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Nimodipine long-acting oral suspension liquid and preparation method thereof

A nimodipine and nimodipine nano-technology, applied in the field of medicine, can solve problems such as unclear effectiveness and safety, low bioavailability, and insoluble drugs in water, so as to improve drug encapsulation rate and drug utilization High rate, increase the effect of effective blood concentration time

Active Publication Date: 2018-08-17
XUZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For patients, especially children, the oral compliance of ordinary tablets is poor, the drug is difficult to dissolve in water, and the dissolution rate is slow, so the onset of action is slow, and the action time is short, and the toxicity is strong after taking multiple times. Low; and the commercially available nimodipine injection has no definite research data for children, and its effectiveness and safety are not clear

Method used

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  • Nimodipine long-acting oral suspension liquid and preparation method thereof
  • Nimodipine long-acting oral suspension liquid and preparation method thereof
  • Nimodipine long-acting oral suspension liquid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Table 1 Prescription of nimodipine oral solution

[0043]

[0044]

[0045] Preparation Process:

[0046] (1) Get 0.75g nimodipine, 0.5g benzoic acid and disperse in 100ml ethanol;

[0047] (2) Add 150ml polyethylene glycol and 125ml glycerin to the above solution, and mechanically stir for 10min until dissolved;

[0048] (3) Take 60ml of purified water and add the prescription amount of sodium dihydrogen phosphate and disodium hydrogen phosphate and mechanically stir for 10 minutes until dissolved;

[0049] (4) Add the prescription amount of maltitol to the solution prepared in (3) and mechanically stir for 10 minutes until dissolved;

[0050](5) Add the solution prepared in (4) above to the solution prepared in (2), and stir mechanically for 10 minutes;

[0051] (6) Dilute the purified water to the prescribed amount, and filter with a 0.45 micron filter element.

Embodiment 2

[0053] Table 2 Prescription of nimodipine oral solution

[0054]

[0055]

[0056] Preparation Process:

[0057] (1) Disperse 0.75g of nimodipine in 100ml of ethanol.

[0058] (2) Add 125ml of polyethylene glycol, 150ml of glycerin, and 5ml of benzyl alcohol to the above solution, and stir mechanically for 10 minutes until dissolved.

[0059] (3) Take 60ml of purified water, add the prescribed amount of citric acid and sodium citrate, and mechanically stir for 10 minutes until dissolved.

[0060] (4) Add the prescribed amount of sucralose to the solution prepared in (3) and mechanically stir for 10 minutes until dissolved.

[0061] (5) Add the solution prepared in (4) above to the solution prepared in (2), and stir mechanically for 10 minutes.

[0062] (6) Dilute the purified water to the prescribed amount, filter with a 0.45 micron filter element, perform quality inspection, and pack in a brown glass bottle.

Embodiment 3

[0064] Example 3

[0065] After the sample was kept away from light and sealed for 3 months under accelerated stability (40°C, RH75%), the content of nimodipine was detected by liquid phase.

[0066]

[0067] We can find out by experiment, the stability of this invention prescription process nimodipine is high.

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Abstract

The invention discloses nimodipine long-acting oral suspension liquid and a preparation method thereof. The nimodipine long-acting oral suspension liquid is prepared from the following components in parts by weight: 0.1 to 0.3 part of nimodipine nano-particle, 0.1 to 0.3 part of nimodipine, 0.1 to 2 parts of sweetening agent, 1 to 5 parts of pH buffering agent, 0.1 to 2 parts of preservative and 90 to 100 parts of solvent. A carrier material of the nimodipine nano-particle is a combinant of polylactic acid-hydroxyacetic acid copolymer and pluronic F68, and the pluronic F68 is 5 to 40 percent by mass of the carrier material. The nimodipine long-acting oral suspension liquid disclosed by the invention is convenient to orally take and has a good taste; a part of medicines exists in a free state, so that absorption speed can be accelerated and an effect takes quickly; a part of medicines are carried in the polylactic acid-hydroxyacetic acid copolymer and pluronic F68 nano-particles, so that a first pass effect can be reduced, a medicine utilization ratio is high, the drug load of the nano-particles is large, an entrapment ratio is high, release is slow, the acting time is long, the administration frequency is reduced, the defect of existing marketed dosage forms is overcome; the preparation method has the advantages of good reproducibility, good repeatability, and easiness for being strongly implemented and popularized on the industry.

Description

technical field [0001] The invention relates to a nimodipine oral long-acting suspension and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Subarachnoid hemorrhage (SAH) is a very serious common disease, mainly caused by rupture of blood vessels at the base of the brain or on the surface of the brain, and blood flowing into the subarachnoid space. The main complications are cerebral vasospasm, cerebral hemorrhage Water, rebleeding, etc. The World Health Organization survey shows that the incidence rate in China is about 2.0 / 100,000 person-years, and it is also reported that it is 6-20 / 100,000 person-years per year. Migraine (migraine) is the most common type of primary headache clinically, clinically characterized by paroxysmal moderate to severe, throbbing headache as the main manifestation, most of the onsets are in children and adolescence, and the incidence peaks in young and middle-aged adults. [0003] Nimodi...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/51A61K47/34A61K47/10A61K31/4422A61P9/10A61P25/06A61P27/16A61P9/12
CPCA61K9/0053A61K9/10A61K9/5146A61K9/5153A61K31/4422A61P9/10A61P9/12A61P25/06A61P27/16
Inventor 张彦卓王静王方李晓楠
Owner XUZHOU MEDICAL UNIV
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