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Sofosbuvir and dalatasvir double-layer tablet and preparation method thereof

A technology of sofosbuvir and daclatasvir, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of different dissolution behaviors, and improve the accuracy of medication rate, improving dissolution rate and stability, and preventing loss

Pending Publication Date: 2021-10-01
FUJIAN COSUNTER PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] In order to solve the problem that the existing two pharmaceutical preparations have different dissolution behaviors in the body and need to be purchased separately and wait for administration, the present invention provides a double-layer tablet of sofosbuvir and daclatasvir, which is used for the treatment of hepatitis C virus infection and has a relatively High dissolution rate, better stability and stronger efficacy

Method used

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  • Sofosbuvir and dalatasvir double-layer tablet and preparation method thereof
  • Sofosbuvir and dalatasvir double-layer tablet and preparation method thereof
  • Sofosbuvir and dalatasvir double-layer tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] For a Cable with Dallas oseltamivir phosphate Bouvet bilayer tablet, comprising a first ply and a second ply, the first ply comprises cords phosphorus Bouvet 200mg, mannitol 150mg, microcrystalline cellulose 250mg, cross-linked sodium carboxymethyl cellulose 30mg, povidone 50mg, 10mg magnesium stearate; Dara said second ply comprises oseltamivir 30mg, anhydrous lactose 75mg, microcrystalline cellulose 50mg, croscarmellose cellulose, sodium 5mg, povidone 5mg, magnesium stearate 10mg.

[0043] Cable phosphorus Bouvet above production method Dallas bilayer tablet as oseltamivir,

[0044] Preparation S1 cable phosphorus particles Bouvet

[0045] S11 micronization process: Weigh weight of said respective cable phosphorus Bouvet micronized treatment, the cable phosphorus particles after micronization Bouvet by less than 0.25mm;

[0046] The raw material mixed S12: Increment method using the same amount of phosphorus Bouvet cable with mannitol, microcrystalline cellulose and crosc...

Embodiment 2

[0057] Example 2: A Schodikikir with Dallawei Double-layer sheet including the first sheet and a second sheet, the first layer contains 400 mg, the mannitol 150mg, microcrystals Cellulose 200mg, 45 mg of crosslinked carboxymethylcellulose sodium crosslinked carboxymethylcellulose, 60 mg of stearate, magnesium stearate 45mg; the second layer contains 60 mg of Dallavi, anhydrous lactose 100mg, microcrystalline cellulose 100 mg, Crosslinked carboxymethylcellulose 10 mg, polyesterin 10 mg, magnesium stearate 20 mg.

[0058] The preparation method of the above-mentioned Schodikovir and Dallawei double-layer sheet is as follows.

[0059] Preparation of S1 Sony Phosphi Granules

[0060] S11 micronization treatment: Weigh the corresponding weight of the soil phosphori to carry out micronization treatment, so that the particles of the micronized sobblewell are less than 0.25 mm;

[0061] S12 raw material mixing: Use an equal amount of additive sodiol, microcrystalline, and cross-linked car...

Embodiment 3

[0071] Example 3: A Schodikikir and Dallawei Double-layer sheet including a first sheet and a second sheet, and the first sheet contains 200 mg, mannitol 100mg, microcrystals. Cellulose 150 mg, 3 mg of crosslinked carboxymethylcellulose, 50 mg of polyesterone, 20 mg of stearate. Corresponding, the second layer contains the following weight component, including Dallasiwell hydrochloride 33mg, anhydrous lactose 100mg, microcrystalline cellulose 50 mg, 5 mg of crosslinked carboxymethylcellulose 5mg, pp 10 mg , Stearate 15 mg.

[0072] The preparation method of the above-mentioned Schodikovir and Dallawei double-layer sheet is as follows.

[0073] Preparation of S1 Sony Phosphi Granules

[0074] S11 micronization treatment: Weigh the corresponding weight of the soil phosphori to carry out micronization treatment, so that the particles of the micronized sobblewell are less than 0.25 mm;

[0075] S12 raw material mixing: Use an equal amount of additive sodiol, microcrystalline, and cros...

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Abstract

The invention relates to a sofosbuvir and dalatasvir double-layer tablet and a preparation method thereof, and belongs to the field of medicines. according to the sofosbuvir and dalatasvir double-layer tablet, a first layer of tablet contains sofosbuvir; and the second layer tablet comprises daratasvir or / and pharmaceutically acceptable salts thereof. The preparation method comprises the following steps: micronizing sofosbuvir, mixing the micronized sofosbuvir with the filler and the disintegrating agent, adding the adhesive, granulating, drying, and mixing with the lubricant to prepare sofosbuvir granules; uniformly mixing dalatasvir or / and pharmaceutically acceptable salt thereof with a filler and a disintegrating agent, adding an adhesive, granulating, and mixing with a lubricant to prepare dalatasvir granules; sofosbuvir particles and dalatasvir particles are respectively prepared into a first layer tablet and a second layer tablet, the first layer tablet and the second layer tablet are pressed to obtain a plain tablet, and the plain tablet is coated to form a double-layer tablet. The double-layer tablet disclosed by the invention is used for treating hepatitis C, and has relatively high dissolution rate, better stability and stronger drug effect.

Description

Technical field [0001] The present invention relates to the preparation of a medicament, in particular to a rope and Dallas oseltamivir phosphate Bouvet bilayer tablet and preparation method. Background technique [0002] Cable phosphorus Bouvet (Sofosbuvir, Sovaldi) developed by the US company Gilead Sciences, approved and listed on the 2014 FDA, approved the listing in China in September 2017. Cable bouvet phosphorus is essential for viral replication of hepatitis C virus (HCV) non structural protein 5B (NS5B) ribonucleic acid (RNA) - dependent RNA polymerase inhibitor. Depending on the type of hepatitis C virus, phosphorus Bouvet cable clinical cure rate of 30% to 97%. [0003] Cable phosphorus bouvet structural formula as follows: [0004] [0005] Dara oseltamivir (Daclatasvir, Daklinza) is highly selective inhibitor developed by the Bristol-Myers Squibb's hepatitis C NS5A protein. Dara hydrochloride tablets oseltamivir combination with other drugs for the treatment of adu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K9/24A61K31/4178A61K31/7072A61K47/38A61K47/32A61K47/26A61P1/16A61P31/14
CPCA61K9/209A61K9/2054A61K9/2027A61K9/2018A61K9/2806A61K31/7072A61K31/4178A61P1/16A61P31/14A61K2300/00
Inventor 姚建堤周巧云
Owner FUJIAN COSUNTER PHARMA CO LTD