A formulation of pentoxifylline and hesperidin for hemorrhoids and acute fissure

Abstract

A formulation of pentoxifylline and hesperidin for hemorrhoids and acute fissure [0005] The present invention discloses a formulation of pentoxifylline and hesperidin for hemorrhoids and acute fissure. The formulation comprises pentoxifylline at a percentage of 90%, hesperidin at a percentage of 10% along with excipients. The formulation of pentoxifylline and hesperidin aids in enhancing the flow of blood by decreasing the viscosity. The improved blood flow aids in alleviating the symptoms caused by hemorrhoids and acute fissure. The formulation inhibits the activity of phosphodiesterase aiding in increased production of cyclic adenosine monophosphate (cAMP) in the skeletal muscle leading to vasodilation. Vasodilation aids in decreased venous hypertension and enhanced blood flow in the rectal blood vessels. The formulation of pentoxifylline and hesperidin exhibits antioxidant and anti-inflammatory properties.

Description

A formulation of pentoxifylline and hesperidin for hemorrhoids and acute fissurePriority Claim:

[0001] This application claims priority from the provisional application numbered 202311053856 filed with Indian Patent Office, Chennai on 11thAugust 2023 entitled “A formulation of pentoxifylline and hesperidin for hemorrhoids and acute fissure”, the entirety of which is expressly incorporated herein by reference.PREAMBLE TO THE DESCRIPTION:

[0002] The following specification describes the invention and the manner in which it is to be performed:DESCRIPTION OF THE INVENTION Technical field of the invention

[0003] The present invention discloses a formulation with a combination of pentoxifylline and hesperidin for treatment of hemorrhoids and acute fissure. More specifically, the formulation is effective in enhancing the blood flow by decreasing the viscosity aiding in alleviating the symptoms of hemorrhoids and acute fissure. Background of the invention

[0004] Hemorrhoids, commonly referred to as piles, are caused by swollen and inflamed veins around the rectum and anus. The common risk factors of hemorrhoids are straining during bowel movements, chronic constipation, diarrhea, low-fiber diet, abdominal obesity, ageing, pregnancy, frequent heavy lifting.

[0005] Hemorrhoids are categorized into external hemorrhoids and internal hemorrhoids. External hemorrhoids are caused by inflammation of skin around the anus. Internal hemorrhoids are caused by inflammation of the lining of lower rectum and anus.

[0006] The common symptoms of hemorrhoids are anal itching, tender lumps at the anal canal, anal pain while sitting. The symptoms of external hemorrhoids subside in a short period of time. The symptoms for internal hemorrhoids are rectal bleeding and prolapse. Hemorrhoids are diagnosed by performing physical exam, medical history, rectal exam for internal hemorrhoids, anoscopy, sigmoidoscopy.

[0007] The remedies for the management of mild hemorrhoids are by the consumption of high-fiber foods, use of topical treatments, oral pain relievers, and interventions including external hemorrhoid thrombectomy, hemorrhoidectomy and hemorrhoid stapling.

[0008] The medication for hemorrhoids aims at relieving swelling, burning, pain and itching. The medication for hemorrhoids causes several side effects. The side effects caused by the administration of hemorrhoids are rash, itching or swelling of the face or tongue or throat, dizziness and trouble breathing. The administration of oral medication for treating hemorrhoids focuses on treating the symptoms alone.

[0009] Acute fissures are caused by the tearing of the anal canal. The causes of acute fissures are constipation, persistent diarrhea, large or hard stools, childbirth. The symptoms for anal fissure are anal bleeding and sharp pain. Acute fissures and hemorrhoids comprise similar symptoms and can occur together.

[0010] Pentoxifylline is a vasoactive agent aiding in reduction of viscosity of blood hence improving the blood flow. Pentoxifylline aids in reducing the viscosity of blood by decreasing erythrocyte aggregation and stimulating fibrinolysis to reduce plasma fibrinogen concentrations. Further, pentoxifylline aids in decreased adhesion of platelets to the vessel wall in circulatory disorders. Additionally, pentoxifylline has immunomodulatory effects aiding in inhibition of production of inflammatory cytokines.

[0011] Hesperidin is a bioflavonoid made of flavanone glycoside. Hesperidin is commonly derived from citrus trees exhibiting properties of antioxidant and antiinflammation. Hesperidin possesses therapeutic potential in the management of heart disease, blood vessel disorders, metabolic disorders, and neurodegenerative diseases. Hesperidin primarily aids in promoting peripheral blood flow and improves endothelial function.

[0012] The Patent Application No. CN101744822A entitled “Medicinal composition for treating hemorrhoids ” discloses a medicinal composition for treating hemorrhoids comprising pentoxifyllinum and ketorolac tromethamine. The composition comprising pentoxifyllinum and ketorolac tromethamine is at a ratio of 0.021:1. The composition is administered orally and applied externally. The composition is externally administered in the form of gel and ointment. The composition is administered orally in the form of tablet, capsule, drop pill, granule, powder and oral liquid. The composition aids in the treatment for anorectal diseases including hemorrhoids.

[0013] The Patent Application No. CN101919860A entitled “Medicine composite containing pentoxifyllinum and diclofenac and application thereof" discloses a medicine composite comprising pentoxifyllinum and diclofenac. The pharmaceutical composition comprising pentoxifyllinum and diclofenac is at a ratio of 0.0110 to 1. The composition comprising diclofenac comprises diclofenac officinal salt selected from a group of diclofenac sodium and diclofenac potassium. The pharmaceutical composition is administered orally and through external preparations. The pharmaceutical composition administered through external preparations in the form of gel and ointment. The pharmaceutical composition is administered orally in the form of tablet, capsule, slow releasing tablet, slow releasing capsule and osmotic pump controlled releasing tablet. The pharmaceutical composition aids in the treatment for hemorrhoids and arthritis.

[0014] The Patent Application No. IN202311008961A entitled “HERBAL GEL FOR TREATMENT OF PILES” discloses a herbal gel for the treatment of piles. The herbal gel composition comprises hesperidin at a concentration of Img / lOOmggel, curcumin at a concentration of 2mg / 100mg gel, gallic acid at a concentration of 0.6mg / 100mg gel, carbopol 934 at a concentration of 0.40-1.10g, sodium carboxymethyl cellulose at a concentration range of 0.9g- 1.60g, methyl at a concentration of 0.18g, propyl paraben at a concentration of 0.02g, 5 to 6 drops of triethanolamine, glycerine at a concentration of 15ml and water up to 100ml. The process comprises steps of mixing carbopol 934 and sodium carboxy methyl cellulose polymer in 78.60 ml of distilled water with continuous stirring simultaneously, mixing 0.18 gm of methylparaben and 0.02 gm of propylparaben dissolved in 4.00 mL of distilled water in a beaker, adding the prepared solution in Carbopol 934 and sodium carboxy methyl cellulose polymer gel adding 0.2gm of triethanolamine and 15ml of glycerine and adding hesperidin, gallic acid and curcumin. The herbal gel composition exhibits 71.69% hesperidin release in 5 hours ,72.5% curcumin release in 5 hours, and 74.8% gallic acid release in 5 hours. The herbal gel composition is stable for a duration of 90 days. The herbal gel is an anti-inflammatory composition aiding in inhibition of oedema at the recto anal part.

[0015] Although several compositions exist for the management of hemorrhoids, the treatment options aim at relieving symptoms temporarily and possess several side effects. Hence, there is a necessity for a composition for hemorrhoids and acute fissure aiding in effective management of the symptoms with minimal side effects.Summary of the Invention

[0016] In order to overcome the drawbacks of the state of art, the present invention discloses a formulation comprising pentoxifylline and hesperidin for treatment of hemorrhoids and acute fissure. The formulation comprises pentoxifylline at a concentration of 90% by weight, hesperidin at a concentration of 10% by weight and other excipients. The excipients for the formulation are selected from a group comprising titanium dioxide, polyethylene glycol (PEG), magnesium stearate, colloidal silicon dioxide, hydroxypropyl cellulose, Hypromellose.

[0017] The combination of pentoxifylline and hesperidin is effective in management of hemorrhoids and acute fissure. The inhibition of phosphodiesteraseby the formulation enhances cyclic adenosine monophosphate (cAMP) resulting in vasodilation. The vasodilation caused by the formulation reduces venous hypertension. Additionally, the formulation inhibits the synthesis of tumor necrosis factor (TNF) - a aiding in improved blood flow and reduced inflammation of blood vessels of the rectum.Brief description of the drawings:

[0018] The foregoing and other features of embodiments will become more apparent from the following detailed description of embodiments when read in conjunction with the accompanying drawings. In the drawings, like reference numerals refer to like elements.

[0019] FIG 1 tabulates the formulation of pentoxifylline and hesperidin according to an embodiment of the invention.Detailed description of the invention:

[0001] In order to more clearly and concisely describe and point out the subject matter of the claimed invention, the following definitions are provided for specific terms, which are used in the following written description.

[0002] The term “ Hemorrhoids ” refers to inflamed and swollen veins of the lower rectum and anus.

[0003] The term “ Acute fissure ” refers to damage to the lining of the anal canal.

[0004] The present invention discloses a formulation of combination of pentoxifylline and hesperidin for hemorrhoids and acute fissure. The formulation aids in improving the blood flow by decreasing the viscosity. The formulation further aids in enhancing lymphatic flow and exhibits antioxidant and antiinflammatory properties.

[0020] The present invention discloses a formulation of pentoxifylline and hesperidin. FIG 1 tabulates the formulation of pentoxifylline and hesperidinaccording to an embodiment of the invention. The formulation comprises pentoxifylline at a concentration of 90% by weight, hesperidin at a concentration of 10% by weight and other excipients. The excipients for the formulation are selected from a group comprising titanium dioxide, polyethylene glycol (PEG), magnesium stearate, colloidal silicon dioxide, hydroxypropyl cellulose, hypromellose.

[0021] The formulation comprising pentoxifylline aids in the reduction of viscosity of blood. The reduction of viscosity of blood improves the flow of blood in people with hemorrhoids. Enhancing the blood flow aids in relieving the symptoms of hemorrhoids and acute fissure including pain, irritation and discomfort. Furthermore, the formulation aids in prevention of occurrence of symptoms for hemorrhoids and acute fissure. The formulation further comprises a bioflavonoid hesperidin. Hesperidin exhibits the properties of antioxidant, anti-inflammation hence acts as an immunomodulatory agent. Hesperidin aids in increasing the peripheral blood flow and improves lymphatic flow.

[0022] The combination of pentoxifylline and hesperidin is effective in management of hemorrhoids and acute fissure. The inhibition of phosphodiesterase by the formulation enhances cyclic adenosine monophosphate (cAMP) resulting in vasodilation. The vasodilation caused by the formulation reduces venous hypertension. Additionally, the formulation inhibits the synthesis of tumor necrosis factor (TNF) - a aiding in improved blood flow and reduced inflammation of blood vessels of the rectum.

Claims

Claims:I Claim,1. A formulation for treatment of hemorrhoids and acute fissure, the formulation comprises: a. pentoxifylline at a concentration of 90% by weight; b. hesperidin at a percentage of 10% by weight; and c. one or more excipients wherein said active ingredients are mixed with the excipients.

2. The formulation as claimed in claim 1, wherein the excipients are selected from a group comprising titanium dioxide, polyethylene glycol (PEG), magnesium stearate, colloidal silicon dioxide, hydroxypropyl cellulose, hypromellose.

3. The formulation as claimed in claim 1, wherein the formulation reduces the viscosity of blood thus improving the blood flow.

4. The formulation as claimed in claim 1, wherein the formulation reduces the inflammation of blood vessels of rectum.

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