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Tolvaptan medicinal composition and preparation method thereof

A technology of tolvaptan and a composition, applied in the field of medicine, can solve the problems of insufficient absorption in the gastrointestinal tract, limited dosage form and route of administration, etc.

Inactive Publication Date: 2010-12-22
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to its low water solubility, the problem of tolvaptan is insufficient absorption from the gastrointestinal tract, and the dosage form and route of administration are limited. There are literatures showing that tolvaptan is in the form of an amorphous solid preparation to solve the above problems

Method used

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  • Tolvaptan medicinal composition and preparation method thereof
  • Tolvaptan medicinal composition and preparation method thereof
  • Tolvaptan medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The recipe for making 1000 tablets is as follows:

[0045] Raw materials

Weight (G)

Tolvaptan

15

Hydroxypropyl Beta Cyclodextrin

15

Microcrystalline Cellulose pH102

30

Cross-linked polyvinylpyrrolidone

10

pregelatinized starch

10

lactose

20

Magnesium stearate

1

[0046] steps include

[0047] a) Preparation and processing of raw and auxiliary materials: the raw materials are processed by jet milling; they are mixed with the prescribed amount of hydroxypropyl beta-cyclodextrin, ground and pulverized to make a mixture powder.

[0048] b) Weighing and mixing: Weigh the above-mentioned mixture and other auxiliary materials according to the prescription amount and calculate the feeding amount after checking by two people, and mix them evenly in an equal and incremental manner.

[0049] c) Intermediate inspection: Take the above-mentioned uniformly mixed raw and auxiliary ...

Embodiment 2

[0054] The recipe for making 1000 tablets is as follows:

[0055] Raw materials

Weight (G)

Tolvaptan

30

Hydroxypropyl Beta Cyclodextrin

30

Microcrystalline Cellulose pH102

60

Cross-linked polyvinylpyrrolidone

20

pregelatinized starch

20

lactose

40

[0056] Magnesium stearate

2

[0057] steps include

[0058] a) Preparation and processing of raw and auxiliary materials: the raw materials are processed by jet milling; they are mixed with the prescribed amount of hydroxypropyl beta-cyclodextrin, ground and pulverized to make a mixture powder.

[0059] b) Weighing and mixing: Weigh the above-mentioned mixture and other auxiliary materials according to the prescription amount and calculate the feeding amount after checking by two people, and mix them evenly in an equal and incremental manner.

[0060] c) Intermediate inspection: Take the above-mentioned uniformly mixed...

Embodiment 3

[0065] The recipe for making 1000 tablets is as follows:

[0066] Raw materials

Weight (MG)

Tolvaptan

60

Hydroxypropyl Beta Cyclodextrin

60

Microcrystalline Cellulose pH102

120

Cross-linked polyvinylpyrrolidone

40

pregelatinized starch

40

lactose

80

Magnesium stearate

4

[0067] steps include

[0068] a) Preparation and processing of raw and auxiliary materials: the raw materials are processed by jet milling; they are mixed with the prescribed amount of hydroxypropyl beta-cyclodextrin, ground and pulverized to make a mixture powder.

[0069] b) Weighing and mixing: Weigh the above-mentioned mixture and other auxiliary materials according to the prescription amount and calculate the feeding amount after checking by two people, and mix them evenly in an equal and incremental manner.

[0070] c) Intermediate inspection: Take the above-mentioned uniformly mixed raw and a...

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Abstract

The invention relates to a tolvaptan medicinal composition and a preparation method thereof. 1,000 tablets of the composition consist of 15 to 60 grams of tolvaptan, 15 to 60 grams of hydroxypropyl-beta-cyclodextrin, 30 to 120 grams of microcrystalline cellulose with pH of 102, 10 to 40 grams of cross-linked polyvinylpyrrolidone, 10 to 40 grams of pregelatinized starch, 20 to 80 grams of lactose and 1 to 10 grams of magnesium stearate. In the preparation method, the conventional preparation technology is adopted after the tolvaptan and the hydroxypropyl-beta-cyclodextrin are subjected to special processing. The prepared tolvaptan medicinal composition has the advantages of high fluidity, high dissolution, small tablet weight variation, high stability, high biological utilization degree and good therapeutic effect.

Description

technical field [0001] The invention belongs to the technical field of medicines, and more precisely relates to a preparation method of tolvaptan tablets. Background technique [0002] Tolvaptan, chemical name: N-[4-[(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepine-1-yl)carbonyl ]-3-methylphenyl]-2-methylbenzamide. [0003] Its structural formula is: [0004] [0005] Molecular formula: C 26 h 25 ClN 2 o 3 [0006] Molecular weight: 448.94 [0007] Pharmacological type: Tolvaptan can increase the concentration of sodium ions in the serum, help excrete excess water from the urine, and at the same time, enhance the ability of the kidneys to process water. [0008] Mechanism of action: Tolvaptan is a selective vasopressin V 2 Receptor antagonists, which interact with V 2 The affinity of the receptor is 1.8 times higher than that of arginine vasopressin (AVP), compared with V 1a The receptor has a 29-fold higher affinity. [0009] Indications: Indications f...

Claims

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Application Information

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IPC IPC(8): A61K31/55A61K9/20A61K47/40A61P7/08A61P9/04A61P1/16A61P5/00
Inventor 严洁黄欣
Owner TIANJIN HANKANG PHARMA BIOTECH
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