Medicinal preparation with inhibiting effect on tumor metastasis

Abstract

The invention relates to a medicinal preparation with inhibiting effect on tumor metastasis, which contains steroidal saponin extractives. The effective active components of the medicinal preparation comprise the following eight steroidal saponin general extractives which are eight steroid saponins: steroidal saponin I, steroidal saponin II, dioscin, gracillin, steroidal saponin H, steroidal saponin VII, saponin A (pennogenin-3-O-alpha-L-isodulcitol-yl(1-4)-[alpha-L-isodulcitol-yl(1-2)]-alpha-L-isodulcitol-yl(1-2)-beta-D-heteroside) and saponin B (pennogenin-3-O-alpha-L-isodulcitol-yl(1-4)-[alpha-L-isodulcitol-yl(1-2)]-alpha-L-isodulcitol-yl(1-3)-beta-D-heteroside), and the effective active components of the medicinal preparation also comprise medical dressings. The weight content of the eight steroidal saponin general extractives is 5%-30%, and the weight content of the medical dressings is 70%-95%. The invention is a medicinal preparation with less toxic and side effects and inhibiting effect on tumor metastasis.

Description

technical field

[0001] The invention belongs to the field of pharmacy, in particular to a pharmaceutical preparation with anti-tumor metastasis effect. Background technique

[0002] The Chinese Pharmacopoeia records P. polyphylla Smith var. yunnanensis and P. polyphylla Smith var. chinensis as the base plants of P. polyphylla. It has been reported in the literature that papaya saponins have good inhibitory effects on a variety of animal transplanted tumors S180, S37, EAC, ARS, and L759. However, there is no research report on the separation and purification of the effective part of papaya saponin and its antitumor effect. At present, most of the existing patents are for the research on the total saponins of Papilionaceae, including its preparation process, application in the treatment of gynecological diseases and research on its dosage forms. Our research group has also applied for patent 200810052092.2 to report on the preparation process and anti-tumor effect of its tot...

Examples

Embodiment 1

[0018] Preparation of the total extracts of eight kinds of papaya saponins

[0019] Reconstitute the total saponins (80mg / ml) of Pachyphylla saponins (80mg / ml) with methanol, and then separate them in the preparative liquid phase C18 column (YMC-Pack ODS-A, Japan). The mobile phase is chromatographic methanol with a flow rate of 3ml / min. Analyze, collect the 2nd, 3rd peak, obtain 8 kinds of total extracts (PM) of saponins of papaya saponins.

[0020] After intragastric administration of the above-mentioned total saponins extract (150 mg / kg) of Pachyphylla chinensis, blood was taken 2 hours, the serum was centrifuged at 3500 r / min for 15 minutes, the supernatant was taken, extracted with ethyl acetate, the upper layer was evaporated to dryness, redissolved in methanol, and the serum Scientific analysis:

[0021] LC-MS n The analysis found that papaya saponin I (diosgenin-3-O-α-L-arabinosyl (1→4)-[α-L-rhamnosyl (1→2 )]-β-D-glucoside), barley saponin II (diosgenin-3-O-α-L-rham...

Embodiment 2

[0038] Capsules: (by weight percentage)%

[0039] Total extracts of eight kinds of papaya saponins 10

[0040] cornstarch 61

[0041] Dextrin 10

[0042]Microcrystalline Cellulose 10

[0043] Calcium monohydrogen phosphate 3

[0044] Micronized silica gel 6

[0045] Add appropriate amount of 85% ethanol to the above auxiliary materials to make a soft material, pass through a 20-mesh sieve to granulate, dry at 40°C for 1 hour, pass through a 20-mesh sieve for granulation, pour the obtained granules into capsules, and make a finished product. Each capsule contains 30mg of papaya saponin.

Embodiment 3

[0047] Tablet (by weight percentage)%

[0048] Eight kinds of papaya saponins total extract 10

[0049] cornstarch 70

[0050] Dextrin 10

[0051] Sodium carboxymethyl starch 8

[0052] Magnesium Stearate 2

[0053] Mix the above excipients except magnesium stearate evenly, add appropriate amount of ethanol to moisten to make soft material, pass through a 20 mesh sieve to granulate, dry at 40°C for 1 hour, pass through a 20 mesh sieve for granulation, add stearic acid in equal amounts Magnesium, mixed evenly, and tableted to obtain the final product.

technical field

[0001] The invention belongs to the field of pharmacy, in particular to a pharmaceutical preparation with anti-tumor metastasis effect. Background technique

[0002] The Chinese Pharmacopoeia records P. polyphylla Smith var. yunnanensis and P. polyphylla Smith var. chinensis as the base plants of P. polyphylla. It has been reported in the literature that papaya saponins have good inhibitory effects on a variety of animal transplanted tumors S180, S37, EAC, ARS, and L759. However, there is no research report on the separation and purification of the effective part of papaya saponin and its antitumor effect. At present, most of the existing patents are for the research on the total saponins of Papilionaceae, including its preparation process, application in the treatment of gynecological diseases and research on its dosage forms. Our research group has also applied for patent 200810052092.2 to report on the preparation process and anti-tumor effect of its tot...

Examples

Embodiment 1

[0018] Preparation of the total extracts of eight kinds of papaya saponins

[0019] Reconstitute the total saponins (80mg / ml) of Pachyphylla saponins (80mg / ml) with methanol, and then separate them in the preparative liquid phase C18 column (YMC-Pack ODS-A, Japan). The mobile phase is chromatographic methanol with a flow rate of 3ml / min. Analyze, collect the 2nd, 3rd peak, obtain 8 kinds of total extracts (PM) of saponins of papaya saponins.

[0020] After intragastric administration of the above-mentioned total saponins extract (150 mg / kg) of Pachyphylla chinensis, blood was taken 2 hours, the serum was centrifuged at 3500 r / min for 15 minutes, the supernatant was taken, extracted with ethyl acetate, the upper layer was evaporated to dryness, redissolved in methanol, and the serum Scientific analysis:

[0021] LC-MS n The analysis found that papaya saponin I (diosgenin-3-O-α-L-arabinosyl (1→4)-[α-L-rhamnosyl (1→2 )]-β-D-glucoside), barley saponin II (diosgenin-3-O-α-L-rham...

Embodiment 2

[0038] Capsules: (by weight percentage)%

[0039] Total extracts of eight kinds of papaya saponins 10

[0040] cornstarch 61

[0041] Dextrin 10

[0042]Microcrystalline Cellulose 10

[0043] Calcium monohydrogen phosphate 3

[0044] Micronized silica gel 6

[0045] Add appropriate amount of 85% ethanol to the above auxiliary materials to make a soft material, pass through a 20-mesh sieve to granulate, dry at 40°C for 1 hour, pass through a 20-mesh sieve for granulation, pour the obtained granules into capsules, and make a finished product. Each capsule contains 30mg of papaya saponin.

Embodiment 3

[0047] Tablet (by weight percentage)%

[0048] Eight kinds of papaya saponins total extract 10

[0049] cornstarch 70

[0050] Dextrin 10

[0051] Sodium carboxymethyl starch 8

[0052] Magnesium Stearate 2

[0053] Mix the above excipients except magnesium stearate evenly, add appropriate amount of ethanol to moisten to make soft material, pass through a 20 mesh sieve to granulate, dry at 40°C for 1 hour, pass through a 20 mesh sieve for granulation, add stearic acid in equal amounts Magnesium, mixed evenly, and tableted to obtain the final product.

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