CN1217655C - Fibrauretine slow releasing prepn - Google Patents
Fibrauretine slow releasing prepn Download PDFInfo
- Publication number
- CN1217655C CN1217655C CN 03135781 CN03135781A CN1217655C CN 1217655 C CN1217655 C CN 1217655C CN 03135781 CN03135781 CN 03135781 CN 03135781 A CN03135781 A CN 03135781A CN 1217655 C CN1217655 C CN 1217655C
- Authority
- CN
- China
- Prior art keywords
- fibrauretine
- release
- sustained
- fibrauretin
- preparation
- 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.)
- Expired - Lifetime
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- 238000013268 sustained release Methods 0.000 claims abstract description 38
- 239000012730 sustained-release form Substances 0.000 claims abstract description 38
- 238000002360 preparation method Methods 0.000 claims abstract description 25
- RLQYRXCUPVKSAW-UHFFFAOYSA-M 2,3,9,10-tetramethoxy-5,6-dihydroisoquinolino[2,1-b]isoquinolin-7-ium;chloride Chemical compound [Cl-].COC1=C(OC)C=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=C1 RLQYRXCUPVKSAW-UHFFFAOYSA-M 0.000 claims description 64
- RIDQRIPSFYHEGL-UHFFFAOYSA-N fibrauretin Natural products CC12CC=C3C(=O)OC(CC3(C)C1C(=O)C=CC2=O)c4cocc4 RIDQRIPSFYHEGL-UHFFFAOYSA-N 0.000 claims description 64
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 44
- 239000008187 granular material Substances 0.000 claims description 32
- 238000002156 mixing Methods 0.000 claims description 23
- 235000019359 magnesium stearate Nutrition 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 22
- 239000000203 mixture Substances 0.000 claims description 13
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims description 7
- 235000010413 sodium alginate Nutrition 0.000 claims description 7
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- 239000002002 slurry Substances 0.000 claims description 5
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 4
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- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 3
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Landscapes
- Medicinal Preparation (AREA)
Abstract
The present invention discloses a fibrauretine sustained-release preparation. The preparation contains 40% to 70% of fibrauretine, 10% to 30% of auxiliary material which has the sustained-release function, and balance of other kinds of auxiliary material according to the weight percentage. The preparation can exist in a frame type preparation, a membrane control type preparation, a porous matrix type preparation and an osmotic pump type preparation, or microcapsules, microspheres and small pills are firstly prepared, and then, the sustained-release preparation is prepared. The preparation can prolong the action time of medicine, can reduce the number of times of taking medicine, can reduce the side effect of medicine and can enhance the medication elasticity.
Description
Technical field
The present invention relates to contain the compositions of fibrauretin, more particularly, the present invention relates to a kind of slow releasing preparation of fibrauretin.
Background technology
The Caulis Fibraureae prime system is from a kind of alkaloid hydrochloric acid palmatine of the stem proposition of menispermaceae plant Caulis Fibraureae (Fibraurea tinctoria Lour).Fibrauretin is xanchromatic acicular crystal; Nothing is smelt, and flavor is extremely bitter.Easy molten hot water, slightly soluble ethanol or chloroform, insoluble ether.Fibrauretin has effects for removing toxic heat, is used for gynecological inflammation, bacillary dysentery, enteritis, respiratory tract and urinary tract infection, surgical infection, eye conjunctivitis etc.Because of having has a broad antifungal spectrum, determined curative effect, characteristics that toxic and side effects is little, be widely used clinically.The domestic fibrauretin preparation of having developed has fibrauretin injection, fibrauretin sheet, fibrauretin capsule, fibrauretin collyrium, fibrauretin bolt at present.Wherein crude drug fibrauretin and fibrauretin sheet thereof, fibrauretin injection have recorded in one one of Pharmacopoeia of the People's Republic of China version in 1977, clinically with fibrauretin sheet use amount maximum.
Because most gynecological inflammations are chronic disease, can determine curative effect (every day 2 times, each 1 1～3 course of treatment with the injection treatment of fibrauretin, every 20mg, seven days one courses of treatment), tablet generally take 3 can produce effects more than the course of treatment (every 100mg, every day 1～3 time, each 2～4, seven days one courses of treatment), if escalated dose or prolongation Time of Administration, better effects if, but cause that easily patient's stomach receives uncomfortable symptom, disappear after the drug withdrawal.Fibrauretin sheet oral number of times every day is more, and dosage is bigger, and patient takes comparatively trouble, and exists and easily miss with take medicine night longly and can not keep the therapeutic effect that effective blood drug level and performance continue blanking time, the blind area in the treatment occurs.
Summary of the invention
The objective of the invention is at the deficiencies in the prior art, a kind of fibrauretine sustained-release preparation is provided.Described fibrauretine sustained-release preparation prolongs action time, reduces medicining times, reduces side effects of pharmaceutical drugs and improves patient's medication compliance with different release mechanism.
Purpose of the present invention is achieved by following technical proposals.
The invention provides a kind of fibrauretine sustained-release preparation, said preparation contains following composition by weight percentage:
Fibrauretin 40%～70%
Play the adjuvant 10%～30% of slow releasing function
Other adjuvant surplus.
Described fibrauretine sustained-release preparation comprises the various preparations of matrix type, film controlling type, porous matrix type, osmotic pump type etc., also comprises and makes the various preparations that microcapsule, microsphere, piller etc. are made preparation more earlier.
The adjuvant of described slow releasing function mainly comprises framework material and coating material, and two kinds of materials can be used separately or use in conjunction.The adoptable adjuvant of framework material has cellulose derivative class (ethyl cellulose, methylcellulose, hypromellose, hydroxypropyl cellulose, sodium carboxymethyl cellulose etc.), crylic acid resin (crylic acid resin II, III etc.), polyvinyl class (polyvinylpyrrolidone, polyvinyl alcohol, polystyrene, polrvinyl chloride etc.), natural product and extract class (spermaceti, zein, sodium alginate, gelatin, guar gum, cholesterol etc.) and some other adjuvant (octadecanol alkane, nylon, chitin, stearic acid, Polyethylene Glycol, carbomer etc.) wherein one or more.Coating material can adopt cellulose acetate, polylactic acid, cellulose acetate-phthalate, carboxymethylethylcellulose etc. wherein one or more.
Described other adjuvant is porogen, plasticizer, lubricant, binding agent, solvent, excipient etc.Porogen can adopt sucrose, lactose, mannitol, methylcellulose, sodium lauryl sulphate etc.Plasticizer can adopt glycerol, Oleum Ricini, Polyethylene Glycol etc.Binding agent can adopt polyvinylpyrrolidone, ethyl cellulose, starch slurry etc.Lubricant can adopt magnesium stearate, Pulvis Talci, liquid paraffin etc.Solvent can adopt ethanol, water, acetone, methanol, chloroform etc.Excipient can adopt starch, dextrin etc.
The dosage form of fibrauretine sustained-release preparation of the present invention is mainly tablet, also can be dosage forms such as pill, granule.
Instructions of taking: tablet is made the dosage of every 300mg, and only need take 2 every day, and what significantly reduced every day takes number of times and sheet number.
Fibrauretine sustained-release preparation of the present invention can adopt following method preparation:
Fibrauretin and framework material, porogen are mixed, add binding agent granulate, add direct compression behind the lubricant.
Fibrauretin is mixed with framework material or fibrauretin mixes with the excipient adjuvant, add binding agent and make medicated core, granule, pill, tablet etc., reuse coating material and plasticizer carry out coating.
The present invention is based on stripping, diffusion, three kinds of release principle design of infiltration, can be according to different release demands apply in a flexible way framework material and coating material, and can earlier medicine be made and carry out coating (or not coating) behind the matrix tablet again; Or make conventional granule or piller, carry out coating by different levels, also can a part coating not, another part press the different-thickness coating, mixes tabletting afterwards.
The present invention finds that from experiment the hardness of the consumption of framework material, porogen in the matrix sustained release tablet and tablet all has the influence of significance to the release in vitro behavior of slow releasing preparation.The consumption of framework material has the greatest impact, and is the size of tablet hardness secondly.The hardness of strengthening tablet helps controlling the release of medicine, but its effect is limited.The acquisition of hardness should be prerequisite with the normal operation of tablet machine.The rational hardness that has been determined by experiment tablet is 7～10kg, and the reasonable volume of having determined framework material on this basis again is 10%～30%.In addition porogen to the molding of tablet extremely release behavior to a certain degree influence is arranged, the very few release fully that is unfavorable for medicine of consumption, consumption too much can destroy slow release effect again.Also used bag film-coat technology in the fibrauretine sustained-release preparation in a large number, the selection of coating material and the composition of coating membrane have influenced the slow release effect of preparation to a great extent, single with the slice, thin piece bad mechanical property has appearred behind the coating material coating, than easy fracture, phenomenons such as clothing film quality difference, therefore added plasticizer, the film forming ability of coating material increases substantially, and the pliability of clothing film and intensity have also obtained enhancing.
The present invention has all done experimental study in depth to fibrauretine sustained-release stability of formulation and release in vitro degree.
A. fibrauretine sustained-release stability of formulation test
1. influence factor's test
The tablet of unlap put respectively carry out influence factor's test under 60 ℃, 92.5%RH and the 4000Lx illumination, respectively at sampling and measuring content and release after 10 hours.
2. reserved sample observing test
With tablet packing back respectively at sampling and measuring content and release after 3,6,12,24,36 months.
3. result
3.1 it is after the illumination 10 days, to related substance, content, release influence not quite, influential to character.Behind the high temperature 10 days, to related substance, content, release influence not quite, darken.High humidity influences little to related substance, content, release after 10 days, influential to character.
3.2 packing back this product has stability preferably, and is all up to specification to related substance, content, dissolution, appearance luster.
The preliminarily stabilised result of the test of fibrauretine sustained-release preparation is as shown in table 1.
Table 1. fibrauretine sustained-release preparation preliminarily stabilised result of the test
| Pilot project | High temperature (60 ℃) | High humidity (92.5%) | High light (4000Lx) | Reserved sample observing (24 months) |
| Content | Up to specification | Up to specification | Up to specification | Up to specification |
| Release 2h | 34.0～35.6％ | 34.1～35.7％ | 34.2～35.7％ | 34.1～35.6％ |
| 4h | 56.0～57.3％ | 56.0～57.2％ | 55.9～57.3％ | 56.0～57.2％ |
| 8h | 82.6～83.6％ | 82.3～83.5％ | 82.6～83.7％ | 82.8～83.8％ |
B. fibrauretine sustained-release preparation inside and outside release research
1. the external release research of fibrauretine sustained-release sheet
1.1 material and instrument
Fibrauretine sustained-release sheet (every 300mg, self-control) common plain sheet (every 100mg, our factory's product, lot number 20020903), ZRS-4 type intelligence dissolution test instrument (Radio Factory of Tianjin Univ.), LC-2010A type high performance liquid chromatography (day island proper Tianjin).
1.2 test method and result
Get fibrauretine sustained-release sheet and common plain each a slice of sheet sample, 900ml purification water as solvent, 37 ℃ of temperature, rotating speed 100r/min, respectively at 1,2,4,6,8,10,12 hour timing spot sampling 5ml (replenishing the same medium of 5ml simultaneously), 0.45 μ m filtering with microporous membrane, high-efficient liquid phase technique is measured the cumulative release amount, calculates relative cumulative release percentage rate.The cumulative release rate of fibrauretine sustained-release sheet and fibrauretin sheet is as shown in table 2.
The cumulative release rate of table 2. fibrauretine sustained-release sheet and fibrauretin sheet
| Time (hour) | 1 | 2 | 4 | 6 | 8 | 10 | 12 |
| The ordinary tablet slow releasing tablet | 80.0％ 16.9％ | 81.0％ 35.1％ | 82.0％ 56.4％ | 82.1％ 75.6％ | 82.1％ 83.4％ | 82.12％ 91.3％ | 82.1％ 93.1％ |
Result of the test shows that ordinary tablet surpasses 80% 1 hour cumulative release rate, and release amount does not after this have to change substantially, and the sustained-release tablets release effect is obvious, 12 hours curve Higuchi equation, and 12 hours release amounts can reach more than 90%.Fibrauretine sustained-release sheet of the present invention progressively discharged medicine in 12 hours, keep the required blood drug level of treatment, and effect is lasting, the purpose of convenient drug administration thereby reach.
The fibrauretine sustained-release sheet at Canis familiaris L. body giving drugs into nose for dynamics research
2.1 experiment material and instrument
10 of fibrauretine sustained-release sheet (every 300mg, self-control) common plain sheets (every 100mg, our factory's product product, lot number 20020903), LC-2010A type high performance liquid chromatography (day island proper Tianjin), healthy mongrel, body weight (5.3 ± 0.6) kg.
2.2 experimental technique
Testing preceding 10 healthy mongrels fed 3～5 days through adaptability.Tried evening the previous day and behind the feeding be fasting to after the administration four hours on an empty stomach morning on the same day, whole process be can't help drinking-water.Mongrel is divided into two groups at random, and 5 every group, one group of per os is irritated reference product fibrauretin sheet 300mgkg
-1, another group per os is irritated test sample fibrauretine sustained-release sheet 300mgkg
-1, respectively at adopting femoral artery to get blood in 0.5,1,2,3,4,5,6,8,10,12,24 hour before the administration with after the administration, the blood sample centrifugalize goes out serum, and serum is preserved to be analyzed in-20 ℃ of refrigerators, press high-efficient liquid phase technique mensuration blood drug level.
2.3 behind the healthy mongrel oral administration of experimental result, the blood drug level (μ g/ml) of different time sees Table 3. in the body
The drug-time curve data of table 3. fibrauretine sustained-release sheet and ordinary tablet
| Time (h) | 0.5 | 1 | 2 | 3 | 4 | 5 | 6 | 8 | 10 | 12 | 24 |
| The ordinary tablet slow releasing tablet | 2.01 1.25 | 3.69 2.04 | 5.63 3.20 | 3.02 4.36 | 2.11 4.55 | 1.53 4.65 | 0.63 4.62 | 0.20 4.12 | 0.09 2.87 | 0.03 1.69 | 0.01 0.02 |
Curve data handles that to obtain kinetic parameter as shown in table 4 during according to the medicine of fibrauretine sustained-release sheet and ordinary tablet.
The kinetic parameter of oral fibrauretine sustained-release sheet of table 4. Canis familiaris L. and ordinary tablet
| AUC(μg·h/ml) | MRT(h) | t max(h) | C max(μg/ml) | |
| Ordinary tablet | 8.66±2.34 | 3.96±1.20 | 0.92±0.12 | 5.63±1.32 |
| Slow releasing tablet | 15.35±3.36 | 9.25±3.10 | 3.36±0.62 | 4.65±1.01 |
Single dose is given AUC (drug-time curve area), MRT (mean residence time) and the t of oral fibrauretine sustained-release sheet of Canis familiaris L. and ordinary tablet
Max(peak time) exists significant difference (P＜0.01), C
Max(peak concentration) there was no significant difference (P＞0.05). wherein the AUC of fibrauretine sustained-release sheet is 1.8 times of ordinary tablet, t
MaxWith MRT all than the prolongation of ordinary tablet, C
MaxLow than ordinary tablet.The relative bioavailability of slow releasing tablet and ordinary tablet (F) by formula F=(for test piece AUC/ reference sheet AUC) * 100% is calculated as 177%.
2.4 discuss
The t of fibrauretin slow releasing preparation
MaxLong with MRT than ordinary preparation, show that the administration time of slow releasing preparation prolongs; C
MaxLow than ordinary preparation, show that the toxic and side effects of slow releasing preparation is less.The elimination speed ratio ordinary tablet of slow releasing tablet slow as can be seen from the drug-time curve of fibrauretine sustained-release sheet, oral administration 3-9 hour blood drug level is the held stationary level always, slow release effect is obvious, and in the valid density scope, substantially overcome the peak valley phenomenon of blood drug level, reach the minimizing medicining times, reduced the purpose of toxic and side effects.The situation of external release is consistent with this trend substantially.The release result of inside and outside shows that all the fibrauretine sustained-release sheet truly has than ordinary tablet slow, characteristics that bioavailability is high.
In sum, compared with prior art, the present invention has following beneficial effect:
1. can make the blood drug level of human body keep the long period, very fast decline unlike ordinary preparation, " peak valley " phenomenon of having avoided the ordinary preparation frequent drug administration to be occurred has improved safety, effectiveness and the adaptability of medicine.Reduced and taken the GI irritation that fibrauretin produces for a long time.
2. medicine-releasing performance is good, and blood drug level is steady, and release mechanism that can be different prolongs action time, reduces administration number of times, has improved compliance of patients greatly, and is easy to use and carry.
3. can reduce the accumulated dose of medication, reach maximum efficacy with minimum doses, the fibrauretin cost of material is expensive, makes slow releasing preparation and has saved cost.Promote the exploitation of the novel form of fibrauretin, effectively brought into play the pharmacological action of fibrauretin.Market potential is big, is the good medicine of treatment gynecological inflammation.
4. product stability is good, technology favorable reproducibility and mechanization degree height, the production equipment of available routine and prepared.
Description of drawings
Fig. 1 is the sketch map of technological process of the present invention;
Fig. 2 is fibrauretine sustained-release sheet and ordinary tablet release curve chart;
Fig. 3 is the medicine curve chart in a period of time of fibrauretine sustained-release sheet and ordinary tablet;
The specific embodiment
By specific embodiment given below and typical application embodiment, can further be well understood to the present invention.But they are not limitation of the invention.
Embodiment 1
[component] fibrauretin 300mg
HPMC(K4M) 150mg
Lactose 100mg
Magnesium stearate 6mg
[method for making] with fibrauretin and HPMC, lactose mixing, is dissolved in making wetting agent in the ethanol and making soft material, granulate, and drying, granulate adds the magnesium stearate mixing, and tabletting promptly gets the fibrauretine sustained-release sheet.
Embodiment 2
[component] fibrauretin 400mg
Hypromellose 80mg
Dextrin 20mg
Sodium lauryl sulphate is an amount of
Ethanol is an amount of
Magnesium stearate is an amount of
[method for making] with fibrauretin and sodium lauryl sulphate, hypromellose, dextrin mixing, the system soft material, and 20 mesh sieves are granulated, and dry, 18 order granulate add the magnesium stearate mixing, and tabletting promptly gets the fibrauretine sustained-release sheet.
Embodiment 3
[component] fibrauretin 300mg
Sodium alginate 180mg
Anhydrous calcium chloride 20mg
Magnesium stearate 5mg
[method for making] adds 2% sodium alginate slurry granulation with fibrauretin, sodium alginate and anhydrous calcium chloride mix homogeneously, and drying adds the magnesium stearate mixing, and granulate, tabletting promptly get the fibrauretine sustained-release sheet.
Embodiment 4
[component] fibrauretin 500mg
Stearic acid 40mg
Ethyl cellulose is an amount of
Ethanol is an amount of
Magnesium stearate 5mg
[method for making] adds 10% ethyl cellulose ethanol liquid granulation with fibrauretin and stearic acid mixing, and drying adds the magnesium stearate mixing, and granulate, tabletting promptly get the fibrauretine sustained-release sheet.
Embodiment 5
[component] fibrauretin 400mg
Glyceryl monostearate 80mg
Microcrystalline Cellulose 100mg
Magnesium stearate 6mg
[method for making] adds the mixture of fibrauretin and microcrystalline Cellulose lentamente with tristerin fusion in water-bath, allows its slow cooling under constantly stirring.Cross 14 mesh sieves then and granulate, add magnesium stearate, mixing, tabletting promptly get the fibrauretine sustained-release sheet.
Embodiment 6
[component] fibrauretin 400mg
Ethyl cellulose 100mg
[method for making] is dispersed in fibrauretin in the ethanol liquid of ethyl cellulose, and the pulverizing to the constant weight of evaporate to dryness, agglomerate vacuum drying, granulation, tabletting promptly get the fibrauretine sustained-release sheet.
Embodiment 7
[component] fibrauretin 300mg
Ethyl cellulose 90mg
Hydroxypropyl cellulose 50mg
Octadecanol 50mg
Lactose 20mg
[method for making] is wetting agent system soft material with fibrauretin, ethyl cellulose, hydroxypropyl cellulose, octadecanol, lactose mixing with ethanol, and 20 mesh sieves are granulated, drying, and granulate, tabletting promptly get the fibrauretine sustained-release sheet.
Embodiment 8
[component] slow-releasing granules part
Fibrauretin 200mg
Ethyl cellulose 30mg
Acrylic resin is an amount of
Octadecanol is an amount of
Lactose 15mg
The immediate-release granules part
Fibrauretin 100mg
Starch 25mg
12% starch slurry is an amount of
Pulvis Talci is an amount of
[method for making] slow-releasing granules: with the fine powder mixing of ethyl cellulose, acrylic resin, octadecanol and lactose, with adding fibrauretin fine powder system soft material, the granulation of sieving, drying, granulate behind an amount of dissolve with ethanol; Immediate-release granules: with fibrauretin and starch mixing, with 12% starch slurry system soft material, the granulation of sieving, drying, granulate.With two kinds of abundant mixings of granule, weigh, add an amount of Pulvis Talci, mixing, tabletting promptly get the fibrauretine sustained-release sheet.
Embodiment 9
[component] fibrauretin 300mg
Hexadecanol 70mg
HPMC 50mg
Acrylic resin 50mg
Sodium lauryl sulphate is an amount of
Magnesium stearate is an amount of
[method for making] fully mixes the back with 2%HPMC aqueous solution system soft material with medicine and adjuvant mix homogeneously, and cross 18 mesh sieves and granulate, drying, granulate adds the magnesium stearate mixing, and tabletting promptly gets the fibrauretine sustained-release sheet.
Embodiment 10
[component] granule A
Fibrauretin 500mg
Hydroxypropyl methylcellulose (400cps) 180mg
Hydroxypropyl methylcellulose (15cps) 4mg
Granule B
Precipitated calcium carbonate 70mg
Magnesium carbonate 20mg
Mannitol 15mg
Carboxymethyl cellulose 2mg
[method for making] adds Pulvis Talci with two kinds of granule mixings, and mixing, tabletting promptly get the fibrauretine sustained-release sheet.
Embodiment 11
[component] sheet heart
Fibrauretin 400mg
Lactose 50mg
Ethyl cellulose 8mg
90% ethanol is an amount of
Magnesium stearate is an amount of
Semipermeable membrane
Cellulose acetate 7g
PEG400 is an amount of
Acetone adds to 100ml
[method for making] adds ethyl cellulose ethanol liquid system soft material with fibrauretin and lactose mix homogeneously, crosses 16 mesh sieve system wet granulars, and drying is crossed 14 mesh sieve granulate, carries out tabletting behind the adding magnesium stearate mixing, coating, and laser boring promptly gets the fibrauretine sustained-release sheet.
Embodiment 12
[component] label
Fibrauretin 500mg
Mannitol 50mg
Magnesium stearate 6mg
Coating solution
Fibrauretin 100mg
Cellulose acetate 150mg
Acetone adds to 100ml
[method for making] adds water system granule, drying with fibrauretin and mannitol mix homogeneously, granulate carries out tabletting behind the adding magnesium stearate mixing, with the aqueous acetone solution spray coating that contains fibrauretin, cellulose acetate, drying, laser boring (aperture: 0.25mm), promptly get the fibrauretine sustained-release sheet.
Embodiment 13
[component] sheet heart
Fibrauretin 400mg
Ethyl cellulose 100mg
95% ethanol is an amount of
Magnesium stearate 5mg
Coating solution
Two cellulose acetate 6g
PEG400 5ml
Diethyl phthalate 5ml
Acetone adds to 100ml
[method for making] adds binding agent after getting principal agent and the abundant mixing of adjuvant, and the system soft material is crossed 20 order nylon sieve series wet granulars, dry, the granulate that sieves, and tabletting, coating promptly get the fibrauretine sustained-release sheet.
Embodiment 14
[component] fibrauretin 500mg
5% ethyl cellulose toluene ethanol liquid is an amount of
Microcrystalline Cellulose 45mg
Starch 10mg
Magnesium stearate is an amount of
[method for making] makes the granule of suitable size with fibrauretin, with 5% ethyl cellulose toluene ethanol liquid coating.Granule behind the coating is added microcrystalline Cellulose, starch and magnesium stearate, and tabletting promptly gets the fibrauretine sustained-release sheet behind the mixing.
Embodiment 15
[component] fibrauretin 500mg
Ethyl cellulose 100mg
95% ethanol is an amount of
Pulvis Talci is an amount of
Two cellulose acetate 20mg
Acetone is added to 100ml
[method for making] adds ethyl cellulose ethanol liquid system soft material with fibrauretin and ethyl cellulose mix homogeneously, and 18 orders are granulated, drying, and granulate adds the Pulvis Talci mixing, and tabletting with two cellulose acetate acetone solution spray coatings, promptly gets the fibrauretine sustained-release sheet.
Embodiment 16
[component] ball core
Fibrauretin 500mg
Starch is an amount of
Dextrin is an amount of
Ethanol is an amount of
Coating solution
Acrylic resin II 5g
PEG400 0.8g
Diethyl phthalate 0.01g
Pulvis Talci is an amount of
Ethanol adds to 100ml
[method for making] makes the micropill ball heart with the abundant mixing of starch, dextrin of fibrauretin and proper proportion with certain density ethanol in coating pan, take out drying.Get the dry ball heart of making, weigh after removing fine powder, put coating in the coating pan, promptly get the fibrauretin controlled release micro pill, can further be processed into other dosage forms.
Claims (1)
1. fibrauretine sustained-release sheet, every comprises fibrauretin 300mg, sodium alginate 180mg, anhydrous calcium chloride 20mg, magnesium stearate 5mg, and adopt the preparation of following method: with fibrauretin, sodium alginate and anhydrous calcium chloride mix homogeneously, be benchmark, add 2% sodium alginate slurry and granulate with the weight of mixture, dry, add the magnesium stearate mixing, granulate, tabletting promptly get the fibrauretine sustained-release sheet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03135781 CN1217655C (en) | 2003-09-05 | 2003-09-05 | Fibrauretine slow releasing prepn |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03135781 CN1217655C (en) | 2003-09-05 | 2003-09-05 | Fibrauretine slow releasing prepn |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1491644A CN1491644A (en) | 2004-04-28 |
| CN1217655C true CN1217655C (en) | 2005-09-07 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03135781 Expired - Lifetime CN1217655C (en) | 2003-09-05 | 2003-09-05 | Fibrauretine slow releasing prepn |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1726914B (en) * | 2004-07-27 | 2011-02-09 | 中国人民解放军军事医学科学院毒物药物研究所 | Slow release tablet of rotundine and production process |
| CN100335035C (en) * | 2004-10-25 | 2007-09-05 | 张帆 | Preparation method and application of Chinese medicinal preparation for ophthalmology |
| CN102626397A (en) * | 2012-04-25 | 2012-08-08 | 云南植物药业有限公司 | Hydrophilic gel type palmatine sustained-release tablet and preparation method thereof |
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