CN100464744C - Orally disintegrated Ubenimex tablet and its prepn process - Google Patents
Orally disintegrated Ubenimex tablet and its prepn process Download PDFInfo
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- CN100464744C CN100464744C CNB2005100168319A CN200510016831A CN100464744C CN 100464744 C CN100464744 C CN 100464744C CN B2005100168319 A CNB2005100168319 A CN B2005100168319A CN 200510016831 A CN200510016831 A CN 200510016831A CN 100464744 C CN100464744 C CN 100464744C
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- ubenimex
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Abstract
The orally disintegrated Ubenimex tablet consists of Ubenimex as active component and supplementary material including disintegrating agent, soluble diluent, adhesive and lubricant. The disintegrating agent is mixture of 2 or 3 of low substituted hydroxypropyl cellulose, cross-linked carboxymethyl cellulose, cross-linked sodium carboxymethyl starch, cross-linked polyvidon and microcrystalline cellulose. The preparation process is the combination of wet pelletizing and direct tabletting. The orally disintegrated Ubenimex tablet has fast disintegration, administration convenience, fast absorption, high bioavailability, and less irritation to gastrointestinal tract.
Description
Technical field
The invention belongs to medicine and preparation method thereof field, particularly a kind of oral cavity disintegration tablet and preparation method thereof.
Background technology
Ubenimex is by activation antineoplastic immune function, and presents antitumor action.Have the effect that suppresses cell proliferation, single with or with other chemotherapeutic also with can suppressing tumor growth and transfer, and can prolong survival time of patients.Ubenimex is mainly used in acute and chronic leukaemic as immunomodulator.
Ubenimex is a peroral dosage form in the market.Such as authentication code is the glad capsule of hundred scholars of the accurate word of traditional Chinese medicines (1998) X-348.Adopted name is the ubenimex ubenimex, and chemical name is N-[(2S, 3R)-and 4-phenyl-2-maloyl group]-the L-leucine.The glad capsule of hundred scholars and other chemotherapy drugs in combination are used for acute myeloid leukaemia, chronic myelogenous leukemia, lung squamous cancer, malignant melanoma, the treatment of gastric cancer etc., and and radiotherapy unite the treatment that is used for nasopharyngeal carcinoma etc.Also be used for the immunologic hypofunction disease that various factors causes, try out in the treatment of myelodysplastic syndromes and PRCA disease.Glad capsular usage of hundred scholars and consumption are adult 30mg, and qd is oral on an empty stomach.The child is cut down according to the circumstance.Symptom lighter and long-term user also can take weekly 2～3 times.
The cancer patient mostly has symptoms of emesis after radiotherapy or chemotherapy, so the patient's oral medication under medication inconvenience, particularly old man, child, dysphagia or the special environment is more inconvenient; Also be unfavorable for absorption of human body.
Summary of the invention
The technical problem to be solved in the present invention provides a kind of taking convenience, and absorbs the solid rapid release ubenimex preparation fast, that bioavailability is high.Another technical problem that will solve of the present invention provides the preparation method of Orally disintegrated Ubenimex tablet.
Orally disintegrated Ubenimex tablet of the present invention is made up of active constituents of medicine ubenimex and adjuvant, and adjuvant comprises disintegrating agent, solubility diluent, binding agent and lubricant; Wherein press the mass percent of tablet, ubenimex accounts for 5%～30%, and disintegrating agent accounts for 8%～22%, and the solubility diluent accounts for 45%～70%, binder constitutes 0%～8%, lubricant account for 3%～5%; Disintegrating agent is 2～3 kinds of mixing in low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, crospovidone, the microcrystalline Cellulose; The solubility diluent is mannitol or xylitol or Sorbitol or maltose alcohol or erythrol; Binding agent is polyvidone or hydroxypropyl cellulose; Lubricant is one or both mixing in micropowder silica gel, stearic acid, ultra micro polyoxyethylene glycol, the silicon dioxide.
The adjuvant of Orally disintegrated Ubenimex tablet can also comprise correctives, and promptly essence is or/and sweetener, and correctives can account for 0～7% of tablet by quality; Correctives can be one or more mixing in citric acid, orange flavor, Herba Menthae essence, flavoring banana essence, the aspartame; Sweetener also can be selected from sodium saccharinate, stevioside, aspartame, neohesperidin dihydrochalcone etc.
The pharmacology of Orally disintegrated Ubenimex tablet, indication, usage and dosage are identical with the glad capsule of hundred scholars.
The present invention also discloses a kind of preparation method of Orally disintegrated Ubenimex tablet, and this preparation method adopts wet granulation and direct compression process process combined.
Concrete technical process is, with active constituents of medicine ubenimex, solubility diluent, binding agent batch mixing by mass percentage, crosses 100 mesh sieves, with ethanol system soft material, crosses 40 mesh sieves and granulates, then in 40～60 ℃ of dryings 25～40 minutes, with 80 mesh sieve granulate; Add the lubricant tabletting again with the granule mixing after at last disintegrating agent being crossed 100 mesh sieves.
Can when ubenimex, diluent, bonding agent batch mixing, add correctives by mass percentage.
The present invention adopts in prescription and directly adds disintegrating agent and adopt different disintegrating agent ratio and combination, can reach the effect of rapid disintegrate, not only can improve compressibility but also can improve disintegration.
The present invention makes oral cavity disintegration tablet with ubenimex can make things convenient for medication, does not need water or only needs low amounts of water, need not to chew, and medicine places on the tongue, after rapid dissolving of chance saliva or the disintegrate, borrows swallowing act to go into the stomach onset.Its more common solid orally ingestible absorbs fast, and the bioavailability height is a kind of novel solid quick releasing formulation.Extensively covered by the medicine after fast the collapsing because of gastrointestinal tract mucous, so onset is rapid.And medicine can the through port transmucosal absorbs, and removed first pass effect from, and having reduced stimulates gastrointestinal.Oral cavity disintegration tablet of the present invention does not need in mouth under water can obey, and has solved especially because of drinking water inconvenience or the difficulty that the cancer patient of symptoms of emesis can not medication is arranged.
The specific embodiment
Following examples 1～6 provide 6 groups of prescriptions of the present invention.The active constituents of medicine of each prescription and the component of adjuvant and consumption thereof are listed in table 1.In the table 1, the consumption unit of each component is " gram ", and the total amount of each component is 100 grams, can prepare 1000 Orally disintegrated Ubenimex tablets, the every heavy 100mg of sheet.
Embodiment 1
Press mass ratio in the prescription of present embodiment, the active constituents of medicine ubenimex accounts for 5%.Disintegrating agent is that low-substituted hydroxypropyl cellulose and microcrystalline Cellulose account for 19%; Solubility diluent Sorbitol accounts for 60%; The binding agent polyvidone accounts for 5%; Lubricant silica comprises 4%; In addition, correctives aspartame and Herba Menthae essence account for 7%.
Embodiment 2
Press mass ratio in the prescription of present embodiment, the active constituents of medicine ubenimex accounts for 10%.Disintegrating agent is that low-substituted hydroxypropyl cellulose and crospovidone account for 21%; Solubility diluent maltose alcohol accounts for 54%; The binding agent polyvidone accounts for 5%; Lubricant silica comprises 5%; In addition, there are correctives aspartame and orange flavor to account for 5%.
Embodiment 3
Press mass ratio in the prescription of present embodiment, the active constituents of medicine ubenimex accounts for 10%.Disintegrating agent is that crosslinked carboxymethyl fecula sodium and microcrystalline Cellulose account for 16%; The solubility diluent mannitol accounts for 68%; The binding agent hydroxypropyl cellulose accounts for 2%; Lubricant micropowder silica gel and silica comprises 4%.
Embodiment 4
Press mass ratio in the prescription of present embodiment, the active constituents of medicine ubenimex accounts for 10%.Disintegrating agent is that low-substituted hydroxypropyl cellulose and crospovidone account for 18%; Solubility diluent xylitol accounts for 58%; The binding agent polyvidone accounts for 6%; Lubricant ultra micro polyoxyethylene glycol and silica comprises 5%; In addition, there is the correctives flavoring banana essence to account for 3%.
Embodiment 5
Press mass ratio in the prescription of present embodiment, the active constituents of medicine ubenimex accounts for 10%.Disintegrating agent is that low-substituted hydroxypropyl cellulose and cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose account for 16%; Solubility diluent erythrol accounts for 67.5%; Lubricant stearic acid and silica comprises 3.5%; In addition, there is the correctives citric acid to account for 3%.
Present embodiment does not use binding agent.
Embodiment 6
Press mass ratio in the prescription of present embodiment, the active constituents of medicine ubenimex accounts for 30%.Disintegrating agent is that cross-linking sodium carboxymethyl cellulose and microcrystalline Cellulose account for 9%; Solubility diluent maltose alcohol accounts for 46%; The binding agent polyvidone accounts for 8%; Lubricant micropowder silica gel and silica comprises 4%; In addition, there is the correctives citric acid to account for 3%.
Embodiment 7
With the arbitrary component in the disintegrating agent of handling agar replacement embodiment 1～6, effect is identical.
With the arbitrary component in the lubricant of sodium stearyl fumarate or magnesium stearate replacement embodiment 1～6, effect is identical.
Also can reach the purpose of flavoring with the aspartame in sodium saccharinate, stevioside, aspartame or the neohesperidin dihydrochalcone alternate embodiment 1,2.
Embodiment 8
Its preparation method of preferred Orally disintegrated Ubenimex tablet: after ubenimex, diluent, binding agent, correctives crossed 100 mesh sieves, with 50% ethanol system soft material, the granulation of mistake 40 mesh sieves was then in 50 ℃ of dryings 30 minutes, with 80 mesh sieve granulate.Then disintegrating agent is crossed behind 100 mesh sieves with the granule mixing and added tabletting behind the lubricant again.
Table 1
Claims (3)
1, a kind of Orally disintegrated Ubenimex tablet is made up of active constituents of medicine ubenimex and adjuvant, it is characterized in that, adjuvant comprises disintegrating agent, solubility diluent, binding agent and lubricant; Wherein press the mass percent of tablet, ubenimex accounts for 5%～30%, and disintegrating agent accounts for 8%～22%, and the solubility diluent accounts for 45%～70%, binder constitutes 0%～8%, lubricant account for 3%～5%; Disintegrating agent is 2～3 kinds of mixing in low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, crospovidone, the microcrystalline Cellulose; The solubility diluent is xylitol or Sorbitol or maltose alcohol; Binding agent is polyvidone or hydroxypropyl cellulose; Lubricant is one or both mixing in micropowder silica gel, stearic acid, ultra micro polyoxyethylene glycol, the silicon dioxide.
2, according to the described Orally disintegrated Ubenimex tablet of claim 1, it is characterized in that adjuvant also has correctives; Correctives accounts for 0～7% of tablet by quality; Correctives is one or both mixing in citric acid, orange flavor, Herba Menthae essence, flavoring banana essence, sodium saccharinate, stevioside, aspartame, the neohesperidin dihydrochalcone.
3, a kind of preparation method of Orally disintegrated Ubenimex tablet as claimed in claim 1, Orally disintegrated Ubenimex tablet is made up of active constituents of medicine ubenimex and adjuvant; Adjuvant comprises disintegrating agent, solubility diluent, binding agent and lubricant; Wherein press the mass percent of tablet, ubenimex accounts for 5%～30%, and disintegrating agent accounts for 8%～22%, and the solubility diluent accounts for 45%～70%, binder constitutes 0%～8%, lubricant account for 3%～5%; Preparation process is, with active constituents of medicine ubenimex, solubility diluent, binding agent batch mixing by mass percentage, crosses 100 mesh sieves, with ethanol system soft material, crosses 40 mesh sieves and granulates, then in 40～60 ℃ of dryings 25～40 minutes, with 80 mesh sieve granulate; Add the lubricant tabletting again with the granule mixing after at last disintegrating agent being crossed 100 mesh sieves.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100168319A CN100464744C (en) | 2005-05-30 | 2005-05-30 | Orally disintegrated Ubenimex tablet and its prepn process |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100168319A CN100464744C (en) | 2005-05-30 | 2005-05-30 | Orally disintegrated Ubenimex tablet and its prepn process |
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| Publication Number | Publication Date |
|---|---|
| CN1706373A CN1706373A (en) | 2005-12-14 |
| CN100464744C true CN100464744C (en) | 2009-03-04 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNB2005100168319A Expired - Fee Related CN100464744C (en) | 2005-05-30 | 2005-05-30 | Orally disintegrated Ubenimex tablet and its prepn process |
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Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101002931B (en) * | 2006-01-19 | 2010-09-22 | 上海秀新臣邦医药科技有限公司 | Ubenimex tablet and its preparing method |
| CN101601649B (en) * | 2009-07-20 | 2011-05-04 | 山东大学 | Ubenimex fat emulsion injection and preparation method thereof |
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2005
- 2005-05-30 CN CNB2005100168319A patent/CN100464744C/en not_active Expired - Fee Related
Non-Patent Citations (6)
| Title |
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| 口腔崩解片的研制. 张辉等.海南医学，第14卷第9期. 2003 |
| 口腔崩解片的研制. 张辉等.海南医学，第14卷第9期. 2003 * |
| 口腔崩解片研制简介. 李玉云等.实用中西医结合临床，第3卷第2期. 2003 |
| 口腔崩解片研制简介. 李玉云等.实用中西医结合临床，第3卷第2期. 2003 * |
| 国产乌苯美司联合化疗治疗复发性难治性恶性淋巴瘤的临床观察. 夏一军等.浙江实用医学，第6期. 2000 |
| 国产乌苯美司联合化疗治疗复发性难治性恶性淋巴瘤的临床观察. 夏一军等.浙江实用医学，第6期. 2000 * |
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| CN1706373A (en) | 2005-12-14 |
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