05 | 江苏神龙药业股份有限公司 | Lipoic acid dispersible tablet and preparation method thereof |
GB2586745B (en) * | 2018-03-13 | 2023-04-05 | Nuchido Ltd | Compositions |
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