CN102488680B - Ibuprofen diphenhydramine dispersing tablet and preparation method thereof - Google Patents
Ibuprofen diphenhydramine dispersing tablet and preparation method thereof Download PDFInfo
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- CN102488680B CN102488680B CN 201110432646 CN201110432646A CN102488680B CN 102488680 B CN102488680 B CN 102488680B CN 201110432646 CN201110432646 CN 201110432646 CN 201110432646 A CN201110432646 A CN 201110432646A CN 102488680 B CN102488680 B CN 102488680B
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Abstract
The invention provides an ibuprofen diphenhydramine dispersing tablet, which consists of the following components in percentage by mass: 40 percent of ibuprofen, 5 percent of diphenhydramine hydrochloride or 7.6 percent of diphenhydramine citrate, 30-43 percent of a filler, 5-15 percent of a disintegrant, 2-8 percent of a bonding agent, 0.1-1 percent of a surfactant, 1.5-4 percent of a lubricating agent and 0.5-1.5 percent of a flavoring agent, wherein the filler is at least two of microcrystalline cellulose, pre-gelatinized starch, lactose and mannite; the disintegrant is cross-linked sodium carboxymethylcellulose and/or cross-linked polyvidone; the bonding agent is polyvidone K30; the surfactant is sodium dodecyl sulfate; the lubricating agent is magnesium stearate and superfine silica gel powder; and the flavoring agent is aspartame and steviosin. The invention further provides a preparation method of the dispersing tablet. The preparation method is easy and convenient to operate, has low cost, and is suitable for industrial production. An obtained product has stable and controllable quality, attractive appearance, good mouthfeel and proper hardness, is fully disintegrated in water at the temperature of 20+/-1 DEG C within 3 minutes, and passes through a No.2 sieve; and the medicament dissolvability is over 85 percent 30 minutes later.
Description
Technical field
The invention belongs to the pharmaceutics field, relate to a kind of pharmaceutical preparation, also relate to method of making preparation.
Background technology
Pain be numerous disease with symptom, also be a kind of disease with physiology-psychology-multiple characteristics such as society.The reason that causes pain is a lot, generally mainly cause by the noxious stimulation that causes tissue injury, as lancinate, noxious stimulation that mechanical irritation such as rod hits and electric current, strong acid, highly basic etc. cause.Pain is divided into sharp pain and dull pain again, and the pain sensation of sharp pain is stronger, and the persistent period is shorter, and for example twinge, angor, burning pain and electric shock appearance pain etc. are more common in the pain that wound, operation, inflammation, visceral injury and malignant tumor etc. cause; The pain sensation of dull pain is lighter, and the persistent period is longer, for example distending pain, vexed pain, ache and dull pain etc., be more common in the pain that neuralgia, chronic joint disease, muscle soft-tissue strain, chronic internal organs inflammation etc. cause.Sleep is the needed a kind of complete resting state of body allaying tiredness, is the neuroregulation process that the central nervous system initiatively produces.High-quality sleep is extremely important concerning the people.Sleep disorder even sleep disordered illness are like insomnia, can have a strong impact on people's life, study and work with the dyskinesia of breathing relevant sleep disorder, non-respiratory disorder property excessive daytime is drowsiness, sleep disorder, parasomnias, sleep due to the circadian rhythm disorder is correlated with, independent syndrome etc.Recently discover that interact between pain and the sleep disorder, influence each other, pain causes sleep disorder the most easily, and sleep disorder can enhancing body to the sensitivity of pain, thereby form a vicious cycle.
Ibuprofen (ibuprofen); Chemistry 2-(4-isobutyl phenenyl) propanoic acid by name; Have analgesia, antiinflammatory and antipyretic effect; Main through suppressing the synthetic of epoxidase minimizing prostaglandin; Alleviate the tissue hyperemia, the swelling that cause because of prostaglandin and reduce the sensitivity of peripheral nerve, can be used for treating the moderate pain that general flu or influenza, muscle skeleton property pain and various chronic dull pain and various inflammation cause, be widely used in arthralgia such as rheumatic arthritis, rheumatoid arthritis at present the pain sensation.Diphenhydramine (Diphenhydramine); Chemistry DMAE two methyl phenyl ethers anisoles by name; Be the H1 receptor blocking agent, can reduce body histamine is reacted, eliminate various allergic symptoms such as urticaria, pollinosis, allergic rhinitis etc.; Also have stronger central inhibitory action and slight calmness, antiemetic effect, can be used for preventing motion sicknesses such as seasick, carsick, airsick.Ibuprofen and diphenhydramine coupling can treat pain and with sleep disorder, the insomnia that elimination or alleviation cause because of light, moderate pain improves sleep quality.At present; The dosage form of ibuprofen diphenhydramine compound preparation has liquid capsule and conventional tablet; Like the refined dimension liquid capsule (every contains ibuprofen 200mg, diphhydramine hydrochloride 25mg) and the refined dimension coated tablet (every contains ibuprofen 200mg, diphenhydramine citrate 38mg) of U.S. Wyeth, the ibuprofen diphenhydramine citrate sheet of India DrReddy's drugmaker (every contains ibuprofen 200mg, diphenhydramine citrate 38mg) etc.But there are problems such as disintegrate is slow, the principal agent stripping is slow, onset is slow, bioavailability is low in conventional tablet more.
Dispersible tablet means meets water disintegrate and homodisperse tablet rapidly.The main difference point of itself and conventional tablet is disintegration and dispersing uniformity higher requirement being arranged, and the disintegration in the time of 20 ± 1 ℃ should be less than 3 minutes, and the granule after the disintegrate should be able to be all through No. 2 sieves.The dispersible tablet drug release rate is fast, rapid-action, bioavailability is high; Can alleviate or avoid because of the too high untoward reaction such as stimulation of local drug concentration gastrointestinal mucosa; Carry, easy to use; Both orally-ingestible or add aqueous dispersion after swallow, also can chew or contain to suck and take, be specially adapted to the patient of old man, child and dysphagia.But up to now, all do not see the research report of ibuprofen diphenhydramine dispersible tablet both at home and abroad, do not have the Related product listing yet.Therefore, development ibuprofen diphenhydramine dispersible tablet has good market prospect.
Summary of the invention
In view of this, one of the object of the invention is to provide a kind of ibuprofen diphenhydramine dispersible tablet, rapid disintegrate of ability and homodisperse in water, and steady quality, mouthfeel is good.
For achieving the above object, the present invention provides following technical scheme:
Ibuprofen diphenhydramine dispersible tablet, it is composed of the following components by mass percentage to write out a prescription: ibuprofen 40%, diphhydramine hydrochloride 5% or diphenhydramine citrate 7.6%, filler 30% ~ 43%, disintegrating agent 5% ~ 15%, binding agent 2% ~ 8%, surfactant 0.1% ~ 1%, lubricant 1.5% ~ 4% and correctives 0.5% ~ 1.5%; Said filler is at least two kinds in microcrystalline Cellulose, pregelatinized Starch, lactose and the mannitol; Said disintegrating agent is cross-linking sodium carboxymethyl cellulose and/or polyvinylpolypyrrolidone; Said binding agent is a 30 POVIDONE K 30 BP/USP 30; Said surfactant is a sodium lauryl sulphate, and said lubricant is magnesium stearate and micropowder silica gel, and said correctives is aspartame and steviosin.
Filler reaches the prescription of dispersible tablet more preferably with any two or three coupling in microcrystalline Cellulose, pregelatinized Starch, lactose and the mannitol than independent use a kind of hardness, friability and disintegration time of tablet of more guaranteeing wherein.
Disintegrating agent is cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone coupling more preferably.The disintegration time of gained tablet also can reach the requirement of dispersible tablet when cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone used separately, but the two coupling by a certain percentage can be reached better disintegrate effect.
Hypromellose, 30 POVIDONE K 30 BP/USP 30 and Polyethylene Glycol can use as binding agent, and the present invention is 30 POVIDONE K 30 BP/USP 30 more preferably.Ibuprofen is an insoluble drug, makes binding agent with 30 POVIDONE K 30 BP/USP 30 aqueous solutions, not only is easy to evenly moisteningly, and can make the ibuprofen granule surface become hydrophilic, helps the disintegrate and the stripping of medicine.
Ibuprofen is an insoluble drug, and to the olighydria affinity, its hole is difficult for being penetrated by water, adds the wettability that an amount of surfactant helps to increase tablet, guarantees quick disintegrate of tablet and homodisperse.But surfactant was selected not at that time, also possibly influence the disintegrate of tablet.Through investigation, preferred surfactant sodium lauryl sulphate of the present invention, it not only helps the disintegrate of tablet and the stripping of medicine, but also good lubrication is arranged.
Ibuprofen has certain acid and the content in the present invention prescription higher; Diphhydramine hydrochloride or diphenhydramine citrate also have certain bitterness and zest; In prescription, add an amount of correctives and can cover above-mentioned poor taste, improve mouthfeel, improve patient's drug compliance.The correctives that tablet is commonly used has saccharin sodium, aspartame, steviosin, glycyrrhizin, xylitol etc.Through investigation, preferred aspartame of correctives of the present invention and steviosin coupling, cool taste, sweet taste is lasting, and heat is low.
Adjuvant is formed under the situation about confirming in prescription, and the present invention has done further screening and optimization to the weight proportion of adjuvant component in the prescription.The weight proportion scope of the adjuvant component that screens as previously mentioned.The ibuprofen diphenhydramine dispersible tablet that in this ratio range, makes, equal disintegrate and homodisperse rapidly in water, and steady quality, mouthfeel is better.
As a kind of optimized technical scheme, the prescription of said ibuprofen diphenhydramine dispersible tablet by mass percentage can be composed of the following components: ibuprofen 40%, diphenhydramine citrate 7.6%, microcrystalline Cellulose 25%, mannitol 11%, cross-linking sodium carboxymethyl cellulose 6%, 30 POVIDONE K 30 BP/USP 30 6%, sodium lauryl sulphate 0.2%, magnesium stearate 1.8%, micropowder silica gel 1%, aspartame 1% and steviosin 0.4%.
As a kind of optimized technical scheme, the prescription of said ibuprofen diphenhydramine dispersible tablet by mass percentage can be composed of the following components: ibuprofen 40%, diphenhydramine citrate 7.6%, microcrystalline Cellulose 14%, pregelatinized Starch 5%, lactose 18.8%, polyvinylpolypyrrolidone 7%, 30 POVIDONE K 30 BP/USP 30 2.6%, sodium lauryl sulphate 0.4%, magnesium stearate 2%, micropowder silica gel 1.6%, aspartame 0.6% and steviosin 0.4%.
As a kind of technical scheme of the best, the prescription of said ibuprofen diphenhydramine dispersible tablet by mass percentage can be composed of the following components: ibuprofen 40%, diphenhydramine citrate 7.6%, microcrystalline Cellulose 22%, mannitol 18.4%, cross-linking sodium carboxymethyl cellulose 2%, polyvinylpolypyrrolidone 4.2%, 30 POVIDONE K 30 BP/USP 30 2%, sodium lauryl sulphate 0.6%, magnesium stearate 1.2%, micropowder silica gel 0.6%, aspartame 1% and steviosin 0.4%.
Two of the object of the invention is to provide a kind of method for preparing above-mentioned ibuprofen diphenhydramine dispersible tablet, and easy and simple to handle, cost is low, and constant product quality is fit to suitability for industrialized production.
For achieving the above object, the present invention provides following technical scheme:
The method for preparing of said ibuprofen diphenhydramine dispersible tablet may further comprise the steps:
A. each component pulverize separately became the fine powder of 100 mesh sieves in will writing out a prescription; Using water dissolutioies to process mass percent concentration the 30 POVIDONE K 30 BP/USP of recipe quantity 30 is 2% solution;
B. get ibuprofen, filler and the surfactant of recipe quantity, and the disintegrating agent of 3/4ths recipe quantities and correctives, mix homogeneously; The adding mass percent concentration is 2% 30 POVIDONE K 30 BP/USP 30 solution system soft materials, and 24 mesh sieves are granulated, 55 ± 5 ℃ of dryings; 24 mesh sieve granulate get the dried granule of ibuprofen;
C. get the diphhydramine hydrochloride or the diphenhydramine citrate of recipe quantity, and the disintegrating agent and the correctives of residue recipe quantity, mix homogeneously gets the diphenhydramine pre-composition;
D. with the dried granule of ibuprofen of step b gained and the diphenhydramine pre-composition mix homogeneously of step c gained, add the lubricant of recipe quantity again, mix homogeneously, tabletting promptly makes ibuprofen diphenhydramine dispersible tablet.
The method for preparing of ibuprofen diphenhydramine dispersible tablet of the present invention adopts the wet granule compression tablet method; 1) because ibuprofen and diphhydramine hydrochloride or diphenhydramine citrate are met water the tendency that chemical reaction takes place is arranged; Therefore the present invention granulates ibuprofen separately earlier; Again diphhydramine hydrochloride or diphenhydramine citrate are added in the dried granule behind the granulate, thereby reduce the direct contact of two kinds of medicines, guarantee the stability of dispersible tablet in wet environment; 2) in addition, the adding method of disintegrating agent has three kinds of interior addition, outer addition and inside and outside additions in the tablet, and the present invention discovers, disintegrating agent is fashionable by adding inside and outside the mass ratio 3:1, more helps the quick disintegrate of dispersible tablet; 3) because ibuprofen, diphhydramine hydrochloride or diphenhydramine citrate all have certain poor taste; Therefore inside and outside addition is also selected in the interpolation of correctives among the present invention; Being about to a correctives part adds before granulation; Another part adds after granulation, thereby makes the granule of dispersible tablet inside and outside all sweet, on mouthfeel, more is prone to accepted by the patient.
Beneficial effect of the present invention is: the invention provides a kind of ibuprofen diphenhydramine dispersible tablet, select acceptable accessories for use and adjuvant component and proportioning thereof are screened and optimized, it is reasonable in design to write out a prescription; Simultaneously, the present invention also designs the method for preparing of ibuprofen diphenhydramine dispersible tablet and optimizes, and is easy and simple to handle; With low cost, be applicable to suitability for industrialized production, products obtained therefrom is stable and controllable for quality; Appearance looks elegant, mouthfeel is good, and hardness is suitable; Complete disintegrate is also sieved through No. 2 in 3 minutes in 20 ± 1 ℃ of water; Drug dissolution all reaches more than 85% in the time of 30 minutes, reaches the prescription of Chinese Pharmacopoeia version in 2010 to dispersible tablet, in treatment pain and aspect sleep disorder, have a good application prospect.
The present invention is " Chongqing City's veterinary drug Engineering Technical Research Centre " research project.
The specific embodiment
In order to make the object of the invention, technical scheme and advantage clearer, carry out detailed description in the face of the preferred embodiments of the present invention down.
Embodiment 1
Prescription:
| Component | Quality (g) | Mass percent (%) |
| Ibuprofen | 200 | 40 |
| Diphhydramine hydrochloride | 25 | 5 |
| Microcrystalline Cellulose | 90 | 18 |
| Pregelatinized Starch | 110 | 22 |
| Cross-linking sodium carboxymethyl cellulose | 37 | 7.4 |
| 30 POVIDONE K 30 BP/USP 30 | 20 | 4 |
| Sodium lauryl sulphate | 1 | 0.2 |
| Magnesium stearate | 8 | 1.6 |
| Micropowder silica gel | 5 | 1 |
| Aspartame | 3 | 0.6 |
| Steviosin | 1 | 0.2 |
| Gross weight | 500 | 100 |
Method for preparing:
A. each component pulverize separately became the fine powder of 100 mesh sieves in will writing out a prescription; Using water dissolutioies to process mass percent concentration the 30 POVIDONE K 30 BP/USP of recipe quantity 30 is 2% solution;
B. get ibuprofen, microcrystalline Cellulose, pregelatinized Starch and the sodium lauryl sulphate of recipe quantity; And the cross-linking sodium carboxymethyl cellulose of 3/4ths recipe quantities, aspartame and steviosin, mix homogeneously, adding mass percent concentration are 2% 30 POVIDONE K 30 BP/USP 30 solution system soft materials; 24 mesh sieves are granulated; 55 ± 5 ℃ of dryings, 24 mesh sieve granulate get the dried granule of ibuprofen;
C. get the diphhydramine hydrochloride of recipe quantity, and cross-linking sodium carboxymethyl cellulose, aspartame and the steviosin of residue recipe quantity, mix homogeneously gets the diphenhydramine pre-composition;
D. with the dried granule of ibuprofen of step b gained and the diphenhydramine pre-composition mix homogeneously of step c gained; The magnesium stearate and the micropowder silica gel that add recipe quantity again; Mix homogeneously, tabletting promptly makes 1000 of ibuprofen diphenhydramine dispersible tablets; Every contains ibuprofen 200mg, diphhydramine hydrochloride 25mg.
Quality examination:
The ibuprofen diphenhydramine dispersible tablet any surface finish that present embodiment makes, attractive in appearance; Lightly seasoned, grittiness slightly; Hardness is 6.6 ~ 7.3kg, and friability is 0.62%, and external complete disintegrate in 2.9 minutes is also through No. 2 sieves in 20 ± 1 ℃ of water, and the ibuprofen dissolution is 85% in the time of 30 minutes, and the diphhydramine hydrochloride dissolution is 86%.
Embodiment 2
Prescription:
| Component | Quality (g) | Mass percent (%) |
| Ibuprofen | 200 | 40 |
| Diphhydramine hydrochloride | 25 | 5 |
| Microcrystalline Cellulose | 60 | 12 |
| Lactose | 90 | 18 |
| Pregelatinized Starch | 47 | 9.4 |
| Cross-linking sodium carboxymethyl cellulose | 30 | 6 |
| Polyvinylpolypyrrolidone | 10 | 2 |
| 30 POVIDONE K 30 BP/USP 30 | 15 | 3 |
| Sodium lauryl sulphate | 2 | 0.4 |
| Magnesium stearate | 8 | 1.6 |
| Micropowder silica gel | 8.5 | 1.7 |
| Aspartame | 3 | 0.6 |
| Steviosin | 1.5 | 0.3 |
| Gross weight | 500 | 100 |
Method for preparing:
A. each component pulverize separately became the fine powder of 100 mesh sieves in will writing out a prescription; Using water dissolutioies to process mass percent concentration the 30 POVIDONE K 30 BP/USP of recipe quantity 30 is 2% solution;
B. get ibuprofen, microcrystalline Cellulose, pregelatinized Starch, lactose and the sodium lauryl sulphate of recipe quantity; And 3/4ths cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, aspartame and steviosin, mix homogeneously, adding mass percent concentration are 2% 30 POVIDONE K 30 BP/USP 30 solution system soft materials; 24 mesh sieves are granulated; 55 ± 5 ℃ of dryings, 24 mesh sieve granulate get the dried granule of ibuprofen;
C. get the diphhydramine hydrochloride of recipe quantity, and cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, aspartame and the steviosin of residue recipe quantity, mix homogeneously gets the diphenhydramine pre-composition;
D. with the dried granule of ibuprofen of step b gained and the diphenhydramine pre-composition mix homogeneously of step c gained; The magnesium stearate and the micropowder silica gel that add recipe quantity again; Mix homogeneously, tabletting promptly makes 1000 of ibuprofen diphenhydramine dispersible tablets; Every contains ibuprofen 200mg, diphhydramine hydrochloride 25mg.
Quality examination:
The ibuprofen diphenhydramine dispersible tablet surface that present embodiment makes is brighter and cleaner; Lightly seasoned sweet, grittiness slightly; Hardness is 4.8 ~ 5.6kg, and friability is 0.49%, and external complete disintegrate in 2.1 minutes is also through No. 2 sieves in 20 ± 1 ℃ of water, and the ibuprofen dissolution is 91% in the time of 30 minutes, and the diphhydramine hydrochloride dissolution is 88%.
Embodiment 3
Prescription:
| Component | Quality (g) | Mass percent (%) |
| Ibuprofen | 200 | 40 |
| Diphenhydramine citrate | 38 | 7.6 |
| Microcrystalline Cellulose | 125 | 25 |
| Mannitol | 55 | 11 |
| Cross-linking sodium carboxymethyl cellulose | 30 | 6 |
| 30 POVIDONE K 30 BP/USP 30 | 30 | 6 |
| Sodium lauryl sulphate | 1 | 0.2 |
| Magnesium stearate | 9 | 1.8 |
| Micropowder silica gel | 5 | 1 |
| Aspartame | 5 | 1 |
| Steviosin | 2 | 0.4 |
| Gross weight | 500 | 100 |
Method for preparing:
A. each component pulverize separately became the fine powder of 100 mesh sieves in will writing out a prescription; Using water dissolutioies to process mass percent concentration the 30 POVIDONE K 30 BP/USP of recipe quantity 30 is 2% solution;
B. get ibuprofen, microcrystalline Cellulose, mannitol and the sodium lauryl sulphate of recipe quantity; And the cross-linking sodium carboxymethyl cellulose of 3/4ths recipe quantities, aspartame and steviosin, mix homogeneously, adding mass percent concentration are 2% 30 POVIDONE K 30 BP/USP 30 solution system soft materials; 24 mesh sieves are granulated; 55 ± 5 ℃ of dryings, 24 mesh sieve granulate get the dried granule of ibuprofen;
C. get the diphenhydramine citrate of recipe quantity, and cross-linking sodium carboxymethyl cellulose, aspartame and the steviosin of residue recipe quantity, mix homogeneously gets the diphenhydramine pre-composition;
D. with the dried granule of ibuprofen of step b gained and the diphenhydramine pre-composition mix homogeneously of step c gained; The magnesium stearate and the micropowder silica gel that add recipe quantity again; Mix homogeneously, tabletting promptly makes 1000 of ibuprofen diphenhydramine dispersible tablets; Every contains ibuprofen 200mg, diphenhydramine citrate 38mg.
Quality examination:
The ibuprofen diphenhydramine dispersible tablet any surface finish that present embodiment makes, attractive in appearance; Cool taste, lightly seasoned sweet, no grittiness; Hardness is 5.7 ~ 6.3kg, and friability is 0.65%, external complete disintegrate in 2.6 minutes and in 20 ± 1 ℃ of water through No. 2 sieves, and the ibuprofen dissolution is 93% in the time of 30 minutes, the diphenhydramine citrate dissolution is 90%.
Embodiment 4
Prescription:
| Component | Quality (g) | Mass percent (%) |
| Ibuprofen | 200 | 40 |
| Diphenhydramine citrate | 38 | 7.6 |
| Microcrystalline Cellulose | 70 | 14 |
| Mannitol | 73 | 14.6 |
| Pregelatinized Starch | 30 | 6 |
| Cross-linking sodium carboxymethyl cellulose | 20 | 4 |
| Polyvinylpolypyrrolidone | 35 | 7 |
| 30 POVIDONE K 30 BP/USP 30 | 10 | 2 |
| Sodium lauryl sulphate | 2 | 0.4 |
| Magnesium stearate | 9 | 1.8 |
| Micropowder silica gel | 8 | 1.6 |
| Aspartame | 1 | 0.2 |
| Steviosin | 4 | 0.8 |
| Gross weight | 500 | 100 |
Method for preparing:
A. each component pulverize separately became the fine powder of 100 mesh sieves in will writing out a prescription; Using water dissolutioies to process mass percent concentration the 30 POVIDONE K 30 BP/USP of recipe quantity 30 is 2% solution;
B. get ibuprofen, microcrystalline Cellulose, mannitol, pregelatinized Starch and the sodium lauryl sulphate of recipe quantity; And the cross-linking sodium carboxymethyl cellulose of 3/4ths recipe quantities, polyvinylpolypyrrolidone, aspartame and steviosin, mix homogeneously, adding mass percent concentration are 2% 30 POVIDONE K 30 BP/USP 30 solution system soft materials; 24 mesh sieves are granulated; 55 ± 5 ℃ of dryings, 24 mesh sieve granulate get the dried granule of ibuprofen;
C. get the diphenhydramine citrate of recipe quantity, and cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, aspartame and the steviosin of residue recipe quantity, mix homogeneously gets the diphenhydramine pre-composition;
D. with the dried granule of ibuprofen of step b gained and the diphenhydramine pre-composition mix homogeneously of step c gained; The magnesium stearate and the micropowder silica gel that add recipe quantity again; Mix homogeneously, tabletting promptly makes 1000 of ibuprofen diphenhydramine dispersible tablets; Every contains ibuprofen 200mg, diphenhydramine citrate 38mg.
Quality examination:
The ibuprofen diphenhydramine dispersible tablet any surface finish that present embodiment makes, attractive in appearance; Cool taste, flavor be sweeter, do not have an obvious grittiness; Hardness is 4.9 ~ 5.7kg, and friability is 0.60%, external complete disintegrate in 3 minutes and in 20 ± 1 ℃ of water through No. 2 sieves, and the ibuprofen dissolution is 88% in the time of 30 minutes, the diphenhydramine citrate dissolution is 85%.
Embodiment 5
Prescription:
| Component | Quality (g) | Mass percent (%) |
| Ibuprofen | 200 | 40 |
| Diphenhydramine citrate | 38 | 7.6 |
| Microcrystalline Cellulose | 110 | 22 |
| Mannitol | 92 | 18.4 |
| Cross-linking sodium carboxymethyl cellulose | 10 | 2 |
| Polyvinylpolypyrrolidone | 21 | 4.2 |
| 30 POVIDONE K 30 BP/USP 30 | 10 | 2 |
| Sodium lauryl sulphate | 3 | 0.6 |
| Magnesium stearate | 6 | 1.2 |
| Micropowder silica gel | 3 | 0.6 |
| Aspartame | 5 | 1 |
| Steviosin | 2 | 0.4 |
| Gross weight | 500 | 100 |
Method for preparing:
A. each component pulverize separately became the fine powder of 100 mesh sieves in will writing out a prescription; Using water dissolutioies to process mass percent concentration the 30 POVIDONE K 30 BP/USP of recipe quantity 30 is 2% solution;
B. get ibuprofen, microcrystalline Cellulose, mannitol and the sodium lauryl sulphate of recipe quantity; And the cross-linking sodium carboxymethyl cellulose of 3/4ths recipe quantities, polyvinylpolypyrrolidone, aspartame and steviosin, mix homogeneously, adding mass percent concentration are 2% 30 POVIDONE K 30 BP/USP 30 solution system soft materials; 24 mesh sieves are granulated; 55 ± 5 ℃ of dryings, 24 mesh sieve granulate get the dried granule of ibuprofen;
C. get the diphenhydramine citrate of recipe quantity, and cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, aspartame and the steviosin of residue recipe quantity, mix homogeneously gets the diphenhydramine pre-composition;
D. with the dried granule of ibuprofen of step b gained and the diphenhydramine pre-composition mix homogeneously of step c gained; The magnesium stearate and the micropowder silica gel that add recipe quantity again; Mix homogeneously, tabletting promptly makes 1000 of ibuprofen diphenhydramine dispersible tablets; Every contains ibuprofen 200mg, diphenhydramine citrate 38mg.
Quality examination:
The ibuprofen diphenhydramine dispersible tablet any surface finish that present embodiment makes, attractive in appearance; Cool taste, pleasant, sugariness is moderate, the flavor good no grittiness; Hardness is 4.7 ~ 5.3kg, and friability is 0.42%, external complete disintegrate in 1.7 minutes and in 20 ± 1 ℃ of water through No. 2 sieves, and the ibuprofen dissolution is 96% in the time of 30 minutes, the diphenhydramine citrate dissolution is 92%.
Embodiment 6
Prescription:
| Component | Quality (g) | Mass percent (%) |
| Ibuprofen | 200 | 40 |
| Diphenhydramine citrate | 38 | 7.6 |
| Microcrystalline Cellulose | 70 | 14 |
| Lactose | 94 | 18.8 |
| Pregelatinized Starch | 25 | 5 |
| Polyvinylpolypyrrolidone | 35 | 7 |
| 30 POVIDONE K 30 BP/USP 30 | 13 | 2.6 |
| Sodium lauryl sulphate | 2 | 0.4 |
| Magnesium stearate | 10 | 2 |
| Micropowder silica gel | 8 | 1.6 |
| Aspartame | 3 | 0.6 |
| Steviosin | 2 | 0.4 |
| Gross weight | 500 | 100 |
Method for preparing:
A. each component pulverize separately became the fine powder of 100 mesh sieves in will writing out a prescription; Using water dissolutioies to process mass percent concentration the 30 POVIDONE K 30 BP/USP of recipe quantity 30 is 2% solution;
B. get ibuprofen, microcrystalline Cellulose, lactose, pregelatinized Starch and the sodium lauryl sulphate of recipe quantity; And the polyvinylpolypyrrolidone of 3/4ths recipe quantities, aspartame and steviosin, mix homogeneously, adding mass percent concentration are 2% 30 POVIDONE K 30 BP/USP 30 solution system soft materials; 24 mesh sieves are granulated; 55 ± 5 ℃ of dryings, 24 mesh sieve granulate get the dried granule of ibuprofen;
C. get the diphenhydramine citrate of recipe quantity, and polyvinylpolypyrrolidone, aspartame and the steviosin of residue recipe quantity, mix homogeneously gets the diphenhydramine pre-composition;
D. with the dried granule of ibuprofen of step b gained and the diphenhydramine pre-composition mix homogeneously of step c gained; The magnesium stearate and the micropowder silica gel that add recipe quantity again; Mix homogeneously, tabletting promptly makes 1000 of ibuprofen diphenhydramine dispersible tablets; Every contains ibuprofen 200mg, diphenhydramine citrate 38mg.
Quality examination:
The ibuprofen diphenhydramine dispersible tablet any surface finish that present embodiment makes, attractive in appearance; Lightly seasoned sweet, no grittiness; Hardness is 4.6 ~ 5.8kg, and friability is 0.54%, external complete disintegrate in 2.4 minutes and in 20 ± 1 ℃ of water through No. 2 sieves, and the ibuprofen dissolution is 94% in the time of 30 minutes, the diphenhydramine citrate dissolution is 91%.
Explanation is at last; Above embodiment is only unrestricted in order to technical scheme of the present invention to be described; Although through invention has been described with reference to the preferred embodiments of the present invention; But those of ordinary skill in the art should be appreciated that and can make various changes to it in form with on the details, and the spirit and scope of the present invention that do not depart from appended claims and limited.
Claims (2)
1. ibuprofen diphenhydramine dispersible tablet; It is characterized in that it is composed of the following components by mass percentage to write out a prescription: ibuprofen 40%, diphenhydramine citrate 7.6%, microcrystalline Cellulose 22%, mannitol 18.4%, cross-linking sodium carboxymethyl cellulose 2%, polyvinylpolypyrrolidone 4.2%, 30 POVIDONE K 30 BP/USP 30 2%, sodium lauryl sulphate 0.6%, magnesium stearate 1.2%, micropowder silica gel 0.6%, aspartame 1% and steviosin 0.4%.
2. the method for preparing of the described ibuprofen diphenhydramine of claim 1 dispersible tablet is characterized in that, may further comprise the steps:
A. each component pulverize separately became the fine powder of 100 mesh sieves in will writing out a prescription; Using water dissolutioies to process mass percent concentration the 30 POVIDONE K 30 BP/USP of recipe quantity 30 is 2% solution;
B. get ibuprofen, microcrystalline Cellulose, mannitol and the sodium lauryl sulphate of recipe quantity; And the cross-linking sodium carboxymethyl cellulose of 3/4ths recipe quantities, polyvinylpolypyrrolidone, aspartame and steviosin, mix homogeneously, adding mass percent concentration are 2% 30 POVIDONE K 30 BP/USP 30 solution system soft materials; 24 mesh sieves are granulated; 55 ± 5 ℃ of dryings, 24 mesh sieve granulate get the dried granule of ibuprofen;
C. get the diphenhydramine citrate of recipe quantity, and cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, aspartame and the steviosin of residue recipe quantity, mix homogeneously gets the diphenhydramine pre-composition;
D. with the dried granule of ibuprofen of step b gained and the diphenhydramine pre-composition mix homogeneously of step c gained, add the magnesium stearate and the micropowder silica gel of recipe quantity again, mix homogeneously, tabletting promptly makes ibuprofen diphenhydramine dispersible tablet.
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| US9855227B2 (en) * | 2015-12-18 | 2018-01-02 | The Procter & Gamble Company | Quick dissolving diphenhydramine oral dosage form |
| CN105476971A (en) * | 2016-01-19 | 2016-04-13 | 海南高升医药科技开发股份有限公司 | Medical composition for treating cold and preparation method of medical composition |
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| US20090214648A1 (en) * | 2008-02-15 | 2009-08-27 | Malathi Kandakatla | Pharmaceutical formulations comprising ibuprofen and diphenhydramine |
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| CN101264329A (en) * | 2008-04-25 | 2008-09-17 | 北京阜康仁生物制药科技有限公司 | Medicinal composition for diminishing inflammation and ease pain and preparation and use thereof |
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