CN1682709A - Furosemide oral disintegration tablet and its preparing method - Google Patents
Furosemide oral disintegration tablet and its preparing method Download PDFInfo
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- CN1682709A CN1682709A CN 200410023915 CN200410023915A CN1682709A CN 1682709 A CN1682709 A CN 1682709A CN 200410023915 CN200410023915 CN 200410023915 CN 200410023915 A CN200410023915 A CN 200410023915A CN 1682709 A CN1682709 A CN 1682709A
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- furosemide
- oral cavity
- disintegration tablet
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- cavity disintegration
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Abstract
The present invention provides a kind of orally disintegrated furosemide tablet and its preparation process. During taking the orally disintegrated furosemide tablet, there is no need of drinking water, and this makes the taking easy. The orally disintegrated furosemide tablet has the material pre-treated before tabletting so as to reduce the amount of water insoluble supplementary material. The orally disintegrated furosemide tablet has proper size and fast leaching rate, and may be produced with one conventional tabletting machine.
Description
Technical field
The present invention relates to a kind of diuretic oral cavity disintegration tablet and preparation method thereof that can be used for, relate to a kind of furosemide oral cavity disintegration tablet and preparation method thereof particularly.
Background technology
Furosemide, chemical name are the 2-[(2-furfuryl) amino]-5-(sulfamoyl)-4-chlorobenzoic acid.Furosemide is as a kind of diuretic, be used for the treatment of edema disease, hypertension, hyperpotassemia and hypercalcemia, dilutional hyponatremia, acute drug toxic poisoning clinically, the prophylaxis of acute renal failure, hypersecretion of antidiuretic hormone diseases (FUSAIMI PIAN description) such as (SIADH).At present the Frusemide oral preparation of listing has only FUSAIMI PIAN, and patient's drinking-water of suffering from above-mentioned disease is taken medicine and can be increased patient's burden, and therefore developing a kind of oral formulations that need not to drink water has crucial clinical meaning.
The preparation method that oral cavity disintegration tablet is commonly used is direct compression process and granulating tabletting process, but these two kinds of preparation methoies all need to use in a large number water-fast efficient disintegrating agent and the filler with disintegrate miscellaneous function, make that oral cavity disintegration tablet can residual insoluble matter after the disintegrate in mouth.Electrostatic force between little, mobile poor, the drug particles of the bulk density of furosemide raw material is strong in addition, need a large amount of mobile strong adjuvants to dilute, and the patient is relatively poor to the tablet compliance of large volume, therefore improve the drug loading of oral cavity disintegration tablet adjuvant, improve the mobile of principal agent and reduce the technological difficulties that supplementary product consumption becomes preparation furosemide oral cavity disintegration tablet.The inventor by adjusting adjuvant proportioning and take tabletting before preconditioning technique solved above-mentioned technical barrier, adopt common sheeting equipment just to prepare the heavy moderate oral cavity disintegration tablet of sheet, and solved low, the frangible problem of most oral cavity disintegration tablet hardness.
Summary of the invention
The invention provides a kind of furosemide oral cavity disintegration tablet.
The invention provides the preparation method of furosemide oral cavity disintegration tablet.
Furosemide oral cavity disintegration tablet provided by the invention comprises furosemide, filler, disintegrating agent and lubricant substantially, and its weight consists of furosemide 5-40%: filler 30-80%: disintegrating agent 5-25%: lubricant 0.1-5%.
Oral cavity disintegration tablet provided by the invention, filler can be selected from one or more in lactose, sucrose, microcrystalline Cellulose (MCC), pregelatinized Starch, mannitol, sorbitol, the dextrin; Disintegrating agent can be selected from one or more in low-substituted hydroxypropyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa), carboxymethyl starch sodium (CMS-Na), crosslinked polyethylene pyrrole Lip river alkane ketone (PVPP), the crosslinked carboxymethyl fecula sodium (CCMS-Na); Disintegrating agent is selected from one or more in sodium carbonate, sodium bicarbonate, potassium bicarbonate, potassium carbonate, citric acid, the tartaric acid; Lubricant can be selected from one or more in magnesium stearate, Polyethylene Glycol, Stepanol MG, micropowder silica gel, the Pulvis Talci.
Oral cavity disintegration tablet provided by the invention, it also can contain in adhesive, solubilizing agent, the correctives one or more.Adhesive can be polyethylene pyrrole Lip river alkane ketone (PVP), hydroxypropyl methylcellulose battalion (HPMC) or its combination; Solubilizing agent can be one or more in polyethylene pyrrole Lip river alkane ketone (PVP), poloxamer, tween, the Polyethylene Glycol; Correctives can be aspartame, stevioside or its combination, and the weight ratio of correctives is 0.01-1.0%.。
Preparation method provided by the invention is direct compression or pelletizing press sheet, but all adopts the medicine method for pretreating.The recipe quantity furosemide is mixed with the filler or the disintegrating agent of a small amount of good fluidity in the prescription, add an amount of short chain alcohol as wetting agent moistening said mixture, under moisture state, fully mix principal agent and mobile adjuvant, the amount that adds alcohol is can be made into suitable soft just degree of being, with above-mentioned moistening material intensive drying in air dry oven, sieving for standby.Short chain alcohol is volatile ethanol, isopropyl alcohol or its combination.
Direct compression process is prepared as follows: standby with crossing 80 mesh sieves after each adjuvant drying, take by weighing recipe quantity adjuvant and above-mentioned pretreated principal agent and adjuvant mixture respectively, fully the laggard interline body burden of mix homogeneously is measured, and with conventional tablet machine tabletting, the hardness of control tablet is 2-5kg/cm
2, get final product with common bubble-cap formula packaging material packing.
The concrete preparation method of pressed disc method after granulating: each adjuvant is crossed 80 mesh sieves, take by weighing recipe quantity adjuvant and above-mentioned pretreated principal agent and adjuvant mixture respectively, behind the mix homogeneously, add binding agent and make suitable soft, granulation, dry, granulate, carry out the intermediate assay, with conventional tablet machine tabletting, the hardness of control tablet is 2-4kg/cm
2, get final product with common bubble-cap formula packaging material packing.Pelletizing press sheet also can not adopt pretreated adjuvant, according to preparation prescription and the preparation of conventional granulating tabletting process.
Oral cavity disintegration tablet provided by the invention, dissolution rate is fast, and is rapid-action, and the granule after the disintegrate can pass through the screen cloth of 0.425 μ m fully.
The oral cavity disintegration tablet of the present invention's preparation can use conventional tablet manufacturing equipment to produce, and the tablet of preparation has suitable hardness, can use conventional plastic-aluminum bubble-cap formula packing, is not transported the restriction with condition of storage.When oral cavity disintegration tablet is taken, medicine is placed on the lingual surface, does not need water, also need not to chew, medicine can borrow swallowing act to go into the stomach onset in 1-60 disintegrate fully in second after the medicine disintegrate, greatly facilitate the emergency case patient's medication under part dysphagia or the special environment.
Figure: the comparison of furosemide conventional tablet and oral cavity disintegration tablet stripping curve.
Specific embodiment
Preparation example 1
| Furosemide | ????10％ |
| Microcrystalline Cellulose | ????45％ |
| The direct compression lactose | ????34.2％ |
| The low-substituted hydroxypropyl methylcellulose | ????10％ |
| Aspartame | ????0.2％ |
| Magnesium stearate | ????0.5％ |
Preparation: the furosemide that takes by weighing recipe quantity mixes with 20% microcrystalline Cellulose, adds an amount of moistening of dehydrated alcohol, abundant mixing principal agent and mobile adjuvant under moisture state.With above-mentioned moistening material intensive drying in 50 ℃ of air dry ovens, it is standby to cross 80 mesh sieves.Each adjuvant is dry in advance, and 80 mesh sieves are standby excessively.Take by weighing each adjuvant of residue by recipe quantity, furosemide and other adjuvant mix homogeneously after desire is handled.Measure intermediate content, tabletting behind the adding magnesium stearate mix homogeneously.
With the diameter is the scrobicula stamping of 6mm, the heavily about 100mg of sheet, and the control tablet hardness is at 2-5kg/cm
2Not adding jolting by disintegration time mensuration method shown in two appendix of pharmacopeia, to measure disintegration be 31 seconds, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Preparation example 2
| Furosemide | ????20％ |
| Microcrystalline Cellulose | ????35％ |
| Mannitol | ????29.9％ |
| Pregelatinized Starch | ????12％ |
| Cross-linking sodium carboxymethyl cellulose | ????12％ |
| 3.0% polyethylene pyrrole Lip river alkane ketone K30 alcoholic solution | In right amount |
| Aspartame | ????0.1％ |
| Magnesium stearate | ????0.5％ |
Preparation: it is standby that each composition is crossed 80 mesh sieves in advance.Take by weighing each composition by recipe quantity, with furosemide and other adjuvant mix homogeneously.Add the soft ability of an amount of system of 3.0% polyethylene pyrrole Lip river alkane ketone K30 alcoholic solution, 20 mesh sieves are granulated, 40 degree air dry oven oven dry, 18 mesh sieve granulate.Measure intermediate content, tabletting promptly behind the adding magnesium stearate mix homogeneously.
With the diameter is the scrobicula stamping of 6mm, the heavily about 100mg of sheet, and the control tablet hardness is at 2-4kg/cm
2, not adding jolting by two appendix disintegration time mensurations of pharmacopeia method, to measure disintegration be 51 seconds, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Preparation example 3
| Furosemide | ????15％ |
| Microcrystalline Cellulose | ????48％ |
| Sucrose | ????24.0％ |
| Crosslinked polyethylene pyrrole Lip river alkane ketone | ????10％ |
| Sodium bicarbonate | ????2.3％ |
| Citric acid | ????2.5％ |
| Aspartame | ????0.2％ |
| Pulvis Talci | ????0.5％ |
Preparation: the furosemide that takes by weighing recipe quantity mixes with 48% microcrystalline Cellulose, adds an amount of moistening of dehydrated alcohol, abundant mixing principal agent and mobile adjuvant under moisture state.With above-mentioned moistening material intensive drying in 50 ℃ of air dry ovens, it is standby to cross 80 mesh sieves.
Each adjuvant is dry in advance, and 80 mesh sieves are standby excessively.Take by weighing each adjuvant of residue by recipe quantity, furosemide and other adjuvant mix homogeneously after desire is handled.Measure intermediate content, tabletting behind the adding magnesium stearate mix homogeneously.
With the diameter is the scrobicula stamping of 6mm, the heavily about 100mg of sheet, and the control tablet hardness is at 2-5kg/cm
2, not adding jolting by disintegration time mensuration method shown in two appendix of pharmacopeia, to measure disintegration be 18 seconds, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Preparation example 4
| Furosemide | ????10％ |
| Microcrystalline Cellulose | ????30％ |
| Mannitol | ????37.2％ |
| The low-substituted hydroxypropyl methylcellulose | ????15％ |
| Potassium bicarbonate | ????2.3％ |
| Tartaric acid | ????2.7％ |
| Poloxamer | ????2％ |
| Aspartame | ????0.3％ |
| Magnesium stearate | ????0.5％ |
Preparation: the furosemide that takes by weighing recipe quantity mixes with 15% low substituted hydroxy-propyl methylcellulose, poloxamer is joined in the mixture of above-mentioned furosemide and adjuvant after with an amount of anhydrous alcohol solution, under moisture state, fully mix principal agent and mobile adjuvant.With above-mentioned moistening material intensive drying in 45 ℃ of air dry ovens, it is standby to cross 80 mesh sieves.
Each adjuvant is dry in advance, and 80 mesh sieves are standby excessively.Take by weighing each adjuvant of residue by recipe quantity, furosemide and other adjuvant mix homogeneously after desire is handled.Measure intermediate content, tabletting behind the adding magnesium stearate mix homogeneously.
With the diameter is the scrobicula stamping of 6mm, the heavily about 100mg of sheet, and the control tablet hardness is at 2-5kg/cm
2, not adding jolting by disintegration time mensuration method shown in two appendix of pharmacopeia, to measure disintegration be 35 seconds, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Preparation example 5
| Furosemide | ????40％ |
| Microcrystalline Cellulose | ????25％ |
| Mannitol | ????20％ |
| The low-substituted hydroxypropyl methylcellulose | ????14.0％ |
| Aspartame | ????0.1％ |
| Magnesium stearate | ????0.9％ |
Preparation: the furosemide that takes by weighing recipe quantity mixes with the microcrystalline Cellulose and the low substituted hydroxy-propyl methylcellulose of recipe quantity, adds an amount of moistening of dehydrated alcohol, fully mixes principal agent and above-mentioned adjuvant under moisture state.With above-mentioned moistening material intensive drying in 50 ℃ of air dry ovens, it is standby to cross 80 mesh sieves.
Each adjuvant is dry in advance, and 80 mesh sieves are standby excessively.Take by weighing each adjuvant of residue by recipe quantity, furosemide and other adjuvant mix homogeneously after desire is handled.Measure intermediate content, tabletting behind the adding magnesium stearate mix homogeneously.
With the diameter is the scrobicula stamping of 8mm, the heavily about 200mg of sheet, and the control tablet hardness is at 2-5kg/cm
2Not adding jolting by disintegration time mensuration method shown in two appendix of pharmacopeia, to measure disintegration be 53 seconds, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Claims (8)
1. a furosemide oral cavity disintegration tablet comprises furosemide, filler, disintegrating agent, lubricant substantially, and its weight consists of furosemide 5-40%: filler 30-80%: disintegrating agent 5-25%: lubricant 0.1-5%.
2. oral cavity disintegration tablet according to claim 1, filler can be selected from one or more in lactose, sucrose, microcrystalline Cellulose (MCC), pregelatinized Starch, mannitol, sorbitol, the dextrin; Disintegrating agent can be selected from one or more in low-substituted hydroxypropyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa), carboxymethyl starch sodium (CMS-Na), crosslinked polyethylene pyrrole Lip river alkane ketone (PVPP), the crosslinked carboxymethyl fecula sodium (CCMS-Na); In sodium carbonate, sodium bicarbonate, potassium bicarbonate, potassium carbonate, citric acid, the tartaric acid one or more; Lubricant can be selected from one or more in magnesium stearate, Polyethylene Glycol, Stepanol MG, micropowder silica gel, the Pulvis Talci.
3. oral cavity disintegration tablet according to claim 1 and 2, it also can contain in adhesive, solubilizing agent, the correctives one or more.
4. oral cavity disintegration tablet according to claim 3, adhesive can be polyethylene pyrrole Lip river alkane ketone (PVP), hydroxypropyl methylcellulose battalion (HPMC) or its combination; Solubilizing agent can be one or more in polyethylene pyrrole Lip river alkane ketone (PVP), poloxamer, tween, the Polyethylene Glycol; Correctives can be aspartame, stevioside or its combination, and the weight ratio of correctives is 0.01-1.0%.。
5. the preparation method of the arbitrary described oral cavity disintegration tablet of claim 1-4 is direct compression or pelletizing press sheet.
6. preparation method according to claim 5 is characterized by direct compression and pelletizing press sheet and all adopts the medicine method for pretreating.
7. preparation method according to claim 6, the medicine method for pretreating is that the furosemide of recipe quantity is mixed with the filler or the disintegrating agent of a small amount of good fluidity in the prescription, add an amount of short chain alcohol as wetting agent moistening said mixture, under moisture state, fully mix principal agent and mobile adjuvant, the amount that adds alcohol is can be made into suitable soft just degree of being, with above-mentioned moistening material intensive drying in air dry oven, sieving for standby.
8. preparation method according to claim 7, short chain alcohol can be volatile ethanol, isopropyl alcohol or its combination.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410023915 CN1682709A (en) | 2004-04-14 | 2004-04-14 | Furosemide oral disintegration tablet and its preparing method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410023915 CN1682709A (en) | 2004-04-14 | 2004-04-14 | Furosemide oral disintegration tablet and its preparing method |
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| CN1682709A true CN1682709A (en) | 2005-10-19 |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102512393A (en) * | 2011-12-19 | 2012-06-27 | 浙江华海药业股份有限公司 | Oral disintegrated tablet containing tolvaptan |
| CN104490753A (en) * | 2014-12-05 | 2015-04-08 | 海南卫康制药(潜山)有限公司 | Furosemide composition freeze-dried tablet and preparation method thereof |
| CN107157994A (en) * | 2017-06-09 | 2017-09-15 | 董鹏 | A kind of sublingual oral formulations of Torasemide |
| CN110538157A (en) * | 2019-09-10 | 2019-12-06 | 华益药业科技(安徽)有限公司 | furosemide tablet and preparation method thereof |
| CN120093702A (en) * | 2025-03-12 | 2025-06-06 | 思南县人民医院 | Compound furosemide tablet and preparation method thereof |
-
2004
- 2004-04-14 CN CN 200410023915 patent/CN1682709A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102512393A (en) * | 2011-12-19 | 2012-06-27 | 浙江华海药业股份有限公司 | Oral disintegrated tablet containing tolvaptan |
| CN104490753A (en) * | 2014-12-05 | 2015-04-08 | 海南卫康制药(潜山)有限公司 | Furosemide composition freeze-dried tablet and preparation method thereof |
| CN107157994A (en) * | 2017-06-09 | 2017-09-15 | 董鹏 | A kind of sublingual oral formulations of Torasemide |
| CN110538157A (en) * | 2019-09-10 | 2019-12-06 | 华益药业科技(安徽)有限公司 | furosemide tablet and preparation method thereof |
| CN120093702A (en) * | 2025-03-12 | 2025-06-06 | 思南县人民医院 | Compound furosemide tablet and preparation method thereof |
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