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Solid preparation of palbociclib isethionate and preparation method thereof

A technology of piperidine isethionate and piperidine isethionate, applied in the field of pharmaceutical preparations, can solve the problems of poor solubility, large hygroscopicity and the like

Pending Publication Date: 2021-12-07
JIANGSU FOOD & PHARMA SCI COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of this, the application provides a solid preparation of palbociclib isethionate and a preparation method thereof. The present invention provides a tablet of palbociclib isethionate and a preparation process thereof. The optimized product of the present invention uses hydroxy Palbociclib ethanesulfonate is used as the raw material drug, and the dosage form is improved into palbociclib isethionate tablets, which can solve the problems of poor solubility and large hygroscopicity, and meet the quality and stability requirements, and can be popularized in production

Method used

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  • Solid preparation of palbociclib isethionate and preparation method thereof
  • Solid preparation of palbociclib isethionate and preparation method thereof
  • Solid preparation of palbociclib isethionate and preparation method thereof

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Effect test

Embodiment 1

[0044] In order to investigate the ratio of filler microcrystalline cellulin to lactose, the following three formulations were prepared, and pH4.5 acetate buffer was selected as the medium for formulation screening, and the investigation index was the dissolution rate in 15 minutes in the pH4.5 medium (dissolution assay is carried out to tablet according to Pharmacopoeia), see table 2 below for details.

[0045] Table 2 The composition of prescriptions with different filler ratios

[0046]

[0047]

[0048] The results of filler ratio investigation are as follows:

[0049] From figure 1 The dissolution data is available, and the change in the ratio of the filler microcrystalline cellulose to lactose has no obvious effect on the dissolution. According to experience, the dosage of microcrystalline cellulose: lactose = 2:1 is selected.

Embodiment 2

[0051] The prescriptions of 4%, 6%, and 8% disintegrants were prepared, and the dissolution rate of different proportions of disintegrants in pH4.5 medium was investigated for 15 minutes, as shown in Table 3 below.

[0052] Table 3 Preparation of different disintegrant dosage prescriptions

[0053]

[0054] The investigation result of disintegrant dosage is as follows:

[0055] From figure 2 Dissolution data are available, 4% disintegrant prescription can not reach 85% in 15 minutes, and there is no significant difference in dissolution between 6% and 8% disintegrants, so 6% disintegrant is selected as the optimal ratio .

Embodiment 3

[0057] Disintegrant crospovidone is the key functional excipient in the prescription. We consider selecting disintegrants from different manufacturers for screening, preparing prescriptions, and investigating their dissolution behavior in acetate buffer at pH 4.5. See Table 4.

[0058] Table 4 Preparation of disintegrant prescriptions from different manufacturers

[0059]

[0060] The inspection results of different manufacturers of disintegrants are as follows:

[0061] From image 3 Dissolution data are available, and there is no significant difference in the dissolution of disintegrants from the two manufacturers. In this study, imported cross-linked polyvinyl chloride from BASF in Germany was selected as the disintegrant in the prescription.

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and discloses a solid preparation of palbociclib isethionate and a preparation method thereof. The solid preparation is a palbociclib isethionate tablet and is prepared by dry granulation and tabletting, and the repose angle of particles obtained by dry granulation is less than 45 degrees; and the preparation auxiliary materials of the palbociclib isethionate tablet comprise a filling agent, a disintegrating agent, a flow aid and a lubricating agent. According to the optimized product, the palbociclib isethionate is taken as a raw material medicine, and the dosage form is improved to be palbociclib isethionate tablet. The invention establishes and optimizes a set of complete preparation process of the palbociclib isethionate tablet, finally obtains the optimal prescription and preparation process of the palbociclib isethionate tablet, can solve the problems of poor solubility and high hygroscopicity, meets the quality and stability requirements, and can be popularized in production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a solid preparation of palbociclib isethionate and a preparation method thereof, in particular to a prescription and a preparation process of palbociclib isethionate tablets. Background technique [0002] Palbociclib is the world's first CDK4 / 6 kinase inhibitor approved by the US FDA on February 3, 2015. It is developed, produced and sold by Pfizer. Approved together with letrozole (Letrozole) as endocrine-based first-line therapy for the treatment of menopausal women with androgen receptor (ER) positive, human epidermal growth factor receptor 2 (HER2) negative advanced breast cancer patients. [0003] In the treatment of ER-positive, HER2-negative locally advanced or metastatic breast cancer, palbociclib has a good curative effect when used in combination with aromatase inhibitors as the initial endocrine therapy for postmenopausal female patients; Listed in h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/26A61K47/32A61K47/04A61K47/12A61K31/519A61P35/00A61P35/04
CPCA61K9/2054A61K9/2018A61K9/2027A61K9/2009A61K9/2013A61K9/2095A61K31/519A61P35/00A61P35/04
Inventor 王静孙嘉怡杨猛
Owner JIANGSU FOOD & PHARMA SCI COLLEGE
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