CN1271997C - Oral disintegration tablets contg. p-acetaminophenol, and prepn. method therefor - Google Patents
Oral disintegration tablets contg. p-acetaminophenol, and prepn. method therefor Download PDFInfo
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- CN1271997C CN1271997C CN 200410007552 CN200410007552A CN1271997C CN 1271997 C CN1271997 C CN 1271997C CN 200410007552 CN200410007552 CN 200410007552 CN 200410007552 A CN200410007552 A CN 200410007552A CN 1271997 C CN1271997 C CN 1271997C
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- acetaminophen
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Abstract
The present invention relates to an oral disintegration tablet containing paracetamol and a preparation method thereof. The oral disintegration tablet comprises an effective dose of paracetamol and medicinal excipient capable of quickly disintegrating and releasing medicines in the mouth cavity, wherein the medicinal excipient can be a water soluble filling agent, a disintegrating agent, a lubricating agent, a wetting agent or an adhesive. The oral disintegration tablet has the advantages of quick disintegration, quick effect, little residue in the intestinal tract, full absorption, low side effect, convenient medication and good taste.
Description
Technical field
The present invention relates to a kind of acetaminophen oral cavity disintegration tablet and preparation method thereof.
Background technology
Acetaminophen is an acetophenone amine antipyretic analgesic.By suppressing Cycloxygenase, selectivity suppresses synthesizing of hypothalamus thermotaxic centre prostaglandin, causes the peripheral blood vessel expansion, perspires and reaches the antipyretic effect, and its refrigeration function intensity is similar to aspirin; By suppressing the synthetic of prostaglandin etc. and discharge, improve the threshold of pain and play analgesic activity, belong to the periphery analgesic, effect is than a little less than the aspirin, only to light, moderate pain is effective.Think in ntipyretic analgesic medicine that at present choice drug should be an acetaminophen, because its side effect is little, good effect, acetaminophen is one of most widely used medicine in the whole world, being No.1 antipyretic analgesic on the international medical market, also is one of kind of output maximum in China's crude drug simultaneously.
The acetaminophen structural formula is as follows:
Present acetaminophen dosage form commonly used: ordinary tablet, chewable tablet, slow releasing tablet, effervescent tablet, dispersible tablet, capsule, granule, effervescent granule, syrup, suppository, drop etc.Wherein oral formulations needs with water delivery service or slice, thin piece hardness very big more; this patient for dysphagia or water intaking inconvenience takes and has certain difficulty; and take at school or kindergarten oneself for child patient also very inconvenient, so existing these dosage forms can't satisfy patient's demand fully.
Summary of the invention
The object of the invention is to provide a kind of can overcome insufficient acetaminophen novel form of above-mentioned dosage form and preparation method thereof.
The present invention relates to a kind of acetaminophen oral cavity disintegration tablet, comprising the acetaminophen of effective dose and can be in the oral cavity rapidly disintegrate discharge the pharmaceutically acceptable excipient of medicine.
The acetaminophen oral cavity disintegration tablet contains principal agent acetaminophen, filler, disintegrating agent, lubricant, also contains binding agent or wetting agent.
Various main materials and auxiliary materials weight shares prescription in the total amount shared ratio as follows:
A principal agent 5～50%
B filler 10～50%
C disintegrating agent 5～65%
D lubricant 0.3～5%
E binding agent or wetting agent 0.5～10%
Filler is selected the good adjuvant of water solublity for use, and erythrose, mannitol, sorbitol, xylitol or other are convenient to the adjuvant that moisture content infiltrates tablet, or the mixture of above two or more material.
Disintegrating agent is selected cross-linking sodium carboxymethyl cellulose (CCNa), crospolyvinylpyrrolidone (PVPP), crosslinked carboxymethyl fecula sodium (CCMS-Na), low-substituted hydroxypropyl cellulose (L-HPC), microcrystalline Cellulose (MCC) for use, or the mixture of above two or more material.
Can also select gas-producing disintegrant citric acid, tartaric acid, fumaric acid, sodium bicarbonate, sodium glycine carbonate, Glycine sodium fumarate for use.
Lubricant can be selected magnesium stearate, Pulvis Talci or its mixture for use.
The optional water of wetting agent, ethanol or its mixture; Binding agent can be selected starch slurry, polyvidone and various cellulose family for use, or the mixture of above two or more material.
For covering the peculiar taste of acetaminophen, can also add the correctives that accounts for prescription gross weight 2～10% in the present invention, aspartame, cyclamate, saccharin sodium, Mentholum and various fruit powder essence etc. all can satisfy the requirement that improves acetaminophen oral cavity disintegration tablet mouthfeel.
This dosage form adopts wet granulation technology, can use conventional tablet pharmaceutical equipment to produce.
Concrete preparation method is as described below:
Take by weighing acetaminophen (crossing 100 mesh sieves), filler, correctives or part disintegrating agent; add an amount of wetting agent or binding agent behind the mix homogeneously and granulate, dry (50 ℃); to remain disintegrating agent, lubricant etc. and dried particles mix homogeneously; the adding lubricant that is up to the standards, the mix homogeneously tabletting.
For the particularity of disintegrating tablet disintegrate, we have formulated relevant detection method:
The dissolve scattered time limit algoscopy is got this product a slice, puts in the glass dish, gets the scale dropper and measures 1ml37 ℃ of water and directly drip on unilateral, and the control rate of addition was finished in 30 seconds, timing simultaneously checks during to 45 seconds that this product Ying Rong clears entirely, do not clear entirely as molten, get hard paper and scratch, hard core must not be arranged, get 6 of this product, operation in accordance with the law all should be up to specification.
Molten shot degree algoscopy is got this product a slice, shines inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2000) lower device requirement, and hanging basket bottom screen cloth is replaced by 26 eye mesh screens, this product is put in the disintegration tester hanging basket, regulate the hanging basket height, make the bottom screen cloth concordant, and when this product contact water surface, pick up counting with the water surface, in the time of 45 seconds, mention the hanging basket inspection, should get 6 of this product all by screen cloth, operation in accordance with the law all should be up to specification.
As stated above the present invention and acetaminophen ordinary tablet are compared mensuration, the present invention is all up to specification, and ordinary tablet all can not be qualified, and acetaminophen oral cavity disintegration tablet disintegration time of the present invention is significantly shorter than ordinary tablet.
The acetaminophen oral cavity disintegration tablet is little sweet in cool taste, runs in the oral cavity after the saliva rapidly that disintegrate becomes fine particle, swallows conveniently.This dosage form has following advantage:
First disintegrate is rapid, and drug effect is fast.Tablet of the present invention can be in one minute in mouth disintegrate fast, be beneficial to the rapid stripping of medicine, shorten dissolution time, accelerate its absorption, make medicine bring into play curative effect rapidly.
Second drug absorption is abundant.The present invention is disintegrate before reaching gastrointestinal tract, is dispersed into fine particle at gastrointestinal tract, and medicine distributes in the gastrointestinal tract large tracts of land, makes the absorption of medicine more abundant, so also helps improving bioavailability of medicament.
The 3rd taking convenience, good mouthfeel.The present invention needn't use water delivery service, and saliva can make its disintegrate or be partly dissolved, and mouthful in no foreign body sensation owing to wherein add suitable filler and the correctives cool taste sweet compliance that the patient takes medicine that helps improving of distinguishing the flavor of.This kind tablet can place the mouth water delivery service, also can be placed in the water and take after the disintegrate, can also directly place to swallow after the mouth disintegrate and take, for taking medicine, the patient provides very big convenience, compare with liquid preparation and have dosage advantage accurately, the present invention can guarantee that medicine is in time taken, dosage is accurate and curative effect is rapid.
Selected adjuvant all is the adjuvants that are suitable for this tablet of preparation.Water-soluble filler such as erythrose, mannitol can dissolve rapidly in mouth, absorbs heat during dissolving, and cool taste is little sweet, and is very little to the disintegrate influence, is suitable for the preparation of oral cavity disintegration tablet.Microcrystalline Cellulose is that filler has effect with the collaborative disintegrate of disintegrating agent again, and its compressibility gets final product compression moulding when pressure is very little fortunately, because it is porous tubular structured, is beneficial to moisture content and enters tablet inside and impel the slice, thin piece disintegrate.Selected disintegrating agent mostly is efficient disintegrating agent, uses the disintegrate effect that can reach good on a small quantity, and gas-producing disintegrant contacts a spot of moisture content just can produce the disintegrate that a large amount of bubbles promote slice, thin piece.Various disintegrating agents are united use, can reach the purpose that makes the rapid disintegrate of slice, thin piece.The little hardship of acetaminophen raw material is share with aspartame and each essence correctives and can be improved its bitterness, makes the mouthfeel of slice, thin piece suitable.
The specific embodiment
Acetaminophen oral cavity disintegration tablet of the present invention contains principal agent, water-soluble filler, disintegrating agent, lubricant, also contains wetting agent or binding agent, the main materials and auxiliary materials weight share prescription in the total amount shared preferred proportion as follows:
Principal agent 20～40%
Water-soluble filler 20～50%
Disintegrating agent 10～60%
Lubricant 0.5～3%
Binding agent or wetting agent 1～5%
Preferred erythrose of water-soluble filler and mannitol.
Disintegrating agent preferably microcrystalline cellulose (MCC), low-substituted hydroxypropyl cellulose (L-HPC), citric acid and sodium bicarbonate.
Lubricant preferably talc powder.
Wetting agent or binding agent be the second alcohol and water preferably.
The preferred cyclamate of correctives, aspartame and various fruity powder essence.
With following embodiment the present invention is described.
Embodiment 1: preparation acetaminophen oral cavity disintegration tablet
Prescription:
The composition weight percentage by weight
Acetaminophen 100 grams 24%
Mannitol 160 grams 38.4%
Aspartame 1.2 grams 0.28%
Sodium bicarbonate 5 grams 1.2%
Citric acid 5.7 grams 1.37%
Microcrystalline Cellulose 120 grams 28.8%
Polyvinylpyrrolidone (PVPP) 20 grams 4.8%
Essence 0.8 gram 0.2%
Pulvis Talci 4 grams 0.96%
Gross weight 416.7 grams
Make 1000 altogether
Preparation technology:
Take by weighing acetaminophen, mannitol, aspartame by recipe quantity, fully mix, with 50% ethanol water (V/V) system soft material, crossing 32 mesh sieves granulates, 50 ℃ of oven dry, take by weighing by prescription and to add adjuvant sodium bicarbonate, citric acid, microcrystalline Cellulose, polyvinylpyrrolidone (PVPP), essence, Pulvis Talci, mix homogeneously, tabletting.Analyzing and testing: content 100.2%, dissolution 98.3%, dissolve scattered time limit, molten shot degree are all qualified.
Embodiment 2: preparation acetaminophen oral cavity disintegration tablet
Prescription:
The composition weight percentage by weight
Acetaminophen 100 grams 20%
Erythrose 240 grams 47.9%
Cyclamate 7.2 grams 1.44%
Sodium bicarbonate 5 grams 1%
Citric acid 5.7 grams 1.1%
Microcrystalline Cellulose 98 grams 19.57%
Low-substituted hydroxypropyl cellulose (L-HPC) 40 grams 7.98%
Essence 0.8 gram 0.16%
Pulvis Talci 4 grams 0.8%
Gross weight 500.7 grams
Make 1000 altogether
Preparation technology:
Take by weighing acetaminophen, erythrose, cyclamate, microcrystalline Cellulose (half amount) by recipe quantity, fully mix, with 50% ethanol water (V/V) system soft material, crossing 32 mesh sieves granulates, oven dry, take by weighing by prescription and to add adjuvant sodium bicarbonate, citric acid, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose (L-HPC), essence, Pulvis Talci, mix homogeneously, tabletting.Analyzing and testing: content 99.7%, dissolution 96.8%, dissolve scattered time limit, molten shot degree are all qualified.
Embodiment 3: preparation acetaminophen oral cavity disintegration tablet
Prescription:
The composition weight percentage by weight
Acetaminophen 100 grams 24.8%
Erythrose 140 grams 34.76%
Cyclamate 7.2 grams 1.79%
Sodium bicarbonate 5 grams 1.24%
Citric acid 5.7 grams 1.42%
Microcrystalline Cellulose 120 grams 29.8%
Low-substituted hydroxypropyl cellulose (L-HPC) 20 grams 5%
Essence 0.8 gram 0.2%
Pulvis Talci 4 grams 0.99%
Gross weight 402.7 grams
Make 1000 altogether
Preparation technology:
Take by weighing acetaminophen, erythrose, cyclamate by recipe quantity, fully mix, with 50% ethanol water (V/V) system soft material, crossing 32 mesh sieves granulates, oven dry, take by weighing by prescription and to add adjuvant sodium bicarbonate, citric acid, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose (L-HPC), essence, Pulvis Talci, mix homogeneously, tabletting.Analyzing and testing: content 101%, dissolution 98.8%, dissolve scattered time limit, molten shot degree are all qualified.
Embodiment 4: preparation acetaminophen oral cavity disintegration tablet
Prescription:
The composition weight percentage by weight
Acetaminophen 100 grams 29%
Erythrose 65 grams 18.8%
Cyclamate 17.5 grams 5%
Sodium bicarbonate 4 grams 1.16%
Citric acid 12 grams 3.48%
Microcrystalline Cellulose 110 grams 31.9%
Low-substituted hydroxypropyl cellulose (L-HPC) 31.5 grams 9.1%
Essence 0.8 gram 0.23%
Pulvis Talci 4 grams 1.16%
Gross weight 344.8 grams
Make 1000 altogether
Preparation technology:
Take by weighing acetaminophen, erythrose, cyclamate by recipe quantity, mix homogeneously, 50% ethanol water (V/V) system soft material, crossing 32 mesh sieves granulates, oven dry, take by weighing by prescription and to add adjuvant sodium bicarbonate, citric acid, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose (L-HPC), essence, Pulvis Talci, mix homogeneously, tabletting.Analyzing and testing: content 100.5%, dissolution 98.6%, dissolve scattered time limit, molten shot degree are all qualified.
Embodiment 5: preparation acetaminophen oral cavity disintegration tablet
Prescription:
The composition weight percentage by weight
Acetaminophen 100 grams 20.7%
Erythrose 170 grams 35.17%
Cyclamate 17.5 grams 3.62%
Sodium bicarbonate 5 grams 1.03%
Citric acid 5 grams 1.03%
Microcrystalline Cellulose 144 grams 29.8%
Cross-linking sodium carboxymethyl cellulose (CCNa) 36 grams 7.45%
Essence 0.8 gram 0.16%
Pulvis Talci 5 grams 1.03%
Gross weight 483.3 grams
Make 1000 altogether
Preparation technology:
Take by weighing acetaminophen, erythrose, cyclamate by recipe quantity, mix homogeneously, 5% polyvidone, 95% alcoholic solution system soft material, cross 32 mesh sieves and granulate, dry, take by weighing by prescription and add adjuvant sodium bicarbonate, citric acid, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose (CCNa), essence, Pulvis Talci, mix homogeneously, tabletting.Analyzing and testing: content 99.6%, dissolution 97.8%, dissolve scattered time limit, molten shot degree are all qualified.
Claims (3)
1, a kind of acetaminophen oral cavity disintegration tablet, acetaminophen, erythrose, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose and other adjuvants by effective dose are formed, and it is characterized in that weight share proportion in the prescription total amount is: acetaminophen 20～29%, erythrose 18.8～47.9%, microcrystalline Cellulose and low-substituted hydroxypropyl cellulose 27.55～41.0% and other adjuvants are formed.
2, acetaminophen oral cavity disintegration tablet according to claim 1 is characterized in that other adjuvants are selected from lubricant, correctives, wetting agent or binding agent.
3, a kind of method for preparing the described acetaminophen oral cavity disintegration tablet of claim 1, it is characterized in that: take by weighing acetaminophen, erythrose, cyclamate, fully mix, with percent by volume is 50% ethanol water system soft material, the granulation of sieving, oven dry takes by weighing by prescription and to add adjuvant sodium bicarbonate, citric acid, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, essence, Pulvis Talci, mix homogeneously, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410007552 CN1271997C (en) | 2004-02-27 | 2004-02-27 | Oral disintegration tablets contg. p-acetaminophenol, and prepn. method therefor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410007552 CN1271997C (en) | 2004-02-27 | 2004-02-27 | Oral disintegration tablets contg. p-acetaminophenol, and prepn. method therefor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1559390A CN1559390A (en) | 2005-01-05 |
| CN1271997C true CN1271997C (en) | 2006-08-30 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410007552 Expired - Fee Related CN1271997C (en) | 2004-02-27 | 2004-02-27 | Oral disintegration tablets contg. p-acetaminophenol, and prepn. method therefor |
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| Country | Link |
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| CN (1) | CN1271997C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020246120A1 (en) * | 2019-06-07 | 2020-12-10 | あゆみ製薬株式会社 | Orally disintegrating tablet and manufacturing method therefor |
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| WO2008089774A1 (en) * | 2007-01-22 | 2008-07-31 | Crd Saidal | Formulation of an orodispersible tablet based on coated paracetamol |
| CN102743366B (en) * | 2012-07-16 | 2013-11-20 | 海南葫芦娃制药有限公司 | Paracetamol effervescent granule and identification method thereof |
| CN102872173A (en) * | 2012-10-22 | 2013-01-16 | 济南百鸣生物制药有限公司 | Compound acetaminophen orally disintegrating tablet for beasts and birds and preparation method for compound acetaminophen orally disintegrating tablet |
| CN103599093B (en) * | 2013-11-18 | 2016-06-01 | 中国医学科学院生物医学工程研究所 | A kind of anti-HPV pharmaceutical preparation and purposes |
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| CN106562935B (en) * | 2016-09-23 | 2018-06-19 | 广东药科大学 | A kind of paracetamol colorful cartoon oral disintegrating tablet and preparation method for 3D printing |
| CN110101672A (en) * | 2019-05-07 | 2019-08-09 | 安徽金太阳生化药业有限公司 | A kind of paracetamol tablets and preparation method thereof |
| CN111920774B (en) * | 2020-08-06 | 2022-08-12 | 河北君临药业有限公司 | Paracetamol tablet and preparation method thereof |
| CN114129524A (en) * | 2021-09-30 | 2022-03-04 | 山东齐都药业有限公司 | Paracetamol tablet and preparation method thereof |
-
2004
- 2004-02-27 CN CN 200410007552 patent/CN1271997C/en not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020246120A1 (en) * | 2019-06-07 | 2020-12-10 | あゆみ製薬株式会社 | Orally disintegrating tablet and manufacturing method therefor |
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| Publication number | Publication date |
|---|---|
| CN1559390A (en) | 2005-01-05 |
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Owner name: SYSCAN MICRO PHOTOELECTRIC TECHNOLOGY (SHENZHEN) C Free format text: FORMER NAME OR ADDRESS: SYSCAN MICRO PHOTOELECTRIC TECHNOLOGY (SHENZHEN) CO., LTD.; OUYI PHARMACEUTICAL INDUSTRY CO., LTD., SHIJIAZHUANG PHARMACEUTICAL GROUP |
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| CP03 | Change of name, title or address |
Address after: 050051 No. 276 West Zhongshan Road, Hebei, Shijiazhuang Co-patentee after: Shijiazhuang Ouyi Pharma Co., Ltd. Patentee after: Zhongqi Pharm Tech (Shijiazhuang) Co., Ltd., Shiyao Group Address before: 050051 No. 276 West Zhongshan Road, Hebei, Shijiazhuang Co-patentee before: Ouyi Pharmaceutical Co., Ltd., Shijia Zhuang Pharmaceutical Group Patentee before: Zhongqi Pharm Tech (Shijiazhuang) Co., Ltd., Shiyao Group |
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| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20060830 Termination date: 20150227 |
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