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MLE (multi lamellar emulsion), made from the synthetic ceramide PC-9, which is similar to natural ceramides, is an exact recreation of intercellular lipid layers. MLE is a drug delivery system that, upon application, enters stratum corneum with ease, reinforces skin barrier function, releases the drug over a reasonable amount of time by staying in the epidermis, and thereby increases the drug’s effectiveness and reduces the side effects.
Inflammatory skin condition
Atopic dermatitis
Contact dermatitis
Seborrheic dermatitis
local corticosteroids
Increasedanti-inflammatory effects
Improved release of chemicalagents from the stratum corneum
Prevention of damage in skin barrier Increased production of AMPs
Increased production ofanti-microbial peptide(AMPs)
Increased treatmenteffects of steroids
Prevention ofsecondary infection
Anti-inflammation
Reduction in intercellular lipidsin dead skin cells
Reduction in AMPs production
Increase in infections
Damages in the skin barrier
Increase in inflammation
Treatment effect of local corticosteroids Side effects of local corticosteroids regarding skin conditions and skinbarrier function
Sheu HM, et al., British J Dermatol 1997; 136:884-890Kao JS, et al., J Invest Dermatol 2003; 120:4456-464
MometasoneMLE
In the case of corticosteroids, an increase in effectiveness inevitably results in an increase in side
effects. Thus minimizing side effects can be called an underlying goal of cosmetic corticosteroids.
Stratum corneum, the outermost layer of the skin, is in charge of protecting the skin from harmful
factors and plays a vital role in maintaining an adequate level of moisture. Stratum corneum is
composed of corneous cells and intercellular lipids, which act as the skin barrier.
Side effects have been reduced once more due to the combination
of mometasone, a safe steroid whose side effects were already
minimized, and MLE technology.Dermotasone
Synthesis inhibition of lipidsin the corium derma
allergen allergen various bacteria various bacteria
stra
tum
cor
neum
epid
erm
isde
rma
moisture
epid
erm
isde
rma
moisture
allergen various bacteria
epid
erm
isde
rma
moisture
<Atopic/sensitive skin with damaged skin barrier> <Absorption of MLE by damaged skin barrier> <Healthy skin restored by MLE>
▶Test subjects
Species: Hairless mouse (hairless mice are widely used in animal testing because their skin structure is very similar to
that of human skin)
▶Procedure
a. Day 0- After their TEWL, hydration and thickness are measured, they are grouped according to their TEWL values.
b. After grouping, the drug is applied to them at 9:00AM and at 17:00PM.
c. The steps above are repeated until the morning of day 2.
d. Day 3 - Their TEWL, hydration and thickness are measured again.
Estimating TEWL (Transepidermal Water Loss)▶TEWL amount: A measure of the amount of moisture evaporated from the skin excluding the amount caused by sweating.
Indicates epidermal permeability barrier function.
▶Most commonly used method to measure skin barrier function
▶The normal range for TEWL is between 0.1~0.4mg/m2. It is proportionate to the amount of damage to epidermal permeability
barrier caused by damages to the stratum corneum.
▶Measuring apparatus: TEWameter TM 300 (Courage & Khazaka, Cologne, Germany)
Measuring the moisture level in the stratum corneum▶Measuring the level of moisture in the stratum corneum using the skin capacitance
▶Measuring apparatus: Corneometer CM 820 (Courage & Khazaka, Cologne, Germany)
Testing procedure
Estimation of level of skin barrier damage
Measuring the moisture level
Normal MLE CreamMLE Lotion Existing CreamExisting Lotion
Normal MLE CreamMLE Lotion Existing CreamExisting Lotion
20
15
10
5
03 Day
80
75
70
65
60
553 Day
Contains similar ceramide for patients of age 4 and above with eczematous skin conditions. A manifold for evaluating Mometasone MLE Creamʼs effectiveness of treatment and skin barrier function, double blind test, anda comparative clinical study with Methylprednisolone aceponate 0.1%
Primary effectiveness Evaluation results: PGA treatment success rate
Primary Effectiveness Evaluation Variable: PGA Treatment Success Rate
Primary effectiveness evaluation (PGA) results show that Dermotasone MLE Cream statistically superior to its competition
PGA Effectiveness Rating: (# of Patients considered fully recovered or
improved by PGA standards / Total # of Patients) X 100(%)
▶ Patients: 175 individuals aged 4 and above with symmetrical eczema lesion
▶ Product: Dermotasone MLE Cream
▶ Product compared: Methylprednisolone aceponate 0.1%
▶ Treatment period: At most 2 weeks
▶ Effectiveness evaluation variable
Primary effectiveness evaluation variable: PGA improvement factor
Secondary effectiveness evaluation variable: transepidermal water loss, itch VAS improvement factor
▶ Clinical study site: Myung-Ji Hospital, Yonsei University Hospital, Seoul University Hospital, Gangnam Sungshim Hospital, Incheon Sungmo Hospital
▶ Duration: 11/19/2009, 6/15/2010
Day 15 Full recovery
Improvement
Protection
Stability
Worsening
Total
Effective 1)
90% C.I.2)
1) Full recovery or Improvement
2) 90% confidence interval for difference between two groups computed from matched-pairs table
72(45.28%)
47(29.56%)
28(17.61%)
12(7.55%)
-
159(100.0%)
119(74.84%)
(20.08%, 34.01%)
DermotasoneMLE
(N=159)
Methylprednisoloneaceponate 0.1%
(N=159)
Methylprednisoloneaceponate 0.1%
(N=165)
PP ITT=LOCF
DermotasoneMLE
(N=165)
72(43.64%)
47(28.48%)
31(18.79%)
15(9.09%)
-
165(100.0%)
119(72.12%)
(19.31%, 32.81%)
28(17.61%)
48(30.19%)
61(38.36%)
22(13.84%)
-
159(100.0%)
76(47.80%)
28(16.97%)
48(29.09%)
63(38.18%)
25(15.15%)
-
1(0.61%)
165(100.0%)
76(46.06%)
Methylprednisoloneaceponate 0.1%
Dermotasone MLE 100
80
60
40
20
0Day 4 Day 8 Day 15
ResearchSubject
PGA Improvement Factor : treatment success rate of
the overall evaluation of the patient’s clinical response upon completion
of clinical study
PGA Evaluation: After rating the patient on scaling, erythema,
vesiculation, pruritus, and burning/pain each on a scale of 0 through 2,
the five ratings are added up to produce a final sum. (0: No symptoms,
1: Mild, 2: Medium, 3: Severe)
Evaluation Results and Standards• Full Recovery: Symptom Improvement 100%
• Improvement: Symptom Improvement over 75%
• Protection: Symptom Improvement over 50%
• Stability: Symptom Improvement below 50%
• Worsening: Symptom Worsening
Study Design
Secondary Effectiveness Evaluation Variable: TEWL
Secondary Effectiveness Evaluation Variable: VAS Improvement Factor
Results of TEWL measurements.
After four days of using Dermotasone MLE, the experimental group showed a statistically significant improvement when
compared to the control group.
Results of VAS measurements
After two weeks of using Dermatasone MLE, the experimental group showed a statistically significant improvement when
compared to the control group.
Multi-component clinical testing of eczema patients four years or older - Dermotasone MLE, the experimental drug, when compared to the Reference drug,
Mometasone furoate in MLE (Dermotasone MLETM) in Eczema Treatment
- displayed statistically significant superiority in the primary effectiveness evaluation variable PGA improvement rate,
- and displayed statistically significant superiority in the secondary effectiveness evaluation variables TEWL and VAS.
- No adverse drug reactions or other serious reactions resulted from either the experimental drug or the control drug.
Dermotasone MLE cream showed statistically significant effectiveness results in treating eczema. No unusual adverse drug reactions were found besides the ones that exist in the Reference drug and other existing external steroid medications.
Methylprednisoloneaceponate 0.1%
Dermotasone MLE 100
80
60
40
20
0
(%)
Day 4
TEWL Improvement Factor of Per Protocol group
VAS Improvement Factor of Per Protocol group
Day 8 Day 15
17.12%
16.02%
23.63%32.74%
29.86%
48.30%
P-value=0.0070
P-value=0.0001
P-value=0.0001
Methylprednisoloneaceponate 0.1%
Dermotasone MLE 100
80
60
40
20
0
(%)
Day 4 Day 8 Day 15
40.56%
37.46%
61.22%
75.41%65.38%
83.28%
P-value=0.0001
Trans-epidermal water loss: TEWL- Measure TEWL with TEWameter
- Improvement Factor (%) = [(TEWLday1-TEWL각 visit)/TEWLday1]X100(%)
Itch Scale (VAS)- The change in itchiness in the test subject between the baseline
and the end of the test.
- Improvement Factor (%) = [(VASday1-VAS각 visit)/VASday1]X100(%)
Test ResultSummary
✽✽
✽✽
✽✽
✽✽
Dermotasone cream once a day VSFluocinolone acetonide 0.025%Three times a day
Dermotasone cream once a day VSTriamcinolone acetonide 0.1% Twice a day
No. of patientstreated(evaluated)
Treatment outcomedecrease in total sign andsymptom severity score(%)
Treatment X Duration(wk)
In children(aged between 6mo and 12y)
r, db, pg
nb
r, db
r, nb
21
5
5
5
24
24
5
11
10
12
12
Studydesign
Duration(days)
No. ofsubjects
Effect on serumcortisol levels
MOM
HYDV
MOM
CLO
MOM
HYD
0.1% cr od X≤ 3
0.2% cr bid X≤ 3
0.1% cr od X 3
0.05% cr bid X 3
0.1% cr od X ≤ 6
1.0% cr bid X ≤ 6
111
112
30(30)
30(30)
24(23)
24(19)
87.2
78.6
86.1
66.1
95
75
bid=twice daily; CLO=clobetasone; cr=cream; HYD=hydrocortisone; HYDV=hydrocortisone valerate; MOM=mometasone; od=once daily; p≤0.001 vs comparator
< STUDY 1 > < STUDY 2 >
< STUDY 1 >
< STUDY 2 >
Decr
ease
in to
tal s
ign
and
sym
ptom
sco
re(%
)
Duration of treatment (days)
MOM(n=109)
FLU(n=109)
**P<0.001 vs comparator
MOM 0.1% ung od 15g/day
HYDB 1.0% ung od 15g/day
MOM 0.1% ung 10g/day(20h/day)a
MOM 0.1% ung 30g/day(22h/day)a
MPA 0.1% ung 30g/day(22h/day)a
MOM 0.1% cr 16g/day(11h/day)a
HYDB 0.1% cr 16g/day(11h/day)a
MOM ≡ HYDB
No effect on serum cortisol levels
MOM ≡ MPA
MOM > HYDB
a:Application under airtight occlusion.cr=cream; db=double-blind; HYDB=hydrocortisone butyrate; MOM=mometasone; MPA=methylprednisolone aceponate; nb=nonblind; od=once daily; pg=parallel group; r=randomised; ung=ointment; ≡indicates similar effect; > indicates significantly greater effect.
Treatment
▶ Atopic dermatitis
▶ Psoriasis vulgaris
▶ The Impact of Momerasone on HPA Axis
60
50
40
30
20
10
4 8 15 22
Duration of treatment (days)
MOM(n=66)
TRI(n=66)60
50
40
30
20
10
4 8 15 22
Potent
Safe
Active Ingredient/Dose
Appearance
Effect
Directions
Storage
Packing Unit
Drug Information
Dongkoo products Guide to potencies of topical corticosteroids
Group Generic Name Brand Name
In 1g, Mometasone Furoate --- 1mg
Cream - Complete uniform white cream
Lotion - White or light brown lotion
Alleviation of itch and inflammation from skin conditions in reaction to corticoids
Directions: Once daily, apply small amount to affected area and lightly rub until it fully permeates.
Refrain from putting bandages on the area.
Storage: Airtight container, 1~30°C
cream-15g, 30g, 500g
lotion-30g
1) Drugs. 1998 Jan; 55(1): 145-632) Australas J Dermatol. 1991; 32(2): 85-913) J Am Acad Dermatol. 1991 Apr; 24(4): 603-74) Cutis 1988 Nov; 42(5): 480-5, 1996 Feb;57:13-185) N Z Med J. 1993 May 26; 106(956): 203-56) J Int Med Res. 1990 Nov-Dec; 18(6): 460-77) Today's Therapeutic Trends 1988; 5: 25-35, 1990;8(3):21-348) Drug Saf 1994; 10(5): 406-129) Br J Dermatol 1982; 107 Suppl. 23: 24-910) J Steroid Biochem Mol Biol 1993 Feb; 44: 141-511) Skin Pharmacol 1993; 6(3): 187-9212) J Am Acad Dermatol 1993 Oct: 29: 576-8013) Today's Ther Trends 1988; 5(4): 25-3514) Eur J Clin Pharmacol 1995; 48(2): 123-5
15) Skin Res 1990; 32(3): 395-40216) Dermatol Venereol 1993; 2(3): 225-3017) Int J Clin Pharmacol Ther 1995 Apr: 33: 187-918) Int J Dermatol 1989 Jun: 28: 342-419) Z Hautkr 1991; 66(9): 785-720) Br J Dermatol 1995 Jan: 132: 66-821) Schering-Plough Corporation Limited. data on file, November 199722) Proceedings of the 55th Annual Meeting of the American Academy of Dermatology: 1997 Mar 21-26:San Francisco23) Poster presentation in the 19th World Congress of Dermatology, Sydney, Australia, Jun 15-20, 199724) Curr Ther Res 1990 Jul; 48: 128-3925) Am J Clin Dermatol 2002; 3 (1): 47-58
Ref.)
Ultra Ⅰ
Ⅱ
Ⅲ
High
Medium
Mild
Low
Very Low
Ⅳ
Ⅴ
Ⅵ
Ⅶ
Clobetasol propionate 0.05% ointment, solution
Fluocinonide 0.05% cream
Desoximetasone 0.05% gel
Diflucortolone Valerate 0.3%* ointment
Fluticasone Propionate 0.005% ointment
Mometasone furoate 0.1% cream, lotion
Prednicarbate 0.1% ointment
Clobetasone butyrate 0.05% ointment
Prednicarbate 0.25% lotion
Betamethasone Valerate 0.1% cream
Fluticasone Propionate 0.05% cream
Triamcinolone acetonide 0.1% cream
Prednisolone valeroacetate 0.3% cream, lotion
Clobetasone butyrate 0.05% cream
Desonide 0.05% cream, lotion
Alclometasone dipropionate 0.05% cream
Hydrocortisone 1%
Hydrocortisone 2.5%
Domo-horn Solution/Ointment/Cream
Dermotasone MLE Cream/Lotion
Bade Cream
Dongkoo Dermo Lotion
Cordicare Lotion
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