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Long-circulating rabeprazole liposome composition and preparation method and application thereof

A technology of rabeprazole fat and rabeprazole, which is applied in the field of long-circulation rabeprazole liposome composition and its preparation, can solve the instability of rabeprazole oral preparations and the leakage of drug phospholipid bimolecules , particle size and distribution increase, etc., to achieve good product stability, solve thermal discoloration, and improve bioavailability

Inactive Publication Date: 2015-04-29
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Clinically, rabeprazole has the following disadvantages: ①Rabeprazole sodium is stable under strong alkaline conditions, and its pH value is adjusted to a maximum of 12. It is beyond the tolerance range of the human body, and there is a certain safety risk; ② Rabeprazole is easily decomposed and deteriorated when exposed to light, heat, oxidation and acid, and a considerable part of it produces sulfonyl compounds (inactive ingredients). ③ Oral preparations of rabeprazole are extremely unstable under acidic conditions, and if taken directly orally, they will be degraded in gastric acid, making the bioavailability significantly lower; ④ When Rabeprazole ordinary injection is compatible with glucose solution , there will be a sauce yellow phenomenon, which proves that rabeprazole has been destroyed in large quantities, and there is a certain risk of injection
[0010] The stability of liposomes is an important issue that limits the development of liposome formulations. When freeze-drying or spray drying makes liposomes, after liposome reconstitution Its particle size is generally doubled, so it is easy to coagulate, fuse, and settle during the reconstitution process, resulting in a significant increase in particle size and distribution, and the drug is easy to leak from the phospholipid bimolecule

Method used

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  • Long-circulating rabeprazole liposome composition and preparation method and application thereof
  • Long-circulating rabeprazole liposome composition and preparation method and application thereof
  • Long-circulating rabeprazole liposome composition and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1 Preparation of long-circulation rabeprazole liposome freeze-dried powder injection

[0062] Prescription: (1000 bottles)

[0063] Component Dosage

[0064] Rabeprazole 20g

[0065] Hydrogenated Soy Phosphatidylcholine 120g

[0066] Cholesterol 60g

[0067] Cultured Phosphatidylethanolamine 10g

[0068] α-Tocopherol 0.4g

[0069] Edetate Calcium Sodium 0.4g

[0070] Trehalose 60g

[0071] Preparation Process:

[0072] (1) Add 20g of rabeprazole, 120g of hydrogenated soybean phosphatidylcholine, 60g of cholesterol and 0.4g of α-tocopherol into 2000ml of ethanol, heat to 45°C, stir and disperse evenly, and filter through a 0.22μm organic membrane;

[0073] (2) Add 60g of trehalose and 0.4g of calcium sodium edetate to 2000ml of 10mmol / L phosphate buffer solution (pH = 7.0), shake and stir to dissolve, filter through a 0.22μm water membrane, and store at 45°C Lower heat preservation;

[0074] (3) Slowly add the solution prepared in step (1) into the ...

Embodiment 2

[0079] Example 2 Preparation of long-circulation rabeprazole liposome freeze-dried powder injection

[0080] Prescription: (1000 bottles)

[0081] Component Dosage

[0082] Rabeprazole 20g

[0083] Distearoylphosphatidylcholine 80g

[0084] Cholesterol 20g

[0085] Cultured Phosphatidylethanolamine 20g

[0086] α-Tocopherol 0.6g

[0087] Edetate Disodium 0.6g

[0088] Trehalose 50g

[0089] Preparation Process:

[0090] (1) Add 20g of rabeprazole, 100g of distearoylphosphatidylcholine, 40g of cholesterol and 0.6g of α-tocopherol into 1600ml of ethanol and tert-butanol solution with a volume ratio of 3:1, heat to 45°C and stir Uniform dispersion, 0.22μm organic membrane filtration;

[0091] (2) Add 50g trehalose and 0.6g edetate disodium into 1600ml citrate buffer solution (pH = 7.0) with a concentration of 10mmol / L, shake and stir to dissolve, filter through a 0.22μm water membrane, and filter at 45 Keep warm at ℃;

[0092] (3) Slowly add the solution item obtai...

Embodiment 3

[0097] Example 3 Preparation of long-circulation rabeprazole liposome freeze-dried powder injection

[0098] Prescription: (1000 bottles)

[0099] Component Dosage

[0100] Rabeprazole 20g

[0101] Dipalmitoyl Phosphatidylcholine 160g

[0102] Cholesterol 50g

[0103] Cultured Phosphatidylethanolamine 20g

[0104] α-Tocopherol 1.0g

[0105] Edetate Calcium Sodium 1g

[0106] Sucrose 20g

[0107] Preparation Process:

[0108] (1) Add 20g of rabeprazole, 130g of hydrogenated soybean phosphatidylcholine, 50g of cholesterol, 20g of cultured phosphatidylethanolamine and 0.7g of α-tocopherol into 2000ml of ethanol, heat to 45°C and stir to disperse evenly. membrane filtration;

[0109] (2) Add 60g of sucrose and 1g of calcium sodium edetate to 2000ml of 10mmol / L phosphate buffer solution (pH = 7.0), shake and stir to dissolve, filter through a 0.22μm water film, and keep warm at 45°C ;

[0110] (3) Slowly add the solution item obtained in step (1) into the solution item...

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Abstract

The invention relates to the field of medicinal preparations, specifically to a long-circulating rabeprazole liposome composition and its preparation method and application. The composition comprises rabeprazole, lecithin, cholesterol, Phosphatidylethanolamine Pegol, an antioxidant, metal chelate and a freeze-drying protective additive. The liposome injection provided by the invention has good re-dissolubility. After redissolution, particle size is uniform and stability is excellent. Quality of a preparation product is enhanced, half-life period of rabeprazole in the blood circulation system is prolonged, and bioavailability is higher.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a long-circulation rabeprazole liposome composition and its preparation method and application. Background technique [0002] Rabeprazole, chemical name: 2-[[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl]-1H-benzo Imidazole, molecular formula: C 18 h 20 N 3 o 3 S, molecular weight: 358.44, chemical structural formula: [0003] . [0004] Rabeprazole is a derivative of benzimidazole, a new type of proton pump inhibitor, without anticholinergic and anti-H2 histamine properties, but can be attached to gastric parietal cells by inhibiting the H+ / Na+-ATPase of gastric parietal cells to reduce gastric acid secretion. This enzyme system is regarded as an acid proton pump, so rabeprazole sodium acts as a proton pump inhibitor in the stomach to block the production of gastric acid, and this effect is dose-related. Animal experiments have confirmed that rab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/19A61K9/20A61K31/4439A61P1/04
Inventor 陈庆财伏世建蔡继兰刘留成金雪锋
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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