Tumor inhibiting medicine composition and purpose thereof

Abstract

The invention discloses a solid tumor inhibiting medicine composition composed of arctigenin and a pyrimidine nucleotide synthetic inhibitor, wherein a weight ratio of the components is 1:0.001-1000, and preferably 1:0.01-100. Pharmacodynamic tests show that, the medicine composition provides substantial synergetic effects in the treatments of solid tumors, especially leukemia. The medicine composition provided by the invention has advantages of wide tumor inhibiting spectrum, small side effect, low treatment cost, and good prospect in clinical application.

Description

technical field

[0001] The invention relates to an anti-tumor pharmaceutical composition and its use, in particular to a composition containing arctigenin and pyrimidine nucleotide synthesis inhibitors and its use against solid tumors, belonging to the technical field of medicines. Background technique

[0002] Tumor cells grow faster than most normal cells and need to synthesize more nucleotides as precursors for DNA and RNA synthesis, so they are more sensitive to nucleotide synthesis inhibitors than normal cells. A range of chemotherapeutic agents work by inhibiting one or more enzymes of the nucleotide synthesis pathway.

[0003] Nucleotide is the basic unit of ribonucleic acid and deoxyribonucleic acid, and is the precursor of nucleic acid synthesis in vivo. Nucleotides are distributed along with nucleic acids in the nucleus and cytoplasm of various organs, tissues, and cells in organisms, and as components of nucleic acids, they participate in basic life activities su...

Examples

Embodiment 1

[0062] The preparation of embodiment 1 arctigenin and capecitabine tablet

[0063] The tablet formulation of table 7 arctigenin and capecitabine composition

[0064]

[0065] Preparation process: Pass arctigenin and capecitabine through 80-mesh sieve respectively, weigh according to the prescription amount, mix evenly, then mix evenly with hydroxypropyl cyclodextrin in equal increments, pass through 60-mesh sieve, and then mix with Mix the rest of the excipients in the prescribed amount evenly, measure the content of the semi-finished product, calculate the weight of the tablet, and press the tablet.

Embodiment 2

[0066] Embodiment 2 Preparation of Arctigenin Gemcitabine Sustained Release Tablets

[0067] Table 8 Sustained-release tablet formulations of arctigenin and gemcitabine compositions

[0068]

[0069] Preparation process: Weigh arctigenin, gemcitabine, carbomer, and hydroxypropyl cellulose in prescription quantities and mix evenly. Take another appropriate amount of 8% starch slurry solution, add it to the mixed powder, mix evenly to make a soft material, pass through a 16-mesh sieve to granulate, and dry below 60°C. After the drying is completed, use an 18-mesh sieve to carry out granulation, sieve out the fine powder in the dry granules, mix with the sieved magnesium stearate, and then mix with the dry granules evenly, and press into tablets to obtain the product.

Embodiment 3

[0070] Embodiment 3 Preparation of arctigenin and tegafur microemulsion composition preparation

[0071] Table 9 arctigenin and tegafur microemulsion composition preparation 1

[0072]

[0073] Preparation process: Weigh 30 mg caprylic acid glyceride and 50 mg emulsifier OP, add to 20 mg propylene glycol, and mix well to obtain a suspension solution. Accurately weigh 25 mg of arctigenin and 0.25 mg of tegafur, add them to the suspension solution, and ultrasonically dissolve the arctigenin and tegafur to obtain the microemulsion concentrate of the arctigenin and tegafur composition. The microemulsion concentrate obtained above is diluted with water according to the weight ratio of 1:10-20 to a clear solution to obtain the microemulsion.

technical field

[0001] The invention relates to an anti-tumor pharmaceutical composition and its use, in particular to a composition containing arctigenin and pyrimidine nucleotide synthesis inhibitors and its use against solid tumors, belonging to the technical field of medicines. Background technique

[0002] Tumor cells grow faster than most normal cells and need to synthesize more nucleotides as precursors for DNA and RNA synthesis, so they are more sensitive to nucleotide synthesis inhibitors than normal cells. A range of chemotherapeutic agents work by inhibiting one or more enzymes of the nucleotide synthesis pathway.

[0003] Nucleotide is the basic unit of ribonucleic acid and deoxyribonucleic acid, and is the precursor of nucleic acid synthesis in vivo. Nucleotides are distributed along with nucleic acids in the nucleus and cytoplasm of various organs, tissues, and cells in organisms, and as components of nucleic acids, they participate in basic life activities su...

Examples

Embodiment 1

[0062] The preparation of embodiment 1 arctigenin and capecitabine tablet

[0063] The tablet formulation of table 7 arctigenin and capecitabine composition

[0064]

[0065] Preparation process: Pass arctigenin and capecitabine through 80-mesh sieve respectively, weigh according to the prescription amount, mix evenly, then mix evenly with hydroxypropyl cyclodextrin in equal increments, pass through 60-mesh sieve, and then mix with Mix the rest of the excipients in the prescribed amount evenly, measure the content of the semi-finished product, calculate the weight of the tablet, and press the tablet.

Embodiment 2

[0066] Embodiment 2 Preparation of Arctigenin Gemcitabine Sustained Release Tablets

[0067] Table 8 Sustained-release tablet formulations of arctigenin and gemcitabine compositions

[0068]

[0069] Preparation process: Weigh arctigenin, gemcitabine, carbomer, and hydroxypropyl cellulose in prescription quantities and mix evenly. Take another appropriate amount of 8% starch slurry solution, add it to the mixed powder, mix evenly to make a soft material, pass through a 16-mesh sieve to granulate, and dry below 60°C. After the drying is completed, use an 18-mesh sieve to carry out granulation, sieve out the fine powder in the dry granules, mix with the sieved magnesium stearate, and then mix with the dry granules evenly, and press into tablets to obtain the product.

Embodiment 3

[0070] Embodiment 3 Preparation of arctigenin and tegafur microemulsion composition preparation

[0071] Table 9 arctigenin and tegafur microemulsion composition preparation 1

[0072]

[0073] Preparation process: Weigh 30 mg caprylic acid glyceride and 50 mg emulsifier OP, add to 20 mg propylene glycol, and mix well to obtain a suspension solution. Accurately weigh 25 mg of arctigenin and 0.25 mg of tegafur, add them to the suspension solution, and ultrasonically dissolve the arctigenin and tegafur to obtain the microemulsion concentrate of the arctigenin and tegafur composition. The microemulsion concentrate obtained above is diluted with water according to the weight ratio of 1:10-20 to a clear solution to obtain the microemulsion.

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