CN104490856A - Compound quinhydrone liposome and preparation method thereof - Google Patents
Compound quinhydrone liposome and preparation method thereof Download PDFInfo
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- CN104490856A CN104490856A CN201410699147.4A CN201410699147A CN104490856A CN 104490856 A CN104490856 A CN 104490856A CN 201410699147 A CN201410699147 A CN 201410699147A CN 104490856 A CN104490856 A CN 104490856A
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- liposome
- compound
- quinhydrone
- hydrochinone
- retinoic acid
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Abstract
The invention discloses compound quinhydrone liposome and a preparation method thereof. The compound quinhydrone liposome comprises drug active components such as retinoic acid and quinhydrone, and accessory materials. The compound quinhydrone liposome comprises, by weight, 1.0-6.0% of quinhydrone, 0.1-1.0% of retinoic acid, 70.0-85.0% of phosphatide, 15.0-25.0% of cholesterol and 0.1-1.0% of sodium bisulfate. The preparation method comprises the following steps of adding waterless ethanol and chloroform into quinhydrone, retinoic acid and sodium hydrogen sulfate for full dissolution, mixing the obtained solution and a waterless ethanol-chloroform solution of phosphatide and cholesterol to obtain a uniform mixed solution, carrying out vacuum pressure reduction, removing the organic solvent so that a uniform dry film is obtained, adding a preheated 0.2M phosphoric acid buffer into the uniform dry film, carrying out rotary evaporation washing on the film and carrying out ultrasonic treatment to obtain the compound quinhydrone liposome. The compound quinhydrone liposome has a stable structure, oxidation resistance and no irritation, has clear effects of treating chloasma, freckle and hyperpigmentation after inflammation, can promote skin targeting penetration, improves curative effects and has good effects.
Description
Technical field
The present invention relates to technical field of pharmaceuticals, particularly relate to a kind of compound hydrochinone liposome and preparation method thereof.
Background technology
Hydroquinone is the first-selected medication of the facial skin hyperpigmentary disorders local application of department of dermatologry branch of Chinese Medical Association experts recommend, clinically be used for the treatment of pigmentation spots after chloasma, freckle and inflammation, due to the hydroquinone structure of hydroquinone, character extremely unstable, very easily oxidation stain and losing efficacy, be a kind of photosensitive material, under illumination and alkali condition more so, thus limit its clinical practice.
Tretinoin is the Metabolic Intermediate of vitamin A, by the mitosis of reconciliation statement chrotoplast and the renewal of epidermis cell, can eliminate tiny wrinkle, reduce the roughness of skin, alleviate mottle, but zest is larger, patient compliance is bad, limits its clinical practice.
Liposome is a kind of small vesicle of bilayer of similar biofilm structure, as pharmaceutical carrier, drug encapsulation can be formed the spherical pastille liposome of superminiature in its lipoids bilayer.Liposome itself is little to human toxicity, and medicine is encapsulated in liposome, can reduce the release rate of medicine, prolong drug action time, reduces untoward reaction, strengthens pharmacological action, can also promote drug absorption at dermal topical application.
Summary of the invention
The invention provides a kind of compound hydrochinone liposome and preparation method thereof, the present invention is by being wrapped in liposome the compound preparation making compound hydrochinone liposome by hydroquinone and tretinoin.Improve the oxidation resistance of hydroquinone, again reduce the zest of tretinoin simultaneously, can promote that skin targeting permeates, anti-oxidation and extend the storage time, reduce skin irritation untoward reaction, the advantage such as heighten the effect of a treatment, and meets Clinical practice demand.
The present invention adopts following technical scheme:
Compound hydrochinone liposome of the present invention, comprise active constituents of medicine retinoic acid, hydroquinone and adjuvant, the percentage by weight of described compound hydrochinone liposome is composed as follows: hydroquinone 1.0% ~ 6.0%, retinoic acid 0.1% ~ 1.0%, phospholipid 70.0% ~ 85.0%, cholesterol 15.0% ~ 25.0%, sodium bisulfate 0.1% ~ 1.0%.
Preferred: the percentage by weight of described compound hydrochinone liposome is composed as follows: hydroquinone 2.9%, retinoic acid 0.5%, phospholipid 76.9%, cholesterol 19.2%, sodium bisulfate 0.5%.
The concrete steps of the preparation method of compound hydrochinone liposome of the present invention are as follows: first by hydroquinone, retinoic acid, sodium bisulfate adds dehydrated alcohol and chloroform fully dissolves, then mix with the dehydrated alcohol chloroformic solution of phospholipid and cholesterol, vacuum decompression, remove organic solvent, obtain even dry film, add the 0.2M phosphate buffer of preheating, rotary evaporation is ultrasonic after washing film, obtains compound hydrochinone liposome.
Phosphate buffer pH is 5.7.
Good effect of the present invention is as follows:
Compound hydrochinone liposomal product Stability Analysis of Structures of the present invention, antioxidation, nonirritant, the determined curative effect such as pigmentation spots after treatment chloasma, freckle and inflammation, can promote that skin targeting permeates, heighten the effect of a treatment, effective.
Detailed description of the invention
The following examples describe in further detail of the present invention.
Embodiment 1:
Solution A: hydroquinone 0.06g, retinoic acid 10mg, sodium bisulfate 10mg adds 4ml dehydrated alcohol, 2ml chloroformic solution fully dissolves;
Solution B: phosphatidase 1 .6g, cholesterol 0.4g are added 6ml dehydrated alcohol, 1ml chloroformic solution fully mixes;
Solution C: solution A mixed with solution B, in 40 DEG C of vacuum decompressions, removes organic solvent, obtains even dry film.Add preheating 0.2M phosphate buffer (pH5.7) 50ml, rotate after washing film, ultrasonic 30min, cross 0.8 μm of filter membrane, obtain compound hydrochinone liposome, 4 DEG C of placements are for subsequent use.
Embodiment 2:
Solution A: hydroquinone 0.06g, retinoic acid 10mg, sodium bisulfate 10mg adds 4ml dehydrated alcohol, 2ml chloroformic solution fully dissolves;
Solution B: phosphatidase 1 .5g, cholesterol 0.5g are added 6ml dehydrated alcohol, 1ml chloroformic solution fully mixes;
Solution C: solution A mixed with solution B, in 40 DEG C of vacuum decompressions, removes organic solvent, obtains even dry film.Add preheating 0.2M phosphate buffer (pH5.7) 50ml, rotate after washing film, ultrasonic 30min, cross 0.8 μm of filter membrane, obtain compound hydrochinone liposome, 4 DEG C of placements are for subsequent use.
The liposome that the present invention obtains, places December at 4 DEG C of refrigerators and stablizes, and after treatment chloasma, freckle and inflammation, pigmentation spots etc. are effective.10 routine patient with chloasma participate in this research, respectively at patient facial region both sides application compound hydrochinone liposome and hydroquinone cream, within 1 month after the treatment, 6 months, carry out shade mensuration, to compare its curative effect.Result display patient facial region uses that compound hydrochinone liposome side chloasma color obviously shoals, scope obviously reduces, and compound hydrochinone liposome zest is less, and patient's compliance is better.
Although illustrate and describe embodiments of the invention, for the ordinary skill in the art, be appreciated that and can carry out multiple change, amendment, replacement and modification to these embodiments without departing from the principles and spirit of the present invention, scope of the present invention is by claims and equivalents thereof.
Claims (4)
1. a compound hydrochinone liposome, comprise active constituents of medicine retinoic acid, hydroquinone and adjuvant, it is characterized in that: the percentage by weight of described compound hydrochinone liposome is composed as follows: hydroquinone 1.0% ~ 6.0%, retinoic acid 0.1% ~ 1.0%, phospholipid 70.0% ~ 85.0%, cholesterol 15.0% ~ 25.0%, sodium bisulfate 0.1% ~ 1.0%.
2. compound hydrochinone liposome as claimed in claim 1, is characterized in that: the percentage by weight of described compound hydrochinone liposome is composed as follows: hydroquinone 2.9%, retinoic acid 0.5%, phospholipid 76.9%, cholesterol 19.2%, sodium bisulfate 0.5%.
3. prepare the method for compound hydrochinone liposome as claimed in claim 1 or 2 for one kind, it is characterized in that: the concrete steps of described method are as follows: first by hydroquinone, retinoic acid, sodium bisulfate adds dehydrated alcohol and chloroform fully dissolves, then mix with the dehydrated alcohol chloroformic solution of phospholipid and cholesterol, vacuum decompression, remove organic solvent, obtain even dry film, add the 0.2M phosphate buffer of preheating, rotary evaporation is ultrasonic after washing film, obtains compound hydrochinone liposome.
4. preparation method as claimed in claim 3, is characterized in that: phosphate buffer pH is 5.7.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410699147.4A CN104490856A (en) | 2014-11-27 | 2014-11-27 | Compound quinhydrone liposome and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410699147.4A CN104490856A (en) | 2014-11-27 | 2014-11-27 | Compound quinhydrone liposome and preparation method thereof |
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| Publication Number | Publication Date |
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| CN104490856A true CN104490856A (en) | 2015-04-08 |
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| CN201410699147.4A Pending CN104490856A (en) | 2014-11-27 | 2014-11-27 | Compound quinhydrone liposome and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108567599A (en) * | 2018-07-24 | 2018-09-25 | 合肥华盖生物科技有限公司 | A kind of preparation method of high-performance moisture saver mask |
| CN110585180A (en) * | 2019-09-25 | 2019-12-20 | 中国热带农业科学院环境与植物保护研究所 | Specific antidote for treating paraquat acute poisoning |
-
2014
- 2014-11-27 CN CN201410699147.4A patent/CN104490856A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108567599A (en) * | 2018-07-24 | 2018-09-25 | 合肥华盖生物科技有限公司 | A kind of preparation method of high-performance moisture saver mask |
| CN110585180A (en) * | 2019-09-25 | 2019-12-20 | 中国热带农业科学院环境与植物保护研究所 | Specific antidote for treating paraquat acute poisoning |
| WO2021057721A1 (en) * | 2019-09-25 | 2021-04-01 | 中国热带农业科学院环境与植物保护研究所 | Specific antidotal drug for treating paraquat acute poisoning |
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Application publication date: 20150408 |