Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Emtricitabine-containing tablet and preparation method thereof

A technology for emtricitabine and tablets, which is applied in the field of drug preparation, can solve the problems of affecting tablet stability, release of active ingredients, instability of acids, bases and oxidants, incomplete suitability for AIDS patients, etc., and achieves easy industrial production, Accurate dosage and high dissolution effect

Inactive Publication Date: 2014-08-27
BEIJING UNION PHARMA FACTORY +1
View PDF5 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, fixed-dose compound preparations suitable for foreign populations are not completely suitable for Chinese AIDS patients, and it is inconvenient to adjust the dose
And, in the preparation of the medicine containing emtricitabine at present, capsule and oral solution are first-selected by most producers, and this is because the dose of emtricitabine is relatively large, if made into tablet, cause tablet weight to be heavier when the excipient addition amount is many large, difficult to take
In addition, emtricitabine is unstable to acid, alkali and oxidant, and if the excipients used in the preparation of tablets are improperly selected, it will affect the stability of the tablet and the release of active ingredients.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Emtricitabine-containing tablet and preparation method thereof
  • Emtricitabine-containing tablet and preparation method thereof
  • Emtricitabine-containing tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0045] The proportioning ratio of raw materials and auxiliary materials in Examples 1 to 3 is shown in Table 1, and the preparation methods are basically the same, and reference can be made to the preparation method in Example 1 below.

[0046] Table 1

[0047]

[0048] The preparation method of the tablet containing emtricitabine in embodiment 1 comprises the following steps:

[0049] (a) The preparation method of the adhesive (50% ethanol solution of 10% povidone K30) is as follows: dissolve 4.8 g of povidone K30 in 43.2 g of 50% ethanol aqueous solution, stir until dissolved, and set aside.

[0050] (b) Preparation of mixture granules: as shown in Table 1, add the required amount of emtricitabine, lactose and carboxymethyl starch sodium into the wet mixing granulator, stir and mix for 400 seconds, and wait until the mixture is uniform , add 48g of 10% povidone K30 in 50% ethanol solution to the granulator, wet granulate for 90 seconds, and dry at 60°C until the water co...

Embodiment 4～6

[0053] Examples 4 to 6 are as shown in Table 2. For the preparation method, refer to the preparation method of Example 1, wherein in step (2), after 60 seconds of wet granulation, dry at 50°C.

[0054] Table 2

[0055]

Embodiment 7～10

[0057] The proportioning ratio of raw materials and auxiliary materials in Examples 7-10 is shown in Table 3. For the preparation method, refer to the preparation method of Example 1, wherein in step (2), after wet granulation for 120 seconds, dry at 70°C.

[0058] table 3

[0059]

[0060] Long-term Stability Test

[0061] The sample of the emtricitabine-containing tablet prepared in Example 1 was subjected to a long-term stability test at room temperature, and the results are shown in Table 4.

[0062] Table 4

[0063] time

character

tablet weight difference

Dissolution (%)

Content (%)

relative substance(%)

0 months

Compliance

Compliance

99.98

95.98

0.42

March

Compliance

Compliance

101.97

95.70

0.51

June

Compliance

Compliance

100.79

96.26

0.34

September

Compliance

Compliance

99.12

95.56

0.42

December

Compliance ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to an emtricitabine-containing tablet, which is composed of emtricitabine accounting for 30-80% of the total weight of the tablet and pharmaceutical adjuvants accounting for 20-70% of the total weight of the tablet. The pharmaceutical adjuvants contain a diluents accounting for 10-30% of the total weight of the tablet and a disintegrating agent accounting for 3-10% of the total weight of the tablet. The tablet provided by the invention has the characteristics of good stability, high l dissolution rate, appropriate tablet weight, and convenient drinking. Due to adoption of the single active component emtricitabine, the dosage is accurate. During use, the dosage can be adjusted according to the actual situation, thus facilitating combined use with other antiviral drugs. The preparation method provided by the invention has the advantages of simple process, cheap and easily available adjuvants, and easy industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a tablet containing emtricitabine and a preparation method thereof. Background technique [0002] Acquired immunodeficiency syndrome (AIDS) is a malignant infectious disease caused by human immunodeficiency virus (HIV). HIV is a single-stranded RNA virus of two types: HIV-1 and HIV-2. HIV-1 is the main type of HIV in the world, accounting for 95%, and HIV-2 is concentrated in West Africa. The main routes of transmission are sexual contact, blood transmission and mother-to-child transmission. [0003] HIV is the pathogen that causes AIDS. However, after HIV enters the human body, what it attacks is the central cell of the human immune system - T4 lymphocytes, resulting in excess resistance of the human body, thus producing vaccines for other people to use. HIV HIV is a virus that attacks the internal organs of the human body. It takes the most importa...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/513A61P31/18
Inventor 潘显道吕亚光吕昭云王迷娟张猛张颖王珂赵立敏
Owner BEIJING UNION PHARMA FACTORY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com