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Eutectic crystal formed by orlistat and proton pump inhibitor, composition thereof, and application of eutectic crystal or composition

A proton pump inhibitor, orlistat technology, applied in the field of medicine, can solve the problem of no synergistic antibacterial and antitumor effects

Inactive Publication Date: 2020-02-04
ZHONGSHAN WANHAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no technical teaching in the prior art that co-crystals composed of orlistat and PPIs simultaneously produce synergistic antibacterial and antitumor effects

Method used

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  • Eutectic crystal formed by orlistat and proton pump inhibitor, composition thereof, and application of eutectic crystal or composition
  • Eutectic crystal formed by orlistat and proton pump inhibitor, composition thereof, and application of eutectic crystal or composition
  • Eutectic crystal formed by orlistat and proton pump inhibitor, composition thereof, and application of eutectic crystal or composition

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preparation example Construction

[0069] 1 Preparation of eutectic

[0070] The present invention refers to the grinding method disclosed by Scott C. McKellar et al. (Crystal Growth & Design 2014, 14, 5, 2422-2430) to prepare the co-crystal described in the present invention.

[0071] Specifically, a certain molar ratio of orlistat and a proton pump inhibitor is placed in a ball mill, and ground at a frequency of 30-60 Hz for 15-60 minutes at room temperature. The frequency and grinding time of the ball mill were optimized and screened with the melting range of the product ≤ 2°C as the standard.

[0072] 2 Confirmation and characterization of the co-crystal structure

[0073] 2.1 Determination of eutectic formation and preliminary detection of purity

[0074] A single eutectic was considered to have formed if the milled product had a melting range below 2°C.

[0075] 2.2 Determination of the molar ratio of orlistat to proton pump inhibitors in the cocrystal

[0076] The present invention adopts 1 H-NMR (5...

Embodiment 1

[0085] Embodiment 1. Preparation of orlistat omeprazole co-crystal

[0086] Take 61.920g of orlistat and 129.565g of omeprazole, mix them well, place them in a planetary ball mill, grind them at a speed of 300r / min for 30min, collect the product, and obtain 188.267g of off-white powder with a melting point of 114.9-116.8°C . After recrystallization with ethanol, 187.924g of white crystalline powder was obtained, with a melting point of 114.8-115.7°C and an R value of 0.317.

Embodiment 2

[0087] Embodiment 2. Preparation of orlistat omeprazole co-crystal

[0088] Take 124.433g of orlistat and 86.355g of omeprazole, mix them well, place them in a planetary ball mill, grind them for 50min at a speed of 350r / min, and collect the product to obtain 199.564g of off-white powder with a melting point of 125.7-127.6°C . After recrystallization with acetone, 199.167g of white crystalline powder was obtained, with a melting point of 123.5-124.4°C and an R value of 1.047.

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Abstract

The invention provides a eutectic crystal formed by orlistat and a proton pump inhibitor. The proton pump inhibitor is selected from one of omeprazole, esomeprazole, pantoprazole, rabeprazole and lansoprazole, or a pharmaceutically acceptable salt thereof. The eutectic crystal can simultaneously generate synergistic antibacterial and antitumor effects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a co-crystal composed of orlistat and a proton pump inhibitor, its composition and application. Background technique [0002] Tumors with secondary bacterial infections are a major problem in the treatment of oncology patients. Drugs with antibacterial and anti-tumor activities are expected to improve the clinical efficacy of patients with tumors with secondary bacterial infections while reducing their treatment costs . [0003] Orlistat is currently a commonly used weight loss drug in China. CN110357812A and CN110314232A disclose that orlistat has certain antibacterial effects on various bacteria; Has a certain inhibitory effect. [0004] Proton pump inhibitors (PPIs) represented by omeprazole are clinically commonly used anti-gastric ulcer drugs. CN110279865A and CN110327335A respectively disclose the antibacterial and antitumor effects of PPIs. [0005] Drug co...

Claims

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Application Information

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IPC IPC(8): C07D305/12A61K31/365C07D401/12A61K31/4439A61P35/00A61P31/04A61P35/02
CPCA61P31/04A61P35/00A61P35/02C07B2200/13C07D305/12C07D401/12Y02A50/30
Inventor 向飞杜志博杨衍秋苏海娟彭韪
Owner ZHONGSHAN WANHAN PHARM CO LTD
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