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Dry powder inhalation, preparation method and application thereof

A dry powder inhaler, powder technology, applied in the field of pharmaceutical preparations, can solve problems such as difficulties

Inactive Publication Date: 2010-03-17
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the prior art, it is still difficult to effectively deliver drugs directly to the lesions of lung cancer—deep lung or alveoli

Method used

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  • Dry powder inhalation, preparation method and application thereof
  • Dry powder inhalation, preparation method and application thereof
  • Dry powder inhalation, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Prescription: Hydroxycamptothecin 50mg main drug

[0063] Lactose 5g Excipients

[0064] Leucine 0.5g Excipients

[0065] Ammonium carbonate 23g Foaming agent

[0066]Sodium hydroxide solution Appropriate amount pH adjuster

[0067] Distilled water 300mL solvent

[0068] Add the above-mentioned main ingredients, auxiliary materials and foaming agent into distilled water, stir to nearly dissolve, and adjust the pH to 10.5 with sodium hydroxide solution. Spray drying according to the following conditions: inlet temperature 130°C, liquid spray speed 3mL / min, hot air volume 90%, atomizing air flow rate 700L / hour, and prescription B was obtained. Repeat the above experiment without adding ammonium carbonate to obtain prescription A as a control.

[0069] Scanning electron micrographs of the spray-dried particles are shown in figure 1 A and figure 1 b. The results show that the addition of ammonium carbonate has a great influence on the appearance of the spray-dried p...

Embodiment 2

[0074] Prescription: recombinant human interferon α-2b (potency 1.6×10 8 IU / mg) main drug

[0075] Lactose Excipients

[0076] Lysine Excipients

[0077] Leucine Excipients

[0078] ammonium carbonate blowing agent

[0079] pH 7.0 Citric Acid-Disodium Hydrogen Phosphate Solvent

[0080] An appropriate amount of lactose was dissolved in a citric acid-disodium hydrogen phosphate buffer system with pH 7.0 to make a lactose solution with a concentration of 1.4%, and a small amount of lysine was added as an active protective agent for interferon and an appropriate amount of leucine (to make it The concentration is 6% of the solute content) as a dispersion aid. Add an appropriate amount of recombinant human interferon α-2b to make the concentration of interferon 1.12×10 6 IU / mL, finally add the ammonium bicarbonate of series concentration, make the content of ammonium bicarbonate be respectively 0%, 50%, 70%, 80%, 90% of solute content, spray dry according to the following con...

Embodiment 3

[0086] Prescription: Etoposide liposome main drug, solvent

[0087] Mannitol Excipients

[0088] Leucine Excipients

[0089] ammonium carbonate blowing agent

[0090] Take 0.2g of etoposide, 1.2g of soybean lecithin and 0.4g of cholesterol, dissolve in 25mL of chloroform, and remove the chloroform by rotary evaporation in a water bath at 30°C to obtain the etoposide-phospholipid complex; another 150mL of pH7.4 phosphate buffer solution was added to Into the above complex, ultrasonic treatment for 30 minutes, to obtain etoposide liposomes. Add 1g mannitol, 0.5g leucine and 7g ammonium carbonate to the liposome solution, spray dry according to the following conditions: inlet temperature 105°C, spray speed 3mL / min, hot air volume 90%, atomizing air flow rate 700L / Hour. The above experiment was repeated without adding ammonium carbonate as a control.

[0091] The deposition results showed that the deposition rate of the formulation without ammonium carbonate was only 11.2%, ...

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Abstract

The invention relates to a dry powder inhalation with low-density or ultralow-density inhalable medicinal powder, a method for preparing the dry powder inhalation and application of the dry powder inhalation in preparing medicament for treating tumor, in particular lung tumor. The dry powder inhalation can deliver the tumor medicament to the lung directly so as to improve the medicament effect andreduce side effect; and the 'foaming' technology adopted for preparing the dry powder inhalation optimizes the micromeritic properties of the medicinal powder, and greatly improves the deposition performance of the tumor medicinal dry powder inhalation. The dry powder inhalation, the preparation method and the application thereof are also suitable for preparing non-vector dry powder inhalation toovercome the defects of uneven mixture between medicament and vector easily occurring in the dry powder inhalation.

Description

technical field [0001] The present invention relates to a dry powder inhaler with low-density or ultra-low-density inhalable drug powder, a preparation method of the dry powder inhaler and the use of the dry powder inhaler in preparing medicines for treating tumors, especially lung tumors Applications. [0002] The invention belongs to the technical field of pharmaceutical preparations. Background technique [0003] In terms of preparation forms, inhalants mainly include liquid preparations for Inhations (Liquid Preparations for Inhations), metered-dose inhalers (Pressured Metered-Dose Preparations for Inhations, MDIs) and dry powder inhalers (Dry powder Inhations, DPIs). For metered dose inhalers. However, metered-dose inhalers have some disadvantages that are difficult to overcome, such as low transport efficiency (less than 20% of the labeled amount), containing Freon that destroys the ozone layer, and patients are not easy to coordinate the triggering of the device wit...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K9/14A61K45/00A61P35/00
Inventor 王成港王春龙江荣高薛艳
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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