Asarin composite freeze-dried powder for injection

A technology of freeze-dried powder injection and asarone, which is applied in the direction of freeze-dried delivery, drug combination, powder delivery, etc., can solve the problems of large proportion of excipients added, many types of excipients, and unsatisfactory reconstitution effect, etc., to achieve guaranteed The effects of stability, improving solubility, and reducing the amount of excipients

Active Publication Date: 2011-06-08
SHANDONG LUOXIN PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The defect of this patent is that there are many types of auxiliary materials added, and the proportion of auxiliary materials added is large, and the reconstitution effect is still not ideal

Method used

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  • Asarin composite freeze-dried powder for injection
  • Asarin composite freeze-dried powder for injection
  • Asarin composite freeze-dried powder for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The composition is:

[0046] Asarum 8.0g

[0047] 95% ethanol 40ml

[0048] Mannitol 80.0g

[0049] Add water for injection to 1000ml

[0050] After lyophilization, 500 bottles are made.

[0051] (1) Prepare a 0.1% polysorbate-80 deionized water solution as an anti-solvent;

[0052] (2) Prepare an ether solution with a mass percentage of 0.1g / ml asarone as a solvent;

[0053] (3) Under the conditions of 2~6℃ and stirring speed of 600 rpm, add solvent to the anti-solvent quickly, and the volume ratio of solvent to anti-solvent is 1:15; after white crystals are produced, the crystals and solution are heated at 42℃ Aging for 2 hours under the conditions, filtering, washing, filter cake dispersion and spray drying; the obtained ultrafine particles of Asarone are obtained by laser particle size measuring instrument to obtain CSD curve and figure 1 the same;

[0054] (4) Dissolving the superfine particles of Asarone in 95% ethanol in proportion to obtain liquid A;

[0055] (5) Dissolve ma...

Embodiment 2

[0058] The prescription is:

[0059] Asarum 8.0g

[0060] 100% ethanol 80ml

[0061] Mannitol 80.0g

[0062] Add water for injection to 1000ml

[0063] After lyophilization, 500 bottles are made.

[0064] (1) Prepare a 0.5% polysorbate-80 deionized water solution as an anti-solvent;

[0065] (2) Prepare an ether solution with a mass percentage of 1g / ml Asarone as a solvent;

[0066] (3) Under the conditions of 6°C and stirring speed of 1200 rpm, the solvent was quickly added to the anti-solvent, and the volume ratio of the solvent to the anti-solvent was 1:21; after white crystals were produced, the crystals and the solution were kept at 55°C After aging for 5 hours, after filtering, washing, filter cake dispersion and spray drying, the obtained ultrafine particles of Asarone are obtained by laser particle size measuring instrument to obtain CSD curve and figure 1 the same;

[0067] (4) Dissolving the ultrafine particles of Asarone in 100% ethanol in proportion to obtain liquid A;

[0068]...

Embodiment 3

[0071] The prescription is:

[0072] Asarum 6.0g

[0073] 98% ethanol 40ml

[0074] Mannitol 24.0g

[0075] Add water for injection to 1000ml

[0076] After lyophilization, 500 bottles are made.

[0077] (1) Prepare a 0.25% polysorbate-80 mass percent deionized water solution as an anti-solvent;

[0078] (2) Prepare an ether solution with a mass percentage of 0.5g / ml asarone as a solvent;

[0079] (3) Under the conditions of 4℃ and stirring speed of 1000 rpm, add solvent to the anti-solvent quickly, and the volume ratio of solvent to anti-solvent is 1:20; after white crystals are produced, the crystals and solution are kept at 45℃ After aging for 3 hours, filtering, washing, filter cake dispersion and spray drying; the obtained ultrafine particles of Asarone were obtained by laser particle size measuring instrument to obtain the CSD curve and figure 1 the same;

[0080] (4) Dissolving the ultrafine particles of Asarone in 98% ethanol in proportion to obtain liquid A;

[0081] (5) Dissolve ...

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Abstract

The invention relates to an asarin injection preparation and in particular relates to an asarin composite aseptic freeze-dried powder preparation for injection. The asarin composite freeze-dried powder for injection comprises 4 to 8 grams of asarin, 40 to 80ml of ethanol of which the volume ratio is between 95 and 100 percent and 24 to 80 grams of mannitol. The raw materials is added with water for injection to a volume of 1,000 to 2,000ml and the obtained product is freeze-dried to prepare 500 to 1,000 bottles of the freeze-dried powder, wherein the asarin is ultrafine particles prepared by an anti-solvent crystallization method. The asarin composite preparation for injection also comprises 0.01 to 10 grams of polysorbate-80, preferably 1 to 8 grams of polysorbate-80. Due to adoption of the ultrafine particles of the asarin, which is prepared by the anti-solvent crystallization method, the asarin composite aseptic freeze-dried powder preparation for injection greatly improves solubility property of the asarin so as to obtain the freeze-dried powder preparation with excellent stability and redissolution property by adding a small quantity of cosolvent or without adding the cosolvent when preparing the asarin preparation.

Description

Technical field [0001] The invention relates to an injection preparation of Asarone, in particular to a sterile freeze-dried powder injection preparation of Asarone composition for injection. Background technique [0002] Asarum (2,4,5-trimethoxy-1-propenylbenzene), mainly exists in the volatile oil of Araceae plant Acorus calamus and other plants. Tests have shown that this product can obviously prevent asthma attacks and is close to waiting. Because of its antitussive effect, it also has certain choleretic and sedative effects. Clinically, it is mainly used for the treatment of bronchial asthma, chronic bronchitis, pneumonia and chronic obstructive pulmonary disease with acute inflammation of the lungs. [0003] In recent years, due to the increase of air pollution and the development of the chemical industry, the incidence of asthma has gradually increased. In the 1940s, the incidence of asthma in developed countries was about 0.5%. According to reports in the United States, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/09A61P11/06A61P11/00
Inventor 李明华宋显荣郭中明
Owner SHANDONG LUOXIN PHARMA GRP CO LTD
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