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Dantrolene sodium freeze-dried powder injection for injection and preparation method thereof

A technology for freeze-dried powder injection and dantrolene sodium, applied in the field of medicine, can solve the problems of poor resolubility of dantrolene sodium freeze-dried powder for injection, poor water solubility of dantrolene sodium, low bioavailability and the like, and achieves considerable Economic and social benefits, short administration time, and simple preparation process

Active Publication Date: 2012-01-04
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] And dantrolene sodium has poor water solubility, is difficult to absorb, and has low bioavailability, and the dissolution rate is the limiting factor for drug absorption
When the present inventors studied the dantrolene sodium freeze-dried powder for injection, it was found that the dantrolene sodium freeze-dried powder for injection prepared by the above method had poor resolubility and contained more insoluble particles.

Method used

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  • Dantrolene sodium freeze-dried powder injection for injection and preparation method thereof
  • Dantrolene sodium freeze-dried powder injection for injection and preparation method thereof
  • Dantrolene sodium freeze-dried powder injection for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] [embodiment 1] the preparation of dantrolene sodium crystal

[0084] 1) Dissolving dantrolene sodium in a propylene glycol solvent to make a concentration of 10% dantrolene sodium solution is placed in a reactor in a constant temperature water bath with a temperature of 5° C.;

[0085] 2) Turn on the agitator, add the dantrolene sodium solution into water at a rotating speed of 2000r / min, stir for 18min to form a slurry, wherein the volume ratio of the dantrolene sodium solution to water is 1:20;

[0086] 3) The obtained slurry was left to stand for 3 hours, vacuum filtered and dried to obtain dantrolene sodium crystals.

[0087] According to FT-IR analysis, the molecular structure of dantrolene sodium did not change before and after ultra-micronization;

[0088] The X-ray powder diffraction spectrogram (XRD spectrogram) that uses Cu-K α ray measurement to the prepared dantrolene sodium crystal is shown in figure 1 , whose characteristic peaks are displayed at 2θ of 7...

Embodiment 1

[0093] [Preparation Example 1] Dantrolene Sodium Freeze-Dried Powder for Injection

[0094] Prescription: per 1000 prescriptions

[0095]

[0096] Preparation Process:

[0097] 1) take the dantrolene sodium and lactose of prescription quantity;

[0098] 2) Add 6000ml of water for injection and prescribed amount of dantrolene sodium into the liquid preparation tank, then add the prescribed amount of lactose, and fully stir to dissolve;

[0099] 3) adjust the pH value of the solution to 9.7 with 1mol / L sodium bicarbonate;

[0100] 4) Add water for injection to make up to 8000ml, and mix well;

[0101] 5) Add 0.03% activated carbon to the clear solution, stir and absorb for 30 minutes, then use a 0.45 μm microporous membrane filter to decarbonize, filter through a 0.45 μm primary sterile filter, and filter through a 0.45 μm secondary terminal sterile filter. In the liquid bottle, take the above-mentioned medicinal liquid to measure the content and pH value of the semi-fini...

Embodiment 2

[0107] [Preparation Example 2] Dantrolene Sodium Freeze-Dried Powder for Injection

[0108] Prescription: per 1000 prescriptions

[0109]

[0110] Preparation process: the specific operation steps are the same as in Example 1, and the difference from Example 1 is that the freeze-drying in step 6) is:

[0111] Pre-freezing stage: reduce the temperature of the shelf to -48°C at a rate of 0.70°C / min, and after the temperature of the subpackaged filtrate product drops to -35°C, continue to keep warm for 4 hours, and the temperature of the cold hydrazine drops rapidly below -50°C. Open the well valve of the box and evacuate until the vacuum in the box reaches about 10pa;

[0112] Primary drying stage: Slowly raise the shelf temperature to -2°C at a rate of 0.30°C / min, keep warm, and keep warm for 4 hours after the ice crystals of the product in the primary drying completely disappear;

[0113] Secondary drying stage: raise the temperature of the shelf to 17°C at a rate of 0.53...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a dantrolene sodium freeze-dried powder injection for injection and a preparation method thereof. The freeze-dried powder injection is prepared by freeze drying dantrolene sodium, lactobiose, a pH regulator and water for injection, wherein a mass ratio of the dantrolene sodium to the lactobiose is (1:0.5) to (1:2.5). The preparation method comprises the following steps of: adding the dantrolene sodium to the lactobiose in a prescription amount into the water for the injection, stirring, regulating the pH value to 9.0 to 10.5 by using the pH regulator, adding active carbon for injection, removing a heat source, decolorizing, filtering for decarburizing, performing fine filtering by using a filter membrane, packaging in separate bags, freezing and drying. The dantrolene sodium freeze-dried powder injection is studied on the basis of a freeze-dried process, namely the dantrolene sodium freeze-dried powder injection is cooled, heated by a small margin and is cooled again, so that the moisture of the freeze-dried product is reduced, and the freeze-dried product is high in redissolution and visible foreign matters and does not have insoluble granules. The dantrolene sodium freeze-dried powder injection for the injection is high in resolubility, clarity and stability, and low impurity content.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a dantrolene sodium freeze-dried powder for injection and a preparation method thereof. Background technique [0002] Dantrolene sodium, chemical name: 1-[[[5-(4-nitrophenyl)-2-furyl]-nitroso]amino]-2-4 imidazolindione sodium salt hydrate, English name : 1-[[[5-(4-Nitrophenyl)-2-furanyl]methylene]amino]-2,4-imidazolidinedione sodium salt, CAS number: 14663-23-1, molecular weight: 399.29, molecular formula: C 14 h 9 N 4 NaO 5 3.5H 2 O, the structural formula is as follows: [0003] [0004] Dantrolene sodium is a muscle relaxant that directly possesses skeletal muscle. Its main site of action is the release of calcium ions from the vesicle network of skeletal muscle to weaken muscle contraction. Dantrolene sodium is different from general muscle relaxants. Its unique mechanism is that it is directly used in skeletal muscle, and inhibits muscle contraction by inhibiting th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/4178A61P21/02
Inventor 钟正明马鹰军王小树罗韬
Owner HAINAN JINRUI PHARMA
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