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Preparation of taxane pH sensitive nanoparticles composite for oral administration and application thereof

A taxane and nanoparticle technology, which can be used in drug combinations, non-active components of polymer compounds, and medical preparations with non-active components, etc., can solve problems such as poor compliance, reduce toxicity, increase dispersion, and improve oral administration. The effect of bioavailability

Inactive Publication Date: 2012-10-03
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, it is often necessary to use large doses of corticosteroids and H1, H2 receptor blockers before using paclitaxel injection in clinical practice, and the compliance is extremely poor

Method used

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  • Preparation of taxane pH sensitive nanoparticles composite for oral administration and application thereof
  • Preparation of taxane pH sensitive nanoparticles composite for oral administration and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weigh 10mg taxane and 400mg pH sensitive material L100-55, dissolved in 40ml absolute ethanol to form the organic phase; weigh 200mg Poloxamer 188 and dissolve it in 100ml distilled water to form the water phase; use 7 # The bone marrow puncture needle quickly injects the organic phase into the stirred water phase, stirs for 5 minutes, evaporates the organic solvent in a 40°C water bath under vacuum, and concentrates to obtain the oral pH-sensitive taxane nanoparticle nanoparticle colloid solution.

Embodiment 2

[0027] Weigh 10mg taxane and 400mg pH sensitive material L100, dissolved in 40ml absolute ethanol to form the organic phase; weigh 200mg Poloxamer 188 and dissolve it in 100ml distilled water to form the water phase; use 7 # Rapidly inject the organic phase into the stirred water phase with a bone marrow puncture needle, stir for 5 minutes, and evaporate the organic solvent in a water bath at 40°C under vacuum, and concentrate to obtain an oral pH-sensitive taxane nanoparticle colloidal solution.

Embodiment 3

[0029] Weigh 10mg taxane and 400mg pH sensitive material S100, dissolved in 40ml absolute ethanol to form the organic phase; weigh 200mg Poloxamer 188 and dissolve it in 100ml distilled water to form the water phase; use 7 # Rapidly inject the organic phase into the stirred water phase with a bone marrow puncture needle, stir for 5 minutes, and evaporate the organic solvent in a water bath at 40°C under vacuum, and concentrate to obtain an oral pH-sensitive taxane nanoparticle colloidal solution.

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Abstract

The invention relates to a preparation of taxane pH sensitive nanoparticles composite for oral administration and application thereof. The invention is characterized in that taxane medicine is enveloped in nanoparticles made of a pH sensitive high polymer material to prepare a nanometer dose administration system. The system can obviously improve the dissolution rate of slightly soluble medicine,has obvious pH sensitivity, and releases medicine at the particular position of intestinal tract, which is favorable to improving the bioavailability and local targeted performance of the medicine. The preparation has good application foreground in the tumour treatment, in particular to the local tumour treatment of gastrointestinal tract.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to the preparation and application of a taxane pH-sensitive nanoparticle composition for oral administration. Background technique [0002] Paclitaxel, also known as taxane, is a diterpenoid isolated from the bark of Taxus plants. In the early 1970s, paclitaxel was proven to have anti-tumor activity. Its anti-cancer mechanism is unique, mainly inducing and promoting tubulin polymerization and assembly, stabilizing microtubules, and inhibiting tumor cell growth. On December 29, 1992, the US FDA approved taxane for the first time for the treatment of metastatic ovarian cancer that failed other chemotherapeutic drugs, and later approved it for metastatic breast cancer refractory to platinum drugs. Cancer, breast cancer, lung cancer have significant curative effect. However, since paclitaxel belongs to the biopharmaceutical classification II compound (low solubility and low pe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/08A61K9/10A61K31/337A61K47/44A61K47/42A61K47/32A61K47/38A61P35/00
Inventor 张强王坚成吴翠栓
Owner PEKING UNIV
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