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Alendronate sodium powder inhalation used for respiratory drug delivery and preparation method and application thereof

A technology of alendronate sodium and powder spray, applied in the field of alendronate sodium powder spray, can solve the problems of low efficiency, increased risk of side effects such as kidney toxicity, etc., and achieves simple production and preparation process, prevention and safety. The effect of overcoming side effects and reducing side effects

Active Publication Date: 2016-06-08
杭州东博医药科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the characteristic of alendronate sodium entering the blood, most of it is quickly excreted through the kidneys, and a small part is deposited in the bones, so the efficiency of absorbing into the blood and indirectly to the respiratory tract is very low, and the side effects such as renal toxicity are increased. The risk of such a small particle size of alendronate sodium micropowder and its powder is not ideal for COPD or asthma medication

Method used

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  • Alendronate sodium powder inhalation used for respiratory drug delivery and preparation method and application thereof
  • Alendronate sodium powder inhalation used for respiratory drug delivery and preparation method and application thereof
  • Alendronate sodium powder inhalation used for respiratory drug delivery and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0196] Get 1000g of alendronate sodium crude drug, and load it into the QS100 pulverizer. The pulverization condition is 0.7MPa pulverization pressure, 3 hours, pulverization 4 times, obtain alendronate sodium fine powder.

[0197] Determination of alendronate sodium content, with 6mg / capsule sub-packed in hard capsules to get final product. Laser particle size measurement results: British Malvern Instruments Ltd. laser particle size analyzers measured the particle size of capsule content powders of different batches. As a result, the percentage of the above-mentioned samples with a particle size of less than 20 μm was greater than 90%, while the percentage of the portion with a particle size of less than 5 μm was less than 50%. Observe the capsule content powder with an electron microscope. Under a 10,000-fold SEM electron microscope, it can be seen that the powder is a single fine particle with no adhesion, no agglomerates, good dispersion, and an irregular three-dimensiona...

Embodiment 2

[0200] Get 50g of alendronate sodium crude drug, and load it into the AO pulverizer. The pulverization conditions were 0.7 MPa pulverization pressure, 2.5 hours, and pulverization twice. Obtain alendronate sodium micropowder. Determination of alendronate sodium content, with 2mg / capsule sub-package in hard capsules to get final product. Laser particle size measurement results: British Malvern Instruments Ltd. laser particle size analyzers measured the particle size of capsule content powders of different batches. As a result, the percentage of the above-mentioned samples with a particle size of less than 20 μm was greater than 90%, while the percentage of the portion with a particle size of less than 5 μm was less than 50%. Observe the capsule content powder with an electron microscope. Under a 10,000-fold SEM electron microscope, it can be seen that the powder is a single fine particle with no adhesion, no agglomerates, good dispersion, and an irregular three-dimensional st...

Embodiment 3

[0203] The alendronate sodium nebulizer prepared in Example 1 was used to measure the droplet distribution with an atomization absorption device, and 12.7% was deposited in the primary distribution bottle; 78.2% was deposited in the secondary distribution bottle. After the administration of the alendronate sodium powder spray in this example, the lungs of the rats were taken for HPLC analysis, and the results showed that the lung volume was 83.40% to 92.2%.

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Abstract

The invention provides alendronate sodium powder inhalation used for respiratory drug delivery and a preparation method and application thereof. Alendronate sodium powder inhalation includes single-component alendronate sodium micro powder and does not include auxiliary materials. In the production and preparation process of the alendronate sodium micro powder, other auxiliary materials or solvents are not involved, and alendronate sodium raw material medicine is directly smashed to prepare the alendronate sodium micro powder. The alendronate sodium powder inhalation can improve the breathing function of a chronic obstructive pulmonary disease (COPD) rat by about 40% and has a better effect than salbutamol sulfate with a common usage amount, and drug resistance of salbutamol sulfate and other beta2 receptor stimulants can be eliminated. The powder inhalation mainly makes sedimentation in the trachea, bronchia, bronchiole and other pulmonary respiratory ducts to directly take effect after drug-delivery inhalation, the diastolic function of the respiratory ducts becomes effective rapidly, and the drug effect lasts for a long time; the alendronate sodium powder inhalation enters pulmonary alveoli, is low in absorption and blood-entering amount, can avoid systematic side effects and is suitable for being developed to be a drug for treating COPD and asthma.

Description

technical field [0001] The invention belongs to the field of pharmacy and pharmaceutics, and relates to an alendronate sodium powder mist for respiratory tract administration and its preparation method and application, especially alendronate, which is mainly deposited in the respiratory tract after inhalation and directly exerts its drug effect. Sodium Phosphonate Powder. Background technique [0002] Alendronate sodium (Alendronate) is a small molecular compound drug with a molecular weight of 249.97, which is similar in structure to sodium aminopyrophosphate. The existing dosage form is oral tablet, the main effect is to hinder bone reabsorption, and is used for treating and preventing osteoporosis in postmenopausal women. The pharmacological mechanism of its action is based on the affinity of alendronate sodium for bone hydroxyapatite crystals, selectively inhibiting osteoclastic resorption during the bone remodeling cycle. In 1995, the US FDA approved alendronate sodiu...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/663A61P19/10A61P11/06A61P11/00A61P29/00
CPCA61K31/663A61K9/0073A61K9/14
Inventor 陈燃陆泉张婕褚梦思
Owner 杭州东博医药科技开发有限公司
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