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Paclitaxel gastric residence molecular imprinting controlled release administration system and preparation method thereof

A molecular imprinting and gastric retention technology, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of high-sensitivity cardiotoxicity, low solubility, and limited clinical application, etc. To achieve the effect of easy operation and simple preparation process

Active Publication Date: 2017-12-01
TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, it is often administered by intravenous injection. Because of the extremely low solubility of PTX in water (<6μg / mL), the PTX preparations currently used in clinical use are mostly prepared with polyoxyethylene castor oil-ethanol (1:1), and diluted before use. At this time, due to the conversion of the solvent, PTX is easy to precipitate and precipitate, and the solubilizer polyoxyethylene castor oil is easy to cause adverse reactions such as hypersensitivity, neurotoxicity, nephrotoxicity, and cardiotoxicity, and can dissolve the intravenous infusion tube during administration. Even if hydrocortisone is used at the same time, the incidence of allergic reactions still reaches 10%-30%, which greatly limits its clinical application

Method used

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  • Paclitaxel gastric residence molecular imprinting controlled release administration system and preparation method thereof
  • Paclitaxel gastric residence molecular imprinting controlled release administration system and preparation method thereof
  • Paclitaxel gastric residence molecular imprinting controlled release administration system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The gastric retention system is to increase the absorption of drugs, improve bioavailability, and prolong the residence time of drugs in the stomach. In order to investigate the floating performance of the drug, the floating characteristics of the paclitaxel gastric retention controlled sustained-release drug delivery system and the blank control group without liquid crystal monomer and POSS were observed within 24 hours. The specific operation steps are as follows:

[0037] a. Preparation method of molecularly imprinted drug carrier of gastric retention controlled sustained release drug delivery system using paclitaxel as template:

[0038]The formula is as follows: (mass percentage)

[0039] Paclitaxel 1.83%

[0040] Methacrylic acid 0.55%

[0041] Ethylene glycol dimethacrylate 3.17%

[0042] Liquid crystal monomer 4.51%

[0043] Polyhedral oligosilsesquioxane 24.17%

[0044] Azobisisobutyronitrile 0.93%

[0045] Toluene 52.85%

[0046] Acetonitrile 11.99%. ...

Embodiment 2

[0055] Paclitaxel equilibrium adsorption experiment was used to study the specific adsorption performance of the new molecularly imprinted polymer with paclitaxel as the template on the template molecule paclitaxel. Adsorption isotherms in the range of 0.5–5 mmol / L. The specific operation steps are as follows:

[0056] a. Synthesize the molecularly imprinted drug carrier MIP of the intragastric retention controlled sustained-release drug delivery system with paclitaxel as the template by the same method as above (Example 1). The non-imprinted polymer NIP does not add the template molecule paclitaxel, and the rest of the steps are the same as the synthesis of MIP.

[0057] b. Weigh 10.0 mg of dry novel paclitaxel molecularly imprinted polymers and non-imprinted polymers containing liquid crystal monomers and POSS, respectively, and put them into 5 mL centrifuge tubes, add 2.0 mL paclitaxel ethanol solution with a concentration of 0.5-5 mmol / L , put it into a shaker (power 100 ...

Embodiment 3

[0064] The drug release experiment in vitro is a model study of the drug release kinetics of the liquid crystal monomer loaded with paclitaxel and the new molecularly imprinted polymer of POSS. In order to investigate the release model of the drug, the total amount of drug released in a certain period of time was measured by the liquid crystal monomer loaded with paclitaxel and the new molecularly imprinted polymer of POSS, the non-imprinted polymer, and the blank control group without liquid crystal and POSS. The specific operation steps are as follows:

[0065] a. Synthesize the molecularly imprinted drug carrier MIP of the intragastric retention controlled sustained release drug delivery system with paclitaxel as the template by the above method (Example 1), and the synthesis of the paclitaxel molecularly imprinted polymer without liquid crystal monomer and POSS in the control group except without adding Except for the liquid crystal monomer and POSS, the other steps are th...

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Abstract

The invention relates to a paclitaxel gastric residence molecular imprinting controlled release administration system and a preparation method thereof. The paclitaxel gastric residence molecular imprinting controlled release administration system comprises the following raw materials by mass: 0.62-2.71% of template molecule paclitaxel, 0.53-0.62% of methacrylic acid, 3.07-3.58% of ethylene glycol dimethacrylate, 2.62-9.19% of liquid crystal monomers, 16.22-29.19% of polyhedral oligomeric silsesquioxane, 0.90-1.05% of azodiisobutyronitrile, 51.05-53.49% of methylbenzene and 11.58-13.52% of acetonitrile. The preparation method comprises the following steps: dissolving paclitaxel, methacrylic acid, liquid crystal monomers, polyhedral oligomeric silsesquioxane, azodiisobutyronitrile and ethylene glycol dimethacrylate in a solution of a pore-foaming agent; performing a reaction for 4 h in a water bath at 53 DEG C; performing grinding; at first, performing Soxhlet extraction for 72 h by use of methyl alcohol: acetic acid; then performing Soxhlet extraction for 12 h by use of methyl alcohol; and performing air-drying at the room temperature. The paclitaxel gastric residence molecular imprinting controlled release administration system is stable in physical and chemical property and obvious in imprinting effect and has a remarkable controlled release effect as a drug carrier; and compared with a non-imprinted polymer, the paclitaxel gastric residence molecular imprinting controlled release administration system has the advantages that in-vitro release has a zero-order release model, the in-vivo metabolism time of paclitaxel is prolonged, and the medicine bio-usability is improved.

Description

technical field [0001] The invention relates to a paclitaxel intragastric retention molecularly imprinted controlled and sustained-release drug delivery system, that is, paclitaxel is used as a template, and a molecularly imprinted polymer added with liquid crystal monomer and POSS is used as a sustained and controlled release drug carrier. Drug release in vivo, and at the same time, the preparation method of liquid crystal with paclitaxel as template molecule and POSS imprinted carrier was developed. The addition of liquid crystal monomers makes molecularly imprinted polymers (MIPs) have the molecular recognition properties of specific adsorption template molecules; and polyhedral oligomeric silsesquioxane is a new type of organic-inorganic hybrid material, which can Combining the advantages of organic materials and inorganic materials can make the polymer have high porosity and good thermal stability. In addition, these two substances make the polymer have unique floating pr...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/24A61K47/32A61K47/06A61K31/337A61P35/00
CPCA61K9/0002A61K9/0065A61K31/337A61K47/06A61K47/24A61K47/32
Inventor 黄艳萍张莉萍刘照胜
Owner TIANJIN MEDICAL UNIV
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