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CN102078326A - Topically applied composition containing povidone iodine and mometasone furoate - Google Patents

Topically applied composition containing povidone iodine and mometasone furoate Download PDF

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Publication number
CN102078326A
CN102078326A CN2009102287861A CN200910228786A CN102078326A CN 102078326 A CN102078326 A CN 102078326A CN 2009102287861 A CN2009102287861 A CN 2009102287861A CN 200910228786 A CN200910228786 A CN 200910228786A CN 102078326 A CN102078326 A CN 102078326A
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China
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pharmaceutical composition
povidone iodine
momestasone furoate
gel
preparation
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孙亮
陈松
赵琳
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Tianjin Jinyao Group Co Ltd
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Tianjin Jinyao Group Co Ltd
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Abstract

The invention relates to a topically applied composition containing povidone iodine and mometasone furoate, in particular to a topically applied pharmaceutical composition which contains the micronized mometasone furoate, the povidone iodine and one or more physiologically acceptable excipients applicable to topical application; and in the pharmaceutical composition, the content of the povidone iodine is 1%-10%, and the content of the mometasone furoate is 0.01%-0.1%.

Description

Compositions is used in the part of containing povidone iodine and momestasone furoate
Technical field:
The present invention relates to a kind of is that the part of active component makes pharmaceutical composition with povidone iodine and glucocorticoid.
Background technology:
Scytitis such as eczema (eczema), allergic dermatitis (allergic dermatitis), atopic dermatitis (atopic dermatitis) urticaria (Urticaria) etc. all is to be caused allergy and caused scytitis by certain allergen, the allergic effect that causes skin allergic reaction is original multiple, wherein viral, fungus, infection such as antibacterial cause one of major reason of scytitis, (detection and the clinical meaning thereof of allergy dermatitis patients serum fungus specific IgE such as Yuan Wei, Zunyi Medical College's journal, in February, 2004,24-25) disclose in 136 routine allergic dermatitis patients and have 96 examples to be diagnosed as the merging fungal infection, the document thinks that fungal infection is an important sensitizing agent in the various skin inflammation such as allergic dermatitis.Glucocorticoid is widely used in the treatment scytitis, but because the immunosuppressive action of glucocorticoid, makes glucocorticoid not only can not reach antiphlogistic effect when being used for the treatment of the inflammation that the skin surface fungal infection causes, and can make the inflammation aggravation on the contrary.Influenced the application of glucocorticoid when the treatment scytitis.Moreover because allergic dermatitis and noninfective allergic dermatitis that infection such as fungus cause are quite similar on surface symptoms, be difficult to differentiate, therefore cause mistaken diagnosis clinically easily, thereby delay treatment as not adopting microscopic examination.And the dermatosis that causes for infection such as dermatophytess, though in treatment, do not use glucocorticoid, but because the sensitization of microorganisms such as fungus, often be attended by the generation of allergic skin inflammation, (corticosteroid is to the influence of fungus for Jia Dongmei etc., foreign medical science skin cypridology fascicle, 2003 the 29th the 4th phases of volume, 201-203) disclose in the cutaneous fungal infection experiment, after adopting antifungal drug treatment to infection to eliminate, animal often also has the inflammatory crust to exist, and illustrates that scytitis often more is difficult to treatment than infection itself.
Rhinitis is a kind of common disease, mainly is divided into several types such as acute rhinitis, chronic rhinitis and allergic rhinitis, and wherein the acute disease rhinitis is the acute inflammation of nasal membrane, main viral infection, and Chang Jifa bacterial infection; Chronic rhinitis thoroughly and is not repeatedly shown effect relevant often by the acute rhinitis development with the secondary infection of merging antibacterial, treatment
Allergic rhinitis are first-selected to adopt local glucocorticoid to treat, for viral or produced the acute or chronic rhinitis of secondary infection, often will adopt antiviral or antibiotic therapy when treatment, the allergen of part allergic rhinitis itself also is microorganisms such as virus, fungus, antibacterial in addition.Xu Geng (the local glucocorticoid treatment new ideas of non-allergic effect persistence rhinitis (chronic rhinitis), clinical ENT ﹠ HN Surgery Dept. magazine the 21st the 14th phase of volume of July in 2007,636-638) think that glucocorticoid also can be used for chronic rhinitis, nosal inflammations such as sinusitis, but because glucocorticoid itself can cause the reduction of local immunity power as a kind of immunosuppressant, might cause partial fungal infection, therefore (nose is with the correct using method of corticosteroid for Yin Mingde, clinical ENT ﹠ HN Surgery Dept. magazine the 21st the 2nd phase of volume of January in 2007,49-50) think that nose with glucocorticoid in use, for the respiratory tract tuberculosis infection, undressed fungus, antibacterial, the patient Ying Shenyong of general viral infection and eye herpes simplex, it denys concurrent fungal infection that the long-term prescription patient should make regular check on that nasal mucosa and nasopharynx part have, therefore the range of application of local glucocorticoid when the treatment rhinitis has considerable restraint, all exist the use taboo for the rhinitis that exists cause pathogeny imcrobe infection, in addition because the multiformity of chronic rhinitis pathogenic microorganism, general antibiotic is in topical treatment effect and not obvious, and wrong use antibiotic is easier brings many potential side effect.
Povidone iodine (PVP-I is called for short PI) is the complex of polyvinylpyrrolidone (PVP) and iodine, claims povidone iodine again, contains available iodine 9～12%, is a kind of broad-spectrum powerful disinfectant, and virus, antibacterial, fungus and mycotic spore are all had stronger killing action.Little to skin irritation, toxicity is low, and effect is lasting.Safe in utilization, easy.To organizing basic nonirritant, be used for the sterilization of skin and mucosa, as perform the operation preceding cleaning, operative site and wound disinfection.Its sterilizing mechanisms mainly is by discharging free hydration iodine performance bactericidal action, the polyvidone possess hydrophilic property, it is the carrier that iodine is transported to cell membrane, after complex touches cell wall, the free-iodine that discharges combines with the aminoacid of tropina, make its degeneration, the proteic active group of simultaneous oxidation antibacterial oleo stock and make microorganism dead rapidly.The common working concentration of betagen solution is 0.1%～10%.Existing Acu-Dyne is mainly povidone iodine gel agent, suppository, ointment, solution, content 1%-10% do not wait (Chinese Pharmacopoeia two ones 2005 editions, 823-824).Shao Zhongyi etc. (curative effect of betagen solution treatment tinea pedis is inquired into, Jinggangshan College's journal (natural science), and in March, 2009 is 105-106) with cutaneous fungal infection diseases such as betagen solution treatment tinea pedis.(clinical research of povidone iodine emulsifiable paste treatment tinea pedis, Hebei medical science, 785-786) also disclose the clinical research for the treatment of tinea pedis with the povidone iodine emulsifiable paste in July, 2008 to Shao Yi etc.
It is the medical composite for eye of active component with glucocorticoid and povidone iodine that Chinese patent application CN200780008873.5 discloses a kind of, but in the disclosed compositions of this application, preferred povidone iodine content is 0.5%～2% in this application, 17-hydroxy-11-dehydrocorticosterone content is 0.005%～0.02% technical scheme, but also point out in this application, too high or too low povidone iodine content all can influence with the content of different glucocorticoids and obtain stability of formulation, and Chinese patent application CN200910070061.4 discloses a kind of pharmaceutical composition that adopts povidone iodine and cyclodextrin to comprise glucocorticoid.Show in this application description that the composition stable that adopts 17-hydroxy-11-dehydrocorticosterone micropowder and povidone iodine to make is relatively poor, cause formulation products effect duration weak point, be difficult to satisfy the requirement of producing and using.
Momestasone furoate (CAS:83919-23-7, Mometasone Furoate) is a kind of new external, the nonfluorinated class of the development and production of U.S. Schering Plough company, but contain " potent " glucocorticoid hormone preparation of halogen, at first went on the market in the U.S. in 1987.It has the chlorine atom on 9 and 21 of corticosteroid hormone structure, on 17 (2 ') position a furoate (also can be described as heterocycle) is arranged.Its chemical structural formula is: two chloro-11 β of 9 α-21-, 17 α-two hydroxy-16 alpha--methyl-pregnane-1 ,-diene-3,20-diketone-17 (2 ') furoate.Be widely used in airway disorders such as treatment dermatosis, asthma, allergic rhinitis.
Summary of the invention:
The discovery that we are surprised contains the pharmaceutical composition of micronized momestasone furoate micropowder and povidone iodine, is not using under the situation of cyclodextrin inclusion compound, also can realize stability and curative effect preferably.
The invention provides a kind of upward acceptable topical application pharmaceutical composition that is suitable for the adjuvant of topical application of micronize momestasone furoate, povidone iodine and one or more physiologys that contains.
Described pharmaceutical composition, povidone iodine content are 1%～10% preferred 1%～5%, and momestasone furoate content is 0.01%～0.1%, preferred 0.05%～0.1%.
Part provided by the invention makes pharmaceutical composition can be mixed with ointment, gel, suspensoid, spray etc., and all are applicable to the local preparation that uses.The local adjuvant that uses that is applicable to of described pharmaceutical composition includes but are not limited to one or more in pH regulator agent, antibiotic antiseptic, antioxidant, cosolvent, osmotic pressure regulator, viscosity modifier, surfactant, rheology control agent, oil-phase component, wetting agent, the stabilizing agent, and the water of surplus.
PH regulator agent in the described adjuvant can be enumerated but is not limited only to phosphoric acid and salt, boric acid and salt thereof, citric acid and salt thereof, acetic acid and salt thereof, tartaric acid and salt thereof, hydrochloric acid, sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, tromethane etc.A kind of in preferred hydrochloric acid, sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium bicarbonate, the potassium bicarbonate.
Described osmotic pressure regulator can be enumerated but be not limited only to glycerol, propylene glycol, sodium chloride, potassium chloride, Sorbitol, mannitol etc., preferably adopts the sodium chloride of 0.4%-0.9%.
Described viscosity modifier can be enumerated but be not limited only to sodium carboxymethyl cellulose, hydroxyethyl-cellulose, hydroxypropyl emthylcellulose, hydroxypropyl cellulose, polyvinyl alcohol, carboxy vinyl polymer, polyvinyl pyrrolidone etc., consumption preferred 0.1%～2%.Described viscosity modifier also can be used as suspending agent.
Described wetting agent can be enumerated but be not limited only in glycerol, propylene glycol, sorbitol, preferred glycerol.Described wetting agent consumption preferred 4%～10%, preferred especially 5%.
Described antibiotic antiseptic can include but are not limited to benzoic acid, benzyl alcohol, p-Hydroxybenzoate (nipalgin), comprise in methyl hydroxybenzoate, ethyl hydroxybenzoate, the propylparaben one or more, preferred especially p-Hydroxybenzoate (nipalgin), described antibiotic antiseptic consumption is preferably 0.1%.
The optional non-ionic surface active agent of described surfactant, can enumerate but be not limited only to tween 80, polyoxyethylene hydrogenated Oleum Ricini 60, Polyethylene Glycol-stearate, Macrogol 4000, lecithin, sucrose ester, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene glycol and analog thereof, peregal a-20 poloxamer, tyloxapol, consumption is preferably 0.1%～2%.
The pH of pharmaceutical composition provided by the invention is selected from 5-7.
When part of the present invention makes pharmaceutical composition make gel, described adjuvant contains water and is the carbomer resin as rheology control agent, be preferably carbomer 934 and/or Acritamer 940 and/or Carbopol 941 especially, consumption is 0.1%～1% of a pharmaceutical composition weight, preferred 0.2% to 0.5%.
When part of the present invention makes pharmaceutical composition make ointment, described adjuvant also contains wetting agent, oil-phase component 20%～30%, described wetting agent includes but are not limited to glycerol, propylene glycol, sorbitol, consumption is 1%～15%, preferably glycerine, described oil-phase component comprise one or more in solid in the oil-phase component, consistency modifiers, the emulsifying agent.
Solid in the described oil-phase component includes but are not limited to one or more of stearic acid, paraffin, Cera Flava, higher alcohol, described higher alcohol is the monohydric alcohol of 16～22 carbon atoms, preferred hexadecanol and/or octadecanol, described oil-phase component consumption is 1%～15%.
Described consistency modifiers includes but are not limited to one or more in vaseline, liquid paraffin, the vegetable oil, preferred vaseline and/or liquid Paraffin, and the consumption of described consistency modifiers is 5%～20%.
Described emulsifying agent, include but are not limited to the derivant of soap class emulsifying agent, polyoxyethylene ether, preferably as the glyceryl monostearate of soap class emulsifying agent and/or as the peregal A-20 of polyoxy ether class emulsifying agent, total consumption of described emulsifying agent is 1～18%, preferred soap class emulsifying agent consumption is 0.5%～10%, and polyoxy ether class emulsifying agent consumption is 0.5%～8%.
Described higher alcohol also plays the effect of surfactant simultaneously in emulsifiable paste.Percentage ratio of the present invention is the percentage by weight of relative pharmaceutical composition.
The preferred micropowder of momestasone furoate that the present invention uses changes into the microgranule that micronization becomes D90≤50 μ m.
Described pharmaceutical composition can be prepared in order to following method:
The preparation of momestasone furoate suspension:
Momestasone furoate, water, viscosity modifier are placed container, and stirring or ultrasonic obtains the principal agent suspension;
Get proper amount of water for injection, other adjuvant dissolvings that add recipe quantity stir evenly, and add the povidone iodine dissolving of recipe quantity, mix with the momestasone furoate suspension, add water for injection to recipe quantity, and packing promptly.
When described preparation of pharmaceutical compositions becomes ointment, can prepare in order to following method:
(1) preparation of oil phase
That gets recipe quantity is heated to fusing (60 ℃～90 ℃) as oil-phase component, and (available in case of necessity an amount of organic solvent dissolution stirs while adding to evenly promptly described antibiotic antiseptic.
(2) preparation of emulsifiable paste
The momestasone furoate suspension is heated to 60～90 ℃, the povidone iodine dissolving that adds recipe quantity, the wetting agent that is heated to same temperature is joined in the clathrate aqueous solution, mixing, the oil-phase component that will be heated to 60～90 ℃ again joins in the clathrate aqueous solution, stir while adding evenly to condensation promptly.
When described preparation of pharmaceutical compositions becomes gel, when part of the present invention makes pharmaceutical composition make gel, described adjuvant contains water and is the carbomer resin as rheology control agent, be preferably carbomer 934 and/or Acritamer 940 and/or Carbopol 941 especially, consumption is 0.1%～1% of a pharmaceutical composition weight, preferred 0.2% to 0.5%.
For fear of the degraded of material in the process of pharmaceutical compositions, preferably use noble gas, all solution of helium or nitrogen purge for example, and under atmosphere of inert gases, carry out all steps.
Pharmaceutical composition provided by the invention can be prepared and be called different dosage forms, can be according to " pharmaceutics (the 5th edition) " disclosed prescription and prepared in (Cui Fude, People's Health Publisher, in November, 2005).Described
The invention also discloses the application of described local medicine composition in preparation treatment human or animal's scytitis or infective inflammation disease drug.
The invention also discloses the application of described local medicine composition in preparation treatment human or animal's nosal inflammation or infective inflammation disease drug.All preparations that are applicable to that the part is used such as described ointment, gel, suspensoid, spray both can have been made skin-use preparation, and can prepare again becomes nasal formulations.
The part that provides of inventing makes pharmaceutical composition, by preferred 21 glucocorticoid---momestasone furoates that replace for the chlorine atom, overcome the prejudice that glucocorticoid and Acu-Dyne in the prior art can't stable existences, momestasone furoate micropowder and povidone iodine have not directly been made compound preparation adding under the situation of other stabilizing agents, and the gained stability of formulation is higher, can satisfy the requirement in the Chinese Pharmacopoeia 2005 editions.Can be when the local inflammation that causes be infected in treatment and povidone iodine and glucocorticoid are made compound recipe, when killing the pathogen that causes infection, antiinflammatory action by glucocorticoid, treat the allergy that cause of disease is produced timely and the inflammation that causes, when treatment, can produce synergy, the inflammatory reaction that has caused because of allergy when having avoided the treatment of simple application povidone iodine eliminates slower shortcoming, also overcome the taboo that glucocorticoid can not be applied to the scytitis that fungal infection causes.Often merge especially the reality of the scytitis mistaken diagnosis of the clinical practice of fungal infection and fungal infection and non-infection, when having improved curative effect, enlarged the scope of application, reduced the incidence rate of mistaken diagnosis for the present allergic dermatitis of China.In like manner, Pharmaceutical composition provided by the invention is as nasal formulations the time, not only be applicable to allergic rhinitis, also be applicable to rhinitis, sinusitis that virus, antibacterial or fungal infection produce, compare with Donisolone with simple nose, overcome the use taboo for infectious rhinitis, indication is wider.
The specific embodiment:
The Pharmaceutical composition of preparing among the embodiment provided by the invention is all in 1000g.Employed momestasone furoate is micronized microgranule, adopts fluid energy mill to be crushed to the micropowder that particle diameter is D90≤50 μ m
The preparation of embodiment 1 momestasone furoate aqueous suspension
Momestasone furoate 0.1g polyvinylpyrrolidone 5g povidone iodine 10g
Water for injection is to 1000g
The water preparation: get momestasone furoate, povidone iodine, the polyvinylpyrrolidone of recipe quantity, be dissolved in the 500ml water, stirring or ultrasonic to evenly is added to the prescription water gaging promptly.Momestasone furoate %=0.01%, povidone iodine %=1% is filled to the suspension branch that obtains in the aerosol container and can makes nasal spray
The preparation of embodiment 2 momestasone furoate aqueous suspensions
Momestasone furoate 0.5g polyvinylpyrrolidone 10g povidone iodine 30g
Water for injection is to 1000g
According to the method preparation of embodiment 1, promptly.Momestasone furoate %=0.05%, povidone iodine %=3%
The suspension branch that obtains is filled in the aerosol container can makes nasal spray
The preparation of embodiment 3 momestasone furoate aqueous suspensions
Momestasone furoate 1g polyvinylpyrrolidone 10g povidone iodine 50g
Water for injection is to 1000g
According to the method preparation of embodiment 1, promptly.Momestasone furoate %=0.1%, povidone iodine %=5%
The suspension branch that obtains is filled in the aerosol container can makes nasal spray
The preparation of embodiment 4 momestasone furoate aqueous suspensions
Momestasone furoate 1g polyvinylpyrrolidone 10g povidone iodine 100g
Water for injection is to 1000g
According to the method preparation of embodiment 1, promptly.Momestasone furoate %=0.1%, povidone iodine %=10%
The suspension branch that obtains is filled in the aerosol container can makes nasal spray
Embodiment 5-1 ointment
Povidone iodine 10g, glycerol 50g polyvinylpyrrolidone 10g
Momestasone furoate 1g water for injection is to 1000g
Oil-phase component:
White vaseline 60g octadecanol 30g liquid Paraffin 30g glyceryl monostearate 50g peregal a-2010g
(1) preparation of oil phase
The oil-phase component of getting recipe quantity is heated to 70 ℃, adds to be dissolved in an amount of organic solvent, and the glycerol of getting recipe quantity again is heated to same temperature and slowly joins in the oil phase, stirs while adding to evenly promptly.
(2) preparation of suspension
Get momestasone furoate, povidone iodine, the polyvinylpyrrolidone of recipe quantity, be dissolved in the 500ml water, stirring or ultrasonic to evenly is added to the prescription water gaging promptly.
(3) preparation of emulsifiable paste
Suspension is heated to 65 ℃, and the oil-phase component that is heated to 70 ℃ is joined in the inclusion complex in solution, stir while adding evenly to condensation promptly.Momestasone furoate %=0.1%, povidone iodine %=1%
The preparation of embodiment 5-2 gel
Povidone iodine 10g, glycerol 50ml, carbomer 934 5g
Momestasone furoate 1g water for injection is to 1000g
The carbomer 934 of getting recipe quantity adds glycerol, adding 500ml purified water swelling as gel-type vehicle, slow joining in the gel-type vehicle stirs evenly, momestasone furoate, povidone iodine with recipe quantity is scattered in the suitable quantity of water again, slowly join in the gel-type vehicle and stir evenly, with the sodium hydroxide adjust pH to 5.5 of an amount of 1mol/L, the water of adding surplus promptly.Momestasone furoate %=0.1%, povidone iodine %=1%
The preparation of embodiment 6-1 ointment
Povidone iodine 30g, glycerol 120g polyvinylpyrrolidone 10g
Momestasone furoate 1g water for injection is to 1000g
The prescription of oil phase:
White vaseline 30g octadecanol 120g liquid Paraffin 10g glyceryl monostearate 20g peregal a-2050g
Preparation:
Method according to embodiment 5-1 is mixed with ointment, momestasone furoate %=0.1%, povidone iodine %=3%.
The preparation of embodiment 6-2 gel
Povidone iodine 30g, glycerol 50ml, carbomer 934 10g
Momestasone furoate 1g water for injection is to 1000g
The carbomer 934 of getting recipe quantity adds glycerol, adding 500ml purified water swelling as gel-type vehicle, slow joining in the gel-type vehicle stirs evenly, again with momestasone furoate, the povidone iodine of recipe quantity, be scattered in the suitable quantity of water, slowly join in the gel-type vehicle and stir evenly, with the sodium hydroxide adjust pH to 5.5 of an amount of 1mol/L, the water of adding surplus promptly.Momestasone furoate %=0.1%, povidone iodine %=3%.
The preparation of embodiment 7-1 ointment
Povidone iodine 50g, glycerol 100g
Momestasone furoate 1g water for injection is to 1000g
The prescription of oil phase:
White vaseline 90g octadecanol 60g liquid Paraffin 60g glyceryl monostearate 10g peregal a-2030g
Preparation:
Method according to embodiment 5 is mixed with ointment, momestasone furoate %=0.1%, povidone iodine %=5%
The preparation of embodiment 7-2 gel
Povidone iodine 50g, glycerol 50ml, carbomer 934 7g
Momestasone furoate 1g water for injection is to 1000g
The carbomer 934 of getting recipe quantity adds glycerol, adding 500ml purified water swelling as gel-type vehicle, slow joining in the gel-type vehicle stirs evenly, momestasone furoate, povidone iodine with recipe quantity is scattered in the suitable quantity of water again, slowly join in the gel-type vehicle and stir evenly, with the sodium hydroxide adjust pH to 5.5 of an amount of 1mol/L, the water of adding surplus promptly.Momestasone furoate %=0.1%, povidone iodine %=5%.
The preparation of embodiment 8-1, ointment
Povidone iodine 80g, glycerol 100g
Momestasone furoate 1g water for injection is to 1000g
The prescription of oil phase:
White vaseline 90g octadecanol 60g liquid Paraffin 60g glyceryl monostearate 10g peregal a-20 30g
Method according to embodiment 5 is mixed with ointment, momestasone furoate %=0.1%, povidone iodine %=8%
Embodiment 8-2 gel
Povidone iodine 80g, glycerol 50ml, carbomer 934 10g
Momestasone furoate 1g water for injection is to 1000g
The carbomer 934 of getting recipe quantity adds glycerol, adding 500ml purified water swelling as gel-type vehicle, slow joining in the gel-type vehicle stirs evenly, momestasone furoate, povidone iodine with recipe quantity is scattered in the suitable quantity of water again, slowly join in the gel-type vehicle and stir evenly, with the sodium hydroxide adjust pH to 5.5 of an amount of 1mol/L, the water of adding surplus promptly.Momestasone furoate %=0.1%, povidone iodine %=8%
Embodiment 9-1 ointment
Povidone iodine 100g, glycerol 100g
Momestasone furoate 1g water for injection is to 1000g
The prescription of oil phase:
White vaseline 90g octadecanol 60g liquid Paraffin 60g glyceryl monostearate 10g peregal a-2030g
Preparation:
(1) preparation of oil phase
The oil-phase component of getting recipe quantity is heated to 70 ℃, and the glycerol of getting recipe quantity again is heated to same temperature and slowly joins in the oil phase, stirs while adding to evenly promptly.
(2) preparation of emulsifiable paste
Inclusion complex in solution is heated to 65 ℃, the oil-phase component that is heated to 70 ℃ is joined in the inclusion complex in solution, stir while adding evenly to condensation promptly.
Embodiment 9-2 gel
Povidone iodine 100g, glycerol 50ml, carbomer 934 10g
Momestasone furoate 1g water for injection is to 1000g
The carbomer 934 of getting recipe quantity adds glycerol, adding 500ml purified water swelling as gel-type vehicle, slow joining in the gel-type vehicle stirs evenly, momestasone furoate, povidone iodine with recipe quantity is scattered in the suitable quantity of water again, slowly join in the gel-type vehicle and stir evenly, with the sodium hydroxide adjust pH to 5.5 of an amount of 1mol/L, the water of adding surplus promptly.
Embodiment 10 povidone iodine stability experiments
The preparation of experiment medicine: the pharmaceutical composition that embodiment 1-4 is made is sub-packed in respectively in the 10ml solution bottle.The compositions that embodiment 9-1 and 9-2 are made is divided respectively and is filled in the 10g PAP.
The experiment medicine is grouped as follows:
Embodiment number 1 2 3 4 9-1 9-2
Packet number 1 2 3 4 5 6
PI％ 1 3 5 10 10 10
Experimental technique: get 15 experiment medicines,, carry out stability test under the situation of relative humidity 75% ± 5% for every group at 40 ℃ ± 2 ℃.Survey content of iodine respectively at storage time sampling in 0 month, 1 month, 3 months, get 5 at every turn.The employing titrimetry is measured, and every medicine to be measured is got 5g move in the 125ml beaker, adds the 1% starch indicator solution of 1ml, to blue complete obiteration, determines used sodium thiosulfate volume with this solution of 0.001N sodium thiosulfate solution titrated.
Titratable iodine (mg)=V (ml consumes the volumetric solution volume) * 5.076 (mg/ml)/2
The titratable iodine number that calculates see the following form (x ± s, n=5):
The experiment group number 1 2 3 4 5 6
0 month/mg 4.92±0.41 14.5±2.1 25.0±1.8 48.2±1.9 48.2±1.9 48.2±1.9
1 month/mg 4.85±0.50 14.2±1.1 24.5±2.1 47.5±2.2 47.5±2.2 47.5±2.2
3 months/mg 4.75±0.49 13.5±1.0 23.6±2.3 45.8±2.1 45.8±2.1 45.8±2.1
Reduce % 3.5 4.9 5.6 5.0 4.6 5.0
Simultaneously, adopting HPLC to survey the changes of contents of each experimental group 17-hydroxy-11-dehydrocorticosterone, is 100% with initial content.
The variation of experimental group 1～6 17-hydroxy-11-dehydrocorticosterone content sees the following form: (x ± s, n=5),
The experiment group number 1(％) 2(％) 3(％) 4(％) 5(％) 6(％)
1 month 98.2±0.53 98.5±0.48 98.3±0.51 98.6±0.46 98.1±0.58 98.2±0.48
3 months 96.3±0.43 96.2±0.51 96.2±0.46 94.7±0.49 94.9±0.42 94.3±0.53
Reduce % 3.7 3.8 3.8 5.3 5.1 5.7
Stability experiment shows that the preparation active constituent content that provides in the embodiment of the invention descends and all is no more than 10% in experiment periods, meet the requirement in the Chinese Pharmacopoeia 2005 editions.Can satisfy and produce and the needs that store.
The therapeutic effect of the allergic skin inflammation that 14 pairs of Cavia porcellus fungal infection of embodiment cause
Laboratory animal: albino guinea-pig, one-level, male and female half and half, body weight 200-250g plant in Britain
Fungal infection: alpha fungus (bacterium T 5cT.men-tagrophyte, trichophyton), provide by China Committee for Culture Collection of Microorganisms medical mycology center, recover its pathogenicity before the experiment and be inoculated in husky fort agar (Sabrouraud dextrose agarSDA) slant tube, 26 ℃ of cultivations are carefully scraped behind the 10d and are got bacterium colony, make with normal saline to contain spore count 10 5/ ml suspension
Get Cavia porcellus, electricity consumption pushes away one side depilation 3cm * 8cm area at its back, behind the 24h, with the broken depilation face of aseptic fine sandpaper sassafras central authorities skin, with slight oozing of blood degree of being, causing area is 2cm * 6cm rectangle wound face, on wound face, evenly inoculate above-mentioned bacterial strains suspension, every 1cm again 2Inoculation 1ml.Room temperature keeps 30 ℃, behind the 10d animal inoculation fungus go out skin occur erythra, squama or or crust, scrape bark fetching rash, squama or crust microscopy and can see alpha fungus mycelia and spore., represent lesion degree with " 0,1,2,3,4 " classification, criterion is: the no skin lesion of expression in 0 fen, 1 is divided into the point-like erythema, is divided into the gamut erythema, and 3 are divided into redness, squama, and 4 are divided into erythema, the incrustation that overruns.Getting scoring is that Cavia porcellus more than 3 minutes is divided into 5 groups at random, and 10 every group, administration and grouping see the following form:
Numbering Administration
Experimental group 1 Embodiment 7-1 makes ointment, momestasone furoate content 0.1%, PI%=5%
Experimental group 2 Embodiment 7-2 makes gel, momestasone furoate content 0.1%, PI%=5%
Matched group 1 Commercially available momestasone furoate emulsifiable paste, content 0.1%
Matched group 2 Commercially available povidone iodine emulsifiable paste, content 5%
Matched group 3 Positive controls adopts normal saline
Experimental technique, each experimental group is administered once every day, evenly smears the experiment medicine in the laboratory animal affected part once at every turn, and it is identical that each organizes each administration emulsifiable paste amount, and 3d, 7d after administration mark to the laboratory animal affected part respectively:
Figure G2009102287861D00091
From experimental data as can be seen, the experimental group 1-2 of employing embodiment of the invention pharmaceutical composition compares with matched group 1-2 behind treatment 7d all significant curative effect, not only have 70～80% laboratory animal skin lesion to be completely recovered, and all laboratory animals are all negative through fungal culture.
Adopt matched group 1 laboratory animal skin lesion when continuing medication of glucocorticoid emulsifiable paste not only not alleviate to 7d, also increase the weight of to some extent than the matched group 6 that adopts normal saline on the contrary, illustrate that using glucocorticoid merely is unaccommodated for treatment of fungal infections owing to there is the local immunity inhibitory action.
For the matched group 6 that adopts 5% povidone iodine emulsifiable paste, though produced certain curative effect, still have 70% laboratory animal still to have skin lesion, and fungal culture shows that all laboratory animals are all negative, because fungal infection has caused the allergy of skin, the scytitis of generation is also not exclusively eliminated along with the disappearance of infecting in the scytitis of fungal infection in explanation.

Claims (10)

1. a topical application pharmaceutical composition that contains furoyl mometasone and povidone iodine contains one or more physiologys and goes up the acceptable adjuvant that is suitable for topical application, it is characterized in that described momestasone furoate is micronized microgranule.
2. pharmaceutical composition as claimed in claim 1 is characterized in that described povidone iodine content is 1%～10%, and momestasone furoate content is 0.01%～0.1%.
3. pharmaceutical composition as claimed in claim 2 is characterized in that described povidone iodine content is preferably 1%～5%.
4. as claim 2 or 3 described pharmaceutical compositions, it is characterized in that described momestasone furoate content is 0.05%～0.1%.
5. as arbitrary described pharmaceutical composition in the claim 1 to 4, described pharmaceutical composition can ointment, gel, suspendible liquor, spray.
6. as arbitrary described pharmaceutical composition in the claim 1 to 5, the described adjuvant that is applicable to topical application includes but are not limited to one or more in pH regulator agent, antioxidant, cosolvent, osmotic pressure regulator, viscosity modifier, surfactant, rheology control agent, the stabilizing agent, and the water of surplus.
7. as the arbitrary described pharmaceutical composition of claim 1-15, when it is characterized in that described compositions is gel, also comprise rheology control agent, described rheology control agent is the carbomer resin.
8. pharmaceutical composition as claimed in claim 16 is characterized in that described carbomer resin is carbomer 934 and/or Acritamer 940 and/or Carbopol 941, and consumption is 0.1%～1% of a pharmaceutical composition weight.
9. as arbitrary described Pharmaceutical composition in the claim 1 to 19, the application in preparation human or animal nosal inflammation medicine.
10. as arbitrary described Pharmaceutical composition in the claim 1 to 19, the application in preparation human or animal skin inflammation medicine.
CN2009102287861A 2009-11-26 2009-11-26 Topically applied composition containing povidone iodine and mometasone furoate Pending CN102078326A (en)

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102319202A (en) * 2011-09-30 2012-01-18 江西三九药业有限公司 Mometasone furoate gel and preparation method thereof
CN102448496A (en) * 2011-06-22 2012-05-09 江苏德达医药科技有限公司 Pharmaceutical composition containing iodine and steroid and its use for treating rhinitis diseases
CN102949723A (en) * 2011-11-30 2013-03-06 天津金耀集团有限公司 Medicinal composition containing glucocorticoid and NOS (Nitric Oxide Synthase) inhibitor for treating skin inflammation
CN103127137A (en) * 2011-11-30 2013-06-05 天津金耀集团有限公司 Medicine combination with hydrocortisone butyrate and nitric oxide synthase (NOS) inhibitor and for treating skin inflammation
CN103127136A (en) * 2011-11-30 2013-06-05 天津金耀集团有限公司 Skin drug composition containing methylprednisolone aceponate and amino acid
CN111787954A (en) * 2018-02-23 2020-10-16 格兰马克专业公司 Treatment of allergic rhinitis in pediatric subjects using a combination of mometasone and olopatadine
CN112773808A (en) * 2013-10-04 2021-05-11 格兰马克专业公司 Treatment of allergic rhinitis using a combination of mometasone and olopatadine

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102448496A (en) * 2011-06-22 2012-05-09 江苏德达医药科技有限公司 Pharmaceutical composition containing iodine and steroid and its use for treating rhinitis diseases
CN102448496B (en) * 2011-06-22 2015-04-15 江苏德达医药科技有限公司 Medicine composition having iodine and steroid and application to treatment of rhinitis
CN102319202A (en) * 2011-09-30 2012-01-18 江西三九药业有限公司 Mometasone furoate gel and preparation method thereof
CN102949723A (en) * 2011-11-30 2013-03-06 天津金耀集团有限公司 Medicinal composition containing glucocorticoid and NOS (Nitric Oxide Synthase) inhibitor for treating skin inflammation
CN103127137A (en) * 2011-11-30 2013-06-05 天津金耀集团有限公司 Medicine combination with hydrocortisone butyrate and nitric oxide synthase (NOS) inhibitor and for treating skin inflammation
CN103127136A (en) * 2011-11-30 2013-06-05 天津金耀集团有限公司 Skin drug composition containing methylprednisolone aceponate and amino acid
CN112773808A (en) * 2013-10-04 2021-05-11 格兰马克专业公司 Treatment of allergic rhinitis using a combination of mometasone and olopatadine
CN111787954A (en) * 2018-02-23 2020-10-16 格兰马克专业公司 Treatment of allergic rhinitis in pediatric subjects using a combination of mometasone and olopatadine
CN111787954B (en) * 2018-02-23 2023-09-05 格兰马克专业公司 Treatment of allergic rhinitis in pediatric subjects with a combination of mometasone and olopatadine

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