Tetrodotoxin quick-release pellet preparation and its preparation method and use

A technology of tetrodosin and pellets, which is applied in the field of pharmaceutical preparation technology and application, can solve the problems of inability to take oral administration, poor compliance of injections, short half-life of drugs, etc., and achieve rapid onset of analgesic effect, rapid drug release, The effect of high drug application rate

Active Publication Date: 2016-11-02
XIAMEN ZHAOYANG BIOLOGICAL ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved in the present invention is the short half-life of the medicine that exists in the development of tetrodosin medicine, and the problems such as the poor compliance of the injection for clinical application (cannot be administered orally).

Method used

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  • Tetrodotoxin quick-release pellet preparation and its preparation method and use
  • Tetrodotoxin quick-release pellet preparation and its preparation method and use
  • Tetrodotoxin quick-release pellet preparation and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Formula 1

[0031]

[0032]

[0033] Preparation:

[0034] (1) Preparation of drug solution: take by weighing 600 mg of tetrodoxine according to the formula, add 200 mL of 0.3% acetic acid solution to dissolve, then dissolve in an aqueous solution containing 67.5 g of hypromellose (HPMC) to prepare 1500 g of drug solution.

[0035] (2) Spraying medicine at the bottom of the fluidized bed: 4000g of microcrystalline cellulose blank ball core is placed in the fluidized bed, start the fluidized bed, set the parameters of the fluidized bed medicine: fan air volume 150m 3 h -1 , Liquid supply pump speed 5r min -1 , The temperature of the material is controlled at 30-40°C, the atomization pressure is 0.16MPa, and the drug is applied in a fluidized state. After the drug is applied, it is fluidized and dried for 15 minutes.

[0036] (3) Fluidized bed coating-protective film layer: take 3800g of pure water according to the formula, add 200g of hypromellose (HP...

Embodiment 2

[0038] Example 2 Formula 2

[0039]

[0040] Preparation:

[0041] (1) Preparation of the drug solution: take by weighing Tetradosin 100mg according to the formula, add 0.1% citrate solution 300mL and dissolve, then be dissolved in the aqueous solution that contains povidone (PVP) 7.5g and be mixed with 1500g drug solution.

[0042] (2) Spray medicine at the bottom of the fluidized bed: place 4000g of sucrose blank ball cores in the fluidized bed, start the fluidized bed, set the parameters of the fluidized bed medicine: fan air volume 150m 3 h -1 , Liquid supply pump speed 5r min -1, The temperature of the material is controlled at 30-40°C, the atomization pressure is 0.16MPa, and the drug is applied in a fluidized state. After the drug is applied, it is fluidized and dried for 15 minutes.

[0043] (3) Fluidized bed coating-protective film layer: Weigh 3800g of pure water according to the formula, add 200g of acrylic resin under stirring, stir to dissolve, and prepare ...

Embodiment 3

[0044] Embodiment 3 Formula 3

[0045]

[0046] Preparation:

[0047] (1) Preparation of drug solution: take by weighing 1200 mg of tetrodoxine according to the formula, add 720 mL of 0.6% hydrochloric acid solution to dissolve, then dissolve in an aqueous solution containing 65 g of syrup to prepare 1500 g of drug solution.

[0048] (2) Spray medicine at the bottom of the fluidized bed: place 4000g of sucrose blank ball cores in the fluidized bed, start the fluidized bed, set the parameters of the fluidized bed medicine: fan air volume 150m 3 h -1 , Liquid supply pump speed 5r min -1 , The temperature of the material is controlled at 30-40°C, the atomization pressure is 0.16MPa, and the drug is applied in a fluidized state. After the drug is applied, it is fluidized and dried for 15 minutes.

[0049] (3) Fluidized bed coating-protective film layer: take 3800g of pure water according to the formula, add 200g of acrylic resin under stirring, stir and dissolve, and prepare...

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Abstract

The invention discloses a tetrodotoxin quick-release pellet preparation and its preparation method and use and relates to the field of a medicinal preparation technology and use. The tetrodotoxin quick-release pellet preparation is suitable for oral administration and utilizes a blank pellet core as a carrier and a tetrodotoxin aqueous solution containing a cosolvent and a binder as a drug feeding solution. A weight ratio of the tetrodotoxin to the pellet core is 0.0025%-0.3% and an oral dosage of the tetrodotoxin is less than or equal to 300 micrograms. The tetrodotoxin quick-release pellet preparation has the advantages of high superimpose rate, good content uniformity, fast drug release rate and fast pain easing. The tetrodotoxin quick-release pellet preparation has the characteristics of good clinical use compliance and high safety. The blank pellet core fluidized bed-based drug superimpose method is suitable for preparation of a very low specification tetrodotoxin oral preparation.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparation technology and application, in particular to a preparation of tetrodoxine quick-release pellets, a preparation method and application thereof. Background technique [0002] Tetradoxine (Tetradotoxin) is a marine biotoxin mainly extracted from the viscera of puffer fish. It is a highly selective sodium ion channel blocker and has the functions of analgesia and controlling the withdrawal symptoms of opioid dependence. Tetradoxine is an amino perhydroquinazoline compound, its structure is a clathrate orthoester, usually in the form of "zwitterions", and the guanidino group in the structure is a necessary functional group for its activity. Tetradosin is unstable in an acidic or alkaline environment, and is easily dehydrated and decomposed into non-toxic products. Oral administration is generally considered not a suitable way of administration. Therefore, the common way of administration in c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/529A61K47/26A61K47/38A61P29/00A61P25/36
CPCA61K9/0002A61K9/1623A61K9/1652A61K31/529
Inventor 洪碧红孙继鹏易瑞灶
Owner XIAMEN ZHAOYANG BIOLOGICAL ENG
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