CN101468020A - Cefdinir dry suspension agent - Google Patents

Abstract

The invention belongs to the novel technical field of medicament, specifically relates to cefdinir dry suspension applied to the treatment of inflection caused by staphylococcus, streptocoaus, propionibacterium, gonococcus, colibacillus, Klebsiella pneumoniae, proteus mirabilis, hemophilus influenzae, and Providence bacteria such as pharyngolaryngitis, tonsillitis , bronchitis, pneumonia, pyelonephritis, cystitis and gynaecologic, surgical, dermal, and soft tissue infection.

Description

Cefdinir dry suspension agent

Technical field

The invention belongs to the medicine new technical field, a kind of novel form that relates to cefdinir, be used for the treatment of the infection that staphylococcus, streptococcus, propionibacterium, gonococcus, escherichia coli, Cray diphtheria, proteus mirabilis, hemophilus influenza, Pu Luweidengsi bacterium etc. cause, as pharyngolaryngitis, tonsillitis, bronchitis, pneumonia, pyelonephritis, cystitis, gonococcal urethritis and gynecological, surgery, skin, soft tissue dye etc.Specifically a kind of Cefdinir dry suspension agent.

Background technology

Since the seventies, cephalosporin entered Chinese market, advantage such as strong with antibacterial action, that clinical efficacy is high, toxicity is low, anaphylaxis is few was used widely clinical, and its consumption sum is soaring gradually to more than 50% of anti-infectives total value.But through clinical use for many years, antibacterial has produced general drug resistance to first generation cephalosporin, also in continuous rising, the clinician presses for a new generation the antibiosis of beta-lactamase stable (promptly being difficult for producing drug resistance) is usually substituted existing kind to the resistant rate of second generation cephalosporin.So the focus of drug development in recent years just concentrates on third and fourth peroral dosage form cephalosporin in generation.According to statistics, in 14 kinds of cephalosporins that since the nineties, gone on the market, three, four generation product just have 11 kinds, peroral dosage form account for 9 kinds more than.

Cefdinir (cefdinir) is the third generation oral cephalosporin that Japanese rattan pool company develops, and it has not only kept the high stability to beta-lactamase, and has improved third generation cephalosporin such as cefixime only to G ^-The bacterium effect is strong, and to G ⁺The deficiency of bacterium effect difference has characteristics such as has a broad antifungal spectrum, curative effect height, toxicity are low.In December, 1991 is first in Japan's listing, and commodity are by name

In December, 1997 obtains the FDA approval in U.S.'s listing, and commodity are by name

1999 in Korea S listing, calendar year 2001 the Tianjin Central Pharmaceutical Co., Ltd Cefdinir capsule of producing go on the market at home, commodity generation by name is held up the Buddhist nun

Cefdinir is in another third-generation cephalosporin kind in early stage---and carry out structural modification on the cefixime basis and obtain, remedied the shortcoming of original third generation cephalosporin a little less than, made it become a broad ectrum antibiotic truly the gram positive bacteria effect.Be characterized in and avoid chemical sproof generation in the phase I of treatment with regard to having enough antibacterial abilities.Through the strictness checking in 8 years, U.S. FDA announced that cefdinir can be used for community acquired pneumonia, acute episode of chronic bronchitis, acute upper jaw sinusitis, pharyngitis and tonsillitis, gonococcal urethritis, adnexitis, cystitis, intrauterine infection, non-complex skin and the skin histology infection etc. that caused by staphylococcus aureus, streptococcus pneumoniae, streptococcus pyogenes, hemophilus influenza and cattamolar's bacteria safely and effectively.

In Japan, 1759 examples are accepted in the clinical research of cefdinir, and effective percentage is 84.3% (1240 examples/1471 examples).Effective percentage to various infection is respectively potentiality purulent disease 86.7% (222 examples/256 examples), surgical field infects 87.9% (51 examples/58 examples), respiratory system infection disease 83.7% (339 examples/405 examples), urinary tract infection 83.9% (376 examples/448 examples), department of obstetrics and gynecology infection disease 88.3% (127 examples/143 examples), ophthalmology infection disease 88.1% (37 examples/42 examples), department of otorhinolaryngology infection disease 73.9% (88 examples/119 examples).

According to Watanabe etc., in-vitro antibacterial experiment showed, cefdinir clinical use for many years after, its antibacterial activity to clinical main pathogenic bacterium does not reduce.Chinese People's Liberation Army General Hospital clinical pharmacology base shows 6 kinds of antibiotic external bacteriostatic experiments such as cefdinirs in the recent period, to domestic clinical isolating pathogenic bacterium, cefdinir has very high killing action (comprise to first and second cephalosporin produce chemical sproof bacterial strain) in generation.

Have clinical data to show, to some indication, cefdinir 300mg 1 day 1 time and 100mg1 days 3 times therapeutic scheme do not have difference on cure rate.Based on cefdinir has a broad antifungal spectrum, long characteristics of aftereffect time, it is competent at fully in passing through preface therapy (SAT).(annotate: promptly when antibiotic through parenteral administration (as intravenously administrable), suitably control (it is normal that every index is recovered) behind the sensitive organism infection symptoms, a kind of Therapeutic Method that changes oral administration into early also claims " conversion therapy ".The advantage of passing through the preface therapy is convenient drug administration, and is safe and effective, reduces expenses, and reduces risks.〕

Anti-infectives is the 4th in the sales volume of 1999-2000 whole world medical product, and sales volume is sustainable growth trend.And in China, anti-infectives then accounts for the first place of total sales volume, and wherein the consumption amount of cephalosporin drug accounts for about 50% of hospital's antibiotic amount of money greatly, and the portion maximum is subjected to numerous doctors and patient's generally approval.Cefdinir is an oral broad-spectrum cephalosporin with good pharmacokinetic properties and time dependence bactericidal action, compare with medicines such as cefixime, cefpodoxime, cefuroxime, cefaclor and cefprozils, cefdinir significantly strengthens staphylococcic antibacterial activity.Stable to 13 kinds of common beta-lactamases, be a kind of rare efficient, safety, antibacterials easily, obtained extensive use clinically, and the adverse events incidence rate is low.And domestic manufacturer is few, and kind is single.

The chemical structural formula of cefdinir is:

Molecular formula: C ₁₄H ₁₃N ₅O ₅S ₂

Molecular weight: 395.42

The characteristics of cefdinir:

1, cefdinir is a broad ectrum antibiotic, almost can be used for the treatment of various infectious disease, and evident in efficacy, obviously is better than like product such as cefaclor, cefixime, cefuroxime etc.

2, extremely stable to beta-lactamase, be difficult for producing drug resistance, abroad after clinical application for many years, its antibacterial activity does not reduce.

3, because its has a broad antifungal spectrum, aftereffect time are long, be competent at fully, make things convenient for patient's medication and reduce risks in passing through the preface therapy.

4, domestic production producer is few, has only Tianjin central authorities' Pharmaceutical and Japanese Fujisawa Pharmaceutical Co., Ltd (Xi'an Yang Sen packing) to produce capsule and granule at present, and is few with variety competition.

5, medical insurance kind, the market promotion is convenient.

Summary of the invention

The object of the invention be to provide a kind of good stability, quality height, evident in efficacy, untoward reaction is little is dry suspension of making of principal agent and preparation method thereof with the cefdinir.

A kind of dry suspension that contains cefdinir of the present invention is made up of following component:

50 parts of cefdinirs

100 parts of sucrose

200 parts of lactose

150 parts in mannitol

450 parts in dextrin

2 parts of xanthan gum

10 parts of carboxymethyl starch sodium

0.32 part of aspartame

4.8 parts of strawberry essences

60% ethanol is an amount of

A kind of dry suspension that contains cefdinir of the present invention is achieved through the following technical solutions:

Cefdinir, dextrin, sucrose, lactose, mannitol, carboxymethyl starch sodium, xanthan gum are crossed 100 mesh sieves, mix to stir 30 minutes, dissolving in the aspartame of recipe quantity, strawberry essence to 60% ethanol is done binding agent, the system soft material.30 mesh sieves are granulated, 55-60 ℃ of oven dry, and 30 mesh sieve granulate, promptly.

A kind of dry suspension that contains cefdinir that the present invention obtains has that method is simple, good stability, characteristics that quality is high.

Following examples but do not limit the present invention in any way in order to explanation the present invention.

Embodiment 1: 1000 bags of specifications

Prescription:

Cefdinir 50g

Sucrose 100g

Lactose 200g

Mannitol 150g

Dextrin 450g

Xanthan gum 2g

Carboxymethyl starch sodium 10g

Aspartame 0.32g

Strawberry essence 4.8g

60% ethanol is an amount of

Method for making:

Cefdinir, dextrin, sucrose, lactose, mannitol, carboxymethyl starch sodium, xanthan gum are crossed 100 mesh sieves, mix to stir 30 minutes, dissolving in the aspartame of recipe quantity, strawberry essence to 60% ethanol is done binding agent, the system soft material.30 mesh sieves are granulated, 55-60 ℃ of oven dry, and 30 mesh sieve granulate, promptly.

Embodiment 2: 10000 bags of specifications

Prescription:

Cefdinir 500g

Sucrose 1000g

Lactose 2000g

Mannitol 1500g

Dextrin 4500g

Xanthan gum 20g

Carboxymethyl starch sodium 100g

Aspartame 3.2g

Strawberry essence 48g

60% ethanol is an amount of

Method for making:

Cefdinir, dextrin, sucrose, lactose, mannitol, carboxymethyl starch sodium, xanthan gum are crossed 100 mesh sieves, mix to stir 30 minutes, dissolving in the aspartame of recipe quantity, strawberry essence to 60% ethanol is done binding agent, the system soft material.30 mesh sieves are granulated, 55-60 ℃ of oven dry, and 30 mesh sieve granulate, promptly.

Claims (9)

1. a Cefdinir dry suspension agent is characterized in that this dry suspension is is the suspensoid that principal agent is made with the cefdinir.

2. according to the described Cefdinir dry suspension agent of claim 1, it is characterized in that this dry suspension is to be used for the treatment of the infection that staphylococcus, streptococcus, propionibacterium, gonococcus, escherichia coli, Cray diphtheria, proteus mirabilis, hemophilus influenza, Pu Luweidengsi bacterium etc. cause, as pharyngolaryngitis, tonsillitis, bronchitis, pneumonia, pyelonephritis, cystitis, gonococcal urethritis and gynecological, surgery, skin, soft tissue dye etc.

3. according to the described Cefdinir dry suspension agent of claim 1, it is characterized in that this dry suspension forms including but not limited to following component:

50 parts of cefdinirs

100 parts of sucrose

200 parts of lactose

150 parts in mannitol

450 parts in dextrin

2 parts of xanthan gum

10 parts of carboxymethyl starch sodium

0.32 part of aspartame

4.8 parts of strawberry essences

60% ethanol is an amount of.

4. Cefdinir dry suspension agent according to claim 3 is characterized in that described filler is sucrose, dextrin, mannitol, lactose, but is not limited to these filleies.

5. Cefdinir dry suspension agent according to claim 3 is characterized in that described correctives is aspartame, strawberry essence, but is not limited to these correctivess.

6. Cefdinir dry suspension agent according to claim 3 is characterized in that described suspending agent is xanthan gum, carboxymethyl starch sodium, but is not limited to this suspending agent.

7. Cefdinir dry suspension agent according to claim 3 is characterized in that described binding agent is an ethanol, but is not limited to this binding agent.

8. according to claim 3,4,5,6,7 described Cefdinir dry suspension agents, one of prescription that it is characterized in that this dry suspension is:

Cefdinir 50g

Sucrose 100g

Lactose 200g

Mannitol 150g

Dextrin 450g

Xanthan gum 2g

Carboxymethyl starch sodium 10g

Aspartame 0.32g

Strawberry essence 4.8g

60% ethanol is an amount of.

9. the preparation method of Cefdinir dry suspension agent according to claim 8 is characterized in that may further comprise the steps:

Cefdinir, dextrin, sucrose, lactose, mannitol, carboxymethyl starch sodium, xanthan gum are crossed 100 mesh sieves, mix to stir 30 minutes, dissolving in the aspartame of recipe quantity, strawberry essence to 60% ethanol is done binding agent, the system soft material.30 mesh sieves are granulated, 55-60 ℃ of oven dry, and 30 mesh sieve granulate, promptly.