CN109010297A - A kind of cefprozil tablet and preparation method thereof - Google Patents
A kind of cefprozil tablet and preparation method thereof Download PDFInfo
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- CN109010297A CN109010297A CN201811249881.5A CN201811249881A CN109010297A CN 109010297 A CN109010297 A CN 109010297A CN 201811249881 A CN201811249881 A CN 201811249881A CN 109010297 A CN109010297 A CN 109010297A
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- cefprozil
- parts
- medicine
- microsphere
- tablet
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- WDLWHQDACQUCJR-ZAMMOSSLSA-N (6r,7r)-7-[[(2r)-2-azaniumyl-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-[(e)-prop-1-enyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)/C=C/C)C(O)=O)=CC=C(O)C=C1 WDLWHQDACQUCJR-ZAMMOSSLSA-N 0.000 title claims abstract description 66
- 229960002580 cefprozil Drugs 0.000 title claims abstract description 66
- 238000002360 preparation method Methods 0.000 title claims description 20
- 239000004005 microsphere Substances 0.000 claims abstract description 46
- 239000003814 drug Substances 0.000 claims abstract description 34
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 26
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 26
- 102000009027 Albumins Human genes 0.000 claims abstract description 14
- 108010088751 Albumins Proteins 0.000 claims abstract description 14
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims abstract description 13
- 229920002472 Starch Polymers 0.000 claims abstract description 13
- 239000008101 lactose Substances 0.000 claims abstract description 13
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims abstract description 13
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 13
- 239000000377 silicon dioxide Substances 0.000 claims abstract description 13
- 239000011734 sodium Substances 0.000 claims abstract description 13
- 229910052708 sodium Inorganic materials 0.000 claims abstract description 13
- 239000008107 starch Substances 0.000 claims abstract description 13
- 235000019698 starch Nutrition 0.000 claims abstract description 13
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 30
- 239000007864 aqueous solution Substances 0.000 claims description 12
- 239000006210 lotion Substances 0.000 claims description 12
- 239000012188 paraffin wax Substances 0.000 claims description 10
- 238000003756 stirring Methods 0.000 claims description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 9
- 239000003995 emulsifying agent Substances 0.000 claims description 8
- 239000007788 liquid Substances 0.000 claims description 7
- 238000005406 washing Methods 0.000 claims description 7
- 230000001804 emulsifying effect Effects 0.000 claims description 5
- 238000010438 heat treatment Methods 0.000 claims description 5
- 239000000843 powder Substances 0.000 claims description 5
- 238000002604 ultrasonography Methods 0.000 claims description 5
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 3
- 238000005520 cutting process Methods 0.000 abstract description 2
- 238000004519 manufacturing process Methods 0.000 abstract description 2
- 239000002994 raw material Substances 0.000 description 6
- 230000007062 hydrolysis Effects 0.000 description 4
- 238000006460 hydrolysis reaction Methods 0.000 description 4
- 238000000338 in vitro Methods 0.000 description 4
- 239000003921 oil Substances 0.000 description 4
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 4
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 238000011001 backwashing Methods 0.000 description 3
- 210000003128 head Anatomy 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 241000894006 Bacteria Species 0.000 description 1
- 206010007882 Cellulitis Diseases 0.000 description 1
- 229930186147 Cephalosporin Natural products 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 201000008197 Laryngitis Diseases 0.000 description 1
- 206010024971 Lower respiratory tract infections Diseases 0.000 description 1
- 201000007100 Pharyngitis Diseases 0.000 description 1
- 206010035664 Pneumonia Diseases 0.000 description 1
- 206010057190 Respiratory tract infections Diseases 0.000 description 1
- 206010062255 Soft tissue infection Diseases 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 206010006451 bronchitis Diseases 0.000 description 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 1
- 229940124587 cephalosporin Drugs 0.000 description 1
- 150000001780 cephalosporins Chemical class 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000011109 contamination Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000011806 microball Substances 0.000 description 1
- 210000003695 paranasal sinus Anatomy 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 206010044008 tonsillitis Diseases 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 208000025301 tympanitis Diseases 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1658—Proteins, e.g. albumin, gelatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
- A61K9/204—Polyesters, e.g. poly(lactide-co-glycolide)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2063—Proteins, e.g. gelatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- Oncology (AREA)
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- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of cefprozil tablet, the component including following weight proportion: 400-450 parts of medicine-containing microsphere, 20-25 parts of lactose, 10-12 parts of low-substituted hydroxypropyl cellulose, 5-7 parts of sodium carboxymethyl starch, 0.5-1 parts of silica, 0.7-0.8 parts of magnesium stearate；For medicine-containing microsphere using PLA- albumin complex microsphere as carrier, Cefprozil drugloading rate is 10%-15%.The present invention contains Cefprozil using PLA- albumin complex microsphere, the stability of Cefprozil can be effectively improved, and the peculiar smell for reaching certain slow release effect, while completely cutting off Cefprozil drug itself, avoid the addition of the corrigent in tablet manufacture.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, and in particular to a kind of Cefprozil tablet with slow release effect.
Background technique
Cefprozil belongs to second generation semi-synthetic cephalosporins antibiotic, can be used in light, moderate caused by sensitive bacteria,
Lower respiratory tract infection (such as pharyngitis, laryngitis, tonsillitis, pneumonia, bronchitis), Respiratory infections (such as tympanitis, nasal sinus
Inflammation etc.), skin and skin soft-tissue infection's (such as cellulitis, epifolliculitis, trauma infection contamination).
Existing regular dosage form is Cefprozil dispersible table, due to the peculiar smell of its drug itself, needs to be added in tabletting and rectify
Taste agent.And since Cefprozil is to water, thermally labile, when storing improperly, solution decomposes and goes bad, to drop
The low therapeutic effect for influencing Cefprozil.The half-life period of Cefprozil is shorter simultaneously, and only 1.3 hours.
Summary of the invention
The purpose of the present invention is to solve drawbacks described above existing in the prior art, a kind of stable storage is provided and is had
There is the cefprozil tablet of slow release effect.
In order to reach said effect, the present invention provides a kind of cefprozil tablets, the component including following weight proportion: contain
400-450 parts of medicine microballoon, 20-25 parts of lactose, 10-12 parts of low-substituted hydroxypropyl cellulose, 5-7 parts of sodium carboxymethyl starch, titanium dioxide
0.5-1 parts of silicon, 0.7-0.8 parts of magnesium stearate；Using PLA- albumin complex microsphere as carrier, Cefprozil carries the medicine-containing microsphere
Dose is 10%-15%.
Preferred ingredient proportion are as follows: 420 parts of medicine-containing microsphere, 20 parts of lactose, 10 parts of low-substituted hydroxypropyl cellulose, carboxymethyl starch
7 parts of sodium, 0.5 part of silica, 0.7 part of magnesium stearate；The medicine-containing microsphere is using PLA- albumin complex microsphere as carrier, cephalo
Propylene drugloading rate is 12%.
The present invention also provides the preparation methods of above-mentioned cefprozil tablet, comprising the following steps:
(1) Cefprozil powder is taken to be dissolved in 40-60 DEG C of pure water, the Cefprozil that preparation concentration is 12-20mg/mL
Aqueous solution；
(2) PLA- albumin complex microsphere is taken to be dissolved in the Cefprozil being prepared in step (1) under ultrasonic state
In aqueous solution, emulsifier and paraffin, stirring and emulsifying 30min at 40 DEG C is added, and ultrasound homogenizes preparation lotion；The white egg of PLA-
The additional amount of white complex microsphere is that 100mg is added in every milliliter of Cefprozil aqueous solution；
(3) it takes heating paraffin to 125-135 DEG C, the lotion that step (2) is prepared slowly is instilled under stirring, is added dropwise to complete
At, it is cooled to room temperature after isothermal curing 10min, ether is added, washing is sufficiently stirred, be centrifuged, pour out upper layer oil ether liquid, it is so heavy
After backwashing is washed 2-4 times, and most ether is waved, and is freeze-dried to obtain medicine-containing microsphere；
(4) after taking medicine-containing microsphere, lactose, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch premixing by weight ratio, add
Enter silica, magnesium stearate mixing, direct tablet compressing is up to the cefprozil tablet.
Wherein, the concentration of Cefprozil aqueous solution is 15mg/mL in step (1).
The preferred polyoxyethylene sorbitan monoleate of emulsifier.
The preferred 4mL/min of rate of addition of lotion in step (3).
The present invention has the advantage that compared with prior art wraps Cefprozil using PLA- albumin complex microsphere
It carries, the stability of Cefprozil can be effectively improved, and reach certain slow release effect, while completely cutting off Cefprozil drug itself
Peculiar smell avoids the addition of the corrigent in tablet manufacture.Due to the mobility of medicine-containing microsphere itself, tabletting can be reduced
The addition of silica in journey.
Detailed description of the invention
Fig. 1 is the In-vitro release curves of Cefprozil medicine-containing microsphere of the present invention.
Specific embodiment
The present invention is described in detail combined with specific embodiments below.
Embodiment 1
The raw material of cefprozil tablet of the present invention forms are as follows: and 420 parts of medicine-containing microsphere, 20 parts of lactose, low-substituted hydroxypropyl cellulose
10 parts, 7 parts of sodium carboxymethyl starch, 0.5 part of silica, 0.7 part of magnesium stearate.
Wherein, medicine-containing microsphere the preparation method is as follows:
(1) Cefprozil powder is taken to be dissolved in 40-60 DEG C of pure water, the Cefprozil water that preparation concentration is 15mg/mL
Solution；
(2) PLA- albumin complex microsphere is taken to be dissolved in the Cefprozil being prepared in step (1) under ultrasonic state
In aqueous solution, emulsifier and paraffin, stirring and emulsifying 30min at 40 DEG C is added, and ultrasound homogenizes preparation lotion；The white egg of PLA-
The additional amount of white complex microsphere is that 100mg is added in every milliliter of Cefprozil aqueous solution；
(3) it takes heating paraffin to 125-135 DEG C, the lotion (rate of addition that step (2) is prepared slowly is instilled under stirring
It for 4mL/min), is added dropwise to complete into, is cooled to room temperature after isothermal curing 10min, ether is added, washing is sufficiently stirred, be centrifuged, incline
Upper layer oil ether liquid out, so repeated washing 2-4 times, wave most ether, are freeze-dried to obtain medicine-containing microsphere.
Microballoon hydrolysis is carried out to the medicine-containing microsphere being prepared, it is 12% that its drugloading rate, which is calculated,.
The medicine-containing microsphere being prepared is taken to add by raw material proportioning and lactose, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch
Enter and be pre-mixed 20min in mixing machine, add silica, magnesium stearate continuess to mix 10min, direct tablet compressing is up to the head
Spore propylene piece.
Release in vitro is carried out to the cefprozil tablet being prepared, the release in vitro of detection different time sections Cefprozil contains
Amount calculates Cefprozil and adds up release rate (Q), and preparation-obtained cefprozil tablet has In-vitro release curves as shown in Figure 1:
There is certain slow release effect.
It takes the cefprozil tablet being prepared to carry out accelerated test and long-term stable experiment, carries out at regular intervals micro-
Ball hydrolysis measurement Cefprozil content is made as a result as shown in the following table 1, table 2 in each table with the Cefprozil content for testing starting point
Relative amount calculating is carried out for labelled amount.
1 accelerated test result of table
| Time (moon) | 0 | 1 | 2 | 3 | 4 | 5 | 6 |
| Cefprozil content | 100% | 100% | 99.95% | 99.73% | 99.41% | 99.24% | 99.07% |
2 long-term stable experiment result of table
| Time (moon) | 0 | 3 | 6 | 9 | 12 | 18 | 24 |
| Cefprozil content | 100% | 99.98% | 99.95% | 99.87% | 99.62% | 99.39% | 99.12% |
As seen from the above table, the cefprozil tablet that the present invention is prepared has good stability, and wherein Cefprozil is not susceptible to
It decomposes or rotten.
Embodiment 2
The raw material of cefprozil tablet of the present invention forms are as follows: and 400 parts of medicine-containing microsphere, 20 parts of lactose, low-substituted hydroxypropyl cellulose
10 parts, 5 parts of sodium carboxymethyl starch, 0.5 part of silica, 0.7 part of magnesium stearate.
Wherein, medicine-containing microsphere the preparation method is as follows:
(1) Cefprozil powder is taken to be dissolved in 40-60 DEG C of pure water, the Cefprozil water that preparation concentration is 20mg/mL
Solution；
(2) PLA- albumin complex microsphere is taken to be dissolved in the Cefprozil being prepared in step (1) under ultrasonic state
In aqueous solution, emulsifier and paraffin, stirring and emulsifying 30min at 40 DEG C is added, and ultrasound homogenizes preparation lotion；The white egg of PLA-
The additional amount of white complex microsphere is that 100mg is added in every milliliter of Cefprozil aqueous solution；
(3) it takes heating paraffin to 125-135 DEG C, the lotion that step (2) is prepared slowly is instilled under stirring, is added dropwise to complete
At, it is cooled to room temperature after isothermal curing 10min, ether is added, washing is sufficiently stirred, be centrifuged, pour out upper layer oil ether liquid, it is so heavy
After backwashing is washed 2-4 times, and most ether is waved, and is freeze-dried to obtain medicine-containing microsphere.
Microballoon hydrolysis is carried out to the medicine-containing microsphere being prepared, it is 15% that its drugloading rate, which is calculated,.
The medicine-containing microsphere being prepared is taken to add by raw material proportioning and lactose, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch
Enter and be pre-mixed 20min in mixing machine, add silica, magnesium stearate continuess to mix 10min, direct tablet compressing is up to the head
Spore propylene piece.
Embodiment 3
The raw material of cefprozil tablet of the present invention forms are as follows: and 450 parts of medicine-containing microsphere, 25 parts of lactose, low-substituted hydroxypropyl cellulose
10-12 parts, 7 parts of sodium carboxymethyl starch, silica 1 part, 0.8 part of magnesium stearate.
Wherein, medicine-containing microsphere the preparation method is as follows:
(1) Cefprozil powder is taken to be dissolved in 40-60 DEG C of pure water, the Cefprozil water that preparation concentration is 12mg/mL
Solution；
(2) PLA- albumin complex microsphere is taken to be dissolved in the Cefprozil being prepared in step (1) under ultrasonic state
In aqueous solution, emulsifier (conventional emulsifier) and paraffin, stirring and emulsifying 30min at 40 DEG C is added, and ultrasound homogenizes preparation
Lotion；The additional amount of the PLA- albumin complex microsphere is that 100mg is added in every milliliter of Cefprozil aqueous solution；
(3) it takes heating paraffin to 125-135 DEG C, the lotion that step (2) is prepared slowly is instilled under stirring, is added dropwise to complete
At, it is cooled to room temperature after isothermal curing 10min, ether is added, washing is sufficiently stirred, be centrifuged, pour out upper layer oil ether liquid, it is so heavy
After backwashing is washed 2-4 times, and most ether is waved, and is freeze-dried to obtain medicine-containing microsphere.
Microballoon hydrolysis is carried out to the medicine-containing microsphere being prepared, it is 10% that its drugloading rate, which is calculated,.
The medicine-containing microsphere being prepared is taken to add by raw material proportioning and lactose, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch
Enter and be pre-mixed 20min in mixing machine, add silica, magnesium stearate continuess to mix 10min, direct tablet compressing is up to the head
Spore propylene piece.
Claims (6)
1. a kind of cefprozil tablet, it is characterised in that: the cefprozil tablet includes the component of following weight proportion: medicine-containing microsphere
400-450 parts, 20-25 parts of lactose, 10-12 parts of low-substituted hydroxypropyl cellulose, 5-7 parts of sodium carboxymethyl starch, silica 0.5-1
Part, 0.7-0.8 parts of magnesium stearate；Using PLA- albumin complex microsphere as carrier, Cefprozil drugloading rate is the medicine-containing microsphere
10%-15%.
2. cefprozil tablet according to claim 1, it is characterised in that: the cefprozil tablet includes following weight proportion
Component: 420 parts of medicine-containing microsphere, 20 parts of lactose, 10 parts of low-substituted hydroxypropyl cellulose, 7 parts of sodium carboxymethyl starch, silica
0.5 part, 0.7 part of magnesium stearate；Using PLA- albumin complex microsphere as carrier, Cefprozil drugloading rate is the medicine-containing microsphere
12%.
3. the preparation method of cefprozil tablet described in claim 1, which comprises the following steps:
(1) Cefprozil powder is taken to be dissolved in 40-60 DEG C of pure water, the Cefprozil that preparation concentration is 12-20mg/mL is water-soluble
Liquid；
(2) PLA- albumin complex microsphere is taken to be dissolved in the Cefprozil being prepared in step (1) under ultrasonic state water-soluble
In liquid, emulsifier and paraffin, stirring and emulsifying 30min at 40 DEG C is added, and ultrasound homogenizes preparation lotion；The PLA- albumin is multiple
The additional amount for closing microballoon is that 100mg is added in every milliliter of Cefprozil aqueous solution；
(3) it takes heating paraffin to 125-135 DEG C, the lotion that step (2) is prepared slowly is instilled under stirring, is added dropwise to complete into,
It is cooled to room temperature after isothermal curing 10min, ether is added, washing is sufficiently stirred, be centrifuged, pour out upper layer oil ether liquid, so repeated
Washing 2-4 times, waves most ether, is freeze-dried to obtain medicine-containing microsphere；
(4) after taking medicine-containing microsphere, lactose, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch premixing by weight ratio, two are added
Silica, magnesium stearate mixing, direct tablet compressing is up to the cefprozil tablet.
4. preparation method according to claim 3, it is characterised in that: the concentration of the Cefprozil aqueous solution is 15mg/
mL。
5. the preparation method according to claim 4, it is characterised in that: the emulsifier uses polyoxyethylene sorbitan monoleate.
6. preparation method according to claim 5, it is characterised in that: the rate of addition of lotion is in the step (3)
4mL/min。
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1843360A (en) * | 2006-05-24 | 2006-10-11 | 山东蓝金生物工程有限公司 | Slow release injection containing cefradine |
| CN102091044A (en) * | 2011-01-27 | 2011-06-15 | 海南美大制药有限公司 | Cefuroxime axetil lipid microsphere solid preparation |
| CN103417509A (en) * | 2013-08-15 | 2013-12-04 | 华北制药河北华民药业有限责任公司 | Cefprozil tablet and preparation method thereof |
| CN103524533A (en) * | 2013-10-10 | 2014-01-22 | 珠海金鸿药业股份有限公司 | Cefprozil compound, and dispersible tablets, dry suspension and preparation method thereof |
-
2018
- 2018-10-25 CN CN201811249881.5A patent/CN109010297A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1843360A (en) * | 2006-05-24 | 2006-10-11 | 山东蓝金生物工程有限公司 | Slow release injection containing cefradine |
| CN102091044A (en) * | 2011-01-27 | 2011-06-15 | 海南美大制药有限公司 | Cefuroxime axetil lipid microsphere solid preparation |
| CN103417509A (en) * | 2013-08-15 | 2013-12-04 | 华北制药河北华民药业有限责任公司 | Cefprozil tablet and preparation method thereof |
| CN103524533A (en) * | 2013-10-10 | 2014-01-22 | 珠海金鸿药业股份有限公司 | Cefprozil compound, and dispersible tablets, dry suspension and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 刘世芸: "白蛋白聚乳酸缓释微球的制备及体外释放研究", 《合肥工业大学学报(自然科学版)》 * |
| 方亮: "《药剂学》", 31 March 2016, 中国医药科技出版社 * |
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Application publication date: 20181218 |