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Sulphur butyl ether-beta-cyclodextrin clathrate compound of cinnarizine, formulated product and preparation method thereof

A technology of cyclodextrin inclusion compound and sulfobutyl ether, which is applied in the field of medicine, can solve the problems of poor thermal stability, low drug concentration in solution injections, and poor drug safety and patient compliance.

Inactive Publication Date: 2008-12-03
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, cinnarizine is almost insoluble in water, and the concentration of traditional injection is only 20mg / 20mL after adding an organic solubilizer, so the drug safety and patient compliance are poor
Moreover, its solution type injection contains a lower drug concentration, and its thermal stability is much worse than that of solid preparations.

Method used

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  • Sulphur butyl ether-beta-cyclodextrin clathrate compound of cinnarizine, formulated product and preparation method thereof
  • Sulphur butyl ether-beta-cyclodextrin clathrate compound of cinnarizine, formulated product and preparation method thereof
  • Sulphur butyl ether-beta-cyclodextrin clathrate compound of cinnarizine, formulated product and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Preparation of Sulfobutyl Ether-β-Cyclodextrin Inclusion Compound of Cinnarizine

[0079] Ingredients Dosage

[0080] Cinnarizine 2.7×10 -2 mol

[0081] Sulfobutyl ether-β-cyclodextrin 13.4×10 -2 mol

[0082] Hydrochloric acid amount

[0083] Appropriate amount of sodium hydroxide

[0084] Dissolve the prescribed amount of sulfobutyl ether-β-cyclodextrin in about 600 mL of water for injection, and adjust the pH to 1.0-2.0 with hydrochloric acid. Take another prescribed amount of cinnarizine and add it to the above solution, stir and ultrasonically dissolve it, then add sodium hydroxide to adjust the pH to 3.0, which is the clathrate solution. The clathrate solution is freeze-dried to obtain white clathrate powder.

[0085] Note:

[0086] 1. The amount of cinnarizine in the prescription can be increased or decreased according to the specific situation, and the range is not limited.

[0087] 2. In the prescription, the molar ratio of CN:SBE-β-CD can be selected a...

Embodiment 2

[0089] Preparation of Sulfobutyl Ether-β-Cyclodextrin Inclusion Compound of Cinnarizine

[0090] The clathrate solution in Example 1 was spray-dried to obtain white clathrate powder.

Embodiment 3

[0092] Preparation of inclusion compound injection powder (freeze-drying method)

[0093] Add appropriate amount of proppants or excipients (such as mannitol, sorbitol, xylitol) to the clathrate solution in Example 1, any one or any of isotonic regulators (sodium chloride, citric acid, etc.) Mixture of two or more), stir or (and) ultrasonic to make into a homogeneous solution. After adding an appropriate amount of activated carbon and stirring to remove pyrogens, filter to remove carbon. Then filter with a 0.22μm microporous membrane, and add water for injection to 1000mL. Aseptically fill in vials, 2mL / bottle, freeze-dry, stopper and cap to obtain freeze-dried powder for injection.

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Abstract

the invention belongs to the drug technical field, disclosing a sulphur butyl ether-beta- cyclodextrin(SBE-beta-CD) clathrate compound of cinnarizine, a preparation thereof and a preparation method thereof. The water soluble beta- cyclodextrin derivative SBE-beta-CD is used as a coating material to prepare the cinnarizine clathrate compound. The process comprises the following steps that: the BE-beta-CD is dissolved in proper amount of water, the pH value is adjusted by hydrochloric acid, the cinnarizine is added in the mixed solution and stirred for ultrasonic dissolution, the mixed solutionobtained is added with sodium hydroxide to adjust the pH value, a clathrate solution is obtained, and the clathrate solution is subject to freeze drying or spray drying to form clathrate compound powder; the clathrate compound solution obtained is subject to degerming, pyrogen removal, sterile filling and freeze drying to obtain freeze-dry powder needles for injection; the clathrate compound solution is subject to spray drying, and the obtained powder is directly subject to sterile subpackaging or mixed with proper amount of auxiliary materials for sterile subpackaging; and the clathrate compound powder can be mixed with other auxiliary materials to prepare tablets, capsules and particles, etc. according to requirements.

Description

Technical field: [0001] The invention relates to the technical field of medicine, and relates to a sulfobutyl ether-beta-cyclodextrin inclusion compound of cinnarizine, a formulation and a preparation method thereof. Inclusion complex preparations include injection powders, tablets, capsules, granules and the like. Background technique: [0002] Cinnarizine (CN) is a new type of diphenylpiperazine calcium ion channel antagonist, which has the effect of dilating vascular smooth muscle and can significantly improve coronary circulation and cerebral circulation. , bradykinin, vasopressin, dopamine, etc. have antagonistic effects, can relieve vasospasm, and prevent vascular embrittlement at the same time. Oral administration has no effect on blood pressure. After intravenous injection, it can cause a short-term drop in blood pressure, but it is absorbed quickly. The antispasmodic effect is stronger than papaverine, but weaker than flunarizine. The drug is currently mainly use...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/40A61K31/495A61P9/12A61P9/10A61P9/08A61K47/69
Inventor 何仲贵王安娜王永军
Owner SHENYANG PHARMA UNIVERSITY
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