CN1634014A - Sodium ferulate oral disintegrating tablet and its preparation process - Google Patents
Sodium ferulate oral disintegrating tablet and its preparation process Download PDFInfo
- Publication number
- CN1634014A CN1634014A CN 200410096460 CN200410096460A CN1634014A CN 1634014 A CN1634014 A CN 1634014A CN 200410096460 CN200410096460 CN 200410096460 CN 200410096460 A CN200410096460 A CN 200410096460A CN 1634014 A CN1634014 A CN 1634014A
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- Prior art keywords
- sodium
- sodium ferulate
- tablet
- essence
- ferulate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- NCTHNHPAQAVBEB-WGCWOXMQSA-M sodium ferulate Chemical compound [Na+].COC1=CC(\C=C\C([O-])=O)=CC=C1O NCTHNHPAQAVBEB-WGCWOXMQSA-M 0.000 title claims abstract description 40
- 238000002360 preparation method Methods 0.000 title claims abstract description 24
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- 239000002994 raw material Substances 0.000 claims abstract description 6
- 239000011248 coating agent Substances 0.000 claims description 39
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- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 28
- 239000000203 mixture Substances 0.000 claims description 23
- 239000000843 powder Substances 0.000 claims description 13
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 12
- 229920003134 Eudragit® polymer Polymers 0.000 claims description 12
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 12
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- 239000003814 drug Substances 0.000 abstract description 7
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- 238000001035 drying Methods 0.000 description 6
- 241000208340 Araliaceae Species 0.000 description 5
- 238000001514 detection method Methods 0.000 description 5
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- 239000007788 liquid Substances 0.000 description 5
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- KSEBMYQBYZTDHS-HWKANZROSA-M (E)-Ferulic acid Natural products COC1=CC(\C=C\C([O-])=O)=CC=C1O KSEBMYQBYZTDHS-HWKANZROSA-M 0.000 description 4
- 239000004148 curcumin Substances 0.000 description 4
- 235000001785 ferulic acid Nutrition 0.000 description 4
- KSEBMYQBYZTDHS-HWKANZROSA-N ferulic acid Chemical compound COC1=CC(\C=C\C(O)=O)=CC=C1O KSEBMYQBYZTDHS-HWKANZROSA-N 0.000 description 4
- KSEBMYQBYZTDHS-UHFFFAOYSA-N ferulic acid Natural products COC1=CC(C=CC(O)=O)=CC=C1O KSEBMYQBYZTDHS-UHFFFAOYSA-N 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
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- 239000007931 coated granule Substances 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
- 206010013786 Dry skin Diseases 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
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- 229940079593 drug Drugs 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
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- 238000010298 pulverizing process Methods 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
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- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 208000019505 Deglutition disease Diseases 0.000 description 1
- 102000002045 Endothelin Human genes 0.000 description 1
- 108050009340 Endothelin Proteins 0.000 description 1
- 229940118365 Endothelin receptor antagonist Drugs 0.000 description 1
- 241000167880 Hirundinidae Species 0.000 description 1
- 208000001407 Vascular Headaches Diseases 0.000 description 1
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- 230000036592 analgesia Effects 0.000 description 1
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- 230000010100 anticoagulation Effects 0.000 description 1
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- 239000008280 blood Substances 0.000 description 1
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- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 description 1
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- XDROKJSWHURZGO-UHFFFAOYSA-N isopsoralen Natural products C1=C2OC=CC2=C2OC(=O)C=CC2=C1 XDROKJSWHURZGO-UHFFFAOYSA-N 0.000 description 1
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- KZJWDPNRJALLNS-VJSFXXLFSA-N sitosterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CC[C@@H](CC)C(C)C)[C@@]1(C)CC2 KZJWDPNRJALLNS-VJSFXXLFSA-N 0.000 description 1
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Abstract
The invention discloses a sodium ferulate orally disintegrating tablet and its preparation, wherein the tablet is prepared by using sodium ferulate as raw material, using bulking agent, crumbling agent, flavoring agent, flow aid, and lubricating agent as adjuvant, using bonding agent or dressing material based on specific situation, or charging right amount of effervescent agent, then using specific preparing procedure and employing a tablet compressing machine for pelleting. The invention realizes quick disintegrating speed, good taste, the tablet can be taken under the condition of waterless, it has the advantages of fast effect, improved compliance for the patients, and increased curative effect of the medicament.
Description
Technical field
The present invention relates to a kind of have antioxidation and free radical scavenging effect; can protect cell membrane not oxidated and anticoagulant and thrombosis; the clinical atherosclerosis that is used for; treatment blood vessel embolism vasculitis, the Orally disintegrated sodium ferulate tablet preparation of diseases such as acute cerebral thrombosis and migraine.
Background technology
Sodium ferulate is the sodium salt of the main component ferulic acid of traditional blood-activating and stasis-removing Radix Angelicae Sinensis, Rhizoma Chuanxiong, and chemical name is: 3-methoxyl group-4-Hydroxycinnamic Acid sodium salt dihydrate claims angelicin etc. again.
Sodium ferulate is non-peptide-like endothelin receptor antagonist, has multiple pharmacological effect: but the vasoconstriction that the antagonism Endothelin causes, boost and vascular smooth muscle cell proliferation; Increase the synthetic of NO, lax vascular smooth muscle; Anticoagulant and thrombosis, anticoagulation, improve the hemorheology feature; Also can suppress the synthetic of cholesterol, blood fat reducing; Have antioxidation and free radical scavenging effect simultaneously, can protect cell membrane not oxidated, the control lipid peroxidation injury; Energy enhance immunity function, and have certain analgesia, spasmolysis.
The clinical coronary heart disease (atherosclerosis) that is mainly used in of sodium ferulate, treatment blood vessel embolism vasculitis, thrombocytopenia, acute cerebral thrombosis, vascular headache and migrainous treatment.
The dosage form of existing sodium ferulate preparation has: drop pill, capsule, injection and ordinary tablet.
Because dosage form needs a large amount of water to send down when most of oral formulations are taken, this makes the patient of many old peoples, infant or dysphagia, water intaking inconvenience be difficult to take.Injection often is easy to generate anaphylaxis or untoward reaction etc. again, and it is big that the while injection also exists operation easier, and the patient suffering is also big, makes and medical treatment cost high the shortcoming that patient economy burden is heavy.Therefore, be necessary to prepare and take convenient dosage form to satisfy the multiple needs that clinical treatment and family use.
Summary of the invention
The objective of the invention is to improve the deficiency of existing sodium ferulate aspect peroral dosage form, provide a kind of taking convenience, absorption is rapid-action, bioavailability is high Orally disintegrated sodium ferulate tablet preparation to extensive patients and medical personnel.Needn't drink water when the present invention relates to take, in the oral cavity, only need get final product rapid disintegrate or dissolving in tens seconds, swallow with the liquid of sleeping and to finish Orally disintegrated sodium ferulate tablet of taking medicine and preparation method thereof.
One, prescription
The Orally disintegrated sodium ferulate tablet that reaches of the present invention comprises the material medicine sodium ferulate, needs following former, the auxiliary material of 9 classes altogether, and wherein: when not making Cotton seeds, then do not use coating material, effervescent also can for selecting adjuvant for use as one sees fit.
Sodium ferulate (5-50) %, binding agent (0-5) %, filler (10-80) %, disintegrating agent (2-35) %, correctives (1-40) %, coating material (0-40) %, effervescent (0-30) %, fluidizer (0.01-5) %, lubricant (0.3-3) %.Wherein:
Binding agent includes but are not limited to starch, pregelatinized Starch, dextrin, maltodextrin, sucrose, arabic gum, gelatin, methylcellulose, carboxymethyl cellulose, ethyl cellulose, polyvinyl alcohol, Polyethylene Glycol, polyvinylpyrrolidone (PVP), alginic acid and alginate, xanthan gum, hydroxypropyl cellulose and hydroxypropyl emthylcellulose (HPMC), can use use also capable of being combined separately.
Filler include but are not limited to mannitol (granular or powdery), xylitol, sorbitol, maltose, Chi ?alcohol, microcrystalline Cellulose, PROSOLV
SMCC, polymerization sugar (EMDEX
), coupling sugar, glucose, lactose, sucrose, dextrin and starch etc., can use separately, also can applied in any combination, consumption is generally (10-80) %.
Disintegrating agent includes but are not limited to crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), low substituted hydroxy-propyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa) and soybean polysaccharide (EMCOSOY
) etc., can use use also capable of being combined separately.
Correctives includes but are not limited to mannitol, xylitol, stevioside, lactose, fructose, sucrose, protein sugar, maltose alcohol, glycyrrhizin, Sodium Cyclamate, gelatin, aspartame, flavoring banana essence, flavoring pineapple essence, vanillin, fragrant citrus essence, flavoring orange essence, Herba Menthae essence, ginseng essence, strawberry essence, citric acid, citric acid etc., can use use also capable of being combined separately.
Coating material includes but are not limited to gelatin, arabic gum, alginate, chitosan, carboxymethyl cellulose salt, cellulose acetate phthalate ester, ethyl cellulose, methylcellulose, hypromellose, crylic acid resin (homemade acrylic resin I, II, III, IV, Eudragit
Series), polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol etc., can use use also capable of being combined separately.
Fluidizer includes but are not limited to micropowder silica gel, Pulvis Talci, Cab-O-sil, Arosil, hydrated sodium aluminosilicate etc., can use use also capable of being combined separately.
Lubricant includes but are not limited to magnesium stearate, calcium stearate, zinc stearate, glyceryl monostearate, Polyethylene Glycol, hydrogenated vegetable oil, sodium stearyl fumarate, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium laurylsulfate, magnesium laurylsulfate, Stepanol MG and Pulvis Talci etc., can use use also capable of being combined separately.
Effervescent includes but are not limited to the mixture of malic acid, citric acid or citric acid and sodium bicarbonate or sodium carbonate.
Two, preparation method
The Orally disintegrated sodium ferulate tablet that reaches of the present invention, its preparation method is a direct compression process, the manufacturer with preparation conventional tablet all can adopt.
The sodium ferulate bitter in the mouth, the present invention can adopt two kinds of distinct methods to carry out flavoring or taste masking: 1. adopt the direct flavoring of correctives; 2. in advance sodium ferulate is carried out powder coating with taste masking.
Concrete preparation method is as follows:
The preprocess method of first step sodium ferulate:
1. directly flavoring method-this law is granulated to the sodium ferulate raw material or is not dealt with, and directly enters for second step;
2. powder coating taste masking---get selected coating material, with the dissolving of the solvent that adapts with it and to be diluted to debita spissitudo standby, getting sodium ferulate again places ebullated bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get sodium ferulate powder coating granule, dry back sieving for standby;
Second step took by weighing correctives and sodium ferulate or the feed particles after first step taste masking processing according to quantity, and mix homogeneously is standby;
3. piller medicine-feeding coating taste masking---get celphere and put in coating pan or centrifugal coating granulator or the fluid bed, spray into binding agent, progressively add the mixture of drug powder or drug powder and adjuvant, make the pastille micropill; Or medicine made suspension, Emulsion or be dissolved into solution, the pastille micropill is made on the surface of above-mentioned suspension, Emulsion or the solution spray core of falling the ball, coating material on the external packets of micropill, drying, standby;
4. stir the system micropill coating taste masking of granulating---ferulic acid is mixed with suitable adjuvant, described adjuvant comprises sucrose, lactose, mannitol, dextrin, beta-schardinger dextrin-, starch, microcrystalline Cellulose, Polyethylene Glycol, magnesium stearate, can use separately also and can unite use, mixed material is put in the High Speed Stirring Machine and is stirred, add binding agent simultaneously and make granule, in the dry rearmounted coating pan of granule or centrifugal coating granulator or the fluid bed with selected coating material coating, drying, standby;
The 3rd step took by weighing filler, disintegrating agent, effervescent, fluidizer and mix homogeneously according to quantity, made evenly again with through second mixing of materials that goes on foot gained, and adding lubricant mixing is standby;
The 4th step gained material detects through intermediate, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Beneficial effect
Tablet is a kind of conventional dosage forms, because of its steady quality, dosage accurately, take, easy to carry, mechanization degree is high, low one of the at present the most frequently used dosage form that becomes of production cost, but because of the tablet extrusion forming, disintegrate is slow, bioavailability is lower, and part patient swallows comparatively difficult, thereby promoting the use of to a certain extent of tablet is restricted.The oral administration solid quick releasing formulation becomes a focus, particularly oral cavity disintegration tablet of new drug development in recent years for this reason, because of its taking convenience, rapid-action, bioavailability is high, the good emphasis that becomes tablet exploitation of mouthfeel.
Oral cavity disintegration tablet is meant not to be needed water or only needs low amounts of water, need not to chew, and tablet places lingual surface, disintegrate rapidly after the chance saliva, or borrow and swallow power, medicine can be gone into the tablet of stomach onset.The characteristics of oral cavity disintegration tablet are that absorption is fast, bioavailability is high, and intestinal is residual few, and side effect is low, avoids liver first-pass effect etc.
Specific embodiment
For the preparation method of Orally disintegrated sodium ferulate tablet of the present invention better is described, in conjunction with directly flavoring method and powder coating taste masking method are as follows for an embodiment respectively:
Embodiment one direct flavoring method
One. prescription
1. raw material---sodium ferulate 50.0g;
2. binding agent---polyvinylpyrrolidone K-30 0.5g;
3. filler---mannitol 78.5g;
PROSOLV
SMCC 5.0g；
4. correctives---aspartame 1.0g;
Ginseng essence 1.0g;
5. disintegrating agent---crospolyvinylpyrrolidone 8.0g;
L-HPC 4.0g；
6. fluidizer---micropowder silica gel 1.0g;
7. lubricant---magnesium stearate 1.0g.
Make 1000 altogether, specification: the 50mg/ sheet.
Two. preparation method
1) get the sodium ferulate raw material pulverizing, granulate, cross 26 mesh sieves with polyvinylpyrrolidone K-30, standby;
2) with micropowder silica gel, ginseng essence, PROSOLV
SMCC and aspartame are crossed 40 mesh sieves respectively, and mix homogeneously adds the sodium ferulate granule of having granulated again, and mix homogeneously is standby;
3) get mannitol, L-HPC and crospolyvinylpyrrolidone and cross 40 mesh sieves respectively, mix homogeneously will add and mix homogeneously through the raw material of flavoring again, adds sodium stearyl fumarate and mix homogeneously at last;
4) intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment two powder coating taste masking methods
One. prescription
1. raw material---sodium ferulate 50.0g;
2. coating material---Eudragit
E100 7.0g;
Eudragit
NE30D (doing) 3.0g;
3. filler---mannitol 90.0g;
Microcrystalline Cellulose 10.0g;
4. correctives---aspartame 1.0g;
Ginseng essence 1.0g;
5. disintegrating agent---crospolyvinylpyrrolidone 10.0g;
L—HPC 5.0g；
6. fluidizer---micropowder silica gel 1.0g;
7. lubricant---sodium stearyl fumarate 1.0g.
Make 1000 altogether, specification: the 50mg/ sheet.
Two. preparation method
1) gets Eudragit
E100 and Eudragit
NE30D Eudragit
NE30D is with 95% dissolve with ethanol and to be diluted to finite concentration standby;
2) get sodium ferulate and place ebullated bed to seethe with excitement, spray into above-mentioned solution by certain speed and carry out powder coating, make sodium ferulate powder coating granule, dry back is standby;
3) with mannitol, microcrystalline Cellulose, micropowder silica gel, PVPP, L-HPC, aspartame, sodium stearyl fumarate and ginseng essence mix homogeneously, again and sieve after the coated granule mixing standby;
4) intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment three effervescent flavoring methods
One. prescription
1. raw material---sodium ferulate 50.0g;
2. binding agent---polyvinylpyrrolidone K-30 0.5g;
3. effervescent---citric acid 15.5g;
Sodium bicarbonate 12.0g;
4. filler---mannitol 48.0g;
PROSOLV
SMCC 5.0g；
5. correctives---aspartame 1.0g;
Fragrant citrus essence 1.0g;
6. disintegrating agent---crospolyvinylpyrrolidone 10.0g;
L-HPC 5.0g；
7. fluidizer---micropowder silica gel 1.0g;
8. lubricant---sodium stearyl fumarate 1.0g.
Make 1000 altogether, specification: the 50mg/ sheet.
Two. preparation method
1) get sodium ferulate and citric acid raw material and mix the back pulverizing, granulate, cross 26 mesh sieves with polyvinylpyrrolidone K-30, standby;
2) get sodium bicarbonate and pulverize, granulate, cross 26 mesh sieves with polyvinylpyrrolidone K-30, standby;
3) adjuvant that all the other are all is crossed mix homogeneously behind 40 mesh sieves respectively, adds the granule of having granulated again, and mix homogeneously is standby;
4) intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment four pillers medicine-feeding coating taste masking method
One. prescription
1. raw material---sodium ferulate 50.0g;
2. adjuvant---starch 15.0g
3. celphere (grain warp: 200 microns) 10.0g;
4. binding agent-PVP
K30Ethanol liquid contains PVP
K305.0g;
5. coating material---Eudragit
E100 10.0g;
Eudragit
NE30D (doing) 4.0g;
6. filler---mannitol 70.0g;
Microcrystalline Cellulose 10.0g;
7. correctives---aspartame 1.0g;
Fragrant citrus essence 1.0g;
8. disintegrating agent---crospolyvinylpyrrolidone 10.0g;
L-HPC 5.0g；
9. fluidizer---micropowder silica gel 1.0g;
10. lubricant---sodium stearyl fumarate 1.0g.
Make 1000 altogether, specification: the 50mg/ sheet.
Two. preparation method
1 with ferulic acid, starch mixing for standby use;
2 celphere are put in the centrifugal granulator machine, spray into binding agent, add the ferulic acid mixed material that mixes, the preparation micropill;
Use coating material liquid coating after the 3 micropill dryings, drying.
The 4 adjuvant mix homogeneously that all the other are all add the coated granule that has made again, and mix homogeneously is standby;
5 intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment five mixer granulator system micropill coating taste masking methods
One. prescription
1. raw material---sodium ferulate 50.0g;
2. adjuvant---starch 35.0g
Dextrin 5.0g
Sucrose 10.0g
Magnesium stearate 1.0g
3. binding agent---70% ethanol liquid is an amount of
4. coating material---Eudragit
E100 10.0g;
Eudragit
NE30D (doing) 4.0g;
5. filler---mannitol 80.0g;
Microcrystalline Cellulose 10.0g;
6. correctives---aspartame 1.0g;
Fragrant citrus essence 1.0g;
7. disintegrating agent---crospolyvinylpyrrolidone 10.0g;
L-HPC 5.0g；
8. fluidizer---micropowder silica gel 1.0g;
9. lubricant---magnesium stearate 1.0g.
Make 1000 altogether, specification: the 50mg/ sheet.
Two. preparation method
1 with ferulic acid, starch, dextrin, sucrose, magnesium stearate mixing, puts in the mixer granulator, mixes;
2 spray into binding agent, stir the preparation micropill;
Use coating material liquid coating after the 3 micropill dryings, drying.
The 4 adjuvant mix homogeneously that all the other are all add the coated granule that has made again, and mix homogeneously is standby;
5 intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Claims (8)
1. one kind has antioxidation and free radical scavenging effect; can protect cell membrane not oxidated and anticoagulant and thrombosis; the clinical atherosclerosis that is used for; treatment blood vessel embolism vasculitis; the Orally disintegrated sodium ferulate tablet of disease such as acute cerebral thrombosis and migraine; by supplementary materials such as sodium ferulate, filler, disintegrating agent, correctives, fluidizer, lubricants; according to circumstances can also add binding agent, effervescent or coating material; proportioning with suitable forms through specific method for preparing.It is characterized in that its prescription is composed as follows: sodium ferulate (5-50) %, binding agent (0-5) %, filler (10-80) %, disintegrating agent (2-35) %, correctives (1-40) %, coating material (0-40) %, effervescent (0-30) %, fluidizer (0.01-5) %, lubricant (0.3-3) %.
2. various adjuvants of addressing according to claim 1 is characterized in that selection kind separately is as follows:
Binding agent---include but are not limited to starch, pregelatinized Starch, dextrin, maltodextrin, sucrose, arabic gum, gelatin, methylcellulose, carboxymethyl cellulose, ethyl cellulose, polyvinyl alcohol, Polyethylene Glycol, polyvinylpyrrolidone (PVP), alginic acid and alginate, xanthan gum, hydroxypropyl cellulose and hydroxypropyl emthylcellulose (HPMC), can use use also capable of being combined separately.
Filler---include but are not limited to mannitol (granular or powdery), xylitol, sorbitol, maltose, Chi ?alcohol, microcrystalline Cellulose, PROSOLV
SMCC, polymerization sugar (EMDEX
), coupling sugar, glucose, lactose, sucrose, dextrin and starch etc., can use separately, also can applied in any combination, consumption is generally (10-80) %.
Disintegrating agent---include but are not limited to crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), low substituted hydroxy-propyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa) and soybean polysaccharide (EMCOSOY
) etc., can use use also capable of being combined separately.
Correctives---include but are not limited to mannitol, xylitol, stevioside, lactose, fructose, sucrose, protein sugar, maltose alcohol, glycyrrhizin, Sodium Cyclamate, gelatin, aspartame, flavoring banana essence, flavoring pineapple essence, vanillin, fragrant citrus essence, flavoring orange essence, Herba Menthae essence, ginseng essence, strawberry essence, citric acid, citric acid etc., can use use also capable of being combined separately.
Coating material---include but are not limited to gelatin, arabic gum, alginate, chitosan, carboxymethyl cellulose salt, cellulose acetate phthalate ester, ethyl cellulose, methylcellulose, hypromellose, crylic acid resin (homemade acrylic resin I, II, III, IV, Eudragit
Series), polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol etc., can use use also capable of being combined separately.
Fluidizer---include but are not limited to micropowder silica gel, Pulvis Talci, Cab-O-sil, Arosil, hydrated sodium aluminosilicate etc., can use use also capable of being combined separately.
Lubricant---include but are not limited to magnesium stearate, calcium stearate, zinc stearate, glyceryl monostearate, Polyethylene Glycol, hydrogenated vegetable oil, sodium stearyl fumarate, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium laurylsulfate, magnesium laurylsulfate, Stepanol MG and Pulvis Talci etc., can use use also capable of being combined separately.
3. a preparation method that is used for the Orally disintegrated sodium ferulate tablet that claim 1 addresses is characterized in that by following
Step is formed:
The pretreatment of first step sodium ferulate:
(1) directly flavoring---this law is granulated to the sodium ferulate raw material or is not dealt with, and directly enters for second step;
(2) powder coating taste masking---get selected coating material, with the dissolving of the solvent that adapts with it and to be diluted to debita spissitudo standby, getting sodium ferulate again places ebullated bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get sodium ferulate powder coating granule, dry back sieving for standby;
Second step took by weighing correctives and sodium ferulate or the feed particles after first step taste masking processing according to quantity, and mix homogeneously is standby;
The 3rd step took by weighing filler, disintegrating agent, effervescent, fluidizer and mix homogeneously according to quantity, made evenly again with through second mixing of materials that goes on foot gained, and adding lubricant mixing is standby;
The 4th step gained material detects through intermediate, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
4. the preparation method of addressing according to claim 3 is characterized in that: the method for the first step (2) need be used coating material that sodium ferulate is carried out taste masking in advance and handle.
5. the preparation method of addressing according to claim 4, it is characterized in that: the coating material that is used for the taste masking processing is gelatin, arabic gum, alginate, chitosan, carboxymethyl cellulose salt, cellulose acetate phthalate ester, ethyl cellulose, methylcellulose, hypromellose, crylic acid resin (homemade acrylic resin I, II, III, IV, Eudragit
Series), any one or two or more mixture such as polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol.
6. any preparation method of addressing according to claim 3 is characterized in that: according to circumstances also can add the adjuvant effervescent.
7. the effervescent of addressing according to claim 6, it is characterized in that: this adjuvant is the mixture of malic acid, citric acid or citric acid and sodium bicarbonate or sodium carbonate.
8. preparation method that is used for the Orally disintegrated sodium ferulate tablet that claim 1 addresses, the hardness that it is characterized in that the tablet that obtains are between 10 to 45 newton, and disintegration time is at 1-60 in second.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100964605A CN1303990C (en) | 2004-12-01 | 2004-12-01 | Sodium ferulate oral disintegrating tablet and its preparation process |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100964605A CN1303990C (en) | 2004-12-01 | 2004-12-01 | Sodium ferulate oral disintegrating tablet and its preparation process |
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| Publication Number | Publication Date |
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| CN1634014A true CN1634014A (en) | 2005-07-06 |
| CN1303990C CN1303990C (en) | 2007-03-14 |
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| CNB2004100964605A Expired - Fee Related CN1303990C (en) | 2004-12-01 | 2004-12-01 | Sodium ferulate oral disintegrating tablet and its preparation process |
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| CN (1) | CN1303990C (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1302772C (en) * | 2005-05-24 | 2007-03-07 | 中国人民解放军第二军医大学 | Orally disintegrated sodium ferulate tablet and its prepn process |
| CN101919803A (en) * | 2010-07-16 | 2010-12-22 | 钟术光 | A kind of controlled release preparation |
| CN102320956A (en) * | 2011-10-17 | 2012-01-18 | 山东罗欣药业股份有限公司 | Sodium ferulate composition freeze-dried powder injection and preparation method thereof |
| CN102357086A (en) * | 2011-11-01 | 2012-02-22 | 上海理工大学 | Cefprozil orally disintegrating tablets |
| CN102846564A (en) * | 2011-06-28 | 2013-01-02 | 南京亿华药业有限公司 | A cefprozil tablet and its preparation method |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1235576C (en) * | 2002-05-16 | 2006-01-11 | 中国人民解放军第二军医大学 | Slow-released dosage form of sodium ferulate and preparation process thereof |
| CN1225241C (en) * | 2003-07-30 | 2005-11-02 | 北京中西经纬释药技术有限公司 | Oral disintegrant tablet and its preparation method |
-
2004
- 2004-12-01 CN CNB2004100964605A patent/CN1303990C/en not_active Expired - Fee Related
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1302772C (en) * | 2005-05-24 | 2007-03-07 | 中国人民解放军第二军医大学 | Orally disintegrated sodium ferulate tablet and its prepn process |
| CN101919803A (en) * | 2010-07-16 | 2010-12-22 | 钟术光 | A kind of controlled release preparation |
| CN102846564A (en) * | 2011-06-28 | 2013-01-02 | 南京亿华药业有限公司 | A cefprozil tablet and its preparation method |
| CN102846564B (en) * | 2011-06-28 | 2013-10-09 | 南京亿华药业有限公司 | A cefprozil tablet and its preparation method |
| CN102320956A (en) * | 2011-10-17 | 2012-01-18 | 山东罗欣药业股份有限公司 | Sodium ferulate composition freeze-dried powder injection and preparation method thereof |
| CN102357086A (en) * | 2011-11-01 | 2012-02-22 | 上海理工大学 | Cefprozil orally disintegrating tablets |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1303990C (en) | 2007-03-14 |
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Address after: 100083 Haidian District, Xueyuan Road, No. 30, A building, room No. 15, room, room 15 Patentee after: COSCI MED-TECH Co.,Ltd. Address before: 100080, Haidian District satellite building, No. 63, Zhichun Road, Beijing, room 1410, Beijing Patentee before: COSCI MED-TECH Co.,Ltd. |
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