Tenofovir alafenamide enteric-coated tablet and preparation method thereof

A technology of alafenamide enteric and tenofovir, which is applied in the field of medicine, can solve problems such as the lack of research on alafenamide enteric-coated preparations, and achieve improved safety and effectiveness, complete coating, The effect of uniform intestinal distribution

Active Publication Date: 2019-04-05
中润药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as of now, there is no relevant research on tenofovir alafenamide enteric-coated preparations at home and abroad.

Method used

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  • Tenofovir alafenamide enteric-coated tablet and preparation method thereof
  • Tenofovir alafenamide enteric-coated tablet and preparation method thereof
  • Tenofovir alafenamide enteric-coated tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065]

[0066] The preparation method comprises the steps of:

[0067] 1) Granulation: Weigh 25 parts of tenofovir alafenamide, 28 parts of dextrin, 28 parts of starch, 14 parts of lactose, and 5 parts of cross-linked povidone, and add them into a wet mixing granulator. Mixing, making soft materials, granulating, drying, granulating and other process steps to obtain granular inner cores;

[0068] 2) enteric coating: use 95% ethanol as solvent, add 76.3 parts of L100, stir until dissolved, continue to add 15.8 parts of triethyl citrate, 7.9 parts of talcum powder, stir and mix with a mixer for 45 minutes, then pass the suspension through an 80-mesh sieve to make an enteric coating solution, and use a flow Chemical bed coating technology, evenly spray the enteric coating solution on the granular inner core, until the weight of the enteric coating increases by 5.0-8.0%, and dry at 40-50°C for 3 hours to obtain enteric-coated granules;

[0069] 3) Tablet compression: Mix 73...

Embodiment 2

[0072]

[0073] The preparation method of the tenofovir alafenamide enteric-coated tablets in Example 2 is the same as in Example 1, except that the prescription of the tenofovir alafenamide enteric-coated tablets is the prescription in Example 2.

Embodiment 3

[0075]

[0076]

[0077] The preparation method of the tenofovir alafenamide enteric-coated tablets in Example 3 is the same as in Example 1, except that the prescription of the tenofovir alafenamide enteric-coated tablets is the prescription in Example 3.

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Abstract

The invention discloses a tenofovir alafenamide enteric-coated tablet and a preparation method thereof. The enteric-coated tablet comprises a tablet core and a peripheral layer, wherein the tablet core contains enteric particles, a second filler, a second disintegrating agent and a glidant; the enteric particles contain an inner core and an enteric coating; and the inner core contains tenofouvir alafenamide, a first filler and a first disintegrating agent. The tenofovir alafenamide enteric-coated tablet is prepared by the preparation method successfully, and the limitation that the tablet mustbe taken with food is broken; and the bioavailability and the efficacy can not be affected by the type and amount of the food, and the safety and effectiveness of medication are improved through theenteric-coated tablet. The enteric-coated tablet is prepared by the process of enteric-coated multi-unit granule tabletting, so that the tablet is uniformly distributed after being taken orally, and the stimulation to the gastrointestinal tract caused by the excessive local concentration of drug is avoided. At the same time, the problems of poor compressibility of the tenofovir alafenamide, much fine powder from dry granulation, and uneven subsequent enteric-coated coating are overcame through the tenofovir alafenamide enteric-coated tablet. The preparation process is simple and the preparation conditions are controllable.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tenofovir alafenamide enteric-coated tablet and a preparation method thereof. Background technique [0002] The "2017 Global Hepatitis Report" shows that there are 30 million chronic hepatitis B patients in my country, and only 2 million people have received treatment, which is less than 1 / 10 of the total. At present, hepatitis B still ranks first among the four major infectious diseases that my country focuses on prevention and control, and patients with hepatitis B are mainly treated with nucleoside drugs, with tenofovir or entecavir being the first choice. [0003] Tenofovir alafenamide is an ester prodrug of tenofovir, and its ordinary tablet has been approved for marketing in Europe, America and Japan, but it has not yet been marketed in my country. Compared with tenofovir that has been on the market, the clinical dosage of tenofovir alafenamide is smaller, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/20A61K47/38A61K31/675A61P31/20A61P1/16
CPCA61K9/2054A61K9/2081A61K9/2866A61K31/675A61P1/16A61P31/20
Inventor 魏林华朱少璇何清林俊生易德平张传宝
Owner 中润药业有限公司
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