Pharmaceutical composition for treating diabetic neuropathy and preparation method thereof

A technology of composition and medicine, which is applied in the fields of pharmaceutical composition for treating diabetic neuropathy and its preparation, epalrestat tablet and its preparation, and can solve the problem of the average dissolution rate of epalrestat tablets and the difference in dissolution rate between tablets. Large and other problems, to achieve the effect of improving bioavailability, increasing average dissolution rate, accelerating release and absorption

Pending Publication Date: 2022-07-19
YANGTZE RIVER PHARM GRP NANJING HAILING PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] What the present invention will solve is the technical problem that the average dissolution rate of existing epalrestat tablets and the difference in dissolution rate between tablets are relatively large, thereby proposing a kind of epalrestat pharmaceutical composition and preparation method thereof

Method used

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  • Pharmaceutical composition for treating diabetic neuropathy and preparation method thereof
  • Pharmaceutical composition for treating diabetic neuropathy and preparation method thereof
  • Pharmaceutical composition for treating diabetic neuropathy and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Prescription: epalrestat 45.45%, mannitol 47%-48%, low-substituted hypromellose 4.0%, hypromellose 1-3%, magnesium stearate 1.0%, appropriate amount of water (to prepare adhesive )

[0036] preparation:

[0037] 1) Micro-differentiate the prescription amount of epalrestat and pulverize to different particle sizes in the following table;

[0038] 2) adding water to the recipe quantity of hypromellose, the preparation hypromellose concentration is 3%;

[0039] 3) adding the micronized epalrestat, mannitol and low-substituted hydroxypropyl cellulose of the recipe quantity into a wet mixing granulator in order for mixing, adding step 2) binder, and granulating;

[0040] 4) in step 3) granule, add recipe quantity lubricant, mix well, press tablet;

[0041] 5) Add the coating material of the recipe quantity, coat, and get the product.

[0042] The dissolution curves of formulations with different particle sizes of raw materials in 1.5% SDS-pH4.5 medium were determined. Th...

Embodiment 2

[0049] Prescription: epalrestat 45.45%, mannitol 46.05%, low-substituted hypromellose 4.00%, hypromellose 3.50%, magnesium stearate 1.00%, appropriate amount of water (to prepare binder)

[0050] Preparation: Same as Example 1.

[0051]Determination of the dissolution curves of formulations with different particle sizes of raw materials in 1.5% SDS-pH4.5 medium:

[0052]

[0053]

[0054] The results show that when the particle size of the raw material is D90≤6μm, the cumulative dissolution rate at each time point is higher than that of the reference preparation or similar to the reference preparation, and f2>70. Equivalence study, the test results are shown in the table:

[0055]

[0056] The results show that when the particle size D90 of the raw material is less than or equal to 6 μm, the geometric mean value and confidence interval of the prepared preparation are both improved.

Embodiment 3-5

[0058]

[0059] preparation:

[0060] 1) Differentiate the prescription amount of epalrestat to a particle size of D90≤6μm;

[0061] 2) water is added to recipe quantity hypromellose, and is mixed with the aqueous solution of concentration (w / w) 5%;

[0062] 3) take by weighing epalrestat (micronized), mannitol, and the adhesive prepared in step 2) according to the prescribed dosage and transfer it to the fluidized bed for granulation;

[0063] 4) In step 3) the granules are mixed with low-substituted hydroxypropyl cellulose in the recipe quantity, then a lubricant in the recipe quantity is added, mixed evenly, and pressed into tablets.

[0064] Dissolution profiles of different examples in 1.5% SDS-pH 4.5 medium:

[0065]

[0066]

[0067] It can be seen from Examples 3-5 that although the dissolution curves of each formulation in 1.5% SDS-pH4.5 medium are similar to those of the reference formulation, except for 60 and 90 min, the cumulative dissolution at other t...

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Abstract

The invention discloses a pharmaceutical composition for treating diabetic neuropathy and a preparation method thereof, and particularly relates to an epalrestat tablet and a preparation method thereof, the epalrestat tablet comprises 40-50% of epalrestat, 45-50% of mannitol, 1-5% of a disintegrating agent, 1-5% of an adhesive and 0.5-2% of a lubricant, and the particle size D90 of the epalrestat tablet is less than or equal to 15 microns. According to the epalrestat pharmaceutical composition disclosed by the invention, epalrestat is crushed until the particle size (D90) is less than 15 microns, so that the specific surface area of raw material medicine particles is increased, the release and absorption of effective components are accelerated, the average dissolution rate and bioavailability of prepared epalrestat tablets are improved, and the dissolution rate difference between the tablets is reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and discloses a pharmaceutical composition for treating diabetic neuropathy and a preparation method thereof, in particular to an epalrestat tablet and a preparation method thereof. Background technique [0002] Diabetic peripheral neuropathy is a common complication of diabetes. Its main pathological changes are distal neuropathy, staged demyelination and nerve fiber loss. The main clinical manifestations are pain, numbness and hypoesthesia. Failure to treat it incorrectly can easily lead to muscle atrophy or even amputation, which is one of the main causes of disability in diabetes. As a representative drug of aldose reductase inhibitor, epalrestat can play a therapeutic role by blocking the polyol pathway and reducing the production of carboxymethyl lysine. Epalrestat, chemical name: 5-[(1Z,2E)-2-methyl-3-phenyl-2-propenylidene]-4-oxo-2-thio-3-thiazole Alkanoic acid, a reversible n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/32A61K31/426A61K47/38A61K47/32A61P3/10A61P25/02
CPCA61K9/2866A61K9/2853A61K9/2054A61K9/2027A61K31/426A61P3/10A61P25/02
Inventor 吴炎杨丹苏叶青
Owner YANGTZE RIVER PHARM GRP NANJING HAILING PHARM CO LTD
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