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A kind of pharmaceutical composition of Thiopeptidecycline

A technology of thiopeptidecycline and its composition, which is applied in the field of thiopeptidecycline pharmaceutical composition, can solve the problems of drug efficacy or safety that cannot be successfully developed into medicines, and achieve strong anti-(drug-resistant) bacteria activity, A wide variety of effects with significant application value

Active Publication Date: 2021-06-22
NANJING BIOTICA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to improve water solubility, scientists have carried out a series of structural modifications and transformations on the dehydroalanine, indole ring and pyridine ring in the structure of thiopeptidecycline, but they have not been successfully developed into drugs due to problems such as drug efficacy or safety. (J Org Chem, 2002, 67:8699; J Nat Prod, 2005, 68:550; Bioorg Med Chem Lett, 2004, 14:3743)

Method used

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  • A kind of pharmaceutical composition of Thiopeptidecycline

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1 Thiopeptidecycline HPLC detection method and standard curve

[0037] Thiopeptidecycline bulk drug needs to be dissolved in DMSO to 1 mg / mL, and the pharmaceutical composition needs to be diluted to 1 mg / mL with the corresponding solution for detection.

[0038] Chromatographic column: Waters Atlantis C18 chromatographic column (4.6×150mm, 5μm)

[0039] Mobile phase A: pure medium containing 1‰TFA

[0040] Mobile phase B: 1‰TFA in acetonitrile

[0041] Mobile phase elution gradient:

[0042] time (min) 0 30 31 34 Mobile phase B% 30 60 90 90

[0043] Flow rate: 1.0mL / min

[0044] Detection wavelength: 362nm

[0045] Injection volume: 10μL

[0046] Column temperature: 40°C

[0047] Sample concentration: generally determined as 1mg / mL

[0048] Under the above-mentioned chromatographic conditions, the peak shape of thiopepticycline is good, and the retention time of thiopepticycline is about 17.5min.

[0049] Precisely weigh th...

Embodiment 2

[0051] The examples of thiopeptidecycline compositions listed in this patent are only for illustration and do not limit the scope of application of the present invention.

[0052] Weigh 500 mg of thiopeptidecycline powder, put it in a 100ml beaker, add 7ml of water for injection, stir well, adjust the pH value to 2.0-4.0 with different pH regulators, stir to dissolve thiopeptidecycline, add water for injection to 10ml, and centrifuge Remove the insoluble matter, and after diluting with water for injection, HPLC detects the degradation of the main drug and determines the dissolution. It was tested that the main drug thiopeptidecycline did not degrade, and the solubility of thiopeptidecycline at pH 2.0-4.0 was basically the same under the action of a specific pH regulator. When the pH regulator is hydrochloric acid, the solubility of thiopeptidecycline is 0.35mg / mL; when the pH regulator is citric acid, the solubility is 0.27mg / mL; when the pH regulator is acetic acid, the solub...

Embodiment 3

[0054] The examples of thiopeptidecycline compositions listed in this patent are only for illustration and do not limit the scope of application of the present invention.

[0055] Weigh 500 mg of thiopeptidecycline powder, put it in a 100ml beaker, add 7ml of water for injection, stir well, adjust the pH value to 5.0 with different pH regulators, stir to dissolve thiopeptidecycline, add water for injection to 10ml, and centrifuge to remove insoluble After being diluted with water for injection, HPLC detects the degradation of the main drug and measures the dissolution. It has been tested that the main drug thiopeptidecycline has not been degraded. When the pH regulator is hydrochloric acid, the solubility of thiopeptidecycline is 0.11mg / mL; when the pH regulator is citric acid, the solubility is 0.06mg / mL; when the pH regulator is acetic acid, the solubility is 0.07mg / mL; when the pH When the regulator is malic acid, the solubility is 0.11mg / mL; when the pH regulator is nitri...

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Abstract

Thiopeptidecycline is a thiopeptide antibiotic with strong anti-drug-resistant bacteria activity. It has broad clinical application prospects, but the disadvantage of poor solubility needs to be improved urgently. The invention discloses a pharmaceutical composition of thiopeptidecycline, which can significantly increase the solubility of thiopeptidecycline and increase the clinical application value of thiopeptidecycline. In addition, the thiopeptidecycline composition disclosed in the present invention can be used to prepare aqueous solution injections, non-aqueous solution injections, emulsion injections, suspension injections and sterile powders for injection.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical composition of thiopeptidecycline, which increases the solubility of poorly soluble thiopeptidecycline by preparing the pharmaceutical composition. Background technique [0002] Poor water solubility is one of the important reasons why many active new chemical entities (NCEs) cannot be approved for marketing (JPharmacol Toxicol, 2009, 44:235). According to incomplete statistics, in recent years, the proportion of insoluble compounds in the new drug development product line has rapidly increased from about 40% ten years ago to 60%-70%, and this proportion may be even higher for injections. Therefore, how to effectively solve the solubility problem of compounds and improve the druggability of compounds has become one of the important challenges in the development of new drugs (Front Pharmacol, 2017, 8:261). [0003] At present, the convention...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/12A61K9/08A61K9/19A61K47/40A61K47/12A61K47/18A61K9/107A61K47/44A61K47/24A61K9/10A61K47/28A61K47/10A61K47/02A61K47/14A61K47/26A61K47/22A61P31/04
CPCA61K9/0019A61K9/08A61K9/10A61K9/107A61K9/19A61K38/12A61K47/02A61K47/10A61K47/12A61K47/14A61K47/183A61K47/22A61K47/24A61K47/26A61K47/28A61K47/40A61K47/44
Inventor 陈依军吴旭日钱军建
Owner NANJING BIOTICA PHARMA
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