Tretinoin/TA-beta-CD clathrate, cream containing tretinoin/TA-beta-CD clathrate, and preparation methods of tretinoin/TA-beta-CD clathrate and cream

A technology of retinoic acid and clathrates, which is applied in the direction of active ingredients of hydroxyl compounds, non-active ingredients of polymer compounds, ointment delivery, etc., can solve the problems of no obvious improvement of retinoic acid absorption and poor transdermal absorption effect, and achieve Improve the effect of transdermal absorption, strong operability and simple process

Inactive Publication Date: 2016-07-06
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] It has been reported in previous studies that retinoic acid was made into β-CD inclusion compound, which solved the stability problem of retinoic acid to a certain extent. However, when it is administered as a cream, transdermal absorption requires a certain amount of matrix Lipophilic, but the β-CD used to carry retinoic acid in previous studies is hydrophilic, so that the absorption of retinoic acid has not been significantly improved, so the transdermal absorption effect is poor

Method used

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  • Tretinoin/TA-beta-CD clathrate, cream containing tretinoin/TA-beta-CD clathrate, and preparation methods of tretinoin/TA-beta-CD clathrate and cream
  • Tretinoin/TA-beta-CD clathrate, cream containing tretinoin/TA-beta-CD clathrate, and preparation methods of tretinoin/TA-beta-CD clathrate and cream
  • Tretinoin/TA-beta-CD clathrate, cream containing tretinoin/TA-beta-CD clathrate, and preparation methods of tretinoin/TA-beta-CD clathrate and cream

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The preparation of embodiment 1 retinoic acid / TA-β-CD clathrate

[0054] Weigh 100g of TA-β-CD and retinoic acid according to the ratio of substances 1:0.5, mix with a vortex mixer for 1min to make a physical mixture, divide the physical mixture into 2mL ampoules and seal them, and place them in a temperature-controlled heater , heated at 75°C for 2 hours with sealed and programmed temperature control, left to room temperature, and taken out to obtain the retinoic acid / TA-β-CD inclusion complex.

Embodiment 2

[0055] Preparation of Example 2 Retinoic Acid / TA-β-CD Inclusion Compound

[0056] Weigh 100 g of TA-β-CD and retinoic acid according to the ratio of substances of 1:1, mix them with a vortex mixer for 1 min to make a mixture, divide the physical mixture into 2 mL ampoules and seal them, place them in a temperature-controlled heater, After heating at 75°C for 2 hours with a sealed program and temperature control, it was left to room temperature and taken out to obtain the retinoic acid / TA-β-CD inclusion complex.

Embodiment 3

[0057] The preparation of embodiment 3 retinoic acid / TA-β-CD clathrate

[0058] Weigh 100g of TA-β-CD and retinoic acid according to the ratio of 1:3, mix with a vortex mixer for 1min to make a physical mixture, divide the physical mixture into 2mL ampoules and seal them, and place them in a temperature-controlled heater , heated at 75°C for 2 hours with sealed and programmed temperature control, left to room temperature, and taken out to obtain the retinoic acid / TA-β-CD inclusion complex.

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Abstract

The invention belongs to the field of pharmaceutical preparation research of pharmaceutical engineering, and particularly relates to a tretinoin/TA-beta-CD clathrate and preparation of cream containing the tretinoin/TA-beta-CD clathrate. The prepared tretinoin/TA-beta-CD clathrate can improve photostability and thermostability of tretinoin. The cream containing the tretinoin/TA-beta-CD clathrate has characteristics of improved transdermal permeability, slow-released medical molecules, and lasting action time, and can reduce irritation and toxic and side functions of tretinoin. Besides the cream, the tretinoin/TA-beta-CD clathrate can further be widely applied to research of various preparation forms. The preparation methods adopted in the invention are mature, simple, and convenient, are suitable for massive production, and can bring considerable economic benefit.

Description

technical field [0001] The invention belongs to the research field of pharmaceutical preparations in medical engineering, in particular to the preparation of a retinoic acid / TA-β-CD inclusion compound and a cream containing the retinoic acid / TA-β-CD inclusion compound, and its application scope relates to clinical medicine Formulation and aesthetic medicine and other fields. Background technique [0002] Retinoic acid (Tretinoin) has the effects of anti-keratosis, anti-inflammation, and anti-sebum, and is one of the first-selected drugs for acne treatment at home and abroad in recent years. However, the structure of retinoic acid is an organic weak acid with conjugated double bonds, which is easy to oxidize, and is extremely unstable when exposed to light and in the air. Stimulation, therefore, enhancing the stability of retinoic acid, reducing discomfort, and improving its bioavailability are the primary problems to be solved urgently in clinical application of retinoic ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K31/203A61K9/06A61P17/10
Inventor 王齐放李三鸣刘洪卓车鑫
Owner SHENYANG PHARMA UNIVERSITY
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