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A kind of antiretroviral pharmaceutical composition and preparation method thereof

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

Active Publication Date: 2022-08-09
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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  • A kind of antiretroviral pharmaceutical composition and preparation method thereof
  • A kind of antiretroviral pharmaceutical composition and preparation method thereof
  • A kind of 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 comprising a nucleoside reverse transcriptase inhibitor and an integrase inhibitor and one or more pharmaceutically acceptable excipients, wherein the The weight ratio of nucleoside reverse transcriptase inhibitor and integrase inhibitor is 4:1; the nucleoside reverse transcriptase inhibitor (NRTI) comprises lamivudine, abacavir, zidovudine One or more combinations of doxycycline, emtricitabine, didanosine, stavudine, entecavir, zalcitabine, dexelvucitabine, elvucitabine or pharmaceutically acceptable derivatives or mixtures thereof, the present application Preferably emtricitabine or a pharmaceutically acceptable derivative or a mixture thereof; the integrase inhibitor comprising dolutegravir, elvitegravir, raltegravir, bictegravir, cabotegravir or a pharmaceutically acceptable derivative or a mixture thereof One or more combinations, preferably dolutegravir or a pharmaceutically acceptable der...

Embodiment 2

[0049] Prescription: as shown in Table 1:

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

[0051]

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

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

[0054] (a1) 50 mg of mesoporous silica was ultrasonically treated at 25 °C for 30 min by ultrasonic vibration technology, and configured into a suspension with a mass concentration of 13%, directly using an air atmospheric plasma jet device at a power of 750 W and a height of 14.13 The suspension was treated under mm conditions for 4 min, then centrifuged at 2500 rpm for 13 min to obtain a precipitate, washed with absolute ethanol 4 times, 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 anhydrous ethanol, and perform ultrasonic treatment at intervals of 2 seconds at...

Embodiment 3

[0068] Prescription: as shown in Table 2

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

[0070]

[0071] A preparation method of an antiretroviral compound package chip is as follows:

[0072] (a) Preparation of the core part:

[0073] (a1) 50 mg of mesoporous silica was ultrasonically treated at 30 °C for 40 min by ultrasonic vibration technology, and configured into a suspension with a mass concentration of 15%, directly using an air atmospheric pressure plasma jet device at a power of 850 W and a height of 14.13 The suspension was treated under the condition of mm for 7 min, then centrifuged at 3000 rpm for 10 min to obtain the precipitate, washed with absolute ethanol for 5 times, and vacuum freeze-dried to obtain the modified mesoporous silica.

[0074] (a2) Dissolve the modified mesoporous silica obtained in step (a1) and 50 mg of dolutegravir in an appropriate amount of anhydrous ethanol, and perform ultrasonic treatment at interval...

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Abstract

The invention discloses an antiretroviral pharmaceutical composition, which comprises a nucleoside reverse transcriptase inhibitor and an integrase inhibitor and one or more pharmaceutically acceptable excipients, wherein the The weight ratio of the nucleoside reverse transcriptase inhibitor and the integrase inhibitor is 4:1. Also disclosed is a preparation method of the composition. In the preparation method, plasma-modified mesoporous silica is used as a carrier to prepare dolutegravir-modified mesoporous silica solid dispersion, and the dolutegravir is improved. The bioavailability of the tablet is improved; the tablet is designed to be chip-packed and the penetration hole is set on the tablet core, which improves the dissolution rate of the main drug dolutegravir in the tablet core, and makes the two main drugs dolutegravir and emtricitabine. The dissolution rate is synchronized, the synergistic effect of the two main drugs is increased, the stability of the tablet is improved, and the curative effect is enhanced. few.

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), namely acquired immunodeficiency syndrome, 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] There is still a lack of effective drugs to cure HIV infection worldwide. The current treatment goals: first, to turn AIDS from a terminal illness into a chronic disease. As long as the patient adheres to the drug and does not develop drug resistance, he can live a healthy life; the second is to reduce the HIV viral load in the patient to a very low level, It has become a "controllable and preventable chronic disease". [0004] Emtricitabine (FTC) is the lat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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