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Cyclodextrin metal organic framework composition for improving dissolution of indometacin

A technology of indomethacin cyclodextrin and metal organic framework, which is applied in the directions of drug combination, organic active ingredient, medical preparation of non-active ingredient, etc., can solve the problems of high preparation cost, toxicity, poor solubility, etc. The ability to maintain saturation, the ability to maintain supersaturation, and the effect of improving dissolution behavior

Active Publication Date: 2021-03-26
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, not all metal-organic frameworks are biocompatible. The metal ions of reported MOFs are mostly transition metals, and the organic ligands are mostly aromatic compounds with poor solubility. These materials are not only expensive to prepare, but also cause environmental pollution. More importantly, it poses a threat to the safety of biological tissues and has certain toxicity, which seriously limits the application in the field of biomedicine

Method used

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  • Cyclodextrin metal organic framework composition for improving dissolution of indometacin
  • Cyclodextrin metal organic framework composition for improving dissolution of indometacin
  • Cyclodextrin metal organic framework composition for improving dissolution of indometacin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1: Preparation of indomethacin cyclodextrin metal organic framework composition

[0045] (1) Preparation of neutralized CD-MOF: Weigh γ-CD (648 mg, 0.5 mmol) and KOH (224 mg, 4 mmol), dissolve in 20 mL of distilled water, and filter the mixture through a 0.45 μm PTFE membrane, Add 2mL of methanol and place in a glass beaker. The glass was placed in a closed system filled with methanol, and after standing at 50°C for 6 hours, microcrystals precipitated. Take the supernatant of the mother liquor and add cetyltrimethylammonium bromide (CTAB, 8mg·mL -1 ), let stand overnight, centrifuge the precipitate and supernatant, wash the precipitate 3 times with isopropanol, and remove excess CTAB. The pellet was submerged in 10 mL of ethanol containing 1 mL of acetic acid and suspended for 2 h to obtain neutralized CD-MOF. The mixture was centrifuged to separate the precipitate and supernatant, and the precipitate was washed with ethanol three times. Finally, the white cr...

Embodiment 2

[0053] Example 2: Characterization of indomethacin-cyclodextrin metal-organic framework compositions

[0054] (1) Morphological and elemental composition analysis ( figure 1 ):

[0055] The morphology and particle size of the CD-MOF and IMC@CD-MOF prepared in Example 1 were investigated using a scanning electron microscope (Quanta FEG 250SEM) in field emission mode, and the X-ray energy dispersive spectrometer (EDX) equipped with the instrument was used to analyze the elements of the sample composition. Before the samples were observed, gold was plated for 60 s with a sputter coater. An Everhart-Thornley detector (ETD) was used to set the spot size to 3 nm, the electron beam energy to 20.00 kV, and the working distance to 8.9 mm.

[0056] like figure 1 As shown, both CD-MOF and IMC@CD-MOF are regular cubes with a particle size distribution of about 2-10 microns. After loading IMC, the apparent morphology does not change significantly. The results of EDX visually show the ...

Embodiment 3

[0078] Example 3: Research on the drug loading of indomethacin cyclodextrin metal organic framework composition

[0079] (1) nuclear magnetic method ( Figure 9 ):

[0080] Weigh 5-10 mg of the IMC@CD-MOF prepared in Example 1 and dissolve it in a mixed solvent of 350 microliters of deuterated DMSO and 250 microliters of deuterated water, and monitor the drug loading by NMR.

[0081] Drug loading (%)=N IMC × M IMC / (N IMC × M IMC +N CD-MOF × M CD-MOF )×100

[0082] N IMC Indicates the number of molecular moles of IMC, M IMC Indicates the molecular mass of IMC, N CD-MOF Indicates the number of molecular moles of IMC@CD-MOF, M CD-MOF Indicates the molecular mass of IMC.

[0083] like Figure 9 As shown, the integral unit of the anomeric hydrogen proton of γ-CD is set to 8, representing one cyclodextrin molecule; the combined integral of the aromatic proton signal of IMC at the chemical shift of 7.59ppm in the composition is 2.72, representing 0.68 IMC molecules. T...

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Abstract

The invention discloses a cyclodextrin metal organic framework composition for improving dissolution of indometacin. According to the composition, the cyclodextrin metal organic framework material isimmersed and stirred in an ethanol solution of indometacin, the solubility and dissolution rate of indometacin are improved, a relatively high supersaturation degree can be maintained in the dissolution process, and the problem of physical instability in the amorphous indometacin dissolution gelatinization and storage process is avoided. The cyclodextrin metal organic framework composition has theadvantages of low-price and easily available raw materials, environment friendliness, safety and simple steps, and is suitable for industrial production.

Description

technical field [0001] The invention generally relates to the technical field of medical materials, in particular to a cyclodextrin metal-organic framework composition for improving indomethacin dissolution. Background technique [0002] Non-steroidal anti-inflammatory drugs are the most widely used drugs in the world. They mainly have anti-inflammatory effects and have very effective antipyretic, analgesic and anti-inflammatory activities. They are widely used clinically in acute rheumatic and rheumatoid joints. Inflammation, osteoarthritis, ankylosing spondylitis, relief of various fever and pain symptoms. Its mechanism of action is to inhibit the biosynthesis of prostaglandins by inhibiting cyclooxygenase, thereby inhibiting the occurrence and development of inflammation. The research on non-steroidal anti-inflammatory drugs began with the use of sodium salicylate at the end of the 19th century. After the 1940s, non-steroidal anti-inflammatory drugs developed rapidly. Am...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/22A61K31/405A61P29/00
CPCA61K47/6951A61K47/22A61K31/405A61P29/00
Inventor 蔡挺雷雨竹彭亚运
Owner CHINA PHARM UNIV
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