Solid-phase nano micelle and preparation method thereof

A technology of nanomicelles and drug-loaded micelles, which can be used in pharmaceutical formulations, medical preparations of non-active ingredients, non-effective ingredients of polymer compounds, etc., and can solve problems such as limited diffusion free volume, large molecular weight, and unsatisfactory effects. , to achieve the effect of improving bioavailability, high cohesion, and prolonging the circulation time in the body

Inactive Publication Date: 2011-09-28
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The use of polymers to prepare insoluble drugs in nanoparticles is expected to overcome the problem of drug leakage. However, due to the large molecular weight (usually tens of thousands) of the hydrophobic segment of polymer nanoparticles, the inner core is solidified after forming and has strong cohesion. , the free volume of diffusion (free volume of diffusion) is very limited, it is difficult for water to diffuse into, and it is also difficult for the drug to dissolve from the carrier. In vivo application is often excreted with the carrier without dissolution, and the effect is not ideal.

Method used

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  • Solid-phase nano micelle and preparation method thereof
  • Solid-phase nano micelle and preparation method thereof
  • Solid-phase nano micelle and preparation method thereof

Examples

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Effect test

Embodiment 1

[0039] Embodiment 1: Preparation of solid phase nano micelles and observation of product particle size and morphology.

[0040] Polyoxyethylene 600 mono / distearate, Polyoxyethylene 400 monostearate, Benze 56, Benze 76, Benze 78, Benze 97, Lipocol C-10, Volpo S-10, Lipocol S - 10 or their mixture (0.2-5g), dissolved in 100ml aqueous solution containing 1-5 (w / v%) lactose, the water temperature is kept at 50°C. Model drug furosemide 20mg, naproxen 80mg or paclitaxel 10mg were dissolved in 5ml ethyl acetate. The drug solution is added dropwise to the surfactant solution, the water temperature is kept at 50° C., the organic solvent is removed by stirring or rotary evaporation, and a clear drug-loaded micellar solution is obtained. Spray drying (parameters: the inlet temperature is lower than the bluish point of the micellar solution; spray speed: 1ml / min; spray drying air pressure: 1.5kgf / cm 2 ;Air velocity: >0.25m 3 / min), to obtain dry powder.

[0041] The particle size and ...

Embodiment 2

[0044] Example 2: Preparation of solid-phase nanomicelles and their in vivo and in vitro evaluation as poorly soluble drug delivery carriers.

[0045] Polyoxyethylene 600 mono / distearate, Polyoxyethylene 400 monostearate, Benze 56, Benze 76, Benze 78, Benze 97, Lipocol C-10, Volpo S-10, Lipocol S -10 or their mixture (0.2-5g) and model drug furosemide 10-500mg, naproxen 10-500mg or paclitaxel 10-100mg are dissolved in 10ml of ethanol. The solution is added dropwise to 100 ml of an aqueous solution containing 1-10 (w / v%) mannitol, and the water temperature is maintained at 50° C. The organic solvent was removed by stirring or rotary evaporation to obtain a clear drug-loaded micellar solution. Spray drying (parameters: inlet temperature is lower than the cloud point of micellar solution; spray speed: 1ml / min; spray drying air pressure: 1.5kgf / cm2; air flow rate:> 0.25m3 / min) to obtain dry powder.

[0046] In vivo and in vitro evaluation of solid-phase nanomicelles as poorly so...

Embodiment 3

[0052] Example 3: The formulation of paclitaxel-loaded solid-phase nanomicelles improves the oral bioavailability of the drug.

[0053] Dissolve Benzaze 76 (1g) and Paclitaxel 10-100mg in 10ml of ethyl acetate, remove the organic solvent by rotary evaporation, add 100ml of aqueous solution containing 1-5 (w / v, %) dextran, keep the water temperature at 50°C, stir to obtain clarification drug-loaded micellar solution. Spray drying (parameters: the inlet temperature is lower than the bluish point of the micellar solution; spray speed: 1ml / min; spray drying air pressure: 1.5kgf / cm 2 ;Air velocity: >0.25m 3 / min) to obtain a dry powder.

[0054] The paclitaxel-loaded solid-phase nanomicelle preparation was reconstituted with water to form a paclitaxel suspension containing 1 mg / ml, and administered to SD rats by intragastric administration (dose: 2.67 mg / kg). , 2, 4, 8, 12, and 24 hours later, blood was taken from the orbital vein, anticoagulated with heparin, centrifuged at 3,0...

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Abstract

The invention discloses a 'solid-phase nano micelle' as well as a preparation method and application thereof as a carrier for water-insoluble medicines, wherein the solid-phase nano micelle comprises a small molecular surfactant which has the molecular weight below 10000Da, is solid and small in aqueous solubility at body temperature and has the Krafft point not lower than the body temperature. The solid-phase nano micelle is prepared by thermal dissolution-spray drying. At the temperature higher than the Krafft point, the surfactant has high water solubility, an encapsulated drug exists in aform of micelle, and at the body temperature or room temperature, the water solubility is reduced, the micelle exists in a form of solid-phase nano particles. The preparation can significantly improve the solubility of insoluble medicines, and offers proper releasing features to the insoluble medicines in order to enhance the bioavailability of the insoluble medicines.

Description

technical field [0001] The invention relates to the field of chemical pharmacy, in particular to a preparation method of solid-phase nano-micelle and its application as a poorly water-soluble drug carrier. Background technique [0002] With the widespread application of combinatorial chemistry, high-throughput screening and other technologies in drug development, a large number of active drug candidates have been designed, synthesized or discovered, of which more than 40% of candidate drugs are water-insoluble drugs, which are difficult to use conventional preparations Technology is prepared into shape, so it is often discarded early in product development. Improving the water solubility and bioavailability of poorly soluble drugs by formulation technology is an urgent problem to be solved no matter for the development of new drugs or the improvement of the curative effect of existing preparations, and has important scientific and social economic value. [0003] In recent y...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/34A61K47/36A61K47/32A61K47/42A61K47/20A61K47/24A61K47/26
Inventor 高小玲陈红专
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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