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Anti-cancer slow-release agent containing glucocorticoid hormone

A technology for corticosteroids and sustained-release agents, applied in the field of anti-cancer sustained-release agents, can solve problems such as treatment failure, accelerated drug release, edema, etc. Effect

Inactive Publication Date: 2007-08-29
JINAN KANGQUAN PHARMA TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above factors greatly limit the effective diffusion of drugs into solid tumors and tumors, thus constituting the main obstacle to tumor chemotherapy.
[0007] Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure
Local application of anticancer sustained-release agents often causes local edema, or accelerates drug release, which is not conducive to drug entry into solid tumors, effective diffusion and drug maintenance in tumors

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0138] Put 80mg of polylactic acid (PLGA, 50:50) with a peak molecular weight of 10000-25000 into the container, add 100ml of dichloromethane, dissolve and mix well, add 2mg of methylprednisolone and 18mg of gemcitabine, and shake again The organic solvent was removed by vacuum drying. The dried solid composition is immediately shaped, and then ray sterilized after being dispensed to obtain an anti-cancer sustained release containing 2% methylprednisolone and 18% gemcitabine. All are percentages by weight. The drug release time of the anti-solid tumor drug composition in vitro in physiological saline is 24-28 days, and the drug release time under the skin of mice is 25-40 days.

Embodiment 2

[0140] As described in Example 1, the difference is that the excipient is polylactic acid (PLGA, 75:25) with a peak molecular weight of 25000-45000, and the anti-cancer active ingredients and weight percentage are: 0.1-10% cortisone, strong Pine, prednisolone, methylprednisolone, clobetasone butyrate, hydrocortisone butyrate, dexamethasone, betamethasone, triamcinolone, triamcinolone acetonide, mometasone furoate, skin Relax, Flumethasone pivalate, Trimethasone valerate, Betamethasone dipropionate, Clofloxasone, Clobemethasone, Beclosone, Halometasone, Beclomethasone dipropionate, Budesonide Or fluticasone and 5-30% bleomycin, daunorubicin, nogamycin, puromycin, axorubicin, idarubicin, clarithromycin, adazo, doxorubicin, Combinations of epirubicin, valrubicin, pirarubicin, losanantrone, losoxantrone, mitoxantrone, piroxantrone, tiloxantrone, or lorzocin.

Embodiment 3

[0142] Put 70 parts of polystyrene propane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into the container, add appropriate amount of dichloromethane, dissolve and mix well and add 5 parts Dexamethasone and 25 parts of doxorubicin were shaken again and spray-dried to prepare injection microspheres containing 5% dexamethasone and 25% doxorubicin. Then the microspheres were suspended in physiological saline containing 15% mannitol to prepare the corresponding suspension type sustained-release injection with a viscosity of 20cp-300cp (at 20°C-30°C). The release time of the sustained-release injection in physiological saline in vitro is 30-45 days, and the release time under the skin of mice is about 40-45 days.

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Abstract

The present invention relates to an anti-cancer slow-release preparation containing glucocorticoid. It is a slow-release injection formed from slow-release microsphere and solvent. The slow-release microsphere includes anti-cancer effective component and slow-release auxiliary material, the solvent is a special solvent containing suspension adjuvant. The anti-cancer effective component is combination of glucocorticoid selected from cortisone, prednisone, clobetasone, dexamethasone, betamethasone, triamcinolone, triamcinolone acetonide, halometasone monohyudrate and fluocinonide, etc. and anti-cancer medicine selected from anti-tumor antibiotic and / or antimetabolite medicine. The slow-release auxiliary material is selected from bio-degradable absorbable high-molecular multimer and its polymer or mixture, and the viscosity of suspension adjuvant is 80 cp-3000 cp. Said anti-cance preparation also can be made into slow-release implantation preparation.

Description

(1) Technical field [0001] The invention relates to an anti-cancer slow-release agent containing glucocorticoid, which belongs to the technical field of medicine. Specifically, the present invention provides a sustained-release injection and a sustained-release implant containing glucocorticoid. The anti-cancer sustained-release agent can effectively reduce local edema, reduce the sudden release of the drug, and facilitate the effective diffusion of the drug into the solid tumor and the tumor. (2) Background technology [0002] Traditional chemotherapy is not selective, and it is difficult to form an effective drug concentration or therapeutic dose locally on the tumor. The effect is poor and the toxicity is high. Simply increasing the drug or radiation dose is limited by systemic toxicity. See Kong et al. "Intratumoral placement of cisplatin plus system carmustine in the treatment of rat brain tumors", Journal of Surgical Oncology, 69, pages 76-82, 1998 (Kong Q et al., J SurgOnc...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00A61K47/10A61K47/26A61K47/36A61K47/42
Inventor 孔庆忠刘玉燕张红军俞建江
Owner JINAN KANGQUAN PHARMA TECH