US2022096420A1PendingUtilityA1

Acetylcholinesterase Inhibitors for Treatment of Dermatological Conditions

Assignee: ATTILLAPS HOLDINGSPriority: Jun 19, 2014Filed: Jun 8, 2021Published: Mar 31, 2022
Est. expiryJun 19, 2034(~7.9 yrs left)· nominal 20-yr term from priority
A61K 36/185A61K 9/2013A61K 31/27A61K 9/02A61K 31/473A61K 9/2009A61K 9/4858A61K 31/55A61K 9/0075A61K 31/683A61K 9/4825A61K 9/4866A61K 9/2054A61K 36/324A61P 17/00A61K 31/662
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Claims

Abstract

Embodiments of the invention involve treating skin afflictions by the topical or oral use of acetylcholinesterase inhibitor. By effectively reducing or eliminating the population of Demodex mites in affected skin areas and areas where Demodex mites may exist, this treatment achieves a more complete remission of clinical signs and symptoms of the skin afflictions than any previously described method. Embodiments of the invention are useful for treating skin afflictions including common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis, acne necrotica milliaris, psoriasis, steroid induced dermatitis, primary irritation dermatitis and rosacea.

Claims

exact text as granted — not AI-modified
1 - 90 . (canceled) 
     
     
         91 . A pharmaceutical formulation for topical administration to treat a mite-induced skin affliction, the pharmaceutical composition comprising an acetylcholinesterase inhibitor selected from the group consisting of: physostigmine, demecarium, donepezil, tacrine, echothiophate, diisopropyl fluorophosphate, lactucopicrin,  boswellia, Celastrus paniculatus , coumarins, galantamine, huperzine A, or a prodrug or pharmaceutically acceptable salt thereof. 
     
     
         92 . The pharmaceutical formulation of  claim 91 , formulated in a carrier lotion, cream, soap, wash, shampoo or gel. 
     
     
         93 . The pharmaceutical formulation of  claim 92 , wherein the acetylcholinesterase inhibitor has a concentration of between 0.001% to 5% by weight. 
     
     
         94 . The pharmaceutical formulation of  claim 92 , wherein the acetylcholinesterase inhibitor has a concentration that is the lowest concentration effective for killing  Demodex  mites. 
     
     
         95 . The pharmaceutical formulation of  claim 91 , further comprising one or more pharmaceutically acceptable carriers, excipients, buffers, emulsifiers, surfactants, electrolytes or diluents. 
     
     
         96 . The pharmaceutical formulation of  claim 91 , further comprising an ophthalmologically acceptable excipient selected from the group consisting of: buffered saline; mineral oil; vegetable oils; petroleum jelly; Miglyol™ 182; alcohol solutions; and liposomes or liposome-like products. 
     
     
         97 . The pharmaceutical formulation of  claim 91 , further comprising: preservatives, antioxidants, antibiotics and/or immunosuppressants. 
     
     
         98 . The pharmaceutical formulation of  claim 91  formulated in a pad or gelled stick. 
     
     
         99 . The pharmaceutical formulation of  claim 91 , wherein the acetylcholinesterase inhibitor has a concentration in the formulation selected to kill at least a portion of  Demodex brevis  and/or  Demodex folliculorum  mites or to render at least a portion of said  Demodex brevis  and/or  Demodex folliculorum  mites unable to reproduce. 
     
     
         100 . The pharmaceutical formulation of  claim 91 , wherein the acetylcholinesterase inhibitor concentration topically administered to the skin corresponds to between 0.01 mg/kg body mass to 50 mg/kg body mass. 
     
     
         101 . The pharmaceutical formulation of  claim 91 , wherein the acetylcholinesterase inhibitor is physostigmine or a pharmaceutically acceptable salt thereof. 
     
     
         102 . The pharmaceutical formulation of  claim 91 , wherein the mite-induced skin affliction is one or more of common acne, seborrheic dermatitis, perioral dermatitis, an acneiform rash, transient acantholytic dermatosis, acne necrotica miliaris, steroid induced dermatitis, primary irritation dermatitis or  rosacea ; and the mite induced skin affliction is from  Demodex brevis  and/or  Demodex folliculorum  mites. 
     
     
         103 . The pharmaceutical formulation of  claim 91 , wherein the skin affliction affects facial skin, eyelids, or both facial skin and eyelids. 
     
     
         104 . The pharmaceutical formulation of  claim 91 , wherein the formulation is configured to facilitate penetration of the acetylcholinesterase inhibitor to a subdermal region. 
     
     
         105 . The pharmaceutical formulation of  claim 91 , further comprising dimethyl sulfoxide (DMSO). 
     
     
         106 . A method of treating a skin affliction associated with  Demodex brevis  and/or  Demodex folliculorum  mites, the method comprising the step of:
 topically applying to an individual having the skin affliction the pharmaceutical formulation of  claim 91 .   
     
     
         107 . The method of  claim 104 , further comprising the step of:
 topically applying the pharmaceutical formulation in a continued intermittent regime sufficient for prophylactic control of  Demodex  mite population in hair follicles and/or skin of the individual.   
     
     
         108 . A method of making the pharmaceutical formulation of  claim 91 , the method comprising the steps of:
 providing a therapeutically effective amount of the acetylcholinesterase inhibitor with a pharmaceutically acceptable carrier.   
     
     
         109 . The method of  claim 108 , wherein the pharmaceutically acceptable carrier comprises an ointment, cream, gel, paste, foam, aerosol, suppository, pad or gelled stick. 
     
     
         110 . The method of  claim 108 , further comprising the step of:
 providing an ophthalmologically acceptable excipient selected from the group consisting of: buffered saline, mineral oil, vegetable oils such as corn or  arachis  oil, petroleum jelly, Miglyol 182, alcohol solutions, and liposomes.

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