A kind of cilostazol liposome solid formulation

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: 2022-03-25
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 cilostazol liposome solid preparations is low and the drug loading is low, while methanol and acetone As a solvent, the toxic and side effects are relatively large

Method used

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  • A kind of cilostazol liposome solid formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0031] Preparation:

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

[0033] (2) Add the above mass parts of acetic acid-sodium acetate buffer solutio...

Embodiment 2

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

[0039] Preparation:

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

[0041] (2) Add the above mass parts of acetic acid-sodium acetate buffer solutio...

Embodiment 3

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

[0047] Preparation:

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

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

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Abstract

The invention discloses a cilostazol liposome solid preparation, which is prepared by the following method: first dissolving cilostazol in acetic acid, and then mixing dioleoylphosphatidylcholine and dimyristoylphosphatidylcholine , poloxamer P188, cholesterol succinate monoester to form a lipid film solution; then add acetic acid-sodium acetate buffer for dispersion and emulsification; then add lactose, sodium carboxymethyl starch, microcrystalline cellulose, magnesium stearate , finely dispersed after mixing; freeze-dried. The invention improves the drug loading capacity of cilostazol and the encapsulation rate of liposome of cilostazol, and at the same time, 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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Patent Type & Authority Patents(China)
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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