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BR-102020021170-B1 - COMPOSITION, ORAL FORMULATIONS AND USE

BR102020021170B1BR 102020021170 B1BR102020021170 B1BR 102020021170B1BR-102020021170-B1

Abstract

COMPOSITION, ORAL FORMULATIONS AND USE. The present invention relates to a composition and oral formulations in the form of a varnish comprising active ingredients of natural origin. A further object of the present invention is its use in the preparation of a medicament for the control of biofilms, hypersensitivity and dental erosion. The area of application of the present invention is dentistry.

Inventors

  • ALINE ROGÉRIA FREIRE DE CASTILHO
  • REGINA MARIA PUPPIN RONTANI

Assignees

  • UNIVERSIDADE ESTADUAL DE CAMPINAS - UNICAMP

Dates

Publication Date
20260317
Application Date
20201015

Claims (7)

  1. 1. Dental composition characterized by comprising: - 1.5% to 4.5% theobromine; - 1.5% to 4.5% farnesol; - 1.5% to 4.5% quercetin; - pharmaceutically acceptable excipients; and - pharmaceutically acceptable vehicles.
  2. 2. Composition according to claim 1, characterized in that the excipients may be selected from: - 1% selected from CMC (carboxymethylcellulose), hydroxyethylcellulose, gelatin, gums, carbomer, preferably gelatin; - 0.05% to 0.1%, preferably 0.05% of preservatives selected from methylparaben, propylparaben, ethylparaben, butylparaben, benzoic acid, sodium benzoate, preferably methylparaben; - 3% to 7%, preferably 5%, selected from glucose, sucrose, mannitol, saccharin, sodium cyclamate, aspartame, preferably sorbitol; - 8% to 12%, preferably 10%, selected from lanolin, paraffin, petrolatum, preferably petrolatum; - 20% to 30%, preferably 30%, selected from polyethylene glycol (PEG), rosin, preferably Polyethylene Glycol (PEG); and distilled water QSP (sufficient quantity).
  3. 3. Dental formulation, as defined in claims 1 to 2, characterized by comprising: - 1.5% theobromine; - 1.5% farnesol; - 1.5% quercetin; - 1% gelatin; - 0.05% methylparaben; - 5% sorbitol; - 10% petrolatum; - 30% polyethylene glycol (PEG); and - distilled water QSP (quantity sufficient).
  4. 4. Dental formulation as defined in claims 1 to 2 characterized by comprising: - 4.5% theobromine; - 4.5% farnesol; - 4.5% quercetin; - 1% gelatin; - 0.05% methylparaben; - 5% sorbitol; - 10% petrolatum; - 30% polyethylene glycol (PEG); and - distilled water QSP (quantity sufficient).
  5. 5. Use of the composition as defined in claims 1 to 2, characterized by being in the preparation of a medicament for the control of biofilms, hypersensitivity and dental erosion.
  6. 6. Use of the formulation as defined in claim 3, characterized by being in the preparation of a medicament for the control of biofilms, hypersensitivity and dental erosion.
  7. 7. Use of the formulation as defined in claim 4, characterized by being in the preparation of a medicament for the control of biofilms, hypersensitivity and dental erosion.

Description

Field of invention [001] The present invention relates to an oral composition and formulations in the form of a varnish comprising active ingredients of natural origin. A further object of the present invention is its use in the preparation of a medicament for the control of biofilms, hypersensitivity and dental erosion. [002] The field of application of the present invention is dentistry. Fundamentals of the invention: [003] Dental caries, the most prominent biofilm-dependent pathology in the population, has a high prevalence and causes severe damage to the stomatognathic system (Pitts et al., 2017). Basically, the pathogenesis of caries involves different groups of bacteria, with the presence of mutans group streptococci and lactobacilli being particularly relevant, as they predominantly produce lactic acid and are responsible for the establishment and development of the carious lesion, respectively (Struzycka, 2014). [004] Since the initial adhesion of Streptococcus mutans is dependent on sucrose, a substrate from the diet, for the formation of cariogenic biofilm (Pitts et al., 2017), the use of formulations capable of altering polysaccharide production can prevent the accumulation of acidogenic microorganisms on the tooth surface (Bowen et al., 2018). [005] Considered abundant sources of bioactive compounds, natural products and their derivatives are currently indicated as the most successful strategy in the development of therapeutic agents (Castilho et al., 2007; Pereira et al., 2016). For this reason, natural compounds have been widely explored in the pharmaceutical industry in search of therapeutic protocols with excellent antimicrobial activity and safety for health (Newman & Cragg, 2016; Guo, 2017). Flavonoids comprise an extensive group of phenolic secondary metabolites widely available in plants and foods, whose chemical structure includes two phenol rings linked by three carbons (Koes, 1994). [006] Flavonoids exhibit a wide range of biological properties, including antibacterial, antiprotozoal, anti-inflammatory, antioxidant, estrogenic, and vascular activities (Crozier et al., 2009). Among the various flavonoids cited in the literature, quercetin (3,3′,4′,5,7-pentahydroxyflavone) stands out as a potent antioxidant and anti-inflammatory (Guan et al., 2012; Orsolic et al., 2013; Napimoga et al., 2013). [007] trans-trans-farnesol (tt-farnesol, 3,7,11-trimethyl-2,6,10-dodecatrien-1-ol), in turn, is a sesquiterpene alcohol found in essential oils of citrus fruits, used in the cosmetic industry due to its aroma (Koo et al., 2002b). Biologically, this terpenoid promotes the inhibition of acid production and glucan synthesis by S. mutans (Koo et al., 2003, 2005), in addition to apparently modifying the permeability and fluidity of the bacterial cell membrane, thus reducing the secretion of GTFs (Koo, Jeon, 2009). In addition to the antimicrobial activity of tt-farnesol (Castilho et al., 2019), anti-inflammatory and antitumor activities are also reported in the literature (Jung et al., 2018). [008] On the other hand, theobromine (3,7-dimethylxanthine), a compound belonging to the xanthine family, plays an important role in the dental remineralization process, acting as a moderator of the dissolution of calcium, phosphate, and magnesium (Amaechi et al., 2013). This characteristic inherent to theobromine is of great value in initial caries processes (white spot lesions), since it can optimize the reduction of enamel mineral loss during cariogenic challenge (Amaechi et al., 2013). [009] In dentistry, dental gels and varnishes are widely used strategies for the topical application of fluoride in order to control dental caries (Mishra et al., 2017). Generally prepared in alcohol bases, these formulations dry very quickly when applied to tooth surfaces, exhibiting strong adhesion to the tooth structure, allowing for the continuous and slow release of the active ingredient (Cardoso et al., 2014). Another advantage of this vehicle is that it depends less on patient cooperation (Mishra et al., 2017). [0010] Despite the considerable body of scientific evidence regarding the antimicrobial potential of compounds of natural origin, an effective delivery vehicle has not yet been developed that is less dependent on patient cooperation, safe, and capable of maintaining adequate salivary levels of the antimicrobial active ingredient in the oral cavity, reducing the metabolism and growth of cariogenic microorganisms and at the same time exhibiting remineralizing potential. [0011] Due to the biological properties of natural compounds, the characterization of formulations for the control of dental caries and remineralization of initial lesions, containing different active ingredients, is a relevant alternative in Dentistry. However, the use of new preventive materials based on bioactive compounds must involve not only the ability to inhibit cariogenic microorganisms but also the ability to be biologically acceptable and a