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Chlormadinone acetate self-microemulsion composition and preparing method and application thereof

A technology of chlormadinone and self-microemulsion, which is applied in the direction of drug combination, pharmaceutical formula, emulsion delivery, etc., can solve the problem of low curative effect, reduce the dosage, improve the compliance of use, and improve the oral bioavailability degree of effect

Active Publication Date: 2018-08-10
上海市生物医药技术研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, the research on the new formulation of chlormadinone has not been reported in the literature, people expect to develop a lower dose of chlormadinone, but the efficacy is not inferior to the original drug. new oral formulations of

Method used

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  • Chlormadinone acetate self-microemulsion composition and preparing method and application thereof
  • Chlormadinone acetate self-microemulsion composition and preparing method and application thereof
  • Chlormadinone acetate self-microemulsion composition and preparing method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0043] The pre-prescription study of embodiment 1 chlormadinone self-microemulsion composition

[0044] 1. Determination of equilibrium solubility of chlormadinone in each auxiliary material

[0045] Take 2ml each of the oil phase, surfactant and co-surfactant into a 10ml stoppered test tube, add excess chlormadinone raw material (about 50mg) respectively, vortex and mix well, and shake in a constant temperature water bath shaker at 37°C 72h (110rpm) to reach the dissolution equilibrium, take 1ml to 1.5ml EP tube, centrifuge (15000rpm, 10min), the supernatant is diluted with isopropanol, HPLC sample analysis, determination of chlormadinone in each oil phase, surface The equilibrium solubility in active agent and cosurfactant, measurement result is shown in Table 1. The results showed that different excipients had different dissolving abilities to chlormadinone, and the dissolution order of each oil relative to chlormadinone was as follows: Labrafac Lipophile WL 1349>oleic aci...

Embodiment 2

[0073] Embodiment 2 The preparation of self-microemulsion composition

Embodiment 21

[0075] Accurately weigh 100 mg of chlormadinone raw material, add 6 g of diethylene glycol monoethyl ether to dissolve the drug, and then add 8 g of polyethylene glycol 400, 20 g of Tween-80 and 16 g of ethyl oleate in sequence under magnetic stirring , after forming a transparent and uniform self-microemulsion composition, divide it into 50 parts on average, each part is equivalent to containing 2 mg of the main drug chlormadinone, which is equivalent to a single dose of the original drug The amount of chlormadinone contained.

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Abstract

The invention discloses a chlormadinone acetate self-microemulsion composition and a preparing method and application thereof. The chlormadinone acetate self-microemulsion composition comprises a maindrug chlormadinone acetate and adjuvants, wherein the adjuvants include oil-phase ethyl oleate, surfactant tween-80, auxiliary surfactant diethylene glycol monoethyl ether and polyethylene glycol 400. The in-vitro releasing ratio of the chlormadinone acetate self-microemulsion composition is obviously higher than that of brand-name drugs. Besides, as is shown by mouse in-vivo pharmacokinetic study, compared with the oral bioavailability of the brand-name drugs, the oral bioavailability of the chlormadinone acetate self-microemulsion composition is almost doubled. Therefore, by using the chlormadinone acetate self-microemulsion composition clinically, the drug dosage of chlormadinone can be potentially lowered, and thus the chlormadinone acetate self-microemulsion composition has the advantages that the side effect of drugs is lowered, and the using compliance of drug users is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a chlormadinone self-microemulsion composition, a preparation method and application thereof. Background technique [0002] Chlormadinone, chemical name: 6-chloro-17a-acetoxy-pregna-4,6-diene-3,20-dione, is the first-generation progestogen drug with strong progesterone activity, Antiestrogenic activity and weak glucocorticoid activity, no androgenic activity and antimineralocorticoid activity. Their mechanisms of action vary depending on their ingredients, formulation, dosage and usage. For example, the compound preparation composed of it and estrogen is mainly used to inhibit ovulation, the small dose used alone is mainly used to hinder fertilization, and the large dose is mainly used to prevent implantation. [0003] At present, the most widely used preparation form of the drug in clinical practice is the original research drug produced by a Ge...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/14A61K47/26A61K47/10A61K31/57A61P15/18A61P15/00A61P29/00A61P17/10A61P17/08A61P17/14A61P13/08
CPCA61K9/1075A61K31/57A61K47/10A61K47/14A61K47/26A61P13/08A61P15/00A61P15/18A61P17/08A61P17/10A61P17/14A61P29/00
Inventor 黄婷曾佳陈建兴陈良康郑伟曹云峰
Owner 上海市生物医药技术研究院
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