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Solid preparation of epalrestat solid dispersion and preparation method thereof

A technology of solid dispersion and epalrestat, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulations, etc., which can solve the problems of difficult absorption and utilization of preparations, low in vitro dissolution rate, Poor solubility and other problems, to achieve the effect of improving bioavailability, easy preparation process, and accelerated dissolution rate

Inactive Publication Date: 2016-12-07
YANGTZE RIVER PHARM GRP NANJING HAILING PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Epalrestat belongs to BSC II substances with low solubility and high permeability. It has poor solubility and low dissolution rate in vitro. It is difficult to effectively absorb and utilize it with common preparations.

Method used

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  • Solid preparation of epalrestat solid dispersion and preparation method thereof
  • Solid preparation of epalrestat solid dispersion and preparation method thereof
  • Solid preparation of epalrestat solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The solid preparation of the epalrestat solid dispersion of the present embodiment is made up of epalrestat solid dispersion and auxiliary materials, wherein said epalrestat solid dispersion is made up of epalrestat raw material, solubilizer meglumine and carrier material PEG-4000 and PEG-6000 are composed according to the weight ratio of 1:0.5:0.5; the excipients include filler mannitol, disintegrant low-substituted hydroxypropyl cellulose and sodium carboxymethyl starch, binder hydroxypropyl methyl base cellulose and glidant micropowder silica gel; the ratio of epalrestat solid dispersion and auxiliary materials is according to weight: 100 parts of solid dispersion, 14.75 parts of filler, 7.5 parts of disintegrant, 2.5 parts of binder, auxiliary 0.25 part of liquid agent, as shown in table 1:

[0034] Table 1 The prescription ratio of epalrestat solid dispersion and auxiliary materials (specification 50mg, 1000 tablets)

[0035]

[0036]

[0037] The preparatio...

Embodiment 2

[0042] The solid preparation of the epalrestat solid dispersion of the present embodiment is made up of epalrestat solid dispersion and auxiliary materials, wherein said epalrestat solid dispersion is made up of epalrestat raw material, solubilizer meglumine and carrier material PVPK30 is composed according to the weight ratio of 1:5:5; the excipients include filler microcrystalline cellulose, disintegrant low-substituted hydroxypropyl cellulose, binder hydroxypropyl cellulose and glidant talc; The ratio of other solid dispersions and auxiliary materials is shown in Table 2:

[0043] Table 2 The prescription ratio of epalrestat solid dispersion and auxiliary materials (specification 50mg, 1000 tablets)

[0044]

Prescription volume (g)

Prescription ratio (%)

Epalrestat solid dispersion

550.00

89.4

microcrystalline cellulose

17.65

2.9

Low-substituted hydroxypropyl cellulose

33.83

5.5

Hypromellose

12.30

2.0

...

Embodiment 3

[0050] The solid preparation of the epalrestat solid dispersion of the present embodiment is made up of epalrestat solid dispersion and auxiliary materials, wherein said epalrestat solid dispersion is made up of epalrestat raw material, solubilizer meglumine and carrier material Mannitol is composed according to the weight ratio of 1:0.2:10; the auxiliary materials include filler lactose, binder hydroxypropyl methylcellulose, disintegrant cross-linked polyvinylpyrrolidone and glidant micropowder silica gel; The ratio of other solid dispersions and auxiliary materials is shown in Table 3:

[0051] Table 3 The prescription ratio of epalrestat solid dispersion and excipients (specification 50mg, 1000 capsules)

[0052]

Prescription volume (g)

Prescription ratio (%)

Epalrestat solid dispersion

560.00

92.6

lactose

13.54

2.2

Hydroxypropylmethylcellulose

18.15

3.0

Cross-linked polyvinylpyrrolidone

12.10

2.0

M...

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Abstract

The invention belongs to the field of pharmaceutical preparations and particularly relates to a solid preparation of epalrestat solid dispersion and a preparation method thereof. The solid preparation of epalrestat solid dispersion is composed of epalrestat solid dispersion and auxiliaries, wherein the epalrestat solid dispersion is made from epalrestat material, a solubilizer and a carrier material according to a weight ratio of 1:(0.2-5):(0.5-10); the preparation method includes: dispersing the carrier material in an organic solvent, adding the solubilizer and epalrestat to obtain a mixed solution, spray-drying the mixed solution to obtain epalrestat solid dispersion powder, and adding the auxiliaries to produce tablets or capsules. The solid preparation of epalrestat solid dispersion provided herein is better in solubility, the quantity of the solid preparation to dissolve in a difficultly soluble medium can be greatly increased, bioavailability of the solid preparation is thus improved, and efficacy of the solid preparation is guaranteed; the preparation process is easy to control and is available for large-scale production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid preparation of epalrestat solid dispersion and a preparation method thereof. Background technique [0002] Solid dispersion technology is a new technology for highly dispersing insoluble drugs in solid carrier materials to form solid dispersions. In the solid dispersion formed by the insoluble drug and a suitable carrier, the drug exists in a microcrystalline state, an amorphous state, a colloidal dispersed state or a molecularly dispersed state, and has a large degree of dispersion. When it contacts with gastrointestinal fluid, The dissolution rate of the drug is accelerated, which can promote the absorption of the drug and improve the bioavailability. Solid dispersions can be regarded as intermediates for the preparation of immediate-release, sustained-release or enteric-coated preparations of drugs. [0003] First launched in Japan in 1992, epal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/426A61K47/34A61K47/32A61K47/26A61K47/18A61P3/10A61P13/12A61P9/14A61P25/00
CPCA61K9/1617A61K9/1635A61K9/1641A61K9/1652A61K31/426
Inventor 苏凤刘杨束志凌丁菲贾树田
Owner YANGTZE RIVER PHARM GRP NANJING HAILING PHARM CO LTD
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