Cilostazol liposome solid agent

A technology of cilostazol lipid and cilostazol, which is applied in the field of pharmacy, can solve the problems of low drug loading, large toxic and side effects, and low encapsulation efficiency, and achieve reduction of toxic and side effects, simplified preparation method, and high encapsulation efficiency. Improved effect

Active Publication Date: 2020-12-01
药大制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent improves the solubility, stability and bioavailability of cilostazol liposomes through liposomes, but the encapsulation efficiency of cilostazo

Method used

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  • Cilostazol liposome solid agent

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Experimental program
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Effect test

Example Embodiment

[0029] Example 1

[0030] Raw materials and their quality: cilostazol 14g, dioleoyl phosphatidylcholine 10g, dimyristoyl phosphatidylcholine 8g, poloxamer P188 3g, cholesterol succinate monoester 5g, lactose 16g, carboxymethyl Sodium starch base 0.5g, microcrystalline cellulose 1g, magnesium stearate 0.5g, acetic acid 3.5g, acetic acid-sodium acetate buffer 86g with pH value of 6-6.5;

[0031] Preparation:

[0032] (1) Add the acetic acid of the above-mentioned mass parts into the pear-shaped bottle, place it in an ice-water bath of 8~12° C. and stir, with a stirring speed of 150rpm~200rpm, add the cilostazol of the above-mentioned mass parts to dissolve, and then add the above-mentioned mass parts of Dioleoylphosphatidylcholine, dimyristoylphosphatidylcholine, poloxamer P188, cholesterol succinic acid monoester, continue to stir to form a uniform lipid film solution;

[0033] (2) adding the acetic acid-sodium acetate buffer solution of the above-mentioned mass parts to the ...

Example Embodiment

[0037] Example 2

[0038]Raw materials and their quality: cilostazol 14g, dioleoyl phosphatidylcholine 18g, dimyristoyl phosphatidylcholine 14g, poloxamer P188 6g, cholesterol succinate monoester 8g, lactose 23g, carboxymethyl Starch sodium 0.9g, microcrystalline cellulose 3g, magnesium stearate 1.3g, acetic acid 3.5g, acetic acid-sodium acetate buffer 86g with pH value of 6-6.5;

[0039] Preparation:

[0040] (1) Add the acetic acid of the above-mentioned mass parts into the pear-shaped bottle, place it in an ice-water bath of 8~12° C. and stir, with a stirring speed of 150rpm~200rpm, add the cilostazol of the above-mentioned mass parts to dissolve, and then add the above-mentioned mass parts of Dioleoylphosphatidylcholine, dimyristoylphosphatidylcholine, poloxamer P188, cholesterol succinic acid monoester, continue to stir to form a uniform lipid film solution;

[0041] (2) adding the acetic acid-sodium acetate buffer solution of the above-mentioned mass parts to the lipid...

Example Embodiment

[0045] Example 3

[0046] Raw materials and their quality: cilostazol 14g, dioleoyl phosphatidylcholine 27g, dimyristoyl phosphatidylcholine 22g, poloxamer P188 10g, cholesterol succinate monoester 12g, lactose 32g, carboxymethyl 15g sodium starch base, 8g microcrystalline cellulose, 2g magnesium stearate, 3.5g acetic acid, 86g acetic acid-sodium acetate buffer with pH value of 6-6.5;

[0047] Preparation:

[0048] (1) Add the acetic acid of the above-mentioned mass parts into the pear-shaped bottle, place it in an ice-water bath of 8~12° C. and stir, with a stirring speed of 150rpm~200rpm, add the cilostazol of the above-mentioned mass parts to dissolve, and then add the above-mentioned mass parts of Dioleoylphosphatidylcholine, dimyristoylphosphatidylcholine, poloxamer P188, cholesterol succinic acid monoester, continue to stir to form a uniform lipid film solution;

[0049] (2) adding the acetic acid-sodium acetate buffer solution of the above-mentioned mass parts to the ...

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Abstract

The invention discloses a cilostazol liposome solid agent. The agent is prepared by a following method: dissolving cilostazol in acetic acid, and mixing an obtained mixture with dioleoyl phosphatidylcholine, dimyristoyl phosphatidylcholine, poloxamer P188 and cholesterol succinic acid monoester to form a lipid membrane solution; then adding an acetic acid-sodium acetate buffer solution and carrying out dispersion and emulsification; adding lactose, sodium carboxymethyl starch, microcrystalline cellulose and magnesium stearate, performing mixing, and carrying out refined dispersion; and performing freeze drying. According to the preparation method, the cilostazol drug loading capacity and the cilostazol liposome encapsulation efficiency are improved, meanwhile, the preparation method is simpler, the technological process is shortened, and the raw materials in the production process are safe and non-toxic.

Description

technical field [0001] The invention relates to a cilostazol liposome solid, in particular to a cilostazol liposome solid and a preparation method thereof, belonging to the technical field of pharmacy. Background technique [0002] Cilostazol is a typical intracellular cAMP PDE (cyclic AMP phosphodiesterase) inhibitor, and it has been known that it inhibits platelet aggregation and dilates arteries by inhibiting PDE activity. It plays an important role in anti-inflammatory and anti-ulcer effects, lowering blood pressure, prevention and treatment of asthma and cerebral infarction, and improvement of cerebral circulation. [0003] Due to the low water solubility of cilostazol (≤1 μg / ml), and it has been demonstrated that orally administered cilostazol is mainly absorbed in the upper gastrointestinal tract and its absorption decreases as it moves to the lower gastrointestinal tract, currently, The marketed preparations of cilostazol mainly include tablets, capsules, granules a...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/10A61K47/12A61K47/24A61K47/26A61K47/28A61K47/36A61K47/38A61K31/4709A61P7/02A61P9/00A61P9/10A61P9/12A61P11/06A61P29/00
CPCA61K9/127A61K47/24A61K47/10A61K47/28A61K47/26A61K47/36A61K47/38A61K47/12A61K31/4709A61P7/02A61P29/00A61P9/12A61P11/06A61P9/10A61P9/00
Inventor 郝静梅周高翔
Owner 药大制药有限公司
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