Topical pharmaceutical bases for wound and scar treatment

Abstract

The present disclosure refers to topical pharmaceutical bases that include a synergistic combination of pracaxi oil, andiroba oil, copaiba balsam, and ucuuba butter. Further, these topical pharmaceutical bases are proposed for treating skin conditions in mammals, such as, for example wounds and scars. The topical pharmaceutical bases provide healing, moisturizing, anti-inflammatory, antibacterial, and antifungal effect. Additionally, the topical pharmaceutical bases enable an effective administration of specific active pharmaceutical ingredients (APIs), thereby improving treatment outcomes. Topical pharmaceutical compositions including the topical pharmaceutical bases increase the residence time of APIs within a wound or scar, thereby improving the penetration of APIs into the affected area. Also, the topical pharmaceutical bases provide relatively uniform distribution of the APIs within the topical pharmaceutical compositions. Further, the topical pharmaceutical compositions release APIs slowly, thereby enhancing treatment effectiveness.

Claims

1. A topical pharmaceutical composition comprising a pharmaceutically effective amount of at least one active pharmaceutical ingredient, and a synergistically effective amount of about 5% w/w to about 50% w/w ucuuba butter, about 5% w/w to about 50% w/w copaiba balsam, about 5% w/w to about 50% w/w andiroba oil, and about 5% w/w to about 50% w/w pracaxi oil.

2. The topical pharmaceutical composition of claim 1 further comprising at least one natural component selected from the group consisting of buriti oil, bacaba oil, acai oil, ojon oil, murumuru butter, and tucuma oil.

3. The topical pharmaceutical composition of claim 1 further comprising at least one natural component selected from the group consisting of about 1% w/w to about 20% w/w buriti oil, about 1% w/w to about 20% w/w bacaba oil, about 1% w/w to about 20% w/w acai oil, about 1% w/w to about 20% w/w ojon oil, about 1% w/w to about 20% w/w murumuru butter, and about 1% w/w to about 20% w/w tucuma oil.

4. The topical pharmaceutical composition of claim 1 further comprising at least one natural component selected from the group consisting of about 5% w/w buriti oil, about 5% w/w bacaba oil, about 5% w/w acai oil, about 5% w/w ojon oil, about 5% w/w murumuru butter, and about 5% w/w tucuma oil.

Description

DETAILED DESCRIPTION

(1) The present disclosure is here described in detail with reference to embodiments illustrated in the drawings, which form a part here. Other embodiments may be used and/or other changes may be made without departing from the spirit or scope of the present disclosure. The illustrative embodiments described in the detailed description are not meant to be limiting of the subject matter presented here.

(2) Definitions

(3) As used here, the following terms have the following definitions:

(4) Active Pharmaceutical Ingredients (APIs) refer to chemical compounds that induce a desired effect, and include agents that are therapeutically effective, prophylactically effective, or cosmeceutically effective.

(5) Balsam refers to oily or viscous oleoresins, usually having benzoic or cinnamic acid.

(6) Butter refers to a moisturizing product obtained of oils extracted from seeds and nuts. Butters are solid at room temperature, but melt on the skin.

(7) Oil refers to a vegetable substance that may be clear, odorless, viscous, hydrophobic, liquid or liquefiable at room temperature. Oils are widely used in cosmetics due to its hypoallergenic and noncomedogenic properties.

(8) Treating and Treatment refers to reduction in severity and/or frequency of symptoms, elimination of symptoms and/or underlying cause, prevention of the occurrence of symptoms and/or their underlying cause, and improvement or remediation of damage.

(9) Description of the Disclosure

(10) The present disclosure refers to topical pharmaceutical bases that include a synergistic combination of pracaxi oil, andiroba oil, copaiba balsam, and ucuuba butter. Further, these topical pharmaceutical bases are proposed for treating skin conditions in mammals, such as, for example wounds, scars, and the like.

(11) In some embodiments, the topical pharmaceutical bases provide healing, moisturizing, anti-inflammatory, antibacterial, and antifungal effect. In these embodiments, the topical pharmaceutical bases include one or more naturally occurring substances, including one or more oils rich in essential fatty acids. Further to these embodiments, the topical pharmaceutical bases include oils having properties that increase wound healing process, thereby enabling treatment of scars.

(12) Formulation

(13) In some embodiments, the topical pharmaceutical bases include natural components from the Amazon forest. In these embodiments, topical pharmaceutical bases include a synergistic combination of pracaxi oil, andiroba oil, copaiba balsam, and ucuuba butter. Further to these embodiments, the natural components exhibit moisturizing, antimicrobial, and healing properties.

(14) In an example, the topical pharmaceutical bases include a synergistic combination of: pracaxi oil in a concentration from about 5% w/w to 50% w/w; andiroba oil in a concentration from about 5% w/w to 50% w/w; copaiba balsam in a concentration from about 5% w/w to 50% w/w; and ucuuba butter in a concentration from about 5% w/w to 50% w/w.

(15) In this example, each of the aforementioned components possesses significant healing properties. Further to this example, aforementioned components employed together improve the effectiveness of the wound healing process as well as the treatment of scars.

(16) In other embodiments, the topical pharmaceutical bases include one or more natural components, such as, for example buriti oil, bacaba oil, acai oil, ojon oil, murumuru butter, and/or tucuma oil, among others. In these embodiments, the concentration of each natural component within topical pharmaceutical bases is from about 1% w/w to 20% w/w, preferably about 5% w/w.

(17) In some embodiments, the topical pharmaceutical bases include suitable active pharmaceutical ingredients (APIs), such as, for example antibiotic, antifungal, corticosteroids, non-steroidal anti-inflammatories, antibacterials, antivirals, and analgesics, among others. In these embodiments, aforementioned non-steroidal anti-inflammatory drugs include diclofenac, ketoprofen, ibuprofen, naproxen, and piroxicam, among others.

(18) In other embodiments, topical pharmaceutical bases are employed within topical pharmaceutical compositions for scar treatments. In these embodiments, the topical pharmaceutical compositions include suitable APIs, such as, for example tamoxifem, metaxalone, and tranilast, among others.

(19) Pracaxi Oil

(20) Pracaxi oil is obtained from the seed oil of the Pentaclethara macroloba tree, or pracaxi tree. The pracaxi tree is a deciduous tree from the legumes family, growing in altitudes below about 600 meters in many parts of northern Brazil, Guyana, Trinidad, and parts of Central America, and may reach between about 8 and about 35 meters in height. Pracaxi trees may sometimes be found in wetlands, and are resistant to water logging.

(21) Pracaxi seeds include from about 45% to 48% fat, about 27% to 28% protein, and about 12% to 14% carbohydrates (see Table 1). Pracaxi seed oil includes the highest known natural concentration of behenic acid (about 20%) in a vegetable fat, more than six times higher than in peanut oil, and also includes about 35% of oleic acid. In some cases, pracaxi seed oil may include greater percentages of the aforementioned behenic acid and oleic acid. The oleic acid and lauric acid, contained within pracaxi oil are effective vehicles for delivering drugs through the skin.

(22) TABLE-US-00001 TABLE 1 General composition of pracaxi oil. Components Composition % Fat 45-48 Protein 27-28 Carbohydrates 12-14

(23) In an example, the fatty acid composition of the pracaxi oil is illustrated below in Table 2. Compositions vary depending on the region and conditions in which the pracaxi tree grows.

(24) TABLE-US-00002 TABLE 2 Fatty acid composition of the pracaxi oil. Fatty Acids Carbon Atoms Composition % Lauric 12:00 1.30 Myristic 14:00 1.21 Palmitic 16:00 2.04 Stearic 18:00 2.14 Oleic 18:10 44.32 Linoleic 18:20 1.96 Linolenic 18:30 2.31 Behenic 22:00 9.67 Lignoceric 24:00 14.81

(25) TABLE-US-00003 TABLE 3 Specifications of the pracaxi oil. Indicators Reference Value Texture Solid below 18.5 C., liquid viscous texture above this temperature Color Translucent yellow, yellowish-white when solid Odor Almost odorless Melting point 18.5 C. Refractive index (40 C.) 1.4690 Iodine value 65-70 g I2/100 g Saponification value 170-180 mg KOH/g Acid value 3-5 mg KOH/g Peroxide value 5-10 mEQ/kg Density (25) 0.917 g/cm.sup.3

(26) Pracaxi oil has been widely employed within pharmaceutical compositions because of its cosmetic, therapeutic, and medicinal properties. Pracaxi oil is rich in organic acids with antioxidant, antibacterial, antiviral, antiseptic, antifungal, anti-parasitic, and anti-hemorrhagic properties. Because pracaxi oil possesses many of the aforementioned properties, pracaxi oil can be suitable oil for helping in the treatment of wounds and scars.

(27) Pracaxi oil has a high amount of solid matter, not fatty acids, which makes pracaxi oil solidifies in cooler temperatures. The solid matter has gentle moisturizing and high cellular renewal promoting properties. It includes vitamin E, and has essential fatty acids, which make pracaxi oil suitable for topical pharmaceutical compositions.

(28) Andiroba Oil

(29) Andiroba oil is extracted from the Carapa guianensis tree. Andiroba oil is rich in omega-3 fatty acid, which is fast absorbed into the skin balancing the production of chemicals that cause inflammation, thereby improving blood circulation, diminishing the swelling and reducing pain. Andiroba oil is also a rich source of essential fatty acids, including oleic, palmitic, myristic and linoleic acids, and includes non-fatty components, such as, for example triterpenes, tannins, and alkaloids, which are isolated as andirobina and carapina.

(30) Andirobia has healing and insect repelling properties that are attributed to the presence of limonoids. Limonoids have been proven to possess antiviral, antifungal, antibacterial, anti-neoplastic, insecticide, and anti-inflammatory properties.

(31) Andiroba oil is one of the most commonly sold medicinal oils in the Amazon. Mixed with honey and copaiba oil, andiroba oil is a very popular anti-inflammatory medication used to treat throat infections and influenza. Andiroba oil also strengthens and embellishes hair, and when used in soap andiroba oil acts as a remedy for acne. Due to andiroba oil's enhanced skin penetration, andiroba oil is often used in massages to relieve bruises, dislocations, arthritis and rheumatism, as well as to sooth the surface of the skin and to bleach superficial stains.

(32) In an example, the fatty acid composition of the andiroba oil is illustrated below in Table 4.

(33) TABLE-US-00004 TABLE 4 Fatty acid composition of the andiroba oil Fatty Carbon Acids Atoms Composition % Myristic 14:00 0.3300 Palmitic 16:00 28.0300 Stearic 18:00 8.6900 Oleic 18:10 49.0800 Linoleic 18:20 11.0300 Linolenic 18:30 1.3500 Arachidic 20:00 0.2200 Behenic 22:00 0.3400

(34) Copaiba Balsam

(35) Copaiba balsam is extracted from the bark of the Copaifera officinalis Jacq. tree, where copaiba balsam accumulates in cavities within the tree trunk. The chemical composition of the oil-resin of copaiba includes approximately 72 sesquiterpenes (hydrocarbons) and 28 diterpenes (carboxylic acids), and the oil is composed by about 50% of each of these terpenes. Diterpenes are attributed in the majority for therapeutic applications, a scientifically proven fact. Sesquiterpenes are partially responsible for the aroma of the oil-resin and also have antiulcer, antiviral, and anti-rhinovirus properties. Researchers have found that the oil-resin of copaiba exhibits anti-inflammatory effects; these anti-inflammatory effects may be higher than that found in pharmaceutical compositions comprising diclofenac sodium even by two folds.

(36) The inhabitants of the Amazon employ copaiba balsam as a topical treatment for wound healing, to stop bleeding, skin sores and psoriasis, all types of pain, skin disorders and for inflammation. Copaiba balsam may also have diuretic, antibacterial, expectorant, disinfectant, and stimulant properties, being the highest known natural source of caryophyllene, a well-known plant chemical that has been documented strong anti-inflammatory effects, among other therapeutically effects. In the cosmetic industry, copaiba balsam is used as a component of fragrance in perfumes and in cosmetics, such as, for example soaps and creams, because of its antimicrobial, anti-inflammatory, and emollient properties.

(37) Ucuuba Butter

(38) Ucuuba butter is obtained from the seeds of the Virola sebifera tree. Ucuuba butter includes high concentrations of lauric, myrist and palmitic acids, as well as vitamins C and A. It also accounts for 70% concentration of trimyristin, a triglyceride of myristic acid that is an aromatic essential oil largely used by the cosmetic, pharmaceutical and food industries.

(39) The inhabitants of the amazon have used ucuuba butter for the treatment of rheumatism, arthritis, colic, ulcers, and hemorrhoids. Amazonian fishers mix ucuuba butter with buriti oil, and spread all over their bodies; this mix helps to avoid sun burn and also protects the skin from dehydration. Also, some skin products produced employing ucuuba butter have shown anti-inflammatory, healing, and anti-septic properties. This butter may also aid in water retention in the skin, thereby helping to restore elasticity to the skin and improving mature skin appearance.

(40) In an example, the fatty acid composition of the ucuuba butter is illustrated below in Table 5.

(41) TABLE-US-00005 TABLE 5 Fatty acid composition of the ucuuba butter Fatty Carbon Acids Atoms Composition % Lauric 12:00 18.1700 Myristic 14:00 73.8400 Palmitic 16:00 8.0000

(42) Administration

(43) In some embodiments, the topical pharmaceutical bases are directly administered onto the affected area, in a dosage that varies according to the size or weight of the patient. In these embodiments, a single dose is enough to observe healing within the next 7 days after administration.

(44) In some embodiments, the topical pharmaceutical bases are in a dosage form selected from the group consisting of: pharmaceutically acceptable liquids, creams, oils, lotions, ointments, gels, roll-on liquids, skin patches, sprays, glass bead dressings, and synthetic polymer dressings, among others.

(45) In some embodiments, the topical pharmaceutical bases are applied manually with or without an applicator, such as, for example a dropper or pipette; an applicator, such as, for example a swab, brush, cloth, pad, roll-on device, and sponge, among others; or with any other applicator, such as, for example a solid support including paper, cardboard or a laminate material, including material with flocked, glued or otherwise fixed fibers, among others.

(46) In some embodiments, topical pharmaceutical compositions including the topical pharmaceutical bases increase the residence time of APIs within a wound or scar, thereby improving the penetration of APIs into the affected area. In these embodiments, the topical pharmaceutical bases provide relatively uniform distribution of the APIs within the topical pharmaceutical compositions. Further to these embodiments, the topical pharmaceutical compositions release APIs slowly, thereby enhancing treatment effectiveness.

(47) While various aspects and embodiments have been disclosed, other aspects and embodiments are contemplated. The various aspects and embodiments disclosed are for purposes of illustration and are not intended to be limiting, with the true scope and spirit being indicated by the following claims.