JP2005533795A5 - - Google Patents

Claims (18)

One or more physiologically active agents;
One or more dermal penetration enhancers;
A pharmaceutically acceptable carrier comprising a volatile solvent; and
High pressure gas containing HFC-134a ;
A pharmaceutical composition for transdermal delivery, comprising a carrier , a high pressure gas, and a permeation enhancer combined to provide a single phase solution of one or more physiologically active agents.   The pharmaceutical composition according to claim 1, wherein the volatile solvent has a vapor pressure higher than 35 mmHg at atmospheric pressure and a temperature of 32 ° C.   The composition of claim 1 substantially free of an adhesive for forming a film on the skin.   A composition according to claim 1 which maintains a drying time of less than 2 minutes, more preferably less than 1 minute. _ The composition of claim 4 wherein the high pressure gas consists essentially of HFC-134a. The pharmaceutical composition of claim 1 wherein the high pressure gas is 15 vol% to 50 vol% of the total pharmaceutical composition. The pharmaceutical composition according to claim 6 , wherein the high-pressure gas is 20 to 40% by volume of the composition.   The pharmaceutical composition of claim 1, wherein the permeation enhancer comprises one or more sunscreen esters. _ 1 or more sunscreen ester is _C 8 _{-C 18} alkyl _cinnamate, C 8 _{-C 18} alkyl _{methoxycinnamate,} according to claim 8, wherein is selected from the group consisting of C 8 _{-C 18} alkyl salicylate and mixtures thereof Pharmaceutical composition. The pharmaceutical composition according to claim 9 , wherein the permeation enhancer is octyl salicylate or padimate-0 . _ 9. The pharmaceutical composition according to claim 8 , comprising 0.1% to 10% by weight of a dermal permeation enhancer. _ The pharmaceutical composition of claim 1, wherein the volatile solvent comprises ethanol, isopropanol or a mixture thereof and provides a single phase of a permeation enhancer and a high pressure gas. Volatile solvent acetone, chloroform, lower alcohols or mixtures thereof and also contains, and pharmaceutical composition according to claim 1 wherein present at 40 vol% to 80 vol% of the total pharmaceutical composition. The solvent is acetone, chloroform, lower alcohols or mixtures thereof and also contains, and pharmaceutical composition according to claim 1 wherein present at 50 vol% to 70 vol% of the total pharmaceutical composition.   Steroids, hormone derivatives, non-steroidal anti-inflammatory drugs, opioid analgesics, antiemetics, antiestrogens, aromatase inhibitors, 5-alpha reductase inhibitors, anxiolytics, prostaglandins, anti-viral drugs, anti-migraine compounds Antihypertensive drugs, anti-malarial compounds, bronchodilators, antidepressants, anti-Alzheimer's drugs, anticholinergics, neuroleptic and antipsychotic drugs, anti-Parkinson's drugs, antiandrogens and appetite suppressants The pharmaceutical composition according to claim 1, comprising one or more physiologically active agents selected from the group consisting of: One or more physiologically acceptable agents are testosterone, estradiol, ethinyl estradiol, levonorgestrel, progesterone, norethisterone acetate, ibuprofen, ketoprofen, flurbiprofen, naproxen, diclofenac, fentanyl, buprenorphine, scopolamine, prochlorperazine , Metoclopramide, ondansetron, tamoxifen, epithiostanol, exemestane, darifenacin, 4-hydroxy-androstenedione and its derivatives, finasteride, dutasteride, turosteride, LY191704, MK-386, alprazolan, alprostadil, prostasis Kulin and its derivatives, melatonin, n-docosanol, tromantazine, acyclo Bill's lipophilic prodrug, low molecular weight heparin, enoxaparin, sumatriptan, amlodipine, nitrendipine, primaquine, minoxidil and its prodrugs, pilocarpine, salbutamol, terbutaline, salmeterol, ibogaine, bupropian, loliprin, tacrine , M ENT (7- Methyl-19-testosterone), or mazindol or any of the pharmaceutically acceptable salts or derivatives described above, and more preferably, as a physiological agent, apomorphine, oxybutynin, fentanyl, ropinirole, granisetron, rivastigmine , Buspirone, rizatriptan, zolmitriptan, lacidipine, tropisetron, olanzapine and methylphenidate or any of the above drugs 15. The pharmaceutical composition according comprising acceptable salt or derivative thereof.   A high pressure gas contained in a chamber of a spray application device comprising a valve for delivering the composition from the chamber, a nozzle for dispersing the composition as an aerosol, and means for providing a metered dose of aerosol from the nozzle. 2. The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition is held in a pressure state in the chamber so as to be kept in a liquid state. Through application to the skin of a composition in the form of a single phase solution comprising a physiologically active agent, a dermal permeation enhancer, a pharmaceutically acceptable carrier containing a volatile solvent, and HFC-134a high pressure gas. Use of a physiologically active agent in the manufacture of an aerosol composition for skin delivery .