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Stable palmitic-acid paliperidone long-acting preparation

A technology of paliperidone and palmitic acid, which is applied in the field of medicine, can solve the problems of affecting product release and absorption process, slow release rate, particle aggregation, etc., achieve good resuspension, overcome particle size growth and release degree Reduced, good dispersibility effect

Active Publication Date: 2016-11-23
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this suspension is convenient for clinical administration, as a suspension of insoluble drugs, this product is prone to particle aggregation during storage, or particle size increase due to Ostwald ripening, etc. Phenomenon
For poorly soluble drugs, the aggregation of product particles or the increase in particle size can cause the release rate to slow down, thereby affecting the release and absorption process of the product in vivo

Method used

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  • Stable palmitic-acid paliperidone long-acting preparation
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  • Stable palmitic-acid paliperidone long-acting preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Example 1 Preparation of Paliperidone Palmitate Block Composition (Specification: 312mg / ml)

[0082] Prescription: Paliperidone Palmitate 312g

[0083] Polysorbate 80 for Injection 15g

[0084] Sodium Carboxymethyl Cellulose 12g

[0085] Mannitol 40g

[0086] Sodium dihydrogen phosphate 0.9

[0087] Sodium hydroxide to adjust the pH to 7

[0088] Add water for injection* to 1000ml;

[0089] (*Used in recipe but removed during processing)

[0090] Preparation Process:

[0091] (1) Preparation of Paliperidone Palmitate Sterile Suspension

[0092] A sterile jet mill was used to control the crushing pressure to 3-5 bar, and the sterile paliperidone palmitate was crushed to an effective particle size of 2-15 μm. Weigh 12g of sodium carboxymethylcellulose, put it in about 500ml of water for injection, swell and dissolve; then take 15g of polysorbate 80 for injection, 40g of mannitol, 0.9g of sodium dihydrogen phosphate, stir and dissolve, and dissolve with 0.5M hydro...

Embodiment 2

[0099] Example 2 Preparation of Paliperidone Palmitate Sterile Block Composition (Specification: 312mg / ml ）

[0100] Prescription: Paliperidone Palmitate 312g

[0101] Polysorbate 80 for Injection 15g

[0102] Sodium Carboxymethyl Cellulose 12g

[0103] Mannitol 40g

[0104] Sodium dihydrogen phosphate 0.9g

[0105] NaOH Adjust pH to 7.0

[0106] Add water for injection* to 1000ml

[0107] (*Used in recipe but removed during processing)

[0108] Preparation Process:

[0109] (1) Preparation of Paliperidone Palmitate Sterile Suspension

[0110] Weigh 12g sodium carboxymethylcellulose, put it in about 500ml water for injection, swell and dissolve; then take 15g polysorbate 80 for injection, 40g mannitol, 0.9g sodium dihydrogen phosphate, stir and dissolve, and dissolve with 0.5M hydrogen The sodium oxide solution was used to adjust the pH to 7.0. Weigh 312g of sterile paliperidone palmitate, mix and shear until uniformly dispersed, add water for injection, and adjus...

Embodiment 3

[0117] Example 3 Preparation of Paliperidone Palmitate Sterile Block Composition (Specification: 156mg / ml)

[0118] Prescription: Sterile Paliperidone Palmitate 156g

[0119] Polysorbate 80 for Injection 10g

[0120] Sodium Carboxymethyl Cellulose 8g

[0121] Mannitol 30g

[0122] Sodium dihydrogen phosphate 2.5g

[0123] NaOH Adjust pH to 7.0

[0124] Add water for injection* to 1000ml

[0125] (*Used in recipe but removed during processing)

[0126] Preparation Process:

[0127] (1) Preparation of Paliperidone Palmitate Sterile Suspension

[0128] Weigh 8g of sodium carboxymethylcellulose, put it in about 500ml of water for injection, swell and dissolve; then take 10g of polysorbate 80 for injection, 30g of mannitol, and 2.5g of sodium dihydrogen phosphate, stir and dissolve, and dissolve with 0.5M hydrogen The sodium oxide solution was used to adjust the pH to 7.0. Weigh 156g of sterile paliperidone palmitate and add it to the above solution, stir and shear unti...

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Abstract

The invention relates to a stable palmitic-acid paliperidone long-acting preparation, and aims to provide a palmitic-acid paliperidone massive composition with excellent dispersity, composite suspension property and stable physical properties. The available palmitic-acid paliperidone massive composition provided by the invention is prepared by the steps of freezing and drying a suspension containing palmitic-acid paliperidone.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a stable long-acting preparation of paliperidone palmitate. The long-acting preparation is a block composition, has good physical stability, chemical stability and resuspendability, and is convenient Long-term storage, transportation and clinical application. Background technique [0002] The chemical name of paliperidone palmitate is (±)-3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl] -6,7,8,9-tetrahydro-2-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl palmitate has the chemical structure shown in formula I: [0003] [0004] Formula I [0005] Paliperidone palmitate is the prodrug of paliperidone, which is hydrolyzed into paliperidone in vivo, which is the main metabolite of risperidone. It is currently believed that the mechanism of action of paliperidone is through the central dopamine 2 (D 2 ) receptors and 5-hydroxytryptamine (5HT 2A ) mediate...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/519A61K47/38A61K47/26A61P25/18
CPCA61K9/0002A61K9/0019A61K9/19A61K31/519A61K47/26A61K47/38
Inventor 张勇杨清敏王栋海张明会
Owner QILU PHARMA
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