Limaprost nanoemulsion preparation for vertebral canal injection of antisternum

The technology of limaprost and spinal canal is applied in the field of pharmaceutical preparations, which can solve the problems of short validity period, poor stability and high storage conditions, and achieve the effects of remarkable curative effect, qualified pyrogen inspection, and overcoming low oral bioavailability.

Active Publication Date: 2012-01-25
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Aiming at the common problems of poor stability, short validity period, high storage conditions, and low bioavailability of oral preparations in the current prostacyclin preparations, the purpose of the present invention is to prepare limaprost which can be used for storage at room temperature and spinal canal injection. Prime Nanoemulsion

Method used

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  • Limaprost nanoemulsion preparation for vertebral canal injection of antisternum
  • Limaprost nanoemulsion preparation for vertebral canal injection of antisternum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Preheat 60g of soybean oil for injection to 65°C, add 10g of refined soybean lecithin and stir with hand to form a uniform oil phase, then slowly add 3mg of limaprost raw material drug, stir at 70°C at high speed (8000 rpm) for 3 minutes, Dissolve it evenly in the oil phase; dilute 20g of glycerin for injection, 35mg of emulsion stabilizer sodium citrate, and 35mg of emulsion stabilizer citric acid with an appropriate amount of water for injection preheated to 60~70°C to form a uniform water Phase; pour the above water phase into the mixer, slowly drop the oil phase into the water phase under the stirring condition of 10000 rpm, stir for 10 minutes, and form milky white colostrum after uniform dispersion; add the colostrum to Preheat to 60~70℃ water for injection to reach the full amount, transfer to a high-pressure homogenizer, homogenize 10 times under 8000 Psi pressure, take a sample to measure the particle size until the average particle size is below 200 nanometers,...

Embodiment 2

[0044]Preheat 70g of soybean oil for injection to 60~70°C, add 15g of refined lecithin with hand-held stirring to form a uniform oil phase, then slowly add 4mg of limatoprost raw material drug, stir at 70°C at high speed (8000 rpm) 4 Minutes to make it evenly dissolve in the oil phase; Dilute 10g of glycerin for injection, 25mg of emulsion stabilizer sodium citrate, 25mg of emulsion stabilizer citric acid with an appropriate amount of water for injection preheated to 60~70℃ to form a uniform The water phase; the above water phase is poured into the mixer, the oil phase is slowly dropped into the water phase under the stirring condition of 10000 rpm, stirred for 10 minutes, and milky white colostrum is formed after uniform dispersion; the colostrum Add it to the water for injection preheated to 60~70°C to reach the full amount, transfer it to a high-pressure homogenizer, homogenize it under 15000 Psi pressure for 8 times, take a sample to measure the particle size until the aver...

Embodiment 3

[0046] Preheat 50g of hydrogenated corn oil to 69°C, add 15g of polyoxyethylene castor oil and stir with hand to form a uniform oil phase, then slowly add 6mg of limaprost raw material drug, stir at 70°C at high speed (8000 rpm) for 3 minutes , so that it is uniformly dissolved in the oil phase; dilute 30g of glycerin for injection, 50mg of emulsion stabilizer sodium citrate, and 50mg of emulsion stabilizer citric acid with an appropriate amount of water for injection preheated to 60~70°C to form a uniform Water phase: pour the above water phase into the mixer, slowly drop the oil phase into the water phase under the stirring condition of 9000 rpm, stir for 12 minutes, and form milky white colostrum after uniform dispersion; add the colostrum Add the full amount to the water for injection preheated to 60~70°C, transfer to the high-pressure homogenizer, homogenize 10 times under the pressure of 10,000 Psi, take samples to measure the particle size until the average particle size...

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Abstract

The invention provides a limaprost nanoemulsion preparation for vertebral canal injection of antisternum, particularly relates to a limaprost nanoemulsion which contains citric acid and sodium citrate emulsion stabilizer, wherein the weight proportion of the citric acid and the sodium citrate in the emulsion stabilizer is 1:1, so the problem of unstable limaprost liquid preparation is solved. Thepreparation can be used for vertebral canal injection of the antisternum, so the defect that only few medicines of the existing oral limaprost tablet reach the focus part due to a first pass effect is solved, the therapeutic effect is improved, and the operative treatment rate is lowered, so the clinical use is benefited.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a nanoemulsion preparation, in particular to a limatoprost nanoemulsion preparation with high bioavailability, stable quality, and can be used for spinal canal injection. Background technique [0002] The chemical names of Limaprost are: [0003] (E)-7-[(1R,2R,3R)-3-hydroxy-2-[(3S,5S)-(E)-3-hydroxy-5-methyl-1-nonenyl]-5-oxocyclopentyl]- 2-heptenoic acid, the structural formula is as follows: [0004] [0005] This product is a derivative of prostaglandin E1, which can increase the content of cyclic adenosine monophosphate (cAMP) and inhibit the generation of thromboxane A2 (TXA2). It has the functions of dilating blood vessels, increasing blood flow and inhibiting platelet aggregation and adhesion. Animal experiments also show It can increase the blood flow of nerve tissue and improve nerve function. It is clinically used to improve various ischemic sy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P19/08A61P9/08A61K9/107A61K31/5575A61P29/00
Inventor 刘红星张扬程栎王伟张伟强刘玉静
Owner BEIJING TIDE PHARMA
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