CN101637461A - Moguisteine dispersible tablet and preparation method thereof - Google Patents
Moguisteine dispersible tablet and preparation method thereof Download PDFInfo
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Abstract
The invention relates to a moguisteine dispersible tablet and a preparation method thereof. The moguisteine dispersible tablet comprises the following components in portion by weight: 5 to 45 portionsof moguisteine, 10 to 50 portions of disintegrating agent, 20 to 80 portions of filling agent, 0.5 to 3.0 portions of flavouring agent, 0.4 to 1.5 portions of lubricating agent, and 0.5 to 2.5 portions of binding agent. The moguisteine dispersible tablet has the advantages of high dissolubility, quick response, quick release, obvious effect, conclusive curative effect and the like. The moguisteine dispersible tablet can be applied to cough relief.
Description
Technical field
The present invention relates to pharmaceutical field, specifically, the present invention relates to a kind of moguisteine dispersible tablet and preparation method thereof.
Background technology
Cough is a kind of important reflexive protection mechanism, can discharge expectorant and foreign body in the respiratory tract by coughing, the cleaning of protection respiratory tract and unobstructed, thus protect from infection.If but continue violent cough, patient's misery not only, and easily produce other complication.Along with the aging of society and the aggravation of environmental pollution, the sickness rate of respiratory system disease constantly rises, and the eliminating phlegm and relieving cough medicine will be the important component part of medicine for respiratory system, therefore needs to select suitable cough medicine to come relieving cough.
Moguisteine (moguisteine) is a kind of acetylcholine agonist, periphery non-narcotic antitussive medicine by the exploitation of Switzerland Roche company, and it does not have influence to the central nervous system, and does not have addiction.The original shape medicine of moguisteine can not be gone into blood, decomposes immediately after entering in the body, and metabolite can be drained in body fully, and nothing is accumulated.In the clinical research of one group of randomized, double-blind placebo, moguisteine makes respiratory system disease patient's cough symptom reduce 42%, and placebo only can make the cough symptom reduce 14%, and both compare has significant difference.In addition, do not see report, that is the toleration of moguisteine is good relevant for the moguisteine serious adverse reaction.Clinical research shows that also moguisteine can be taken for 3 times on the 1st, each 100mg.Hence one can see that, and moguisteine has the advantages that the antitussive effect is obvious, toxic and side effects is low and dosage is little.
Yet, moguisteine be the white of low melting point (about 60 ℃) to off-white powder, should be noted that and avoid it that fusion takes place in dry run.In addition, the dissolubility of moguisteine in water is low, easily causes the bioavailability of made oral solid formulation low.
In order to satisfy dissimilar patients' medication demand, particularly in order to satisfy child, old man and to the patient's that swallows solid preparation (for example tablet and capsule) difficulty medication demand, need develop the moguisteine novel form that adopts new application method, effectively improve the compliance that the patient takes medicine.
Thus, the present invention provides a kind of dispersible tablet of moguisteine in advance, the patient that it is specially adapted to child, old man and takes the solid preparation difficulty, thus be used for the treatment of because the cough due to the acute and chronic respiratory system disease that infection, stimulation, inflammation and tumor cause.
Summary of the invention
In one aspect, the invention provides a kind of moguisteine dispersible tablet, it comprises: the moguisteine of 5 weight portions-45 weight portion; The disintegrating agent of 10 weight portions-50 weight portion; The filler of 20 weight portions-80 weight portion; 0.5 the correctives of weight portion-3.0 weight portion; 0.4 the lubricant of weight portion-1.5 weight portion; 0.5 the binding agent of weight portion-2.5 weight portion.
Moguisteine dispersible tablet of the present invention preferably comprises: the moguisteine of 15 weight portions-30 weight portion; The disintegrating agent of 20 weight portions-35 weight portion; The filler of 35 weight portions-60 weight portion; 0.5 the correctives of weight portion-1.0 weight portion; 0.6 the lubricant of weight portion-1.0 weight portion; 0.5 the binding agent of weight portion-1.5 weight portion.
In moguisteine dispersible tablet of the present invention, disintegrating agent is preferably and is selected from starch, pregelatinized Starch, carboxymethyl starch sodium, L-hydroxypropyl cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, sodium alginate and the microcrystalline Cellulose etc. one or more; Filler is preferably and is selected from lactose, mannitol, pregelatinized Starch, microcrystalline Cellulose and the calcium hydrogen phosphate one or more; Correctives is preferably and is selected from that Herba Menthae essence, stevioside, A Siba are sweet, in flavoring orange essence and the orange flavor one or more; Lubricant is preferably and is selected from micropowder silica gel, magnesium stearate and the Pulvis Talci one or more; Binding agent is preferably selected from polyvidone and hydroxypropyl methylcellulose.
Preferably fully disintegrate and reach homogeneously dispersed state in 3 minutes of moguisteine dispersible tablet of the present invention, and the accumulation dissolution of moguisteine effective ingredient in 10 minutes is more than 60%.
In one aspect of the method, the invention provides a kind of preparation method of moguisteine dispersible tablet, it may further comprise the steps: (1) mixes the moguisteine of 5 weight portions-45 weight portion, the disintegrating agent of 10 weight portions-50 weight portion, the filler of 20 weight portions-80 weight portion and the correctives of 0.5 weight portion-3.0 weight portion, makes pre-composition; (2) the binding agent system soft material of adding 0.5 weight portion-2.5 weight portion in pre-composition; (3) with the gained soft material granulation; (4) with the gained particle drying; (5) with dried granule granulate; (6) lubricant that adds 0.4 weight portion-1.5 weight portion mixes, and carries out tabletting.
The preparation method of moguisteine dispersible tablet of the present invention preferably also comprises: before the moguisteine raw material is crossed 100 mesh sieves in step (1), and the step of disintegrating agent, filler, correctives and lubricant being crossed 60 orders-80 mesh sieve.
In the preparation method of moguisteine dispersible tablet of the present invention, the granulation in the step (3) is preferably undertaken by the method for crossing the 16-24 mesh sieve; Drying in the step (4) is preferably undertaken by the method for forced air drying under 40 ℃ of conditions; Granulate in the step (5) is preferably undertaken by the method for dried granule being crossed the 24-30 mesh sieve.
In the preparation method of moguisteine dispersible tablet of the present invention, preferably, binding agent was dissolved in the dehydrated alcohol before using in advance, make that the concentration of gained solution is 3-10% (weight/volume).
Moguisteine dispersible tablet of the present invention has following effect: the dissolubility that 1. can further improve the moguisteine principal agent, promptly, moguisteine is met water can form even viscosity suspension rapidly, be dispersed into granule in the rapid disintegrate of gastrointestinal tract, the medicine distribution area is increased, absorption point increases, avoid ordinary preparation too high in the gastrointestinal tract local drug concentration, shortcomings such as stimulating gastrointestinal mucous membrane have reduced untoward reaction, have improved patient's adaptability greatly; 2. to the patient of child, gerontal patient and dysphagia, moguisteine dispersible tablet can be disperseed back and fruit juice, milk and clothes in water; 3. compare with common moguisteine sheet, moguisteine dispersible tablet of the present invention is rapid-action, rapid release, effect is obvious and curative effect is conclusive; 4. the production technology of moguisteine dispersible tablet of the present invention is simple, and the Production and Packaging cost is low, and transportation, storage are conveniently.
Description of drawings
Fig. 1 is the blood drug level-time graph of male beasle dog after taking moguisteine dried dispersible tablet of the present invention.
The specific embodiment
In the present invention, " dispersible tablet " is meant rapid disintegrate of energy and homodisperse tablet in water.In moguisteine dispersible tablet of the present invention, moguisteine is an insoluble drug, needs to add good disintegrating agent, swellability adjuvant and some other filleies of disintegrating property, to guarantee dispersible tablet disintegrate rapidly, stripping.According to the regulation of Chinese Pharmacopoeia 2005 editions, dispersible tablet also should carry out dissolution and dispersing uniformity inspection respectively except carrying out the general inspection project under " tablet " item.
In the present invention, " dissolution " be meant in the regulation medium, under certain condition, and the speed and the degree of medicine stripping from solid preparations such as tablet or capsule.Dissolution can be used for weighing the quality of solid preparation; Estimate the interior bioavailability of body of solid preparation; And estimate and screening preparation process, prescription and dosage form.Its concrete assay method can be with reference to " appendix is described carries out for two of Chinese pharmacopoeia (version in 2005).
According to version in 2005 " Chinese pharmacopoeia as can be known:, if the undesirable absorption that just might influence medicine of dispersed homogeneous degree, thereby influence the effectiveness and the safety of medicine because insoluble drug original just being difficult for disperses to the regulation of " dispersing uniformity ".Therefore dispersible tablet must carry out the dispersing uniformity inspection.Its concrete assay method can be with reference to " appendix is described carries out for two of Chinese pharmacopoeia (version in 2005).
In moguisteine dispersible tablet of the present invention, moguisteine is as the principal agent of described dispersible tablet, its be the about 60 ℃ white of fusing point to off-white powder, molecular weight is 339.41, and has molecular formula as follows:
In moguisteine dispersible tablet of the present invention, the content of moguisteine principal agent is 5 weight portions-45 weight portions, is preferably 10 weight portions-40 weight portion, more preferably 15 weight portions-30 weight portion.Make the content of moguisteine principal agent in described moguisteine dispersible tablet satisfy above-mentioned scope, can make that the dispersible tablet of making is good disintegration, stripping is fast, and stripping is complete, and make the dispersible tablet sheet that makes heavily suitable, cost is low, can satisfy need of industrial production.
In the present invention, described moguisteine dispersible tablet also comprises other adjuvant.In the present invention, described adjuvant comprises disintegrating agent, filler, correctives, lubricant and binding agent.
In multiple adjuvant of the present invention, disintegrating agent is preferably and is selected from starch, pregelatinized Starch, carboxymethyl starch sodium, L-hydroxypropyl cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, sodium alginate and the microcrystalline Cellulose etc. one or more; Filler is preferably and is selected from lactose, mannitol, pregelatinized Starch, microcrystalline Cellulose and the calcium hydrogen phosphate one or more; Correctives is preferably and is selected from that Herba Menthae essence, stevioside, A Siba are sweet, in flavoring orange essence and the orange flavor one or more; Lubricant is preferably and is selected from micropowder silica gel, magnesium stearate and the Pulvis Talci one or more; Binding agent is preferably selected from polyvidone and hydroxypropyl methylcellulose.
With regard to the disintegrating agent that the present invention uses, except using above-mentioned disintegrating agent, can also use other disintegrating agent, for example, can also use methacrylic acid and divinylbenzene copolymer resins, guar gum, glucosan, citric acid or tartaric acid and sodium bicarbonate or sodium carbonate gas-producing disintegrant, Herba Xanthii glue etc.In addition, the consumption of disintegrating agent in moguisteine dispersible tablet of the present invention is 10 weight portions-50 weight portions, is preferably 15 weight portions-45 weight portion, more preferably 20 weight portions-35 weight portion.Make the content of disintegrating agent in moguisteine dispersible tablet satisfy above-mentioned scope and can guarantee to make that the consumption of disintegrating agent is less under the fast prerequisite of the rapid stripping of disintegrating agent of the present invention.
With regard to the filler that the present invention uses, except using above-mentioned filler, can also use other filler, for example, can also use starch, dextrin, sorbitol, calcium sulfate etc.In the present invention, the content of filler is 20 weight portions-80 weight portions, be preferably 30 weight portions-70 weight portion, 35 weight portions-60 weight portion more preferably, make the content of filler in moguisteine dispersible tablet satisfy molding and disintegrate that above-mentioned scope can help dispersible tablet, the stripping of medicine, and the sheet of the feasible dispersible tablet of making is heavily suitable, satisfies need of industrial production.
With regard to the correctives that the present invention uses, except using above-mentioned correctives, can also use other correctives, for example, can also use xylitol, sucrose, saccharin sodium, strawberry essence, rose essence, flavoring pineapple essence, flavoring banana essence.In the present invention, the content of correctives is 0.5 weight portion-3.0 weight portion, be preferably 0.5 weight portion-1.0 weight portion, make the content of correctives in moguisteine dispersible tablet satisfy the bitterness that above-mentioned scope can be corrected medicine effectively, make the dispersible tablet aqueous solution that makes fragrant and sweet good to eat, help patient and accept.If correctives content is higher than 3.0 weight portions, then is unfavorable for compression molding, and influences the disintegration of tablet.
With regard to the lubricant that the present invention uses, except using above-mentioned lubricant, can also use other lubricant, for example, can also use sodium laurylsulfate, hydrogenated vegetable oil, Semen Tritici aestivi starch.In the present invention, the content of lubricant is 0.4 weight portion-1.5 weight portion, is preferably 0.6 amount part-1.0 weight portions, makes the content of lubricant in moguisteine dispersible tablet satisfy above-mentioned scope and can guarantee the drug particles good fluidity, and is easy to manufacture and packing is accurate.
Preferably, according to " method described in two appendix of Chinese pharmacopoeia (version in 2005) is measured, moguisteine dispersible tablet of the present invention can be in 3 minutes disintegrate and reach homogeneously dispersed state fully, and the accumulation dissolution of moguisteine effective ingredient in 10 minutes is more than 60%.
In one aspect of the method, the invention provides a kind of preparation method of moguisteine dispersible tablet, it may further comprise the steps: (1) mixes the moguisteine of 5 weight portions-45 weight portion, the disintegrating agent of 10 weight portions-50 weight portion, the filler of 20 weight portions-80 weight portion and the correctives of 0.5 weight portion-3.0 weight portion, makes pre-composition; (2) the binding agent system soft material of adding 0.5 weight portion-2.5 weight portion in pre-composition; (3) with the gained soft material granulation; (4) with the gained particle drying; (5) with dried granule granulate; (6) lubricant that adds 0.4 weight portion-1.5 weight portion mixes, and carries out tabletting.
Preparation method of the present invention preferably also comprises: before the moguisteine raw material is crossed 100 mesh sieves in step (1), and the step of disintegrating agent, filler, correctives and lubricant being crossed 60 orders-80 mesh sieve.
In preparation method of the present invention, the granulation in the step (3) is preferably undertaken by the method for crossing the 16-24 mesh sieve; Drying in the step (4) is preferably undertaken by the method for forced air drying under 40 ℃ of conditions; Granulate in the step (5) is preferably undertaken by the method for dried granule being crossed the 24-30 mesh sieve.
In preparation method of the present invention, preferably, binding agent was dissolved in the dehydrated alcohol before using in advance, make that the concentration of gained solution is 3-10% (weight/volume).
In preparation method of the present invention, as indicated above moguisteine and all the other adjuvants are sieved before, can pulverize these materials.Crushing process mainly relies on the effect that adds mechanical force to destroy the intermolecular cohesiveness of described material and realizes.Material to be pulverized is subjected to producing very big stress and temperature in the part after the effect of external force and raises.The molecular separating force that surpasses material itself when stress can produce the crack and develop into the crack, then broken at last or cracking.The applied force that crushing process is commonly used has: impulsive force, compression stress, shearing force, bending force, abrasive power etc.In addition, the character for the treatment of material, degree of grinding difference, required externally applied forces is also different.
In the present invention, can adopt different grinding modes according to the requirement of the granularity of the character for the treatment of comminuting matter, product and the different conditions such as form of disintegrating apparatus, for example, inaccessible pulverize with the pulverizing of freely pulverizing, open a way with the circulation pulverizing, dry pulverization process is with waterproof pulverization, pulverize at low temperature and mix pulverizing etc.Wherein, dry pulverization process is that material is in the crushing operation that carries out under the drying regime.In the production of medicine, adopt dry pulverization process mostly.
In crushing process, can adopt polytype pulverizer, specifically select any pulverizer then to depend on granularity requirements to crushed products etc.Pulverizer commonly used has ball mill, impact grinder, fluid energy mill etc.
For the present invention, can adopt impact type Universalpulverizer method method that moguisteine principal agent and various adjuvant are pulverized.
Various materials can sieve it after pulverizing and finishing again.Screening is that varigrained material is carried out isolating operation by granule size.The medicine sieve of screening usefulness is divided into two kinds by its manufacture method, and a kind of is the dotting punch sieve, ties up to the sieve aperture of going out circle on the metallic plate and forms.Another kind is a wire gauze sieve, is to form with the tinsel of certain mechanical strength or the braiding of other nonmetal wire.
According to the industrial standard of China, medicine sieve " order " numerical table commonly used shows, promptly represents with the screen number on each inch (25.4mm) length.For example, per inch has the screen size in 100 holes to be labeled as 100 mesh sieves, and can claim 100 order powder by the powder of 100 sieves.In the present invention, respectively moguisteine and adjuvant are crossed 120 orders and 100 mesh sieves, operation helps making the moguisteine principal agent and the adjuvant mix homogeneously of poorly water-soluble like this, thereby helps the stripping of medicine.
After material sieves, with they mixings.Blending process is extremely important, and is particularly all the more so to the situations such as medicine of taking continuously for a long time.Drug content is inhomogeneous to bring great influence to bioavailability and therapeutic effect, even brings danger.Mixing for material is handled, and can adopt several different methods to carry out, for example, and V-type mixing method, the mixing method of milling, stirring slot type mixing method etc.In the present invention, mainly adopt the V-type mixing method to carry out mixing, this method is used very extensive, and mixing velocity is fast, easy and simple to handle.
Then, in the gained mixture, add binding agent system soft material.In the present invention, described binding agent is to be selected from a kind of in polyvidone and the hydroxypropyl methylcellulose.In addition, before using these binding agents, polyvidone and hydroxypropyl methylcellulose are dissolved in the dehydrated alcohol in advance, make that the concentration of gained solution is 3-10% (weight/volume).
Use the gained soft material granulation then.In medicine was produced, the method for granulating of extensive use can be divided into three major types: wet granulation, dry granulation and spray granulation.Wherein, wet granulation at first be liquid in the binding agent with the material particles moistened surface, make and produce adhesion strength between powder, then liquid build bridge with the effect that adds mechanical force under make the particulate method of definite shape and size.Formed granule is final after drying fixed with the form of solid bridge.The example of wet granulation has extruding to granulate, rotate the granulator granulation, high-speed stirred is granulated and fluidized bed granulation.
Then, carry out dried.The dry run of wet stock is the process that a heat transfer and mass transfer carry out simultaneously.In commercial production, the differences such as size of the character of material to be dried, degree of drying, production capacity, drying means that is adopted and equipment are also different.According to the mode of operation classification, drying means can be divided into batch (-type), continous way.Can be divided into gerotor type, vacuum type according to the operating pressure classification.Can be divided into conductive drying, convective drying, radiant drying, dielectric heating drying according to the heating means classification.And in dry run, can use multiple drying equipment, for example tray dryer, fluidized bed dryer, spray dryer, infrared dryer, microwave dryer etc.In the present invention, adopt tray dryer that the gained material is dried to water content and be less than or equal to 1 weight portion, this is dried particles.
Behind the dry materials, measure its water content, to determine whether drying reaches requirement.Fei Xiufa or toluene method are the methods of accurately measuring moisture.In the present invention, according to " Chinese pharmacopoeia (2005 editions) determination of water method is used Switzerland's prunus mume (sieb.) sieb.et zucc. Teller-Tuo benefit karl Fischer moisture test apparatus (METTLER TOLEDO DL32), adopts Fei Xiufa that the moisture in the dried material is measured.
At last, the dried particles with gained carries out tabletting through behind the granulate.Tablet machine commonly used can be divided into single punch tablet machine and rotary tablet machine by structure; Can be divided into round tablet machine and special-shaped tablet machine by compressed tablet shape; Can be divided into by the compression number of times and once to suppress tablet machine and secondary compacting tablet machine etc.Can select multiple sheeting equipment for use during tabletting, for example single punch tablet machine, 16 towards rotary tablet machine, 19 towards rotary tablet machine, 27 towards rotary tablet machine, 33 towards rotary tablet machine etc.In the present invention, adopt the tablet machine of one-shot to carry out tabletting.
So far, can obtain moguisteine dispersible tablet of the present invention, tablet can be rounded, and any surface finish.
Thus, moguisteine dispersible tablet of the present invention and the dispersible tablet by method of the present invention preparation have bioavailability height, the patient advantages such as the good and stable storing of compliance of taking medicine.
Followingly come the present invention is further specified, should be appreciated that to the invention is not restricted to these embodiment with reference to embodiment.In following examples 1-6, prepare 1000 moguisteine dispersible tablets respectively according to the method described in the embodiment 1-6.
At first, the moguisteine principal agent is crossed 100 mesh sieves, adjuvant (comprising disintegrating agent carboxymethyl base Starch Sodium, filler mannitol, the sweet and magnesium stearate lubricant of correctives A Siba) is crossed 60 orders-80 mesh sieve.
Then, it is sweet to take by weighing 25g moguisteine, 50g carboxymethyl starch sodium, 100g mannitol and 1.0g A Siba respectively, they are pressed equivalent incremental method mixing, the alcoholic solution system soft material that in the gained mixture, adds 3% (weight/volume) polyvidone of 40ml, cross 24 mesh sieves and granulate forced air drying under 40 ℃ of conditions again.
Pellet after the oven dry is crossed 24 mesh sieve granulate, to wherein adding the 1.6g magnesium stearate, mixing, tabletting promptly gets moguisteine dispersible tablet of the present invention.
According to " method described in two appendix of Chinese pharmacopoeia (version in 2005) is measured, and be 0.6 minute the disintegration of the dispersible tablet among this embodiment.
Embodiment 2
Prepare moguisteine dispersible tablet according to the method described in the embodiment 1, difference be to take by weighing the 50g moguisteine as principal agent, take by weighing 20g cross-linking sodium carboxymethyl cellulose and 50g polyvinylpolypyrrolidone as disintegrating agent, take by weighing 80g mannitol and 100g pregelatinized Starch as filler, to take by weighing 1.2g A Siba sweet in correctives, and the alcoholic solution of 5% (weight/volume) polyvidone that uses 60ml as binding agent, 3g magnesium stearate as lubricant.
According to " method described in two appendix of Chinese pharmacopoeia (version in 2005) is measured, and be 1.1 minutes the disintegration of the dispersible tablet among this embodiment.
Embodiment 3
Prepare moguisteine dispersible tablet according to the method described in the embodiment 1, difference be to take by weighing the 75g moguisteine as principal agent, take by weighing the 80g polyvinylpolypyrrolidone as disintegrating agent, take by weighing 100g microcrystalline Cellulose and 150g mannitol as filler, to take by weighing 1.5g A Siba sweet in correctives, and the alcoholic solution of 5% (weight/volume) polyvidone that uses 75ml as binding agent, 4g magnesium stearate as lubricant.
According to " method described in two appendix of Chinese pharmacopoeia (version in 2005) is measured, and be 2.1 minutes the disintegration of the dispersible tablet among this embodiment.
Embodiment 4
Prepare moguisteine dispersible tablet according to the method described in the embodiment 1, difference be to take by weighing the 100g moguisteine as principal agent, take by weighing 50g cross-linking sodium carboxymethyl cellulose and 80g polyvinylpolypyrrolidone as disintegrating agent, take by weighing the 200g microcrystalline Cellulose as filler, to take by weighing 2g A Siba sweet in correctives, and the alcoholic solution of 5% (weight/volume) polyvidone that uses 100ml as binding agent, 4g magnesium stearate as lubricant.
According to " method described in two appendix of Chinese pharmacopoeia (version in 2005) is measured, and be 1.5 minutes the disintegration of the dispersible tablet among this embodiment.
Embodiment 5
Prepare moguisteine dispersible tablet according to the method described in the embodiment 1, difference be to take by weighing the 150g moguisteine as principal agent, take by weighing 40g low-substituted hydroxypropyl cellulose and 120g polyvinylpolypyrrolidone as disintegrating agent, take by weighing 100g microcrystalline Cellulose and 100g mannitol as filler, to take by weighing 4g A Siba sweet in correctives, and the alcoholic solution of 5% (weight/volume) polyvidone that uses 150ml as binding agent, 5g magnesium stearate as lubricant.
According to " method described in two appendix of Chinese pharmacopoeia (version in 2005) is measured, and be 1.8 minutes the disintegration of the dispersible tablet among this embodiment.
Embodiment 6
Prepare moguisteine dispersible tablet according to the method described in the embodiment 1, difference be to take by weighing the 200g moguisteine as principal agent, take by weighing 50g low-substituted hydroxypropyl cellulose and 200g polyvinylpolypyrrolidone as disintegrating agent, take by weighing 250g mannitol as filler, to take by weighing 5g A Siba sweet in correctives, and the alcoholic solution of 5% (weight/volume) polyvidone that uses 250ml as binding agent, 7g magnesium stearate as lubricant.
According to " method described in two appendix of Chinese pharmacopoeia (version in 2005) is measured, and be 2.5 minutes the disintegration of the dispersible tablet among this embodiment.
Embodiment 7: moguisteine dispersible tablet dispersing uniformity and dissolution in vitro detect
1. the moguisteine dispersible tablet dispersing uniformity is checked
According to " the dispersible tablet uniformity detecting method of putting down in writing in two appendix of Chinese pharmacopoeia (version in 2005), get respectively embodiment 1-6 moguisteine dispersible tablet each 2, put in 20 ℃ ± 1 ℃ the 100ml water, jolting 3 minutes, the result is the whole disintegrates of the moguisteine dispersible tablet of embodiment 1-6 and passes through sieve No. two.The results are shown in Table 1.
2. the mensuration of moguisteine dispersible tablet dissolution in vitro
According to " the method for putting down in writing among two appendix XC of Chinese pharmacopoeia (version in 2005), measure the dissolution in vitro of the moguisteine dispersible tablet among the embodiment 1-6 respectively, described method is as follows: get the moguisteine dispersible tablet among each embodiment, 0.3 weight % lauryl sodium sulfate aqueous solution with 900ml is dissolved described dispersible tablet as dissolution medium, after 45 minutes, the 10ml that takes a sample automatically is as specimen with 75 rev/mins speed stirrings; Other gets an amount of moguisteine standard substance (deriving from Switzerland Roche Holding Ag), adds described dissolution medium dissolving, is mixed with the solution that contains 60 μ g among every 1ml, adopt spectrophotography, measure above-mentioned two kinds of solution absorbency respectively at 274nm wavelength place, thus, calculate every dissolution.The dispersible tablet that the accumulation dissolution reaches labelled amount 80% is up to specification.The results are shown in Table 1.
Table 1: the cumulative in vitro dissolution and the disintegration of the moguisteine dispersible tablet among the embodiment 1-6
As can be seen from Table 1, the internal energy whole disintegrates in 3 minutes of the moguisteine dispersible tablet of embodiment 1-6 also can be sieved by No. 2, meet that " Chinese pharmacopoeia is about the regulation of disintegration.Yet, because specification (content) difference of moguisteine principal agent among the embodiment 1-6, and this medicine poorly water-soluble, not stripping completely of medicine in the short period of time, thus cause the initial period dissolution that bigger difference is arranged, but the absolute magnitude of stripping is more or less the same.It is complete that the moguisteine dispersible tablet of embodiment 1-6 can stripping in 45 minutes, and dissolution is all more than 90%.
Embodiment 8: measure moguisteine dispersible tablet agent of the present invention at the intravital blood drug level of beasle dog
12 male beasle dogs (body weight 10-13.2kg) (deriving from Zhongshan University zoopery center) are divided into 2 groups at random.In one group, irritate stomach respectively and give the moguisteine dispersible tablet of every beasle dog with preparation among the embodiment 4 therein, medication is to irritate stomach every day once, each 100mg; In other one group, irritate stomach in the same manner respectively and give every beasle dog with homemade moguisteine reference tablet (deriving from Dongguan TaiLi Biology Engineering Co., Ltd).After the administration respectively at 0.25 hour, 0.5 hour, 1 hour, 1.5 hours, 2 hours, 3 hours, 6 hours, 8 hours and 12 hours by every beasle dog lower limb venous blood collection 3ml, blood sample is measured blood drug level with the HPLC-MS method of setting up after treatment.Make the average blood drug level and the time relation curve of moguisteine dispersible tablet of the present invention and commercially available moguisteine tablet reference substance, see Fig. 1.
As shown in Figure 1, compare with the moguisteine tablet, take moguisteine dispersible tablet of the present invention and have following characteristics: drug absorption is rapid, and peak time is fast, the peak concentration height.It is rapid to show that preparation of the present invention has an onset, the bioavailability height, and preparation technology is simple, characteristics such as taking convenience.
The present invention is not limited to the foregoing description, should be appreciated that those skilled in the art can make various modifications and change to the present invention under the condition that does not break away from the spirit and scope of the invention.
Claims (10)
1. moguisteine dispersible tablet, it contains:
The moguisteine of 5 weight portions-45 weight portion; The disintegrating agent of 10 weight portions-50 weight portion; The filler of 20 weight portions-80 weight portion; 0.5 the correctives of weight portion-3.0 weight portion; 0.4 the lubricant of weight portion-1.5 weight portion; 0.5 the binding agent of weight portion-2.5 weight portion.
2. moguisteine dispersible tablet according to claim 1, it contains:
The moguisteine of 15 weight portions-30 weight portion; The described disintegrating agent of 20 weight portions-35 weight portion; The described filler of 35 weight portions-60 weight portion; 0.5 the described correctives of weight portion-1.0 weight portion; 0.6 the described lubricant of weight portion-1.0 weight portion; 0.5 the described binding agent of weight portion-1.5 weight portion.
3. moguisteine dispersible tablet according to claim 1, wherein said disintegrating agent are to be selected from starch, pregelatinized Starch, carboxymethyl starch sodium, L-hydroxypropyl cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, sodium alginate and the microcrystalline Cellulose etc. one or more; Described filler is to be selected from lactose, mannitol, pregelatinized Starch, microcrystalline Cellulose and the calcium hydrogen phosphate one or more; Described correctives be selected from that Herba Menthae essence, stevioside, A Siba are sweet, in flavoring orange essence and the orange flavor one or more; Described lubricant is to be selected from micropowder silica gel, magnesium stearate and the Pulvis Talci one or more; Described binding agent is selected from polyvidone and hydroxypropyl methylcellulose.
4. moguisteine dispersible tablet according to claim 1, wherein this moguisteine dispersible tablet fully disintegrate and reach homogeneously dispersed state in 3 minutes, and the accumulation dissolution of moguisteine effective ingredient in 10 minutes is more than 60%.
5. method for preparing the described moguisteine dispersible tablet of claim 1, it may further comprise the steps:
(1) moguisteine of 5 weight portions-45 weight portion, the disintegrating agent of 10 weight portions-50 weight portion, the filler of 20 weight portions-80 weight portion and the correctives of 0.5 weight portion-3.0 weight portion are mixed, make pre-composition;
(2) the binding agent system soft material of adding 0.5 weight portion-2.5 weight portion in described pre-composition;
(3) with the gained soft material granulation;
(4) with the gained particle drying;
(5) with dried granule granulate;
(6) lubricant that adds 0.4 weight portion-1.5 weight portion mixes, and carries out tabletting.
6. method according to claim 5, this method also comprises:
Before the moguisteine raw material is crossed 100 mesh sieves in step (1), and the step of described disintegrating agent, described filler, described correctives and described lubricant being crossed 60 orders-80 mesh sieve.
7. method according to claim 5, wherein the granulation described in the step (3) is to be undertaken by the method for crossing the 16-24 mesh sieve.
8. method according to claim 5, wherein the drying described in the step (4) is to be undertaken by the method for forced air drying under 40 ℃ of conditions.
9. method according to claim 4, wherein the granulate described in the step (5) is to be undertaken by the method for described dried granule being crossed the 24-30 mesh sieve.
10. method according to claim 5, wherein said binding agent will be dissolved in the dehydrated alcohol before using in advance, made that the concentration of gained solution is 3-10% (weight/volume).
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| CN200810126261A CN101637461A (en) | 2008-07-28 | 2008-07-28 | Moguisteine dispersible tablet and preparation method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102078308A (en) * | 2010-12-29 | 2011-06-01 | 蚌埠丰原涂山制药有限公司 | Aspirin lysine dispersible tablet and preparation method thereof |
| CN102192971A (en) * | 2011-03-18 | 2011-09-21 | 辽宁省计量科学研究院 | Disintegration time limit testing standard substance and preparation method thereof |
| CN102578564A (en) * | 2011-11-01 | 2012-07-18 | 江苏江山制药有限公司 | Preparation method for rapid-disintegrating directly-pressed particle mannitol preparation |
| CN111150710A (en) * | 2020-01-21 | 2020-05-15 | 于广华 | Medicament composition of high-load lubricant and preparation method thereof |
-
2008
- 2008-07-28 CN CN200810126261A patent/CN101637461A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102078308A (en) * | 2010-12-29 | 2011-06-01 | 蚌埠丰原涂山制药有限公司 | Aspirin lysine dispersible tablet and preparation method thereof |
| CN102192971A (en) * | 2011-03-18 | 2011-09-21 | 辽宁省计量科学研究院 | Disintegration time limit testing standard substance and preparation method thereof |
| CN102192971B (en) * | 2011-03-18 | 2013-09-04 | 辽宁省计量科学研究院 | Disintegration time limit testing standard substance and preparation method thereof |
| CN102578564A (en) * | 2011-11-01 | 2012-07-18 | 江苏江山制药有限公司 | Preparation method for rapid-disintegrating directly-pressed particle mannitol preparation |
| CN111150710A (en) * | 2020-01-21 | 2020-05-15 | 于广华 | Medicament composition of high-load lubricant and preparation method thereof |
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