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Hydrochloric acid Fasudil liposome injection and new application thereof

A technology of fasudil hydrochloride and fasudil hydrochloride, which is applied in the field of liposome injection of fasudil hydrochloride and its preparation, can solve problems such as poor stability, achieve the improvement of curative effect, increase the encapsulation rate, The effect of reducing leakage

Inactive Publication Date: 2009-12-16
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] For the poor stability of current fasudil hydrochloride injection, the object of the present invention is to provide a stable fasudil hydrochloride injection, specifically, through the combination of a certain amount of excipients and active ingredients, using pH value gradient method makes Fasudil hydrochloride liposome injection of the present invention, well solved the above-mentioned problems of Fasudil hydrochloride injection, obtains satisfactory technical effect

Method used

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  • Hydrochloric acid Fasudil liposome injection and new application thereof
  • Hydrochloric acid Fasudil liposome injection and new application thereof
  • Hydrochloric acid Fasudil liposome injection and new application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1 Preparation of Fasudil Hydrochloride Liposomes

[0061] Prescription (1000 sticks):

[0062] Fasudil Hydrochloride 15g

[0063] Dilauroyl Phosphatidylglycerol 180g

[0064] Cholesterol 90g

[0065] Polysorbate 80 30g

[0066] Sodium chloride 11.7g

[0067] Citric acid-sodium citrate buffer solution with pH 4.5 300ml

[0068] Preparation Process

[0069] (1) Dissolve 180g of dilauroylphosphatidylglycerol, 90g of cholesterol and 30g of polysorbate 80 in 1000ml of hexane, slowly inject 1000ml of 0.05mol / L ammonium sulfate solution under stirring, heat and stir to remove n-hexane, place in an ice bath Ultrasound for 20 minutes to obtain blank liposomes;

[0070] (2) Blank liposome is placed in the dialysis bag, seals, and the dialysis bag is placed in 0.9% sodium chloride aqueous solution 975ml and dialyzes for 22 hours, removes the ammonium sulfate in the liposome external phase;

[0071] (3) Dissolve 15g of fasudil hydrochloride in 500ml of water, hea...

Embodiment 2

[0080] Example 2 Preparation of Fasudil Hydrochloride Liposomes

[0081] Prescription (1000 sticks):

[0082] Fasudil Hydrochloride 30g

[0083] Dioleoylphosphatidylglycerol 120g

[0084] Cholesterol 24g

[0085] Polysorbate 80 150g

[0086] Glycerin 300g

[0087] Phosphoric acid-dipotassium hydrogen phosphate buffer solution at pH 5.2 500ml

[0088] Preparation Process

[0089] (1) Dissolve 120g of dioleoylphosphatidylglycerol, 24g of cholesterol and 150g of polysorbate 80 in 1200ml of methanol, slowly inject 1200ml of 0.02mol / L ammonium sulfate solution under stirring, heat and stir to remove the methanol, put it in an ice bath and sonicate 20min, get blank liposome;

[0090] (2) Blank liposome is placed in the dialysis bag, seals, and the dialysis bag is placed in 1125ml of 20% glycerol aqueous solution and dialyzes for 20 hours, removes the ammonium sulfate in the liposome external phase;

[0091] (3) Dissolve 30g of fasudil hydrochloride in 800ml of water, kee...

Embodiment 3

[0104] Example 3 Preparation of Fasudil Hydrochloride Liposomes

[0105] Prescription (1000 sticks):

[0106] Fasudil Hydrochloride 15g

[0107] Soy Phosphatidylinositol 120g

[0108] Cholesterol 60g

[0109] Polysorbate 80 55g

[0110] Glucose 65g

[0111] Phosphoric acid-disodium hydrogen phosphate buffer solution with a pH value of 5.8 300ml

[0112] Preparation Process

[0113] (1) Dissolve 120g of soybean phosphatidylinositol, 60g of cholesterol and 55g of polysorbate 80 in 1000ml of acetone, slowly inject 1000ml of 0.1mol / L ammonium sulfate solution under stirring, heat and stir to evaporate the acetone, and put it in an ice bath for 10 minutes of ultrasound , to obtain blank liposomes;

[0114] (2) Place the blank liposome in the dialysis bag, seal it, place the dialysis bag in 975ml of 5% glucose aqueous solution and dialyze for 22 hours, remove the ammonium sulfate in the liposome external phase;

[0115] (3) Dissolve 15g of fasudil hydrochloride in 500ml ...

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Abstract

The invention discloses hydrochloric acid Fasudil liposome injection and new application thereof. The injection mainly comprises the following components according to parts by weight: 1 part of hydrochloric acid Fasudil, 2 to 20 parts of phospholipid, 0.5 to 10 parts of cholesterol and 1 to 8 parts of polysorbate 80. Simultaneously, the hydrochloric acid Fasudil liposome injection also can be used for treating vertebral artery type cervical spondylosis.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to a liposome injection of fasudil hydrochloride and a preparation method thereof. It can also be used to treat vertebral artery type cervical spondylosis. Background technique [0002] Vertebral artery type cervical spondylosis is a common symptom type of cervical spondylosis, a class of syndromes and signs caused by insufficient blood supply of the vertebral artery system. Modern medicine believes that there are many pathogenic factors of vertebral artery insufficiency, mainly including: (1) the length balance between the vertebral artery and the cervical spine is destroyed, resulting in twisting and spasm of the vertebral artery and poor blood supply, causing insufficient oxygen supply in the brain; (2) Bone lesions and scar compression in the cervical spine; (3) Lesions in the vertebral artery; (4) Changes in the cardiovascular and blood systems; (5) Effects of cervical spine activitie...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/551A61K47/34A61P19/08A61P9/10A61K47/26
Inventor 王明
Owner HAINAN LINGKANG PHARMA CO LTD
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