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Medicinal composition containing temsirolimus and preparation method of medicinal composition

A technology of composition and esterification, which is applied in the field of pharmaceutical composition containing temsirolimus ester compound and its preparation, can solve problems such as hypersensitivity, increased irritation or toxicity, and vascular atrophy, so as to reduce production costs, Improved stability and process safety

Inactive Publication Date: 2013-02-27
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

solved at the same time Non-aqueous composite solvents such as ethanol and propylene glycol in the prescription lead to increased irritation or toxicity, hypersensitivity reactions caused by clinical application, serious side effects such as vascular atrophy, and the compatibility of the two-bottle preparation of the freeze-dried preparation disclosed in the CN1829514A patent is complicated Sexuality and easy to cause secondary pollution risk, high cost and other issues

Method used

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  • Medicinal composition containing temsirolimus and preparation method of medicinal composition
  • Medicinal composition containing temsirolimus and preparation method of medicinal composition
  • Medicinal composition containing temsirolimus and preparation method of medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Because the water solubility of temsirolimus ester compound is very poor, solubilizer is needed to solubilize, the contriver is to commonly used cosolvent polysorbate 80 in the injection, polyethylene glycol stearate 15 (Solutol-HS15), Tocopheryl polyethylene glycol succinate (TPGS), sodium deoxycholate, etc. were screened, and the prescription was designed as follows:

[0029] Co-solvent screening of temsirolimus ester lyophilized preparation

[0030]

[0031] The above prescription was studied on the influencing factors at 40°C, and the results are shown in the table below:

[0032]

[0033] The experimental results show that in four typical co-solvents polysorbate 80, polyethylene glycol stearate 15 (Solutol-HS15), tocopherol polyethylene glycol succinate (TPGS), sodium deoxycholate , the stability of the pharmaceutical composition containing the temsirolimus ester compound of polyethylene glycol stearate 15 (Solutol-HS15) is the best, so in follow-up research, ...

Embodiment 2

[0035] according to Formulation of Concentrate A concentrate of temsirolimus ester was prepared as a control. outsourcing A concentrate formulation served as a control. Concentrate Prescription

[0036]

[0037] Dissolving the prescribed amount of active ingredients sirolimus ester, anhydrous citric acid, and d,l-alpha-tocopherol in a composite solvent of absolute ethanol and propylene glycol, filling according to the content, filling with nitrogen, and capping. The sirolimus ester concentrate was used as a control.

Embodiment 3

[0039] Prescription of temsirolimus ester freeze-dried pharmaceutical composition

[0040] Component role

ingredients

Dosage

active ingredient

sirolimus ester

25mg

excipient

Trehalose

750mg

stabilizer

anhydrous citric acid

0.25mg

Antioxidants

α-tocopherol

0.75mg

Co-solvent

Solutol-HS15

250mg

solvent

Solvents used in the process and eventually removed

water and tert-butanol

[0041] Dissolve the active ingredient temsirolimus ester compound, anhydrous citric acid and α-tocopherol in the prescribed amount in tert-butanol to make the oil phase, dissolve Solutol-HS15 and trehalose in water to make the water phase, and the water phase oil After the phases were mixed, the volume was adjusted to 5 g, and then stirred to clarify to obtain a freeze-dried stock solution.

[0042] After the above preparation was freeze-dried, filled with nitrogen, capped, and stored at 25°C...

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PUM

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Abstract

The invention relates to a medicinal composition containing temsirolimus and a preparation method of the medicinal composition. Polyethylene glycol stearate 15 as latent solvent is added in a formula, so that the problem of settlement generated by clinically using physiological saline to dilute a temsirolimus freeze-dried powder injection is effectively solved, further the content of an isomer of the temsirolimus and the content of oxidative degradation impurities are reduced and the stability and the safety of the medicament are improved. The freeze-dried medicinal composition disclosed by the invention is simple in preparation process and low in production cost and is suitable 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 temsirolimus ester compound and a preparation method thereof. Background technique [0002] Sirolimus ester compound (English name, Temsirolimus) is 42-bis-hydroxymethyl propionate of rapamycin, and its structural formula is as follows: [0003] [0004] This compound was first disclosed in US Patent No. 5,362,718A, and it exhibits inhibition of cell growth and reproduction in in vivo and in vitro models, rather than cytotoxicity, and it can also delay the development time of tumors or the recurrence time of tumors. The mechanism of action is considered to be similar to that of sirolimus, mainly by binding to the cytoplasmic protein FKBP and forming a complex, inhibiting the enzyme mTOR (mammalian target of rapamycin, also known as FKBP12-sirolimus-related protein [FRAP]). Inhibition of mTOR kinase activity leads ...

Claims

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Application Information

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IPC IPC(8): A61K31/436A61K47/34A61P37/02A61P29/00A61P31/10A61P35/00
CPCA61K47/30A61K31/436A61K9/19A61P29/00A61P31/10A61P35/00A61P37/02
Inventor 苏正兴曹金全王端统王晓微李俊英姜丽丽李正邦
Owner ZHEJIANG HISUN PHARMA CO LTD
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