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Medicinal composition containing amorphous palbociclib solid dispersion, and preparation method thereof

A solid dispersion, Palbociclin technology, applied in the field of treating cancer, pharmaceutical compositions containing amorphous Palbociclin solid dispersion and its preparation field, can solve the problem of affecting drug bioavailability, low absorption of original drugs, and patient Health hazards and other issues, to achieve the effect of improving bioavailability, good dispersion and amorphous state, and low price

Inactive Publication Date: 2017-12-26
SHANGHAI FANGNAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the drug is a poorly soluble drug, and its extremely low water solubility seriously affects the bioavailability of the drug
In addition, the drug efficacy varies greatly among patients. 13% of patients have extremely low absorption of the original research drug. Taking it after meals can slightly increase the absorption of the drug. Eating low-fat food equivalent to 3 grams of peanut oil can increase the absorption by 12%, while Eating high-fat food equivalent to 67 grams of peanut oil can increase absorption by 21%, but high-fat food also has considerable harm to the health of patients

Method used

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  • Medicinal composition containing amorphous palbociclib solid dispersion, and preparation method thereof
  • Medicinal composition containing amorphous palbociclib solid dispersion, and preparation method thereof
  • Medicinal composition containing amorphous palbociclib solid dispersion, and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Any physical form of palbocillin can be used to prepare the solid dispersion of amorphous palbocillin.

[0048] Dissolve palbocicillin (50 mg) and povidone K30 (100 mg) in n-butanol (600 μl), anisole (900 μl) and methanol (600 μl), heat to 60 °C and stir Dissolved, then added microcrystalline cellulose (50 mg). The above solution was rapidly cooled to -10°C, a yellow solid was precipitated, filtered, and vacuum-dried to obtain a composition of amorphous palbocicillin solid dispersion and microcrystalline cellulose, and the X-ray powder diffraction pattern of the composition deducted the carrier There is no characteristic peak of palbocillin crystal form after the background peak of pharmaceutical excipients.

Embodiment 2

[0050] Dissolve palbocillin (50 mg) and polyethylene glycol 4000 (200 mg) in ethanol (600 microliters) and water (600 microliters), stir and mix well at -40 °C, then add microcrystalline cellulose (50 mg). The above solution was slowly concentrated to dryness in a rotary evaporator to obtain a yellow solid, that is, the composition of amorphous palbocicillin and microcrystalline cellulose. In the X-ray powder diffraction pattern of the composition, the carrier and pharmaceutical excipients were deducted. There is no characteristic peak of palbocillin crystal form after the background peak.

Embodiment 3

[0052] Add palbocillin (5 g) and polyethylene glycol 8000 (10 g) into methanol (300 ml), heat to 60° C. and stir to dissolve, then add croscarmellose sodium (0.1 g). Dry the above solution with JISL micro spray dryer LSD-48, maintain the inlet temperature at 60°C and the outlet temperature at 50°C, collect the outlet material to obtain a yellow solid, and further vacuum dry to obtain amorphous palbocillin solid dispersion and cross-linked carboxymethyl Based on the composition of sodium cellulose, in the X-ray powder diffraction pattern of the composition, there is no characteristic peak of the palbocillin crystal form after deducting the background peaks of the carrier and the pharmaceutical excipient.

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Abstract

The invention relates to a medicinal composition containing an amorphous palbociclib solid dispersion. The medicinal composition contains a solid dispersion formed by palbociclib and an organic carrier, and at least one pharmaceutically acceptable auxiliary material, the palbociclib accounts for 20-80% of the total weight of the solid dispersion, and the auxiliary material accounts for 0.1-80% of the weight of the solid dispersion, wherein the palbociclib is an amorphous form, the background peaks of the organic carrier and the pharmaceutically acceptable auxiliary material exist in the X-ray powder diffracted spectrum of the composition, and the characteristic peak of palbociclib crystals does not exist in the spectrum. The invention also relates to a preparation method of the medicinal composition of amorphous palbociclib. The medicinal composition of the palbociclib has good stability and dispersibility, increases the dissolvability of the palbociclib, is in favor of improving the bioavailability of a medicinal preparation and the medicine absorption of bodies, and keeps good physical stability and chemical stability under accelerated test conditions. The preparation method of the amorphous composition has the advantages of simplicity in operation, low cost, good reappearance, easiness in realization, and suitableness for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical composition containing amorphous palbocicillin solid dispersion, a preparation method thereof, and an application of the composition for treating cancer. Background technique [0002] Palbociclib, the chemical name is 6-acetyl-8-cyclopentyl-5-methyl-2-[5-(1-piperazinyl)pyridin-2-ylamino]-8H-pyrido [2,3-d]pyrimidin-7-one, trade name Ibrance, is an oral new drug developed by Pfizer for the treatment of metastatic breast cancer, palbocillin is an inhibitor of cyclin-dependent kinase 4, 6 Drugs mainly prevent cells from G1 phase to S phase by inhibiting CDK4 / 6 activity, thereby inhibiting DNA synthesis. Clinical trial studies have found that palbocillin combined with letrozole is very effective for postmenopausal patients with locally invasive breast cancer or newly diagnosed estrogen receptor (ER) positive, HER-2 negative patients. Palbocilli...

Claims

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Application Information

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IPC IPC(8): A61K47/32A61K31/519A61K47/10A61K47/38A61K47/36A61K47/42A61K47/22A61P35/00A61P35/02
CPCA61K31/519A61K47/10A61K47/22A61K47/32A61K47/36A61K47/38A61K47/42
Inventor 张席妮熊志刚周涛胡涛
Owner SHANGHAI FANGNAN PHARMA
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