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Particles of surface nanoscale coarse structure and preparation method and application thereof

A rough-structured, nano-scale technology, which can be used in medical preparations without active ingredients, medical preparations containing active ingredients, and pharmaceutical formulations, and can solve the problems of harsh condition control, low yield, and complicated steps.

Active Publication Date: 2016-05-04
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, a variety of methods for modifying the surface roughness of DPI carrier particles have been developed. For example, recrystallization under different conditions can obtain crystal forms with specific shapes or aspect ratios in a certain range. The recrystallization method requires strict control of conditions, and the steps Complicated, extremely low yield, poor product stability
Freeze-drying is also used to prepare carrier particles with rough surfaces. Although the product can be obtained in one step, this method has a wide range of particle size and shape distribution and poor particle fluidity, which is not the best choice for inhalation of carrier particles.

Method used

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  • Particles of surface nanoscale coarse structure and preparation method and application thereof
  • Particles of surface nanoscale coarse structure and preparation method and application thereof
  • Particles of surface nanoscale coarse structure and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Dissolve lactose, mannitol, trehalose, and chitosan in water respectively, and prepare solutions with a concentration of 20 mg / ml respectively, and then use a spray dryer to spray dry the above solutions to prepare single carrier particles. The parameters of spray drying are as follows: The air temperature is 140°C, the outlet air temperature is 87°C, the pump liquid rate is 7ml / min, the nozzle diameter is 0.71mm, the atomization pressure is 150Kpa, and the air flow rate is 0.60m 3 / h.

[0046] The spray-dried carrier granules are mixed with the micronized venlafaxine drug granules at a mass ratio of 20:1, and packed into No. 3 capsules (10 ± 0.5 mg / capsule), to obtain the venlafaxine dry powder inhaler. Next Generation Pharmaceutical Impactor (NGI, figure 2 ) to evaluate the in vitro drug deposition rate of venlafaxine dry powder inhalation.

[0047] Detection method: Take 1 capsule of the test product of the above-mentioned venlafaxine dry powder inhaler, and put it ...

Embodiment 2

[0053] Dissolve any two of lactose, mannitol, trehalose and chitosan in water at a mass ratio of 50:50 to prepare solutions with a concentration of 20 mg / ml, and then use a spray dryer to spray dry the above solutions to prepare Binary carrier particles, the parameters of spray drying are as follows: the air inlet temperature is 140°C, the air outlet temperature is 87°C, the pump liquid rate is 7ml / min, the nozzle diameter is 0.71mm, the atomization pressure is 150Kpa, and the air flow rate is 0.60m 3 / h.

[0054] The carrier particle after the spray drying is prepared venlafaxine dry powder inhaler by the method for embodiment 1, adopts new-generation pharmaceutical collider to measure the drug effective deposition rate of venlafaxine dry powder inhaler (detection method is the same as embodiment 1) , the results are shown in Table 1: the binary carrier particles prepared from mannitol and chitosan had the highest effective drug deposition rate, reaching 49.14%.

Embodiment 3

[0056] Dissolve mannitol and chitosan with a mass ratio of 50:50 in ethanol or water with a volume fraction of 30%, and prepare solutions with a concentration of 20 mg / ml respectively, and then use a spray dryer to spray dry the above solutions to prepare binary Carrier particles, spray drying parameters are as follows: air inlet temperature is 140°C, air outlet temperature is 87°C, pump liquid rate is 7ml / min, nozzle diameter is 0.71mm, atomization pressure is 150Kpa, air flow rate is 0.60m 3 / h.

[0057] The carrier particle after the spray drying is prepared venlafaxine dry powder inhaler by the method for embodiment 1, adopts the drug effective deposition rate of venlafaxine dry powder inhaler to measure venlafaxine dry powder inhaler by adopting new generation (detection method is the same as embodiment 1 ). The result is as image 3 It is shown that the carrier particle prepared by using 30% ethanol as the solvent has a higher effective drug deposition rate than the pu...

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Abstract

The invention relates to particles of a surface nanoscale coarse structure and a preparation method and application thereof. The particles of the surface nanoscale coarse structure are prepared through a method which comprises the steps that micromolecular sugar alcohol and macromolecular sugar are dissolved in water or an ethanol water solution, and the obtained solution is subjected to spray drying; the mass ratio of the micromolecular sugar alcohol to the macromolecular sugar is 10:90-90:10, the total concentration of the micromolecular sugar alcohol and the macromolecular sugar is 10-50 mg / ml, and the volume fraction of ethanol in the ethanol water solution is 1.0%-50.0%. The particles of the surface nanoscale coarse structure prepared through the method are of a shell-core structure, the core is the macromolecular sugar, and the shell is the micromolecular sugar alcohol; as a result, the particles have surfaces with proper roughness, and appropriate acting force can be generated between the particles and an active drug when the particles are used as a carrier of a dry powder inhaler, so that the effective deposition rate of the drug is increased, and the dry powder inhaler prepared from the carrier has high lung delivery efficiency.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a particle with a nanoscale rough structure on the surface, a preparation method thereof and an application thereof as a dry powder inhalation carrier. Background technique [0002] For specific lung diseases, such as cystic fibrosis, asthma, chronic lung infection or lung cancer, it is necessary to deliver drugs locally through the lungs to the patient. Compared with the oral route of administration, the main advantages of pulmonary administration include: (1) reduced systemic side effects and dosage, (2) avoiding the degradation of the active drug in the gastrointestinal tract environment and the hepatic first-pass effect, (3) Rapid onset of action: Large surface area of ​​lung absorption membrane (~100m 2 ) and thin (0.1 ~ 0.2μm), the blood flow rate is fast (5L / min). [0003] Drug delivery formulations for pulmonary inhalation can be mainly divided into ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/36A61K47/26A61K31/58A61K31/137
CPCA61K9/0073A61K9/1623A61K9/1652A61K9/1682A61K31/137A61K31/58
Inventor 潘昕黄莹彭婷婷张雪娟
Owner SUN YAT SEN UNIV
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