CN1589883A - Oral cavity disintegration tablet for treating gout and its preparation method - Google Patents
Oral cavity disintegration tablet for treating gout and its preparation method Download PDFInfo
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- CN1589883A CN1589883A CN 200410025052 CN200410025052A CN1589883A CN 1589883 A CN1589883 A CN 1589883A CN 200410025052 CN200410025052 CN 200410025052 CN 200410025052 A CN200410025052 A CN 200410025052A CN 1589883 A CN1589883 A CN 1589883A
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- oral cavity
- cavity disintegration
- disintegration tablet
- treatment gout
- allopurinol
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Abstract
An oral disintegrating tablet for treating gout is prepared from allopurinol, disintegrant, soluble polyol, filler, penetrant, lubricant, sweetening agent, and essence.
Description
Technical field
The present invention relates to the dosage form of medicine, relate in particular to oral cavity disintegration tablet of treatment gout and preparation method thereof.
Background technology
Gout is that uric acid is too high and be deposited on one group of different substantiality disease of the tissue injury that joint, soft tissue, bone marrow, kidney etc. locate to cause in the blood that causes owing to long-term purine metabolic disturbance, with in, old age and the stomach patient comparatively more sees.Clinical characters is: hyperuricemia, characteristic acute arthritis are shown effect repeatedly, can find uric acid crystal in the leukocyte of knuckle synovia, and tophus forms, and its severe patient can cause joint movement disorder and deformity, kidney urate calculus and or gouty excess of the kidney matter pathological changes.
At present, gout still there is not the radical cure medicine.According to the pathogeny of gout, the medicine of treatment gout can reduce the level of uric acid in the blood by suppressing the synthetic of uric acid or promoting the drainage of uric acid, thereby reduces uric acid in the joint or the calmness of kidney, and produces therapeutical effect.
Allopurinol is an xanthine oxidase inhibitor, allopurinol and major metabolite oxypurinol thereof can suppress xanthine oxidase, and but xanthine oxidase catalysis hypoxanthine is converted into xanthine, be converted into uric acid again, uric acid is synthetic to be reduced so allopurinol and oxypurinol make, reduce blood plasma and urine uric acid concentration, make the uric acid content in blood and the urine be reduced to the following level of dissolubility, prevent that uric acid from forming crystallization deposition in joint and hetero-organization thereof, also helps the in-house uric acid crystal of gout patient to dissolve again.Allopurinol is synthesizing by purine new in the effect inhibition body to hypoxanthine-guanine monophosphate nucleic acid conversion enzyme also.Oral back 24 hours blood uric acid concentration of this product just begins to descend, and descends the most obvious during week at 2-4.Allopurinol is white or off-white color crystalline powder; Almost odorless is tasteless.Atomic molten in water or ethanol, insoluble in ether or chloroform; In alkaline solution, dissolve.In the market the dosage form of allopurinol have mostly that onset is slow, bioavailability is not high, to problems such as gastrointestinal irritation are big.
Summary of the invention
The object of the present invention is to provide a kind of rapid-action, improve bioavailability, to the oral cavity disintegration tablet of the little treatment gout of gastrointestinal irritation.
Another object of the present invention is to provide the preparation method of the oral cavity disintegration tablet for the treatment of gout.
The present invention treats the oral cavity disintegration tablet of gout, comprise active constituents of medicine and adjuvant, medicament active composition is an allopurinol, adjuvant comprises disintegrating agent, solubility polyhydric alcohol, filler, penetrating agent, wherein allopurinol accounts for 20%～50% of this tablet weight, disintegrating agent accounts for 5%～15%, and the solubility polyhydric alcohol accounts for 30%～60%, and filler accounts for 10%～30%, penetrating agent accounts for 1%～5%, lubricant accounts for 0.5%～1.5%, sweeting agent accounts for 0.5%～3%, essence accounts for 0.5%～3%; Wherein disintegrating agent is a crospovidone, one or more mixing in cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, the carboxymethyl starch sodium; The solubility polyhydric alcohol is one or more mixing in mannitol, xylitol, Sorbitol and the maltose alcohol; Filler is one or more mixing in pregelatinized Starch, amylum pregelatinisatum, lactose, sucrose and glucose, cellulose and microcrystalline Cellulose, the gelatin; Penetrating agent is that water is had the silicon dioxide of high-affinity, one or more mixing in the maltodextrin; Lubricant is one or more mixing in magnesium stearate, sodium stearyl fumarate, stearic acid, Polyethylene Glycol, the sodium lauryl sulphate; Sweeting agent is one or more in saccharin sodium, aspartame, stevioside, aspartame, acesulfame potassium, the neohesperidin dihydrochalcone; Essence is one or more in Herba Menthae essence, orange flavor, the flavoring banana essence.
The present invention also provides the preparation method of the oral cavity disintegration tablet of treatment gout, with medicament active composition allopurinol and adjuvant mix homogeneously, is pressed into tablet with tablet machine then and gets final product; Perhaps with medicament active composition allopurinol, adjuvant water dissolution, fully mixing joins and is positioned over sharp freezing in the freeze dryer in the mould, is evacuated to dry materials promptly.
The present invention treats the oral cavity disintegration tablet of gout, and its positive effect is:
1, compare with common oral preparation, extensively covered by the medicine after fast the collapsing because of gastrointestinal tract mucous, onset is rapid.And medicine can the through port transmucosal absorbs, and removed first pass effect from, improved bioavailability, and having reduced stimulates gastrointestinal.
2, provide a kind of new dosage form that makes things convenient for for patient with gout.Because oral cavity disintegration tablet does not need in mouth under water can obey, therefore for because of the bad patient of gout function of deglutition has brought Gospel, also the people's oral medication for the inconvenience of drinking water provides convenience.
The specific embodiment
Embodiment 1: 1000 allopurinol oral cavity disintegration tablets of present embodiment preparation (specification: 0.25g), use following compositions:
| Name of material | Inventory |
| Allopurinol | 250g |
| Mannitol | 420g |
| Microcrystalline Cellulose | 150g |
| Crospovidone | 70g |
| Aspartame | 20g |
| Herba Menthae essence | 10g |
| Silicon dioxide | 20g |
| Magnesium stearate | 5g |
Processing step: medicament active composition allopurinol and adjuvant mannitol, microcrystalline Cellulose, crospovidone granule are mixed, add aspartame, Herba Menthae essence and silicon dioxide, magnesium stearate, mix homogeneously places tablet machine to be pressed into tablet again.
The tablet that above-mentioned technology is obtained carries out mouthfeel, Orally disintegrating time, disintegration, friability mensuration.
| Test item | |
| Mouthfeel | Good |
| The Orally disintegrating time limit | 28 seconds |
| Disintegration | 19 seconds |
| Friability | ????0.5％ |
Embodiment 2: 1000 allopurinol oral cavity disintegration tablets of present embodiment preparation (specification: 0.25g), use following compositions:
| Name of material | Inventory |
| Allopurinol | 250g |
| Sorbitol | 400g |
| Glucose | 80g |
| Sucrose | 70g |
| Cross-linking sodium carboxymethyl cellulose | 60g |
| Stevioside | 25g |
| Orange flavor | 10g |
| Silicon dioxide | 20g |
| Sodium stearyl fumarate | 5g |
Processing step: medicament active composition allopurinol and adjuvant sorbitol, glucose, sucrose, cross-linking sodium carboxymethyl cellulose are mixed, add stevioside, orange flavor and silicon dioxide, sodium stearyl fumarate again, mix homogeneously places tablet machine to be pressed into tablet again.
The tablet that above-mentioned technology is obtained carries out mouthfeel, Orally disintegrating time, disintegration, friability mensuration.
| Test item | |
| Mouthfeel | Good |
| The Orally disintegrating time limit | 25 seconds |
| Disintegration | 16 seconds |
| Friability | ????0.6％ |
Embodiment 3: 1000 allopurinol oral cavity disintegration tablets of present embodiment preparation (specification: 0.25g), use following compositions:
| Name of material | Inventory |
| Allopurinol | 250g |
| Mannitol | 200g |
| Sucrose | 220g |
| Gelatin | 50g |
| Hydroxyethyl-cellulose | 40g |
| Herba Menthae essence | 10g |
Processing step: medicament active composition allopurinol and adjuvant mannitol, sucrose, gelatin, hydroxyethyl-cellulose, Herba Menthae essence water are dissolved, and fully mixing joins and is positioned over sharp freezing in the freeze dryer in the mould, is evacuated to dry materials, packs.
The tablet that above-mentioned steps is obtained carries out mouthfeel, Orally disintegrating time, disintegration time mensuration.
| Test item | |
| Mouthfeel | Good |
| The Orally disintegrating time limit | 19 seconds |
| Disintegration | 14 seconds |
Claims (13)
1, the oral cavity disintegration tablet of treatment gout, comprise active constituents of medicine and adjuvant, it is characterized in that medicament active composition is an allopurinol, adjuvant comprises disintegrating agent, solubility polyhydric alcohol, filler, penetrating agent, wherein allopurinol accounts for 20%～50% of this tablet weight, disintegrating agent accounts for 5%～15%, the solubility polyhydric alcohol accounts for 30%～60%, and filler accounts for 10%～30%, penetrating agent accounts for 1%～5%, lubricant accounts for 0.5%～1.5%, sweeting agent accounts for 0.5%～3%, essence accounts for 0.5%～3%.
2, the oral cavity disintegration tablet of treatment gout according to claim 1 is characterized in that disintegrating agent is a crospovidone, one or more mixing in cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, the carboxymethyl starch sodium.
3, the oral cavity disintegration tablet of treatment gout according to claim 2 is characterized in that the solubility polyhydric alcohol is one or more mixing in mannitol, xylitol, Sorbitol and the maltose alcohol.
4, the oral cavity disintegration tablet of treatment gout according to claim 2 is characterized in that filler is one or more mixing in pregelatinized Starch, amylum pregelatinisatum, lactose, sucrose and glucose, cellulose and microcrystalline Cellulose, the gelatin.
5, the oral cavity disintegration tablet of treatment gout according to claim 2 is characterized in that penetrating agent is that water is had the silicon dioxide of high-affinity, one or more mixing in the maltodextrin.
6, the oral cavity disintegration tablet of treatment gout according to claim 2 is characterized in that lubricant is one or more mixing in magnesium stearate, sodium stearyl fumarate, stearic acid, Polyethylene Glycol, the sodium lauryl sulphate.
7, the oral cavity disintegration tablet of treatment gout according to claim 2 is characterized in that sweeting agent is one or more in saccharin sodium, aspartame, stevioside, aspartame, acesulfame potassium, the neohesperidin dihydrochalcone.
8, the oral cavity disintegration tablet of treatment gout according to claim 2 is characterized in that essence is one or more in Herba Menthae essence, orange flavor, the flavoring banana essence.
9,, it is characterized in that containing in per 1000 allopurinol 250g, mannitol 420g, microcrystalline Cellulose 150g, crospovidone 70g, aspartame 20g, Herba Menthae essence 10g, silicon dioxide 20g, magnesium stearate 5g according to the oral cavity disintegration tablet of any one described treatment gout of claim 1～8.
10,, it is characterized in that containing in per 1000 allopurinol 250g, sorbitol 400g, glucose 80, sucrose 70g, cross-linking sodium carboxymethyl cellulose 60g, stevioside 25g, orange flavor 10g, silicon dioxide 20g, sodium stearyl fumarate 5g according to the oral cavity disintegration tablet of any one described treatment gout of claim 1～8.
11,, it is characterized in that containing in per 1000 allopurinol 250g, mannitol 200g, sucrose 220g, gelatin 50g, hydroxyethyl-cellulose 40g, Herba Menthae essence 10g according to the oral cavity disintegration tablet of any one described treatment gout of claim 1～8.
12, the preparation method of the oral cavity disintegration tablet of treatment gout according to claim 1 and 2 is characterized in that medicament active composition allopurinol and adjuvant mix homogeneously are pressed into tablet with tablet machine then and get final product.
13, the preparation method of the oral cavity disintegration tablet of treatment gout according to claim 1 and 2, it is characterized in that medicament active composition allopurinol, adjuvant water dissolution, fully mixing joins and is positioned over sharp freezing in the freeze dryer in the mould, is evacuated to dry materials promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100250520A CN100528163C (en) | 2004-06-10 | 2004-06-10 | Oral cavity disintegration tablet for treating gout and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100250520A CN100528163C (en) | 2004-06-10 | 2004-06-10 | Oral cavity disintegration tablet for treating gout and its preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1589883A true CN1589883A (en) | 2005-03-09 |
| CN100528163C CN100528163C (en) | 2009-08-19 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100250520A Active CN100528163C (en) | 2004-06-10 | 2004-06-10 | Oral cavity disintegration tablet for treating gout and its preparation method |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105287416A (en) * | 2015-11-20 | 2016-02-03 | 世贸天阶制药（江苏）有限责任公司 | Allopurinol tablet and preparation method thereof |
-
2004
- 2004-06-10 CN CNB2004100250520A patent/CN100528163C/en active Active
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105287416A (en) * | 2015-11-20 | 2016-02-03 | 世贸天阶制药（江苏）有限责任公司 | Allopurinol tablet and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN100528163C (en) | 2009-08-19 |
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Owner name: ZHEJIANG RUIDA PHARMACEUTICAL CO., LTD. HANGZHOU S Owner name: HAINAN POLY PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: FAN MINHUA Effective date: 20100707 |
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Free format text: CORRECT: ADDRESS; FROM: 310004 HOUSE 5, BUILDING 9, NO.167, HUANCHENG NORTH ROAD, HANGZHOU CITY, ZHEJIANG PROVINCE TO: 571127 GUILINYANG ECONOMIC AND TECHNOLOGICAL DEVELOPMENT ZONE, MEILAN DISTRICT, HAIKOU CITY, HAINAN PROVINCE |
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| TR01 | Transfer of patent right |
Effective date of registration: 20100707 Address after: 571127 Guilin economic and Technological Development Zone, Meilan District, Hainan, Haikou Co-patentee after: Zhejiang Ruida Pharmaceutical Co., Ltd. Patentee after: Hainan Pulin Pharmaceutical Co., Ltd. Co-patentee after: Hangzhou Saili Medicine Inst. Co., Ltd. Address before: 5, building 9, building 167, building 310004, Ring North Road, Hangzhou, Zhejiang Patentee before: Fan Minhua |
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| CI01 | Correction of invention patent gazette |
Correction item: Patentee Correct: Zhejiang Ridae Pharmaceutical Co., Ltd. False: Zhejiang Ruida Pharmaceutical Co., Ltd. Number: 33 Volume: 26 |
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| CI03 | Correction of invention patent |
Correction item: Patentee Correct: Zhejiang Ridae Pharmaceutical Co., Ltd. False: Zhejiang Ruida Pharmaceutical Co., Ltd. Number: 33 Page: The title page Volume: 26 |
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| C56 | Change in the name or address of the patentee |
Owner name: HAINAN PLOY PHARMACEUTICAL CO., LTD. Free format text: FORMER NAME: HAINAN PULIN PHARMACEUTICAL CO., LTD. |
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| CP01 | Change in the name or title of a patent holder |
Address after: 571127 Guilin economic and Technological Development Zone, Meilan District, Hainan, Haikou Patentee after: Hainan Puli Pharmacy stock Co., Ltd Patentee after: Zhejiang Poly Pharmaceutical Co., Ltd. Patentee after: Hangzhou Saili Medicine Inst. Co., Ltd. Address before: 571127 Guilin economic and Technological Development Zone, Meilan District, Hainan, Haikou Patentee before: Hainan Pulin Pharmaceutical Co., Ltd. Patentee before: Zhejiang Ridae Pharmaceutical Co., Ltd. Patentee before: Hangzhou Saili Medicine Inst. Co., Ltd. |