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Diflucortolone valerate novel crystal form and topical external preparation prepared by same

A technology of diflucorylate valerate and crystal form, which can be applied to anti-inflammatory agents, non-central analgesics, medical preparations containing active ingredients, etc. Efficacy, affecting drug bioavailability and other issues

Active Publication Date: 2013-06-05
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In addition, we also found that with the storage of the existing difluorocorrone valerate cream, the fine powder of difluorocorrone valerate originally distributed in the paste in the state of suspended particles appeared agglomerated
As a result, the particle size of the drug micropowder becomes larger. Although the current drug standards do not provide for the situation of creams, our experiments have found that the increase in the particle size of the drug micropowder directly affects the bioavailability of the drug and thus affects the curative effect.

Method used

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  • Diflucortolone valerate novel crystal form and topical external preparation prepared by same
  • Diflucortolone valerate novel crystal form and topical external preparation prepared by same
  • Diflucortolone valerate novel crystal form and topical external preparation prepared by same

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Embodiment 1

[0055] The preparation of embodiment 1 crystal form I

[0056] Dissolve 10g of diflucorrone valerate in 20ml of tetrahydrofuran, heat until dissolved, filter off the insolubles while hot, then evaporate under reduced pressure, cool down after crystals appear, filter, and dry to obtain diflucorrone valerate crystals Type I.

[0057] Obtained crystals were measured by X-ray powder diffraction, and the measured characteristic peak positions were 2θ=10.0°, 10.9°, 12.6°, 19.9°, 22.9, such as figure 1 shown.

Embodiment 2

[0058] The preparation of embodiment 2 crystal form I

[0059] Add 1 g of diflucoral valerate into 3 mL of tetrahydrofuran, heat to reflux, filter off the insoluble matter while it is hot, then cool down to 5 °C at a rate of 0.1 °C / min, precipitate crystals, filter, and dry to obtain difluorocoron Valerate crystalline form I.

[0060] The obtained crystals were determined by X-ray powder diffraction, and the measured characteristic peak positions were 2θ=10.0°, 10.9°, 12.6°, 19.9°, 22.9°.

Embodiment 3

[0061] The preparation of embodiment 3 crystal form I

[0062] Dissolve 1kg of difluorocorrone valerate in 3L of tetrahydrofuran, heat until dissolved, filter off the insoluble matter, then slowly add 8L of water, add slowly, stir while adding, after the addition, filter and dry to obtain Form I of diflucoral valerate.

[0063] The obtained crystals were determined by X-ray powder diffraction, and the measured characteristic peak positions were 2θ=10.0°, 10.9°, 12.6°, 19.9°, 22.9°.

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Abstract

The invention discloses a diflucortolone valerate novel crystal form and a topical external preparation prepared by the diflucortolone valerate novel crystal form, provides a novel diflucortolone valerate crystal form I, and further provides aqueous preparations with diflucortolone valerate crystal form I micro powder scattered in auxiliary materials in a suspending status. The diflucortolone valerate preparation can avoid agglomeration of the micro powder when stored, and therefore high bioavailability is maintained. Meanwhile, content stability in storage is good.

Description

technical field [0001] The invention relates to a new crystal form of steroid corticosteroid and a local external preparation of steroid corticosteroid Background technique [0002] The molecular formula of diflucortolone valerate (CAS: 59198-70-8, Diflucortolone Valerate) is as follows: [0003] [0004] Diflucorrone valerate is a type of steroid corticosteroid that inhibits inflammatory and allergic skin reactions, and also inhibits reactions associated with accelerated cell regeneration leading to symptoms such as erythema, edema, thickening of the skin, skin Reduction of surface roughness and relief of itching, burning and pain problems. Due to the introduction of 21-valerate in the molecule, the fat solubility of diflucosolone valerate is better, so that a better curative effect can be achieved in external treatment. German patent DE2617655, according to the prior art, we prepared diflucoral valerate crystals, and measured the obtained product by X-ray powder diffr...

Claims

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Application Information

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IPC IPC(8): C07J5/00A61K31/573A61K9/10A61P29/00A61P17/00
Inventor 李娜何运良李静
Owner TIANJIN JINYAO GRP
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