Claims:1. A formulation that is effective against hemorrhoids, comprising: 300 mg to 400 mg of an extract of Euphorbia hirta; said extract of Euphorbia hirta being prepared from the whole plant, 150 mg to 200 mg of an extract of Mimosa pudica, said extract of Mimosa pudica being prepared from the seeds; 50 mg to 150 mg of an extract of Messua ferrea, said extract of Messua ferrea being prepared from the seeds; and 50 mg to 100 mg of an extract of Berberis aristata, said extract of Berberis aristata being prepared from the roots.
2. A formulation that is effective against hemorrhoids as claimed in claim 1, wherein the preparation of the extract of Euphorbia hirta comprises: drying whole plant of Euphorbia hirta under the sun and obtaining coarse powder of Euphorbia hirta using grinder; obtaining a water soluble extract of Euphorbia hirta using water as a polar solvent; passing the water soluble extract of Euphorbia hirta through a special type of bed that is made of muslin cloth, with activated charcoal and purified red ochre being present in the muslin cloth to purify the water soluble extract and increase the concentration of iron in the extract, respectively; evaporation of the water in the water soluble extract of Euphorbia hirta to obtain a solid mass of the extract; spray drying to obtain a completely dry extract of Euphorbia hirta; milling of the Euphorbia hirta extract through a multi mill; and obtaining fine powder of the Euphorbia hirta extract using a blender and shifter.
3. A formulation that is effective against hemorrhoids as claimed in claim 1, said formulation being compressed into a tablet that comprises permitted pharmaceutical excipients, preservatives and coating agents, with: the pharmaceutical excipients being one or more of: 5 mg to 10 mg of starch, 30 mg to 40 mg of gum acacia, and 5 mg to 10 mg of talc or magnesium stearate; the preservatives being one or more of: 0.5 mg to 1 mg of methyl paraben and 0.5 mg to 1 mg of propyl paraben; and the coating agents being one or more of hydroxypropyl methylcellulose and 2% solution of PEG.
, Description:TITLE OF THE INVENTION: FORMULATION THAT IS EFEFCTIVE AGAINST HEMORRHOIDS AND PROCESS OF PREPARATION THEREOF

FIELD OF THE INVENTION
The present disclosure is generally related to formulations that are effective against anorectal diseases. Particularly, the present disclosure is related to a formulation that is effective against hemorrhoids and its process of preparation.
BACKGROUND OF THE INVENTION
Hemorrhoids are a common disease with a prevalence of 4.4%. It affects both genders in the age group between 45 years and 65 years equally. These are distal displacement and prolapse of the hemorrhoidal cushions, distension of the hemorrhoidal arterio-venous anastomoses, or dilation of the veins of the internal hemorrhoidal venous plexus resulting from deterioration of anchoring connective tissue.
Among the various anorectal and colonic diseases, hemorrhoids occupy a prominent position and have been the subject of numerous clinical studies. Hemorrhoidal disease is characterized by fresh blood spots without any pain that occur immediately after defecation. However, pain occurs when the hemorrhoids are secondarily infected, or complicated by thrombosis and anal fissures. Common symptoms are pain, itching, swelling, anal discomfort, and rectal bleeding, which affect quality of life of an individual. Symptoms may be accompanied by thrombosis, pruritis, edema, etc.
Hemorrhoids can be caused by a variety of factors including hormones, genes, inflammation, infection, constipation, exercise, vascular stasis, diet, strain, physical stance in defecation, loss of connective tissue elasticity with increase in age, fast foods, low intake of water, irregular dietary habit, regular travelling, sedentary work style, and mental stress.
Hemorrhoids can be treated through reduction of inflammation and pain, haemostasis, wound healing and protection of vascular walls. Therapeutic treatment of hemorrhoids depends on degree and severity of symptoms, and ranges from dietary and lifestyle modification to radical surgery. Even though surgery is the most effective treatment option for hemorrhoids, it is recommended only at the advanced disease state and it can be associated with considerable complications such as relapse, pain, prolonged convalescence, fecal urgency, and anal stenosis. The main aim of medical treatment is to control acute symptoms of hemorrhoids rather than to cure the hemorrhoids.
There is, therefore, a need in the art for a formulation that is effective against hemorrhoids, provides relief in a short time span, and reduces the chances of recurrence of another hemorrhoidal attack.
SUMMARY OF THE INVENTION
A formulation that is effective against hemorrhoids is disclosed. The formulation comprises: 300 mg to 400 mg of an extract of Euphorbia hirta; said extract of Euphorbia hirta being prepared from the whole plant, 150 mg to 200 mg of an extract of Mimosa pudica, said extract of Mimosa pudica being prepared from the seeds; 50 mg to 150 mg of an extract of Messua ferrea, said extract of Messua ferrea being prepared from the seeds; and 50 mg to 100 mg of an extract of Berberis aristata, said extract of Berberis aristata being prepared from the roots. The formulation may be compressed into a tablet that comprises permitted pharmaceutical excipients, preservatives and coating agents, provides relief in a short time span, and reduces the chances of recurrence of another hemorrhoidal attack. The process of preparation of the formulation is also disclosed.
DETAILED DESCRIPTION OF THE INVENTION
Throughout this specification, the use of the word "comprise" and “include”, and variations such as "comprises" "comprising", “includes”, and “including” may imply the inclusion of an element or elements not specifically recited.
Throughout this specification, the disclosure of any range is to be construed as being inclusive of the lower limit of the range and the upper limit of the range.
A formulation that is effective against hemorrhoids is disclosed. The formulation comprises: 300 mg to 400 mg of an extract of Euphorbia hirta; said extract of Euphorbia hirta being prepared from the whole plant, 150 mg to 200 mg of an extract of Mimosa pudica, said extract of Mimosa pudica being prepared from the seeds; 50 mg to 150 mg of an extract of Messua ferrea, said extract of Messua ferrea being prepared from the seeds; and 50 mg to 100 mg of an extract of Berberis aristata, said extract of Berberis aristata being prepared from the roots.
Euphorbia hirtawas collected from various districts in Maharashtra, such as Latur, Aurangabad, and Pune, in addition to being purchased from different vendors in Mumbai.
Mimosa pudica and Messua ferrea were collected from Shivpuri district in Madhya Pradesh.
Berberis aristata was procured from various important drug markets of India, namely, Aligarh, Mumbai, Amritsar, Bangalore-I, Bangalore-II, Delhi, Hyderabad, Jammu, Lucknow, Trichur, and Varanasi.
The preparation of the extract of Euphorbia hirta comprises the steps of: drying whole plant of Euphorbia hirta (Sun Drying) and obtaining coarse powder of Euphorbia hirta using grinder; obtaining a water soluble extract of Euphorbia hirta using water as a polar solvent; passing the water soluble extract of Euphorbia hirta through a special type of bed that is made of muslin cloth, with activated charcoal and purified red ochre being present in the muslin cloth to purify the water soluble extract and increase the concentration of iron in the extract, respectively; evaporation of the water in the water soluble extract of Euphorbia hirta to obtain a solid mass of the extract; spray drying to obtain a completely dry extract of Euphorbia hirta; milling of the Euphorbia hirta extract through a multi mill; and obtaining fine powder of the Euphorbia hirta extract using a blender and shifter.
300mg to 400mg of the extract of Euphorbia hirta obtained using the method is combined with 150 mg to 200 mg of an extract of Mimosa pudica, said extract of Mimosa pudica being prepared from the seeds; 50 mg to 150 mg of an extract of Messua ferrea, said extract of Messua ferrea being prepared from the seeds; and 50 mg to 100 mg of an extract of Berberis aristata, said extract of Berberis aristata being prepared from the roots, and is formulated into a tablet that comprises permitted pharmaceutical excipients, preservatives and coating agents, with: the pharmaceutical excipients being one or more of: 5 mg to 10 mg of starch, 30mg to 40mg of gum acacia, 5 mg to 10 mg of talc or magnesium stearate, and the like; the preservatives being one or more of: 0.5 mg to 1mg of methyl paraben ,0.5 mg to 1mg of propyl paraben, and the like; and the coating agents being one or more of hydroxypropyl methylcellulose (“HPMC”),2% solution of PEG and the like.
The method of manufacturing of a tablet that comprises the formulation shall now be disclosed. The method comprises the steps of: weighing the above listed active ingredients and starch in powder form and passing them through a Mesh No. 40; making a solution of gum acacia, methyl paraben and propyl paraben; wet granulation to obtain wet granules; drying the wet granules at 65 degrees Centigrade; passing the dried granules through a Mesh No. 12; adding lubricants and compressing using a tablet punching machine.
The process of coating the tablet that comprises the formulation shall now be disclosed. The process comprises the steps of: weighing 750 mg of tablet, de-dusting, and loading to a coating pan; weighing coating materials such as HPMC and PEG making a solution in a stainless steel tank, following by stirring for 30 minutes and filtration; setting a spray gun and starting the coating process; checking the tablet at regular intervals and confirming the completion of the coating process; and polishing the tablet in a polishing pan, weighing, and storing in poly bags.
The efficacy of the formulation shall now be illustrated with the following example:
Persons between 18-80 years, who were diagnosed with internal hemorrhoids of grade 2-3, or external bleeding hemorrhoids were enrolled. The following categories of persons were excluded: those with: thrombosed hemorrhoids, active Anal Fissure, active anal fistula, Grade IV hemorrhoids, Chronic Pain requiring analgesics, antiplatelet and anticoagulation intake other than Aspirin, or cancer; and female patients who were pregnant, or were not using a reliable method of birth control, or were nursing.
For those who passed the eligibility criteria and had given their consent, the symptoms were assessed by counting of bleeding per rectum episodes, in addition to the assessing of quantity, pain, discharge itching, and discomfort on Visual analogue scale (VAS) on a score ranging from 0 (no symptoms) to 100 (severe symptoms). Likewise, constipation was assessed on a scale from 0 to 4 (no constipation, mild constipation, moderate constipation, and severe constipation). Along with haemorrhoids symptoms, painkillers taken were also assessed during study. The enrolled persons were advised to follow dietary restrictions according to the etiology of hemorrhoids and each person received one tablet (each Tablet Contained: 181 mg of Mimosa pudica, 350 mg of Euphorbia hirta,90 mg of Messua ferrea,79 mg of Berberis aristata, and Permitted Preservative sand excipients q.s.) two times a day with warm water for 30 days. They were called for follow up on Week 1, Week 2, and Week4 after the baseline visit.
The following results were obtained:
Out of 320 persons who enrolled, constipation was completely resolved in 156 persons, and the number of persons with severe constipation had drastically decreased from 143(45%) to 9 (3%) at the end of treatment.
There was significant (p<0.05 using paired t-test of baseline score v. Week 4 score) reduction at the end of the study in the mean score of each haemorrhoids symptoms. The baseline score of 84.23± 9.7 for Pain reduced to 40.35 ± 09.22 in week 4. The baseline score of 81.17 ± 11.25 for Discharge reduced to 40.01± 10.5 in week 4. The baseline score of 86.85 ± 8.72 for Itching reduced to 41.23 ±09.21 in week 4. The baseline score of 85.58 ± 8.21 for Discomfort reduced to 42.24 ±10.01 in week 4.
On evaluation at week 4 follow up, it was observed that 303 (95%) persons did not have any bleeding episode, while 6 persons had one episode, 2 had 2 episodes, and 5had 3 episodes of bleeding. Further, there was reduction in count of those consuming pain killers from 129 (40%) to 13 (4%) at the end of study.
It will be apparent to a person skilled in the art that the above description is for illustrative purposes only and should not be considered as limiting. Various modifications, additions, alterations and improvements without deviating from the spirit and the scope of the disclosure may be made by a person skilled in the art. Such modifications, additions, alterations and improvements should be construed as being within the scope of this disclosure.