CN1528273A - Analgesic tramadol hydrochloride oral disintegrating tablet and preparing method thereof - Google Patents
Analgesic tramadol hydrochloride oral disintegrating tablet and preparing method thereof Download PDFInfo
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- CN1528273A CN1528273A CNA200310109622XA CN200310109622A CN1528273A CN 1528273 A CN1528273 A CN 1528273A CN A200310109622X A CNA200310109622X A CN A200310109622XA CN 200310109622 A CN200310109622 A CN 200310109622A CN 1528273 A CN1528273 A CN 1528273A
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- tramadol hydrochloride
- mannitol
- analgesic
- ultram
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Abstract
The present invention relates to an analgesic tramadol hydrochloride oral disintegrant tablet. It is made up by using main medicine tramadol hydrochloride and auxiliary material gelatin and/or mannitol and/or aspartame and/or glucose and/or microcrystal cellulose and/or crosslinked povidone and essence, etc. and adopting freeze-drying or coating, granulating and pressing processes. When it is taken in, it has no need of drinking water, it can be quickly disintegrated in oral cavity, and can be used for curing acute and chronic pain, moderate and light pain due to cancer, pain due to fracture and pain after various operations and toothache, and can obtain good therapeutic effect.
Description
Technical field
The present invention relates to pharmaceutical, specifically analgesic Ultram oral cavity disintegration tablet and preparation method thereof.
Background technology
Tramadol hydrochloride is a 4-phenylpiperidine analgesic, because advantage such as low toleration of the strong addiction of its analgesic activity and dependency be low, and be widely used in clinical.This product is the non-opium central analgesics, though also can combine with opiate receptor, its affinity is very weak, and the affinity of μ receptor is equivalent to 1/6000 of morphine, only is 1/25 of μ receptor to the affinity of κ and δ receptor.Tramadol hydrochloride is a raceme, its (+) enantiomer acts on opiate receptor, (-) enantiomer then suppresses the outstanding reuptake to norepinephrine of neuron, and the outer 5-hydroxy tryptamine concentration of increase neuron, thereby influence pain sensation transmission and produce analgesic activity, its action intensity is 1/8～1/10. of a morphine
Oral cavity disintegration tablet of the present invention, rapid-action except having, absorb fully, the residual characteristics such as few of gastrointestinal, the advantage that taking convenience is more arranged, it only need get final product rapid disintegrate or dissolving in tens seconds in the oral cavity, need not drink water, can finish with swallowing act and to take medicine, be particularly useful for old people and women, child patient.
The present invention is easy to popularize, and formulation and technology is suitable, and its cost and ordinary tablet are close, even lower.The dosage form of the present domestic listing of tramadol hydrochloride has tablet, capsule, slow releasing tablet and injection, conventional tablet and capsule release are rapid inadequately, though and injection can be brought into play drug effect rapidly but administration inconvenience, and life-time service causes big painful to the patient, oral cavity disintegration tablet of the present invention has then been avoided this shortcoming.
Summary of the invention
The object of the present invention is to provide a kind of convenience, obvious results oral cavity disintegration tablet and preparation method thereof of taking medicine.
The present invention can realize by following measure:
One, realizing the quickly disintegrated while of oral cavity, covering the bitterness of tramadol hydrochloride, adopting the freeze drying technology film-making by the taste of adjuvant.By principal agent tramadol hydrochloride and adjuvant by 0.5～2: 8～15 form, every hydrochloric tramadol 25-250mg.Its prescription is composed as follows:
Mannitol 5-80%
Sucrose 5-80%
Gelatin 0.1-10%
Hydroxyethyl-cellulose 0.1-7.5%
Spice 0.1-1.0%
Crucial adjuvant wherein can be: gelatin and/or mannitol and/or A Siba sweet and/or glucose and/or microcrystalline Cellulose and/or polyvinylpolypyrrolidone and essence.Preparation method is: earlier the principal agent tramadol hydrochloride is suspended in the hydroxyethyl cellulose aqueous solution, form solution A, with gelatin, spice, mannitol and sucrose mixed dissolution, form solution B again, it is mixed that the formation solution A is added solution B, and add suitable quantity of water dilution, and abundant mixing, join sharp freezing in the mould, be put into evacuation in the freeze dryer, ice sublimes up into material bone dry, press seal.
Two, realizing the quickly disintegrated while of oral cavity, covering the bitterness of tramadol hydrochloride, adopting the compact technique film-making by coating method.By principal agent tramadol hydrochloride and adjuvant by 0.5～2: 8～15 form, every hydrochloric tramadol 25-250mg.Its prescription is composed as follows:
Ethyl cellulose 2-10%
Polyvinylpyrrolidone 0.5-1.5%
Silicon dioxide 0.5-1.5%
Granular mannitol 15-40%
Mannitol powder 20-40%
Crospolyvinylpyrrolidone 5-15%
Fructus Citri Limoniae essence 0.2-2.0%
The sweet 1-6% of A Siba
Crucial adjuvant wherein can be: gelatin and/or mannitol and/or A Siba sweet and/or glucose and/or microcrystalline Cellulose and/or polyvinylpolypyrrolidone and essence.Preparation method is: with principal agent tramadol hydrochloride powder is principal agent, with ethyl cellulose, polyvinylpyrrolidone and silicon dioxide is coating material, adopt coating taste masking technology, make the coated granule of crystalline particulate tramadol hydrochloride, again with other adjuvant granular mannitol, mannitol powder, crospolyvinylpyrrolidone, Fructus Citri Limoniae essence, the sweet mix homogeneously of A Siba of mix homogeneously, add tabletting behind the lubricant.
The oral cavity disintegration tablet that the present invention makes has following advantage:
Taking convenience: need not when taking to drink water, it is rapid disintegrate that slice, thin piece is put into mouth, enters digestive tract with natural swallowing act.
Gastrointestinal side effect is little: compare with common oral solid formulation, enter gastrointestinal tract after the oral cavity disintegration tablet disintegrate and disperse, extensively cover gastrointestinal mucosa rapidly, significantly alleviate the gastrointestinal upset that tablet causes in Local Residence Time length.
Production cost is low: this tramadol hydrochloride oral cavity disintegration tablet adopts tablet adjuvant commonly used and common film-making prepared, and technology is simple, and production cost is low.
Good in economic efficiency: the novel pharmaceutical formulation exploitation is a fund input minimum in the drug research and development field, a kind of development mode that risk is minimum.This product is 5 classes (change dosage form) new drugs, can exempt to do clinical research, so the lead time is short, and investment repayment is fast.
The specific embodiment
Enumerate four embodiment below, the present invention is further specified.
Embodiment 1
Principal agent tramadol hydrochloride 50g is suspended in the hydroxyethyl-cellulose 75g aqueous solution, form solution A, press the prescription in the adjuvant 1, then 25g gelatin, 645g mannitol, 5g spice and 250g sucrose mixed dissolution, form solution B, it is mixed that the formation solution A is added solution B, and add the suitable quantity of water dilution, and abundant mixing, join sharp freezing in the mould, be put into evacuation in the freeze dryer, ice sublimes up into material bone dry, press seal, packing.
The gross weight of five kinds of adjuvants is 1kg, makes 1000, every adjuvant 1g, principal agent tramadol hydrochloride 50mg.
Embodiment 2
Principal agent tramadol hydrochloride 100g is suspended in the hydroxyethyl-cellulose 100g aqueous solution, form solution A, press the prescription in the adjuvant 1, then 45g gelatin, 800g mannitol, 10g spice and 300g sucrose mixed dissolution, form solution B, it is mixed that the formation solution A is added solution B, and add the suitable quantity of water dilution, and abundant mixing, join sharp freezing in the mould, be put into evacuation in the freeze dryer, ice sublimes up into material bone dry, press seal, packing.
Embodiment 3
Prescription:
Tramadol hydrochloride 50g
Ethyl cellulose 17.45g
Polyvinylpyrrolidone 4.40g
Silicon dioxide 3.65g
Crospolyvinylpyrrolidone 50.0g
Granular mannitol 173.0g
Mannitol powder 174.0g
Fructus Citri Limoniae essence 5.0g
The sweet 20.0g of A Siba
Magnesium stearate 2.0g
Make 1000
Method for making:
1. ethyl cellulose is dissolved in the ethanol, adds polyvinylpyrrolidone and 1/3 amount silicon dioxide while stirring, continue to stir (in the whole granulating coated process, this suspension will keep stirring).
2. will sieve good tramadol hydrochloride raw material and 2/3 amount silicon dioxide is put into fluid bed, heating and the suspension for preparing is injected on the raw material under air flow is granulated.
3. be sprayed onto about 1/3 when amount when suspension, take out the raw material grain, sieve with 500 μ m and sieve.
4. and then put into fluid bed, heating and remaining suspension is injected on the raw material grain coating under air flow.
5. after the coating operation is finished, 60 ℃ of dryings 1 hour.
6. take out above-mentioned tramadol hydrochloride coated granule, sieve with 710 μ m sieve.
7. with recipe quantity granular mannitol and mannitol powder, crospolyvinylpyrrolidone, Fructus Citri Limoniae essence, the sweet mix homogeneously of A Siba.
8. in 7, add the recipe quantity magnesium stearate, mixed 2 minutes.
9. the mixed material in 8 is poured in the tablet machine hopper, adjustment sheet heavily reaches pressure, tabletting.
10. pack labeling after the assay was approved.
Embodiment 4
Prescription:
Tramadol hydrochloride 100g
Ethyl cellulose 35.0g
Polyvinylpyrrolidone 8.0g
Silicon dioxide 6.5g
Crospolyvinylpyrrolidone 60.0g
Granular mannitol 180.0g
Mannitol powder 182.0g
Fructus Citri Limoniae essence 5.0g
The sweet 30.0g of A Siba
Magnesium stearate 2.5g
Make 1000
Method for making:
1. ethyl cellulose is dissolved in the ethanol, adds polyvinylpyrrolidone and 1/3 amount silicon dioxide while stirring, continue to stir (in the whole granulating coated process, this suspension will keep stirring).
2. will sieve good tramadol hydrochloride raw material and 2/3 amount silicon dioxide is put into fluid bed, heating and the suspension for preparing is injected on the raw material under air flow is granulated.
3. be sprayed onto about 1/3 when amount when suspension, take out the raw material grain, sieve with 500 μ m and sieve.
4. and then put into fluid bed, heating and remaining suspension is injected on the raw material grain coating under air flow.
5. after the coating operation is finished, 60 ℃ of dryings 1 hour.
6. take out above-mentioned tramadol hydrochloride coated granule, sieve with 710 μ m sieve.
7. with recipe quantity granular mannitol and mannitol powder, crospolyvinylpyrrolidone, Fructus Citri Limoniae essence, the sweet mix homogeneously of A Siba.
8. in 7, add the recipe quantity magnesium stearate, mixed 2 minutes.
9. the mixed material in 8 is poured in the tablet machine hopper, adjustment sheet heavily reaches pressure, tabletting.
10. pack labeling after the assay was approved.
More than enumerate three embodiment, tramadol hydrochloride 50mg, 100mg be totally two specifications, and when preparing this product, every sheet is heavy variable, drug content 25-250mg/ sheet.
Product of the present invention is used for acute and chronic pain, mild or moderate cancer pain, fracture or various postoperative pain, toothache.
Claims (7)
1. analgesic Ultram, it is characterized in that said tablet is said oral cavity disintegration tablet on the pharmaceutics (Orally Disintegrating Tablets), be made up of principal agent tramadol hydrochloride and pharmaceutic adjuvant, every contains principal agent tramadol hydrochloride 25-250mg.
2. analgesic Ultram according to claim 1 is characterized in that said oral cavity disintegration tablet does not need water in the oral cavity, also need not to chew, and meeting saliva can disintegrate or dissolving; External when carrying out disintegration time mensuration, in the water 2ml, 37 ℃ ± 0.5 ℃ of temperature, static method can disintegrate in 30 seconds, and the granularity after the disintegrate is less than 710 μ m.
3. analgesic Ultram according to claim 1 is characterized in that said pharmaceutic adjuvant comprises: gelatin and/or mannitol and/or A Siba sweet and/or glucose and/or microcrystalline Cellulose and/or polyvinylpolypyrrolidone and essence.
4. analgesic Ultram according to claim 1 is characterized in that said pharmaceutic adjuvant and content (percentage by weight) scope is:
Mannitol 5-80%
Sucrose 5-80%
Gelatin 0.1-10%
Hydroxyethyl-cellulose 0.1-7.5%
Spice 0.1-1.0%
The part by weight of principal agent tramadol hydrochloride and adjuvant is 0.5～2: 8～15.
5. analgesic Ultram according to claim 1 is characterized in that said pharmaceutic adjuvant and content (percentage by weight) scope is:
Ethyl cellulose 2-10%
Polyvinylpyrrolidone 0.5-1.5%
Silicon dioxide 0.5-1.5%
Granular mannitol 15-40%
Mannitol powder 20-40%
Crospolyvinylpyrrolidone 5-15%
Fructus Citri Limoniae essence 0.2-2.0%
The sweet 1-6% of A Siba
The part by weight of principal agent tramadol hydrochloride and adjuvant is 0.5～2: 8～15.
6. the preparation method of the described analgesic Ultram of claim 4, it is characterized in that earlier the principal agent tramadol hydrochloride being suspended in the hydroxyethyl cellulose aqueous solution, form solution A, again with gelatin, spice, mannitol and sucrose mixed dissolution, form solution B, it is mixed that the formation solution A is added solution B, and add the suitable quantity of water dilution, and abundant mixing, join sharp freezing in the mould, be put into evacuation in the freeze dryer, ice sublimes up into material bone dry, press seal.
7. the preparation method of the described analgesic Ultram of claim 5, it is characterized in that with principal agent tramadol hydrochloride powder be principal agent, with ethyl cellulose, polyvinylpyrrolidone and silicon dioxide is coating material, adopt coating taste masking technology, make the coated granule of crystalline particulate tramadol hydrochloride, again with other adjuvant granular mannitol, mannitol powder, crospolyvinylpyrrolidone, Fructus Citri Limoniae essence, the sweet mix homogeneously of A Siba of mix homogeneously, add tabletting behind the lubricant.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200310109622XA CN1528273A (en) | 2003-10-21 | 2003-10-21 | Analgesic tramadol hydrochloride oral disintegrating tablet and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200310109622XA CN1528273A (en) | 2003-10-21 | 2003-10-21 | Analgesic tramadol hydrochloride oral disintegrating tablet and preparing method thereof |
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| CN1528273A true CN1528273A (en) | 2004-09-15 |
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| CNA200310109622XA Pending CN1528273A (en) | 2003-10-21 | 2003-10-21 | Analgesic tramadol hydrochloride oral disintegrating tablet and preparing method thereof |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100348180C (en) * | 2004-12-24 | 2007-11-14 | 河南大学 | Oral disintegration tablet of tramadol hydrochloride and preparation method |
| CN100404025C (en) * | 2005-01-14 | 2008-07-23 | 信谊药厂 | Oral disintegrating tablet containing tramadol hydrochloride and acetaminopher, and its preparation method |
| CN101152190B (en) * | 2006-09-29 | 2010-06-23 | 北京德众万全药物技术开发有限公司 | Orally disintegrating tablets of adefovir dipivoxil and method for preparing the same |
| CN102451164A (en) * | 2010-10-22 | 2012-05-16 | 量子高科（北京）研究院有限公司 | Analgesic oral cavity disintegrating tablet and preparation method thereof |
| CN104739832A (en) * | 2015-03-30 | 2015-07-01 | 南京医科大学 | New application of ligustrazine in field of analgesic drugs |
-
2003
- 2003-10-21 CN CNA200310109622XA patent/CN1528273A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100348180C (en) * | 2004-12-24 | 2007-11-14 | 河南大学 | Oral disintegration tablet of tramadol hydrochloride and preparation method |
| CN100404025C (en) * | 2005-01-14 | 2008-07-23 | 信谊药厂 | Oral disintegrating tablet containing tramadol hydrochloride and acetaminopher, and its preparation method |
| CN101152190B (en) * | 2006-09-29 | 2010-06-23 | 北京德众万全药物技术开发有限公司 | Orally disintegrating tablets of adefovir dipivoxil and method for preparing the same |
| CN102451164A (en) * | 2010-10-22 | 2012-05-16 | 量子高科（北京）研究院有限公司 | Analgesic oral cavity disintegrating tablet and preparation method thereof |
| CN102451164B (en) * | 2010-10-22 | 2015-11-25 | 量子高科（北京）研究院有限公司 | A kind of analgesic oral cavity disintegrating tablet and preparation method thereof |
| CN104739832A (en) * | 2015-03-30 | 2015-07-01 | 南京医科大学 | New application of ligustrazine in field of analgesic drugs |
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