CN1449756A - Difenidol Hydrochloride oral disintegrating tablet and preparation process thereof - Google Patents
Difenidol Hydrochloride oral disintegrating tablet and preparation process thereof Download PDFInfo
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- CN1449756A CN1449756A CN 03119043 CN03119043A CN1449756A CN 1449756 A CN1449756 A CN 1449756A CN 03119043 CN03119043 CN 03119043 CN 03119043 A CN03119043 A CN 03119043A CN 1449756 A CN1449756 A CN 1449756A
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- difenidol hydrochloride
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- hydrochloride oral
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Abstract
The difenidol hydrochloride oral disintegrant tablet includes difenidol hydrochloride, solid body disperse carrier, filling agent, disintegrant, effervescent agent, corrective agent and lubricating agent. Said invention adopts the effervescent principle, at the same time directly adds disintegrant in the prescription so as to attain the effect of quick disintegration. Its process is simple, can use conventional tablet preparation equipment to produce said invented tablet, its disitegration time is about 1-50 sec. so that it is favorable for dissolution and absorption or medicine.
Description
Technical field
The invention belongs to pharmaceutical preparation, relate to the oral cavity disintegration tablet dosage form, relate in particular to and a kind ofly adopt the direct compression process tabletting and have the difenidol hydrochloride oral disintegrant tablet of rapid release effect.
Background technology
Difenidol hydrochloride (difcnidol hydrochloride) chemical name is α, α-diphenyl-1-piperidine butanol hydrochlorate, has another name called diphenidol, diphenidol, difenidol etc., is a non-phenothiazines medicine.This product has intensive town to tell effect, it is incomplete by improving awl end tremulous pulse blood supply, adjust vestibule, the dysautonomia impulsion, suppress vomiting center, improve effect such as nystagmus and reach vertigo and antiemetic effect, the vomiting after dizzy, the vomiting that is used for that multiple disease causes (for example complete, the Meniere of tremulous pulse blood supply, autonomic nervous dysfunction, hypertension, hypotension, cervical vertigo, wound or drug intoxication at the bottom of the vertebra), the surgery anesthesia; Motion sickness (as airsick, seasick, carsickness) there are prevention and therapeutical effect.This product is with its determined curative effect, and characteristics such as few side effects are widely used clinically, on the medical market this medicine conventional tablet and two kinds of dosage forms of injection is only arranged at present.
Conventional tablet need be finished drug administration process by drinking-water and by swallowing act, this dosage form for some old peoples, child, to swallow inconvenient patient's compliance poor, use under some specific conditions is restricted (as lacking drinking water) or weak effect (need improve medication half an hour as doing the anti-kinetosis prophylactic, medication temporarily is weak effect then).Though drug administration by injection is rapid-action, must medical personnel assist, the patient uses inconvenience.
Oral cavity disintegration tablet (orally disintegrating tablet) is emerging in recent years novel form, compare with conventional tablet, this dosage form need not water and also need not to chew, medicine places on the tongue, after meeting the rapid disintegrate of saliva, borrow swallowing act to go into the stomach onset, also can place the Sublingual, medicine absorbs onset by mucosa after the disintegrate rapidly.This dosage form is particularly suitable for some old peoples, child, swallow inconvenient patient or the hydropenia condition of going out under patient take, and have the characteristics rapid-action, that bioavailability is high.
Summary of the invention
The present invention fully takes into account the deficiency that above-mentioned prior art exists, and a kind of preparation technology is simple, taking convenience and provide to people, rapid-action to indication, reach the peak early, the tangible difenidol hydrochloride oral disintegrant tablet preparation of curative effect.
The present invention is to provide the difenidol hydrochloride oral disintegrant tablet preparation, pharmaceutical formulation of the present invention is made up of following component by weight:
Difenidol hydrochloride 2-50
Solid dispersion carrier 1-10
Filler 5-80
Disintegrating agent 5-30
Effervescent 5-25
Correctives 1-20
Lubricant 0.3-3
Fluidizer 0.3-3
The solid dispersion carrier that the present invention proposes can be selected polyvinylpyrrolidone (PVP), Polyethylene Glycol (PEG6000, PEG4000) and composition thereof.
Filler can be selected microcrystalline Cellulose (MCC), dextrin, lactose, starch in the preparation of the present invention.
Disintegrating agent can be selected carboxymethyl starch sodium (CMC-Na) in the preparation of the present invention, low-substituted hydroxypropyl methylcellulose (L-HPC), crospolyvinylpyrrolidone (PPVP), cross-linking sodium carboxymethyl cellulose and composition thereof.
Effervescent can be selected the mixture of citric acid or citric acid and sodium bicarbonate in the preparation of the present invention.
Correctives can be selected natural or artificial sweetening agents such as aspartame, mannitol, stevioside, erythritol in the prescription that the present invention proposes.
Lubricant can be selected magnesium stearate, Stepanol MG, Pulvis Talci etc. in the preparation of the present invention.
Fluidizer can be selected micropowder silica gel, Cab-O-sil, Arosil and hydrated sodium aluminosilicate etc. in the preparation of the present invention.
The preparation of difenidol hydrochloride oral disintegrant tablet of the present invention is: with Mentholum, stevioside, principal agent porphyrize is respectively crossed 80 mesh sieves, stevioside and principal agent mix homogeneously; Microcrystalline Cellulose, citric acid, sodium bicarbonate, crospolyvinylpyrrolidone, polyvinylpyrrolidone are crossed 80 mesh sieves respectively, take by weighing respectively and add mixing in the principal agent that is mixed with in the stevioside successively, the magnesium stearate, the micropowder silica gel that add recipe quantity more respectively, the mixing that sieves carries out the intermediate content detection.Determine the heavy back of sheet tabletting, promptly get oral cavity quick disintegrating slice.
The present invention is as gastrointestinal drug disintegrate and masking agents bitterness and disagreeable taste rapidly, solved deficiency of the prior art preferably, some old peoples, child are swallowed the inconvenient patient of medicine or go out to lack drinking water and the patient of medication temporarily, be undoubtedly Gospel when taking medicine.This pharmaceutical dosage form is the compacting preparation with suitable stiffness, and its suitable stiffness is meant can disruptive enough hardness in preparation and transportation.When taking, medicine is contained in does not need moisture just fully disintegrate in the oral cavity in the mouth, and the time of its disintegrate just can finish in second at 1-50.
Preparation of the present invention can use conventional tablet pharmaceutical equipment to produce and use the pressing process preparation, avoids overlapping investment, and its processing technology is simple, prescription is unique, can give full play to drug effect, has the excellent popularization prospect.
Specific embodiment
Embodiment 1
With the active constituents of medicine difenidol hydrochloride is principal agent, and other composition is that adjuvant is prepared fast disintegrating tablet, and pharmaceutical formulation of the present invention is made up of following component by weight:
A, difenidol hydrochloride 25g
B, microcrystalline Cellulose 12g
C, crospolyvinylpyrrolidone 8.4g
D, citric acid 5.6g
E, sodium bicarbonate 4g
F, polyvinylpyrrolidone 1.2g
G, stevioside 2.8g
H, micropowder silica gel 0.4g
I, magnesium stearate 0.4g
This dosage form can be used conventional tablet pharmaceutical equipment to produce and use the pressing process preparation, and concrete preparation method is as described below: with stevioside, principal agent respectively porphyrize cross 80 mesh sieves, stevioside and principal agent mix homogeneously; Microcrystalline Cellulose, citric acid, sodium bicarbonate, crospolyvinylpyrrolidone, polyvinylpyrrolidone are crossed 80 mesh sieves respectively, take by weighing respectively successively by recipe quantity and to add mixing in the principal agent that is mixed with in the stevioside, the magnesium stearate, the micropowder silica gel that add recipe quantity more respectively, the mixing that sieves carries out the intermediate content detection.Determine the heavy back of sheet tabletting, promptly get oral cavity quick disintegrating slice.
Embodiment 2
Pharmaceutical formulation of the present invention is made up of following component by weight:
A, difenidol hydrochloride 25g
B, microcrystalline Cellulose 12g
C, citric acid 5.6g
D, sodium bicarbonate 4g
E, carboxymethyl starch sodium 8.4g
F, polyvinylpyrrolidone 1.2g
G, stevioside 2.8g
H, micropowder silica gel 0.4g
I, magnesium stearate 0.4g
This dosage form can be used conventional tablet pharmaceutical equipment to produce and use the pressing process preparation, and concrete preparation method is as described below: with stevioside, principal agent respectively porphyrize cross 80 mesh sieves, stevioside and principal agent mix homogeneously; Microcrystalline Cellulose, citric acid, sodium bicarbonate, polyvinylpyrrolidone are crossed 80 mesh sieves respectively, take by weighing respectively according to quantity and add mixing in the principal agent that is mixed with in the stevioside successively, the magnesium stearate, the micropowder silica gel that add recipe quantity more respectively, the mixing that sieves carries out the intermediate content detection.Determine the heavy back of sheet tabletting, promptly get oral cavity quick disintegrating slice.
Embodiment 3
Pharmaceutical formulation of the present invention is made up of following component by weight:
A, difenidol hydrochloride 25g
B, microcrystalline Cellulose 12g
C, crospolyvinylpyrrolidone 8.4g
D, citric acid 4.4g
E, sodium bicarbonate 3.2g
F, polyvinylpyrrolidone 1.2g
G, stevioside 2.8g
H, micropowder silica gel 0.4g
I, magnesium stearate 0.4g
This dosage form can be used conventional tablet pharmaceutical equipment to produce and use the pressing process preparation, and concrete preparation method is as described below: with stevioside, principal agent respectively porphyrize cross 80 mesh sieves, stevioside and principal agent mix homogeneously; Microcrystalline Cellulose, citric acid, sodium bicarbonate, crospolyvinylpyrrolidone, polyvinylpyrrolidone are crossed 80 mesh sieves respectively, take by weighing respectively according to quantity and add mixing in the principal agent that is mixed with in the stevioside successively, the magnesium stearate, the micropowder silica gel that add recipe quantity more respectively, the mixing that sieves carries out the intermediate content detection.Determine the heavy back of sheet tabletting, promptly get oral cavity quick disintegrating slice.
The disintegration of the foregoing description, slice, thin piece hardness, dissolution numerical value is as follows
| Disintegration | Slice, thin piece hardness | Dissolution | |
| Implement 1 example | ? ? ??30s | ? ? ??1.8-2.0kg | 45min stripping quantity in sodium chloride, hydrochloric acid solution is 95.18% |
| Implement 2 examples | ??45s-1min | ??1.8-2.0kg | 45min stripping quantity in sodium chloride, hydrochloric acid solution is 96.00% |
| Implement 3 examples | ??40s-1min | ??1.8-2.0kg | 45min stripping quantity in sodium chloride, hydrochloric acid solution is 97.42% |
Claims (9)
1, a kind of difenidol hydrochloride oral disintegrant tablet preparation, the dosage form that it is characterized in that said preparation is an oral cavity disintegration tablet, its prescription is made up of following component by weight:
Difenidol hydrochloride 2-50
Solid dispersion carrier 1-10
Filler 5-80
Disintegrating agent 5-30
Effervescent 5-25
Correctives 1-20
Lubricant 0.3-3
Fluidizer 0.3-3
2, difenidol hydrochloride oral disintegrant tablet preparation as claimed in claim 1 is characterized in that: the solid dispersion carrier can select polyvinylpyrrolidone (PVP), Polyethylene Glycol (PEG6000, PEG4000) and composition thereof.
3, difenidol hydrochloride oral disintegrant tablet preparation as claimed in claim 1 is characterized in that: filler can be selected microcrystalline Cellulose (MCC), dextrin, lactose, starch.
4, difenidol hydrochloride oral disintegrant tablet preparation as claimed in claim 1 is characterized in that: disintegrating agent can be selected carboxymethyl starch sodium (CMS-Na), low-substituted hydroxypropyl methylcellulose (L-HPC), crospolyvinylpyrrolidone (PPVP) and composition thereof.
5, difenidol hydrochloride oral disintegrant tablet preparation as claimed in claim 1, it is characterized in that: effervescent can be selected the mixture of citric acid or citric acid and sodium bicarbonate.
6, difenidol hydrochloride oral disintegrant tablet preparation as claimed in claim 1 is characterized in that: correctives can be selected aspartame, mannitol, stevioside, erythritol is natural or artificial sweetening agent.
7, difenidol hydrochloride oral disintegrant tablet preparation as claimed in claim 1, it is characterized in that: lubricant can be selected magnesium stearate, Stepanol MG, Pulvis Talci.
8, difenidol hydrochloride oral disintegrant tablet preparation as claimed in claim 1, it is characterized in that: fluidizer can be selected micropowder silica gel, Cab-O-sil, Arosil and hydrated sodium aluminosilicate.
9, a kind of preparation method of difenidol hydrochloride oral disintegrant tablet preparation is characterized in that: concrete preparation method is as described below: with correctives, principal agent respectively porphyrize cross 80 mesh sieves, correctives and principal agent mix homogeneously; Filler, effervescent, disintegrating agent are crossed 80 mesh sieves respectively, take by weighing respectively and add mixing in the principal agent that is mixed with correctives successively, add lubricant, fluidizer more respectively, mixing sieves, carry out the intermediate content detection, determine the heavy back of sheet tabletting, or, promptly get oral cavity quick disintegrating slice with tabletting after the wet granulation drying.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03119043 CN1202825C (en) | 2003-04-30 | 2003-04-30 | Difenidol Hydrochloride oral disintegrating tablet and preparation process thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03119043 CN1202825C (en) | 2003-04-30 | 2003-04-30 | Difenidol Hydrochloride oral disintegrating tablet and preparation process thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1449756A true CN1449756A (en) | 2003-10-22 |
| CN1202825C CN1202825C (en) | 2005-05-25 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03119043 Expired - Fee Related CN1202825C (en) | 2003-04-30 | 2003-04-30 | Difenidol Hydrochloride oral disintegrating tablet and preparation process thereof |
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| Country | Link |
|---|---|
| CN (1) | CN1202825C (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005063267A1 (en) * | 2003-12-31 | 2005-07-14 | Beijing Kexin Bicheng Medical Technology Development Co., Ltd. | The oral disintegratable tablet of ginkgo leaves |
| CN107213124A (en) * | 2017-05-04 | 2017-09-29 | 广西大海阳光药业有限公司 | A kind of preparation of suppression therapy motion sickness and preparation method thereof |
| CN108283625A (en) * | 2018-04-26 | 2018-07-17 | 江苏四环生物制药有限公司 | A kind of preparation method of difenidol hydrochloride piece |
-
2003
- 2003-04-30 CN CN 03119043 patent/CN1202825C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005063267A1 (en) * | 2003-12-31 | 2005-07-14 | Beijing Kexin Bicheng Medical Technology Development Co., Ltd. | The oral disintegratable tablet of ginkgo leaves |
| CN107213124A (en) * | 2017-05-04 | 2017-09-29 | 广西大海阳光药业有限公司 | A kind of preparation of suppression therapy motion sickness and preparation method thereof |
| CN108283625A (en) * | 2018-04-26 | 2018-07-17 | 江苏四环生物制药有限公司 | A kind of preparation method of difenidol hydrochloride piece |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1202825C (en) | 2005-05-25 |
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