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Nimodipine nanocrystallization method and dry suspension thereof

A nimodipine nanometer and nimodipine dry technology, which can be used in cardiovascular system diseases, nervous system diseases, liquid transportation, etc., can solve the problems of improving the stability of liquid preparations and increasing the irritation of drugs, and achieve increased solubility and stability. Dissolution rate, improved bioavailability, narrow distribution effect

Inactive Publication Date: 2018-03-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the ethanol contained in its prescription, the irritation of the drug increases, accompanied by some adverse reactions, and the stability of the liquid preparation needs to be improved during transportation and storage

Method used

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  • Nimodipine nanocrystallization method and dry suspension thereof
  • Nimodipine nanocrystallization method and dry suspension thereof
  • Nimodipine nanocrystallization method and dry suspension thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The nanometerization method of embodiment 1 nimodipine

[0028] Weigh 0.100 g of sodium lauryl sulfate and 0.050 g of poloxamer, add them into a grinding tank, weigh 1.00 g of nimodipine crude drug, put them in a grinding tank, and add 15 g of water into the grinding tank. Place the grinding jar in an ultrasonic cleaner for ultrasonic dispersion for 20 min. Add about 80g of zirconia grinding beads (the mass ratio of the large and small balls is 1:5, the diameter of the large ball is 5mm, and the diameter of the small ball is 0.5mm) into the grinding jar, and balance the grinding jar in pairs on the balance, and then install the grinding jar In a planetary ball mill, grind at 400r / min for 3h to obtain nimodipine nanosuspension. The measured particle diameter is 268.1nm, PDI is 0.19, and potential is -23mV.

Embodiment 2

[0029] The preparation of embodiment 2 nimodipine dry suspension

[0030] Take 50 g of the nimodipine nano-suspension prepared in Example 1 of the present invention, add 0.200 g of hydroxypropyl cellulose and 0.120 g of micropowder silica gel, and stir magnetically for 30 minutes to make it evenly distributed. Spray-dry (inlet temperature 110°C, sample injection speed 3mL / min, pressure-60mbar) to obtain spray-dried powder, add powder essence 0.10g, mix thoroughly to obtain nimodipine dry suspension. Take 0.10g and place it in a test tube, add 15ml of distilled water, and shake for 30s. Its redispersibility is good, its particle diameter is measured to be 285.7nm, its PDI is 0.21, and its potential is -27mV.

Embodiment 3

[0031] Example 3 Nimodipine nanosuspension spray-dried powder in vitro dissolution study

[0032] Nimodipine crude drug, nimodipine common suspension spray dry powder, nimodipine The nimodipine nanosuspension spray-dried powder of Example 2 of the present invention was used for the dissolution contrast experiment, and the samples at different time points were assayed and the cumulative dissolution percentage was calculated. The result shows that the dissolution rate of nimodipine nano-suspension spray-dried powder of the present invention is obviously higher than that of nimodipine bulk drug and nimodipine See attached image 3 . Wherein the preparation method of nimodipine common suspension spray-dried powder is as follows: nimodipine crude drug is passed through a 100-mesh sieve to make a suspension, which is obtained after spray-dried (the prescription is consistent with the nano spray-dried powder).

[0033] Dissolution assay:

[0034] Get appropriate amount of sampl...

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Abstract

The invention relates to the field of pharmaceutical preparations and provides a nimodipine nanocrystallization method and a dry suspension thereof. The method comprises the following steps: nano-crystallizing nimodipine by adopting a medium grinding method; preparing a nano suspension in the presence of a stabilizer and water; then adding a suspending agent and a spray drying protective agent orother auxiliary materials to prepare nano suspension spray drying powder by further spraying and drying; and then adding other auxiliary materials and uniformly mixing to obtain the nimodipine dry suspension. The dry suspension is good in redispersibility, good in stability and convenient to take; nimodipine which is redispersed has small grain size and narrow distribution, and the potential of nimodipine meets the demand. The dissolution rate of the drug is improved obviously, and the bioavailability in vivo of the drug can be improved. Meanwhile, the dry suspension formula and preparation process are simple, and the preparation is safe and effective, has relatively low cost and is easy for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nimodipine nanometerization method and a dry suspension thereof. Background technique [0002] Nimodipine is a second-generation calcium antagonist, which can selectively act on the smooth muscle of cerebral vessels, inhibit the contraction of smooth muscles, thereby dilating cerebral vessels and increasing cerebral blood flow. Because of its good selectivity to cerebrovascular, nimodipine has become an ideal drug for the treatment of ischemic cerebrovascular disease, migraine, cerebral vasospasm caused by subarachnoid hemorrhage and other diseases. Nimodipine was developed by Bayer AG of Germany in the 1980s, and its oral dosage form entered the domestic market in the 1990s. The commercially available oral dosage form of nimodipine mainly contains tablet and capsule at present. However, due to the poor solubility and strong first-pass effect of nimodipine, the bioa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/4422A61P9/10A61P25/06A61P9/08
CPCA61K31/4422A61K9/10A61K47/10A61K47/38
Inventor 蒋曙光俞宏智徐晓畅
Owner CHINA PHARM UNIV
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