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Ultrasound mediated mucosal drug delivery system

A drug delivery system, ultrasound-mediated technology, applied in the direction of drug delivery, pharmaceutical formulation, drug equipment, etc., to achieve the effect of a wide range of applicable dosage forms and a wide range of drug applications

Inactive Publication Date: 2010-10-13
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The technical problem to be solved by the present invention is to provide a drug mucosal drug delivery system composed of air-containing vesicles with acoustic response performance, which can use ultrasound to introduce drugs into the mucosa , reach deep tissue or enter the blood circulation, play a local or systemic therapeutic effect, especially suitable as a mucosal drug delivery system for drugs with poor amphiphilicity and biomacromolecular drugs

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  • Ultrasound mediated mucosal drug delivery system
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  • Ultrasound mediated mucosal drug delivery system

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Embodiment 1

[0035] Water-soluble biomacromolecular drugs such as proteins, peptides, hormones, enzymes, cell growth factors, etc., have large molecular weights and high diffusion resistance, so it is usually difficult to penetrate the mucous membrane and has poor environmental stability. These drugs can be made into stable formulations for mucosal administration using formulation technology. The gas-containing vesicles are dispersed in these systems by first addition or post-addition, and biomacromolecular drugs containing air vesicles are prepared by heating, physically dispersing or combining surfactants, stabilizers, salts, buffers, and suspending agents Preparations for mucosal administration. Air-containing vesicles are composed of biocompatible natural animal and vegetable gums, surfactants, semi-synthetic cellulose, synthetic polymers, proteins, phospholipids or lipid materials. In the first embodiment of the present invention, bovine serum albumin is used as a model drug, and the...

Embodiment 2

[0039] Some amphipathic or poorly soluble drugs, although the molecular weight is not large, are difficult to penetrate the mucosa and exert local deep tissue or systemic therapeutic effects, such as the powerful anti-inflammatory drug dexamethasone, the antifungal drug amphotericin B, the antifungal drug tumor drug paclitaxel, etc. The second embodiment of the present invention uses phospholipids as vesicle material, adopts first addition method to prepare air-containing vesicle freeze-dried emulsion of dexamethasone, and can be made into a liquid preparation by adding an appropriate solution before use.

[0040] Mix 80mg of gelatin and 2ml of water and heat to 60°C as the inner water phase. In addition, 10 mg of phospholipid and 5 mg of dexamethasone were dissolved in 5.5 ml of dichloromethane as the oil phase, and then the oil phase was gradually poured into the water phase under stirring (8000 r / min) to make a W / O emulsion, and the emulsion was cooled to 10°C, add it into...

Embodiment 3

[0043] Spray is a preparation in which the content can be released in the form of mist by means of the pressure of a manual pump, and is suitable for nasal, vaginal, and pulmonary mucosal drug delivery systems. The third embodiment of the present invention uses phospholipids as the vesicle material, and adopts the post-addition method to prepare the calcitonin-containing air vesicle spray.

[0044] Mix 20mg of calcitonin (5000IU / mg) with 2g of propylene glycol alginate uniformly by equal addition method, add to 100ml of 1% gelatin aqueous solution with pH 5 (adjust the pH with hydrochloric acid), add 0.38g of aspartic acid Mix well to make a mixed solution containing calcitonin. In addition, 100mg of phospholipids, 300mg of Tween 80 and 3g of polyethylene glycol 2000 were dissolved in 100ml of tert-butanol at 60°C, mixed evenly, placed at -5°C for 4 hours, and freeze-dried to obtain a freeze-dried powder, which was put into a sealed bottle and filled with Add sulfur hexafluor...

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Abstract

The invention relates to an ultrasound mediated mucosal drug delivery system which disperses a large quantity of vesicles containing gases and having acoustic response properties into the traditional liquid type mucosal drug delivery formulation through a formulation technology so as to promote drugs inside the liquid type mucosal drug delivery formulation to faster enter deep tissues and blood circulation to develop therapeutic action by penetrating through a mucosa under ultrasound mediation. The ultrasound mediated mucosal drug delivery system has wide application range and can meet the requirements of mucosa deep tissues or systemic therapy.

Description

【Technical field】 [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically, the invention relates to an ultrasound-mediated mucosal drug delivery system. 【Background technique】 [0002] The mucosal layer is a barrier for the human body to absorb drugs, and it is difficult for biomacromolecular drugs and drugs with poor amphipathic properties to penetrate the mucosal tissue into deep tissues and blood circulation to exert therapeutic effects. [0003] The current method of promoting drug entry into the mucosal surface mainly relies on chemical penetration enhancers and enzyme inhibitors to increase drug absorption [Huang Jian, Gao Chunsheng, Mei Xingguo. Application of penetration enhancers in macromolecular drug delivery systems. 2006, 33 (6): 654-656], there are also reports of using membrane-penetrating peptides to carry macromolecular protein or polypeptide drugs through the mucosal barrier [Sílvia Pujals, Jimena Fernández-Carneado, ...

Claims

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Application Information

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IPC IPC(8): A61M37/00A61K9/00A61K9/06A61K9/10A61K9/107A61K9/12A61K9/14A61K9/16A61K9/50
Inventor 赵应征鲁翠涛赵爱国
Owner ZHEJIANG HISUN PHARMA CO LTD
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