CN1617709A - Stable topical formulation of clarithromycin - Google Patents
Stable topical formulation of clarithromycin Download PDFInfo
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- CN1617709A CN1617709A CNA028279662A CN02827966A CN1617709A CN 1617709 A CN1617709 A CN 1617709A CN A028279662 A CNA028279662 A CN A028279662A CN 02827966 A CN02827966 A CN 02827966A CN 1617709 A CN1617709 A CN 1617709A
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- clarithromycin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
Abstract
This invention relates to a stable topical formulation of clarithromycin and its use in the treatment of acne.
Description
Invention field
The present invention relates to a kind of stable topical formulation of clarithromycin and the application in the treatment acne thereof.
Background of invention
Acne is the common inflammatory diseases of a kind of sebaceous gland.Corynebacterium acnes normally causes the microorganism of acne infection.
The various Therapeutic Method of treatment acne comprise oral and local application antibacterial and systemic antibiotics at present.Normally used is tetracycline, but also can use other antibiotic, as erythromycin, lincomycin and clindamycin.Although oral these medicines are normally treated the effective ways of acne, its shortcoming is will make systemic exposure in antibiotic for tackling local patholoic change.
The local antibiotic that uses can make when killing the diseased region antibacterial that antibiotic level minimizes in blood circulation and the gastrointestinal systems.This is a kind ofly can effectively treat the local skin pathological changes, as acne, the approach of Noninvasive easily.
U.S. Patent No. 4,132,781 have described a kind of compositions that is used for topical therapeutic acne S﹠S, wherein contain antibiotic and the 2-Pyrrolidone or the N-low alkyl group-2-Pyrrolidone of erythromycin family.
U.S. Patent No. 4,469,684 have described a kind of pharmaceutical composition that is used for treating acne, wherein contain zinc erythromycin and uncle 50-99%-butanols.
U.S. Patent No. 4,299,826 have described the topical application of compositions that is used for treating dermatosis and bacterial origin dermatoses, wherein contain the antibiotic formulations and a kind of carrier that are selected from erythromycin and derivant thereof on a small quantity, contain the Dermol DIPS and the ethanol of infiltration enhancing amount in the carrier.
U.S. Patent No. 5,455,037 has described the stable local cream composition that is used for the treatment of the animal skin infected by microbes, wherein contains erythromycin, polysiloxanes, ethanol, water and emulsifying agent.
Although these patents have all been described the topical formulations of erythromycin and salt and derivant, the erythromycin derivatives of their all not mentioned for example clarithromycins and so on.Clarithromycin is a kind of macrolide antibiotics, and it has the antibacterial activity of very strong resisting gram-positive bacteria, and it has been generally acknowledged that than parent drug has stronger antibacterial activity.
The therapeutic efficiency of used antibiotic composition depends on that composition therefor is carried and passes epidermis and enter deep skin and follicular ability that folliculus and sebum stop up, contains the microorganism that causes acne infection in these folliculus.
Summary of the invention
Unexpected now discovery, by using preparation described here, the local application clarithromycin can effectively be treated acne.Because clarithromycin is unstable in water-bearing media, the topical formulations of preparation clarithromycin is a kind of challenge.
The present invention relates to a kind of stable topical formulation of clarithromycin, described preparation comprises the clarithromycin that is blended in the oil phase; A kind of nonaqueous phase or aqueous emulsions; And other pharmaceutically acceptable excipient.
The invention still further relates to a kind of method for the treatment of acne in the human or animal who needs is arranged, described method comprises that local application contains the preparation of clarithromycin.
Detailed Description Of The Invention
The amount that can be used for clarithromycin of the present invention can change according to the specific symptoms of being treated, the seriousness and the other factors of symptom.Therefore, can be made into the emulsion formulations of varying strength, wherein can contain the clarithromycin that accounts for weight of formulation about 0.1% to about 10%.
According to the present invention, clarithromycin is blended in the suitable oils, described oil phase such as monoglyceride, diglyceride, triglyceride, fatty acid, aliphatic alcohol, vegetable oil, mineral oil, their derivant and mixture.The amount of used oil phase depends on the amount of the dissolved clarithromycin of needs.The amount that can be used for oil phase of the present invention is about 5% to about 40% of weight of formulation.These solubilizing agents can not only dissolved substance, and can also the messenger drug thing isolates and help medicine better penetrate skin with aqueous environment on every side.
The oil mixture of described clarithromycin can be emulsified in the water or add in the non-aqueous excipient.In a kind of preparation, the oil mixture of described clarithromycin is added in the non-aqueous excipient, and described non-aqueous excipient is selected from high molecular and low molecular poly, hexadecanol octadecanol mixture, hexadecanol, cetyl esters wax, lanolin alcohol, microwax, nonionic emulsifing wax, stearyl alcohol, white beeswax, paraffin etc.
Described preparation also can contain other pharmaceutically acceptable excipient, forms agent/emulsifying agent, gellant, antioxidant, antiseptic, agent of neutralization/pH regulator and chelating agen as emulsion.
The emulsion that can be used for these preparations forms the ester that agent or emulsifying agent comprise carbomer, castor oil derivatives, sorbitan fatty ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene alkyl ether, sad and tricaprin, macrogol ester and other nonionic surfactants type.The amount that is used for described emulsion formation agent of the present invention or emulsifying agent is about 5% to about 20% of a weight of formulation.
The gellant that can be used for these preparations comprises the conventional gellant with gelling characteristic, cellulose ether for example, and as hydroxypropyl cellulose, hydroxy methocel, hydroxypropyl emthylcellulose, carboxymethyl cellulose, sodium carboxymethyl cellulose, hydroxylated cellulose etc.; Vinyl alcohol; Vinyl pyrrolidone; Natural gum, as karaya, locust bean gum, guar gum, gellan gum, xanthan gum, arabic gum, Tragacanth, carrageenin, pectin, agar, alginic acid and sodium alginate etc., methacrylate, as by Rohm Pharma with trade name Eudragit
Those that sell and polyacrylate as by B.F.Goodrich with trade name " Carbopol
" sell those.Other gellant comprises that polyoxyethylene-polyoxypropylene is copolymer (poloxamer), as those of commodity by name " Lutrol ".
The amount that can be used for the gellant of preparation depends on used gellant.The gellant of low concentration can make preparation loose or mobile, and this preparation can flow when using, and higher concentration can obtain being difficult for the rigid preparation of coating.The amount of gellant can account for about 0.3% to about 40%, for example about 0.5% to about 30% of weight of formulation.
The chelating agen that can be used for these preparations comprises the known conventional chelating agen in this field, for example disodiumedetate.The consumption of chelating agen can be about 0.005% to about 2.0% of weight of formulation.
According to the present invention, described preparation can comprise the antioxidant that accounts for weight of formulation about 0.005% to about 1.0%, and antioxidant has, for example, butylated hydroxyanisol (BHA), butylated hydroxy-methylbenzene (BHT), tertiary butylated hydroquinone, propyl gallate, alpha-tocopherol etc.Described preparation also can contain antiseptic, and antiseptic accounts for about 0.1% to about 2.0% of weight of formulation.Operable antiseptic comprises phenoxyethanol, nipagin, propyl parabene, Butyl Chemosept, benzyl alcohol etc.
According to the present invention, described preparation also can contain the pH regulator agent.The pH of preparation of the present invention can be transferred to 4.0-8.0.Preferably transfer to pH 6.0-7.0.Described pH regulator agent can be selected from the inorganic or organic basic salt of safety on any reagent of knowing and the pharmacology.The example of inorganic alkaline salt comprises magnesium oxide, magnesium hydroxide, calcium hydroxide, sodium hydroxide, potassium hydroxide, potassium carbonate, sodium bicarbonate etc.The example of organic basic salt comprises carbinolamine, ethanolamine, Propanolamine, trimethanolamine, triethanolamine, alkylamine such as methylamine, ethamine, butylamine, 2-aminopropane. etc.
Preparation described here has preferably stability, and skin is had preferably tack and feels soft and smooth.Preparation of the present invention can use to act on skin area any form easily part, and these forms for example have gel, cream, ointment, lotion, spray etc.
Following examples have been described some preferred topical formulations by method preparation of the present invention and use, but are not to limit its scope.
Embodiment 1-5
The emulsion oil-in-water preparation
| Composition | Content (%w/w) | ||||
| ????1 | ?????2 | ?????3 | ?????4 | ?????5 | |
| Clarithromycin | ????1.0 | ????1.0 | ????1.0 | ????1.0 | ????1.0 |
| Oleic acid | ????5.0 | ????5.0 | ????5.0 | ????5.0 | ????5.0 |
| Isopropyl myristate | ????10.0 | ????20.0 | ????15.0 | ????20.0 | ????10.0 |
| Phenoxyethanol | ????1.0 | ????1.0 | ????1.0 | ????1.0 | ????1.0 |
| Tween 80 | ????2.0 | ????2.0 | ????2.0 | ????2.0 | ????2.0 |
| Lutrol?F127 | ????-- | ????-- | ????-- | ????-- | ????15.0 |
| Carbopol?940 | ????0.5 | ????0.1 | ????0.5 | ????0.4 | ????-- |
| Carbome?1342 | ????0.6 | ????0.6 | ????0.6 | ????0.6 | ????0.6 |
| Triethanolamine | ????1.0 | ????1.25 | ????1.0 | ????1.25 | ????-- |
| Disodiumedetate | ????0.1 | ????0.1 | ????0.1 | ????0.1 | ????0.1 |
| Butylated hydroxyanisol | ????0.05 | ????0.05 | ????0.05 | ????0.05 | ????0.05 |
| Sodium hydroxide (5% solution) is to pH 7.0w/v | ????0.78v/w | ????-- | ????0.76v/w | ????0.63v/w | ?????0.39v/w |
| Essence | ????0.39 | ????0.39 | ????0.39 | ????0.39 | ????0.39 |
| Purified water | Surplus | Surplus | Surplus | Surplus | Surplus |
Butylated hydroxyanisol and clarithromycin are dissolved in oleic acid, add isopropyl myristate, carbomer 1342, polysorbate80 and some purified water then to form Emulsion.With gellant, be dispersed in the purified water separately as carbopol 940, and the dispersion that forms is added above-mentioned clarithromycin emulsion while stirring.Add essence.By adding in the triethanolamine and said preparation, and pH is transferred to 7.0 with sodium hydroxide.With the final weight of purified water adjustment.
Embodiment 6
The clarithromycin lotion
| Composition | Content (%w/w) |
| Clarithromycin | ????1.00 |
| Butylated hydroxyanisol | ????0.05 |
| Oleic acid | ????5.0 |
| Isopropyl myristate | ????15.00 |
| Pemulen TR2 (carbomer 1342) | ????0.60 |
| Phenyl phenol | ????1.00 |
| Disodiumedetate | ????0.1 |
| Tween 80 | ????2.0 |
| Triethanolamine | ????0.60 |
| Essence | ????1.0 |
| Purified water | Surplus |
The method of making lotion is similar to the method for making emulsion.
Embodiment-7
Ointment formulation
| Composition | Content (%w/w) |
| Clarithromycin | ????1.00 |
| Oleic acid | ????5.00 |
| Butylated hydroxyanisol | ????0.05 |
| PEG?4000 | ????25 |
| Essence 00329 | ????0.8 |
| PEG?400 | Surplus |
PEG 4000 is heated to 70 ℃ of fusings in period, adds part PEG 400 then.Clarithromycin is mixed with BHA and oleic acid and essence separately.The PEG and the mixing that the mixture of clarithromycin are added fusing.Regulate weight with PEG 400.
On 70 patients embodiment 3 described preparations are carried out opening, non-comparative research, patient age is 13-31 year, and M-F is 1: 1.The patient handles with 1% clarithromycin gel, every day twice, continues for six weeks.
Effect is studied in monitoring with regard to the following aspects:
(i) number of inflammatory (pimple/pustule and nodules) and non-inflammatory (blackhead) pathological changes.
(ii) greasy to face, erythema, incrustation, calcination and the degree of scratching where it itches are with 0-3 mark (numbness is serious to sensation)
(iii) the general improvements of doctor and patient evaluation is marked (deteriorate into fully and eliminate) with 0-6, and
(iv) the patient estimate as the cosmetics acceptability, represent (disliking enjoying a lot) with 0-5.
It is reported the temporary transient side effect of character gentleness is arranged in 6 patients (8.6%).There is not serious adverse to illustrate that the toleration of this clarithromycin gel is very good.
After estimating all parameters, doctor and patient have made their evaluation to the general improvements of patient's symptom, and be as shown in the table.
General improvements-doctor's evaluation
| Patient's number (%) (n=66) | |
| Remove fully: no evidenc e of disease or symptom | ????2(3.0％) |
| Show fabulous: 75-99% is improved | ????35(53.0％) |
| Performance is good: 50-74% is improved | ????18(27.3％) |
| Table is seen general: 25-49% is improved | ????8(12.1％) |
| Show relatively poor: 1-24% is improved | ????2(3.0％) |
| Situation is not improved | ????1(1.5％) |
| Be worse off | ????0.00 |
From these data as seen, in 2 patients (3%), observed fully and removed, in 53 patients (80.3%), observed the good fabulous performance of arriving, the effectiveness of this explanation treatment.
General improvements-patient's evaluation
| Patient's number (%) (n=66) | |
| Remove fully: no evidenc e of disease or symptom | ????4(6.1％) |
| Show fabulous: 75-99% is improved | ????38(57.6％) |
| Performance is good: 50-74% is improved | ????13(19.7％) |
| Table is seen general: 25-49% is improved | ????8(12.1％) |
| Show relatively poor: 1-24% is improved | ????3(4.6％) |
| Situation is not improved | ????0.00 |
| Be worse off | ????0.00 |
In 55 patients (83%), confirm to have good arrive fabulous performance and elimination fully, only in 11 patients (16.7%), have to be less than 50% improvement.The symptom that does not have the patient to estimate them is not improved or is more serious.This has shown the effectiveness of treatment once more.
Toxicity research
On Sprague Dawley rat, carry out inferior chronic skin toxicity.Every kg body weight 0-1000mg Biaxin is used, totally 28 days in the back that cut animal every day.Do not occur unusually during 28 days medication, and also occur unusually at 14 days recovery period, this has illustrated the safety of preparation.
Owing to described the present invention according to its specific embodiment, some are revised and equivalent variations is conspicuous for those technical staff that are proficient in this field, and are included within the scope of the present invention.
Claims (33)
1. a stable topical formulation of clarithromycin is characterized in that, described preparation comprises the clarithromycin that is blended in the oil phase; A kind of nonaqueous phase or aqueous emulsion; And other pharmaceutically acceptable excipient.
2. preparation as claimed in claim 1, wherein, described clarithromycin accounts for about 0.1% to about 10% of described weight of formulation.
3. preparation as claimed in claim 1, wherein, described oil phase is selected from monoglyceride, diglyceride, triglyceride, fatty acid, aliphatic alcohol, vegetable oil, mineral oil and derivant thereof.
4. preparation as claimed in claim 3, wherein, described fatty acid is selected from lauric acid, myristic acid, Palmic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidonic acid and derivant thereof.
5. preparation as claimed in claim 3, wherein, described vegetable oil is selected from Oleum Glycines, safflower oil, Semen Maydis oil, Oleum Gossypii semen, Oleum Arachidis hypogaeae semen, olive oil, Oleum Cocois, Semen Lini oil and composition thereof.
6. preparation as claimed in claim 3, wherein, described mineral oil is liquid paraffin.
7. preparation as claimed in claim 1, wherein, described oil phase accounts for about 2% to about 40% of described weight of formulation.
8. preparation as claimed in claim 1, wherein, described preparation is an emulsion oil-in-water.
9. preparation as claimed in claim 1, wherein, described nonaqueous phase is selected from high molecular and low molecular poly, hexadecanol octadecanol mixture, hexadecanol, cetyl esters wax, lanolin alcohol, lanoline, microwax, nonionic emulsifing wax, stearyl alcohol, white beeswax, vaseline, paraffin and composition thereof.
10. preparation as claimed in claim 1, wherein, described pharmaceutically acceptable excipient comprises emulsifying agent, gellant, chelating agen, pH regulator agent, antiseptic and antioxidant.
11. preparation as claimed in claim 10, wherein, described emulsifying agent is selected from the ester of carbomer, castor oil derivatives, sorbitan fatty ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene alkyl ether, sad and tricaprin, macrogol ester and other nonionic surfactants type.
12. preparation as claimed in claim 10, wherein, described emulsifying agent accounts for about 5% to about 20% of described weight of formulation.
13. preparation as claimed in claim 10, wherein, described gellant is selected from cellulose ether, vinyl alcohol, vinyl pyrrolidone, natural gum, methacrylate, polyacrylate and poloxamer.
14. preparation as claimed in claim 13, wherein, described cellulose ether is selected from hydroxypropyl cellulose, hydroxy methocel, hydroxypropyl emthylcellulose, carboxymethyl cellulose, sodium carboxymethyl cellulose and hydroxylated cellulose.
15. preparation as claimed in claim 13, wherein, described gummy class is selected from karaya, locust bean gum, guar gum, gellan gum, xanthan gum, arabic gum, Tragacanth, carrageenin, pectin, agar, alginic acid and sodium alginate.
16. preparation as claimed in claim 13, wherein, described methacrylate is that Rohm Pharma is with trade name Eudragit
Those that sell.
17. preparation as claimed in claim 13, wherein, described polyacrylate is that B.F.Goodrich is with trade name " Carbopol
" sell those.
18. preparation as claimed in claim 10, wherein, described gellant accounts for about 0.3% to about 40% of described weight of formulation.
19. preparation as claimed in claim 18, wherein, described gellant accounts for about 0.5% to about 30% of described weight of formulation.
20. preparation as claimed in claim 10, wherein, described chelating agen is a disodiumedetate.
21. preparation as claimed in claim 10, wherein, described chelating agen accounts for about 0.005% to about 2.0% of described weight of formulation.
22. preparation as claimed in claim 10, wherein, described pH regulator agent is selected from magnesium oxide, magnesium hydroxide, calcium hydroxide, sodium hydroxide, potassium hydroxide, potassium carbonate, sodium carbonate etc., and organic salt, as carbinolamine, ethanolamine, Propanolamine, ethamine, butylamine and 2-aminopropane..
23. preparation as claimed in claim 22, wherein, described pH regulator agent is a triethanolamine.
24. preparation as claimed in claim 10, wherein, described antiseptic is selected from phenoxyethanol, benzyl alcohol, nipagin, propyl parabene and Butyl Chemosept.
25. preparation as claimed in claim 10, wherein, described antiseptic accounts for about 0.1% to about 2% of described weight of formulation.
26. preparation as claimed in claim 10, wherein, described antioxidant is selected from butylated hydroxyanisol, butylated hydroxy-methylbenzene, propyl gallate, alpha-tocopherol and tertiary butylated hydroquinone.
27. preparation as claimed in claim 10, wherein, described antioxidant accounts for about 0.005% to about 1.0% of described weight of formulation.
28. preparation as claimed in claim 1, its pH can transfer to about 4.0 to about 8.0.
29. preparation as claimed in claim 1, its pH can transfer to about 6.0 to about 7.0.
30. preparation as claimed in claim 1, wherein, described topical formulations is gel, cream, ointment, lotion or spray.
31. preparation as claimed in claim 30, wherein, described topical formulations is an ointment.
32. the method for a treatment acne in the human or animal who needs is arranged is characterized in that described method comprises the described preparation of local application claim 1.
33. the method for a treatment acne in the human or animal who needs is arranged is characterized in that described method comprises that local application contains the preparation of clarithromycin.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN1243/DEL/01 | 2001-12-13 | ||
| IN1243DE2001 | 2001-12-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1617709A true CN1617709A (en) | 2005-05-18 |
Family
ID=11097143
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA028279662A Pending CN1617709A (en) | 2001-12-13 | 2002-12-12 | Stable topical formulation of clarithromycin |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1458358A1 (en) |
| CN (1) | CN1617709A (en) |
| AU (1) | AU2002347541A1 (en) |
| WO (1) | WO2003049716A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113876696A (en) * | 2021-11-16 | 2022-01-04 | 中国人民解放军海军军医大学第一附属医院 | Clarithromycin hydrogel capable of being locally injected, preparation method and application thereof |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050079228A1 (en) * | 2003-05-30 | 2005-04-14 | Ashish Jaiswal | Clear, stable topical compositions of clarithromycin and processes for their preparation |
| EP1588697A1 (en) * | 2004-04-16 | 2005-10-26 | Kurt H. Prof. Dr. Bauer | Emulsion gel for topical application of pharmaceuticals |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2056445A1 (en) * | 1989-05-26 | 1990-11-27 | Ho-Wah Hui | Injectable clarithromycin composition |
| GB9723669D0 (en) * | 1997-11-07 | 1998-01-07 | Univ Aberdeen | Skin penetration enhancing components |
| BR0010794A (en) * | 1999-05-24 | 2002-06-04 | Sonus Pharma Inc | Emulsion-vehicle for drugs with poor solubility |
| WO2001066117A1 (en) * | 2000-03-09 | 2001-09-13 | Ian Andrew Whitcroft | Treatment of inflammatory dermatoses comprising erythromycin or clarythromycin metronidazole and a gastrointestinal hydrogen pump inhibitor |
-
2002
- 2002-12-12 WO PCT/IB2002/005323 patent/WO2003049716A1/en not_active Application Discontinuation
- 2002-12-12 CN CNA028279662A patent/CN1617709A/en active Pending
- 2002-12-12 EP EP02783471A patent/EP1458358A1/en not_active Withdrawn
- 2002-12-12 AU AU2002347541A patent/AU2002347541A1/en not_active Abandoned
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113876696A (en) * | 2021-11-16 | 2022-01-04 | 中国人民解放军海军军医大学第一附属医院 | Clarithromycin hydrogel capable of being locally injected, preparation method and application thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2002347541A1 (en) | 2003-06-23 |
| WO2003049716A1 (en) | 2003-06-19 |
| EP1458358A1 (en) | 2004-09-22 |
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