Tolvaptan oral preparation and preparation method thereof

A technology of tolvaptan and oral preparations, applied in the field of chemical pharmaceuticals, can solve the problems of affecting bioavailability, dissolution rate reduction, etc., and achieve the effect of ensuring bioavailability
CN113171344AActive Publication Date: 2021-07-27NANJING HEALTHNICE MEDICAL TECH +2
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
NANJING HEALTHNICE MEDICAL TECH
Publication Date
2021-07-27

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Abstract

The invention relates to a tolvaptan oral preparation and a preparation method thereof. The preparation method comprises the following steps: firstly, dispersing a tolvaptan bulk drug into a carrier-hydroxypropyl cellulose and an organic solvent; dispersing the tolvaptan bulk drug in a carrier-hydroxypropyl methylcellulose phthalate and an organic solvent, respectively carrying out spray drying by adopting an explosion-proof closed nitrogen circulation spray dryer, and strictly controlling process parameters in the spray drying process, and drying under reduced pressure to prepare two solid dispersions of tolvaptan: a water-soluble solid dispersion and an enteric solid dispersion, wherein the two solid dispersions are then combined with excipients to prepare tolvaptan oral preparations, the quick-release solid dispersion is dissolved in the stomach, the enteric-soluble solid dispersion is dissolved in the intestinal tract, so that the condition of precipitation caused by overhigh local concentration and oversaturation is reduced, and the bioavailability of the medicine can be better ensured.
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Description

technical field

[0001] The invention belongs to the technical field of chemical pharmacy, and relates to a tolvaptan oral preparation and a preparation method thereof. Background technique

[0002] Tolvaptan (Tolvaptan), the chemical name is N-[4-[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine -1-formyl]-3-methylphenyl]-2-methylbenzamide, the structural formula is as follows:

[0003]

[0004] Tolvaptan is a white crystal or crystalline powder, slightly soluble in methanol or ethanol (99.5), almost insoluble in water, belongs to BCS IV drugs, has low solubility and low permeability properties, and needs to improve its physical and chemical properties to increase its solubility and permeability to achieve the effect of improving dissolution and bioavailability.

[0005] Solid dispersion refers to a dispersion system in which a drug is highly dispersed in a water-soluble material, insoluble or enteric-soluble material in a molecular or amorphous state. Immedia...

Claims

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