Calcipotriol non-water gel

Abstract

A composition for local delivery of calcipotriol is disclosed. The composition comprises (a) not more than 1 wt% of calcipotriol, (b) ethanol, (c) propylene glycol, (d) oleic acid, (e) hydroxy propyl cellulose, (f) glycerol, and (g) 0-5 wt% of water, with the contents being based on the total weight of the composition. The composition has characteristics of high curative effects, low toxicity, stability, capability of guiding or reinforcing delivery of active medicines to skin, and high therapeutic index. The invention also relates to methods of manufacturing and using the composition.

Description

technical field [0001] The present invention relates to a topical non-aqueous skin preparation of calcipotriol, which has high curative effect, low toxicity, stability, and can guide or enhance the delivery of active medicine to the skin, thereby obtaining a higher therapeutic index. The invention also relates to methods of making and using the above compositions. technical background [0002] Calcipotriol is sensitive to light and heat, very easily soluble in 96% alcohol, but extremely insoluble in water (practically insoluble in water, freely soluble inethanol (96 per cent), slightly soluble in methylene chloride.It is sensitive to heat and light .EP5.3), there are ointment varieties on the market, such as the trade name Dalis, its concentration is 0.005% (w / w), suitable for psoriasis vulgaris (psoriasis). However, the molecular weight of calcipotriol is 413 (anhydrous), the molecule is relatively large, and the penetration power is relatively low. The penetration perform...

AI Technical Summary

Problems solved by technology

However, after calcipotriol is made into solid lipid particles, the particle radius will increase significantly, and the fat solubility will further increase, which may be beneficial to improve the penetration of the lipid layer of the skin, but it is not conducive to the penetration into the "water layer" of the skin , thus affecting the speed of its transfer to the skin as a whole, especially to the lesion, thereby affecting its skin bioavailability

In addition, when calcipotriol is made into solid lipid nanoparticles and then added to an aqueous carrier, the stability of the preparation may be affected, such as particle agglomeration, precipitation, etc.

Furthermore, the nanoscale preparation process of solid lipid particles is complicated, and the process reproducibility is poor. At this stage, the technology and conditions for large-scale industry production are not available, so it is difficult to be practically promoted.

[0005] Obviously, performances such as the calcipotriol preparation in the above-mentioned technology such as drug release performance, stability, drug transdermal performance need to be further improved

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