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Antiretroviral pharmaceutical composition and preparation method thereof

An anti-retrovirus and reverse transcriptase inhibition technology, which is applied in antiviral agents, pharmaceutical formulas, sugar-coated pills, etc., can solve the problems of small drug loading and easy aging, and achieve low content of related substances, good stability, The effect of improving wettability

Active Publication Date: 2020-11-27
ANHUI BIOCHEM BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, solid dispersions have disadvantages such as small drug loading and easy aging after long-term storage.

Method used

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  • Antiretroviral pharmaceutical composition and preparation method thereof
  • Antiretroviral pharmaceutical composition and preparation method thereof
  • Antiretroviral pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The present invention provides an antiretroviral pharmaceutical composition, which comprises nucleoside reverse transcriptase inhibitors and integrase inhibitors and one or more pharmaceutically acceptable excipients, wherein the The weight ratio of nucleoside reverse transcriptase inhibitor and integrase inhibitor is 4: 1; Described nucleoside reverse transcriptase inhibitor (NRTI), it comprises lamivudine, abacavir, Zidov One or more combinations of Ding, Emtricitabine, Didanosine, Stavudine, Entecavir, Zalcitabine, dexelvucitabine, elvucitabine or their pharmaceutically acceptable derivatives or their mixtures, this application Emtricitabine or a pharmaceutically acceptable derivative thereof or a mixture thereof is preferred; the integrase inhibitor comprising dolutegravir, elvitegravir, raltegravir, bictegravir, cabotegravir or a pharmaceutically acceptable derivative thereof or a mixture thereof One or more combinations, preferably dolutegravir or its pharmaceutic...

Embodiment 2

[0049] Prescription: as in Table 1:

[0050] Table 1 The formula of the compound package chip of the present invention

[0051]

[0052] A preparation method of an antiretroviral compound package chip is as follows:

[0053] (a) Preparation of tablet core part:

[0054] (a1) 50 mg of mesoporous silica was ultrasonically treated at 25°C for 30 minutes by ultrasonic oscillation technology, and prepared into a suspension with a mass concentration of 13%. The suspension was treated under mm conditions for 4 minutes, then centrifuged at 2500 rpm for 13 minutes to obtain a precipitate, washed 4 times with absolute ethanol, and vacuum freeze-dried to obtain modified mesoporous silica.

[0055] (a2) Dissolve the modified mesoporous silica obtained in step (a1) and 50 mg of dolutegravir in an appropriate amount of absolute ethanol, and perform ultrasonic treatment at intervals of 2 seconds at a frequency of 18KHz and a power of 350W, with an interval of 4 seconds , the total time...

Embodiment 3

[0068] Prescription: as shown in Table 2

[0069] Table 2 The formula of the compound package chip of the present invention

[0070]

[0071]

[0072] A preparation method of an antiretroviral compound package chip is as follows:

[0073] (a) Preparation of tablet core part:

[0074] (a1) 50 mg of mesoporous silica was ultrasonically treated at 30°C for 40 minutes by ultrasonic oscillation technology, and prepared into a suspension with a mass concentration of 15%, and directly used an air atmospheric pressure plasma jet device with a power of 850W and a height of 14.13 The suspension was treated under mm conditions for 7 min, and then centrifuged at 3000 rpm for 10 min to obtain a precipitate, washed 5 times with absolute ethanol, and vacuum freeze-dried to obtain modified mesoporous silica.

[0075] (a2) Dissolve the modified mesoporous silica obtained in step (a1) and 50 mg of dolutegravir in an appropriate amount of absolute ethanol, and perform ultrasonic treatmen...

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Abstract

The invention discloses an antiretroviral pharmaceutical composition. The pharmaceutical composition comprises a nucleoside reverse transcriptase inhibitor, an integrase inhibitor and one or more pharmaceutically acceptable excipients, wherein the weight ratio of the nucleoside reverse transcriptase inhibitor to the integrase inhibitor is 4: 1. The invention also discloses a preparation method ofthe composition. In the preparation method, plasma-modified mesoporous silica is used as a carrier to prepare a dolutegravir and modified mesoporous silica solid dispersion, so that the bioavailability of dolutegravir is improved; a tablet is designed into a coated tablet core, and permeation holes are formed in the tablet core, so that the dissolution rate of the main drug dolutegravir in the tablet core is increased, the dissolution rates of the two main drugs dolutegravir and emtricitabine are synchronous, the synergistic effect of the two main drugs is increased, the stability of the tablet is improved, and the curative effect is enhanced; and the prepared compound coated tablet core is high in bioavailability, good in dissolution effect of active ingredients, good in stability and lowin content of related substances.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an antiretroviral pharmaceutical composition and a preparation method thereof. Background technique [0002] AIDS (Acquired Immune Deficiency Syndrome, AIDS) is an infectious disease caused by human immunodeficiency virus (Human Immunodeficiency Virus, HIV) infection. HIV is a lentivirus that infects cells of the human immune system and is a type of retrovirus. [0003] Currently, there is still a lack of effective drugs to cure HIV infection worldwide. The goals of treatment at the present stage are: first, to turn AIDS from a terminal illness into a chronic disease, so that patients can live a healthy life as long as they persist in taking medication and do not develop drug resistance; second, to reduce the HIV viral load in patients to a very low level, Become a "controllable and preventable chronic disease". [0004] Emtricitabine (FTC) is a newest nucleoside rev...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/513A61K31/5365A61K9/28A61K47/04A61K47/38A61P31/18
CPCA61K45/06A61K31/513A61K31/5365A61K9/28A61K9/2054A61K9/2009A61P31/18
Inventor 陈小峰王哲王志邦朱礼根黄楠刘安友何麓璐夏玉明杜坤
Owner ANHUI BIOCHEM BIO PHARMA
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