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Preparation method of tolvaptan tablet

A protan tablet and tablet compression technology, applied in the field of chemical pharmacy, can solve the problems of poor drug bioavailability and clinical curative effect, low dissolution rate of tolvaptan tablet in vitro, large investment in equipment, etc. Utilization, good clinical efficacy, good effect of bioavailability

Active Publication Date: 2013-05-15
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the preparation method of tolvaptan tablet has complex process, large investment in equipment, high production cost, low in vitro dissolution rate of the prepared tolvaptan tablet, poor bioavailability and clinical curative effect of the drug

Method used

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  • Preparation method of tolvaptan tablet

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Experimental program
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Effect test

Embodiment 1

[0019] Embodiment 1: 1, the raw material of following recipe quantity is made tolvaptan spray powder,

[0020] Tolvaptan 50g Highly substituted-hydroxypropyl cellulose 15g Absolute ethanol 195ml Dichloromethane 455ml

[0021] Preparation:

[0022] A. Pass tolvaptan and highly substituted-hydroxypropyl cellulose through an 80-mesh sieve and mix well.

[0023] B. Take absolute ethanol and dichloromethane according to the prescription and mix them evenly.

[0024] C. Dissolving the mixture in step A in the above solvent.

[0025] D. Spray-dry the mixture in step C into powder, the inlet air temperature: 150-160°C, the outlet air temperature: 80-90°C.

[0026] 2, make 200 tolvaptan tablets with the raw and auxiliary materials of following prescription quantity,

[0027] prescription Dosage (g) Tolvaptan Spray Powder 3.9 lactose 7.4 microcrystalline cellulose 4.14 Hydroxypropylmethylcellulose 0.6 Cross-li...

Embodiment 2

[0030] Embodiment 2: 1, the preparation of tolvaptan spray powder is the same as embodiment 1.

[0031] 2, make 200 tolvaptan tablets with the raw and auxiliary materials of following prescription quantity,

[0032] prescription Dosage Tolvaptan Spray Powder 3.9 lactose 7.4 microcrystalline cellulose 3.54 Hydroxypropylmethylcellulose 0.6 Cross-linked polyvinylpyrrolidone 1.5 water Appropriate amount Magnesium stearate 0.16

[0033] Preparation method: pass the tolvaptan spray powder through a 200-mesh sieve, pass the auxiliary materials through a 100-mesh sieve, and set aside. Accurately weigh the raw materials and all internal auxiliary materials according to the prescription amount, mix them evenly, add appropriate amount of water to prepare soft materials, and pass through a 20-mesh sieve to prepare wet granules; dry at 60°C, pass through a 18-mesh sieve for granulation, and add the prescribed amount of stearin Mag...

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Abstract

The invention discloses a preparation method of a tolvaptan tablet. The preparation method comprises the following steps: 1, mixing tolvaptan with high-substituted hydroxylpropyl cellulose according to a mass ratio of 1:0.2-0.6, crushing them, and sieving by a 60-100 mesh sieve; 2, dissolving throughs in a mixed solution of waterless ethanol and dichloromethane with a volume ratio of 1:1-4, carrying out spray drying to form powder, carrying out reduced pressure drying at 70-90DEG C until that the content of solvents residual in the sprayed powder is qualified; 3, crushing the sprayed powder, sieving by a 180-220 mesh sieve, accurately weighing the sprayed powder, lactose, microcrystalline cellulose and hydroxypropyl methylcellulose according to prescription amounts, uniformly mixing them, and adding a proper amount of water to prepare a soft material; and 4, sieving the soft material by a 15-25 mesh sieve, preparing a wet particle, drying the wet particle at 50-70DEG C until that the content of water in the wet particle is 2-4%, sieving the dried wet particle by a 15-25 mesh sieve, granulating, adding a prescription amount of magnesium stearate, uniformly mixing, and tabletting. The preparation method of the invention has the advantages of ingenious conception, low production cost, high in vitro dissolubility of the prepared tolvaptan tablet, and good biological availability and clinic curative effect of the tolvaptan tablet.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy and relates to a preparation method of tolvaptan tablet. Background technique [0002] When the concentration of sodium ions in the blood plasma decreases, in order to maintain the balance of the concentration of sodium ions inside and outside the cells, extracellular fluid will enter the cells, so that the cells will swell. When brain cells swell, it can lead to various symptoms of hyponatremia. These include dizziness, weakness, headache, nausea, confusion, and reduced consciousness and seizures. Severe hyponatremia can lead to coma and death. [0003] Tolvaptan (Tolvaptan, Chinese chemical name: N-[4-[7-chloro-5-hydroxy-2,3,4,5-tetrahydro-5-benzazepine [0004] -1-formyl]-3-methylphenyl]-2-methylbenzamide) is a selective V2 vasopressin receptor antagonist that can be used to treat congestive heart failure, liver cirrhosis and antidiuretic hormone Hyponatremia due to hyposecretor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/55A61K47/38A61P1/16A61P5/10A61P9/04
Inventor 朱义王一茜戚太林肖捷
Owner SICHUAN BAILI PHARM CO LTD
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