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Fat emulsion of Paricalcitol, its preparation and preparation methods thereof

A technology of paricalcitol and fat emulsion, which is applied in the preparation of the above-mentioned fat emulsion and its preparation, the fat emulsion of paricalcitol, and the preparation field of fat emulsion, which can solve the problems of small irritation and reduce the Irritant, good stability, stable particle size effect

Active Publication Date: 2012-11-14
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Therefore, although the existing paricalcitol preparation technology has solved the dissolution and stability problems of the drug, there are defects in safety and irritation, and a new injection dosage form needs to be developed to obtain less irritation, Safer and stable formulation of paricalcitol for intravenous use

Method used

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  • Fat emulsion of Paricalcitol, its preparation and preparation methods thereof
  • Fat emulsion of Paricalcitol, its preparation and preparation methods thereof
  • Fat emulsion of Paricalcitol, its preparation and preparation methods thereof

Examples

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Effect test

Embodiment 1

[0049] Example 1 Preparation of Paricalcitol Fat Emulsion I

[0050] Add 2 mg of paricalcitol into 100 g of soybean oil for injection preheated to 60° C., stir until it is completely dissolved, and then add 0.1 g of oleic acid to obtain an oil phase. Dissolve 5 g of egg yolk lecithin, 5 g of poloxamer (F-68), 0.3 g of sodium oleate, and 30 g of glycerin for injection in 200 ml of water for injection preheated to 60°C, and mix well to obtain an aqueous phase. Slowly add the oil phase into the water phase, and stir at high speed to obtain an emulsion, adjust the pH to 9.0 with 0.2 mol / L sodium hydroxide solution to obtain colostrum. Add water for injection to 1000ml, and homogenize 8 times under 400bar pressure to obtain Paricalcitol fat emulsion.

Embodiment 2

[0051] Example 2 Preparation of Paricalcitol Fat Emulsion II

[0052] Add 1 mg of paricalcitol to 50 g of soybean oil / MCT for injection (0.5:1) preheated to 60° C., stir until completely dissolved, add 1.0 g of cholic acid, stir and dissolve to obtain an oil phase. Dissolve 20 g of soybean lecithin, 1.0 g of sodium cholate and 40 g of sorbitol in 300 ml of water for injection preheated to 60°C, and mix uniformly to obtain an aqueous phase. Slowly add the water phase into the oil phase, and stir at high speed to obtain an emulsion, and adjust the pH to 4 with 0.2 mol / L sodium bicarbonate solution to obtain colostrum. Add water for injection to 1000ml, homogenize 10 times under 600bar pressure to obtain paricalcitol fat emulsion.

Embodiment 3

[0053] Example 3 Preparation of Paricalcitol Fat Emulsion III

[0054] Add 5 mg of paricalcitol into 200 g of olive oil / fish oil (1:1) preheated to 60°C, stir until completely dissolved, then add 1.5 g of deoxycholic acid, stir and dissolve to obtain an oil phase. Dissolve 40 g of egg yolk lecithin, 10 g of poloxamer (F-68), 3 g of sodium deoxycholate and 70 g of mannitol in 400 ml of water for injection preheated to 60°C, and mix well to obtain an aqueous phase. Slowly add the oil phase into the water phase, and stir with high shear to obtain an emulsion, and adjust the pH to 7.5 with 0.2 mol / L disodium hydrogen phosphate solution. Get colostrum. Water for injection was added to 1000ml, and homogenized 13 times under a pressure of 1100bar to obtain a paricalcitol fat emulsion.

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Abstract

The invention relates to a fat emulsion of Paricalcitol. The fat emulsion comprises oil for injection, an emulsifier, a stabilizer, an isoosmotic adjusting agent, and a pH adjusting agent. Emulsion droplets have an average diameter of 50nm-1000nm. The fat emulsion can be prepared into injection emulsions, freeze-dried emulsions or capsules. Specifically, organic solvents cannot be employed as injections so as to reduce stimulation on blood vessels during injection and avoid injection package material impurity leaching caused by organic solvents, thus ensuring product quality and safety, and reducing the difficulty of product quality control.

Description

Technical field: [0001] The invention relates to a new dosage form of paricalcitol, in particular to a fat emulsion of paricalcitol and a preparation prepared from the fat emulsion. The present invention also relates to the preparation method of the above-mentioned fat emulsion and its preparation. Background technique: [0002] Paricalcitol, chemical name (1R, 3R)-5-[(2E)-2-[(1R, 3aS, 7aR)-1-[(E, 2R, 5S)-6-Hydroxy- 5,6-dimethylhept-3-en-2-y1]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]cyclohexane-1,3-diol , the structural formula is as follows: [0003] [0004] Paricalcitol is an active vitamin D analogue that effectively suppresses parathyroid hormone (PTH) levels. There are injections and capsules available. Paricalcitol is insoluble in water and easily degrades under oxidation, light and acidic conditions, which brings great technical difficulties to the manufacture of intravenous injections. [0005] In order to solve the dissolution and sta...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/19A61K9/48A61K31/592A61P5/20
Inventor 朱学琳兰洁
Owner CHONGQING HUAPONT PHARMA
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