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(12) Patent Application Publication (10) Pub. No.: US 2002/0115618 A1 Rosenbloom (43) Pub US 2002O115618A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2002/0115618 A1 ROSenbloom (43) Pub. Date: Aug. 22, 2002 (54) METHOD AND COMPOSITION FOR THE compounded mixture of a compound that promotes Synthe TOPCAL TREATMENT OF DABETIC sis of nerve growth factor, an aldose reductase inhibitor and NEUROPATHY an antioxidant formulated in a pharmaceutically acceptable carrier. It has been found that this combination of active (76) Inventor: Richard Allen Rosenbloom, Elkins agents provides significant, effective relief of the Symptoms Park, PA (US) of diabetic neuropathy, as well as at least partial recovery of Correspondence Address: lost neurological function in Some cases. In View of the KNOBLE & YOSHIDA consensus in the art that effective combinations of various EIGHT PENN CENTER active agents have not been demonstrated to be effective for SUITE 1350, 1628 JOHN F KENNEDY BLVD the treatment of diabetic neuropathy, the present invention PHILADELPHIA, PA 19103 (US) provides a Surprising and unexpected effect. In addition, the topical compositions of the present invention, when used in (21) Appl. No.: 09/740,811 effective amounts to treat diabetic neuropathy, do not exhibit (22) Filed: Dec. 21, 2000 the Severe Side effects of many prior art compositions proposed for treatment of this ailment, Publication Classification In a Second aspect, a method for the topical administration (51) Int. Cl.' .................. A61K 31/7048; A61K 31/593; of a composition in accordance with the present invention A61K 31/335; A61K 31/365 for the treatment of diabetic neuropathy is disclosed. In the (52) U.S. Cl. ............................ 514/27; 514/168; 514/456; method, an effective amount of the composition of the 514/458; 514/474 invention is topically administered to the areas of the body that have been adversely affected by the diabetic neuropathy (57) ABSTRACT on a regular basis over a period of time Sufficient to provide A method and composition for the treatment of diabetic the beneficial effects of relief from the symptoms and at least neuropathy is disclosed. The composition comprises a cold Some recover of the damaged nerve tissues. US 2002/0115618 A1 Aug. 22, 2002 METHOD AND COMPOSITION FOR THE 0009 Still another approach to the treatment of neuropa TOPCAL TREATMENT OF DABETIC thy is disclosed in U.S. Pat. No. 5,550,249 (Della Ville et NEUROPATHY al.). In this approach, compositions Suitable for treatment of vitamin H deficiencies are administered for the treatment of BACKGROUND OF THE INVENTION neuropathy. This patent relates to biotin Salts with alkano lamines. The compositions may be administered orally, 0001) 1. Field of the Invention parenterally or topically. 0002 The present invention relates to a method and 0010 U.S. Pat. No. 5,665,360 (Mann) relates to the composition for the topical treatment of diabetic neuropathy. treatment of peripheral neuropathies associated with diabe More particularly, the present invention relates to a topical tes mellitus by periodic topical application of a composition composition including a combination of ingredients that containing capsicum oleoresin as the active ingredient. provide a Surprising degree of effective relief from the When applied to the Skin of the affected area, pain and Symptoms of diabetic neuropathy and to a method for burning associated with the neuropathy are said to be administering the topical composition to treat diabetic neu reduced. However, capsicum oleoresin has been shown to ropathy. kill nerve endings in Some cases and thus this composition 0003 2. Description of the Prior Art Suffers from this disadvantage. 0004 Diabetes mellitus is a common disease that is 0.011 U.S. Pat. No. 5,981,594 (Okamoto et al.) relates to usually classified into insulin-dependent and non-insulin a method of treatment of diabetic neuropathy using com dependent types. Both types may be managed by diet, in bined administration of a formulation including as an active combination with insulin in the first type and a variety of ingredient, a prostaglandin I derivative with an anti-diabetic drugs in the Second type. However, while the changes in agent in order to improve nerve conduction Velocities. blood glucose associated with diabetes can usually be man Suitable anti-diabetic agents include oral hypoglycemic aged reasonably Satisfactorily by conscientious patients and agents and insulin. doctors, this does not prevent long term damage to many 0012. The Okamoto patent also contains a detailed dis tissueS as a result of the disease. This damage may take cussion of the various types of neuropathy that may be many forms but the major types are damage to the eyes asSociated with diabetes. According to this patent, nerve (retinopathy), nerves (neuropathy), kidneys (nephropathy) conduction velocity (NCV) is the most widely used method and cardiovascular System, of objectively evaluating the Severity of diabetic neuropathy. 0005 There are many approaches to reducing or prevent This patent also mentions that current methods of treating ing these forms of damage, which are collectively known as diabetic neuropathy Such as dietetic therapy, administration the long-term complications of diabetes. One approach is of insulin, administration of aldose reductase inhibitors or based on damage that results from over-production of the aminoguaninidine to improve abnormal glucose metabo glucose metabolite, Sorbitol, in the cells of the body, Glucose lism, administration of troglitaZone or agents for the can be converted to Sorbitol by the enzyme aldose reductase. improvement of blood flow have been tested but found to be High levels of Sorbitol may be among the causes of diabetic insufficient when a Single drug was used. Also, according to complications Such as diabetic neuropathy. As a result, a this patent, methods of treatment by combined use of number of pharmaceutical companies have been developing different therapeutic agents which have different functions aldose reductase inhibitors for the purpose of reducing had yet to be established. The patent concludes that com diabetic neuropathy. bined drug therapies for diabetic neuropathy, aiming at recovering once reduced nerve conduction Velocity, have not 0006. It has been established that a wide variety of yet been confirmed. flavanoids are effective inhibitors of aldose reductase, including Such flavanoids as quercetin, quercetin and myre 0013 There remains a need in the art for an effective cetrin. However, U.S. Pat. No. 4,232,040 discloses that treatment for diabetic neuropathy that does not suffer from despite the fact that these flavanoids have been shown in in the disadvantage that it causes Severe side effects, as do Vitro Studies to be among the most potent flavanoids for many aldose reductase inhibitors, for example. aldose reductase inhibition, a need exists for aldose reduc 0014. Accordingly, it is the primary object of the present tase inhibitors that can be more effectively used and in lower invention to provide a topical composition that is effective doses than the prior art compounds, including these fla for the treatment of diabetic neuropathy. Vanoids. 0015. It is another object of the present invention to 0007. In fact, numerous patents are devoted to goal of provide a topical composition for the treatment of diabetic developing improved aldose reductase inhibitors. Among neuropathy which does not cause Serve side effects in the these patents are U.S. Pat. Nos. 6,069,168; 5,011,840; 4,210, patients treated with the composition. 667; 4,147,795; 5,866,578; and 5,561,110. Numerous other patents also exist which relate to aldose reductase inhibitors. 0016. These and other objects of the present invention will be apparent from the Summary and detailed descriptions 0008 Another approach to the treatment of neuropathy is of the invention which follow. disclosed in U.S. Pat. No. 5,840,736 (Zelle et al.). In this method, pharmaceutical compositions for Stimulating the SUMMARY OF THE INVENTION growth of neurites in nerve cells comprising a neurotrophic amount of a compound and a nerve growth factor. These 0017. In a first aspect, the present invention relates to a compositions may be administered in a number of ways topical composition for the treatment of diabetic neuropathy. including orally and topically. The composition comprises a cold compounded mixture of US 2002/0115618 A1 Aug. 22, 2002 a compound that promotes Synthesis of nerve growth factor, (19)-triene. The preferred nerve growth factor used in the an aldose reductase inhibitor and an antioxidant formulated topical composition is Vitamin D. Also, pharmaceutically in a pharmaceutically acceptable carrier. It has been found acceptable Salts of the compounds that promote Synthesis of that this combination of active agents provides significant, nerve growth factor may be employed. effective relief of the Symptoms of diabetic neuropathy, as well as at least partial recovery of lost neurological function 0023 The compound that promotes synthesis of nerve in Some cases. In View of the consensus in the art that growth factor is used in an amount effective to promote the effective combinations of various active agents have not synthesis of nerve growth factor of about 10,000 to about 3 been demonstrated to be effective for the treatment of million IU. per kg of the composition. More preferably, the diabetic neuropathy, the present invention provides a Sur compound that promotes Synthesis of nerve growth factor is prising and unexpected effect. In addition, the topical com employed in an amount of about 50,000 to about 2 million positions of the present invention, when used in effective IU per kg of the composition, and most preferably an amounts to treat diabetic neuropathy, do not exhibit the amount of 100,000 to about 1 million IU is used per kg of Severe side effects of many prior art compositions proposed the composition. for treatment of this ailment, 0024. The preferred compounds that induce synthesis of 0.018. In a second aspect, the present invention relates to nerve growth factor may, in addition to this activity, also a method for the topical administration of a composition in function to prevent neurotrophic deficits.
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