CN1457782A - Dry spaxxacin suspension agent for resisting bacterial infection and its preparing method - Google Patents
Dry spaxxacin suspension agent for resisting bacterial infection and its preparing method Download PDFInfo
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- CN1457782A CN1457782A CN 03136149 CN03136149A CN1457782A CN 1457782 A CN1457782 A CN 1457782A CN 03136149 CN03136149 CN 03136149 CN 03136149 A CN03136149 A CN 03136149A CN 1457782 A CN1457782 A CN 1457782A
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Abstract
The present invention relates to a kind o dry Sparxacin suspension agent for resisting bacterial infection and its preparation process. The dry Sparxacin suspension agent is prepared with Sparxacin as active component and through adding stuffing, adsorbent, flow assistant, suspending agent, corrective, surfactant and lubricant. It has high Sparxacin digesting rate and is favorable to taking by old patient and patient with dysphagia.
Description
Technical field
The present invention relates to preparation of a kind of antimicrobial drug and preparation method thereof, specifically, is Sparfloxacin dry suspension and preparation method thereof.
Technical background
Sparfloxacin (Sparfloxacin) is the fluoroquinolone antibacterial agent that the big Japanese pharmaceutical Co. Ltd of Japan develops, it is to introduce amino on 5 of parent nucleus oxidation chinoline backbone, this medicine is strengthened than the antibacterial activity of other fluoroquinolone antibacterial agents to gram positive bacteria, go up fluoridize for 6 and 8, have 3 on 7,5-lupetazin base makes this medicine weaken interaction with fenbufen, theophylline, probenecid.Change through said structure, its bioavailability is improved, half-life prolongs, strengthened antibacterial activity, streptococcus pneumoniae, mycoplasma, chlamydia, legionella pneumophilia, tubercule bacillus and non-type acid-fast bacilli etc. a little less than the existing fluoroquinolone antimicrobial drug effect have also been shown very strong antibacterial efficacy gram positive bacteria and negative bacterium.The oral metenteron of this product absorbs good, and tissue distribution is wide, and the cell intrinsic permeability is strong, eliminates long half time.Only need take medicine once, and just can bring into play the effect of the various bacterial infections of effective treatment in one day.
1. pharmacological experiments shows: Sparfloxacin is a broad spectrum antibiotic, and gram-positive bacteria is comprised that staphylococcus aureus, staphylococcus epidermidis, micrococcus scarlatinae, streptococcus pneumoniae, enterococcus faecalis have obvious antibacterial action; Gram-negative bacteria escherichia coli, Klebsiella, Salmonella, Shigella, vibrio parahaemolytious, Proteus, Enterobacter, Rhodopseudomonas, acinetobacter, neisseria (Diplococcus gonorrhoeae etc.) also had the excellent antibiotic effect.This product also comprises that to mycoplasma, chlamydia, legionella, anaerobe bacteroides fragilis and Mycobacterium also have the excellent antibiotic effect.
The mechanism of action of Sparfloxacin is to play bactericidal action by the effect that suppresses the DNA gyrase in the DNA of bacteria building-up process.
2. antibacterial activity research
2.1 the antibacterial activity in vitro Sparfloxacin has a broad spectrum antibiotic activity external.It relatively sees table 1 for details with similar medicine.
2.2.1 gram positive bacteria Sparfloxacin most important character is the antibacterial activity enhancing to gram positive bacteria.It is to the MIC of PSSA, MSSA
90SBe respectively 0.125～0.25 and 0.06～0.125mg/L, antibacterial activity is ciprofloxacin, ofloxacin 8～16 times, 2～8 times of levofloxacins, and 32～128 times of norfloxacin slightly are inferior to trovafloxacin; MIC to MRSA
90SBe 8～16mg/L, similar to levofloxacin, its antibacterial activity is ciprofloxacin, ofloxacin 2～4 times, and 4～8 times of norfloxacin are slightly poorer than trovafloxacin.MIC to micrococcus scarlatinae
90SBe 0.25～0.5mg/L, its antibacterial activity and trovafloxacin are close, slightly are better than levofloxacin, are 2～8 times of ciprofloxacin, ofloxacin and norfloxacin 4～16 times.MIC to streptococcus pneumoniae
90SBe 0.125～0.5mg/L, its antibacterial activity is consistent with trovafloxacin, is 4～8 times of levofloxacin, ciprofloxacin, ofloxacin 8～16 times, 64～128 times of norfloxacin.
2.1.2 the gram-negative bacteria Sparfloxacin is to the antibacterial activity and the trovafloxacin basically identical of most gram-negative bacterias, be slightly poorer than ciprofloxacin, slightly be better than levofloxacin, and being better than ofloxacin, norfloxacin, it all shows very strong antibacterial activity to hemophilus influenza and moraxelle catarrhalis, Salmonella, Shigella.
To legionella pneumophilia, the MIC of Sparfloxacin and trovafloxacin
90SBeing 0.015mg/L, is 1/2 of ciprofloxacin, ofloxacin, levofloxacin, norfloxacin; To Aeromonas hydrophila, campylobacter jejuni, the antibacterial activity and the trovafloxacin of Sparfloxacin are approaching, are ciprofloxacin, ofloxacin, levofloxacin 2～8 times, are 8～64 times of norfloxacin.
2.1.3 the anaerobe Sparfloxacin is to the MIC of bacteroides fragilis
90SBe 1～4mg/L, its antibacterial activity is apparently higher than ciprofloxacin, ofloxacin, levofloxacin, and for norfloxacin 64～128 times slightly are inferior to trovafloxacin.Antibacterial activity to the bacillus perfringens Sparfloxacin is better than ciprofloxacin, ofloxacin, levofloxacin and norfloxacin.
2.1.4 mycoplasma, chlamydia and mycobacteria be to mycoplasma pneumoniae, the MIC of Sparfloxacin
90SBe 0.125～0.25mg/L, its sensitivity be better than ciprofloxacin (0.78～2mg/L), the husky star of fluorine oxygen (0.78～2mg/L), but be weaker than erythromycin and clarithromycin (0.06mg/L); To chlamydia trachomatis (MIC
90SBe that 0.03～0.125mg/L) activity is respectively ciprofloxacin, ofloxacin 16～32 times, 2～4 times of erythromycin; MIC to mycobacterium tuberculosis
90SBe 0.5mg/L, obviously be better than ciprofloxacin (1～4mg/L), ofloxacin (0.5～3mg/L), norfloxacin (2～8mg/L).
2.2 the antibacterial activity in vivo Sparfloxacin is to the ED of staphylococcus aureus, micrococcus scarlatinae, streptococcus pneumoniae infection mice
50Be respectively 0.828,3.36 and 6.31mg/kg, its activity in vivo is 5～10 times of ciprofloxacin, 3～7 times of ofloxacin, 12～39 times of enoxacin, 33～56 times of norfloxacin.
Sparfloxacin is 0.478 and 1.57mg/kg to the ED50 of escherichia coli, charrin disease mice, and its activity in vivo is 1～2 times of ciprofloxacin, 2～4 times of ofloxacin, 5 times of enoxacin, 10～11 times of norfloxacin.The mouse lung that Klebsiella Pneumoniae and Pseudomonas aeruginosa are caused infects its ED
50Be respectively 1.61 and 2.86mg/kg, its activity in vivo is ciprofloxacin, ofloxacin 2～3 times.
To the mice of mycoplasma pneumoniae, chlamydia infection, the activity in vivo of Sparfloxacin is similar to erythromycin, is better than ciprofloxacin, OFLOXACIN ﹠ LEVOFLOXACIN.
2.3 post antibiotic effect post antibiotic effect (PAE) is meant that the antibacterial short burst is exposed to that its growth continues repressed biological effect after the antibacterials.PAE and open-assembly time, antibacterials concentration are proportionate.The PAE that staphylococcus aureus was produced by the 2mg/L effect of Sparfloxacin in 15,30,60 minutes was respectively 52.6 ± 2.0,36.5 ± 4.1,51.0 ± 5.3 minutes.
2.4 empty the dashing forward of drug resistance DNA gyrase A subunit is that antibacterial is to the drug-fast main mechanism of Sparfloxacin.Antibacterial reduces the permeability of medicine, thus lower accumulate in the born of the same parents concentration be the Sparfloxacin drug resistance and with the reason of other class antimicrobial drug crossing drug resistants.Staphylococcus aureus and various gram-negative bacteria are to the drug-fast spontaneous mutation rate of Sparfloxacin＜10
-9, this be MRSA to other fluoroquinolones drug resistances, still keep reason to the Sparfloxacin sensitivity.But existing report confirms the staphylococcus aureus of anti-Sparfloxacin and exists, and owing to crossing drug resistant, MRSA, the streptococcus pneumoniae of anti-Sparfloxacin also are on the increase.
3. toxicologic study mice, rat are pressed the oral Sparfloxacin of body surface area, and dosage is 3.5～6.2 times of human dosage (400mg), in totally 104 weeks, does not see carcinogenesis.Sparfloxacin is not seen mutagenic action to salmonella strain TA98, TA100, TA1535, TA1537 and large intestine dust bacterial strain WP2, but salmonella strain TA102 is had mutagenic action, can cause escherichia coli dna repairing arrangement; Can cause that Chinese Mus pneumonocyte chromosome is not normal under the cell in vitro poison concentration.The male and female rat is 15.4 times of human dosage (400mg) by the oral Sparfloxacin of body surface area, and its fertility, reproductivity are not had obvious influence.
Table 1. Sparfloxacin and similar medicine to the antibacterial action of clinical common pathogenic bacteria (MICs, mg/L)
| Antibacterial | Antibacterial activity | Sparfloxacin | Ciprofloxacin | Ofloxacin | Levofloxacin | Norfloxacin | Trovafloxacin |
| Responsive staphylococcus aureus (PSSA) MSSA (MSSA) methicillin-resistant staphylococcus aureus (MRSA) methicillin-sensitivity MRSE (MSSE) methicillin resistance MRSE (MRSE) micrococcus scarlatinae of gram positive bacteria penicillin streptococcus pneumonia enterococcus faecalis G-group streptococcus Listeria monocytogenes gram-negative bacteria Klebsiella Proteus EHEC enterobacter cloacae clostridium perfringen enterobacter agglomerans takes labor ground other pseudomonad legionella pneumophilia Aeromonas hydrophila campylobacter jejuni NEISSERIA GONORRHOEAE Neisseria meningitidis anaerobic bacteria bacteroides fragilis Bacillus perfringens Bacillus cereus clostridium of citrobacter serratia marcesens acinetobacter calcoaceticus Salmonella Shigella haemophilus influenzae moraxelle catarrhalis pseudomonas aeruginosa | ??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 50S??MIC 90S??MIC 90S??MIC 90S??MIC 50S??MIC 90S | ?0.06 ?0.125～0.25 ?0.03～0.06 ?0.06～0.125 ?1～8 ?8～16 ?0.125 ?4 ?4～8 ?8～16 ?0.25 ?0.25～0.5 ?0.125～0.25 ?0.125～0.5 ?0.25～0.5 ?0.25～32 ?0.125～0.25 ?0.125～0.5 ?0.125～0.25 ?0.125～0.5 ?0.015～0.06 ?0.06～1 ?0.125～0.25 ?0.25～0.5 ?0.015～0.06 ?0.25～32 ?0.008～0.03 ?0.03～8 ?0.03 ?0.06～2 ?0.06 ?0.125 ?0.06 ?0.25 ?0.125～0.25 ?0.5～4 ?0.008～0.06 ?0.03～16 ?0.03～0.06 ?0.03～0.5 ?0.015 ?0.015～0.03 ?0.004～0.015 ?0.004～0.03 ?0.015～0.06 ?0.03～0.25 ?1～8 ?2～32 ?0.125～1 ?0.5～16 ?0.015 ?0.015 ?0.06 ?0.5 ?0.06 ?0.125 ?0.001 ?0.001 ?0.001～0.004 ?0.001～0.016 ?1 ?1～4 ?≤0.06～0.25 ?- ?0.06 ?0.12 ?- ?0.5～8 | ?0.25～0.5 ?1～2 ?0.25～0.5 ?0.5～2 ?8 ?32～64 ?0.5 ?32 ?8 ?32～64 ?0.25～1 ?0.5～4 ?0.5～4 ?1～4 ?0.5～2 ?1～64 ?0.5～4 ?1～4 ?0.5～4 ?1～4 ?0.015～0.06 ?0.03～2 ?0.03～0.06 ?0.03～0.06 ?0.015～0.03 ?0.25～32 ?0.015～0.03 ?0.06～8 ?0.015 ?0.06～8 ?0.015 ?0.03 ?0.03 ?0.06 ?0.06 ?0.125～4 ?0.06～0.5 ?0.25～256 ?0.015～0.03 ?0.03～0.25 ?0.008～0.015 ?0.008～0.03 ?0.008～0.03 ?0.008～0.03 ?0.06 ?0.06～2 ?0.25～2 ?1～16 ?0.06～0.5 ?0.5～8 ?0.015 ?0.03 ?0.125 ?1 ?0.25 ?1 ?0.001 ?0.001 ?0.004～0.016 ?0.004～0.03 ?2～8 ?4～64 ?0.25～2 ?- ?0.12 ?0.25 ?- ?4～32 | ?0.25～1 ?1～2 ?0.125～0.5 ?0.5～1 ?4～16 ?16～32 ?0.5 ?16 ?8 ?32～64 ?1～2 ?1～8 ?1～4 ?1～8 ?2 ?2～64 ?1～4 ?1～8 ?1～4 ?1～8 ?0.06～0.125 ?0.25～4 ?0.015～0.06 ?0.125～0.25 ?0.06～0.125 ?0.5～32 ?0.015～0.125 ?0.06～16 ?0.125 ?0.25～8 ?0.125 ?0.5 ?0.25 ?1 ?0.25 ?0.5～8 ?0.125～0.5 ?0.5～32 ?0.03～0.125 ?0.03～0.25 ?0.03 ?0.03 ?0.03～0.06 ?0.03 ?0.125～0.25 ?0.125～2 ?2～4 ?4～32 ?0.5～2 ?2～32 ?0.03 ?0.03 ?0.25 ?2 ?0.25 ?0.5 ?0.015 ?0.03～0.08 ?0.06 ?0.06 ?4 ?3.13～50 ?1～2 ?- ?0.12 ?0.25 ?- ?4～16 | ?0.25 ?0.25～1 ?0.06～0.25 ?0.25～0.5 ?2～4 ?8～16 ?0.25 ?4 ?4 ?16 ?0.5 ?0.5～2 ?0.5～1 ?1～2 ?1 ?1～64 ?0.5～1 ?1～2 ?0.5～1 ?1～2 ?0.03～0.006 ?0.125～2 ?0.015～0.06 ?0.06～0.125 ?0.03 ?0.25～16 ?0.008～0.03 ?0.06～8 ?0.03 ?0.06～4 ?0.06 ?0.125 ?0.125 ?0.25 ?0.06～0.125 ?0.125～4 ?0.06～0.5 ?0.25～32 ?0.015～0.06 ?0.03～0.125 ?0.015 ?0.03 ?0.015 ?0.03 ?0.06 ?0.125～1 ?0.5～1 ?2～32 ?0.125～1 ?1～16 ?0.015 ?0.03 ?0.125 ?1 ?0.25 ?0.25 ?- ?- ?0.008 ?0.008 ?2 ?2～12.5 ?0.125～1 ?- ?0.12 ?2 ?- ?2 | 0.5～2 4～16 0.5～2 2～16 32～64 32～128 1 32 32～64 32～128 2～4 8～16 8～32 16～32 4 32～64 8～32 16～32 8～32 16～32 0.06～0.125 0.125～8 0.06～0.125 0.125～0.25 0.06～0.125 0.25～32 0.125 4～32 0.06 0.25～32 0.125 0.25 0.125 0.5 0.125 0.25～8 0.5～2 8 0.03～0.25 0.03～0.5 0.015 0.03 0.015 0.03 0.25 0.25 1～2 16 1～4 4～32 0.03 0.03 0.06 4 8 0.015 0.06～0.1 0.06 0.125 32 128～＞256 2～8 - 0.5 2 - - | ?0.008～0.06 ?0.06～0.125 ?0.008～0.03 ?0.5～2 ?0.25～4 ?1～16 ?0.06 ?4 ?1～8 ?4～64 ?0.06～0.125 ?0.06～1 ?0.06～0.25 ?0.125～0.5 ?0.25～1 ?0.125～16 ?0.06～0.25 ?0.125～0.5 ?0.06～0.25 ?0.125～0.5 ?0.015～0.125 ?0.06～2 ?0.125～0.25 ?0.25～0.5 ?0.015～0.03 ?0.25～0.5 ?0.015～0.03 ?1～8 ?0.03 ?0.06～16 ?0.03 ?0.06 ?0.06 ?0.25 ?0.25 ?0.25～4 ?0.008～0.06 ?0.03～16 ?0.03～0.125 ?0.06～1 ?0.015 ?0.03 ?0.015 ?0.03 ?0.015～0.125 ?0.015～0.5 ?0.5～8 ?2～32 ?0.125～1 ?1～8 ?0.015 ?0.015 ?0.25 ?0.25 ?0.06 ?0.125 ?0.001 ?0.001 ?0.001 ?0.001 ?0.25～1 ?0.25～2 ?- ?- ?0.03 ?0.12 ?- ?- |
Summary of the invention
The objective of the invention is by making the method for Sparfloxacin dry suspension, gerontal patient and dysphagia patients are taken medicine conveniently, improve dissolution rate, give full play to the effect of Sparfloxacin treatment bacterial infection.
For achieving the above object, the present invention adopts following technical scheme: being active component with the Sparfloxacin, is the dry suspension that pharmaceutical formulation is made with filler, adsorbent, fluidizer, suspensoid and/or suspending agent, correctives, surfactant, lubricant.
The active component Sparfloxacin of Sparfloxacin dry suspension of the present invention, its English Sparfloxacin by name, chemical name is 5-amino-1-cyclopropyl-7-(cis-3,5-dimethyl-1-piperazinyl)-6,8-two fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid, structural formula is
Molecular formula is C
19H
22F
2N
4O
3, molecular weight: 392.41.
The used filler of Sparfloxacin dry suspension prescription of the present invention includes but not limited to low-substituted hydroxypropyl cellulose, lactose, sucrose, glucose, mannitol, xylitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, calcium phosphate, calcium carbonate, calcium bicarbonate, starch, carboxymethyl starch, pregelatinized Starch, microcrystalline Cellulose etc.
The used fluidizer of Sparfloxacin dry suspension prescription of the present invention includes but not limited to micropowder silica gel.
The used lubricant of Sparfloxacin dry suspension prescription of the present invention includes but not limited to magnesium stearate, calcium stearate, zinc stearate, Pulvis Talci, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, Polyethylene Glycol 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, sodium chloride, enuatrol, triacetyl glycerine, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium chloride, sodium laurylsulfate, magnesium laurylsulfate etc.
The used adsorbent of Sparfloxacin dry suspension prescription of the present invention includes but not limited to micropowder silica gel, crospolyvinylpyrrolidone, micropowder silica gel, Kaolin, basic magnesium carbonate, light magnesium oxide, aluminium hydroxide desiccant gel etc.
The used surfactant of Sparfloxacin dry suspension prescription of the present invention comprises but is not limited to sodium lauryl sulphate, poloxamer, Tween 80, bromination hexadecane trimethylamine, sodium laurylsulfate, stearyl alcohol sodium sulfonate, polyoxyethylene high fatty alcohol, sucrose ester, sorbitol fatty ester, soybean phospholipid etc.
The used correctives of Sparfloxacin dry suspension prescription of the present invention includes but not limited to steviosin, fructose, glucose, high fructose syrup, Mel, aspartame, protein sugar, xylitol, mannitol, lactose, sorbitol, maltose alcohol, glycyrrhizin, phyllodulcin, Sodium Cyclamate, flavoring banana essence, flavoring pineapple essence, Fructus Citri tangerinae essence, Herba Menthae essence, Fructus Foeniculi, vanillin, Fructus Citri Limoniae essence, cherry essence, rose essence etc.
Used suspensoid and/or the suspending agent of Sparfloxacin dry suspension prescription of the present invention includes but not limited to crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, the poly-ethoxy ethanol of hot phenoxy group, alevaire, the sorbitol anhydride polyethylene glycol monooleate, polyoxyethylene monostearate, polyoxyethylene deriv, Tween 80, the polyoxyethylene alkylphenyl sodium sulfonate, sodium lauryl sulfate, arabic gum, polyvinylpyrrolidone, the tragakanta, pectin, gelatin, carboxymethyl cellulose, methylcellulose, sodium carboxymethyl cellulose, guar gum, micropowder silica gel, Magnesiumaluminumsilicate, hydroxyethyl-cellulose, Kaolin, sodium alginate, kieselguhr, aluminium hydroxide etc.
Described Sparfloxacin dry suspension preparation method is crossed 80 mesh sieves after getting Sparfloxacin and adjuvant drying, pulverizing, with the equivalent incremental method with active component and filler, adsorbent, fluidizer, suspensoid and/or suspending agent, correctives, surfactant, the abundant mix homogeneously of lubricant, packing, promptly.
Below through detecting explanation beneficial effect of the present invention:
One, detects index and method
Dissolution detects sample thief, and according to dissolution method (two appendix XC first methods of Chinese Pharmacopoeia version in 2000), 1000ml is a solvent with acetic acid-sodium-acetate buffer (pH4.5), rotating speed is that per minute 100 changes, operation in the time of 45 minutes, is got solution 10ml in accordance with the law, filter, precision is measured subsequent filtrate 3ml, puts in the 50ml measuring bottle, is diluted to scale with the sodium hydroxide solution of 0.1mol/L, shake up, as need testing solution; Other the Sparfloxacin reference substance that is dried to constant weight of learning from else's experience 105 ℃ is an amount of, with the dissolving of 0.1mol/L sodium hydroxide solution and quantitatively dilution make the solution that contains 6 μ g among every 1ml approximately, product solution in contrast.Get above-mentioned two kinds of solution,, measure trap respectively, calculate every stripping quantity, promptly at the wavelength place of 291nm according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A).
Two, Sparfloxacin sheet (commercially available ordinary tablet) dissolution testing result: 83.6%
Three, example 1 sample dissolution testing result: 98.9%.
Four, example 2 sample dissolution testing results: 99.1%.
Five, example 3 sample dissolution testing results: 97.9%.
The specific embodiment
One, example 1
Sparfloxacin 100g
Micropowder silica gel 600g
Carboxymethyl starch sodium 100g
Microcrystalline Cellulose 100g
Polyvinylpyrrolidone 20g
Crospolyvinylpyrrolidone 20g
Lactose 50g
Steviosin 10g
Magnesium stearate is an amount of
Make 1000 bags
Two, example 2
Sparfloxacin 100g
Polyvinylpyrrolidone 120g
Hydroxypropyl emthylcellulose 40g
Carboxymethyl starch sodium 140g
Steviosin 5g
Magnesium oxide 10g
Micropowder silica gel 20g
Essence 1g
Mannitol adds to 1000g
Magnesium stearate is an amount of
Make 1000 bags
Three, example 3
Sparfloxacin 100g
Steviosin 50g
Hydroxypropyl emthylcellulose 20g
Micropowder silica gel 20g
Essence 10g
Mannitol adds to 1000g
Magnesium stearate is an amount of
Make 1000 bags
The preparation method of above-mentioned example:
Get Sparfloxacin and adjuvant drying, pulverize the back and cross 80 mesh sieves, with the equivalent incremental method with active component and filler, adsorbent, fluidizer, suspensoid and/or suspending agent, correctives, surfactant, the abundant mix homogeneously of lubricant, packing, promptly.
Claims (10)
1. the Sparfloxacin dry suspension is filled a prescription and preparation method thereof, it is characterized in that: it is to be active component with the antibacterials Sparfloxacin, is the dry suspension that pharmaceutical formulation is made with filler, adsorbent, fluidizer, suspensoid and/or suspending agent, correctives, surfactant, lubricant.
2. the active component Sparfloxacin of Sparfloxacin dry suspension according to claim 1, its English name Sparfloxacin, chemical name are 5-amino-1-cyclopropyl-7-(cis-3,5-2 methyl isophthalic acid-piperazinyl)-6,8-two fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid, structural formula is
Molecular formula is C
19H
22F
2N
4O
3, molecular weight: 392.41.
3. the filler in the Sparfloxacin dry suspension pharmaceutical formulation according to claim 1 includes but not limited to low-substituted hydroxypropyl cellulose, lactose, sucrose, glucose, mannitol, xylitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, calcium phosphate, calcium carbonate, calcium bicarbonate, starch, carboxymethyl starch, pregelatinized Starch, microcrystalline Cellulose etc.
4. the fluidizer in the Sparfloxacin dry suspension pharmaceutical formulation according to claim 1 includes but not limited to micropowder silica gel.
5. the lubricant in the Sparfloxacin dry suspension pharmaceutical formulation according to claim 1 includes but not limited to magnesium stearate, calcium stearate, zinc stearate, Pulvis Talci, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, Polyethylene Glycol 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, sodium chloride, enuatrol, triacetyl glycerine, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium chloride, sodium laurylsulfate, magnesium laurylsulfate etc.
6. the adsorbent in the Sparfloxacin dry suspension pharmaceutical formulation according to claim 1 includes but not limited to micropowder silica gel, crospolyvinylpyrrolidone, micropowder silica gel, Kaolin, basic magnesium carbonate, light magnesium oxide, aluminium hydroxide desiccant gel etc.
7. the surfactant in the Sparfloxacin dry suspension pharmaceutical formulation according to claim 1 comprises but is not limited to sodium lauryl sulphate, poloxamer, Tween 80, bromination hexadecane trimethylamine, sodium laurylsulfate, stearyl alcohol sodium sulfonate, polyoxyethylene high fatty alcohol, sucrose ester, sorbitol fatty ester, soybean phospholipid etc.
8. the correctives in the Sparfloxacin dry suspension pharmaceutical formulation according to claim 1 includes but not limited to steviosin, fructose, glucose, high fructose syrup, Mel, aspartame, protein sugar, xylitol, mannitol, lactose, sorbitol, maltose alcohol, glycyrrhizin, phyllodulcin, Sodium Cyclamate, flavoring banana essence, flavoring pineapple essence, Fructus Citri tangerinae essence, Herba Menthae essence, Fructus Foeniculi, vanillin, Fructus Citri Limoniae essence, cherry essence, rose essence etc.
9. suspensoid and/or suspending agent in the Sparfloxacin dry suspension pharmaceutical formulation according to claim 1 include but not limited to crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, the poly-ethoxy ethanol of hot phenoxy group, alevaire, the sorbitol anhydride polyethylene glycol monooleate, polyoxyethylene monostearate, polyoxyethylene deriv, Tween 80, the polyoxyethylene alkylphenyl sodium sulfonate, sodium lauryl sulfate, arabic gum, polyvinylpyrrolidone, the tragakanta, pectin, gelatin, carboxymethyl cellulose, methylcellulose, sodium carboxymethyl cellulose, guar gum, micropowder silica gel, Magnesiumaluminumsilicate, hydroxyethyl-cellulose, Kaolin, sodium alginate, kieselguhr, aluminium hydroxide etc.
10. Sparfloxacin dry suspension preparation method according to claim 1, it is characterized in that: cross 80 mesh sieves after getting Sparfloxacin and adjuvant drying, pulverizing, with the equivalent incremental method with active component and filler, adsorbent, fluidizer, suspensoid and/or suspending agent, correctives, surfactant, the abundant mix homogeneously of lubricant, packing, promptly.
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| CN 03136149 CN1457782A (en) | 2003-05-17 | 2003-05-17 | Dry spaxxacin suspension agent for resisting bacterial infection and its preparing method |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03136149 Pending CN1457782A (en) | 2003-05-17 | 2003-05-17 | Dry spaxxacin suspension agent for resisting bacterial infection and its preparing method |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100339072C (en) * | 2005-12-28 | 2007-09-26 | 严洁 | Methocarbamol dry mixing suspension |
| CN100441194C (en) * | 2004-03-03 | 2008-12-10 | 复旦大学 | Erigeron breviscapus extraction dry suspensoid agent |
| CN101559074B (en) * | 2009-06-01 | 2011-03-30 | 天津市挑战生物技术有限公司 | Coccidiostat-decoquinate dry suspension for livestock and poultry and preparation method thereof |
| CN1903176B (en) * | 2006-08-08 | 2011-07-13 | 江苏济川制药有限公司 | Dry suspensoid of Repirinast and its prepn. method |
| CN102614129A (en) * | 2012-04-16 | 2012-08-01 | 武汉回盛生物科技有限公司 | Enrofloxacin dry suspension |
| CN113980889A (en) * | 2021-11-03 | 2022-01-28 | 复旦大学附属中山医院 | Medicinal preparation for resisting intracellular mycoplasma infection and application thereof |
-
2003
- 2003-05-17 CN CN 03136149 patent/CN1457782A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100441194C (en) * | 2004-03-03 | 2008-12-10 | 复旦大学 | Erigeron breviscapus extraction dry suspensoid agent |
| CN100339072C (en) * | 2005-12-28 | 2007-09-26 | 严洁 | Methocarbamol dry mixing suspension |
| CN1903176B (en) * | 2006-08-08 | 2011-07-13 | 江苏济川制药有限公司 | Dry suspensoid of Repirinast and its prepn. method |
| CN101559074B (en) * | 2009-06-01 | 2011-03-30 | 天津市挑战生物技术有限公司 | Coccidiostat-decoquinate dry suspension for livestock and poultry and preparation method thereof |
| CN102614129A (en) * | 2012-04-16 | 2012-08-01 | 武汉回盛生物科技有限公司 | Enrofloxacin dry suspension |
| CN102614129B (en) * | 2012-04-16 | 2013-12-11 | 武汉回盛生物科技有限公司 | Enrofloxacin dry suspension |
| CN113980889A (en) * | 2021-11-03 | 2022-01-28 | 复旦大学附属中山医院 | Medicinal preparation for resisting intracellular mycoplasma infection and application thereof |
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