Claims
- 1. A pharmaceutical preparation comprising at least one L-ascorbic acid derivative and at least one antimalignant tumor agent, wherein said L-ascorbic acid derivative provides, on culturing zooblast for 20 hours in a culture medium containing the L-ascorbic acid derivative in a concentration of 5 μM, an L-ascorbic acid intracellular cumulative amount equal to or greater than that obtained by culturing the zooblast in a culture medium containing magnesium L-ascorbic acid-2-phosphate in a concentration of 50 μM.
- 2. The pharmaceutical preparation according to claim 1 for the medical treatment of cancer.
- 3. A pharmaceutical preparation comprising at least one L-ascorbic acid derivative and at least one antimalignant tumor agent, wherein said L-ascorbic acid derivative is represented by the following formula (1) and pharmaceutically acceptable salts thereof:
- 4. The pharmaceutical preparation according to claim 3, wherein in formula (1), R1 is one of a phosphoryloxy group, a pyrophosphoryloxy group, a triphosphoryloxy group, a polyphosphoryloxy group, a sulfoxy group and a glycosyloxy group, R2 is one of a hydroxyl group, a phosphoryloxy group, a polyphosphoryloxy group, a sulfoxy group, a glycosyloxy group, an alkoxy group, an alkenyloxy group and a phenoxy group, and at least one of R3 and R4 is an acyloxy group, an alkoxy group, an alkenyloxy group or a phenoxy group.
- 5. The pharmaceutical preparation according to claim 3, wherein in formula (1), R1 is a phosphoryloxy group, and R4 is an acyloxy group having from 10 to 22 carbon atoms.
- 6. The pharmaceutical preparation according to claim 3, wherein the h ydrophobic group is selected from the group consisting of acyloxy groups of lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linoleic acid, linolenic acid and arachidonic acid.
- 7. The pharmaceutical preparation according to claim 3, wherein the L-ascorbic acid derivative comprises an L-ascorbic acid-2-phosphate-6-higher fatty acid ester and pharmaceutically acceptable salts thereof, and said higher fatty acid ester is selected from the group consisting of fatty acid esters of lauric acid, palmitic acid, stearic acid and arachidonic acid.
- 8. The pharmaceutical preparation according to claim 3, wherein the L-ascorbic acid derivative is selected from the group consisting of L-ascorbic acid-2-pyrophosphate esters and pharmaceutically acceptable salts thereof, L-ascorbic acid-2-triphosphate esters and pharmaceutically acceptable salts thereof and L-ascorbic acid-2-polyphosphate esters and pharmaceutically acceptable salts thereof.
- 9. The pharmaceutical preparation according to claim 3, wherein the L-ascorbic acid derivative is selected from the group consisting of sodium L-ascorbic acid-2-phosphate-6-palmitate, L-ascorbic acid-2-phosphate-6-palmitate, L-ascorbic acid-2-phosphate-6-stearate, L-ascorbic acid-2-phosphate-6-oleate and L-ascorbic acid-2-phosphate-6-arachidonate.
- 10. The pharmaceutical preparation according to claim 3, wherein said antimalignant tumor agent is selected from the group consisting of Nitromin (R), cyclophosphamide, merphalan, TIOTEBA, CARBOCON, Protecton (R), bulsfan, nimustine hydrochloride, MITOPURNITOL, ifosfamide, meercaptopurine, thioinosine, cytarabine, decarbazine, fluorouracil, tegaful, ANCITABINE hydrochloride, methotrexate, carmofur, UFT (R), enocitabine, vinblastine sulfate, vincristine sulfate, vindesine sulfate, actinomycin (D), mitomycin C, chromomycin A3, pleomycin hydrochloride, PLEOMYCIN sulfate, daunorubicin hydrochloride, doxorubicin hydrochloride, neocarzinostatin, vebromycin sulfate, aclarubicin hydrochloride, mebitiostan, epitiostanol, tamoxifen citrate, HONPAN, VICIPANIL (R), krestin, lentinan, L-asparginase, aceglatone, procarbazine hydrochloride, floxuridine, MDS KOWA 3000 (R), Estracyt (R), CIZOFERAN, ADRIAMYCIN, mitomycin, cisplatin, CARBOPLATIN, vindesine, vincristine, cyclophosphamido, IFOMAMIDE, pleomycin, pepleomycin, etoposide and Furtulon.
- 11. A method of inhibiting cancer metastasis which comprises administering to a person in need of such treatment a dosage effective amount of at least one L-ascorbic acid derivative which provides, on culturing zooblast for 20 hours in a culture medium containing the L-ascorbic acid derivative in a concentration of 5 μM, an L-ascorbic acid intracellular cumulative amount equal to or greater than that obtained by culturing the zooblast in a culture medium containing magnesium L-ascorbic acid-2-phosphate in a concentration of 50 μM.
- 12. A method of inhibiting cancer metastasis which comprises administering to a person in need of such treatment a dosage effective amount of at least one L-ascorbic acid derivative represented by the following formula (1) and pharmaceutically acceptable salts thereof:
- 13. The method according to claim 12, wherein in formula (1), R1 is one of a phosphoryloxy group, a pyrophosphoryloxy group, a triphosphoryloxy group, a polyphosphoryloxy group, a sulfoxy group and a glycosyloxy group, R2 is one of a hydroxyl group, a phosphoryloxy group, a polyphosphoryloxy group, a sulfoxy group, a glycosyloxy group, an alkoxy group, an alkenyloxy group and a phenoxy group, and at least one of R3 and R4 is an acyloxy group, an alkoxy group, an alkenyloxy group or a phenoxy group.
- 14. The method according to claim 12, wherein in formula (1), R1 is a phosphoryloxy group, and R4 is an acyloxy group having from 10 to 22 carbon atoms.
- 15. A method of treating cancer which comprises administering to a person in need of such treatment a dosage effective amount of the pharmaceutical preparation according to claim 1.
- 16. A method of treating cancer which comprises administering to a person in need of such treatment a dosage effective amount of the pharmaceutical preparation according to claim 3.
- 17. The method according to claim 16, wherein in formula (1), R1 is one of a phosphoryloxy group, a pyrophosphoryloxy group, a triphosphoryloxy group, a polyphosphoryloxy group, a sulfoxy group and a glycosyloxy group, R is one of a hydroxyl group, a phosphoryloxy group, a polyphosphoryloxy group, a sulfoxy group, a glycosyloxy group, an alkoxy group, an alkenyloxy group and a phenoxy group, and at least one of R3 and R4 is an acyloxy group, an alkoxy group, an alkenyloxy group or a phenoxy group.
- 18. The method according to claim 16, wherein in formula (1), R1 is a phosphoryl group, and R4 is an acyloxy group having from 10 to 22 carbon atoms.
- 19. The method according to claim 16, wherein said antimalignant tumor agent is selected from the group consisting of Nitromin (R), cyclophosphamide, merphalan, TIOTEBA, CARBOCON, Protecton (R), bulsfan, nimustine hydrochloride, MITOPURNITOL, ifosfamide, meercaptopurine, thioinosine, cytarabine, decarbazine, fluorouracil, tegaful, ANCITABINE hydrochloride, methotrexate, carmofur, UFT (R), enocitabine, vinblastine sulfate, vincristine sulfate, vindesine sulfate, actinomycin (D), mitomycin C, chromomycin A3, pleomycin hydrochloride, PLEOMYCIN sulfate, daunorubicin hydrochloride, doxorubicin hydrochloride, neocarzinostatin, vebromycin sulfate, aclarubicin hydrochloride, mebitiostan, epitiostanol, tamoxifen citrate, HONPAN, VICIPANIL (R), krestin, lentinan, L-asparginase, aceglatone, procarbazine hydrochloride, floxuridine, MDS KOWA 3000 (R), Estracyt (R), CIZOFERAN, ADRIAMYCIN, mitomycin, cisplatin, CARBOPLATIN, vindesine, vincristine, cyclophosphamido, IFOMAMIDE, pleomycin, pepleomycin, etoposide and Furtulon.
Priority Claims (1)
Number |
Date |
Country |
Kind |
HEI. 9-102785 |
Apr 1997 |
JP |
|
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application is an application filed under 35 U.S.C. §111(a) claiming benefit pursuant to 35 U.S.C. §119(e) (1) of the filing date of the U.S. Provisional Application No. 60/075,483 filed Feb. 23, 1998 pursuant to 35 U.S.C. §111(b).
Provisional Applications (1)
|
Number |
Date |
Country |
|
60075483 |
Feb 1998 |
US |