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Novel tenofovir disoproxil fumarate and preparation method thereof

A new technology of tenofovir fumarate, applied in pharmaceutical formulations, medical preparations containing active ingredients, pill delivery, etc., can solve problems such as poor fluidity, easy to corrode punches for tableting, and sour taste of tablets , to achieve the effect of ensuring product quality, avoiding Maillard reaction and extending shelf life

Inactive Publication Date: 2019-11-29
SUZHOU DAWNRAYS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Chinese patent CN104688747B discloses a tenofovir disoproxil fumarate pharmaceutical composition containing succinic acid and its preparation method, but the addition of a large amount of succinic acid can easily lead to sour taste of the tablet, and the tablet is easily corroded shower
[0007] Tenofovir disoproxil fumarate is hygroscopic, easily hydrolyzed, has poor fluidity, contains primary amino groups, and is prone to Maillard reaction with lactose

Method used

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  • Novel tenofovir disoproxil fumarate and preparation method thereof
  • Novel tenofovir disoproxil fumarate and preparation method thereof
  • Novel tenofovir disoproxil fumarate and preparation method thereof

Examples

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Effect test

Embodiment 1

[0024] This embodiment provides a tenofovir disoproxil fumarate tablet, which is obtained by the following preparation steps:

[0025]

[0026]

[0027] Preparation Process:

[0028] Get tenofovir disoproxil fumarate, microcrystalline cellulose, and crospovidone and mix evenly after sieving, add 0.1mol / l hydrochloric acid aqueous solution 1.5g to make soft material as wetting adhesive, use Extrude and spheronize to obtain pellets, dry until the hydrochloric acid volatilizes, and coat with a moisture-proof film coat to obtain the tenofovir disoproxil fumarate pellets. Take an appropriate amount of pellets, add microcrystalline cellulose, magnesium stearate, croscarmellose sodium and lactose, mix evenly, and press them into tablets.

Embodiment 2

[0030] This embodiment provides a tenofovir disoproxil fumarate tablet, which is obtained by the following preparation steps:

[0031]

[0032]

[0033] Preparation Process:

[0034] Take tenofovir disoproxil fumarate, microcrystalline cellulose, and crospovidone and mix evenly after sieving, add 1.5 g of 1 mol / l hydrochloric acid aqueous solution as a wetting adhesive to obtain a soft material, and use an extrusion The pellets are obtained by a spheronizer, dried until the hydrochloric acid volatilizes, and coated with a moisture-proof film coat to obtain the tenofovir disoproxil fumarate pellets. Take an appropriate amount of pellets, add lactose, microcrystalline cellulose, magnesium stearate, and croscarmellose calcium, mix them evenly, and press them into tablets to obtain the product.

Embodiment 3

[0036] This embodiment provides a tenofovir disoproxil fumarate tablet, which is obtained by the following preparation steps:

[0037]

[0038]

[0039]

[0040] Preparation Process:

[0041] Take tenofovir disoproxil fumarate, microcrystalline cellulose, and crospovidone and mix evenly after sieving, add 1.5 g of 2mol / l hydrochloric acid aqueous solution as a wetting adhesive to obtain a soft material, and use an extrusion The pellets are obtained by a spheronizer, dried until the hydrochloric acid volatilizes, and coated with a moisture-proof film coat to obtain the tenofovir disoproxil fumarate pellets. Take an appropriate amount of pellets, add lactose, starch, talcum powder, and carboxymethyl cellulose calcium to the pellets, mix them evenly, and press them into tablets.

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Abstract

The invention discloses novel tenofovir disoproxil fumarate tablets which are prepared by the following steps: mixing tenofovir disoproxil fumarate, a filling agent and a disintegrating agent, furtheradding a wet adhesive so as to obtain a soft material, preparing pellets by using an extrusion spheronization machine, drying the pellets till hydrochloric acid is volatilized, coating the pellets bya dampproof film so as to obtain tenofovir disoproxil fumarate pellets, adding the filling agent, the disintegrating agent and a lubricant into the pellets, performing uniform mixing, and performingpressing tabletting, so as to obtain the novel tenofovir disoproxil fumarate tablets. As a water solution of diluted hydrochloric acid is creatively used as the wet adhesive, degradation of the tenofovir disoproxil fumarate can be avoided; meanwhile, the coated pellets are mixed with lactose, so that the raw materials can be prevented from a Maillard reaction with the lactose; and the product quality is ensured, the medicine stability is improved, the medicine security is improved, and the preservation time of medicines can be prolonged.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a novel tenofovir disoproxil fumarate tablet and a preparation method thereof. Background technique [0002] Tenofovir disoproxil fumarate is an acyclic nucleoside phosphine diester analogue of adenosine monophosphate. Tenofovir disoproxil fumarate is first hydrolyzed into tenofovir in vivo, and then phosphorylated by cellular enzymes to form tenofovir diphosphate. Tenofovir diphosphate inhibits the activity of HIV-1 reverse transcriptase by competing with the natural substrate 5'-triphosphate and then inserting into the viral DNA to terminate the DNA chain. Tenofovir disoproxil fumarate is used in combination with other antiretroviral drugs to treat HIV-1 infection in adults and children over 12 years old, and can also be used to treat chronic hepatitis B in adults. [0003] Tenofovir disoproxil fumarate is a prodrug, and its active ingredient is tenofovir. Because th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/26A61K31/675A61P31/18
CPCA61K9/2081A61K9/2095A61K9/2054A61K9/2018A61K31/675A61P31/18
Inventor 朱爱军缪建洋陈琛姜安娜
Owner SUZHOU DAWNRAYS PHARM CO LTD
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