CN104644574A - A sildenafil citrate taste-masking preparation - Google Patents
A sildenafil citrate taste-masking preparation Download PDFInfo
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- CN104644574A CN104644574A CN201310581117.9A CN201310581117A CN104644574A CN 104644574 A CN104644574 A CN 104644574A CN 201310581117 A CN201310581117 A CN 201310581117A CN 104644574 A CN104644574 A CN 104644574A
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Abstract
A sildenafil citrate taste-masking preparation and a preparing method thereof are disclosed. The sildenafil citrate taste-masking preparation at least comprises, based on the total weight of tablets, 15-30% of sildenafil citrate, 30-65% of hydroxypropyl cellulose and 15-20% of glyceryl behenate. The preparing method includes: mixing a formula dosage of the sildenafil citrate and a formula dosage of the hydroxypropyl cellulose to prepare melt dispersion, cutting the melt dispersion into particles, grinding the particles together with the glyceryl behenate, fully mixing with other auxiliary materials, and tabletting into tablets for oral administration.
Description
Technical field
The invention belongs to field of medicaments, be specifically related to a kind of sildenafil citrate taste masking preparation and preparation method thereof.
Background technology
Sildenafil citrate is the oral medicine for the treatment of erection disturbance (ED), is a kind of 5 type phosphodiesterase (PDE5) selective depressants special to cyclic guanosine monophosphate (cGMP).Mechanism of action: the physiological mechanism of erection relates to the release of cavernous body of penis intracellular nitric oxide (NO) in sexual stimulus process.NO activates guanylate cyclase and causes cyclic guanosine monophosphate (cGMP) level to increase, and makes smooth muscle loosening in spongy body, blood engorgement.Sldenafil is high selectivity PDE5 (PDE5) inhibitor, and PDE5 expresses at cavernous body of penis camber, and (comprises platelet, blood vessel and visceral smooth muscle, skeletal muscle) in other tissue, expresses low.Sldenafil, by Selective depression PDE5, strengthens nitric oxide (NO)-cGMP approach, raises cGMP level and causes corpus cavernosum smooth muscle to relax, making patients with erectile dysfunction produce natural erectile response to sexual stimulus.Erectile response generally with sldenafil dosage and plasma concentration increase and strengthen.In addition, sldenafil is also used for the treatment of pulmonary hypertension, regardless of sex.
Sildenafil citrate is white to off-white color crystalline powder, and taste is extremely bitter, is slightly soluble in water, methanol, is dissolved in acetonitrile, ethanol or ether hardly.Its listing dosage form is tablet.For the patient having the patient of dysphagia or difficulty, gerontal patient or water intaking inconvenient, the clinical practice of this tablet receives restriction partially or completely.In addition, Sildenafil citrate tablets has larger sheet shape and sheet weight.Known after measured, commercially available Sildenafil citrate tablets (
specification 0.1g, pfizer inc) be the tablet of rhombus biconvex, it is long and wide is respectively 14.5mm and 11.0mm, has more increased the weight of the difficulty of patient swallow, have impact on its clinical adaptability.
Therefore, in order to improve the problems referred to above, need Study and Development to facilitate the novel form of clinical practice, such as oral cavity disintegration tablet.Oral cavity disintegration tablet does not need drinking-water or only needs little water gaging and disintegratable release medicine, without the need to chewing, meets saliva and disintegrate, release in the oral cavity, and for there being the patient of dysphagia or difficulty, the patient medication of gerontal patient or water intaking inconvenience provides a great convenience.
Similar preparation sees report.Patent 201310011700.6 discloses a kind of Pharmaceutical composition containing sildenafil citrate and the pregelatinized Starch of PD-1 type, it is characterized in that this Pharmaceutical composition is in 37 DEG C of water can complete disintegrate in 15 seconds to 30 seconds, and by the screen cloth of 600 ~ 710 μm.Patent 200810166942.1 discloses a kind of oral disintegrative tablet of sildenafil citrate containing diluent.Patent 200810097300.0,200610009940.2 individually discloses sildenafil citrate sublingual tablet.
But, the preparation made according to prescription and the preparation method of published oral disintegrative tablet of sildenafil citrate or sublingual lozenge is found in research, the disagreeable taste of main sildenafil citrate can not be covered completely, although add miscellaneous sweeting agent and correctives in prescription, but the bitterness embodying principal agent all more or less in oral, have impact on the mouthfeel of said preparation to a great extent, limit clinical adaptability and toleration.This is because sildenafil citrate has extremely bitter bitterness, and specification comparatively large (containing sildenafil citrate 140.5mg/ sheet), to be diluted by the adjuvant of routine, the masking methods such as correctives, very difficult realization completely, good taste masking.
Summary of the invention
An object of the present invention is to provide a kind of sildenafil citrate taste masking preparation, at least containing the sildenafil citrate based on tablet total weight amount 15%-30%, the hydroxypropyl cellulose as odor mask based on tablet total weight amount 30%-65% (HPC), based on tablet total weight amount 15%-20% Glyceryl Behenate.
Preferably, sildenafil citrate accounts for 17.5% ~ 25.0% of prescription total amount, is more preferably 22.5%; HPC accounts for 40.0% ~ 55.0% of prescription composition, and being more preferably 48.0%, HPC, can be selected from trade name be Klucel
tMcommercially available prod, preferably from Klucel
tMeLF, Klucel
tMeF, Klucel
tMlF and Klucel
tMone or more in JF; Glyceryl Behenate accounts for 17.5% of prescription composition.
Sildenafil citrate taste masking preparation of the present invention, also comprise pharmaceutically acceptable adjunct ingredient, comprise the filler based on tablet total weight amount 3%-21%, the disintegrating agent of 0.5%-4.0%, the correctives of 0.2%-1.0%, the lubricant of 0.5%-1.5%, wherein said filler is for being selected from xylitol, one or more in sorbitol and mannitol, described disintegrating agent is for being selected from cross-linking sodium carboxymethyl cellulose, one or more in carboxymethyl starch sodium and polyvinylpolypyrrolidone, described correctives be selected from Mint Essence and Fructus Citri Limoniae essence one or both, described magnesium stearate lubricant, one or more in sodium stearyl fumarate.
In above-mentioned adjuvant composition, filler preferably 8.0%, disintegrating agent preferably 2.5%, correctives preferably 0.5%, lubricant preferably 1.0%.
Sildenafil citrate taste masking preparation of the present invention, is prepared from by following method:
(1) sildenafil citrate of recipe quantity is mixed with hydroxypropyl cellulose, make melting dispersion;
(2) melting dispersion is cut to be broken into after diameter is about the granule of 1mm and mixes with Glyceryl Behenate;
(3) milled mixtures, obtains abrasive grains
(4) will grind mix with pharmaceutically acceptable adjunct ingredient, tabletting.
Further, in step (1), the mixture of sildenafil citrate and hydroxypropyl cellulose processes in the double screw extruder of heater, throughput is 1kg/h, temperature is increased to 170 DEG C ~ 200 DEG C gradually by 20 DEG C in by process, finally extrudes at the discharging gate place of diameter 2mm; In step (3), milled mixtures obtains abrasive grains after 20 mesh sieves.
Further, above-mentioned preparation method is: the sildenafil citrate taking recipe quantity is mixed homogeneously with HPC, be placed in double screw extruder, throughput is 1kg/h, and temperature is increased to 180 DEG C gradually by 20 DEG C in by process, finally extrude at the discharging gate place of diameter 2mm, the melting dispersion tow of gained is cut and is broken into the granule that diameter is about 1mm, is mixed by granule, this mixture is placed in impact grinder and grinds with Glyceryl Behenate, by 20 mesh sieves, obtain abrasive grains; The filler of above-mentioned abrasive grains and recipe quantity, disintegrating agent, correctives, mix lubricant are even, then are pressed into and can supply oral tablet.
In the present invention, it is crucial that melting dispersion and Glyceryl Behenate grind altogether, melting dispersion and Glyceryl Behenate co-ground make Glyceryl Behenate be well-dispersed in the surface of melting dispersion granule, enhance taste masking effect, and HPC is not only the medium of melting dispersion, also play taste masking effect, the tablet made based on this has completely eliminated the bitterness and bad mouthfeel that said preparation may run into when oral.
Accompanying drawing explanation
Fig. 1 is the stripping curve contrast of sildenafil citrate melting dispersion taste masking preparation in pure water.
Detailed description of the invention
Technical scheme provided by the invention can be understood more fully with the following Examples.These embodiments intention is described pharmaceutical composition provided by the invention and dosage form, but limits never in any form.
The raw material that following examples use and equipment, except special instruction, are common commercially available.
Twin screw melt extruder model and manufacturer: ME-D16, the special Science and Technology Ltd. in Xinyi, Shenzhen
[embodiment 1] sildenafil citrate melting dispersion-abrasive material taste masking preparation and preparation method thereof altogether
Prescription:
* sldenafil free alkali 100mg is equivalent to, identical with " preparation specification: 0.1g " implication.Lower same.
Preparation method:
The sildenafil citrate taking recipe quantity is mixed homogeneously with HPC, be placed in double screw extruder, throughput is 1kg/h, temperature is increased to 180 DEG C gradually by 20 DEG C in by process, finally extrude at the discharging gate place of diameter 2mm, the melting dispersion tow of gained is cut and is broken into the granule that diameter is about 1mm.Above-mentioned granule mixes with Glyceryl Behenate, this mixture is placed in impact grinder and grinds, then by 20 mesh sieves, obtains abrasive grains; The xylitol of above-mentioned abrasive grains and recipe quantity, cross-linking sodium carboxymethyl cellulose, Fructus Citri Limoniae essence are placed in V-arrangement mixer mixing 10min, then add magnesium stearate mixing 3min, and intermediate, through after the assay was approved, is pressed into the circular tablet of diameter 12mm.Carry out composite packaging with aluminium foil and polrvinyl chloride/polyvinylidene chloride composite hard sheet (PVC/PVDC), get product through mounted box after the assay was approved.
[embodiment 2] sildenafil citrate melting dispersion-abrasive material taste masking preparation and preparation method thereof altogether
Prescription:
| Composition | Classification | Content (mg/ sheet) | Percentage composition (%) |
| Sildenafil citrate | Principal agent | 35.1 | 15.0 |
| HPC(Klucel TMELF) | Diluent/odor mask | 140.6 | 60.0 |
| Glyceryl Behenate | Odor mask | 35.1 | 15.0 |
| Mannitol | Filler/odor mask | 18.0 | 7.7 |
| Carboxymethyl starch sodium | Disintegrating agent | 2.4 | 1.0 |
| Mint Essence | Correctives | 0.7 | 0.3 |
| Magnesium stearate | Lubricant | 2.4 | 1.0 |
| Add up to | 234.3mg | 100.0 |
Preparation method:
The sildenafil citrate taking recipe quantity is mixed homogeneously with HPC, be placed in double screw extruder, throughput is 1kg/h, temperature is increased to 170 DEG C gradually by 20 DEG C in by process, finally extrude at the discharging gate place of diameter 2mm, the melting dispersion tow of gained is cut and is broken into the granule that diameter is about 1mm.Above-mentioned granule mixes with Glyceryl Behenate, this mixture is placed in impact grinder and grinds, then by 20 mesh sieves, obtains abrasive grains; The mannitol of above-mentioned abrasive grains and recipe quantity, carboxymethyl starch sodium, Mint Essence are placed in V-arrangement mixer mixing 10min, then add magnesium stearate mixing 3min, and intermediate, through after the assay was approved, is pressed into the circular tablet of diameter 9mm.Carry out composite packaging with aluminium foil and polrvinyl chloride/polyvinylidene chloride composite hard sheet (PVC/PVDC), get product through mounted box after the assay was approved.
[embodiment 3] sildenafil citrate melting dispersion-abrasive material taste masking preparation and preparation method thereof altogether
Prescription:
| Composition | Classification | Content (mg/ sheet) | Percentage composition (%) |
| Sildenafil citrate | Principal agent | 140.5 | 30.0 |
| HPC(Klucel TMJF) | Diluent/odor mask | 140.5 | 30.0 |
| Glyceryl Behenate | Odor mask | 93.7 | 20.0 |
| Mannitol | Filler/odor mask | 35.1 | 7.5 |
| Sorbitol | Filler/odor mask | 28.1 | 6.0 |
| Polyvinylpolypyrrolidone | Disintegrating agent | 18.7 | 4.0 |
| Fructus Citri Limoniae essence | Correctives | 4.7 | 1.0 |
| Sodium stearyl fumarate | Lubricant | 7.0 | 1.5 |
| Add up to | 468.3mg | 100.0 |
Preparation method:
The sildenafil citrate taking recipe quantity is mixed homogeneously with HPC, be placed in double screw extruder, throughput is 1kg/h, temperature is increased to 200 DEG C gradually by 20 DEG C in by process, finally extrude at the discharging gate place of diameter 2mm, the melting dispersion tow of gained is cut and is broken into the granule that diameter is about 1mm.Above-mentioned granule mixes with Glyceryl Behenate, this mixture is placed in impact grinder and grinds, then by 20 mesh sieves, obtains abrasive grains; The mannitol of above-mentioned abrasive grains and recipe quantity, sorbitol, polyvinylpolypyrrolidone, Fructus Citri Limoniae essence are placed in V-arrangement mixer mixing 10min, then add sodium stearyl fumarate mixing 3min, and intermediate, through after the assay was approved, is pressed into the circular tablet of diameter 11mm.Carry out composite packaging with aluminium foil and polrvinyl chloride/polyvinylidene chloride composite hard sheet (PVC/PVDC), get product through mounted box after the assay was approved.
[embodiment 4] sildenafil citrate melting dispersion-abrasive material taste masking preparation and preparation method thereof altogether
Prescription:
| Composition | Classification | Content (mg/ sheet) | Percentage composition (%) |
| Sildenafil citrate | Principal agent | 70.3 | 17.5 |
| HPC(Klucel TMLF) | Diluent/odor mask | 168.6 | 42.0 |
| Glyceryl Behenate | Odor mask | 60.2 | 15.0 |
| Mannitol | Filler/odor mask | 76.3 | 19.0 |
| Cross-linking sodium carboxymethyl cellulose | Disintegrating agent | 8.0 | 2.0 |
| Carboxymethyl starch sodium | Disintegrating agent | 8.0 | 2.0 |
| Mint Essence | Correctives | 4.0 | 1.0 |
| Magnesium stearate | Lubricant | 6.0 | 1.5 |
| Add up to | 401.4mg | 100.0 |
Preparation method:
The sildenafil citrate taking recipe quantity is mixed homogeneously with HPC, be placed in double screw extruder, throughput is 1kg/h, temperature is increased to 190 DEG C gradually by 20 DEG C in by process, finally extrude at the discharging gate place of diameter 2mm, the melting dispersion tow of gained is cut and is broken into the granule that diameter is about 1mm.Above-mentioned granule mixes with Glyceryl Behenate, this mixture is placed in impact grinder and grinds, then by 20 mesh sieves, obtains abrasive grains; The mannitol of above-mentioned abrasive grains and recipe quantity, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, Mint Essence are placed in V-arrangement mixer mixing 10min, add magnesium stearate mixing 3min again, intermediate, through after the assay was approved, is pressed into the circular tablet of diameter 11mm.Carry out composite packaging with aluminium foil and polrvinyl chloride/polyvinylidene chloride composite hard sheet (PVC/PVDC), get product through mounted box after the assay was approved.
The mouthfeel comparative evaluation of sildenafil citrate melting dispersion-common abrasive material taste masking preparation that [embodiment 5] is optimized
By test preparation: the taste masking preparation described in embodiment 1
Comparative formulation 1: commercially available Sildenafil citrate tablets (
specification 0.1g, pfizer inc)
Comparative formulation 2: adopt the sildenafil citrate taste masking preparation that Chinese Patent Application No. is prepared for technology described in NO.201310011700.6, concrete formulation and technology is as follows:
Prescription:
| Composition | Classification | Content (mg/ sheet) | Percentage composition (%) |
| Sildenafil citrate | Principal agent | 140.5 | 22.5 |
| Partially pregelatinized starch | Filler | 50.0 | 8.0 |
| PVP k30 | Binding agent | 10.0 | 1.6 |
| Lactose | Filler | 260.0 | 41.6 |
| Mannitol | Filler/odor mask | 123.8 | 19.8 |
| Polyvinylpolypyrrolidone | Disintegrating agent | 31.3 | 5.0 |
| Fructus Citri Limoniae essence | Correctives | 3.1 | 0.5 |
| Magnesium stearate | Lubricant | 6.3 | 1.0 |
| Add up to | 625.0mg | — |
Preparation method:
By sildenafil citrate and partially pregelatinized starch mix homogeneously; be placed in fluidised bed granulator; to blow in machine, heating; material is made to be in fluidized state; the PVP k30 aqueous solution spraying into 5% is granulated; appropriate water fill spray if desired to form applicable granule, keeps hot blast temperature 45 ± 5 DEG C, make particle drying to moisture less than 2.5%.By above-mentioned granule by 20 eye mesh screen granulate.Mixed homogeneously with lactose, mannitol, polyvinylpolypyrrolidone, Fructus Citri Limoniae essence and magnesium stearate by above-mentioned granule, tabletting, to obtain final product.
Comparative formulation 3: adopt the sildenafil citrate taste masking preparation that Chinese Patent Application No. is prepared for technology described in NO.200810097300.0, concrete formulation and technology is as follows:
Prescription:
| Composition | Classification | Content (mg/ sheet) | Percentage composition (%) |
| Sildenafil citrate | Principal agent | 140.5 | 22.5 |
| Mannitol | Filler/odor mask | 120.0 | 19.2 |
| HPMC | Binding agent | 12.5 | 2.0 |
| Microcrystalline Cellulose | Filler | 127.0 | 20.3 |
| Lactose | Filler | 200.0 | 32.0 |
| Cross-linking sodium carboxymethyl cellulose | Disintegrating agent | 15.6 | 2.5 |
| Fructus Citri Limoniae essence | Correctives | 3.1 | 0.5 |
| Magnesium stearate | Lubricant | 6.3 | 1.0 |
| Add up to | 625.0mg | — |
Preparation method:
By sildenafil citrate and mannitol mix homogeneously, be placed in impact grinder and fully grind, cross 80 mesh sieves, for subsequent use; By water-soluble for HPMC be made into 5% solution; Above-mentioned sildenafil citrate and mannitol mixture are placed in wet mixing pelletizer, open and stir and shear, add the HPMC aqueous solution of recipe quantity, then add appropriate water and supply amount of liquid, make the state that material reaches applicable, and obtained wet granular.Wet granular is placed in fluidized bed dryer dry, baking temperature is 45 ± 5 DEG C, is dried to moisture less than 2.5%.By above-mentioned granule by 16 eye mesh screen granulate.The microcrystalline Cellulose of above-mentioned granule and recipe quantity, lactose, cross-linking sodium carboxymethyl cellulose, Fructus Citri Limoniae essence and magnesium stearate are mixed homogeneously, tabletting, to obtain final product.
Comparative formulation 4:
A kind of sildenafil citrate melting dispersion taste masking preparation (without grinding altogether)
The present embodiment as a comparison preparation shows the pivotal role of Glyceryl Behenate co-rotational procedure of the present invention in taste masking preparation.
Prescription:
| Composition | Effect | Content (mg/ sheet) | Percentage composition (%) |
| Sildenafil citrate | Principal agent | 140.5 | 22.5 |
| HPC(Klucel TMEF) | Diluent/odor mask | 375.0 | 60.0 |
| Xylitol | Filler/odor mask | 84.5 | 13.5 |
| Cross-linking sodium carboxymethyl cellulose | Disintegrating agent | 15.6 | 2.5 |
| Fructus Citri Limoniae essence | Correctives | 3.1 | 0.5 |
| Magnesium stearate | Lubricant | 6.3 | 1.0 |
| Add up to | 625.0mg | — |
Preparation method:
The sildenafil citrate taking recipe quantity is mixed homogeneously with HPC, be placed in double screw extruder, throughput is 1kg/h, temperature is increased to 180 DEG C gradually by 20 DEG C in by process, finally extrude at the discharging gate place of diameter 2mm, the melting dispersion tow of gained is cut and is broken into the granule that diameter is about 1mm, is then placed in impact grinder and grinds, again by 20 mesh sieves, obtain melting dispersion fine grained; The xylitol of above-mentioned melting dispersion fine grained and recipe quantity, cross-linking sodium carboxymethyl cellulose, Fructus Citri Limoniae essence are placed in V-arrangement mixer mixing 10min, then add magnesium stearate mixing 3min, and intermediate, through after the assay was approved, is pressed into the circular tablet of diameter 12mm.
Above-mentioned test preparation and the 4 kinds of Comparative formulation of being subject to evaluate its mouthfeel respectively.15 health volunteers taste by test preparation and 3 kinds of Comparative formulation at random respectively, and according to mouth feel score, standards of grading are: 1=taste is extremely bitter, and 2=is more bitter, the micro-hardship of 3=, and the atomic hardship of 4=, 5=is without bitterness.Score is higher, and its mouthfeel is better.Evaluation result is as following table.
Result is visible, and the sildenafil citrate melting dispersion-common abrasive material taste masking preparation mouthfeel of the optimization that embodiment 1 provides is better, almost without bitterness, is obviously better than 4 kinds of Comparative formulation.In particular, taste masking preparation of the present invention, compared with Comparative formulation 4, shows the necessity of Glyceryl Behenate co-rotational procedure.
[embodiment 6] is by the taste masking effect of the stripping curve contrast display invention formulation of medicine.
By test preparation: the taste masking preparation of embodiment 1,2,3,4
Comparative formulation: commercially available Sildenafil citrate tablets (
specification 0.1g, pfizer inc), Comparative formulation 4 in " embodiment 5 ".
Assay method: adopt " Chinese Pharmacopoeia " version in 2010 two annex X C dissolution methods first method (basket method), dissolution medium is pure water 900ml; Rotating speed: 100 revs/min; Assay method: ultraviolet spectrophotometry, determined wavelength 290nm.
Stripping curve measurement result is as shown in following table and accompanying drawing 1.
Stripping curve contrast (dissolution, %) of table sildenafil citrate taste masking preparation in pure water
Visible, the phase before releasing, the taste masking preparation release of embodiment 1,2,3,4 is significantly lower than Comparative formulation
and lower than the Comparative formulation 4 without Glyceryl Behenate co-rotational procedure, show tested taste masking preparation firm disintegrate with and subsequent a period of time in, medicine can not release very soon and cause produce bitterness.And after 30 minutes, tested taste masking preparation dissolution all reaches more than 80%, meet preparation Dissolution Standards.
Claims (11)
1. a sildenafil citrate preparation, is characterized in that, at least containing sildenafil citrate, the hydroxypropyl cellulose of 30%-65%, the 15%-20% Glyceryl Behenate based on tablet total weight amount 15%-30%.
2. sildenafil citrate preparation as claimed in claim 1, is characterized in that, at least containing sildenafil citrate, the hydroxypropyl cellulose of 42%-55%, 17.5% Glyceryl Behenate based on tablet total weight amount 17.5%-25%.
3. sildenafil citrate preparation as claimed in claim 2, is characterized in that, at least contains based on the sildenafil citrate of tablet total weight amount 22.5%, the hydroxypropyl cellulose of 48%.
4. sildenafil citrate preparation as claimed in claim 1, it is characterized in that described preparation also comprises pharmaceutically acceptable adjunct ingredient, comprise filler, the disintegrating agent of 0.5%-4.0%, the correctives of 0.2%-1.0%, the lubricant of 0.5%-1.5% based on tablet total weight amount 3%-21%.
5. sildenafil citrate taste masking preparation as claimed in claim 2, it is characterized in that described preparation also comprises pharmaceutically acceptable adjunct ingredient, comprise the filler based on tablet total weight amount 5%-12%, 2.5% disintegrating agent, the correctives of 0.5%, the lubricant of 1%.
6. the sildenafil citrate preparation as described in claim 4 or 5, it is characterized in that, described filler be selected from xylitol, sorbitol and mannitol one or more, described disintegrating agent be selected from cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium and polyvinylpolypyrrolidone one or more, described correctives be selected from Mint Essence and Fructus Citri Limoniae essence one or both, one or more of described magnesium stearate lubricant, sodium stearyl fumarate.
7. sildenafil citrate taste masking preparation as claimed in claim 1, is characterized in that being prepared from by following method:
(1) sildenafil citrate of recipe quantity is mixed with hydroxypropyl cellulose, make melting dispersion;
(2) melting dispersion mixes with Glyceryl Behenate after being cut the granule being broken into diameter 1mm;
(3) milled mixtures, obtains abrasive grains
(4) will grind mix with pharmaceutically acceptable adjunct ingredient, tabletting.
8. sildenafil citrate taste masking preparation as claimed in claim 7, it is characterized in that: in described step (1), the mixture of sildenafil citrate and hydroxypropyl cellulose processes in the double screw extruder of heater, throughput is 1kg/h, temperature is increased to 170 DEG C ~ 200 DEG C gradually by 20 DEG C in by process, finally extrudes at the discharging gate place of diameter 2mm; In step (3), milled mixtures obtains abrasive grains after 20 mesh sieves.
9. prepare a method for sildenafil citrate preparation, it is characterized in that comprising the following steps:
(1) sildenafil citrate of recipe quantity is mixed with hydroxypropyl cellulose, make melting dispersion;
(2) melting dispersion mixes with Glyceryl Behenate after being cut and being broken into granule;
(3) milled mixtures, obtains abrasive grains
(4) will grind mix with pharmaceutically acceptable adjunct ingredient, tabletting.
10. method as claimed in claim 9, is characterized in that: be mixed with the hydroxypropyl cellulose based on tablet total weight amount 30%-65% by the sildenafil citrate based on tablet total weight amount 15%-30% in step (1), make melting dispersion; Step (2) mixes with the Glyceryl Behenate of 15.0% ~ 20.0% after melting dispersion cutting and crushing is become the granule of diameter 1mm.
11. sildenafil citrate taste masking preparations as claimed in claim 4, is characterized in that, comprise the component of following restructuring proportioning:
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106310218A (en) * | 2015-11-27 | 2017-01-11 | 深圳奥萨制药有限公司 | Tablet composition containing enalapril and folic acid and preparation method thereof |
| CN107148267A (en) * | 2014-10-31 | 2017-09-08 | 埃迪制药公司 | Active material particle with dual taste masking technology, its production method and dispersible of the oral cavity comprising it |
| CN111388433A (en) * | 2020-03-27 | 2020-07-10 | 广州白云山医药集团股份有限公司白云山制药总厂 | Sildenafil citrate oral preparation and preparation method thereof |
| CN112206213A (en) * | 2020-10-26 | 2021-01-12 | 广州汇元医药科技有限公司 | Sildenafil citrate composition and preparation method thereof |
| CN113712926A (en) * | 2021-08-31 | 2021-11-30 | 南京恒正药物研究院有限公司 | Sildenafil orally disintegrating tablet |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1688292A (en) * | 2002-09-04 | 2005-10-26 | 兰贝克赛实验室有限公司 | Taste masked dosage forms and processes for their preparation |
| WO2011030351A2 (en) * | 2009-09-03 | 2011-03-17 | Rubicon Research Private Limited | Taste - masked pharmaceutical compositions |
-
2013
- 2013-11-18 CN CN201310581117.9A patent/CN104644574B/en active Active
Non-Patent Citations (1)
| Title |
|---|
| 陶涛: "矫味和掩味技术在口服新剂型中的应用", 《上海医药》 * |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107148267A (en) * | 2014-10-31 | 2017-09-08 | 埃迪制药公司 | Active material particle with dual taste masking technology, its production method and dispersible of the oral cavity comprising it |
| CN106310218A (en) * | 2015-11-27 | 2017-01-11 | 深圳奥萨制药有限公司 | Tablet composition containing enalapril and folic acid and preparation method thereof |
| CN106310218B (en) * | 2015-11-27 | 2019-12-13 | 深圳奥萨制药有限公司 | tablet composition containing enalapril and folic acid and preparation method thereof |
| CN111388433A (en) * | 2020-03-27 | 2020-07-10 | 广州白云山医药集团股份有限公司白云山制药总厂 | Sildenafil citrate oral preparation and preparation method thereof |
| CN111388433B (en) * | 2020-03-27 | 2021-11-23 | 广州白云山医药集团股份有限公司白云山制药总厂 | Sildenafil citrate oral preparation and preparation method thereof |
| CN112206213A (en) * | 2020-10-26 | 2021-01-12 | 广州汇元医药科技有限公司 | Sildenafil citrate composition and preparation method thereof |
| CN113712926A (en) * | 2021-08-31 | 2021-11-30 | 南京恒正药物研究院有限公司 | Sildenafil orally disintegrating tablet |
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Effective date of registration: 20170626 Address after: 518057 Guangdong city of Shenzhen province Nanshan District high-tech road two North Long Hill Haiwang industrial city Applicant after: Shenzhen Neptune medical science and Technology Research Institute Co., Ltd. Address before: 518057 Guangdong city of Shenzhen province Nanshan District high-tech road two North Long Hill Haiwang industrial city Applicant before: Haiwang Pharmaceutical Industry Co., Ltd., Shenzhen |
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