CN1836662A - Prulifloxacin compound preparation - Google Patents
Prulifloxacin compound preparation Download PDFInfo
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- CN1836662A CN1836662A CN 200610067185 CN200610067185A CN1836662A CN 1836662 A CN1836662 A CN 1836662A CN 200610067185 CN200610067185 CN 200610067185 CN 200610067185 A CN200610067185 A CN 200610067185A CN 1836662 A CN1836662 A CN 1836662A
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- Prior art keywords
- prulifloxacin
- pidotimod
- compound preparation
- treatment
- injection
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- 238000002360 preparation method Methods 0.000 title claims abstract description 22
- 229960001224 prulifloxacin Drugs 0.000 title claims description 41
- -1 Prulifloxacin compound Chemical class 0.000 title claims description 13
- PWNMXPDKBYZCOO-UHFFFAOYSA-N Prulifloxacin Chemical compound C1=C2N3C(C)SC3=C(C(O)=O)C(=O)C2=CC(F)=C1N(CC1)CCN1CC=1OC(=O)OC=1C PWNMXPDKBYZCOO-UHFFFAOYSA-N 0.000 claims description 31
- 229960001163 pidotimod Drugs 0.000 claims description 29
- UUTKICFRNVKFRG-WDSKDSINSA-N (4R)-3-[oxo-[(2S)-5-oxo-2-pyrrolidinyl]methyl]-4-thiazolidinecarboxylic acid Chemical compound OC(=O)[C@@H]1CSCN1C(=O)[C@H]1NC(=O)CC1 UUTKICFRNVKFRG-WDSKDSINSA-N 0.000 claims description 26
- 239000003814 drug Substances 0.000 claims description 9
- 239000007924 injection Substances 0.000 claims description 7
- 238000002347 injection Methods 0.000 claims description 7
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
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- 239000002671 adjuvant Substances 0.000 claims description 5
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- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
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Abstract
The compound prulifloxicin preparation is used in treating bacterial infectious diseases. The compound prulifloxicin preparation consists of prulifloxicin 50-600 mg, pidaomode 200-1600 mg and pharmaceutically acceptable supplementary material, and is prepared into various pharmaceutically acceptable preparation forms for treating bacterial infectious diseases clinically. It can raise body's immunity level to strengthen the exogenous bactericidal effect of prulifloxicin.
Description
Technical field
The present invention relates to a kind of Prulifloxacin compound preparation, be used for the treatment of bacterial infection disease.
Background technology
Prulifloxacin (Prulifloxacin) be by Japanese new drug company develop the 4th generation Comprecin, its chemistry is by name: 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1, the 3-Dioxol-4-yl) methyl isophthalic acid-piperazinyl]-4-oxo-4H-[1,3] the sulfur nitrogen heterocycle butane also [3,2-a] quinoline-3-carboxylic acid, molecular formula: C
21H
20FN
3O
6S, molecular weight: 461.46.Prulifloxacin has good pharmacokinetics and pharmacodynamic profile, has a broad antifungal spectrum, little, the difficult drug resistance that produces of side effect, and the clinical bacterial infection that is used for the treatment of has good curative effect.But in recent years, because antibiotic a large amount of uses cause the enhancing of bacterial drug resistance, clinical treatment bacterial infection the puzzlement of problems such as complexity, intractable and repeatability to occur.The patient that the while bacterial infection shows effect repeatedly goes back ubiquity and the low problem of immune level.According to immunologic studies show that of modern times, low immune level causes treatment cycle elongated, and bacterial drug resistance increases, and relies on exogenous antimicrobial drug to be not enough to reach pathogenic bacterium fully merely thoroughly to remove.
Pidotimod is a late nineteen eighties, and what synthesized by Italian Poli chemical industrial company is that a kind of endogenous is regulated medicine, has the body's immunity facilitation, can improve patient's immune level rapidly.Its chemistry (R)-3-[(S)-(5-oxygen-2-pyrrolidinyl) carbonyl by name]-Thiazolidine-4-carboxylic acid, molecular formula: C
9H
12N
2O
4S, molecular weight: 244.26.Pidotimod is a kind of high-purity dipeptides of synthetic, a kind of immunopotentiating agent, and it can promote nonspecific immune reaction to promote specific immune response again.Can strengthen the activate the phagocytic capacity of macrophage and neutrophilic granulocyte, improve its chemotaxis; Activate natural killer cell; The former lymphopoiesis that causes of mitosis promoting, the helper T lymphocyte that changes when making immunologic hypofunction (CD4) recovers normal with the ratio of suppressor T lymphocyte (CD8); By stimulating interleukin-2 and gamma interferon to promote cell immune response.Although all showing pidotimod, animal experiment and clinical trial do not have directly antibiotic and antiviral activity.
At present, also do not have prulifloxacin and pidotimod are united the report that is used for the treatment of bacterial infection disease, the inventor has carried out studying and a large amount of test to the synergism of these two kinds of medication combined application, gets the present invention eventually.
Summary of the invention
The object of the present invention is to provide a kind of compound preparation that can improve patient's immune level and exogenous kill bacteria by endogenous.
In order to realize purpose of the present invention, adopt following technical scheme: a kind of Prulifloxacin compound preparation, the composition characteristic of its active component is:
Prulifloxacin: 50-600mg
Pidotimod: 200-1600mg.
Form by above-mentioned active component, add the pharmaceutics acceptable auxiliary, can make any pharmaceutics acceptable forms.
Described adjuvant is selected from any one or a few in starch, microcrystalline Cellulose, sucrose, dextrin, lactose, Icing Sugar, glucose, sodium chloride, low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose, magnesium stearate, citric acid, sodium sulfite, dextran, Tween 80, mannitol and the Pyrusussuriensis fat.
Described pharmaceutics acceptable forms can be oral agents or injection, and oral agents is tablet, pill, capsule or drop pill, and injection can be liquid drugs injection, powder pin or infusion solution.
When utilizing prulifloxacin and pidotimod to prepare the various dosage form of required medicine, can be according to the conventional production method preparation in pharmaceutics field.As this extract is mixed with one or more carriers, make corresponding dosage forms then.
The mechanism of action of the present invention is as follows: the mechanism of action of prulifloxacin is main by by suppressing the activity of DNA of bacteria topoisomerase II and IV, thereby suppresses the duplicating of DNA of bacteria, transcribes, repair process causes antibacterial death.The chemical constitution uniqueness of prulifloxacin does not almost have photosensitive side reaction.This medicine had both kept the high activity of anti-gram negative bacteria, had obviously strengthened the activity of resisting gram-positive bacteria again, and particularly the antimicrbial power to the gram negative bacteria headed by the bacillus pyocyaneus surpasses all xacin-series medicines that gone on the market at present.All show according in vitro tests and clinical use result, the prulifloxacin antimicrobial spectrum is extensive, and respiratory tract infection, urogenital infections, the infection of ear nose section, digestive system infection, enteritis, skin soft-tissue infection and surgical infection etc. due to staphylococcus, Streptococcus, Pn, Moraxella, large intestine Pseudomonas, shigella, Salmonella, Citrobacter, Klebsiella, Enterobacter cloaca genus, Serratia, Proteus, cholera bacteria, influenza bacterium, the green pus bacterium etc. are all had good therapeutical effect.Because its determined curative effect, side effect are less, moderate cost is well received.
Pidotimod is as immunostimulant, can promote immune level rapidly, can on the course of treatment, cooperate prulifloxacin treatment bacterial infection disease to have temporal concordance, and reach the purpose that shortens the course of treatment and reduce recurrence, also help to reduce the bacterial resistance odds.
Prulifloxacin compound preparation provided by the invention has following beneficial effect with respect to prior art:
(1) two kind of medicine adopts compound preparation, has good synergism, and its scope of application is wider, and clinical each section's common bacterial infects all can bring into play antibacterial activity, can also control the generation of infecting due to other non-common pathogen simultaneously.
All can be evenly distributed in the body after (2) two kinds of drug absorption, there is not interaction in both, also do not have depot action in the body, all discharge through urinary tract in the original shape mode, and safety is good.
The specific embodiment
Below describe technical solution of the present invention and effect in detail by specific embodiment, do not limit practical range of the present invention with this.
Embodiment 1
Prulifloxacin 200g
Pidotimod 800g
Starch 200g
Microcrystalline Cellulose 250g
Low-substituted hydroxypropyl cellulose 80g
Hydroxypropyl cellulose 80g
Microcrystalline Cellulose (outward) 50g
Magnesium stearate (outward) 12g
40% ethanol is an amount of
Tabletting is made 1000
Its preparation method is:
(1) respectively that each is former, adjuvant is crossed 100 mesh sieves
(2) granulate
1. the adjuvant that adds in the recipe quantity is added in the blender, do and mixed 10 minutes;
2. with adding an amount of 40% ethanol in the supplementary material that mixes, be mixed and made into soft material, granulate with 36 mesh sieves;
3. granule is dry in about 60 degrees centigrade, add the adjuvant that recipe quantity adds, mixing is with 36 mesh sieve granulate;
(3) tabletting promptly.
Every contains prulifloxacin 0.2g, pidotimod 0.8g.
Embodiment 2
Get prulifloxacin 200g, pidotimod 800g, Tween 80 15.5g, mannitol 90g, add water for injection 2000ml and make whole dissolvings, add 1% active carbon and reduce phlegm and internal heat formerly, cross 0.22 μ m microporous filter membrane, be sub-packed in 1000 10ml cillin bottles, lyophilization gets powder ampoule agent for injection.
Following examples are all represented with active component.
Embodiment 3: prulifloxacin 50mg; Pidotimod 200mg.
Embodiment 4: prulifloxacin 100mg; Pidotimod 400mg.
Embodiment 5: prulifloxacin 150mg; Pidotimod 600mg.
Embodiment 6: prulifloxacin 200mg; Pidotimod 800mg.
Embodiment 7: prulifloxacin 300mg; Pidotimod 1000mg.
Embodiment 8: prulifloxacin 350mg; Pidotimod 1200mg.
Embodiment 9: prulifloxacin 400mg; Pidotimod 1400mg.
Embodiment 10: prulifloxacin 500mg; Pidotimod 1500mg.
Embodiment 11: prulifloxacin 600mg; Pidotimod 1600mg.
Embodiment 12: prulifloxacin 600mg; Pidotimod 200mg.
Embodiment 12: prulifloxacin 600mg; Pidotimod 800mg.
Treat chronic genito-urinary system with prulifloxacin and pidotimod compound preparation below and infect the report of acute attack clinical efficacy, beneficial effect of the present invention is described.
[purpose] observation prulifloxacin and pidotimod compound preparation infect the clinical efficacy of acute attack to chronic genito-urinary system
[method]
1, case is selected: observe chronic genito-urinary system altogether and infect acute attack patient 95 examples, and wherein male 57 examples, women 38 examples, have following symptom and lab testing at 56.3 years old mean age:
(1) urinary tract irritation frequent micturition, urgent micturition, dysurea.
(2) or companion urine yellow skin is red or a urine mouthful adularescent secretions, lumbago, lower abdomen pain etc.
(3) routine urinalysis sediment microscopic inspection, leukocyte＞10/HP, or a small amount of albumen, erythrocyte.
(4) the stage casing urinary tract is cultivated, and bacteria quantified is cultivated bacterium number＞10
5/ ml.
And get rid of and to suffer from urethra and comprehensively demonstrate,prove tuberculosis of urinary system, lithangiuria, diseases of urinary system cases such as acute and chronic nephritis.All cases are divided into treatment group and matched group at random, and two groups of patient ages, sex and state of an illness are learned check p＞0.05 by statistics, have comparability.
2, observation index:
(1), clinicing symptom observation: it is red to observe frequent micturition before and after the treatment, urgent micturition, dysurea, urine yellow skin, lumbago, symptoms such as lower abdomen pain adopt integration method.
(2), lab index is observed: observe routine urinalysis before and after the treatment, CCMS is cultivated and treatment before and detect neutrophilic granulocyte phagocytic index and phagocytic percentage etc. during drug withdrawal.
3, Therapeutic Method: the treatment group gives prulifloxacin and pidotimod compound preparation (prulifloxacin 200mg, pidotimod 800mg), intravenous drip, Bid, continuous 15 days; Matched group gives prulifloxacin, 200mg, intravenous drip, Bid, continuous 15 days.Two groups symptomatic treatment measure is identical.
4, methods of marking and statistical procedures:
(1), methods of marking (adopting the method for integration assessment)
Clinical symptoms and objective indicator scoring before I, the treatment:
| Symptom | Normally | Idol has outbreak | The not influence work that shows effect is repeatedly had a rest | Continue outbreak and influence the work rest |
| Frequent micturition | (-) | (+) | (++) | (+++) |
| Urgent micturition | (-) | (+) | (++) | (+++) |
| Dysurea | (-) | (+) | (++) | (+++) |
| The urine yellow skin is red | (-) | (+) | (++) | (+++) |
| Few abdomen pain | (-) | (+) | (++) | (+++) |
| Lumbago | (-) | (+) | (++) | (+++) |
1 fen (++) note of (-) note 0 minute (+) note 2 minutes (+++) note 3 minutes
II, treatment back methods of marking:
The symptom that has when being first visit before the treatment is 3 minutes;
Treatment back sx is 2 minutes;
Obviously alleviate is 1 minute;
Transference cure is 0 minute.
(2), statistical procedures: the improvement of clinical symptoms adopts ridit to analyze, the enumeration data X 2 test in this way of other data, measurement data is then with the t check, p＜0.05 conduct has the standard of significance,statistical meaning.
[result]
1, table 1 as seen, the integration of main clinic symptoms changes before and after two groups of patient treatments, treatment group and matched group have significant difference (p＜0.05)
The improvement situation contrast of table 1, two groups of treatment front and back cardinal symptoms
| The integration project | Before the treatment (n) | Treat the 7th day (n) | Treat the 15th day (n) | |||
| Treatment group (n=60) | Matched group (n=35) | Treatment group (n=60) | Matched group (n=35) | Treatment group (n=60) | Matched group (n=35) | |
| Frequent micturition | 123 | 71 | 38 | 31 | 11 | 9 |
| Urgent micturition | 121 | 73 | 32 | 34 | 13 | 11 |
| Dysurea | 102 | 58 | 29 | 28 | 11 | 10 |
| The urine yellow skin is red | 35 | 22 | 7 | 12 | 1 | 2 |
| Lower abdomen pain | 54 | 22 | 8 | 12 | 0 | 1 |
| Lumbago | 86 | 49 | 25 | 23 | 6 | 5 |
2, two groups of patient treatment front and back lab index change
Routine urinalysis, CCMS are cultivated the improvement situation before and after table 2.1 treatment group patient (n=60) treatment
Routine urinalysis, CCMS are cultivated before and after table 2.2 matched group patient (n=35) treatment
The improvement situation
Neutrophilic granulocyte phagocytic index before and after the table 3 liang group patient
Bite the percentage rate situation with the neutrophilic granulocyte sky
| The neutrophilic granulocyte phagocytic index | Neutrophilic granulocyte percentage phagocytosis (%) | |||
| Treatment group (n=60) | Matched group (n=35) | Treatment group (n=60) | Matched group (n=35) | |
| Before the treatment (X ± SD) | 1.01±0.50 | 1.38±0.43 | 44.50±15.65 | 53.12±6.31 |
| Treat the 15th day (X ± SD) | 1.35±0.70 | 1.35±0.37 | 55.10±17.15 | 51.20±9.18 |
[conclusion]
By table 1 to the result of table 3 as can be seen, the treatment group all has significant effect with the final treatment of matched group.Simultaneously, the treatment group that adopts compound preparation is improved obviously aspect lab index, and immunologic function is improved, and particularly functions of neutrophils is improved significantly, and this shows that pidotimod has played the effect of immunological enhancement.Corresponding is, the clinical symptoms of treatment group just had tangible improvement in average the 6th day, and matched group continues to the tenth genius produce effects, gap is (p＜0.05) obviously, the improvement that curative effect has been described is relevant with the raising of immune level really, has proved that also pidotimod and Prulifloxacin compound preparation have the effect that shortens the course of treatment.Studies show that, compound preparation had both improved the anti-infectious immunity ability of body by the pidotimod endogenous, strengthen anti-infectious function and directly kill pathogenic bacterium by prulifloxacin is exogenous again, have the obvious synergistic effect, be used for the clinical treatment bacteria resistance and infect and to have good effect.
Claims (4)
1, a kind of Prulifloxacin compound preparation is characterized in that its active component consists of:
Prulifloxacin: 50-600mg
Pidotimod: 200-1600mg.
2, Prulifloxacin compound preparation according to claim 1 is characterized in that: with described active component, add the pharmaceutics acceptable auxiliary, make the pharmaceutics acceptable forms.
3, Prulifloxacin compound preparation according to claim 2 is characterized in that: described adjuvant is selected from any one or a few in starch, microcrystalline Cellulose, sucrose, dextrin, lactose, Icing Sugar, glucose, sodium chloride, low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose, magnesium stearate, citric acid, sodium sulfite, dextran, Tween 80, mannitol and the Pyrusussuriensis fat.
4, according to claim 2 or 3 described Prulifloxacin compound preparations, it is characterized in that: described pharmaceutics acceptable forms is oral agents or injection, and oral agents is tablet, pill, capsule or drop pill, and injection is liquid drugs injection, powder pin or infusion solution.
Priority Applications (1)
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|---|---|---|---|
| CN 200610067185 CN1836662A (en) | 2006-04-05 | 2006-04-05 | Prulifloxacin compound preparation |
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| Application Number | Priority Date | Filing Date | Title |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102210657A (en) * | 2010-04-01 | 2011-10-12 | 南京长澳医药科技有限公司 | Prulifloxacin tablets and preparation process thereof |
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2006
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102210657A (en) * | 2010-04-01 | 2011-10-12 | 南京长澳医药科技有限公司 | Prulifloxacin tablets and preparation process thereof |
| CN102210657B (en) * | 2010-04-01 | 2016-01-20 | 南京长澳医药科技有限公司 | A kind of prulifloxacin tablet and preparation technology thereof |
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