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Artemether oral micro-emulsion in-situ gel and preparation method thereof

A technology of in-situ gel and artemether, applied in the field of medicine, can solve the problems of unsatisfactory treatment effect of gastric cancer, inability to achieve gastric retention, etc., and achieve the effects of improving bioavailability, prolonging residence time, and good fluidity

Active Publication Date: 2018-09-28
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug delivery system exists in the form of liquid emulsion droplets, which cannot be retained in the stomach, and its therapeutic effect on gastric cancer is not satisfactory

Method used

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  • Artemether oral micro-emulsion in-situ gel and preparation method thereof
  • Artemether oral micro-emulsion in-situ gel and preparation method thereof
  • Artemether oral micro-emulsion in-situ gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1, preparation artemether oral microemulsion in situ gel

[0051] The composition of the prescription is as follows:

[0052]

[0053] The preparation method is as follows:

[0054] (1) Weigh 0.5 g of artemether and 4.5 g of glyceryl triacetate, and dissolve the drug in the oil phase by means of stirring, vortexing, ultrasonication, etc., to obtain the drug-loaded oil phase;

[0055] (2) Take by weighing polyoxyethylene castor oil 4.0g, dehydrated alcohol 2.0g, the two are mixed, get mixed surfactant;

[0056] (3) Weigh 0.26g of gellan gum, add it into 88.65g of water under magnetic stirring to make it completely dispersed, heat to 90°C to dissolve, and add 0.09g of low-viscosity sodium alginate under stirring state, after swelling is complete as an aqueous solution;

[0057] (4) Add drug-loaded oil phase, mixed surfactant, and aqueous phase solution in sequence in a beaker, and stir evenly at room temperature until a transparent and clear solution is o...

Embodiment 2

[0058] Embodiment 2, preparation artemether oral microemulsion in situ gel

[0059] The composition of the prescription is as follows:

[0060]

[0061] The preparation method is as follows:

[0062] (1) Weigh 0.5 g of artemether and 4.5 g of glyceryl triacetate, and dissolve the drug in the oil phase by means of stirring, vortexing, ultrasonication, etc., to obtain the drug-loaded oil phase;

[0063] (2) Take polyoxyethylene castor oil 7.5g, diethylene glycol monoethyl ether 7.5g, mix the two to obtain a mixed surfactant;

[0064] (3) Weigh 0.24g of gellan gum, add it into 79.68g of water under magnetic stirring to make it completely dispersed, heat to 90°C to dissolve, and add 0.08g of low-viscosity sodium alginate under stirring state, after swelling is complete as an aqueous solution;

[0065] (4) Add drug-loaded oil phase, mixed surfactant, and aqueous phase solution in sequence in a beaker, and stir evenly at room temperature until a transparent and clear solution ...

Embodiment 3

[0066] Embodiment 3, preparation artemether oral microemulsion in situ gel

[0067] The composition of the prescription is as follows:

[0068]

[0069] The preparation method is as follows:

[0070] (1) Weigh 0.5 g of artemether and 4.5 g of glyceryl triacetate, and dissolve the drug in the oil phase by means of stirring, vortexing, ultrasonication, etc., to obtain the drug-loaded oil phase;

[0071] (2) Take by weighing polyoxyethylene castor oil 5g, diethylene glycol monoethyl ether 5g, the two are mixed, and mixed surfactant is obtained;

[0072] (3) Weigh 0.26g of gellan gum, add it into 84.65g of water under magnetic stirring to make it completely dispersed, heat to 90°C to dissolve, and add 0.09g of low-viscosity sodium alginate under stirring state, after swelling is complete as an aqueous solution;

[0073] (4) Add drug-loaded oil phase, mixed surfactant, and aqueous phase solution in sequence in a beaker, and stir evenly at room temperature until a transparent ...

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Abstract

The invention belongs to the technical field of medicines and particularly relates to an artemether oral micro-emulsion in-situ gel and a preparation method thereof. The artemether oral micro-emulsionin-situ gel is prepared from the following components of 0.1-0.8% of artemether, 0.9-7.2% of oil phases, 0.4-12% of surfactants, 0.4-12% of cosurfactants, 0.23-0.3% of in-situ gel substrates, 0-0.1%of adhesives and the balance water. The average particle size of emulsion drops of the artemether oral micro-emulsion in-situ gel is 20.90 nm, the emulsion drops are uniform in size, the solubility and releasing rate of the artemether can be increased, and the artemether oral micro-emulsion in-situ gel is stable at the room temperature; the artemether oral micro-emulsion in-situ gel is low in viscosity and good in flowability, the gel is formed immediately in a stomach after oral administration, the detention time of the artemether in the stomach can be prolonged, treatment of a stomach cancerand improving of the bioavailability of the artemether are facilitated; and the preparation technique is easy, operation and filling are easy, and industrial production is facilitated.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an artemether oral microemulsion in-situ gel and a preparation method thereof. Background technique [0002] Artemether is a methyl ether derivative of artemisinin, which is currently mainly used clinically for the treatment of malaria. In recent years, a large number of studies have proved that in addition to antimalarial effects, artemether also has pharmacological effects such as anti-schistosomiasis, anti-inflammation, anti-sepsis, anti-tissue fibrosis, radiosensitization, and anti-tumor. Artemether has a wide range of pharmacological effects, among which, the anti-tumor effect has been paid more and more attention, and more and more related researches have been carried out. As an anti-tumor drug, artemether has gradually been recognized by scholars at home and abroad. Among them, studies have reported that artemether has a certain killing and inhibitory effect ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/00A61K9/107A61K31/357A61K47/44A61P35/00
CPCA61K9/0053A61K9/06A61K9/1075A61K31/357A61K47/44A61P35/00
Inventor 蔡铮薛鸿娇郭坤坤杨兆祥
Owner KPC PHARM INC
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