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Dolutegravir film coated tablet preparation and preparation method thereof

A technology of film coating and dolutegravir, which is applied in the field of dolutegravir film-coated tablet formulation and its preparation, can solve the problems of high cost and achieve the effects of breaking the price monopoly, stable blood concentration and uniform distribution

Inactive Publication Date: 2018-05-08
顾世海
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, domestic research on dolutegravir film-coated tablet preparations is still blank. Facing the high price of new drugs just launched, it is imperative to develop a safe, effective and cheap dolutegravir film-coated tablet preparation.

Method used

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  • Dolutegravir film coated tablet preparation and preparation method thereof
  • Dolutegravir film coated tablet preparation and preparation method thereof
  • Dolutegravir film coated tablet preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Prescription composition: Prescription amount (mg / tablet)

[0044] Dolutegravir 50

[0045] Mannitol 314

[0046] Sodium carboxymethyl starch 32

[0047] Sodium stearyl fumarate 4

[0048] According to above-mentioned prescription quantity, preparation process is as follows:

[0049] (1) Material pretreatment: sieve dolutegravir, diluent, disintegrant, lubricant, and set aside;

[0050] (2) Mixing: Weigh the prescription amount of active drug dolutegravir, diluent, disintegrant, lubricant and mix evenly;

[0051] (3) Place the mixed powder in (2) in a dry granulator for granulation:

[0052] (4) Total mixing: Mix the dry granules prepared in (3) evenly with the prescribed amount of disintegrant and lubricant;

[0053] (5) Compress plain tablets: place the granules prepared in (4) in a high-speed rotary tablet press;

[0054] (6) Film coating: film-coat the qualified tablets prepared in (5).

Embodiment 2

[0056] Dolutegravir 50

[0057] Mannitol 314

[0058] Povidone 32

[0059] Sodium stearyl fumarate 4

[0060] According to above-mentioned prescription quantity, preparation process is as follows:

[0061] (1) Material pretreatment: sieve dolutegravir, diluent, disintegrant, lubricant, and set aside;

[0062] (2) Mixing: Weigh the prescription amount of active drug dolutegravir, diluent, disintegrant, lubricant and mix evenly;

[0063] (3) Place the mixed powder in (2) in a dry granulator for granulation:

[0064] (4) Total mixing: Mix the dry granules prepared in (3) evenly with the prescribed amount of disintegrant and lubricant;

[0065] (5) Compress plain tablets: place the granules prepared in (4) in a high-speed rotary tablet press;

[0066] (6) Film coating: film-coat the qualified tablets prepared in (5).

Embodiment 3

[0068] Dolutegravir 50

[0069] Microcrystalline Cellulose 314

[0070] Sodium carboxymethyl starch 32

[0071] Sodium stearyl fumarate 4

[0072] According to above-mentioned prescription quantity, preparation process is as follows:

[0073] (1) Material pretreatment: sieve dolutegravir, diluent, disintegrant, lubricant, and set aside;

[0074] (2) Mixing: Weigh the prescription amount of active drug dolutegravir, diluent, disintegrant, lubricant and mix evenly;

[0075] (3) Place the mixed powder in (2) in a dry granulator for granulation:

[0076] (4) Total mixing: Mix the dry granules prepared in (3) evenly with the prescribed amount of disintegrant and lubricant;

[0077] (5) Compress plain tablets: place the granules prepared in (4) in a high-speed rotary tablet press;

[0078] (6) Film coating: film-coat the qualified tablets prepared in (5).

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Abstract

The invention discloses a dolutegravir film coated tablet preparation and a preparation method thereof, wherein the dolutegravir film coated tablet preparation comprises the following active components by mass: 10-20% of dolutegravir, 10-90% of a diluent, 2.0-8.0% of a disintegrant, and 0.5-1.5% of a lubricant, wherein the diluent is one or a plurality of materials selected from mannitol, microcrystalline cellulose, lactose and polyethylene glycol, preferably mannitol and microcrystalline cellulose, the disintegrant is one or a plurality of materials selected from croscarmellose sodium, sodiumcarboxymethyl starch, povidone and hypromellose, preferably sodium carboxymethyl starch and povidone, and the lubricant is one or a plurality of materials selected from magnesium stearate, talc powder, micro-powder silica gel and sodium stearyl fumarate, preferably magnesium stearate and sodium stearyl fumarate. According to the present invention, the preparation method has advantages of simple process, high yield, good product stability, easy mass industrial production and the like.

Description

technical field [0001] The invention discloses a dolutegravir film-coated tablet preparation and a preparation method thereof, which are applied in the field of preparation of preparations for treating acquired immune deficiency syndrome (AIDS). Background technique [0002] Acquired Immunodeficiency Syndrome (AIDS), referred to as AIDS, is an infectious disease caused by Human Immunodeficiency Virus (HIV), which is mainly transmitted through contact, mother-to-child transmission, and blood transmission. [0003] According to the 2015 World AIDS Day report, in 2014, about 36.9 million people worldwide were infected with HIV, about 2 million people were newly infected with HIV, and 1.2 million people died of AIDS opportunistic infections. As of June 2015, a total of 15.8 million people received treatment. At present, there are 575,000 surviving HIV-infected persons and patients in my country, and 177,000 people have died. Among them, about 15% of HIV-infected persons are you...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/5365A61K47/26A61K47/38A61K47/10A61K47/36A61K47/32A61P31/18
CPCA61K9/2806A61K9/2018A61K9/2027A61K9/2031A61K9/2054A61K9/2059A61K31/5365
Inventor 顾世海
Owner 顾世海
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