CN1611212A - Anchoic acid emulsifiable paste and its preparing method - Google Patents
Anchoic acid emulsifiable paste and its preparing method Download PDFInfo
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- CN1611212A CN1611212A CN 200310109103 CN200310109103A CN1611212A CN 1611212 A CN1611212 A CN 1611212A CN 200310109103 CN200310109103 CN 200310109103 CN 200310109103 A CN200310109103 A CN 200310109103A CN 1611212 A CN1611212 A CN 1611212A
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Abstract
The present invention relates to a cream for external use-azelaic acid cream and its preparation method. Its formula includes 16-22% of azelaic acid, 72-82% of emulsion type matrix and 2-6% of additive agent, and its preparation method includes the following steps: micropulverizing and sieving acelaic acid, mixing oil phase auxiliary materials, heating and uniformly stirring them; mixing water phase auxiliary materials, heating and uniformly stirring them; then adding water phase solution into the oil phase, continuously stirring them and progressively cooling to below 55 deg.C, adding micropulverized azelaic acid, homogenizing them, cooling to room temperature and filling. Said invention is stable in quality, high in production efficiency and excellent in therapeutic effect.
Description
Technical field
The invention belongs to the pharmaceutical preparations technology field, what be specifically related to is externally used paste Azelaic Acid emulsifiable paste and preparation method thereof.
Background technology
Acne is the common skin diseases of adolescence and middle age.Though this disease does not generally hinder the holistic health in the patient, because good sending out in positions such as face amounts will stay the cicatrix that impairs appearance as untimely treatment, so usually bring heavy mental burden to the patient.
Azelaic Acid is a kind of saturated dicarboxylic acid that exists naturally.
Structural formula: HOOC-(CH
2)
7-COOH
Chemical name: 1, the 7-heptene dicarboxylic acid
Empirical formula: C
9H
16O
4
Nineteen eighty-three Nazzaro-perro etc. chances on this medicine to the remedy of acne effect when other dermatosiss of Azelaic Acid preparation for treating.Thereafter they in a planned way use 15% Azelaic Acid cream on acne patient, 100 examples, confirm that curative effect is obvious really.This part is reported in European Region and caused extensive attention.Bladon in 1986 etc., the 20% Azelaic Acid emulsifiable paste that Cunliffe in 1989 etc. successively provide with German Schering pharmaceutical factory, compare with oral tetracycline or excipient, to further examining, all think evident in efficacy and slight (the Br J Dermatol 1986 of untoward reaction with the effect effect of Azelaic Acid treatment acne; 114:493 and Acta DermatolVenereol 1989; Suppl 143:31).
Fittion in 1991 etc. to the overall merit with Azelaic Acid treatment Cuo are: slight to moderate struvite acne, through 20% Azelaic Acid every day 2 times, 5～6 months treatment, 65～80% patient can obtain good curative effect to fabulous level.Medium acne to the order of severity, there also have 60% patient to obtain to be good in fabulous curative effect.This achievement approximately can with topical application 0.05% tretinoin cream, or 5% peroxidating phenyl methylcarbamate gel, or 2% erythromycin emulsifiable paste, or oral tetracycline 0.5～1。0/ day curative effect is comparable, and the untoward reaction of part or general is then far beyond slightly (Drugs 1991; 41:780).
The mechanism of proving effective during as for Azelaic Acid treatment acne be it is generally acknowledged pathogen such as may removing the affected part propionibacterium acnes with this medicine, is suppressed relevant (the Ucta Dermatol Venerelo1989 of effect such as follicular epithelium hypertrophy keratinization and the formation of minimizing acne; Suppl 1453:14 and Acta Dermatol Venerol1989:Suppl 143:20).
German Schering of the early 1990s pharmaceutical factory at first produces 20% Azelaic Acid emulsifiable paste, special-purpose medicaments supply European market as the treatment acne, trade name Sdinoren hentriaconta-version Martin dale theExtra PHarmacopoeia (1996) records Azelaic Acid and 20% ointment thereof, illustrates that its indication is an acne.
German Schering of nineteen ninety-five pharmaceutical factory is to the clear import Skinoren in China Shen (Chinese translation Si Lian), and Ministry of Public Health is ratified, registration certificate X950550.
Nineteen ninety-five U.S. Allergan pharmaceutical factory also produces 20% Azelaic Acid ointment, trade name Azelex in succession.Report is the Finevin (these product have recorded the Berlex Laboratories in PhysiciansDesk Reference manufacturer) of U.S.'s listing in May calendar year 2001 recently.Its Main Ingredients and Appearance consists of: effective ingredient: the every gram of this product contain Azelaic Acid 0.2 gram (20%, w/w)
Adjuvant: cetearyl alcohol caprylate (cetearyl octanoate), glycerol (glycerin), glyceryl stearate (glyceryl stearate), cetearyl alcohol (cetearyl alcohol), cetyl palmitate (cetylpalmitate), cocoa glyceride (cocoglycerides), PEG-5 glyceryl stearate (PEG-5 glcerylstearate), propylene glycol (propylene glycol) and pure water, make antiseptic with benzoic acid.But its preparation technology sees disclosure is not arranged.
Because Azelaic Acid dissolubility in water less (dissolved 0.24g/100 approximately and restrain water in 20 o'clock) is soluble in boiling water, and patent report is arranged, the ointment that Azelaic Acid makes with dissolved state, its Azelaic Acid concentration limit is 10%, it is promptly destroyed to surpass this concentration emulsifiable paste stability.And its used adjuvant is comparatively special, and is domestic less.
Summary of the invention
The object of the present invention is to provide a kind of Azelaic Acid emulsifiable paste of emulsion-type substrate of high concentration.
Another purpose of the present invention provides a kind of method of Azelaic Acid emulsifiable paste of the emulsion-type substrate for preparing this high concentration.
The present invention is implemented by following technical proposals.
Its material component and weight proportion of Azelaic Acid emulsifiable paste of the present invention can be:
Azelaic Acid 16-22 part
Emulsion-type substrate 72-82 part
Additives 2-6 part
Described emulsion-type substrate is 16 compositionss more than two kinds to octadecanol, white vaseline, liquid paraffin, water, the fatty glyceride, and described adjuvant is sodium lauryl sulphate, propylene glycol, 3-cyclodextrin, benzoic acid.
Its material component and weight proportion of Azelaic Acid emulsifiable paste of the present invention also can be:
Azelaic Acid 16-22 part
16 to octadecanol 4-9 parts
Fatty glyceride 1-4 part
White vaseline 3-6 part
Liquid paraffin 2-5 part
Sodium lauryl sulphate 1-3 part
Propylene glycol 15-25 part
Water adds to 100 parts
Beta-schardinger dextrin-1-4 part
Benzoic acid 1-2 part
It mainly comprises following process steps Azelaic Acid cream preparation method of the present invention in addition:
(1), crosses 200 orders and reach with top sieve with the Azelaic Acid micronization;
(2) get the oil phase adjuvant and be mixed and heated to about 75 ℃-95 ℃, stir;
(3) the water adjuvant is mixed, be heated to about 75 ℃-95 ℃, stir;
(4) aqueous phase solution is joined in the oil phase, constantly stir also and be cooled to 40 ℃-55 ℃ gradually;
(5) add micronized Azelaic Acid and grind evenly, be chilled to the room temperature fill promptly.
And the oil phase adjuvant in the above-mentioned step (2) can be 16 to octadecanol, fatty glyceride, white vaseline, liquid paraffin etc., and heating-up temperature also can be for being heated to 80 ℃-90 ℃;
Water adjuvant in the above-mentioned step (3) can be to be propylene glycol, sodium lauryl sulphate, water, beta-schardinger dextrin-, benzoic acid etc., and heating-up temperature also can be for being heated to 80 ℃-90 ℃;
Gradually chilling temperature interval also can be to be cooled to 40 ℃-45 ℃ gradually in above-mentioned steps (4) medicament.
Azelaic Acid emulsifiable paste of the present invention is through repeatedly experimentation, preferential substrate material and additives kind and with the proportional quantity of principal agent and various host material and additives, the interval of processing step and various chilling temperatures, make the dissolubility of Azelaic Acid reach higher level, and increased stability of drug, principal agent reaches fineness more than 200 orders through micronization processes, more be dispersed in the substrate, form the solid dispersion of homogenizing, shortened the required time of skin absorbs, accelerate the speed of performance curative effect greatly, improved bioavailability.Technological process and control Rational Parameters have easy, steady quality, the characteristics that production efficiency is high controlled.
The beneficial effect that following clinical application research and conclusion further illustrate drops of the present invention.
The routine 14-35 of test selected altogether 121 year homeliness type acne patient.61 routine test group patient's external 20% Azelaic Acid emulsifiable pastes wherein, 60 routine matched group patient externals, 5% peroxidating benzoic acid emulsifiable paste.The test group effective percentage 70.5% as a result, matched group effective percentage 60.0%.Two groups of curative effect there was no significant differences (?=0.8849 P＞0.05 Ridit analyzes).Before and after the test group medication skin lesion integration relatively, have highly significant difference (should decrease integration before and after t=8.86 P＜0.01, the medication of t check=matched group relatively, have highly significant difference (t checks for t=11.41, P＜0.01=.Two groups of local untoward reaction relatively, there was no significant difference (p '=the direct probability method of 0.4498 P＞0.05 Fisher) is not all found systemic adverse reactions for two groups.Conclusion 20% Azelaic Acid breast is crossed treatment homeliness type acne determined curative effect, and is safe in utilization.
Model case (numbering 121A)
The patient, Shen Lingli, the women 17 years old, lives halfway up the hill Shitang village.Came institute to go to a doctor on June 23rd, 1999.
Skin of face pimple, abscess were shown effect 1 year repeatedly, and erythra shows as forehead, buccal portion, lower jaw part skin Semen setariae
22 of the red pimples of size, 3 of neck portion abscess, 12 of hoary hair's acne, 6 of blackhead are diagnosed as homeliness type acne, classification II level.Just do not use any oral and medicine for external use treatment in January before the rash.Give 20% Azelaic Acid emulsifiable paste external curing, be coated with the skin lesion place, early, the evening each with 1 time.The back further consultation of 2 weeks, whelk reduces, and counting is 14, and pustule disappears, and 3 of blackhead, hoary hair's acne are 5.Continue all further consultations of medication to 4, pimple is 5, and blackhead all disappears, 5 of hoary hair's acne.To 6 all further consultations, pimple all disappears, and hoary hair's acne also have 4.Inflammatory damage reduces 100%, and this routine patient's therapeutic evaluation is for curing.Part and systemic adverse reactions do not appear during the medication.
The specific embodiment
The present invention is further illustrated below in conjunction with embodiment, and following each embodiment only is used to illustrate the present invention, but to not restriction of the present invention.
Embodiment one
Take by weighing main ingredient: Azelaic Acid 200g, hexadecanol 60g, monoglyceride 30g, white vaseline 45g, liquid Paraffin 30g, sodium lauryl sulphate 20g, propylene glycol 200g, beta-schardinger dextrin-25g, benzoic acid 15g, water are with addition of to 1000g.Azelaic Acid is ground into micronization, crosses 200 mesh sieves.Get hexadecanol, glyceryl monostearate, white vaseline, liquid paraffin and be mixed and heated to about 80 ℃, stir; Propylene glycol, sodium lauryl sulphate, water, beta-schardinger dextrin-, benzoic acid are mixed, be heated to about 80 ℃, stir, aqueous phase solution is joined in the oil phase, constantly stir and be cooled to gradually about 50 ℃ and add the Azelaic Acid grinding evenly, be chilled to room temperature, the inspection of semifinished product is qualified, and fill promptly.
Embodiment two
Take by weighing main ingredient: Azelaic Acid 160g, octadecanol 40g, tristerin 10g, white vaseline 30g, liquid Paraffin 20g, sodium lauryl sulphate 10g, propylene glycol 150g, beta-schardinger dextrin-10g, benzoic acid 10g, water are with addition of to 1000g.Azelaic Acid is ground into micronization, crosses 300 mesh sieves.Get octadecanol, tristerin, white vaseline, liquid paraffin and be mixed and heated to about 90 ℃, stir; Propylene glycol, sodium lauryl sulphate, water, beta-schardinger dextrin-, benzoic acid are mixed, be heated to about 90 ℃, stir, aqueous phase solution is joined in the oil phase, constantly stir and be cooled to gradually about 40 ℃ and add the Azelaic Acid grinding evenly, be chilled to room temperature, the inspection of semifinished product is qualified, and fill promptly.
Embodiment three
Take by weighing main ingredient: Azelaic Acid 220g, hexadecanol 90g, monoglyceride 40g, white vaseline 60g, liquid Paraffin 50g, sodium lauryl sulphate 30g, propylene glycol 250g, beta-schardinger dextrin-40g, benzoic acid 20g, water are with addition of to 1000g.Azelaic Acid is ground into micronization, crosses 300 mesh sieves.Get hexadecanol, glyceryl monostearate, white vaseline, liquid paraffin and be mixed and heated to about 75 ℃, stir; Propylene glycol, sodium lauryl sulphate, water, beta-schardinger dextrin-, benzoic acid are mixed, be heated to about 75 ℃, stir, aqueous phase solution is joined in the oil phase, constantly stir and be cooled to gradually about 45 ℃ and add the Azelaic Acid grinding evenly, be chilled to room temperature, the inspection of semifinished product is qualified, and fill promptly.
Embodiment four
Take by weighing main ingredient: Azelaic Acid 200g, octadecanol 55g, tristerin 16g, white vaseline 40g, liquid Paraffin 36g, sodium lauryl sulphate 15g, propylene glycol 200g, beta-schardinger dextrin-15g, benzoic acid 18g, water are with addition of to 1000g.Azelaic Acid is ground into micronization, crosses 300 mesh sieves.Get octadecanol, tristerin, white vaseline, liquid paraffin and be mixed and heated to about 78 ℃, stir; Propylene glycol, sodium lauryl sulphate, water, beta-schardinger dextrin-, benzoic acid are mixed, be heated to about 78 ℃, stir, aqueous phase solution is joined in the oil phase, constantly stir and be cooled to gradually about 48 ℃ and add the Azelaic Acid grinding evenly, be chilled to room temperature, the inspection of semifinished product is qualified, and fill promptly.
Claims (7)
1, a kind of Azelaic Acid emulsifiable paste is characterized in that it is made by the component and the weight proportion of following raw materials according:
Azelaic Acid 16-22 part
Emulsion-type substrate 72-82 part
Additives 2-6 part
Described emulsion-type substrate is 16 compositionss more than two kinds to octadecanol, white vaseline, liquid paraffin, water, fatty glyceride, sodium lauryl sulphate, the propylene glycol, and described adjuvant is beta-schardinger dextrin-, benzoic acid.
2, Azelaic Acid emulsifiable paste as claimed in claim 1 is characterized in that it is made by the component and the weight proportion of following raw materials according:
Azelaic Acid 16-22 part
16 to octadecanol 4-9 parts
Fatty glyceride 1-4 part
White vaseline 3-6 part
Liquid paraffin 2-5 part
Sodium lauryl sulphate 1-3 part
Propylene glycol 15-25 part
Water adds to 100
Beta-schardinger dextrin-1-4 part
Benzoic acid 1-2 part
3. the preparation method of Azelaic Acid emulsifiable paste according to claim 1 and 2 is characterized in that comprising following process steps:
(1), crosses 200 mesh sieves with the Azelaic Acid micronization;
(2) get the oil phase adjuvant and be mixed and heated to about 75 ℃-95 ℃, stir;
(3) the water adjuvant is mixed and heated to about 75 ℃-95 ℃, stirs;
(4) aqueous phase solution is joined in the oil phase, constantly stirring and emulsifying also is cooled to 40 ℃-50 ℃ gradually;
(1) adds micronized Azelaic Acid homogenizing, be chilled to the room temperature fill promptly.
4. the preparation method of Azelaic Acid emulsifiable paste according to claim 3 is characterized in that:
Oil phase adjuvant in the step (2) is 16 to octadecanol, fatty glyceride, white vaseline, liquid paraffin etc.
5. according to the preparation method of claim 3 or 4 described Azelaic Acid emulsifiable pastes, it is characterized in that: the water adjuvant in the step (3) is propylene glycol, sodium lauryl sulphate, water, beta-schardinger dextrin-, benzoic acid etc.
6. according to the preparation method of claim 3 or 4 or 5 described Azelaic Acid emulsifiable pastes, it is characterized in that: the heating-up temperature in step (2), (3) is heated to 80 ℃-90 ℃
7. the preparation method of Azelaic Acid emulsifiable paste according to claim 6 is characterized in that: step (4) medicament is cooled to 40 ℃-45 ℃ gradually;
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200310109103 CN1611212A (en) | 2003-12-05 | 2003-12-05 | Anchoic acid emulsifiable paste and its preparing method |
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| CN 200310109103 CN1611212A (en) | 2003-12-05 | 2003-12-05 | Anchoic acid emulsifiable paste and its preparing method |
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| CN1611212A true CN1611212A (en) | 2005-05-04 |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106580812A (en) * | 2017-02-14 | 2017-04-26 | 浙江添月生物科技有限公司 | Acne removing protection cream |
| CN114181072A (en) * | 2021-11-25 | 2022-03-15 | 宏翼(广东)新材料有限公司 | Preparation process of superfine azelaic acid |
| CN114767559A (en) * | 2022-05-14 | 2022-07-22 | 江苏华汀生物科技股份有限公司 | Azelaic acid liposome whitening cream and preparation method thereof |
| CN115475191A (en) * | 2022-10-20 | 2022-12-16 | 江苏集萃新型药物制剂技术研究所有限公司 | Cream for treating acne and preparation method thereof |
| CN115501171A (en) * | 2021-11-02 | 2022-12-23 | 上海丽舒丹医药科技有限公司 | High-concentration azelaic acid emulsifiable paste and preparation process thereof |
-
2003
- 2003-12-05 CN CN 200310109103 patent/CN1611212A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106580812A (en) * | 2017-02-14 | 2017-04-26 | 浙江添月生物科技有限公司 | Acne removing protection cream |
| CN115501171A (en) * | 2021-11-02 | 2022-12-23 | 上海丽舒丹医药科技有限公司 | High-concentration azelaic acid emulsifiable paste and preparation process thereof |
| CN114181072A (en) * | 2021-11-25 | 2022-03-15 | 宏翼(广东)新材料有限公司 | Preparation process of superfine azelaic acid |
| CN114767559A (en) * | 2022-05-14 | 2022-07-22 | 江苏华汀生物科技股份有限公司 | Azelaic acid liposome whitening cream and preparation method thereof |
| CN114767559B (en) * | 2022-05-14 | 2024-05-10 | 江苏亨瑞生物医药科技有限公司 | Azelaic acid liposome whitening cream and preparation method thereof |
| CN115475191A (en) * | 2022-10-20 | 2022-12-16 | 江苏集萃新型药物制剂技术研究所有限公司 | Cream for treating acne and preparation method thereof |
| CN115475191B (en) * | 2022-10-20 | 2023-11-14 | 江苏集萃新型药物制剂技术研究所有限公司 | Cream for treating acne and preparation method thereof |
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