ADAPALENE

Product Description

DayaramPharma Chem also providing Micronized form of Adapalene API and Dayaram PharmaChem is leading manufacturer and exporter of Adapalene API.

DayaramPharma Chem Group Company Niksan Healthcare also manufacturing adapalene gel, adapaleneointment and adapalene cream. So, NIKSAN GROUP manufacturing both API as wellas formulation of ADAPALENE.

DayaramPharma Chem is manufacturing and exporting ADAPALENE from last many year incountry like Brazil, Egypt, Singapore, Jordan, Lebanon, Israel, Vietnam,Bangladesh, Paraguay, Argentina, Dominican Republic, Sudan, Hong Kong,Seychelles, Algeria, Iran, Chile, South Korea, United Kingdom, Australia,Greece, Austria, Serbia,  New Zealand,Sweden, Hungary, Mauritius, Vanuatu, Malta, Kazakistan, Slovenia, Bolivia,Japan, Uganda, Bulgaria, Lithuania, Poland, Sri Lanka, Romania, Uruguay,Russia, Thailand, Afghanistan, Latvia, Lithuania, United Arab Emirates,Seychelles, Peru, Switzerland, Tunisia, France, Australia, Hungary, Finland,Turkey, Pakistan, Rwanda, South Africa, Denmark, Malawi, Croatia, Slovenia,Ireland, Zambia, Cyprus, Nigeria, Uzbekistan, Cameroon, Netherlands, Azarbaijan, Venezuela, Morocco, CoteD Ivoire, St Lucia, South Korea, Congo, Philippines, Colombia, Burkina Faso,Sudan, Guinea , Djibouti, Netherlands, Nigeria and Germany.

Synonyms: 6-(3-(1-Adamantyl)-4-methoxyphenyl)-2-naphthoicacid, Adapalene,Adapaleno, Adapalenum.

IUPAC Name: 6-[3-(adamantan-1-yl)-4-methoxyphenyl]naphthalene-2-carboxylicacid

Storage of  Adapalene

Keep allmedicines out of the reach and sight of children.

Store in acool, dry place, away from direct heat and light.

What is Acne?

Acne is the common cause of skin. People between aged 12-25 aremainly affected with acne, but in some case older and younger people areaffected with acne. Small sebaceous glands lie under our soft skin surface andproduce oil (sebum) that keeps our skin pliantand soft. Tiny pores in our skin allow the sebum to come onto the surface of our skin. In acne, some of these pores become blocked,causing small pimples, blackheads and whiteheads.

Application of Adapalene

Applying adapalene to the areas of our skin with acne will help tounblock pores. It also has some effect on reducing inflammation of skin. It isused in acne to help to unblock pores and to treat blackheads or whiteheads andmildly inflamed spots. It is suitable for use on the face, back and chest.

Adapalene is generallyuse for topical treatment of comedo, papular andpustular acne (acne vulgaris) of the face, chest or back.

Side effect:

The most common side effect of adapalene is dry, red, or scaly skin.Also some adapalene user compliance about feeling ofwarmth and mild stinging or burning or peeling skin or skin pain.

Pharmacodynamics:

Adapalene is a chemically stablecompound. Biochemical and pharmacological profile studies have demonstratedthat adapalene is a modulator of cellular differentiation, keratinization &inflammatory processes all of which represent important features in thepathology of acne vulgaris of the face, chest or back.

Mechanism of action:

Adapalene binds to specific retinoicacid nuclear receptors (gamma and beta receptors) and retinoid X receptors butdoes not bind to the cytosolic receptor protein. Although the exact mode ofaction of adapalene is unknown, it is suggested that topical adapalene maynormalize the differentiation of follicular epithelial cells resulting indecreased microcomedone formation.

Absorption:

Adapalene displays a limited absorptionpotential across the human skin. Only trace amounts (<0.25 ng/ml) of parentsubstance have been found in the plasma of acne patients following chronictopical application of adapalene in controlled clinical trials

Metabolism:

Metabolized mainly by O-demethylation,hydroxylation and conjugation, and excretion is primarily by the biliary route.

Toxicity:
The acute oral toxicity ofadapalene in mice and rats is greater than 10 mL/kg. Chronic ingestion of thedrug may lead to the same side effects as those associated with excessive oralintake of Vitamin A.

CDSCO Approval: Adapalene formulation is approved inIndia by CDSCO in 15.03.2001 Adapalene 0.1% w/w and in 01.05.2003 Adapalene +clindamycin gel and in 31.10.2008 Adapalene 0.1% + Benzoyl Peroxide 2.5% gel.

Formulation in Market:

Adapalene have compatibility with other APIlike clindamycinphosphate and benzoyl peroxide, as itfound in combination formulation in Indian markets are as follow.

Adapalene 1%W/W

Adapalene 0.1% w/w gel

Adapalene 0.3% w/w gel

Adapalene 0.1% w/w + Clindamycin 1% w/w gel

Adapalene 0.1% + Benzoyl Peroxide 2.5% gel

Adapalene0.10 %w/w+Dapsone 5 %w/w

Adapalene0.02 %W/w+Azithromycin 2 %w/w

Adapalene0.1 %w/v+Allantoin 1 %w/w+Clindamycin 1 %w/w

Adapalene0.1 %w/w+Benzoyl peroxide 2.5 %w/w

Reference:

Graziano Castaldi, Pietro Allegrini, Gabriele Razzetti, Mauro Ercoli,"Process for the preparation of adapalene." U.S. PatentUS20060229465, issued October 12, 2006.

US20060229465

Bergfeld WF. The evolving role of retinoids in the management ofcutaneous conditions. Clinician. 1998;16:1–32. [Google Scholar]

Thiboutot DM,Shalita AR, Yamauchi PS, et al. Combination therapy with adapalene gel 0.1% anddoxycycline for severe acne vulgaris: a multicenter, investigator-blind,randomized, controlled study. Skinmed. 2005;4:138–46. [PubMed] [GoogleScholar]

Zhang JZ, LiLF, Tu YT, et al. A successful maintenance approach in inflammatory acne withadapalane gel 0.1% after an initial treatment in combination with clindamycintopical solution 1% or after monotherapy with clindamycin topical solution1% J DermatolTreat. 2004;15:372–8. [PubMed] [GoogleScholar]