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Hollow drug carrying microsphere used for pulmonary drug delivery and preparation method thereof

A drug-loaded microsphere and no-load technology, which is applied in drug combination, respiratory diseases, emulsion delivery, etc., can solve the problems of poor preparation repeatability and treatment repeatability, lower drug encapsulation rate, and inability to deposit for a long time. Easy industrial production, reduced biocompatibility, highly reproducible effects

Inactive Publication Date: 2016-03-30
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The Chinese patent (publication number CN101361716A) adopts the stirring-solvent volatilization method to prepare the drug-loaded microspheres, and its particle size distribution is wide, because the uneven particle size will inevitably cause the problems of poor preparation repeatability and treatment repeatability, and it is difficult to apply to clinical practice
However, the large pores on the microspheres will increase the occurrence of burst release, and at the same time, the encapsulation efficiency of the drug will be reduced, and the drug will be easily lost.
Studies have pointed out (Imai, Y., Miki, T., Ishikawa, T., Aoki, T., and Yamaguchi, T. (2012) Deposition of micrometer particles in pulmonary airways during halation and breathholding, Journal of Biomechanics45, 1809-1815.), microspheres less than 0.5 μm and greater than 5 μm cannot be deposited on the surface of the alveoli for a long time to exert the drug effect

Method used

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  • Hollow drug carrying microsphere used for pulmonary drug delivery and preparation method thereof
  • Hollow drug carrying microsphere used for pulmonary drug delivery and preparation method thereof
  • Hollow drug carrying microsphere used for pulmonary drug delivery and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] The molecular weight of 0.50g is that the polylactic acid of 10,000 is dissolved in the chloroform of 5ml, and add 1ml to contain the aqueous solution of 0.01g bovine serum albumin (used to simulate protein medicine), mechanically stir 8000rpm and stir 1min, this emulsion is added to 40ml of 5wt% gelatin aqueous solution, and then pass the emulsion through a 5.3 μm microporous membrane device to obtain the final emulsion, then stir the emulsion at room temperature for 6 hours to remove the oil phase solvent, and finally wash and dry to obtain the product. Its drug load is 1.2%, and the encapsulation efficiency is 60%.

[0063] Its scanning electron microscope pictures are as figure 1 , the particle size distribution is as figure 2 .

[0064] Depend on figure 1 It can be seen that the obtained hollow drug-loaded microspheres have better sphericity.

[0065] Depend on figure 2 It can be seen that the particle size of the microspheres is between 1-5 μm.

Embodiment 2

[0067] 0.40 g of poly(lactic acid-glycolic acid) with a molecular weight of 30,000 was dissolved in 6 ml of ethyl acetate, and 0.4 ml of an aqueous solution containing 0.04 g of bovine serum albumin was added, mechanically stirred at 8000 rpm for 2 min, and the emulsion was added to 30 ml of 3wt% polyvinylpyrrolidone aqueous solution, and then pass the emulsion through a 6.5 μm microporous membrane device to obtain an emulsion, then stir the emulsion at room temperature for 4 hours to remove the oil phase solvent, and finally wash and dry to obtain the product. Its drug loading capacity is 6.8%, and its encapsulation efficiency is 68%.

[0068] Its scanning electron microscope pictures are as image 3 , the particle size distribution is as Figure 4 .

[0069] Depend on image 3 It can be seen that the obtained hollow drug-loaded microspheres have better sphericity.

[0070] Depend on Figure 4 It can be seen that the particle size of the microspheres is between 1-5 μm. ...

Embodiment 3

[0072] Add sebacic acid (10.0 g) into acetic anhydride (100 mL), heat at 50° C. and reflux for 30 min under nitrogen protection, and distill under reduced pressure to obtain a crude prepolymer. The crude product was washed with petroleum ether-diethyl ether (1:1), filtered, and dried in vacuo (35° C.) for 24 h. Subsequently, the sebacic acid prepolymer was added into the reactor, and reacted at 260° C. for 3.5 hours. Nitrogen gas was injected for 1 min at intervals of 15 min. The obtained crude product was dissolved in chloroform, and n-hexane was added dropwise to the solution while stirring. The precipitate was filtered off and washed with ether. The product was dried under vacuum at 35°C for 24h.

[0073] Dissolve 0.6 g of polysebacic anhydride with a molecular weight of 10,000 in 15 ml of chloroform, and add 1 ml of an aqueous solution containing 0.04 g of bovine serum albumin, mechanically stir at 8000 rpm for 2 min, and add the emulsion to 100 ml of 1.5% wt of sodium...

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Abstract

The present invention provides a hollow drug carrying microsphere used for pulmonary drug delivery and a preparation method thereof. The method is as follows: dissolving a drug in water to form an inner aqueous phase W1; dissolving a biodegradable polymer material into an organic solvent to form an oil phase O; adding the inner aqueous phase W1 into the oil phase O for emulsification for formation of W1 / O emulsion; adding the W1 / O emulsion into an external aqueous phase W2containing a stabilizer to form W1 / O / W2 pre-emulsion; passing the W1 / O / W2 pre-emulsion through a microporous membrane for emulsification to obtain W1 / O / W2 emulsion; and removing an organic solvent of the oil phase of the W1 / O / W2 emulsion to solidify the oil phase, and then washing and freeze-drying to obtain the hollow drug carrying microsphere. According to the method, by use of a membrane emulsification technology, controlled particle size and narrow particle size distribution of the drug carrying microsphere can be ensured. The particle size distribution of the drug carrying microsphere is between 0.5-5mum, the drug loading amount is 1%-13%, the encapsulation efficiency is 50%-82%, and the drug carrying microsphere has good biocompatibility, can instantly release or continuously release 5 hours-30 days, and drug dosage and side effects can be reduced.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a hollow drug-loaded microsphere for pulmonary administration and a preparation method thereof. Background technique [0002] At present, drug-loaded microspheres occupy a very important position in new pharmaceutical preparations. They refer to tiny spherical bodies formed by drug dispersion or adsorption in polymer materials. The diameter of the microspheres is generally 1-500 μm (usually 5-250 μm) ). According to different routes of administration, it can be divided into injection administration, oral administration, pulmonary administration and skin administration, etc. Compared with other routes of administration, pulmonary administration has a large absorption area (approximately 140m 2 ), rich blood flow at the absorption site, can avoid the first-pass effect of the liver, low enzyme activity, thin epithelial barrier and high membrane permeability (membrane thickness ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/113A61K47/34A61P11/00
Inventor 郭宝华赵睿徐军
Owner TSINGHUA UNIV
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