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Palbociclib oral emulsion and preparation method thereof

A technology of emulsion and emulsifier, which is applied in the field of oral emulsion of palbociclib and its preparation, can solve the problems of high oral absorption and impact of palbociclib

Inactive Publication Date: 2018-06-29
SHENZHEN HUALIKANG BIOLOGICAL MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In addition, the results of clinical trials also found that food has a higher impact on the oral absorption of palbociclib

Method used

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  • Palbociclib oral emulsion and preparation method thereof
  • Palbociclib oral emulsion and preparation method thereof
  • Palbociclib oral emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] (1) Weigh 150 mg of tartaric acid and dissolve it in 20 mL of purified water, stir and dissolve completely to obtain a clear and transparent solution; (2) Weigh 125 mg of palbociclib free base and add it to the tartaric acid aqueous solution prepared in the previous step, and stir until completely dissolved; (3) Add 100 mg of sucralose, 5 mL of caprylic capric macrogolglyceride, 4.75 mL of polyethylene glycol 400 and 20 mg of sodium benzoate to the above solution, and stir to dissolve it completely; (4) Add 0.6g of corn oil, 20mg of butylated hydroxytoluene and 20mg of butylated hydroxyanisole were stirred by a high-speed stirrer at a speed of 1000rpm for 10min to obtain the product.

Embodiment 2

[0042] (1) Weigh 100mg of citric acid and 100mg of tartaric acid and dissolve them in 20mL of purified water, stir and dissolve completely to obtain a clear and transparent solution; (2) Weigh 125mg of palbociclib free base and add citric acid and tartaric acid prepared in the previous step Mix the aqueous solution and stir until it dissolves completely; (3) Add 100 mg of aspartame, 9 mL of caprylic capric macrogol glyceride, 2 mL of polyethylene glycol 400 and 20 mg of sodium benzoate to the above solution, and stir to make it completely dissolve; (4) Add 1.5 g of coconut oil and 40 mg of vitamin E to the above aqueous solution, and stir for 10 min at a speed of 1000 rpm with a high-speed stirrer to obtain the product.

Embodiment 3

[0044] (1) Weigh 100 mg of malic acid and dissolve it in 20 mL of purified water, stir and dissolve completely to obtain a clear and transparent solution; (2) Weigh 75 mg of palbociclib free base and add it into the malic acid aqueous solution prepared in the previous step, and stir until dissolved Completely; (3) Add 150 mg of sodium saccharin, 5 mL of polyoxyethylene castor oil, 4.75 mL of polyethylene glycol 400 and 10 mg of sodium benzoate to the above solution, and stir to dissolve it completely; (4) Add 0.1 g of oil to the above aqueous solution Acid and 40 mg of vitamin E were stirred for 10 minutes at a speed of 1000 rpm by a high-speed stirrer to obtain the product.

[0045] Table 1 and Table 2 below show the solubility of palbociclib in aqueous solutions of different pH and in different oils, respectively.

[0046] Table 1. Solubility of palbociclib free base in different buffer solvents

[0047]

[0048] Table 2. Solubility of 20mg palbociclib free base in diffe...

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Abstract

The invention belongs to the field of pharmaceuticals and particularly relates to a palbociclib oral emulsion and a preparation method of the palbociclib oral emulsion. The oral emulsion comprises thefollowing materials by mass: 0.1-1% of palbociclib free alkali or a pharmaceutical salt, 0.1-5% of a medicinal acid ingredient, 0.1-5% of a sweetening agent, 0.01-0.5% of an antioxidant, 0.1-10% of medicinal oil, and 1-10% of a medicinal emulsifier. Compared with the conventional preparation, the palbociclib oral emulsion has a better oral absorption property, and can be used to reduce the oral absorption difference of the palbociclib and improve the bioavailability.

Description

technical field [0001] The invention belongs to the field of pharmacy. More specifically, the present invention relates to an oral emulsion of palbociclib (also known as palbociclib, palbociclib, palbociclib, palbociclib, etc.) and a preparation method thereof. The palbociclib of the present invention may be palbociclib free base or any pharmaceutically acceptable salt thereof. Background technique [0002] Statistics from the World Health Organization show that breast cancer is the second leading cause of cancer death among women worldwide. The incidence of breast cancer has been increasing over the past few decades. It is estimated that by 2020, there will be more than 1.7 million new cases of breast cancer each year. In 2012, there were 1.67 million new cases of breast cancer worldwide, accounting for 25% of all new cancer cases. Among them, there are 883,000 cases in developed countries and 794,000 cases in developing countries. New breast cancer cases are growing a...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/12A61K31/519A61P35/00
CPCA61K9/0053A61K9/107A61K31/519A61K47/12
Inventor 王泽人徐俊陈顺
Owner SHENZHEN HUALIKANG BIOLOGICAL MEDICINE
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