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Tolvaptan solid dispersion preparation and preparation method thereof

A technology of solid dispersion and tolvaptan, which is applied in the field of tolvaptan solid dispersion preparation and its preparation, and can solve problems such as death and coma

Inactive Publication Date: 2018-04-13
FOSHAN TENGRUI MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Severe hyponatremia can lead to coma and death. There is no corresponding research on tolvaptan tablets in patients with severe hyponatremia

Method used

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  • Tolvaptan solid dispersion preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: Tolvaptan solid dispersion tablet

[0041] prescription:

[0042] components

parts by weight

Tolvaptan

1０

Povidone K30

100

Microcrystalline Cellulose 102

50

Croscarmellose Sodium

20

Sodium dodecyl sulfate

10

silica

2

Sheet weight

192

[0043] Preparation process: solvent evaporation method

[0044] Dissolve the prescribed amount of tolvaptan and povidone K30 in a solvent of acetone:methanol (1:3), volatilize under reduced pressure in a water bath at 60°C, vacuum degree 0.07-0.08MPa, and recover organic matter under reduced pressure. After the solvent becomes viscous, continue vacuum drying under reduced pressure for 1 hour, transfer to a vacuum drying oven, dry at 40°C for 48 hours, and pass through an 80-mesh sieve to pulverize to obtain a solid dispersion.

[0045] The prepared solid dispersion was added into the prescribed amount of microcrystalline cellulose pH102...

Embodiment 2

[0046] Embodiment 2: Tolvaptan solid dispersion tablet

[0047] prescription:

[0048] components

parts by weight

Tolvaptan

20

Povidone K30

100

Microcrystalline Cellulose 102

50

Croscarmellose Sodium

20

Sodium dodecyl sulfate

10

talcum powder

2

Sheet weight

207

[0049] Preparation process: solvent evaporation method

[0050]Take the prescribed amount of tolvaptan and povidone K30, dissolve in the solvent of methanol:dichloromethane (4:1), put in a water bath at 60°C, vacuum degree 0.07-0.08MPa, recover the organic solvent under reduced pressure, wait for After becoming viscous, continue vacuum drying under reduced pressure for 1 hour, transfer to a vacuum drying oven, dry at 40°C for 48 hours, and pass through an 80-mesh sieve to pulverize to obtain a solid dispersion.

[0051] The prepared solid dispersion is added into the prescribed amount of microcrystalline cellulose pH102, crospovi...

Embodiment 3

[0052] Embodiment 3: Tolvaptan solid dispersion tablet

[0053] prescription:

[0054] components

parts by weight

Tolvaptan

30

Povidone K30

100

Microcrystalline Cellulose 102

50

Croscarmellose Sodium

20

Sodium dodecyl sulfate

10

silica

2

Sheet weight

212

[0055] Preparation process: solvent evaporation method

[0056] Dissolve the prescribed amount of tolvaptan and povidone K30 in a solvent of acetone:dichloromethane (3:1), in a water bath at 55°C, with a vacuum of 0.07-0.08MPa, and recover the organic solvent under reduced pressure. After becoming viscous, continue vacuum drying under reduced pressure for 3 hours, transfer to a vacuum drying oven, dry at 60°C for 48 hours, and pass through an 80-mesh sieve to pulverize to obtain a solid dispersion.

[0057] The prepared solid dispersion is added to the prescribed amount of pregelatinized starch, low-substituted hydroxypropyl cellulose, ...

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PUM

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a tolvaptan solid dispersion preparation and a preparation method thereof. The tolvaptan solid dispersion preparation comprises tolvaptan, povidone, a specific lubricant, a specific disintegrant and a specific diluent. Owing to the dissolution effect, the bioavailability and the stability, the industrial productionof the tolvaptan solid dispersion preparation is facilitated.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a tolvaptan solid dispersion preparation and a preparation method thereof. Background technique [0002] Tolvaptan is a non-peptide selective antidiuretic hormone V2 receptor antagonist developed by Otsuka. In May 2009, the FDA approved tolvaptan tablets (tolvaptan, Samsca) for the treatment of hyponatremia. It is the only approved treatment for this disease. Oral selective vasopressin antagonists. It is mainly used to treat hyponatremia caused by congestive heart failure, liver cirrhosis, and antidiuretic hormone deficiency syndrome. A number of clinical randomized controlled studies on the use of this product in the treatment of CHF reported in recent years have suggested that oral administration of tolvaptan can increase the concentration of sodium ions in plasma, help excrete excess water from urine, and significantly reduce the weight and weight of patients. Edem...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K47/32A61K47/04A61K47/20A61K47/12A61K47/02A61K31/55A61P9/04A61P1/16A61P3/12
CPCA61K9/1635A61K9/1611A61K9/1617A61K9/2054A61K9/2077A61K31/55
Inventor 王雪峰
Owner FOSHAN TENGRUI MEDICINE TECH CO LTD
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