CN1562067A - Azithromycin oral disintegration tablet and its preparing method - Google Patents
Azithromycin oral disintegration tablet and its preparing method Download PDFInfo
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- CN1562067A CN1562067A CN 200410030577 CN200410030577A CN1562067A CN 1562067 A CN1562067 A CN 1562067A CN 200410030577 CN200410030577 CN 200410030577 CN 200410030577 A CN200410030577 A CN 200410030577A CN 1562067 A CN1562067 A CN 1562067A
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- agent
- azithromycin
- water
- orally disintegrating
- disintegrating tablets
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Links
- 229960004099 azithromycin Drugs 0.000 title claims description 47
- MQTOSJVFKKJCRP-BICOPXKESA-N azithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 MQTOSJVFKKJCRP-BICOPXKESA-N 0.000 title claims description 47
- 238000000034 method Methods 0.000 title description 4
- 239000000945 filler Substances 0.000 claims abstract description 14
- 239000000080 wetting agent Substances 0.000 claims abstract description 13
- 239000000314 lubricant Substances 0.000 claims abstract description 11
- 239000000203 mixture Substances 0.000 claims description 31
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 30
- 239000003795 chemical substances by application Substances 0.000 claims description 20
- 239000006191 orally-disintegrating tablet Substances 0.000 claims description 20
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 19
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 19
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 19
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 19
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 17
- 235000019359 magnesium stearate Nutrition 0.000 claims description 15
- 239000000463 material Substances 0.000 claims description 15
- YTBSYETUWUMLBZ-UHFFFAOYSA-N D-Erythrose Natural products OCC(O)C(O)C=O YTBSYETUWUMLBZ-UHFFFAOYSA-N 0.000 claims description 14
- 206010056474 Erythrosis Diseases 0.000 claims description 14
- 239000003814 drug Substances 0.000 claims description 14
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 13
- YTBSYETUWUMLBZ-IUYQGCFVSA-N D-erythrose Chemical compound OC[C@@H](O)[C@@H](O)C=O YTBSYETUWUMLBZ-IUYQGCFVSA-N 0.000 claims description 12
- 239000011230 binding agent Substances 0.000 claims description 12
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 6
- 229930195725 Mannitol Natural products 0.000 claims description 6
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 6
- 239000000594 mannitol Substances 0.000 claims description 6
- 235000010355 mannitol Nutrition 0.000 claims description 6
- 210000000214 mouth Anatomy 0.000 claims description 6
- 239000011734 sodium Substances 0.000 claims description 5
- 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 claims description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 4
- 229910052708 sodium Inorganic materials 0.000 claims description 4
- 230000001476 alcoholic effect Effects 0.000 claims description 3
- -1 alkane ketone Chemical class 0.000 claims description 3
- KAESVJOAVNADME-UHFFFAOYSA-N 1H-pyrrole Natural products C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 2
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 claims description 2
- 235000010980 cellulose Nutrition 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- 229920003020 cross-linked polyethylene Polymers 0.000 claims description 2
- 239000004703 cross-linked polyethylene Substances 0.000 claims description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 2
- 239000002002 slurry Substances 0.000 claims description 2
- 239000000600 sorbitol Substances 0.000 claims description 2
- 235000010356 sorbitol Nutrition 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 239000000811 xylitol Substances 0.000 claims description 2
- 235000010447 xylitol Nutrition 0.000 claims description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 2
- 229960002675 xylitol Drugs 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims 1
- 239000007884 disintegrant Substances 0.000 abstract description 2
- 239000000853 adhesive Substances 0.000 abstract 1
- 230000001070 adhesive effect Effects 0.000 abstract 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 45
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 28
- 238000002360 preparation method Methods 0.000 description 16
- 108010011485 Aspartame Proteins 0.000 description 15
- 239000000605 aspartame Substances 0.000 description 15
- 235000010357 aspartame Nutrition 0.000 description 15
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 15
- 229960003438 aspartame Drugs 0.000 description 15
- NOOLISFMXDJSKH-UHFFFAOYSA-N p-menthan-3-ol Chemical compound CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 15
- 235000017557 sodium bicarbonate Nutrition 0.000 description 14
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 14
- 239000003826 tablet Substances 0.000 description 14
- 238000007689 inspection Methods 0.000 description 10
- YSXLJTGZMRNQSG-UHFFFAOYSA-L disodium;6-amino-5-[[2-[4-[2-[4-[2-[(2-amino-5-sulfonatonaphthalen-1-yl)diazenyl]phenyl]sulfonyloxyphenyl]propan-2-yl]phenoxy]sulfonylphenyl]diazenyl]naphthalene-1-sulfonate Chemical compound [Na+].[Na+].C1=CC=C2C(N=NC3=CC=CC=C3S(=O)(=O)OC3=CC=C(C=C3)C(C)(C=3C=CC(OS(=O)(=O)C=4C(=CC=CC=4)N=NC=4C5=CC=CC(=C5C=CC=4N)S([O-])(=O)=O)=CC=3)C)=C(N)C=CC2=C1S([O-])(=O)=O YSXLJTGZMRNQSG-UHFFFAOYSA-L 0.000 description 9
- 238000005303 weighing Methods 0.000 description 8
- 235000015165 citric acid Nutrition 0.000 description 7
- 239000002552 dosage form Substances 0.000 description 7
- 239000008187 granular material Substances 0.000 description 7
- 239000002245 particle Substances 0.000 description 7
- 239000011265 semifinished product Substances 0.000 description 7
- 239000000796 flavoring agent Substances 0.000 description 5
- 235000019634 flavors Nutrition 0.000 description 5
- 239000000047 product Substances 0.000 description 5
- 229960004106 citric acid Drugs 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000004744 fabric Substances 0.000 description 4
- 238000005469 granulation Methods 0.000 description 4
- 230000003179 granulation Effects 0.000 description 4
- 229960001407 sodium bicarbonate Drugs 0.000 description 4
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 235000013399 edible fruits Nutrition 0.000 description 3
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 3
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 2
- 238000004132 cross linking Methods 0.000 description 2
- 125000000770 erythrosyl group Chemical group C1([C@H](O)[C@H](O)CO1)* 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 230000000873 masking effect Effects 0.000 description 2
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 210000003296 saliva Anatomy 0.000 description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 2
- 235000019640 taste Nutrition 0.000 description 2
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 description 1
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- HTRWTTRXUXPGEY-UHFFFAOYSA-L C(C=CC(=O)[O-])(=O)[O-].[Na+].NCC(=O)O.[Na+] Chemical compound C(C=CC(=O)[O-])(=O)[O-].[Na+].NCC(=O)O.[Na+] HTRWTTRXUXPGEY-UHFFFAOYSA-L 0.000 description 1
- 101100273639 Carassius auratus ccna1 gene Proteins 0.000 description 1
- 241000606161 Chlamydia Species 0.000 description 1
- 208000019505 Deglutition disease Diseases 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 206010013911 Dysgeusia Diseases 0.000 description 1
- 241000167880 Hirundinidae Species 0.000 description 1
- 241000589248 Legionella Species 0.000 description 1
- 208000007764 Legionnaires' Disease Diseases 0.000 description 1
- 241000204031 Mycoplasma Species 0.000 description 1
- 102000002067 Protein Subunits Human genes 0.000 description 1
- 108010001267 Protein Subunits Proteins 0.000 description 1
- 206010057190 Respiratory tract infections Diseases 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- 206010062255 Soft tissue infection Diseases 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000003444 anaesthetic effect Effects 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 244000052616 bacterial pathogen Species 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 229940109275 cyclamate Drugs 0.000 description 1
- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- RRPFCKLVOUENJB-UHFFFAOYSA-L disodium;2-aminoacetic acid;carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O.NCC(O)=O RRPFCKLVOUENJB-UHFFFAOYSA-L 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
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- 239000001257 hydrogen Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 206010022000 influenza Diseases 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000003589 local anesthetic agent Substances 0.000 description 1
- 239000003120 macrolide antibiotic agent Substances 0.000 description 1
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- 229920003023 plastic Polymers 0.000 description 1
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- 229940085605 saccharin sodium Drugs 0.000 description 1
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- 235000015424 sodium Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
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Abstract
An oral disintegrating tablet of azimycin is prepared from azimycin, water-soluble filler, disintegrant, lubricant, and wetting agent or adhesive.
Description
Technical field
The present invention relates to a kind of Azithromycin orally disintegrating tablets and preparation method thereof.
Technical background
Azithromycin is a kind of macrolide antibiotics, by suppressing the synthetic antibacterial action that reaches of ribosome 50S protein subunit matter in the bacterial cell.Azithromycin can suppress multiple gram-positive cocci, mycoplasma, chlamydia and legionella pneumophilia, especially some important gram negative bacilli such as hemophilus influenza etc. is had good antibacterial activity.The clinical wide model of azithromycin is used for the treatment of respiratory tract infection, skin soft-tissue infection and urogenital infections.
The azithromycin structural formula is as follows
The dosage form of the azithromycin of clinical practice at present has conventional tablet, capsule, suspensoid, injection, granule etc., and how these peroral dosage forms need use water delivery service, and taking medicine for dysphagia or the inconvenient patient of water intaking has certain difficulty; Though granule is the dosage form that aims at the child patient design, owing to most children can not oneself take after mixing it with water, and it is also very inconvenient to take granule when school or kindergarten, so these dosage forms can't satisfy all patients' medication needs fully.
Summary of the invention
The object of the present invention is to provide a kind of novel form that can overcome the insufficient azithromycin of above-mentioned dosage form and preparation method thereof.
The present invention relates to a kind of Azithromycin orally disintegrating tablets, comprising the azithromycin of effective dose and can be in the oral cavity rapidly disintegrate discharge the pharmaceutically acceptable excipient of medicine.
Azithromycin orally disintegrating tablets contains principal agent azithromycin, water-soluble filler, disintegrating agent, lubricant, also contains wetting agent or binding agent.
Various main materials and auxiliary materials weight shares prescription in the total amount shared ratio as follows:
A, principal agent 5～50%
B, water-soluble filler 10～70%
C, disintegrating agent 10～50%
D, lubricant 0.5～5%
E, wetting agent or binding agent 1～10%
Water-soluble filler is selected from erythrose, mannitol, sorbitol, xylitol or other and helps the material of moisture penetration in the pharmaceutical preparation, or the mixture of above two or more material.
Disintegrating agent is selected from microcrystalline Cellulose (MCC), low-substituted hydroxypropyl cellulose (L-HPC), cross-linked carboxymethyl cellulose sodium (CCNa), crosslinked polyethylene pyrrole alkane ketone (PVPP), crosslinked carboxymethylstach sodium (CCMS-Na), or the mixture of above two or more material.
Can also contain gas-producing disintegrant in the above-mentioned disintegrating agent, as citric acid, tartaric acid, fumaric acid, sodium bicarbonate, sodium glycine carbonate, Glycine sodium fumarate or their mixture.
Lubricant can be selected magnesium stearate, Pulvis Talci or its mixture for use.
The optional water of wetting agent, ethanol, or the mixture of the two.
Binding agent can be selected starch slurry, polyvidone or various cellulose family for use, or the mixture of above two or more material.
For covering the bitterness of azithromycin, can also add the correctives that accounts for prescription gross weight 2～10% in the present invention, aspartame, cyclamate, saccharin sodium, Mentholum and various fruit powder essence etc. all can satisfy the requirement that improves the Azithromycin orally disintegrating tablets mouthfeel.
This dosage form adopts wet granulation technology, can use conventional tablet pharmaceutical equipment production.
Concrete preparation method is as described below:
Take by weighing azithromycin, water-soluble filler, correctives by 100 mesh sieves, add an amount of wetting agent or binding agent granulation behind the mix homogeneously, with all the other adjuvants and dried particles mix homogeneously, the qualified back of the inspection of semifinished product adds lubricant, and tabletting promptly behind the mixing.
The present invention runs in the oral cavity after the saliva rapidly that disintegrate becomes fine particle, and in order to investigate disintegrate effect of the present invention, we simulate oral environment and have formulated corresponding dissolve scattered time limit and molten shot degree algoscopy, and method is as follows:
The dissolve scattered time limit algoscopy is got this product a slice, put in the glass dish, getting the scale dropper measures 37 ℃ of water of 1ml and directly drips on unilateral, and the control rate of addition was finished timing simultaneously, inspection during to 45 seconds in 30 seconds, this product Ying Rong clears entirely, do not clear entirely as molten, get hard paper and scratch, hard core must not be arranged.
Molten shot degree algoscopy is got this product a slice, according to inspection technique disintegration (two appendix X of Chinese Pharmacopoeia version in 2000 A) lower device requirement, and hanging basket bottom screen cloth is replaced by 26 eye mesh screens, this product is put in the disintegration tester hanging basket, regulate the hanging basket height and make the bottom screen cloth concordant, and when this product contact water surface, pick up counting, in the time of 45 seconds with the water surface, mention the hanging basket inspection, should all pass through screen cloth.
According to said method the present invention and azithromycin ordinary tablet are checked that the present invention all can moltenly loose in 45 seconds and by screen cloth, ordinary tablet is all defective, disintegration time of the present invention is significantly shorter than ordinary tablet, compares with ordinary tablet, and this dosage form has the following advantage:
The first, disintegrate is rapid, and is rapid-action.The present invention can be in 45 seconds in mouth disintegrate fast, make the rapid stripping of medicine, compare with azithromycin conventional tablet or capsule, shortened dissolution time, accelerate its absorption, make medicine can bring into play the whole body therapeutic effect rapidly.
The second, drug absorption is abundant.The present invention before reaching gastrointestinal tract rapidly disintegrate also be dispersed into trickle granule, cause medicine to distribute in the gastrointestinal tract large tracts of land, absorption point increases, and absorbs more fully, so also helps improving bioavailability of medicament.
The 3rd, medication is convenient, good mouthfeel.The present invention needn't use water delivery service, saliva can make oral cavity disintegration tablet disintegrate or dissolving, both can resemble ordinary tablet swallows, can be placed in the water again and take after the disintegrate, also can need not to take medicine with water swallow, can take whenever and wherever possible, provide a great convenience condition, can guarantee that more medicine takes on time for the patient takes medicine.The present invention has refrigerant Herba Menthae and fruit aroma and does not have obvious abnormal flavour after taste masking is handled, no sand type, help improving the patient take medicine compliance.
The generation of above-mentioned effect be because, it is described: water-soluble fillers such as erythrose and mannitol orally-dissolvable rapidly, cool taste is sweet and tasty, to thermally-stabilised, non-hygroscopic, can increase the hardness of tablet, very little to the disintegrate influence, be the desirable filler of oral cavity disintegration tablet; Microcrystalline Cellulose plays dual parts to fill and disintegrate in this test recipe, it has spongiform porous tubular structured, during pressurized, loose structure is by disorderly and unsystematic and become linear array, plastic deformation in addition, make it meet water after, hydrone enters tablet inside, destroy the hydrogen bond between the crystallite, impel disintegration of tablet; Low-substituted hydroxypropyl cellulose L-HPC has good hygroscopicity, meets water-soluble expanding and microcrystalline Cellulose when being used, and can play the disintegrate effect of the best.Citric acid contacts low amounts of water with sodium bicarbonate just can produce a large amount of bubbles, has helped the disintegrate of tablet more; Mentholum has the bad flavor of smelling that local anesthetic action can masking agents because of it, and cool taste, share as correctives to reach the flavoring effect with sweeting agents such as aspartame and essence.
The specific embodiment
Azithromycin orally disintegrating tablets of the present invention contains principal agent, water-soluble filler, disintegrating agent, lubricant, also contains wetting agent or binding agent, the main materials and auxiliary materials weight share prescription in the total amount shared preferred proportion as follows:
A, principal agent 20～40%
B, water-soluble filler 20～50%
C, disintegrating agent 15～35%
D, lubricant 1～2%
E, wetting agent or binding agent 2～5%
Water-soluble filler is erythrose and mannitol preferably.
Disintegrating agent is microcrystalline Cellulose (MCC), low-substituted hydroxypropyl cellulose (L-HPC), citric acid and sodium bicarbonate preferably.
Correctives is aspartame, Mentholum and various fruit powder essence preferably.
Wetting agent or binding agent be the second alcohol and water preferably.
With following embodiment the present invention is described.
Embodiment 1: the preparation Azithromycin orally disintegrating tablets
The composition weight percentage by weight
Azithromycin 100g 33.3%
Mannitol 88g 29.3%
Aspartame 3g 1%
Mentholum 1g 0.4%
Chocolate powder essence 3g 1%
Water is an amount of
Low-substituted hydroxypropyl cellulose 18g 6%
Microcrystalline Cellulose 72g 24%
Citric acid 3g 1%
Sodium bicarbonate 9g 3%
Magnesium stearate 3g 1%
Gross weight 300g
Make 1000 altogether
Concrete preparation method is as described below:
Take by weighing azithromycin, mannitol, aspartame, Mentholum, chocolate powder essence by 100 mesh sieves; adding suitable quantity of water solution behind the mix homogeneously granulates; take by weighing by prescription and to add adjuvant low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, citric acid and sodium bicarbonate and dried particles mix homogeneously; the qualified back of the inspection of semifinished product adds magnesium stearate, and tabletting promptly behind the mixing.
Embodiment 2: the preparation Azithromycin orally disintegrating tablets
The composition weight percentage by weight
Azithromycin 100g 25%
Erythrose 125g 31.25%
Aspartame 4g 1%
Mentholum 1g 0.25%
Chocolate powder essence 8g 2%
50% ethanol is an amount of
Low-substituted hydroxypropyl cellulose 32g 8%
Microcrystalline Cellulose 96g 24%
Citric acid 6g 1.5%
Sodium bicarbonate 24g 6%
Magnesium stearate 4g 1%
Gross weight 400g
Make 1000 altogether
Concrete preparation method is as described below:
Take by weighing azithromycin, erythrose, aspartame, Mentholum, chocolate powder essence by 100 mesh sieves; adding an amount of 50% alcoholic solution behind the mix homogeneously granulates; with low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, citric acid and sodium bicarbonate and dried particles mix homogeneously; the qualified back of the inspection of semifinished product adds magnesium stearate, and tabletting promptly behind the mixing.
Embodiment 3: the preparation Azithromycin orally disintegrating tablets
The composition weight percentage by weight
Azithromycin 125g 31.25%
Erythrose 125g 31.25%
Aspartame 4g 1%
Mentholum 2g 0.5%
Chocolate powder essence 8g 2%
50% ethanol is an amount of
Polyvinylpolypyrrolidone 40g 10%
Microcrystalline Cellulose 80g 20%
Citric acid 8g 2%
Sodium bicarbonate 4g 1%
Magnesium stearate 4g 1%
Gross weight 400g
Make 1000 altogether
Concrete preparation method is as described below:
Take by weighing azithromycin, erythrose, aspartame, Mentholum, chocolate powder essence by 100 mesh sieves; add an amount of 50% alcohol granulation behind the mix homogeneously; with polyvinylpolypyrrolidone, microcrystalline Cellulose, citric acid and sodium bicarbonate and dried particles mix homogeneously; the qualified back of the inspection of semifinished product adds magnesium stearate, and tabletting promptly behind the mixing.
Embodiment 4: the preparation Azithromycin orally disintegrating tablets
The composition weight percentage by weight
Azithromycin 125g 31.25%
Erythrose 125g 31.25%
Aspartame 4g 1%
Mentholum 2g 0.5%
Chocolate powder essence 10g 2.5%
50% ethanol is an amount of
Cross-linking sodium carboxymethyl cellulose 30g 7.5%
Microcrystalline Cellulose 80g 20%
Citric acid 8g 2%
Sodium bicarbonate 8g 2%
Magnesium stearate 4g 1%
Pulvis Talci 4g 1%
Gross weight 400g
Make 1000 altogether
Concrete preparation method is as described below:
Take by weighing azithromycin, erythrose, aspartame, Mentholum, chocolate powder essence by 100 mesh sieves; add an amount of 50% alcohol granulation behind the mix homogeneously; with cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose, citric acid and sodium bicarbonate and dried particles mix homogeneously; the qualified back of the inspection of semifinished product adds magnesium stearate and Pulvis Talci, and tabletting promptly behind the mixing.
Embodiment 5: the preparation Azithromycin orally disintegrating tablets
The composition weight percentage by weight
Azithromycin 250g 41.67%
Erythrose 180g 30%
Aspartame 6g 1%
Mentholum 2g 0.33%
Fructus Citri sinensis powdered flavor 6g 1%
50% ethanol is an amount of
Low-substituted hydroxypropyl cellulose 40g 6.7%
Microcrystalline Cellulose 80g 13.3%
Citric acid 6g 1%
Sodium bicarbonate 24g 4%
Magnesium stearate 6g 1%
Gross weight 600g
Make 1000 altogether
Concrete preparation method is as described below:
Take by weighing azithromycin, erythrose, aspartame, Mentholum, chocolate powder essence by 100 mesh sieves; adding an amount of 50% alcoholic solution behind the mix homogeneously granulates; with low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, citric acid and sodium bicarbonate and dried particles mix homogeneously; the qualified back of the inspection of semifinished product adds magnesium stearate, and tabletting promptly behind the mixing.
Embodiment 6: the preparation Azithromycin orally disintegrating tablets
The composition weight percentage by weight
Azithromycin 250g 41.67%
Erythrose 150g 25%
Aspartame 6g 1%
Mentholum 2g 0.33%
Fructus Citri sinensis powdered flavor 6g 1%
50% ethanol is an amount of
Crosslinked carboxymethyl fecula sodium 40g 6.67%
Microcrystalline Cellulose 100g 16.67%
Citric acid 24g 4%
Sodium bicarbonate 12g 2%
Magnesium stearate 6g 1%
Pulvis Talci 4g 0.67%
Gross weight 600g
Make 1000 altogether
Concrete preparation method is as described below:
Take by weighing azithromycin, erythrose, aspartame, Mentholum, Fructus Citri sinensis powdered flavor by 100 mesh sieves; add an amount of 50% alcohol granulation behind the mix homogeneously; with crosslinked carboxymethyl fecula sodium, microcrystalline Cellulose, citric acid and sodium bicarbonate and dried particles mix homogeneously; the qualified back of the inspection of semifinished product adds magnesium stearate and Pulvis Talci, and tabletting promptly behind the mixing.
Claims (8)
1, a kind of Azithromycin orally disintegrating tablets, comprising the azithromycin of effective dose and can be in the oral cavity rapidly disintegrate discharge the pharmaceutically acceptable excipient of medicine.
2, according to the described Azithromycin orally disintegrating tablets of claim 1, it is characterized in that containing principal agent azithromycin, water-soluble filler, disintegrating agent, lubricant, also contain wetting agent or binding agent, each main materials and auxiliary materials weight share shared ratio in the prescription total amount is:
A, principal agent 5～50%
B, water-soluble filler 10～70%
C, disintegrating agent 10～50%
D, lubricant 0.5～5%
E, wetting agent or binding agent 1～10%.
3,, it is characterized in that main materials and auxiliary materials weight share shared ratio in the prescription total amount is according to the described Azithromycin orally disintegrating tablets of claim 2:
A, principal agent 20～40%
B, water-soluble filler 20～50%
C, disintegrating agent 5～25%
D, lubricant 1～2%
E, wetting agent or binding agent 2～5%.
4, according to claim 2 or 3 described Azithromycin orally disintegrating tablets, it is characterized in that water-soluble filler selects erythrose, mannitol, sorbitol or xylitol for use, or the mixture of above two or more material.
5, according to claim 2 or 3 described Azithromycin orally disintegrating tablets, it is characterized in that disintegrating agent selects microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, cross-linked carboxymethyl cellulose sodium, crosslinked polyethylene pyrrole alkane ketone or crosslinked carboxymethylstach sodium for use, or the mixture of above two or more material.
6, according to claim 2 or 3 described Azithromycin orally disintegrating tablets, it is characterized in that lubricant selects magnesium stearate or Pulvis Talci for use, or magnesium stearate and talcous mixture.
7, according to claim 2 or 3 described Azithromycin orally disintegrating tablets, it is characterized in that selecting for use wetting agent, is water or ethanol and wetting agent is selected for use, or water and alcoholic acid mixture.
8, according to claim 2 or 3 described Azithromycin orally disintegrating tablets, it is characterized in that selecting for use binding agent, is starch slurry, polyvidone or various cellulose family and binding agent is selected for use, or the mixture of above two or more material.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100305773A CN100490816C (en) | 2004-04-12 | 2004-04-12 | Azithromycin oral disintegration tablet and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100305773A CN100490816C (en) | 2004-04-12 | 2004-04-12 | Azithromycin oral disintegration tablet and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1562067A true CN1562067A (en) | 2005-01-12 |
| CN100490816C CN100490816C (en) | 2009-05-27 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100305773A Expired - Lifetime CN100490816C (en) | 2004-04-12 | 2004-04-12 | Azithromycin oral disintegration tablet and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100490816C (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100415243C (en) * | 2006-02-14 | 2008-09-03 | 山东诚创医药技术开发有限公司 | Composition of water soluble Azithromycin salt |
| CN101926774A (en) * | 2010-08-20 | 2010-12-29 | 安徽安科生物工程（集团）股份有限公司 | Azithromycin powder composite and preparation method thereof |
-
2004
- 2004-04-12 CN CNB2004100305773A patent/CN100490816C/en not_active Expired - Lifetime
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100415243C (en) * | 2006-02-14 | 2008-09-03 | 山东诚创医药技术开发有限公司 | Composition of water soluble Azithromycin salt |
| CN101926774A (en) * | 2010-08-20 | 2010-12-29 | 安徽安科生物工程（集团）股份有限公司 | Azithromycin powder composite and preparation method thereof |
| CN101926774B (en) * | 2010-08-20 | 2011-10-19 | 安徽安科生物工程（集团）股份有限公司 | Azithromycin powder composite and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN100490816C (en) | 2009-05-27 |
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