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Vaginal ring containing non-nucleoside reverse transcriptase inhibitor and its preparation method

A technology of vaginal ring and beta-cyclodextrin, applied in the field of vaginal ring

Active Publication Date: 2020-04-10
SHANGHAI INST OF PLANNED PARENTHOOD RES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, no suitable carrier has been found to solve the above-mentioned problems in the prior art

Method used

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  • Vaginal ring containing non-nucleoside reverse transcriptase inhibitor and its preparation method
  • Vaginal ring containing non-nucleoside reverse transcriptase inhibitor and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] (1) Grinding and mixing 30 mg of "108-13" and 150 mg of hydroxypropyl beta-cyclodextrin with a Retsch-Rm200 mortar mill imported from Germany. Grinding in a mortar grinder for 20 minutes (grinding gap ≤ 0.3 mm), the drug molecule is completely embedded in the molecule of hydroxypropyl beta cyclodextrin to form a new inclusion body.

[0028] (2) Add 350 mg of sodium lauryl sulfate to the inclusion complex formed by the above-mentioned "108-13 and hydroxypropyl beta-cyclodextrin, continue to adopt the Retsch-Rm200 mortar grinder imported from Germany, in the mortar grinder Continue grinding for 20 minutes (grinding gap ≤ 0.3mm), combine the drug molecules and hydroxypropyl beta cyclodextrin in vitro and include a new layer of solubilizing substances.

[0029] (3) The molecular inclusion body formed by combining the above-mentioned drug, hydroxypropyl beta cyclodextrin, and sodium lauryl sulfate, and 2.2g of silicone rubber are mixed together to form a columnar body in the...

Embodiment 2

[0031] (1) Grind 40 mg of "108-13" and 80 mg of hydroxypropyl beta-cyclodextrin in a mortar grinder imported from Germany for 20 minutes (grinding gap ≤ 0.3 mm), A new inclusion complex is formed by fully embedding the drug molecule in the molecule of hydroxypropyl beta cyclodextrin.

[0032] (2) Add 200 mg of sodium lauryl sulfate to the inclusion complex formed by the above-mentioned "108-13 and hydroxypropyl beta-cyclodextrin, continue to adopt the Retsch-Rm200 mortar grinder imported from Germany, in the mortar grinder Continue grinding for 20 minutes (grinding gap ≤ 0.3mm), combine the drug molecules and hydroxypropyl beta cyclodextrin in vitro and include a new layer of solubilizing substances.

[0033] (3) The molecular inclusion body formed by combining the above-mentioned drug, hydroxypropyl beta cyclodextrin, and sodium lauryl sulfate, and 2.4g of silicone rubber are mixed together to form a columnar body in the extruder , embedded in the mold for hot press vulcaniz...

Embodiment 3

[0035] (1) Grinding and mixing 35 mg of "108-13" and 200 mg of hydroxypropyl beta-cyclodextrin with a Retsch-Rm200 mortar mill imported from Germany. Grinding in a mortar grinder for 20 minutes (grinding gap ≤ 0.3 mm), the drug molecule is completely embedded in the molecule of hydroxypropyl beta cyclodextrin to form a new inclusion body.

[0036] (2) Add 250 mg sodium lauryl sulfate to the inclusion complex formed by the above-mentioned "108-13 and hydroxypropyl beta cyclodextrin, continue to adopt the Retsch-Rm200 mortar grinder imported from Germany, Continue grinding for 20 minutes (grinding gap ≤ 0.3mm), combine the drug molecules and hydroxypropyl beta cyclodextrin in vitro and include a new layer of solubilizing substances.

[0037] (3) The molecular inclusion body formed by combining the above-mentioned drug, hydroxypropyl beta cyclodextrin, and sodium lauryl sulfate, and 2.3g of silicone rubber are mixed together to form a columnar body in the extruder , embedded in ...

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Abstract

The invention relates to a pessulum containing a non-nucleoside reverse transcriptase inhibitor and a preparation method of the pessulum. The pessulum comprises N1-(4'-cyanophenyl)-5-(4''-propylene cyano-2'',6''-dimethyl phenol)-4-(N-methyl formamido)-1,2-phenylenediamine, hydroxypropyl betadex and lauryl sodium sulfate. The weight ratio of silicone rubber to N1-(4'-cyanophenyl)-5-(4''-propylene cyano-2'',6''-dimethyl phenol)-4-(N-methyl formamido)-1,2-phenylenediamine to hydroxypropyl betadex to lauryl sodium sulfate is (30-80):(1-5):(3-8):(8-15). The pessulum can precisely release the non-nucleoside reverse transcriptase inhibitor in a controlled mode, and the purpose of efficiently, easily and conveniently treating Aids is achieved.

Description

technical field [0001] The invention relates to a vaginal ring, in particular, the invention relates to a vaginal ring capable of increasing the release of non-nucleoside reverse transcriptase inhibitors and a preparation method thereof. Background technique [0002] Reverse transcriptase is a selective target involved in AIDS drug research, and reverse transcriptase inhibitors are mainly divided into two categories: nucleoside (NRTIs) and non-nucleoside (NNRTIs). [0003] Nucleoside reverse transcriptase inhibitors are the first class of drugs that came out and developed more varieties. They have been clinically proven to have a strong inhibitory effect on HIV replication. Nucleoside reverse transcriptase inhibitors (NRTIs) are the synthesis of HIV The analogue of DNA reverse transcriptase substrate deoxynucleotide, which is converted into active nucleoside triphosphate derivatives in vivo, competes with natural deoxynucleoside triphosphate to bind to HIV reverse transcript...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/61A61K9/00A61K31/277A61P31/18
Inventor 邵海浩姜世勃李元春陆路谢蓝陈旭锋
Owner SHANGHAI INST OF PLANNED PARENTHOOD RES
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