GR1010882B - Methodology for the preparation of a specialized pharmaceutical pilocarpine toothpaste for dry mouth treatment - Google Patents

Abstract

The invention concerns the methodology and production process for the production of a specialized pharmaceutical toothpaste for topical use containing the active substance pilocarpine (cholinergic agonist) and aims to control and treat the condition of dry mouth, as well as to prevent oral cavity diseases (dental plaque, caries, etc.). The advantage of this invention is that pilocarpine toothpaste constitutes a pharmaceutical solution that will meet the modern needs of the dentist to combat dry mouth, compared to current therapeutic approaches (tablets, capsules), contributing in combination to a significant increase in saliva production, a reduction in the required daily use preparations and undesirable side effects from the systematic administration of cholinergic agonists, while at the same time improving overall oral hygiene, offering a pleasant taste, ease of use and better quality of health for the dental patient.

Description

[0001] DESCRIPTION

[0003] METHODOLOGY FOR PREPARING A SPECIALIZED PHARMACEUTICAL PILOCARPINE TOOTHPASTE AND THE PRODUCT PRODUCED THEREFORE FOR TREATING XEROMOUTH

[0005] The invention relates to the methodology for preparing toothpaste, as well as to the product produced thereby for the treatment of xerostomia, i.e. the feeling of dryness in the mouth which is mostly due to reduced function of the salivary glands and reduced saliva production.

[0007] The specific methodology used for the preparation of the toothpaste gives the product in question an advantage over other products aimed at controlling and treating dry mouth, as the innovative methodology results in a treatment for dry mouth in the form of pilocarpine toothpaste without the undesirable side effects observed in other therapeutic approaches (mechanical, chemical or pharmaceutical stimulation) through the systematic administration of cholinergic agonists, usually in the form of tablets or capsules, which cause significant problems in patients (excessive sweating, lacrimation, anxiety, etc.).

[0009] Consequently, the said invention concerns the development of an innovative product for topical use in the form of a specialized pharmaceutical toothpaste, which contains the active substance pilocarpine, a cholinergic agonist, which offers combined relief from the symptoms of dry mouth, prevention against diseases of the oral cavity (dental plaque, caries, etc.), improvement of oral hygiene and reduction of undesirable side effects caused by the systematic per os administration of the substance.

[0011] First, for the preparation of the product, analytical methods and techniques were developed for the chemical and physicochemical analysis of the raw materials (except the active substance) and the intermediate product, namely the cosmetic base (toothpaste), which include the use of ultraviolet/visible spectroscopy, Fourier transform infrared, Raman and NIR, high-pressure liquid chromatography, thermogravimetric analysis, differential scanning calorimetry, X-ray diffraction, polarized optical microscopy and scanning electron microscopy with a detector for the quantification of inorganic elements.

[0013] Subsequently, the necessary pre-formulation studies of the base were conducted, from which all the necessary ingredients were determined, including both substances useful for creating an effective toothpaste to ensure the patient's oral hygiene, such as compounds used against caries, plaque, tartar, antimicrobial substances, abrasive substances, as well as specialized substances that show significant effects in combating dry mouth. The ingredients selected based on their chemical and physicochemical characteristics, i.e. solubility, crystal structure, thermal properties, as well as their chemical compatibility, are glycerin, sodium lauryl sulfate, 2-Pyrrolidone 1-ethenyl Homopolymer, polyacrylic acid, sodium tripolyphosphate, sodium saccharin, silicon oxide, calcium carbonate, cocamidopropyl betaine, mint extract and sodium fluoride. For the above substances, a thorough check of the chemical and physicochemical characteristics of pilocarpine was carried out, from which its compatibility with the aforementioned ingredients at the stage of formulation of the cosmetic base was obtained. Thus, the resulting production formula is as follows:

[0015]

[0017] For the incorporation/encapsulation of pilocarpine in a suitable drug delivery system, with the ultimate goal of incorporating it into the cosmetic base of the pharmaceutical toothpaste, the preparation of a gel was preferred, which constitutes the base for the toothpaste and the vehicle for transporting pilocarpine to the oral cavity, while simultaneously maintaining all the desired organoleptic characteristics (taste, odor, texture, color, mouthfeel, etc.) of the final formulation.

[0019] In particular, the production process for preparing the toothpaste is as follows:

[0021] - Weighing of raw materials

[0022] - Sieving the solids to remove any impurities and break up any agglomerates.

[0023] - Addition to the glycerin production vessel

[0024] - Addition under stirring and simultaneous operation of the homogenizer and stirring of 2-Pyrrolidone, 1-Ethenyl- Homopolymer

[0025] - Stir until completely dissolved

[0026] - Addition under conditions of vigorous stirring and simultaneous operation of the homogenizer of the polyacrylic acid, sodium tripolyphosphate and sodium saccharin.

[0027] - Stir until completely dissolved

[0028] - Addition under gentle stirring in this order and with vacuum aspiration of the silicon oxide and calcium carbonate.

[0029] - Apply vacuum and continue stirring until a homogeneous cream is formed

[0030] - Addition under simultaneous stirring of the sodium lauryl sulfate and the cocamidopropyl betaine.

[0031] - Add under simultaneous stirring and operation of the homogenizer until the mint and sodium fluoride are completely incorporated.

[0032] - Pre-dissolution of the active raw material pilocarpine in glycerin.

[0033] - Adding the solution of the active raw material to the production vessel, where the initial product is contained, under gentle stirring and application of vacuum.

[0034] - Filling into tubes.

Claims (4)

1. CLAIMS 1. The methodology for the preparation of a pharmaceutical toothpaste containing the active substance pilocarpine for the treatment of dry mouth, which method includes the following steps: - Weighing of raw materials - Sieving of solids to remove any impurities and break up any agglomerates. - Addition to the glycerin production tank - Addition under stirring and simultaneous operation of the homogenizer and stirring of 2-Pyrrolidone, 1-Ethenyl- Homopolymer - Stir until completely dissolved - Addition under conditions of vigorous stirring and simultaneous operation of the homogenizer of polyacrylic acid, sodium tripolyphosphate and sodium saccharin. - Stir until completely dissolved - Add under gentle stirring in this order and with vacuum aspiration of the silicon oxide and calcium carbonate - Apply vacuum and continue stirring until a homogeneous cream is formed - Add, while stirring, the sodium lauryl sulfate and the cocamidopropyl betaine. - Add while stirring and operating the homogenizer until the mint and sodium fluoride are completely incorporated. - Pre-dissolution of the active ingredient pilocarpine in glycerin. - Adding the solution of the active raw material to the production vessel, where the initial product is contained, under gentle stirring and application of vacuum - Filling into tubes. The methodology according to claim 1, wherein the preparation of a gel/gel was chosen for incorporating pilocarpine into a suitable drug delivery system. 3. Toothpaste preparation containing the active substance pilocarpine for the treatment of dry mouth. 4. The toothpaste formulation according to claim 3, wherein it reduces the undesirable side effects caused by the systemic per os administration of the active substance.