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 The leading web portal for pharmacy resources, news, education and careers October 23, 2017
Pharmacy Choice - Pharmaceutical News - Patent Issued for Method for Treatment of Acne Using Pharmaceutical Compositions of Clindamycin and Adapalene (USPTO 9636353) - October 23, 2017

Pharmacy News Article

 5/19/17 - Patent Issued for Method for Treatment of Acne Using Pharmaceutical Compositions of Clindamycin and Adapalene (USPTO 9636353)

By a News Reporter-Staff News Editor at Drug Week From Alexandria, Virginia, NewsRx journalists report that a patent by the inventors Mittal, Ravindra (Gujarat, IN); Roy, Sunilendu Bhushan (Gujarat, IN); Kothari, Jay Shantilal (Gujarat, IN); Sheikh, Shafiq (Gujarat, IN); Patel, Jitendra Dasharathlal (Gujarat, IN); Pancholi, Jinesh Suresh (Gujarat, IN), filed on October 19, 2011, was published online on May 2, 2017 (see also Cadila Healthcare Limited).

The patent's assignee for patent number 9636353 is Cadila Healthcare Limited (Ahmedabad, IN).

News editors obtained the following quote from the background information supplied by the inventors: "Acne vulgaris is a skin condition that affects over 85% of all people. Acne is a term for a medical condition of plugged pores typically occurring on the face, neck, and upper torso. Following are four primary factors that lead to the formation of acne vulgaris; (1) increased sebum output resulting in oily, greasy skin; (2) increased bacterial activity normally due to an overabundance of Propionibacterium acnes bacteria; (3) plugging (hypercornification) of the follicle or pilosebaceous duct; and (4) production of inflammation by substances leaking into the dermis which cause inflammatory reactions. The plugged pores result in blackheads, whiteheads, pimples or deeper lumps such as cysts or nodules. Severe cases of acne can result in permanent scarring or disfiguring.

"Acne occurs when the oil glands of the skin called sebaceous glands produce an increased amount of oil. The sebaceous glands are connected to canals in the skin called hair follicles that terminate in openings in the skin called pores. The increased amount of oil secreted by the sebaceous glands is caused by an increase in androgen hormones in both males and females during adolescence or puberty. Accompanying the increase in the amount of oil secreted by the sebaceous glands is an increase in the shedding of the skin lining the hair follicles. The increase in the amount of secreted oil in combination with the increase in the shedding of the skin lining the hair follicles increases the likelihood of the pores being clogged by the shedding skin. A pore clogged by the shedding skin is referred to as a comedo.

"The Propionibacterium acnes (P. acnes) normally reside on the skin. The propionibacterium acnes invade the clogged follicles and grow in the mixture of oil and cells in the hair follicle. It produces chemicals that stimulate inflammation resulting in acne. Acne lesions range in severity from blackheads, whiteheads and pimple, to more serious lesions such as deeper lumps, cysts and nodules.

"In many instances, the inflammation within the acne lesion provides an opportunity for secondary infections to invade and grow in the inflamed hair follicle. Some of these secondary infections can be more serious and more resistant to treatment than the primary Propionibacterium acnes infection.

"Various products and methods are currently available for treatment of acne. The only products that have anti-sebum activity are estrogens and 13 cis-retinoic acid (isotretinoin) and these must be used systemically to be effective. Isotretinoin is used to treat only severe cystic or conglobate acne (Anja Thielitz et al., JDDG, 6, 2008, Pp: 1023-1031). Because of its teratogenic properties, birth defects can occur. Isotretinoin is a powerful drug and can elevate triglycerides, total cholesterol and decrease high-density lipoproteins (HDL). Other side effects include dry skin, dry eyes, itching, headaches, nosebleed, and photosensitivity. It is generally taken for 4-5 months to see improvement. However, all topical retinoic acid preparations may be irritating, and this may contribute to underutilization in clinical practices (Cynthia E Irby et al., J. of Adolescent Health, 43, 2008, Pp-421-424). Recently, one brand of oral contraceptive has been approved for the treatment of acne for patients who request birth control.

"A number of topical and systemic agents are used to lower the number of bacteria that colonize the follicular duct. These include benzoyl peroxide (BP), and BP (5%), erythromycin (3%) combination (Benzamycin.RTM.). BP has antibacterial activity and drying effects and is available over the counter or by prescription. BP is applied once or twice daily for 1-2 months. BP can produce erythema and peeling of skin. BP is often tried first for both non-inflammatory and mild inflammatory acne. Other topical antibiotics include clindamycin and erythromycin. It is known that the combination of topical antibiotic such as clindamycin with other topical agents is more therapeutically effective than either drug used alone (James Q. Del Rosso et al., Drug therapy Topics, Volume 85; January 2010, Pp: 15-24). These topical antibiotics are used as solutions, lotions or gels by prescription only.

"Usually they are applied once or twice daily and results are seen in 1-2 months. Another topical agent, azelaic acid 20% (Azelex.RTM.) also has mild antibacterial effects.

"Systemic antibiotics include tetracycline and its analogs, which are used in low doses for years or until the end of the acne prone years. Most patients with mild inflammatory acne receive a combination of topical antibiotics and tretinoin or other retinoid. Application of topical antibiotic such as clindamycin gel after the pretreatment of skin with topical retinoid such as adapalene gel may contribute significantly to the increased efficacy of therapy (Gaurav K. Jain et al., Indian J Dermatol Venereol Leprol, September-October 2007, Vol-73(5), Pp: 326-329). Several clinical studies have also been performed earlier which demonstrates improved efficacy and tolerability of topical antibiotics and topical retinoids (John E. Wolf E. et al., J Am Acad Dermatol, 2009, Vol-49(3), Pp-S211-S217, and J. Z. Jhang et al., J of Derm Treat, 2004, Vol-15, Pp-372-378). Bacterial resistance does occur so antibiotics may be changed or BP is substituted since resistance does not occur with BP. More severe acne requires systemic antibiotics and topical retinoid. The most severe must receive oral isotretinoin for 4-5 months.

"Various topical products containing combination of clindamycin phosphate and adapalene are available in market. For example, Deriva-CMS.RTM. Gel [marketed by Glenmark Pharmaceuticals Ltd.], Achilles-C.RTM. Gel [marketed by Sandoz Ltd.], Adaple-C.RTM. Gel [marketed by Wallace Pharmaceuticals Ltd.], Zudenina-Plus.RTM. Gel [marketed by Roemmers SAICF], Medapine-AC.RTM. Gel [marketed by Daiichi-Sankyo Co. Ltd.], and Faceclin-A.RTM. Gel [marketed by Piramal].

"There are no drugs that directly affect the inflammatory acne. The retinoids do have some anti-inflammatory properties, but these are poorly described. Topical steroid and even systemic steroids have been used to abort a severe flare of fulminant acne, but these are limited uses because of the side effects. Benzoyl peroxide gels are sometimes used as first aid on acne lesions. These function as a 'drawing poultice', but data supporting this use is not available.

"The treatment for acne centers around opening the pore, killing P. acnes, reducing sebum production and regulating inflammatory responses. Retinoids are the agents to reduce sebum production and open the pore. As a topical agent, adapalene (Differin.RTM.) or tretinoin (Retin-A.RTM.) is used for mild and moderate acne.

"It is often advantageous to be able to deliver the drug over a period of time, such that a desired level of the drug in the target tissue is achieved for a period of time sufficient to achieve the desired result, e.g., killing most of a population of infectious bacterial. Dermatological conditions, such as acne, require multiple delivery strategies because they have multiple delivery requirements, such as killing skin surface bacteria while also penetrating deep into inflamed sebaceous glands to kill bacteria in that locus.

"U.S. Patent Publication No. 2010/0015216 discloses composition for the treatment of acne comprising: a first therapeutic agent selected from the group consisting of: salicylic acid, azelaic acid, adapalene, benzoyl peroxide, antibiotics and combinations thereof; and a second therapeutic agent which comprises a taurine species.

"U.S. Pat. No. 5,962,571 discloses a pharmaceutical composition for the treatment of acne having an acne reduction component in an amount sufficient to reduce the redness and blemishes associated with acne.

"U.S. Patent Publication No. 2010/0029781 discloses a method of preparing a solvent-microparticle (SMP) topical gel formulation comprising a bioactive drug wherein the formulation comprises the drug dissolved in a liquid and the drug in a microparticulate solid form dispersed in the liquid.

"U.S. Patent Publication No. 2010/0068284 discloses a stable fixed dose topical formulation comprising therapeutically effective amounts of adapalene-containing microparticles and clindamycin. However, such formulation may not significantly reduce the incident and severity of acne lesions.

"U.S. Pat. No. 5,894,019 discloses topical compositions comprising lipid and essentially free of emulsifiers and surfactants.

"European Patent No. EP 0671903 B discloses topical compositions in the form of submicron oil spheres.

"Most of the topical preparations contain vehicles comprising permeation enhancers, solvents, and high amount of surfactants to achieve topical compositions for acne treatment. But use of these agents is harmful, especially in chronic application, as many of them cause undesirable effects such as irritation and dryness and resulting in poor patient tolerability.

"In general, current products are effective in reducing the clinical observation of acne but it does not completely eliminate the condition, hence the consumer is not completely satisfied with results of these products.

"Although various over-the-counter products are commercially available to counteract acne condition, such as anti-acne agents for topical use, including salicylic acid, sulfur, lactic acid, glycolic acid, pyruvic acid, urea, resorcinol, N-acetylcysteine, retinoic acid, isotretinoin, tretinoin, adapalene, tazoretene, antibacterials such as clindamycin and erythromycin, vitamins such as zinc, folic acid and nicotinamide, benzoyl peroxide, octopirox, triclosan, azelaic acid, phenoxyethanol, phenoxypropanol, and flavinoids, however, these agents tend to lack in potential to mitigate the acne condition and may have negative side effects when devised in conventional topical formulations.

"Therefore, despite of the wide availability of products for acne, there exists a need to improve effectiveness of anti-acne pharmaceutical agents by developing suitable topical preparations which facilitate drug permeation through the skin, and resulting in enhanced therapeutic activity alongside reducing the instance and severity of adverse events resulting from topical use of these agents."

As a supplement to the background information on this patent, NewsRx correspondents also obtained the inventors' summary information for this patent: "In one general aspect there is provided a method for treating acne comprising administering a topical pharmaceutical composition comprising one or more anti-acne agent/s or salts thereof, wherein the anti-acne agent/s are present in the form of nano size droplets.

"In another general aspect there is provided a method for reducing total number of acne lesions on the skin. The method comprises administering a topical pharmaceutical composition comprising one or more anti-acne agent/s or salts thereof wherein the anti-acne agent/s are present in the form of nano size droplets.

"In another general aspect there is provided a method for reducing total number of inflammatory acne lesions on the skin comprising administering a topical pharmaceutical composition comprising one or more anti-acne agent/s or salts thereof wherein the anti-acne agent/s are present in the form of nano size droplets.

"In another general aspect there is provided a method for reducing total number of non-inflammatory acne lesions on the skin comprising administering a topical pharmaceutical composition comprising one or more anti-acne agent/s or salts thereof wherein the anti-acne agent/s are present in the form of nano size droplets.

"In another general aspect there is provided a method for reducing the incidence and severity of acne lesions on the skin comprising administering a topical pharmaceutical composition comprising one or more anti-acne agent/s or salts thereof wherein the anti-acne agent/s are present in the form of nano size droplets.

"In another general aspect there is provided a method for reducing the incidence and severity of inflammatory acne lesions on the skin comprising administering a topical pharmaceutical composition comprising one or more anti-acne agent/s or salts thereof wherein the anti-acne agent/s are present in the form of nano size droplets.

"In another general aspect there is provided a method for reducing the incidence and severity of non-inflammatory acne lesions on the skin comprising administering a topical pharmaceutical composition comprising one or more anti-acne agent/s or salts thereof wherein the anti-acne agent/s are present in the form of nano size droplets.

"In another general aspect there is provided a method for reducing the incidence and severity of adverse events resulting from treatment of acne by the use of anti-acne agents, comprising administering a topical pharmaceutical composition comprising one or more anti-acne agent/s or salts thereof wherein the anti-acne agent/s are present in the form of nano size droplets.

"Embodiments of the method of treating acne may include one or more of the following features. Applying a topical pharmaceutical composition to the skin which composition further may includes one or more pharmaceutically acceptable excipients. For example, the pharmaceutically acceptable excipients may include one or more of lipids, oils, emulsifiers or surfactants, initiators, pH adjusting agents, emollients, humectants, preservatives, chelating agents, thickening agent, and the like.

"In one general aspect there is provided a method for treating acne comprising administering a topical pharmaceutical composition prepared by the process comprising: a) combining an oily phase comprising one or more anti-acne agent/s or salts thereof along with other pharmaceutically acceptable excipients with an aqueous phase to form an emulsion; b) reducing the particle size of emulsion of step a) to a droplet size having D.sub.90 particle size of less than 500 nm; and c) mixing other pharmaceutically acceptable excipients to emulsion obtained in step b) and converting it into a suitable finished dosage form.

"In another general aspect there is provided a method for improving the local and systemic tolerability of anti-acne agent/s comprising administering a stable topical pharmaceutical composition comprising nano size droplets of one or more anti-acne agent/s or salts thereof.

"The details of one or more embodiments of the invention are set forth in the description below. Other features, objects and advantages of the invention will be apparent from the description and claims."

For additional information on this patent, see: Mittal, Ravindra; Roy, Sunilendu Bhushan; Kothari, Jay Shantilal; Sheikh, Shafiq; Patel, Jitendra Dasharathlal; Pancholi, Jinesh Suresh. Method for Treatment of Acne Using Pharmaceutical Compositions of Clindamycin and Adapalene. U.S. Patent Number 9636353, filed October 19, 2011, and published online on May 2, 2017. Patent URL: http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=9636353.PN.&OS=PN/9636353RS=PN/9636353

Keywords for this news article include: Antineoplastics, Alkenes, Polyenes, Terpenes, Adapalene, Retinoids, Carotenoids, Clindamycin, Azelaic Acid, Cyclohexanes, Cyclohexenes, Electrolytes, Erythromycin, Hydrocarbons, Isotretinoin, Benzoic Acids, Actinobacteria, Cycloparaffins, Topical Agents, Actinomycetales, Benzoyl Peroxide, Biological Factors.

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2017, NewsRx LLC



(c) 2017 NewsRx LLC

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