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New application of thiopeptcin

A technology of thiopeptidylcycline and antibiotics, which is applied in the directions of inactive medical preparations, cyclic peptide components, and pill delivery, etc., can solve the problems such as the anti-anaerobic bacteria, Clostridium difficile effect and activity of thiopeptidylcycline, etc. The effect of super antibacterial activity, strong antibacterial activity and small safety hazard

Active Publication Date: 2016-03-02
NANJING BIOTICA PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In vitro activity studies have shown that Thiopeptidecycline can kill Gram-positive aerobic bacteria at very low concentrations (ng / mL). report

Method used

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  • New application of thiopeptcin
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  • New application of thiopeptcin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 The in vitro anti-Clostridium difficile and its drug-resistant strain activity of thiopeptcycline

[0028] The in vitro antibacterial activity of Thiopeptidecycline was tested against the sensitive Clostridium difficile ATCC9689 strain Clostridium difficile LCN001 and the clinically isolated drug-resistant strain, and compared with vancomycin. According to the broth dilution method recommended by CLSIM11-A7, the minimum inhibitory concentration (MIC) of thiopeptidecycline was determined. According to the measurement needs, the Brooke's broth supplemented with Hemin (5 mg / ml), vitamin K1 (1 μg / ml), lysed horse blood (5%) and oxidase (1:25v / v) was divided into different measurement groups, and then Thiopeptidecycline or vancomycin in DMSO was added. The concentration range of the test drug was 0.025 μg / ml-128 μg / ml. Check the growth of Clostridium difficile in each culture medium, the minimum antibacterial drug concentration at which the experimental bacteria ...

Embodiment 2

[0031] Embodiment 2 Thiopeptidecycline LC-MS / MS detection method

[0032] Add 90 μl of methanol containing 5 ng / ml verapamil to 30 μl of blood or urine sample, vortex for 3 minutes, then centrifuge at 14,000 rpm for 5 minutes, take 80 μl of the supernatant, and inject it into LC-MS / MS for analysis.

[0033] High performance liquid chromatography: Chromatographic column: WatersSymmetry300C183.5μm2.1*100mm;

[0034] Mobile phase A: 10mM ammonium acetate + 0.02% ammonia solution; mobile phase B: methanol;

[0035] Analysis time: 5.2min Injection volume: 5μL Column temperature: 25°C;

[0036] Gradient elution:

[0037] time (min)

Flow rate (mL / min)

B％

0.00

0.4

67

2.40

0.4

67

2.45

0.4

90

3.80

0.4

90

3.85

0.4

67

5.20

0.4

67

[0038] Mass spectrometry: positive ion mode (Agilent6460B)

[0039] Detection ion pair: Thiopeptidecycline: 1437.3→172.0, fragmentor=135, CE=22...

Embodiment 3

[0042] Example 3 Oral Thiopeptidecycline Pharmacokinetics Study

[0043] Thiopeptidecycline liquid preparation method: take a certain amount of thiopeptidecycline, put it in a mixed solvent containing 10% PEG400, 1% Tween 80, and 5mg / ml citric acid at pH 5.0, and shake until it becomes clear to obtain thiopeptidecycline Oral gavage solution.

[0044] Male rats were divided into high, medium and low dose groups according to the purpose of the experiment. Among them, the high dose group is 50 mg / Kg, the middle dose group is 25 mg / Kg, the low 1 dose group is 5 mg / Kg, and the low 2 dose group is 1 mg / Kg. About 0.3 ml of blood samples were collected at each time point of about 15 minutes, 30 minutes, 45 minutes, 1, 2, 4, 6, 8 and 24 hours after the administration for the determination of bioavailability. See Example 2 for the method.

[0045] Table 2 Concentration-time data (ng / ml) of thiopeptidecycline in plasma after oral administration of thiopeptidecycline to rats

[0046] ...

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Abstract

The invention discloses new application of thiopeptcin to preparation of medicine for treating diseases caused by clostridium difficile infection and complications of the diseases. The thiopeptcin has evident activity on the clostridium difficile and the drug-resistant strains of the clostridium difficile and has great clinical application significance. In-vivo tests prove that the thiopeptcin does not enter blood circulation when a patient takes the thiopeptcin orally. According to the features of intestinal administration, the invention further provides a thiopeptcin orally-taken preparation containing a safe and effective dose and a preparing method of the thiopeptcin orally-taken preparation.

Description

technical field [0001] The invention belongs to the field of novel antibiotics and applications thereof, and specifically relates to the new application of thiopeptidecycline against Clostridium difficile and drug-resistant strains thereof and oral preparations of thiopeptidecycline. Background technique [0002] Clostridium difficile (Clostridium difficile) is a Gram-positive anaerobic bacillus, about 3% of the general population have the parasitism of the intestinal tract. Clostridium difficile is an opportunistic pathogen. Under normal circumstances, it is controlled by other bacteria in the human body and will not endanger human health. Clostridium difficile infection (CDI) is usually caused by excessive or irrational use of broad-spectrum antibiotics (clindamycin, ampicillin, cephalosporin, lincomycin, etc.) With the continuous emergence of drug-resistant strains, CDI is increasing. Studies have found that CDI is mainly caused by the cytotoxic effects of toxins A and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61P31/04
CPCA61K9/0007A61K9/0053A61K9/0095A61K9/06A61K9/08A61K9/107A61K9/146A61K9/1641A61K9/1652A61K9/19A61K9/2018A61K9/2054A61K9/2059A61K9/2853A61K9/2866A61K9/2873A61K9/4866A61K9/5031A61K9/5078A61K38/12A61K47/10A61K47/26A61K47/40A61K47/44A61K9/00A61K47/00A61P31/04A61K9/0014A61K9/0056A61K9/2009A61K9/2013A61K9/2027A61K9/2886A61K9/485
Inventor 陈依军钱军建吴旭日
Owner NANJING BIOTICA PHARMA
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