Olaparib pharmaceutical composition and preparation method thereof

Abstract

The invention discloses an olaparib pharmaceutical composition and a preparation method thereof, belongs to the field of pharmaceutical preparation, and particularly relates to the olaparib composition and the preparation method thereof. The composition comprises olaparib and a carrier. The olaparib composition provided by the invention has the advantages of safety, stability and excellent in-vitro dissolution effect.

Description

technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to an olaparib pharmaceutical composition and a preparation method thereof. Background technique

[0002] Olaparib is an oral poly(ADP-ribosyltransferase) (PARP) inhibitor. It mainly blocks the repair of DNA damage, causes the accumulation of DNA damage, and finally kills tumor cells; in addition, it can also increase the sensitivity of cells to other endogenous DNA damage factors; inhibit angiogenesis; enhance the immunity of normal cells, thereby Resist the invasion of cancer cells.

[0003] The therapeutic effect of olaparib on ovarian cancer has been highly recognized. EMEA and FDA successively granted orphan drug certification for olaparib for the treatment of ovarian cancer. Olaparib is currently undergoing clinical research in ovarian cancer, gastric cancer and non-small cell lung cancer with breast cancer susceptibility gene (BRCA) mutations. In the phase II ma...

Examples

Embodiment 1

[0049] Table 1: Prescription Composition of Olaparib Tablets

[0050]

[0051] After olaparib, povidone 12PF and talcum powder are mixed evenly according to the prescription ratio, they are added into a drug hot-melt extruder to prepare a solid dispersion, which is cooled and crushed into suitable granules. Then the above-mentioned granules are evenly mixed with mannitol and remaining talcum powder, and magnesium stearate is added for total mixing. Then the mixed granules are pressed into tablets, and the hardness of the tablets is controlled to be ≥6kg / cm 2 . The tablet core is coated, and the weight of the coating is increased by 3%, and finally the finished product of the olaparib tablet is obtained after being packaged in aluminum-plastic blisters.

Embodiment 2

[0053] Table 2: Prescription Composition of Olaparib Tablets

[0054]

[0055] Using the above-mentioned prescription process, the tablet core is coated, and the weight of the coating is increased by 2%, and finally the finished product of olaparib tablet is obtained after being packaged in aluminum-plastic blisters.

Embodiment 3

[0057] Table 3: Prescription Composition of Olaparib Tablets

[0058]

[0059] Using the above-mentioned prescription process, the tablet core is coated, and the weight of the coating is increased by 3%, and finally the finished product of the olaparib tablet is obtained after being packed in aluminum-plastic blisters.

technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to an olaparib pharmaceutical composition and a preparation method thereof. Background technique

[0002] Olaparib is an oral poly(ADP-ribosyltransferase) (PARP) inhibitor. It mainly blocks the repair of DNA damage, causes the accumulation of DNA damage, and finally kills tumor cells; in addition, it can also increase the sensitivity of cells to other endogenous DNA damage factors; inhibit angiogenesis; enhance the immunity of normal cells, thereby Resist the invasion of cancer cells.

[0003] The therapeutic effect of olaparib on ovarian cancer has been highly recognized. EMEA and FDA successively granted orphan drug certification for olaparib for the treatment of ovarian cancer. Olaparib is currently undergoing clinical research in ovarian cancer, gastric cancer and non-small cell lung cancer with breast cancer susceptibility gene (BRCA) mutations. In the phase II ma...

Examples

Embodiment 1

[0049] Table 1: Prescription Composition of Olaparib Tablets

[0050]

[0051] After olaparib, povidone 12PF and talcum powder are mixed evenly according to the prescription ratio, they are added into a drug hot-melt extruder to prepare a solid dispersion, which is cooled and crushed into suitable granules. Then the above-mentioned granules are evenly mixed with mannitol and remaining talcum powder, and magnesium stearate is added for total mixing. Then the mixed granules are pressed into tablets, and the hardness of the tablets is controlled to be ≥6kg / cm 2 . The tablet core is coated, and the weight of the coating is increased by 3%, and finally the finished product of the olaparib tablet is obtained after being packaged in aluminum-plastic blisters.

Embodiment 2

[0053] Table 2: Prescription Composition of Olaparib Tablets

[0054]

[0055] Using the above-mentioned prescription process, the tablet core is coated, and the weight of the coating is increased by 2%, and finally the finished product of olaparib tablet is obtained after being packaged in aluminum-plastic blisters.

Embodiment 3

[0057] Table 3: Prescription Composition of Olaparib Tablets

[0058]

[0059] Using the above-mentioned prescription process, the tablet core is coated, and the weight of the coating is increased by 3%, and finally the finished product of the olaparib tablet is obtained after being packed in aluminum-plastic blisters.

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