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(12) Patent Application Publication (10) Pub. No.: US 2014/0235570 A1 Hochman (43) Pub

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(12) Patent Application Publication (10) Pub. No.: US 2014/0235570 A1 Hochman (43) Pub US 20140235570A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0235570 A1 Hochman (43) Pub. Date: Aug. 21, 2014 (54) THERAPEUTIC COMPOSITION FOR THE Publication Classification TREATMENT OF PERIANAL DISORDERS (51) Int. Cl. (71) Applicant: David Jonathan Hochman, Winnipeg A613 L/706 (2006.01) (CA) A613 L/4422 (2006.01) A619/00 (2006.01) (72) Inventor: David Jonathan Hochman, Winnipeg A63/67 (2006.01) (CA) (52) U.S. Cl. CPC ........... A6 IK3I/7016 (2013.01); A61 K3I/I67 (21) Appl. No.: 14/183,660 (2013.01); A61 K3I/4422 (2013.01); A61 K 9/0014 (2013.01); A61 K9/0031 (2013.01) USPC ............................................................ 514/53 (22) Filed: Feb. 19, 2014 (57) ABSTRACT O O The invention relates to a composition for the treatment of Related U.S. Application Data perianal disorders. In R the composition includes (60) Provisional application No. 61/766,294, filed on Feb. three components: a) an analgesic, b) a cryoprotective agent 19, 2013. and c) a muscle relaxant. US 2014/0235570 A1 Aug. 21, 2014 THERAPEUTIC COMPOSITION FOR THE sidered Standard therapy as it reduces the anal sphincter tone TREATMENT OF PERIANAL DISORDERS and improves blood Supply to the anal canal, but its significant side effects, including systemic hypotension and headaches, 0001. This application claims the benefit of priority of resulted in very poor patient compliance. With poor compli U.S. Provisional Patent Application No. 61/766,294, filed on ance, these disorders often went incompletely treated and Feb. 19, 2013, and which is incorporated herein in its entirety. resulted in unhealed lesions and continued pain for the indi FIELD OF THE INVENTION vidual. 0011 Topical calcium channel blockers have largely 0002 The present invention relates to a composition for replaced topical nitroglycerine in managing perianal disor the treatment of perianal disorders. More specifically this ders due to their reduced incidence of side-effects, especially invention relates to a topical composition comprising three headaches. Calcium channel blockers directly reduce the tone active agents and the use of said composition in the treatment of the sphincter complex acting on the muscle fibers, again of conditions and disorders affecting the perianal region. with the aim of improving blood Supply to the injured perianal tissue, but, this drug too, is not perfect. Patients continue to BACKGROUND experience pain even while using the medication as resolution 0003 Perianal disorders refers to disorders of the tissue of the pain is only achieved once the injured tissue has healed located around the anus, the opening of the rectum to the completely, often requiring up to 8 to 12 weeks. Topical outside of the body and the anal canal. Injury and trauma to calcium channel blockers, while Successful for many the anal canal or Surrounding tissue can result in extremely patients, do not have success in all individuals and there are painful conditions which can be very difficult for individuals many patients who still experience chronic pain. to tolerate and can be equally difficult to manage medically. 0012 To date, there are few topical therapies that effec 0004 Examples of such perianal disorders include but are tively treat pain from perianal disorders and most patients still not limited to anal fissures, thrombosed external hemorrhoids require significant quantities of oral analgesics to manage and prolapsing internal hemorrhoids. These conditions are their discomfort. Many of the oral analgesics are opioids, very painful and can be extremely difficult to heal. Addition which can result in constipation and cause further discomfort ally, managing the pain and wound healing from Surgical when patients pass hard stools along the raw and healing procedures to this area, such as Surgical hemorrhoidectomy, Surfaces of the injured tissue. fissurectomy, lateral internal sphincterotomy, and fistulo 0013 Surgical treatments have also been used to address tomy, to name just a few, poses a challenge for both patients these conditions. Surgery is typically reserved for patients and the physicians treating them. who have failed more conservative therapies. The surgical 0005. There have been numerous attempts to manage division of a portion of the anal sphincter muscle is performed these painful conditions but none have been truly effective at to reduce the basal sphincter tone and results in improved managing this pain for a variety of reasons. For example, U.S. blood supply to the injured area, thereby allowing it to heal. Pat. No. 5,196.405 teaches hemorrhoidal compositions con But significant complications can result, as dividing this taining disaccharide polysulfate-aluminum compounds Such muscle is permanent and can potentially result infecal incon as Sucralfate. Specifically, this patent teaches that the Sucral tinence and a significantly reduced quality of life. Further fate can be used as a carrier, complexing with the wounded more, the Surgery itself can result in significant pain during area and holding additional pharmaceutical compounds near the healing process. the wounded area. 0014. There remains a need for improved treatments for 0006 U.S. Pat. No. 6,395,736 and U.S. Pat. No. 6,627,632 perianal disorders or conditions. teach compositions comprising NO donors and a number of other possible compounds, including an L-type Ca" channel SUMMARY blocker. 0015. According to a one aspect, there is provided a com 0007 U.S. Pat. No. 6.242,010 teaches a composition com position for the treatment of perianal disorders comprising: prising reduced glutathione and selenium as a selenoamino 0016 a) a first agent that is an analgesic; acid in a Suitable carrier for topical applications for treating ano-rectal wounds. 0017 b) a second agent that is a cytoprotective agent 0008. The commercially available topical agents used to and treat Such disorders typically comprise, a topical steroid 0.018 c) a third agent that is a muscle relaxant. designed to reduce the local inflammation. However, these 0019. According to one embodiment, the analgesic is a agents do nothing to directly treat the underlying pain, nor do Sodium channel blocker, such as Lidocaine. they contribute to improving the individuals healing capac 0020. According to another embodiment, the cytoprotec ity. Additionally, if used too frequently, topical steroids can tive agent is Sucralfate. cause significant atrophy to the perianal skin that can predis 0021. According to a further embodiment, the muscle pose individuals to further injury and complications. relaxant is a calcium channel blocker, Such as nifedipine. 0009 Topical and oral analgesics have also been used, and 0022. According to yet another embodiment, there is pro may temporarily help with the pain of perianal disorders, but vided a composition comprising Lidocaine, nifedipine and fail to treat the underlying cause of the problem. These agents Sucralfate. do not address the sphincter spasm, or hypertonicity and do 0023. According to another aspect, there is provided a little to improve blood supply to the area and to promote composition as described above, in the form of a pharmaceu healing of the injured tissue. tical composition formulated for topical application. 0010 Many topical agents have been tried to manage 0024. According to a yet another aspect, there is provided perianal disorders to mitigate the need for Surgery or to aid in ause of a composition as described above, for the treatment of post-Surgical recovery. Topical nitro-glycerine was once con perianal disorders. US 2014/0235570 A1 Aug. 21, 2014 0025. According to a further aspect, there is provided a effectively and the injury persists. Additionally, because the method of treating perianal disorders comprising administer calcium channel blocker does little to treat the immediate and ing to Subject in need thereof a pharmaceutically effective ongoing pain related to the injury, the patient continues to amount of a composition as described above. suffer. Without relief from their discomfort, patient compli 0026. According to still a further aspect, there is provided ance with the therapy is poor and may lead to failed treatment. a composition as described above, for use in the treatment of 0034. It has been found that multifactorial treatment of perianal disorders. perianal conditions can provide improved outcomes for patients. Namely, addressing the immediate and ongoing pain DESCRIPTION OF THE PREFERRED related to the disruption of the anal lining, combined with EMBODIMENTS reducing the associated sphincter spasm, and improving the 0027. Although any methods and materials similar or blood Supply to the area to allow for healing, and improved equivalent to those described herein can be used in the prac absorption of medication has been found to offer both short tice or testing of the present invention; examples of Suitable and long term relief and to promote healing in patients methods and materials are now described. All publications afflicted with perianal disorders or conditions. mentioned herein are incorporated herein by reference. 0035. A composition comprising three agents has been 0028 Perianal disorders or conditions include any disor prepared to address the three aspects of the negative feedback ders or conditions associated with anal or rectal disease, loop and actina Synergistic manner to provide immediate and injury or trauma, Such as anal fissures, anal ulcers, or Swollen Sustained relief of pain relating to Such lesions and to improve and/or thrombosed hemorrhoids, and incision sites from Sur blood flow to promote healing. gical procedures. 0036. The first agent is an analgesic Such as a sodium 0029 Anal fissure, anal ulcer, and hemorrhoidal diseases channel blocker, that provides immediate short-term pain are relatively common disorders. An anal fissure or ulcer is a relief. Local, topical application of the first agent immedi tear or ulcer of the mucosa or lining tissue of the distal anal ately reduces pain, thereby increasing compliance. The canal. An anal fissure or ulcer can be associated with another reduction in pain also immediately reduces the associated systemic or local disease.
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