Title of Invention

A NOVEL HERBAL BASED COMPOSITION

Abstract

The present invention discloses a process for the preparation of herbal composition for the treatment and alleviation of stress, comprising mixing from 10% to 90% of methyl salicylate and capsicum oleoresin and 90% to 10% of one or more aromatic oils, the balance if any, comprising one or more conventional additives, the composition being optionally dissolved in a conventional carrier. The composition shows increased properties of alleviation and reduction of stress related symptoms due to a combination of counterirritant therapy and aroma therapy. The composition of the invention can be used individually or in combination with any other conventional formulation for relief of stress related symptoms. The composition of the invention can also be used in the form of balms, pasts, or gels. In a particularly important embodiment of the invention, the composition of the invention is in the from of applicator sticks.

Full Text

FORM 2 THE PATENTS ACT, 1970 (39 of 1970) & THE PATENT RULES, 2003 COMPLETE SPECIFICATION (See section 10 and rule 13) TITLE OF THE INVENTION "A HERBAL COMPOSITION" We, GUFIC HEALTHCARE LIMITED, a Company, incorporated under the Companies Act, 1956, of Subash Road A, Ville Parle (E), Mumbai-400057, Maharashtra, India The following specification particularly describes the nature of the invention: Granted Field of the invention The present invention relates to a novel herbal based composition for alleviation and/or reduction of stress related symptoms, a method of preparation of said composition and a method of treatment of stress related symptoms using said composition. Background of the invention Stress is a common phenomenon affecting daily life in the modern world. Stress has been described as a debilitating pressure experienced by individuals in situations that threaten their well being or tax natural resources. Stress can be both a physical phenomenon as well as a mental or emotional phenomenon. Excessive physical action causes a state of 'tiredness' in muscle tissue that leads to physical stress. The body has its own developed mechanisms to cope with physical stress, such as the pumping of adrenaline hormone from the pituitary gland into the blood stream. This release of adrenaline results in excess 'energy' being available to the body for its functions. In so far as mental or emotional stress is concerned, the human body has very few mechanisms to cope with this disorder. One auto-generated method in the body is a comatose or semi-comatose condition equatable with sleep resulting in a step down of brain functions. The body also on occasion copes with mental or emotional stress by releasing adrenaline from the pituitary gland into the blood stream as in the case of physical stress. However, this response is not ideal since the solution to mental or emotional stress is not availability of excess energy but a reduction in the tension factor. The problems of mental stress are compounded by the body being unable to react or release the tension by physical action. This leads to further complications and physical distress evidenced by features such as chronic back or body pain, raised blood pressure, indigestion, headaches or mental features such as irritability, anxiety, palpitations and sweating. At times it also leads to a poorly defined sensation of uneasiness which is accompanied by involuntary spasm of the muscles, especially of head & neck. This could be one more additional cause of headache. Physical action is not a recommended method in all cases of emotional or mental stress since the auto-generated body response of adrenaline pumping exacerbates and in some cases actually induces the above-mentioned disabilities. Mental or emotional stress is also compounded by the action of chemicals present in stimulants/depressants/sedatives such as coffee, tea, alcohol, nicotine, sugar, additives, drugs and environmental toxins. Various attempts have been made to develop external methods, medicaments, and devices for stress therapy. Most treatments aim at treatment of stress related symptoms such as headaches, backaches, depression, etc. since stress itself is a phenomena for which cure is thought impossible. Aromatherapy is a common feature for the treatment of stress related symptoms today. However, in the case of aromatherapy the results are not always uniform and vary depending upon the subject of the treatment. Another common method of treatment recommended for stress or of stress related symptoms such as headaches/body aches is massage. This method has become very popular in the public mind. Unfortunately, massage is a treatment best administered by skilled and trained masseurs. There is at present a lack of skilled and trained masseurs. Massage when done by unskilled or not fully trained masseurs can result in actual grave physical damage to the patient. Other methods popularly advocated for stress relief are meditation, deep breathing exercises, acupuncture, laughter therapy, etc. However, the efficacy of these methods has not been completely established. Various formulations are also available in the market for alleviation of stress related symptoms such as headaches. However, these formulations are normally in the form of balms that require direct local application by hand which leave characteristic odour on the hands. Complementary therapies have been attempted to relieve stress and are found to show particularly better results than any one therapy. However, all the therapies listed above require skilled practitioners of which there is a short supply. Also these therapies cause a disruption in the daily routine and do not provide an instant relief. It is not very well recognised that stress per se does not have treatment. Most treatments are only for stress-related symptoms and help in some measure by producing a feeling of well being in the body. However, most of the treatments available in the art suffer from the disadvantages listed above, i.e. they require skilled personnel for administration, of qualified medical practitioners, cannot be applied instantaneously or are very messy and leave a strong odour characteristic of the ingredients. Some of the methods of treatment are also very expensive and time consuming. It is therefore, imperative to devise a method for the treatment of stress that is easy to practise and does not cause a disruption in daily life. Also, the method should not require external human interference in the form of clinics, massage parlours, etc. which adopt expensive and time consuming methods of treatment. Accordingly, several indigenous plants, particularly of the Mentha, Cinnamomum and Capsicum groups, known in traditional systems of medicine for the cure or prevention of different diseases were studied individually and in combination with other compounds having a pharmaceutical effect. Mentha arviensis is found in temperate reaches of North India (originally imported from Japan). It has long been known to have medicinal properties. Extracts of Mentha are known in traditional systems of medicine to have antifungal, antibacterial and anthelmintic properties. More particularly, the plant extracts are known to cure diseases of the liver and spleen, asthma and for pain in the joints. Cinnamomum camphorum (camphor) is also known to traditionally to be useful as a diaphoretic, skin and cardiac stimulant, and as an external anodyne. Various aromatic oils are also known to provide relief for stress related symptoms to some degree. For example, lemongrass oil and oil of wintergreen are commonly used in aromatherapy for reduction or alleviation of headaches. Oil of wintergreen is also known for use in the treatment of aches, pains, sciatica, and neuralgia. The chief content of oil of wintergreen is methyl salicylate. Extracts of various parts of plants belonging to the Capsicum family are known to help in advanced stages of rheumatism, gout and also in cholera along with other plant extracts from rhubarb and ginger. Rudolf and Gyorgy report a home made drug for the treatment of rheumatism containing mainly menthol, thymol, camphor, peppermint oil, plantain extract, rest-harrow root extract and thyme flower extract (Hung. Teljes HU 44, 705 (CI. A61 K35/78), 1988, 4PP). Wilkinson and Beck report cases of allergic contact dermatitis due to contact with menthol in peppermint (Contact Dermatitis, v. 30(1): p 42-43; 12 ref, 1994). Similar instances of contact dermatitis have been reported by Lee and Lam, after contact with, inter alia, camphor and menthol (Contact Dermatitis, v. 24(1): p 64-65; 1 ref, 1991); (also Wallengren et al report similar effect of enhancement of allergic contact dermatitis due to capsaicin in Contact Dermatitis; v. 24(1): p. 30-34; 14 ref; 1991). Buchbauer et al report the use of various oils extracted from herbs such as camphor, peppermint, basil, thyme etc. in Aromatherapy (Proceedings 23rd International Symposium on Essential Oils, Ayr., Scotland, 1-4, September 9-12, 1992). Burkhard et al report that several plant-derived essential oils are known to have epileptogenic properties due to their content of highly reactive monoterpene ketones (J. Neurol., Germany, 1999, 246/8 [667-670]). Capsaicin (I) is a pungent ingredient present in many varieties of Capsicums and has been reported to be possibly carcinogenic (Gannett et al; J. Org. Chem., v. 53(5), p. 1064-1071; 24 ref; 1988). However, De et al (Phytotherapy Research, v. 7(1): p. 87-89, 1993) report that capsaicin also has medicinal value in that it modifies UV induced lipid peroxidation in the liposomal membrane. Similarly, De and Ghosh also report that capsaicin pre-treatment caused stabilisation of rat lung membrane lipid system (Phytotherapy Research; v. 6(1); p. 34-37; 13 ref; 1992) (also De and Ghosh in Phytotherapy Research; v.7 (4), p. 273-277, 1993). De also reports that repeated treatment with capsaicin causes depletion of neuropeptides from the neurons causing a desensitised state that results in protection for the neurons from chemical irritant induced damage (Int. Conf. Curr. Prog. Med. Aromat. PL Res., Calcutta, India, p. 105, December 30, 1994 -January 1, 1995) (also Palevitch et al in Journal of Herbs, Spices and Medicinal Plants, v. 3(2), p. 55-83, 1995). Potenza et al report that Capsaicin induces a vasodilatant effect independent of the NO mechanism and therefore suggesting activity on the vascular smooth muscles (Polish Journal of Pharmacology; v. 46(4): p. 326-327; 1994). Capsaicin has also been used as an experimental tool in the study of analgesia (Clarke, Lancet, v. 342(8880): p. 1130-5; 5 ref; 1993). Methyl salicylate and its derivatives are widely used in the art as analgesics. They are used individually or in combination with other substances to induce a painkilling effect. Some of the common synergists of methyl salicylate include I-menthol, camphor, thymol, etc. Formulations can be applied both topically or ingested. Taniguchi et al report the widespread use of counterirritants such as I-menthol, methyl salicylate, camphor, thymol and capsaicin in the treatment of mild pains and itches by topical application (Antinociceptive effects of counterirritants, December 1994). However, the study focused on the antinociceptive effects and mechanisms of topical application of I-menthol. The use of external analgesics such as methyl salicylate has also been reported (Gosses, U S Pharm 12 (8), 1987 26, 28, 30, 35-36. 105). Pavelka et al report the experimental trial of an analgesic ointment containing menthol, plant essential oils and camphor in a natural ointment substrate, (brand name Arthrosan) in the treatment of rheumatic disease (Rheumatologia (Slovakia), 1994, 8/2,123-126). Ng et al discloses a combination of salicylic acid and peppermint extract for the treatment of pain by topical application as a traditional Chinese remedy (Arch. Dermatol. [U. S. A.] 1998, 134/11 (1395-1396)). Chan reports that excessive use of preparations containing methyl salicylate can result in severe salicylate poisoning, and in topical analgesic preparations can cause irritant or allergic contact dermatitis (Hum Exp Toxicol (EnglandO, Sep 1995, 15(9), p. 747-50); (see also: Hofman et al, J. of Toxicology, Clinical Toxicology 34(5): p. 596-597, 1996). US Patent 5, 910, 512 relates to an analgesic preparation containing water-soluble capsaicin for topical use. Deal reports the use of capsaicin to manage pain associated with arthritis by topical application (Semin. Arthritis Rheum, USA, 1994, 23/Suppl. 3 [48-52]); (see also: Watson, j Pain Symptom Manage, USA, October 1994, 9(7), p. 425-33; Puett and Griffin, Ann Intern Med, USA, July 15, 1994, 121(2), p. 133-34; Med Lett Drugs Ther, USA, June 26, 1992, 34(873), p. 62-3). Rains and Bryson also report the topical use of capsaicin and its therapeutic potential in osteoarthritis, post-herpetic neuralgia and diabetic neuropathy (Drugs Aging, New Zealand, October 1995, 7(4), p. 317-28). Ortega et al also report the use of a formulation of a capsaicin gel for use in patients with post-herpes pains (Farm Clin 7(1), 1990, 30-34). Cesaro reports, inter alia, the use of capsaicin in the treatment of neuropathic pain (Rev Med Interne, France, 1995, 16/suppl, l(16s-19s). Hautkappe et al report a review of the effectiveness of capsaicin in the treatment of painful cutaneous disorders and neural dysfunction (Clin J Pain, USA, June 1998, 14(2), p. 97-106); (see also: Lipman AG, Clin Geriatr Med, USA, August 1998, 12(3), p. 501-15; Wright JM, Pharmacotherapy, Nov-Dec, 1994, 14(6), p. 689-97; Kingsley-Wade, Pain, 73(2): p. 123-129, Nov. 1997). Hofrnann et al report the use of oil of wintergreen in oriental herbal medication (J. Toxicol. Clinic. Toxicology 34 (5): p. 596 - 597, 1996). Rao et al report the use of myrcene, a monoterpene extracted from lemongrass oil for antinociception in mice at low temperature (J. Pharm. Pharmacol. England, Dec. 1990,42 (12) p. 877 - 878). Objects of the invention Accordingly it is an object of the invention to provide a composition for the treatment of stress related symptoms that is inexpensive and effective. It is a further object of the invention to provide a composition for the treatment of stress related symptoms that is capable of being self-administered by the patient. It is yet another object of the invention to provide a composition for the treatment of stress related symptoms whose application does not cause a major disruption in the daily routine of the patient. It is a further object of the invention to provide a composition whose application involves a relatively easy procedure not requiring external expert human intervention in the form of masseurs, doctors, acupuncturists, chiropractors, and the like. It is another object of the invention to provide a method for combating stress related symptoms that provides instant relief and does not cause a major disruption in daily life. It is yet another object of the invention to provide a composition for the treatment of stress related symptoms such as headaches by easy application and minimal intrusion on a person's daily routine. It is another object of the invention to provide a method for treating stress related symptoms that does not require a long procedural treatment. It is yet another object of the invention to provide a composition for the treatment of stress related symptoms such as headaches that uses the complementary therapies of aromatherapy and counterirritant therapy to enhance relief from the symptoms. It is a further object of the invention to provide a method for the treatment of stress related symptoms using complementary therapies of aromatherapy and counterirritant therapy. Summary of the invention Accordingly, the invention provides a herbal composition for the treatment and alleviation of stress related symptoms, said composition comprising 10 % to 90 % of a combination of methyl salicylate and Capsicum oleoresin and 90 % to 10 % of one or more aromatic oils, the balance if any, comprising one or more conventional additives, the composition being optionally dissolved in a conventional carrier. The composition of the invention is not a mere admixture of the ingredients with only a mere aggregation of their individual properties. The composition of the invention is a synergistic composition showing hitherto unexpected and unknown properties as a result of the interaction of the ingredients contained therein. In one embodiment of the invention, the composition comprises 10 % to 70 % of methyl salicylate and Capsicum oleoresin^ % to 30 % of one or more aromatic oils. In another embodiment of the invention, the composition comprises 10 % to 60 % of methyl salicylate and Capsicum oleoresin?90 % to 40 % of one or more aromatic oils. In a further embodiment of the invention, the Capsicum oleoresin is extracted from Capsicum annum, C minimum, C. baccatum and C. frutescens. In a further embodiment of the invention, the aromatic oils are selected from the group comprising of lemongrass oil, oil of wintergreen and peppermint oil. In another embodiment of the invention, the conventional additives are selected from well known adjuvants, diluents and gels. The invention also relates to a process for the preparation of a herbal composition for the treatment and alleviation of stress related symptoms, said composition comprising 10 % to 90 % of methyl salicylate and Capsicum oleoresin and 90 % to 10 % of one or more aromatic oils, the balance if any, comprising one or more conventional additives, the composition being optionally dissolved in a conventional carrier, the process comprising extracting the respective ingredients in any known manner, dissolving the solids in a conventional carrier, adding if desired, one or more conventional ingredients, to obtain the final composition. The invention also relates to a method for the treatment and/or alleviation of stress related symptoms comprising administering or applying on the affected areas the composition of the invention to the patient. The composition of the invention is prepared by mixing the ingredients in the desired proportions after extraction in a suitable solvent or carrier. The composition of the invention can be used individually or in combination with any other conventional formulation for relief of stress related symptoms. The composition of the invention can also be used in the form of balms, paste, gels or any other topical dosage form. In a particularly important embodiment of the invention, the composition of the invention is in the form of applicator sticks. While not wishing to be bound by any theory, it is believed that the composition of the invention shows increased properties of alleviation and reduction of stress related symptoms due to a combination of counterirritant therapy and aromatherapy. The ingredients in the composition penetrate the skin to the subcutaneous layer and cause minimal irritation, which evokes an inflammatory response; leading to onrush of blood to the affected area. The flow of blood to the affected area results in a sensation of warmth in the region. The nerve endings transmit signals of warmth to the brain overriding pain or ache signals that are arising from other structures. At the same time, certain of the essential oils serve to 'relax' the brain due to their soothing aroma. The active oily ingredients have been formulated in the solid balm stick form to make it an easy to use delivery dosage form. The product has been developed to achieve optimum degree of oil releasing property and spreadability, while maintaining the required hardness and consistency of the balm stick. The manufacturing process is unique as it contains highly volatile active ingredients, therefore, the temperature parameter is critical and the same had to be optimised to develop the product. The stick dosage form has been formulated so as to achieve the end product with an optimum melting range, which can withstand the extremes of climatic temperature conditions. During the manufacturing and filling process, the fill rate of the machine is worked out to an optimum level to achieve the end product, set in an acceptable form. The product filled in the stick container devices is then allowed to pass through a Cooling tunnel where the product finally sets into the balm stick dosage form. The invention will now be described with reference to the following examples, which are not to be construed as limiting the nature and scope of the invention. The examples given below are illustrative and serve only as guidelines for the preparation of the composition of the invention. EXAMPLE 1 A. Preparation of the Bulk IA. Preparation of base: 1. The excipients viz., Cetyl Alcohol (20% - 30%w/w), Hard Paraffin (30% - 40%w/w) and White Soft Paraffin (15% - 25%w/w) are transferred to a steam jacketed S.S. tank fitted with a stirrer. The waxes are melted at a suitable temperature under mixing. 2. The above solution is filtered into a Water jacketed S.S. mixing tank provided with stirrer and a lid. The temperature of the molten mass is maintained between 65°C-75°C. IIA. Preparation and addition of Active Oil Mixture: 1. The active oily ingredients viz., Pudinah Ke Phool (10.00 %w/w), Pudinah Ka Tel (2.00 %w/w), Karpur (3.00 %w/w), Gandapuro Ka Tel (10.00 %w/w), Hari Chai Ka Tel (3.50%w/w) and Mirch Ka Tel (0.025 %w/w) are transferred to a S.S. vessel. 2. The oils are mixed well and Butylated Hydroxytoluene (0.01% - 0.1%w/w) is added to the oil solution. The solid contents are allowed to dissolve completely using a suitable stirrer. 3. The above oil mixture is filtered and mixed into the bulk of Step AI (2), maintained between 65°C-75°C. EXAMPLE 2 B. Filling and Cooling 1. The container devices to be used for filling are cleaned by vacuum to remove any dust or other particles adhering to the device. 2. The clean devices are then arranged in Aluminium holders for filling. 3. The product filling machine is then assembled. The molten mass of Step All (3) maintained between 50°C-60°C is transferred to the hopper of the filling machine. 4. The machine is set at the desired speed so as to achieve an optimum fill rate with an intended fill weight. 5. The filling operation is started and the fill weight variation of the Balm Stick is checked intermittently. 6. The speed and temperature of Cooling tunnel is adjusted so that the molten mass in stick container sets completely while passing through the cooling tunnel. We Claim: 1. A herbal composition for the treatment and alleviation of stress, said composition comprising 10 % to 90 % of methyl salicylate and Capsicum oleoresin and 90 % to 10 % of one or more aromatic oils, the balance if any, comprising one or more conventional additives, the composition being optionally dissolved in a conventional carrier. 2. A composition as claimed in claim 1, wherein the composition comprises 10 % to 70 % of methyl salicylate and Capsicum oleoresin 3. A composition as claimed in claim 1, wherein the composition comprises 10 % to 60 % of methyl salicylate and Capsicum oleoresin and 90 % to 40 % of said one or more aromatic oils. 4. A composition as claimed in claim 1, wherein the capsicum oleoresin is extracted from Capsicum anuum, C. minimum, C. baccatum and C. frutescens. 5. A composition as claimed in claim 1, wherein the conventional additives are selected from known aromatic oils, adjuvants, diluents and gels. 6. A composition as claimed in claim 1, wherein the aromatic oils are selected from the group comprising of lemongrass oil, oil of wintergreen, peppermint oil. 7. A composition as claimed in claim 1 wherein the composition is in the form of a balm, salve or lotion, stick. 8. A composition as claimed in any one of claims 1 to 6 wherein it is in the form of a stick. Dated this the 16th day of January 2002

Documents:

48-mum-2002-cancelld pages(15-10-2007).pdf

48-mum-2002-claims(granted)-(15-10-2007).doc

48-mum-2002-claims(granted)-(15-10-2007).pdf

48-mum-2002-correspondence(15-10-2007).pdf

48-mum-2002-correspondence(ipo)-(27-09-2007).pdf

48-mum-2002-form 1(07-09-2007).pdf

48-mum-2002-form 1(18-01-2002).pdf

48-mum-2002-form 19(18-05-2004).pdf

48-mum-2002-form 2(granted)-(15-10-2007).doc

48-mum-2002-form 2(granted)-(15-10-2007).pdf

48-mum-2002-form 3(18-01-2002).pdf

48-mum-2002-power of authority(18-01-2002).pdf