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Tenofovir disoproxil fumarate dispersible tablets and preparation method thereof

A technology for tenofovir fumarate and disoproxil, which is applied in the field of tenofovir disoproxil fumarate dispersible tablets and their preparation, can solve problems such as restriction and poor compliance, and achieve fast dissolution rate , Small weight difference, one-sided smooth effect

Active Publication Date: 2012-11-14
杭州康本医药科技有限公司 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the existing reports and uses of this medicine, what really only involves is the medicine of its common tablet dosage form, and common tablet medicine generally needs to help swallowing with the help of drinking water or directly swallowing when taking, and this is just to some such as old people. , children and patients with dysphagia have poor compliance, and the use under special conditions such as going out or lack of drinking water will also be greatly restricted

Method used

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  • Tenofovir disoproxil fumarate dispersible tablets and preparation method thereof
  • Tenofovir disoproxil fumarate dispersible tablets and preparation method thereof
  • Tenofovir disoproxil fumarate dispersible tablets and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0063] prescription:

[0064]

[0065] Preparation method: fully mix tenofovir disoproxil fumarate, mannitol, microcrystalline cellulose, lactose, low-substituted hydroxypropyl cellulose, and aspartame, and pulverize them through a 100-mesh sieve. 5% starch aqueous solution is made into 20-mesh wet granules, dried at 55°C for 3 hours, sieved with 18-mesh sieve, added with crospovidone, sodium lauryl sulfate, and magnesium stearate and mixed thoroughly, then the content is determined , the adjustment sheet is repressed into a sheet.

Embodiment 2

[0067] prescription:

[0068] Preparation method: fully mix tenofovir disoproxil fumarate, mannitol, microcrystalline cellulose, lactose, low-substituted hydroxypropyl cellulose, and aspartame, and pulverize them through a 100-mesh sieve. 3% povidone aqueous solution is made into 20-mesh wet granules, dried at 55°C for 3.5 hours, sieved with 18-mesh sieves, added crospovidone, sodium lauryl sulfate, micropowder silica gel, magnesium stearate and fully mixed After uniformity, measure the content, adjust the weight of the tablet and press it into a tablet.

Embodiment 3

[0070] prescription:

[0071] Preparation method: fully mix tenofovir disoproxil fumarate, microcrystalline cellulose, lactose, low-substituted hydroxypropyl cellulose, and aspartame, and pulverize them through a 100-mesh sieve, add an appropriate amount of 5% starch The aqueous solution is made into 20-mesh wet granules, dried at 50°C for 3 hours, sieved with 18-mesh sieve, added with crospovidone, sodium lauryl sulfate, and magnesium stearate and mixed thoroughly, then measuring the content and adjusting the tablet Pressed into pieces.

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Abstract

The invention discloses tenofovir disoproxil fumarate dispersible tablets and a preparation method thereof. The tenofovir disoproxil fumarate dispersible tablets are prepared from tenofovir disoproxil fumarate as an effective pharmaceutical ingredient and pharmaceutically acceptable auxiliary ingredients, wherein the pharmaceutically acceptable auxiliary ingredients comprise a filler, a disintegrant, a lubricant, a surfactant and a flavoring agent. The tenofovir disoproxil fumarate dispersible tablets prepared by the invention have appropriate hardness, small weight difference, bright and clean tablet surfaces and good taste, fully meet the requirements on the disintegration time and dispersion uniformity of dispersible tablets, and notably improve the pharmaceutical bioavailability, and in addition, the tenofovir disoproxil fumarate dispersible tablets have quick dissolution rate, the dissolution percentage of the product is about 80-90% in 2 minutes, and the product is almost completely dissolved in 5 minutes.

Description

(1) Technical field [0001] The invention relates to a dispersible tablet preparation of anti-AIDS virus (HIV) and hepatitis B virus (HBV) drug tenofovir disoproxil fumarate and a preparation method thereof. (2) Background technology [0002] Tenofovir disoproxil fumarate (English name: Tenofovir disoproxil fumarate) is an ester prodrug of tenofovir, which belongs to a new type of nucleotide reverse transcriptase inhibitor, which can inhibit the development of HIV and HBV viruses. copy. Its main mechanism of action is that it is hydrolyzed into tenofovir after oral administration, and tenofovir is phosphorylated by cellular kinases to generate a pharmacologically active metabolite tenofovir diphosphate, which is combined with 5′-triphosphate deoxyadenosine Competing, participating in the synthesis of viral DNA, after entering the viral DNA, due to the lack of 3'-OH group, the DNA elongation is hindered, thereby blocking the replication of the virus. The current clinical app...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/675A61P31/18A61P31/20
Inventor 史磊游金宗蒋善会任海华
Owner 杭州康本医药科技有限公司
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