CN102440973A - Diphenhydramine citrate orally disintegrating tablet and preparation method thereof - Google Patents
Diphenhydramine citrate orally disintegrating tablet and preparation method thereof Download PDFInfo
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- CN102440973A CN102440973A CN2011104326444A CN201110432644A CN102440973A CN 102440973 A CN102440973 A CN 102440973A CN 2011104326444 A CN2011104326444 A CN 2011104326444A CN 201110432644 A CN201110432644 A CN 201110432644A CN 102440973 A CN102440973 A CN 102440973A
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Abstract
The invention discloses a diphenhydramine citrate orally disintegrating tablet, the prescription is composed by the following components in mass percent: 19% of diphenhydramine citrate, 45 swung dash 58% of filler, 15 swung dash 25% of disintegrating agent, 4 swung dash 8% of effervescent disintegrant, 0.5 swung dash 1% of lubricant, 1 swung dash 3% glidant, 1 swung dash 2% of sweetner, 0.2swung dash 0.6% aromatic and 0 swung dash 0.5% of surfactant, wherein the filler uses mannitol, or mannitol and lactose or erythritol, the disintegrating agent uses any one of polyplasdone, crosslinking sodium carboxy methyl cellulose and low substitution hydroxyl propyl cellulose together with microcrystalline cellulose, the effervescent disintegrant comprises citric acid and sodium bicarbonate which have the mass ratio of 1 swung dash 2/1, the lubricant is magnesium stearate, the glidant is aerosil or talcum powder, the sweetner is aspartame or stevia rebaudianum, the aromatic is the pharmaceutically acceptable essence, and the surfactant is lauryl sodium sulfate; and the invention further discloses a preparation method of the orally disintegrating tablet, which is simple to operate, the cost is low, the obtained product is in accordance with the quality requirement of the orally disintegrating tablet, and has attractive appearance, good taste and stable quality.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to a kind of oral cavity disintegration tablet, also relate to the method for preparing of this oral cavity disintegration tablet.
Background technology
Diphenhydramine is the H1 receptor antagonist, can eliminate various allergic symptoms to the effect of antihistamine to blood vessel, gastrointestinal tract and bronchial smooth muscle, but gastric secretion effect that can not the antagonism histamine; Stronger central nerve inhibition effect is arranged, produce calm, hypnotic effect; Cholinolytic effect is arranged, can alleviate bronchospasm; Also have local anesthesia effect and town to tell effect.Be usually used in skin, mucous membrane irritability disease such as pollinosis, urticaria, allergic dermatitis, pollinosis, angioedema and skin pruritus etc. clinically; Also the vomiting that radiotherapy, operation, medicine and motion sickness cause be can suppress, other medicines control parkinson disease and drug-induced EPS also can be combined.At present, the diphenhydramine folk prescription of domestic listing and compound preparation all are active component with the diphhydramine hydrochloride, and dosage form mainly contains conventional tablet, syrup etc.But transformed by liver metabolism because the oral back of diphenhydramine is most of, first pass effect is obvious, in body circulation precontract by metabolism 50%; Therefore; Be necessary to develop the Benahist that a kind of first pass effect is little, bioavailability is high, store simultaneously, carry, taking convenience, patient's compliance is good.
Summary of the invention
In view of this, one of the object of the invention is to provide a kind of Benahist, and first pass effect is little, and bioavailability is high, stores, carries, taking convenience, and patient's compliance is good.
For achieving the above object, the present invention provides following technical scheme:
The diphenhydramine citrate oral cavity disintegration tablet, it is composed of the following components by mass percentage to write out a prescription: diphenhydramine citrate 19%, filler 45 ~ 58%, disintegrating agent 15 ~ 25%, gas-producing disintegrant 4 ~ 8%, lubricant 0.5 ~ 1%, fluidizer 1 ~ 3%, sweeting agent 1 ~ 2%, aromatic 0.2 ~ 0.6% and surfactant 0 ~ 0.5%; Said filler is that mannitol or mannitol and lactose or erythritol share; Said disintegrating agent is that any and the microcrystalline Cellulose in polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose and the low-substituted hydroxypropyl cellulose share; Said gas-producing disintegrant is that mass ratio is citric acid and the sodium bicarbonate of 1 ~ 2:1; Said lubricant is a magnesium stearate; Said fluidizer is micropowder silica gel or Pulvis Talci; Said sweeting agent is aspartame or steviosin; Said aromatic is pharmaceutically acceptable essence; Said surfactant is a sodium lauryl sulphate.
The preferred sugar alcohols of filler of the present invention such as mannitol, erythritol etc. and lactose, their equal no hygroscopicities, soluble in water, and self be with sweet taste, made tablet surface is bright and clean attractive in appearance.Because heat absorption during the sugar alcohols dissolving; Refrigerant sense is arranged when in the oral cavity, dissolving, and the sugariness of lactose is not as sugar alcohols, and heat release during dissolving; There is not refrigerant sense when in the oral cavity, dissolving; Therefore more preferably sugar alcohols of filler of the present invention as mannitol is mixed as filler with erythritol as filler or with mannitol separately, perhaps makes up as filler with the sugar alcohols of larger proportion and than the lactose of small scale.
Orally-disintegrating tablet is not need water, chance saliva disintegrate and dissolved tablet rapidly, and therefore, the selection of disintegrating agent is extremely important.In the preferred polyvinylpolypyrrolidone of disintegrating agent of the present invention, cross-linking sodium carboxymethyl cellulose and the low-substituted hydroxypropyl cellulose any and microcrystalline Cellulose share.Microcrystalline Cellulose is water insoluble; Have good flowability and compressibility; Have filling, disintegrate, lubricated multiple action concurrently, during with the strong polyvinylpolypyrrolidone of swelling behavior, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose Combined application, can improve the porosity of tablet; Strengthen capillarity, make tablet disintegrate fast in low amounts of water.Investigate and find the disintegrate best results that microcrystalline Cellulose and polyvinylpolypyrrolidone share.Gas-producing disintegrant is made up of acid constituents and alkaline constituents, and the two chance water can produce carbon dioxide and reach disintegration, also has certain strong flavor effect in addition.In order to make the disintegrate better effects if of diphenhydramine citrate oral cavity disintegration tablet, the present invention share gas-producing disintegrant and aforementioned disintegrating agent, the acid constituents preferably citric acid of gas-producing disintegrant wherein, the preferred sodium bicarbonate of alkaline constituents.Diphenhydramine citrate is slightly soluble in water, and its hole is difficult for being penetrated by water, adds the wettability that an amount of surfactant helps to increase tablet, makes moisture borrow the capillarity rapid permeability to play disintegration to the sheet heart.But surfactant was selected not at that time, also possibly influence the disintegrate of tablet.Also can be in the present invention prescription with surfactant and disintegrating agent, gas-producing disintegrant Combined application, thus make disintegration rate sooner, disintegrate is more even.Through investigation, surfactant preferably sodium dodecyl sulfate of the present invention, it not only helps the disintegrate of tablet, and good lubrication is also arranged.
Oral cavity disintegration tablet is disintegrate and dissolving rapidly in the oral cavity, so mouthfeel is one of main investigation factor of this dosage form.Diphenhydramine citrate has certain bitterness and zest, in prescription, adds an amount of sweeting agent and aromatic and can cover its poor taste, improves mouthfeel, improves patient's drug compliance.Through investigating preferred aspartame of sweeting agent of the present invention or steviosin.Aspartame is the artificial synthesis edulcorant, unlikely dental caries, and heat is low, is applicable to diabetes, obesity patient; Steviosin is a natural sweetener, does not produce heat, has refrigerant sweet taste and sweet taste lasting.The preferred medicinal essence of aromatic is like Fructus Citri Limoniae essence, apple essence, flavoring orange essence, strawberry essence, Herba Menthae essence etc.
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 that screens as previously mentioned.The diphenhydramine citrate oral cavity disintegration tablet that in the said ratio scope, makes is met saliva disintegrate and dissolving rapidly, and steady quality, and mouthfeel is better.Research is also found; When microcrystalline Cellulose and polyvinylpolypyrrolidone share as disintegrating agent, 1) along with the increase of polyvinylpolypyrrolidone consumption, the disintegration time of tablet reduces gradually; But after its consumption in prescription is greater than 10%; Disintegration time basically no longer changes, and therefore, the consumption of polyvinylpolypyrrolidone is preferably 5% ~ 10% in the prescription; 2) along with the increase of microcrystalline Cellulose consumption, the disintegration time of tablet reduces gradually, but because the water-insoluble of microcrystalline Cellulose; After its consumption in prescription is greater than 15%; Grittiness is obvious, and causes the thickness sense in the lingual surface accumulation, and patient's compliance reduces; Therefore, the consumption of microcrystalline Cellulose is preferably 10% ~ 15% in the prescription.In addition, in fixed prescription under the situation of polyvinylpolypyrrolidone and microcrystalline Cellulose consumption, hour without gas-producing disintegrant or gas-producing disintegrant consumption; Pile up and the sense of generation thickness at lingual surface easily behind the disintegration of tablet, along with the increase of gas-producing disintegrant consumption, the disintegration time of tablet reduces gradually; But when the gas-producing disintegrant consumption is excessive; In disintegrating procedue, foam sense and tart flavour of tablet is strong excessively, and the acid constituents citric acid hygroscopicity of gas-producing disintegrant is strong, the excessive storage that is unfavorable for tablet of consumption; Therefore, the consumption of gas-producing disintegrant is preferably 4 ~ 8% in the prescription.
As a kind of optimized technical scheme, the prescription of said diphenhydramine citrate oral cavity disintegration tablet is composed of the following components by mass percentage: diphenhydramine citrate 19%, mannitol 40%, erythritol 16.5%, microcrystalline Cellulose 10%, polyvinylpolypyrrolidone 5%, citric acid 3%, sodium bicarbonate 2%, magnesium stearate 0.5%, micropowder silica gel 2.5%, aspartame 1% and flavoring orange essence 0.5%.
As a kind of optimized technical scheme, the prescription of said diphenhydramine citrate oral cavity disintegration tablet is composed of the following components by mass percentage: diphenhydramine citrate 19%, mannitol 35%, erythritol 16.7%, microcrystalline Cellulose 10%, polyvinylpolypyrrolidone 8%, citric acid 4%, sodium bicarbonate 2.5%, magnesium stearate 0.5%, Pulvis Talci 2.5%, aspartame 1.5% and Fructus Citri Limoniae essence 0.3%.
As a kind of technical scheme of the best, the prescription of said diphenhydramine citrate oral cavity disintegration tablet is composed of the following components by mass percentage: diphenhydramine citrate 19%, mannitol 46%, microcrystalline Cellulose 15%, polyvinylpolypyrrolidone 8%, citric acid 4%, sodium bicarbonate 2%, magnesium stearate 1%, Pulvis Talci 2.5%, steviosin 1.5%, Fructus Citri Limoniae essence 0.5% and sodium lauryl sulphate 0.5%.
Two of the object of the invention is to provide the method for preparing of said Benahist, and technology is simple, and cost is low, and constant product quality is fit to large-scale industrialization production.
For achieving the above object, the present invention provides following technical scheme:
The method for preparing of diphenhydramine citrate oral cavity disintegration tablet both can adopt direct powder compression, also can adopt the wet granule compression tablet method.
Said direct powder compression is the fine powder that all components pulverize separately in the prescription was become 100 mesh sieves; Take by weighing diphenhydramine citrate, filler, disintegrating agent, gas-producing disintegrant, fluidizer, sweeting agent, aromatic and the surfactant of recipe quantity; Mix homogeneously adds lubricant, mix homogeneously again; Tabletting promptly gets the diphenhydramine citrate oral cavity disintegration tablet.
Said wet granule compression tablet method is the fine powder that all components pulverize separately in the prescription was become 100 mesh sieves, takes by weighing the diphenhydramine citrate and the sweeting agent of recipe quantity, mix homogeneously; Add the disintegrating agent of the filler of recipe quantity, all or part of recipe quantity again or do not add disintegrating agent, mix homogeneously is with alcoholic solution or be dissolved with the alcoholic solution system soft material of surfactant; Cross the sieve series wet granular, drying, granulate sieves; Add the disintegrating agent of residue recipe quantity and gas-producing disintegrant, aromatic and the fluidizer of recipe quantity again, mix homogeneously adds the lubricant of recipe quantity at last; Mix homogeneously, tabletting promptly gets the diphenhydramine citrate oral cavity disintegration tablet.
In above-mentioned wet granule compression tablet method; 1) because diphenhydramine citrate has certain bitterness and zest; The present invention when the design technology route preferably with diphenhydramine citrate and sweeting agent elder generation mix homogeneously, thereby better cover the poor taste of diphenhydramine citrate, improve mouthfeel; 2) the adding method of disintegrating agent has three kinds: addition 1.: the disintegrating agent of whole recipe quantities is added before the system wet granular, thereby make disintegrating agent be present in granule interior; 2. outer addition: the disintegrating agent of whole recipe quantities is added behind granulate, thereby make disintegrating agent be present in outside the granule and between each granule; 3. inside and outside addition: disintegrating agent is divided into two parts, and a by interior addition adding, another part adds by outer addition.When same amount, adopt above-mentioned three kinds of oral cavity disintegration tablets that disintegrating agent adding method makes, its disintegration rate is outer addition＞inside and outside addition＞interior addition, dissolution rate is inside and outside addition＞interior addition＞outer addition, the preferred inside and outside addition of the present invention.3) in wet-granulation process, meet waterishlogging for fear of acid, the alkaline constituents of gas-producing disintegrant and give birth to reaction, the present invention preferably adds gas-producing disintegrant after granulation.4) when wet granulation, the present invention is that 50% alcoholic solution is a wetting agent system soft material with volume fraction preferably, and when containing surfactant in the prescription, the present invention preferably is dissolved in surfactant in the wetting agent and adds.
As a kind of optimized technical scheme, the prescription of said diphenhydramine citrate oral cavity disintegration tablet is composed of the following components by mass percentage: diphenhydramine citrate 19%, mannitol 40%, erythritol 16.5%, microcrystalline Cellulose 10%, polyvinylpolypyrrolidone 5%, citric acid 3%, sodium bicarbonate 2%, magnesium stearate 0.5%, micropowder silica gel 2.5%, aspartame 1% and flavoring orange essence 0.5%; Its preparation method is a direct powder compression.
As a kind of optimized technical scheme, the prescription of said diphenhydramine citrate oral cavity disintegration tablet is composed of the following components by mass percentage: diphenhydramine citrate 19%, mannitol 35%, erythritol 16.7%, microcrystalline Cellulose 10%, polyvinylpolypyrrolidone 8%, citric acid 4%, sodium bicarbonate 2.5%, magnesium stearate 0.5%, Pulvis Talci 2.5%, aspartame 1.5% and Fructus Citri Limoniae essence 0.3%; Its preparation method is a wet granule compression tablet.
As a kind of technical scheme of the best, the prescription of said diphenhydramine citrate oral cavity disintegration tablet is composed of the following components by mass percentage: diphenhydramine citrate 19%, mannitol 46%, microcrystalline Cellulose 15%, polyvinylpolypyrrolidone 8%, citric acid 4%, sodium bicarbonate 2%, magnesium stearate 1%, Pulvis Talci 2.5%, steviosin 1.5%, Fructus Citri Limoniae essence 0.5% and sodium lauryl sulphate 0.5%; Its preparation method is a wet granule compression tablet.
Beneficial effect of the present invention is: the present invention is that active component has prepared oral cavity disintegration tablet with the diphenhydramine citrate, selects acceptable accessories for use and adjuvant component and proportioning thereof are screened and optimized, and it is reasonable in design to write out a prescription; Simultaneously, the present invention also designs the method for preparing of diphenhydramine citrate oral cavity disintegration tablet and optimizes, and is easy and simple to handle, technology maturation; Extra special installation need not acquired by manufacturer can realize large-scale industrialization production, and with low cost, products obtained therefrom is stable and controllable for quality, reaches the prescription of oral cavity disintegration tablet; Appearance looks elegant, mouthfeel is good, and hardness is suitable; In the oral cavity, meet disintegrate fast in the saliva 30 seconds, drug dissolution reaches more than 85% in the time of 5 minutes, trans-oral and esophageal mucosa membrane injury absorption; First pass effect is little, and bioavailability is high, stores, carries, taking convenience; Be suitable for the child, the old man, go into a coma, be unable to leave the bed, permanent disability etc. has the patient of function of deglutition obstacle and the patient who is difficult for obtaining drinking water.
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:
Method for preparing:
Each component pulverize separately in the prescription was become the fine powder of 100 mesh sieves; Get the diphenhydramine citrate of recipe quantity and all adjuvants except that magnesium stearate, mix homogeneously adds the magnesium stearate of recipe quantity again; Mix homogeneously; The control tablet hardness is 7 ± 2N tabletting, promptly gets the diphenhydramine citrate oral cavity disintegration tablet, and every contains diphenhydramine citrate 19mg.
Embodiment 2
Prescription:
Method for preparing:
Each component pulverize separately in the prescription is become the fine powder of 100 mesh sieves, got the diphenhydramine citrate and the steviosin of recipe quantity, mix homogeneously; The mannitol, lactose, microcrystalline Cellulose and the polyvinylpolypyrrolidone that add recipe quantity again, mix homogeneously, using volume fraction is that 50% alcoholic solution is wetting agent system soft material; 30 mesh sieves are granulated, 50 ~ 55 ℃ of aeration-dryings, 30 mesh sieve granulate; Citric acid, sodium bicarbonate, flavoring orange essence and the micropowder silica gel of recipe quantity are joined in the dried granule, and mix homogeneously adds the magnesium stearate of recipe quantity again; Mix homogeneously; The control tablet hardness is 7 ± 2N tabletting, promptly gets the diphenhydramine citrate oral cavity disintegration tablet, and every contains diphenhydramine citrate 19mg.
Embodiment 3
Prescription:
Method for preparing:
Each component pulverize separately in the prescription is become the fine powder of 100 mesh sieves, got the diphenhydramine citrate and the aspartame of recipe quantity, mix homogeneously; The mannitol and the erythritol that add recipe quantity again, and the microcrystalline Cellulose of 1/2nd recipe quantities and polyvinylpolypyrrolidone, mix homogeneously; Using volume fraction is that 50% alcoholic solution is wetting agent system soft material, and 30 mesh sieves are granulated, 50 ~ 55 ℃ of aeration-dryings; 30 mesh sieve granulate join in the dried granule mix homogeneously with the microcrystalline Cellulose of residue recipe quantity and citric acid, sodium bicarbonate, Fructus Citri Limoniae essence and the Pulvis Talci of polyvinylpolypyrrolidone and recipe quantity; The magnesium stearate that adds recipe quantity again, mix homogeneously, the control tablet hardness is 7 ± 2N tabletting; Promptly get the diphenhydramine citrate oral cavity disintegration tablet, every contains diphenhydramine citrate 19mg.
Embodiment 4
Prescription:
Method for preparing:
Each component pulverize separately in the prescription was become the fine powder of 100 mesh sieves, get the diphenhydramine citrate and the aspartame of recipe quantity, mix homogeneously adds the mannitol of recipe quantity again; Mix homogeneously, using volume fraction is that 30% alcoholic solution is wetting agent system soft material, 30 mesh sieves are granulated; 50 ~ 55 ℃ of aeration-dryings, 30 mesh sieve granulate, microcrystalline Cellulose, polyvinylpolypyrrolidone, citric acid, sodium bicarbonate, Herba Menthae essence and the micropowder silica gel with recipe quantity joins in the dried granule again; Mix homogeneously adds the magnesium stearate of recipe quantity, mix homogeneously again; The control tablet hardness is 7 ± 2N tabletting, promptly gets the diphenhydramine citrate oral cavity disintegration tablet, and every contains diphenhydramine citrate 19mg.
Embodiment 5
Prescription:
Method for preparing:
Each component pulverize separately in the prescription was become the fine powder of 100 mesh sieves, and it is that 50% dissolve with ethanol solution is processed solution that the sodium lauryl sulphate of recipe quantity is used volume fraction, gets the diphenhydramine citrate and the steviosin of recipe quantity; Mix homogeneously adds the mannitol of recipe quantity and the microcrystalline Cellulose of 1/2nd recipe quantities and polyvinylpolypyrrolidone again; Mix homogeneously uses the alcoholic solution that is dissolved with sodium lauryl sulphate to be wetting agent system soft material, and 30 mesh sieves are granulated; 50 ~ 55 ℃ of aeration-dryings, 30 mesh sieve granulate join the microcrystalline Cellulose of residue recipe quantity and citric acid, sodium bicarbonate, Herba Menthae essence and the Pulvis Talci of polyvinylpolypyrrolidone and recipe quantity in the dried granule; Mix homogeneously; The magnesium stearate that adds recipe quantity again, mix homogeneously, the control tablet hardness is 7 ± 2N tabletting; Promptly get the diphenhydramine citrate oral cavity disintegration tablet, every contains diphenhydramine citrate 19mg.
The quality examination result of the diphenhydramine citrate oral cavity disintegration tablet that embodiment 1 ~ 5 makes sees the following form.Wherein hardness test adopts YPD-200C matrix agent hardness tester (Shanghai Huanghai Sea medicine inspection Instr Ltd.), detects 10 altogether, averages.78X-6A matrix agent four-function appearance (Shanghai Huanghai Sea medicine inspection Instr Ltd.) is adopted in the friability inspection, checks by 2010 editions two appendix XG tablets of Chinese Pharmacopoeia friability inspection technique, calculates tablet and subtracts weight loss.The disintegration time inspection comprises disintegration time inspection in external disintegration time inspection and the body.Evaluate the requirement of " formulation characteristic of oral cavity disintegration tablet and the quality control meeting summary " of center in JIUYUE, 2003 issue with reference to State Food and Drug Administration's medicine; Static disintegrate method is adopted in external disintegration time inspection; Get 1 of oral cavity disintegration tablet, put in the 5mL beaker that fills 37 ± 0.5 ℃ of distilled water of 2mL, the range estimation disintegration of tablet (does not filter liquid in the beaker till seeing label with 25 eye mesh screens; Basically noresidue on the screen cloth); The record required time of said process is external disintegration time, detects 10 altogether, averages; The disintegration time inspection is 6 healthy volunteer elder generation water cleaning oral cavitys in the body, gets 1 of oral cavity disintegration tablet at random and places lingual surface, not water; Do not chew yet; Allow tongue suitably to move up and down, record tablet complete required time of disintegrate in the oral cavity is disintegration time in the body, averages.Dissolution determination adopts 2010 editions two appendix XC dissolution methods of Chinese Pharmacopoeia, second method, and dissolution medium is a 900mL 0.1mol/L hydrochloric acid solution, and rotating speed is 100r/min, respectively 1; 2,5,10,20; 30, the 45min 5mL that takes a sample is after centrifugal, filtration treatment, according to the concentration of 2010 editions two appendix VD high effective liquid chromatography for measuring of Chinese Pharmacopoeia diphenhydramine citrate; Calculate dissolution, chromatographic condition is following: chromatographic column is Sepax-C18 post (4.6 * 250mm, 5 μ m), and mobile phase is that (volume ratio is 50:50:0.5 to acetonitrile-water-triethylamine; Regulate pH to 7.5 with phosphoric acid), the detection wavelength is 213nm, and column temperature is 30 ℃, and flow velocity is 1.0mL/min.
The quality examination result of the diphenhydramine citrate oral cavity disintegration tablet that table embodiment 1 ~ 5 makes
Explanation is that above embodiment only is used to explain technical scheme of the present invention, does not constitute the restriction to content of the present invention at last.Although the present invention has been done comparatively detailed giving an example through the foregoing description; But those skilled in the art still can be according to summary of the invention part and the described technology contents of embodiment part; In form with on the details it is made various changes, and the spirit and scope of the present invention that do not depart from appended claims and limited.
Claims (6)
1. diphenhydramine citrate oral cavity disintegration tablet; It is characterized in that it is composed of the following components by mass percentage to write out a prescription: diphenhydramine citrate 19%, filler 45 ~ 58%, disintegrating agent 15 ~ 25%, gas-producing disintegrant 4 ~ 8%, lubricant 0.5 ~ 1%, fluidizer 1 ~ 3%, sweeting agent 1 ~ 2%, aromatic 0.2 ~ 0.6% and surfactant 0 ~ 0.5%; Said filler is that mannitol or mannitol and lactose or erythritol share; Said disintegrating agent is that any and the microcrystalline Cellulose in polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose and the low-substituted hydroxypropyl cellulose share; Said gas-producing disintegrant is that mass ratio is citric acid and the sodium bicarbonate of 1 ~ 2:1; Said lubricant is a magnesium stearate; Said fluidizer is micropowder silica gel or Pulvis Talci; Said sweeting agent is aspartame or steviosin; Said aromatic is pharmaceutically acceptable essence; Said surfactant is a sodium lauryl sulphate.
2. diphenhydramine citrate oral cavity disintegration tablet according to claim 1; It is characterized in that it is composed of the following components by mass percentage to write out a prescription: diphenhydramine citrate 19%, mannitol 40%, erythritol 16.5%, microcrystalline Cellulose 10%, polyvinylpolypyrrolidone 5%, citric acid 3%, sodium bicarbonate 2%, magnesium stearate 0.5%, micropowder silica gel 2.5%, aspartame 1% and flavoring orange essence 0.5%.
3. diphenhydramine citrate oral cavity disintegration tablet according to claim 1; It is characterized in that it is composed of the following components by mass percentage to write out a prescription: diphenhydramine citrate 19%, mannitol 35%, erythritol 16.7%, microcrystalline Cellulose 10%, polyvinylpolypyrrolidone 8%, citric acid 4%, sodium bicarbonate 2.5%, magnesium stearate 0.5%, Pulvis Talci 2.5%, aspartame 1.5% and Fructus Citri Limoniae essence 0.3%.
4. diphenhydramine citrate oral cavity disintegration tablet according to claim 1; It is characterized in that it is composed of the following components by mass percentage to write out a prescription: diphenhydramine citrate 19%, mannitol 46%, microcrystalline Cellulose 15%, polyvinylpolypyrrolidone 8%, citric acid 4%, sodium bicarbonate 2%, magnesium stearate 1%, Pulvis Talci 2.5%, steviosin 1.5%, Fructus Citri Limoniae essence 0.5% and sodium lauryl sulphate 0.5%.
5. the method for preparing of each said diphenhydramine citrate oral cavity disintegration tablet of claim 1 to 4 is characterized in that, all components pulverize separately in the prescription is become the fine powder of 100 mesh sieves; Take by weighing diphenhydramine citrate, filler, disintegrating agent, gas-producing disintegrant, fluidizer, sweeting agent, aromatic and the surfactant of recipe quantity; Mix homogeneously adds lubricant, mix homogeneously again; Tabletting promptly gets the diphenhydramine citrate oral cavity disintegration tablet.
6. the method for preparing of each said diphenhydramine citrate oral cavity disintegration tablet of claim 1 to 4 is characterized in that, all components pulverize separately in the prescription is become the fine powder of 100 mesh sieves; Take by weighing the diphenhydramine citrate and the sweeting agent of recipe quantity, mix homogeneously adds the disintegrating agent of the filler of recipe quantity, all or part of recipe quantity again or does not add disintegrating agent; Mix homogeneously with alcoholic solution or be dissolved with the alcoholic solution system soft material of surfactant, is crossed the sieve series wet granular; Drying, the granulate that sieves adds the disintegrating agent of residue recipe quantity and gas-producing disintegrant, aromatic and the fluidizer of recipe quantity again; Mix homogeneously adds the lubricant of recipe quantity, mix homogeneously at last; Tabletting promptly gets the diphenhydramine citrate oral cavity disintegration tablet.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103989639A (en) * | 2014-04-30 | 2014-08-20 | 浙江康乐药业股份有限公司 | Diphenhydramine hydrochloride particles and preparation method thereof |
| CN107510671A (en) * | 2016-06-16 | 2017-12-26 | 杨永新 | A kind of multi-functional auxiliary material composition of oral dosage form and the preparation of oral dosage form |
| CN108366961A (en) * | 2015-12-18 | 2018-08-03 | 宝洁公司 | Rapidly-soluble diphenhydramine peroral dosage form |
| CN113679687A (en) * | 2021-09-29 | 2021-11-23 | 江苏集萃新型药物制剂技术研究所有限公司 | Composite drug release composition, orally disintegrating tablet composition, orally disintegrating preparation and application thereof |
| CN114788817A (en) * | 2021-01-25 | 2022-07-26 | 南京宁丹新药技术有限公司 | Diphenhydramine pharmaceutical composition |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103989639A (en) * | 2014-04-30 | 2014-08-20 | 浙江康乐药业股份有限公司 | Diphenhydramine hydrochloride particles and preparation method thereof |
| CN108366961A (en) * | 2015-12-18 | 2018-08-03 | 宝洁公司 | Rapidly-soluble diphenhydramine peroral dosage form |
| CN108366961B (en) * | 2015-12-18 | 2022-02-18 | 宝洁公司 | Fast dissolving diphenhydramine oral dosage form |
| CN107510671A (en) * | 2016-06-16 | 2017-12-26 | 杨永新 | A kind of multi-functional auxiliary material composition of oral dosage form and the preparation of oral dosage form |
| CN114788817A (en) * | 2021-01-25 | 2022-07-26 | 南京宁丹新药技术有限公司 | Diphenhydramine pharmaceutical composition |
| CN113679687A (en) * | 2021-09-29 | 2021-11-23 | 江苏集萃新型药物制剂技术研究所有限公司 | Composite drug release composition, orally disintegrating tablet composition, orally disintegrating preparation and application thereof |
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