CN102824312B - Aceclofenac enteric-coated pellet particle composition and preparation method thereof - Google Patents
Aceclofenac enteric-coated pellet particle composition and preparation method thereof Download PDFInfo
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Abstract
The invention relates to the field of a medicinal preparation, in particular to an aceclofenac enteric-coated pellet particle composition and a preparation method of the aceclofenac enteric-coated pellet particle composition. The aceclofenac enteric-coated pellet particles are higher in dissolution rate due to the fact that the dissolution rate is more than 75% within 45 minutes, the bioavailability is better and reaches up to 92.67%, and the taste is better. The preparation method is convenient to operate, thereby being suitable for industrial production.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, particularly aceclofenac enteric coated micropill particulate composition and preparation method thereof.
Background technology
Inflammation is very common and important basic pathology process, most of commonly encountered diseases of the trauma infection contamination of body surface and each organ and frequently-occurring disease (as furuncle, carbuncle, pneumonia, hepatitis, nephritis etc.) all belong to diseases associated with inflammation, be body for a kind of defense reaction stimulating, show as red, swollen, hot, bitterly and dysfunction.Wherein, acute inflammation be body the stimulation of pro-inflammatory cytokine is occurred immediately and early reaction.Acutely inflamed main feature is the exudative variation centered by vascular reaction, causes endovascular leukocyte and antibody etc. to see through blood vessel wall and enters inflammatory reaction position, and eliminating pathogen, dilutes and neutralize a toxin, for good condition is created in inflammation reparation.The course of disease of chronic inflammatory disease is longer, and the several months is to more than the several years.Can be delayed by acute inflammation, or because the light also persistent period of stimulation of pro-inflammatory cytokine is longer, be at the beginning chronic process.As tuberculosis or autoimmune disease etc.During chronic inflammatory disease, local patholoic change is changed into master mainly with hypertrophy, goes bad and oozes out lighter; Cell infiltration is main mainly with lymphocyte, macrophage and plasma cell.When inflammation is more serious, due to the effect of pathogenic microorganism and toxin thereof, and the impact of the factor such as local blood circulation obstacle, heating, can there is degeneration, necrosis and organ dysfunction in various degree in the parenchyma of the organs such as the heart, liver, kidney.
Aceclofenac is a new synthetic orally active non-steroid, phenylacetic acid class antiinflammatory, antipyretic, analgesic.Aceclofenac structurally, relevant with the fragrant acid of diclofenac, alclofenac and fragrant chlorine, in clinical practice, the pharmacological action of summary is compared with other non-steroid medicines (NSAIDs), and it act as feature to have obviously antiinflammatory action widely, powerful analgesia and antipyretic and stomach toxicity in Acute and chronic inflammation experimental model.This medicine is gone on the market with exploitations such as trade name Airtl sancin by Spain Pu Ludesi drugmaker for 1992 first.After in succession in the listing of the U.S., Britain.Be applicable to clinically treat rheumatic arthritis, rheumatoid arthritis, osteoarthritis, spondylitis etc.Also be applicable to pain and heating that various diseases causes.
But because aceclofenac itself has pungent sense, there is oral distasteful problem in common oral formulations; And aceclofenac is slightly soluble in water, easily cause the untoward reaction such as dyspepsia, abdominal discomfort, oral cavity and gastrointestinal tract are produced to zest.The distribution area of existing aceclofenac preparation in gastrointestinal tract is little, dissolution is lower, bioavailability is not high, has reduced the curative effect of medicine itself.
Summary of the invention
In view of this, the invention provides aceclofenac enteric coated micropill particulate composition and preparation method thereof.The dissolution of this aceclofenac compositions micropill granule is higher, and within 45 minutes, dissolution all exceedes 75%, and bioavailability is better, and mouthfeel is better, reaches 92.67%.
In order to realize foregoing invention object, the invention provides following technical scheme:
The invention provides a kind of aceclofenac compositions micropill granule, it is comprised of ball core and pharmaceutically acceptable coating material;
Ball core comprises aceclofenac, filler and binding agent;
In g/mL, the mass volume ratio of ball core and pharmaceutically acceptable coating material is 700～800:750～900.
In some embodiments of the invention, in the ball core of aceclofenac compositions micropill granule provided by the invention, the mass ratio of aceclofenac, filler and binding agent is 40～60:700～800:0.5～2.5.
In some embodiments of the invention, the pharmaceutically acceptable coating material of aceclofenac compositions micropill granule provided by the invention comprises acrylic resin, surfactant, plasticizer, wetting agent and screening agent.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, the volume ratio of surfactant, plasticizer, wetting agent is 2.5～7.5:10～20:700～800.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, the mass ratio of acrylic resin and screening agent is 25～35:20～30.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, in g/mL, the mass volume ratio of acrylic resin and wetting agent is 25～35:700～800.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, acrylic resin is acrylic resin II.
Be preferably enteric acrylic resin II, it is obtained in the copolymerization of 50:50 ratio by methacrylic acid and methyl methacrylate, is anionic polymer.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, surfactant is tween 80.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, plasticizer is diethyl phthalate and/or Oleum Ricini.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, wetting agent is ethanol.
As preferably, the concentration of ethanol is 70～95%.
Preferably, the concentration of ethanol is 85～95%.
Preferably, in coating solution, the concentration of acrylic resin II (being preferably enteric acrylic resin II) is 2～12%.
Preferably, in coating solution, the concentration of acrylic resin II (being preferably enteric acrylic resin II) is 2～4%.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, screening agent is Pulvis Talci.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, filler is starch and/or lactose.
In some embodiments of the invention, in aceclofenac compositions micropill granule provided by the invention, binding agent is sodium carboxymethyl cellulose.
The present invention also provides a kind of preparation method of aceclofenac compositions micropill granule, comprises the steps:
Step 1: taking adhesive preparation obtains binder solution, adds aceclofenac, filler, prepares ball core; Spheronization is extruded in concrete adopting, and first will after supplementary material mix homogeneously, add binding agent pill again; Or employing centrifugal granulation, first by supplementary material powder mix homogeneously, get mixed powder and spray into binding agent and amplify and make gradually.
Step 2: get pharmaceutically acceptable coating material preparation and obtain coating solution;
Step 3: get ball core and mix rear coating with coating solution, obtain; Be specially coating solution is carried out being sprayed on ball wicking surface film forming after atomization.
In g/mL, the mass volume ratio of ball core and pharmaceutically acceptable coating material is 7000～8000:750～900.
In some embodiments of the invention, in the ball core of aceclofenac compositions micropill granule provided by the invention, pharmaceutically acceptable coating material comprises acrylic resin, surfactant, plasticizer, wetting agent and screening agent.
In some embodiments of the invention, in the ball core of aceclofenac compositions micropill granule provided by the invention, the mass ratio of the fragrant acid of chlorine, filler and binding agent is 40～60:7000～8000:0.5～2.5.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, the volume ratio of surfactant, plasticizer, wetting agent is 2.5～7.5:10～20:700～800.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, the mass ratio of acrylic resin and screening agent is 25～35:20～30.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, in g/mL, the mass volume ratio of acrylic resin and wetting agent is 25～35:700～800.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, acrylic resin is EudragitⅡ.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, surfactant is tween 80.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, plasticizer is Oleum Ricini.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, wetting agent is ethanol.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, screening agent is Pulvis Talci.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, filler is starch and/or lactose.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, binding agent is sodium carboxymethyl cellulose.
In some embodiments of the invention, in the preparation method of aceclofenac compositions micropill granule provided by the invention, the diameter of ball core is 1.0～1.2mm.
The invention provides aceclofenac enteric coated micropill particulate composition and preparation method thereof.The dissolution of this aceclofenac compositions micropill granule is higher, and within 45 minutes, dissolution all exceedes 75%, and bioavailability is better, and mouthfeel is better, reaches 92.67%.This preparation method is easy and simple to handle, is suitable for suitability for industrialized production.
The specific embodiment
The invention discloses aceclofenac enteric coated micropill particulate composition and preparation method thereof, those skilled in the art can use for reference content herein, suitably improve technological parameter and realize.Special needs to be pointed out is, all similar replacements and change apparent to those skilled in the artly, they are all deemed to be included in the present invention.Method of the present invention and application are described by preferred embodiment, related personnel obviously can change methods and applications as herein described in content of the present invention, spirit and scope or suitably change and combination not departing from, and realizes and apply the technology of the present invention.
In aceclofenac enteric coated micropill particulate composition provided by the invention and preparation method thereof, medicine used, pharmaceutically acceptable adjuvant all can be buied by market.
Below in conjunction with embodiment, further set forth the present invention:
Embodiment 1
Accurately take 2.5g binding agent (sodium carboxymethyl cellulose) and add water 500mL preparation to obtain binder solution, then add 50g aceclofenac, 720g starch, 30g lactose, preparing diameter is the ball core of 1.0mm;
Get 25g EudragitⅡ, 5.5mL tween 80,20mL Oleum Ricini, 750mL ethanol and the preparation of 20g Pulvis Talci and obtain coating solution;
In g/mL, getting ball core is coating after 700:900 mixes with coating solution according to mass volume ratio, obtains.
Embodiment 2
Accurately take 0.5g binding agent (sodium carboxymethyl cellulose) and add water 100mL preparation to obtain binder solution, then add 45g aceclofenac, 680g starch, 20g lactose, preparing diameter is the ball core of 1.1mm;
Get 35g EudragitⅡ, 6.0mL tween 80,10mL Oleum Ricini, 770mL ethanol and the preparation of 30g Pulvis Talci and obtain coating solution;
In g/mL, getting ball core is coating after 800:750 mixes with coating solution according to mass volume ratio, obtains.
Embodiment 3
Accurately take 1.5g binding agent (sodium carboxymethyl cellulose) and add water 300mL preparation to obtain binder solution, then add 55g aceclofenac, 797.5g starch, 25g lactose, preparing diameter is the ball core of 1.0mm;
Get 30g EudragitⅡ, 4.0mL tween 80,15mL Oleum Ricini, 730mL ethanol and the preparation of 25g Pulvis Talci and obtain coating solution;
In g/mL, getting ball core is coating after 750:800 mixes with coating solution according to mass volume ratio, obtains.
Embodiment 4
Accurately take 1.0g binding agent (sodium carboxymethyl cellulose) and add water 200mL preparation to obtain binder solution, then add 50g aceclofenac, 740g starch, 28g lactose, preparing diameter is the ball core of 1.0mm;
Get 32g EudragitⅡ, 5.0mL tween 80,13mL Oleum Ricini, 800mL ethanol and the preparation of 28g Pulvis Talci and obtain coating solution;
In g/mL, getting ball core is coating after 720:850 mixes with coating solution according to mass volume ratio, obtains.
Embodiment 5
Accurately take 2.0g binding agent (sodium carboxymethyl cellulose) and add water 400mL preparation to obtain binder solution, then add 40g aceclofenac, 765g starch, 22g lactose, preparing diameter is the ball core of 1.2mm;
Get 28g EudragitⅡ, 7.5mL tween 80,18mL Oleum Ricini, 750mL ethanol and the preparation of 22g Pulvis Talci and obtain coating solution;
In g/mL, getting ball core is coating after 770:780 mixes with coating solution according to mass volume ratio, obtains.
Embodiment 6
Accurately take 1.8g binding agent and add water 360mL preparation to obtain binder solution, then add 60g aceclofenac, 765g filler, preparing diameter is the ball core of 1.2mm;
Get 30g acrylic resin, 2.5mL surfactant, 16mL plasticizer, 700mL wetting agent and the preparation of 25g screening agent and obtain coating solution;
In g/mL, getting ball core is coating after 730:880 mixes with coating solution according to mass volume ratio, obtains.
Embodiment 7 dissolutions detect
Instrument: ZRK6-B type drug dissolution instrument (University Of Tianjin); Japan Shimadzu LC-10Avp high performance liquid chromatograph.
The mensuration of stripping curve: get the aceclofenac granule that the embodiment of the present invention 1 to 6 makes, according to drug release determination method, take muriatic hydrochloric acid solution 500ml as solvent, rotating speed is per minute 100 to turn, operation in accordance with the law, through 2 hours, the random 0.236mol/L disodium phosphate soln 400ml that is preheated to 37 ℃ that adds in process container, continue operation in accordance with the law, in the time of 5,10,20,30,45,60 and 90 minutes, get solution and filter, precision measures subsequent filtrate 5ml and puts in tool plug test tube, add 0.25mol/L sodium hydroxide solution 1.0ml, shake up, as need testing solution.The aceclofenac reference substance 20mg of potassium hydroxide drying under reduced pressure to constant weight separately learns from else's experience, accurately weighed, put in 100ml measuring bottle, add after ethanol 10ml dissolving, add phosphate buffer (PH6.8) and be diluted to scale, precision measures 5ml and puts in the brown measuring bottle of 50ml, be diluted to scale with above-mentioned buffer, shake up, precision measures 5ml and puts and in tool plug test tube, add 0.25mol/L sodium hydroxide solution 1.0ml, shake up, in contrast product solution.According to the chromatographic condition under assay item, test, get the above-mentioned two kinds of each 20ul injection liquid of solution chromatographies, measure in accordance with the law, calculate the release of every, the results are shown in Table 1, matched group the results are shown in Table 2.
The dissolution determination result of table 1 aceclofenac granule provided by the invention
Table 2 matched group dissolution determination result
Result shows, the aceclofenac granule that the embodiment of the present invention 1 to 6 makes reaches the regulation of the national drug standards (WS1-(X-035)-99Z) to dissolution, and according to dissolution curve, within 45 minutes, dissolution all exceedes 75%.
The impact of adjuvant on dissolution determination: get adjuvant, prepare solution, injection liquid chromatography with dissolution medium.Peak position place at aceclofenac has no chromatographic peak, shows measuring noiseless.
Embodiment 8
Chromatography is differentiated
Principle: in the chromatogram recording under assay item, the retention time of need testing solution main peak should be consistent with the retention time of reference substance solution main peak.Be aceclofenac and reference substance thereof under identical chromatographic conditions, should there is identical retention time.
Chromatographic condition is with chromatographic condition under assay item.
Method according to assay is measured, and the results are shown in Table 3.
Table 3 aceclofenac granule provided by the invention principal agent testing result
| Group | Retention time (min) |
| Embodiment 1 | 3.878 |
| Embodiment 2 | 3.885 |
| Embodiment 3 | 3.873 |
| Embodiment 4 | 3.881 |
| Embodiment 5 | 3.877 |
| Embodiment 6 | 3.883 |
| Reference substance | 3.882 |
The aceclofenac granule that the embodiment of the present invention 1 to 6 makes has identical chromatograph keeping characteristics with reference substance.
The detection of related substance:
Chromatographic condition is with chromatographic condition under assay item.
Specificity and separating degree are investigated: investigate the separation case of this chromatographic system to raw material sample after various destruction (heat-flash destruction, illumination destruction, high temperature destroy, acid destroys and alkali destroys).Destruction methods is as follows:
Acid destroys: get the aceclofenac granule appropriate (being approximately equivalent to principal agent 20mg) that the embodiment of the present invention 1 to 6 makes, add 100ml water dissolution, get 1ml in 10ml scale test tube, add 0.1mol/L hydrochloric acid to 2ml, put in boiling water bath and destroy 4 hours.
Alkali destroys: get the aceclofenac granule appropriate (being approximately equivalent to principal agent 20mg) that the embodiment of the present invention 1 to 6 makes, add 100mI water dissolution, get 1mI in lOml scale test tube, add 0.1mol/L sodium hydroxid to 2mI, put in boiling water bath and destroy 4 hours.
Photo damage: get the aceclofenac granule appropriate (being approximately equivalent to principal agent 20mg) that the embodiment of the present invention 1 to 6 makes, add 100ml water dissolution, get lml in 10ml scale test tube, add water to 2mI, put under sunlight and destroy 8 hours.
High temperature destroys: get the aceclofenac granule appropriate (being approximately equivalent to principal agent 20mg) that the embodiment of the present invention 1 to 6 makes, add 100mI water dissolution, get lml in 10m1 scale test tube, add water to 2ml, put in boiling water bath and destroy 4 hours.
Heat-flash destroys: get the aceclofenac granule appropriate (being approximately equivalent to principal agent 20mg) that the embodiment of the present invention 1 to 6 makes, straight fire is heated to micro-yellow, adds 100ml water dissolution, gets 1ml in 10ml scale test tube, adds water to 2ml.
Above-mentioned each sample is added to mobile phase and make the solution containing aceclofenac 0.01mg in every 1ml, precision measures need testing solution 20ul, and injection liquid chromatography, records chromatogram, investigates the reservation situation of various materials.Result shows, this chromatographic system can be separation with catabolite by principal agent, and separation case is better.Can be used for the related substance inspection of the aceclofenac granule that the embodiment of the present invention 1 to 6 makes.
Related substance inspection technique: get the aceclofenac granule that the embodiment of the present invention 1 to 6 makes appropriate, add mobile phase and make the solution containing aceclofenac 0.lmg in every lml, as need testing solution; It is appropriate that precision measures above-mentioned need testing solution, adds mobile phase and make the solution containing 0.001mg in every lml, liquid in contrast; Precision measures contrast liquid 20ul, and injection liquid chromatography, regulates instrumental sensitivity, and making main constituent peak height is the 20-25% of full scale; Another precision measures need testing solution 20ul, and injection liquid chromatography, records the twice of chromatogram to main constituent peak retention time, measure impurity peak area and, must not be greater than (3.0%) of contrast liquid peak area, the results are shown in Table 4.
The aceclofenac granule related substance check result that table 4 embodiment of the present invention 1 to 6 makes
| Group | Related substance (%) |
| Embodiment 1 | ?0.876 |
| Embodiment 2 | ?0.99 |
| Embodiment 3 | ?0.827 |
| Embodiment 4 | ?0.851 |
| Embodiment 5 | ?0.843 |
| Embodiment 6 | ?0.928 |
According to inspection, related substance inspection is all no more than 1%.
Limit test of microbe:
Get the embodiment of the present invention 1 to 6, by microbial limit test, check, should conform with the regulations.On inspection, three batches of test samples all conform with the regulations.
Assay: the content of the aceclofenac granule that the employing high effective liquid chromatography for measuring embodiment of the present invention 1 to 6 provides.
Instrument: Japanese Shimadzu LC-10Avp high performance liquid chromatograph;
Chromatographic condition:
Immobile phase: octadecylsilane key and silica gel;
Mobile phase: methanol-water-triethylamine-phosphoric acid (67:33:0.3:0.12);
Detect wavelength: 302nm;
Flow velocity: 1.0ml/min.
Assay:
Get contents mixed under content uniformity item even, porphyrize, precision takes in right amount (being approximately equivalent to aceclofenac 20mg), put in the brown measuring bottle of 100ml, add the about 60ml of phosphate buffer, supersound process is dissolved aceclofenac, add ethanol 20ml, add above-mentioned buffer and be diluted to scale, precision measures 5ml, puts in the brown measuring bottle of 50ml, be diluted with water to scale, shake up, precision measures 20ul chromatograph of liquid, records chromatogram.Separately learn from else's experience potassium hydroxide drying under reduced pressure to the aceclofenac reference substance 20mg of constant weight, accurately weighed, be measured in the same method, by external standard method, with calculated by peak area, the results are shown in Table 5.
The aceclofenac particle content measuring result that table 5 embodiment of the present invention 1 to 6 provides
On inspection, the content of the aceclofenac granule that the embodiment of the present invention 1 to 6 provides all, in prescribed limit, has identical content characteristics with the product of being imitated.
The aceclofenac granule that adopts the quality standard check embodiment of the present invention 1 to 6 of above-mentioned research to provide, the results are shown in Table 6.
The aceclofenac granule measurement result that table 6 embodiment of the present invention 1 to 6 provides
Embodiment 9
In order to investigate medicine time dependent rule under the impact of temperature, humidity, illumination, for production, storage, packing, the transportation of medicine provides the foundation of science, by test, set up the effect duration of medicine simultaneously, according to Chinese Pharmacopoeia relevant regulations, the stability of the aceclofenac granule that the embodiment of the present invention 1 to 6 is provided is investigated.
Sample, reagent and instrument:
Sample: the aceclofenac granule that the embodiment of the present invention 1 to 6 provides.
Reagent: methanol (chromatographic eluents, Shandong YuWang Industry Co.,Ltd); Triethylamine (analytical pure, Shenyang He Fu chemical reagent work); Phosphoric acid (analytical pure, Shandong YuWang Industry Co.,Ltd).
Instrument: super calorstat (501 types, Shanghai test apparatus factory); Photoelectric analytical balance (TG328A type, Shanghai balance equipment factory); High performance liquid chromatograph (Japanese Shimadzu Corporation).
Investigation project: the variations such as checkout facility front and back this product outward appearance, color and luster, character.
Test basis: according to Chinese Pharmacopoeia relevant regulations, carry out study on the stability.
Influence factor test: 40 ℃ of temperature, place test in 6 months under relative humidity 75% condition, obviously change does not all occur its inspection item, illustrates that the aceclofenac granule that the embodiment of the present invention 1 to 6 provides is basicly stable.
In room temperature, place test in 6 months, its inspection item does not all occur obviously to change, and illustrates that the aceclofenac granule that the embodiment of the present invention 1 to 6 provides is basicly stable.
Under high humidity, illumination condition, content slightly declines, and under hot conditions, slightly changes.Therefore it is perishable that the aceclofenac granule that the embodiment of the present invention 1 to 6 provides is met light, answer shading to preserve.
Accelerated test: the aceclofenac granule that the embodiment of the present invention 1 to 6 is provided is by commercially available back, is placed in sample under the condition of 40 ℃ ± 2 ℃ of relative humiditys 75% ± 5%, temperature and places and within 6 months, carry out accelerated test.Experimental result shows that its appearance luster, loss on drying, content, related substance etc. relatively had no significant change with 0 time.
Long term test: press commercially available back, the aceclofenac granule that the embodiment of the present invention 1 to 6 is provided is placed and is carried out long term test 36 months under the condition of 25 ℃ ± 2 ℃ of temperature, relative humidity 60% ± 10%, and experimental result shows that its appearance luster, loss on drying, content, related substance etc. relatively had no significant change with 0 time.
It is basicly stable under listing terms of packing that accelerated test and long term test are investigated the aceclofenac granule that result shows that the embodiment of the present invention 1 to 6 provides, this terms of packing can meet medicine to storing the requirement of traffic condition, the storage requirement of the aceclofenac granule that the embodiment of the present invention 1 to 6 is provided is defined as shading, sealing, preserves at cold place.According to current stability test result, with reference to the national drug standards, this product effect duration being fixed tentatively is 24 months.
Embodiment 10
In national northwest, southwest, northeast, North China, the southeast, Central China, choose at random respectively 1080 altogether of each age group, every profession and trade personages, according to age, engaged in trade, be divided into 36 groups, every group of 30 surveyees, the aceclofenac granule that the embodiment of the present invention 1 to 6 is provided carries out mouthfeel evaluation, evaluation criterion is in Table 7, and evaluation result is in Table 28.
Table 7 mouthfeel evaluation criterion
The evaluation result of table 8 aceclofenac granule provided by the invention
By survey result, shown, from national northwest, southwest, northeast, North China, the southeast, Central China's each age group, every profession and trade personage, altogether in 1080 surveyees, the aceclofenac granule mouthfeel satisfaction rate that the embodiment of the present invention 1 to 6 is provided is 92.67%.
The above is only the preferred embodiment of the present invention; it should be pointed out that for those skilled in the art, under the premise without departing from the principles of the invention; can also make some improvements and modifications, these improvements and modifications also should be considered as protection scope of the present invention.
Claims (2)
1. an aceclofenac compositions micropill granule, is characterized in that, it is comprised of ball core and pharmaceutically acceptable coating material;
Described ball core comprises aceclofenac, filler and binding agent;
In g/mL, the mass volume ratio of described ball core and described pharmaceutically acceptable coating material is 700～800:750～900;
In described ball core, the mass ratio of described aceclofenac, described filler and described binding agent is 40～60:700～800:0.5～2.5;
Described pharmaceutically acceptable coating material comprises acrylic resin, surfactant, plasticizer, wetting agent and screening agent;
The volume ratio of described surfactant, described plasticizer, described wetting agent is 2.5～7.5:10～20:700～800;
The mass ratio of described acrylic resin and described screening agent is 25～35:20～30;
In g/mL, the mass volume ratio of described acrylic resin and described wetting agent is 25～35:700～800;
The diameter of described ball core is 1.0～1.2mm;
Described acrylic resin is EudragitⅡ;
Described surfactant is tween 80;
Described plasticizer is Oleum Ricini;
Described wetting agent is ethanol;
Described screening agent is Pulvis Talci;
Described filler is starch and/or lactose;
Described binding agent is sodium carboxymethyl cellulose.
2. a preparation method for aceclofenac compositions micropill granule as claimed in claim 1, is characterized in that, comprises the steps:
Step 1: taking adhesive preparation obtains binder solution, adds aceclofenac, filler, prepares ball core;
Step 2: get pharmaceutically acceptable coating material preparation and obtain coating solution;
Step 3: get described ball core and mix rear coating with described coating solution, obtain;
In g/mL, the mass volume ratio of described ball core and described pharmaceutically acceptable coating material is 700～800:750～900.
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| CN102824312A (en) | 2012-12-19 |
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