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Cilnidipine nano-suspension and preparation method thereof

A technology of nanodipine and cilnidipine, applied in the field of medicine, can solve the problems such as no cilnidipine nanosuspension/nanocrystal report, etc., and achieve the effects of improving in vitro dissolution characteristics, preventing aggregation and ensuring stability

Pending Publication Date: 2020-01-21
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no related report about cilnidipine nanosuspension / nanocrystal

Method used

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  • Cilnidipine nano-suspension and preparation method thereof
  • Cilnidipine nano-suspension and preparation method thereof
  • Cilnidipine nano-suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1: the preparation of cilnidipine nanosuspension

[0044] Weigh 0.20 g of Poloxamer 407 (P407), add it into 50 mL of distilled water, and stir it magnetically to dissolve; then add 1.00 g of cilnidipine raw material, and stir it magnetically for 15 minutes to obtain a coarse suspension. This coarse suspension is then transferred to a nanomill for grinding. The grinding conditions are as follows: the diameter of the yttrium-stabilized zirconia grinding beads is 0.6-0.8 mm, and the rotation speed of the stirring shaft is 2000 rpm. After 60 minutes, a sample was taken, and the measured particle diameter was 435nm, and the PDI was 0.190.

Embodiment 2

[0045] Embodiment 2: the preparation of cilnidipine nanosuspension

[0046] Weigh 0.05g of sodium lauryl sulfate and 0.30g of polyvinylpyrrolidone-vinyl acetate copolymer (PVP VA64), add them into 50mL of distilled water, stir to dissolve; then add 1.00g of cilnidipine raw material, and stir for 15 minutes , to obtain a coarse suspension. This coarse suspension is then transferred to a nanomill for grinding. The grinding conditions are as follows: the diameter of the yttrium-stabilized zirconia grinding beads is 0.6-0.8 mm, and the rotation speed of the stirring shaft is 2500 rpm. After 45 minutes, the sample was taken, and the measured particle size was 312nm, and the potential was -33.6mV. See the results figure 1 a and figure 1 b.

Embodiment 3

[0047] Embodiment 3: the preparation of cilnidipine nanosuspension

[0048] Weigh 0.10 g of sodium lauryl sulfate and 0.30 g of hydroxypropyl cellulose (HPC-SSL), add it into 50 mL of distilled water, and stir it magnetically to dissolve it, add 1.00 g of cilnidipine raw material, and stir it magnetically for 15 minutes to obtain crude suspension. This coarse suspension is then transferred to a nanomill for grinding. The grinding conditions are as follows: the diameter of the yttrium-stabilized zirconia grinding beads is 0.6-0.8 mm, and the rotation speed of the stirring shaft is 2500 rpm. After 45 minutes, a sample was taken, and the measured particle size was 357nm, and the potential was -32.3mV.

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Abstract

The present invention relates to a cilnidipine nano-suspension and a preparation method thereof. The cilnidipine nano-suspension is obtained by a nanometer treatment of cilnidipine and a stabilizer aqueous solution, wherein the stabilizer is a space stabilizer, a charge stabilizer or a combination of the space stabilizer and the charge stabilizer. The prepared cilnidipine nano-suspension has characteristics of high dissolution and high bioavailability, can be used as a preparation finished product or as a preparation intermediate to prepare a solid or liquid state cilnidipine preparation, andcan ensure medicine absorption and medicine effect stability. Besides, the processing technology is feasible, stable and reliable, and provides an easily industrialized technical means and preparationintermediate preparation technology for development of the cinidipine preparation, and thus the manufactured cilnidipine preparation has good oral absorption and application prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a cilnidipine nanosuspension and a preparation method thereof. Background technique [0002] Hypertension is a systemic disease characterized by an increase in systemic arterial blood pressure and accompanied by heart, brain, blood vessel, kidney and other organ functions or organic damage. The main complications of hypertension are coronary heart disease, myocardial infarction, stroke, eye disease and kidney disease. Due to the serious harm of hypertension and its complications, it has become one of the most common cardiovascular diseases and major fatal diseases at home and abroad. [0003] Cinidipine is a novel dihydropyridine Ca 2 + Antagonist that potently inhibits sympathetic neuronal vascular smooth muscle L-type Ca 2 + channel and N-type Ca 2 + The channel has been successfully applied to the clinical treatment of hypertension and angina pectoris with remarkable cura...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/10A61K47/32A61K47/38A61K47/22A61K47/36A61K47/26A61K47/20A61K31/4422A61P9/12A61P9/10
CPCA61K9/10A61K47/10A61K47/32A61K47/38A61K47/22A61K47/36A61K47/26A61K47/20A61K31/4422A61P9/12A61P9/10
Inventor 杨建宏刘强侯延辉刘艳华李莉
Owner NINGXIA MEDICAL UNIV
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