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Amiodarone hydrochloride nanosuspension as well as preparation method and application thereof

A technology of nano-suspension and amiodarone hydrochloride, which is applied in the field of medicine, can solve the problems of poor water solubility and difficulty in forming highly dispersed particle groups, and achieve the effects of less excipients, high product uniformity and high stability

Pending Publication Date: 2021-04-16
HUANGHUAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The inventor tries to solve the technical problem of poor water solubility of amiodarone hydrochloride with nano-suspension, but in the trial production process, the particle size of the resulting suspension is usually in the micron range, and the smallest is around 1-2 microns, which is difficult to form A highly dispersed particle group with a particle size below 1000nm. In order to solve the problem of particle size, the inventor made many adjustments to the preparation process of the nanosuspension, excipients and other parameters, and finally formed a particle size range of 150-800nm. Nanosuspension, the particle size range can even be controlled within a small range of 150-300nm

Method used

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  • Amiodarone hydrochloride nanosuspension as well as preparation method and application thereof
  • Amiodarone hydrochloride nanosuspension as well as preparation method and application thereof
  • Amiodarone hydrochloride nanosuspension as well as preparation method and application thereof

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preparation example Construction

[0063] The following is the screening process of the preparation process of the nanosuspension of the present invention.

[0064] 1. Screening of wet grinding method stabilizer (surfactant)

[0065] Description of the preparation process of amiodarone hydrochloride nanosuspension by wet grinding:

[0066] Take an appropriate amount of amiodarone hydrochloride and a surfactant in a ball mill jar, and add an appropriate amount of ultrapure water. After sealing the ball mill jar, fix it on the ball mill, and set the appropriate speed and time. After the ball milling process is finished, filter and separate the ball milling medium and the compound solution to obtain a nanosuspension solution.

[0067] The contriver is by investigating the impact of different factors (kind and amount of surfactant, grinding speed and grinding time) on the nanosuspension stability, with form, particle size and polydispersity index (PI) as evaluation index, come Determine the best prescription.

...

Embodiment 1

[0135] Dissolve 0.3g of PVP and 0.08g of SDS in 20mL of purified water to obtain a solution; disperse 0.8g of amiodarone hydrochloride into the above solution to prepare a common suspension; add the obtained common suspension to a ball mill, And add 20g of zirconia particles with a diameter of 0.2mm; after the ball mill jar is sealed, put it in the ball mill, set the speed at 35Hz, and grind for 6 hours; then use a glass sand funnel to filter out the zirconia particles to obtain amiodarone hydrochloride nanosuspension. The measured particle diameter is: 204.5nm, and the PDI is 0.217. Then add 5% mannitol, divide the sample into 2 mL vials, pre-freeze at -80°C for 12 hours, and then freeze-dry in a freeze dryer for 24 hours to obtain a loose freeze-dried powder, then add purified water After reconstitution, the particle size increased within 5%.

Embodiment 2

[0137] Dissolve 0.35g of PVP and 0.15g of SDS in 20mL of purified water to obtain a solution; disperse 0.8g of amiodarone hydrochloride into the above solution to prepare a common suspension; add the obtained common suspension to a ball mill and add 20g of zirconia particles with a diameter of 0.2mm; after the ball mill jar is sealed, put it into a ball mill, set the speed at 35Hz, and grind for 8 hours; then use a glass sand funnel to filter out the zirconia particles to obtain ammonium hydrochloride Iodine ketone nanosuspension; the measured particle size is: 321.9nm, and the PDI is 0.298.

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Abstract

The invention belongs to the field of medicines, and particularly relates to an amiodarone hydrochloride nanosuspension as well as a preparation method and application thereof. The amiodarone hydrochloride nanosuspension provided by the invention mainly contains amiodarone hydrochloride and a stabilizer, and the amiodarone hydrochloride nanosuspension is prepared from the following components in parts by weight: 1 to 10 parts of amiodarone hydrochloride and 1 to 10 parts of a stabilizer. The nanosuspension with the particle size ranging from 150 nm to 800 nm is provided through two means, and the method comprises the steps that the nanosuspension is ground through a wet method, and the nanosuspension serves as an intermediate product and is further prepared into an oral preparation or an injection preparation for application. The preparation method comprises the following steps: A, dissolving the stabilizer in water, and dispersing the SKLB610 in the solution to prepare a common suspension; and B, adding a common suspension, and carrying out wet grinding to prepare the nano-suspension. Or an anti-solvent is adopted to precipitate the nano-suspension, and the nano-suspension is used as an intermediate product to be further prepared into an oral preparation or an injection preparation for application. The particle size of the nanosuspension can be effectively and intensively controlled to be 150-800 nm, the product uniformity is high, and the particle size is small.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to amiodarone hydrochloride nanosuspension and its preparation method and application. Background technique [0002] Amiodarone Hydrochloride (Amiodarone Hydrochloride, referred to as AD), also known as Amiodarone, Amiodarone and Amiodarone, is a derivative of benzofuran, and its chemical name is (2-butyl-3-benzene Furanyl)[4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl]methanone hydrochloride is a class III antiarrhythmic drug widely used clinically, mainly For the treatment of coronary artery dilators for angina pectoris, antiarrhythmias and life-threatening ventricular arrhythmias. [0003] Amiodarone hydrochloride is a white to slightly yellow crystalline powder, easily soluble in methanol and ethanol, almost insoluble in water, and belongs to Class II in the Biopharmaceutical Classification System (BCS). Because of its poor water solubility and high fat solubility, it absorbs...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/19A61K31/343A61K47/10A61K47/26A61P9/06A61P9/08
Inventor 游新雨刘会丽刘庆杨晶刘志芳王岩谢语秦
Owner HUANGHUAI UNIV
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