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Clevidipine butyrate lipid microsphere injection and preparation method thereof

A technology of chlorvinyl butyrate and dipine fat, which is applied in the direction of pharmaceutical formula, emulsion delivery, medical preparations containing active ingredients, etc., can solve the problems of cumbersome steps, aggregation and sedimentation, large particle size, etc., and achieve uniform particle size distribution , good stability

Active Publication Date: 2017-08-29
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In the existing method for preparing lodipine butyrate lipid microsphere injection, mostly adopt the method of filtration, screen the lodipine butyrate lipid microsphere with certain particle size, the steps are loaded down with trivial details, and filter membrane is easy to adsorb medicine during filtration, affects The drug content in the preparation is prone to batch-to-batch variance
In addition, the particle size is large, the stability is not good, and aggregation and sedimentation are prone to occur

Method used

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  • Clevidipine butyrate lipid microsphere injection and preparation method thereof
  • Clevidipine butyrate lipid microsphere injection and preparation method thereof
  • Clevidipine butyrate lipid microsphere injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Effect of raw materials on clevidipine butyrate lipid microsphere injection

[0028]

[0029] Preparation method: 1) Water phase: disperse the isotonic agent in the prescribed amount in water for injection, stir until completely dissolved, and adjust the pH to 8.0 with 0.1mol / L NaOH solution;

[0030] 2) Oil phase: weigh the prescribed amount of oil for injection and stabilizer, preheat at 70°C for 2 minutes; add the prescribed amount of clevidipine butyrate, shake well and mix; add emulsifier, and use high-speed dispersion at 70°C Machine shear until the emulsified oil is completely dissolved;

[0031] 3) Slowly add the oil phase to the water phase, add water, and shear with a high-speed disperser at 20,000 rpm for 10 times, each time for 1 min, to obtain stable colostrum.

[0032] 4) Add it into the micro-jet, perform high-pressure homogenization, the pressure of high-pressure homogenization is 15,000 psi, and homogenize 12 times.

[0033] 1. Choice of ...

Embodiment 2

[0053] Example 2 Effect of process conditions on clevidipine butyrate lipid microsphere injection

[0054] 1. Effect of emulsification temperature

[0055] The emulsification temperature refers to the temperature when the oil phase and the water phase are mixed and sheared. The emulsification temperature can affect the fluidity of the oil phase and the water phase, the stability of the drug and the behavior of the surfactant during emulsification. Taking particle size, PDI, drug content and Zeta potential as the main evaluation indicators, the oil-water two-phase was preheated before mixing and shearing. The temperature was set at 40°C, 50°C, 60°C, 70°C, 80°C and 90°C. Effect of emulsification temperature on the physical and chemical stability of clevidipine butyrate lipid microspheres. The results are shown in Table 5.

[0056] Table 5 Effect of emulsification temperature on clevidipine butyrate lipid microspheres

[0057]

[0058] It can be seen from Table 5 that when t...

Embodiment 3

[0076] Example 3 Clevidipine Butyrate Liposphere Injection

[0077] (1) The formula is as follows

[0078]

[0079] (2) Preparation method

[0080] 1) Water phase: Disperse the prescribed amount of glycerin in water for injection and stir until completely dissolved. Adjust the pH to 8.0 with 0.1mol / L NaOH solution.

[0081] 2) Oil phase: Weigh the prescribed amount of soybean oil and oleic acid for injection, preheat to 70°C; add the prescribed amount of clevidipine butyrate, shake well and mix; add soybean lecithin, and use a high-speed disperser to cut to Soy lecithin is all dissolved.

[0082] 3) Slowly add the oil phase to the water phase, add water to 100 mL, and use a high-speed disperser at 20,000 rpm to shear 10 times, 1 min each time.

[0083] 4) Add to the micro jet, pressure 15000psi, homogenize 12 times.

[0084] 5) Bottle it, seal it, and sterilize it at 120°C for 30 minutes.

[0085] (3) Measurement results

[0086] The average particle diameter of the ...

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Abstract

The invention relates to a cleviprex lipid microsphere injection and a preparation method thereof. The cleviprex lipid microsphere injection is composed of cleviprex, oil for injection, an emulsifier, a stabilizer, an isotonic agent, a pH regulator, and water for injection. The preparation method comprises the following steps: dissolving the isotonic agent in the water for injection, and regulating the pH value to 6.0-8.0 with NaOH to obtain a water phase; preheating the oil for injection and the stabilizer at 40-90 DEG C; adding cleviprex, and uniformly shaking to be mixed; adding the emulsifier, and shearing by a high-speed dispersion machine to obtain an oil phase; slowly adding the oil phase in the water phase, and shearing by the high-speed dispersion machine for 1-5min every time for 5-20 times at a shearing speed of 10000-20000rpm to obtain a stable primary emulsion; adding the primary emulsion in a microjet, and carrying out high-pressure homogenizing for 10-20 times at a pressure of 7000-20000psi. The preparation method disclosed by the invention is capable of realizing one-step rapid preparation of the small-particle-size cleviprex lipid microsphere injection.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a clevidipine butyrate lipid microsphere injection and a high-pressure micro-jet rapid preparation method thereof. Background technique [0002] Hypertension is a systemic disease characterized by elevated arterial pressure accompanied by functional or organic changes in the heart, brain, blood vessels, and kidneys. Hypertension is the most common chronic disease in my country and the main risk factor for cardiovascular and cerebrovascular diseases. Clevidipine butyrate is the third-generation short-acting dihydropyridine calcium channel blocker, which is clinically used in perioperative hypertension, acute hypertension, essential hypertension, etc., with remarkable curative effect. Clevidipine butyrate can selectively dilate arteries, reduce systemic vascular resistance and reduce mean arterial pressure, but does not reduce cardiac filling pressu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/4422A61P9/12
Inventor 刘宇陈立江王芳焉喜臣
Owner LIAONING UNIVERSITY
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