Sublingual oral spray for reducing the weight of a consumer

Abstract

The invention relates to a sublingual oral spray for reducing a consumer's weight and for use in obesity treatments, which is a liquid product stored under pressure in a spray device and dispensed as an aerosol, and which has a composition comprising orforglipron, purified water, glycerine, propylene glycol, ethanol, sodium citrate, sodium benzoate, and mint extract flavouring; and wherein, specifically, the product has a composition, expressed as a percentage of the total weight of the mixture, comprising: 4 - 9% orforglipron; 80 - 87.5% purified water; 4 - 6% glycerine; 2 - 4% propylene glycol; 2 - 4% ethanol; 0.30 - 2% sodium citrate; 0.10 - 1% sodium benzoate; and 0.10 - 10% mint extract flavouring.

Description

[0001] DESCRIPTION

[0002] Sublingual oral spray to reduce a consumer's weight

[0003] Object of the invention

[0004] The present invention relates to a new type of spray or liquid product that, stored under pressure, is projected outwards in the form of an aerosol, and is intended to be used to reduce or lower the weight of a consumer.

[0005] The invention falls within the scope of the industry related to the manufacture and marketing of dietary and pharmaceutical products to be used in patients with obesity and / or users who require weight loss.

[0006] Background of the invention

[0007] Obesity is a disease of increasing prevalence, for which there are few therapeutic and dietary tools available. Currently, in our setting, there are very few products approved for the treatment of this type of health problem, the best known being Orlistat and Metformin. Studies show that Orlistat offers better weight control than Metformin and diet and exercise, but Metformin is much more effective at metabolic control. For example, Orlistat does not suppress appetite, but rather reduces the number of calories absorbed in the intestine. These products are available in oral tablet form.

[0008] Similarly, it is known that glucagon-like peptide-1 (GLP-1) receptor agonists are used to help consumers achieve sustained glycemic control and facilitate weight loss. The usual approach to weight loss involves subcutaneous injections and oral tablets, combined with a balanced diet and exercise.

[0009] In contrast to these known treatments, the present invention introduces a new type of product, specifically a sublingual oral spray. Its main active ingredient is orforglipron, and it is designed to take advantage of the high bioavailability and rapid absorption offered by the oral mucosa, eliminating the need for daily injections or tablets. Sublingual administration of dietary and pharmaceutical products has proven to be an effective strategy for improving bioavailability, minimizing first-pass hepatic metabolism, and facilitating rapid systemic absorption. Administering compounds via routes other than oral or injectable has gained interest in recent decades due to its advantages in terms of bioavailability, tolerability, and treatment adherence.

[0010] In this regard, it is also known that orforglipron, a non-peptide agonist of the GLP-1 receptor, has demonstrated efficacy in the management of obesity and type 2 diabetes in its oral formulation in recent clinical studies. However, as with other oral treatments, its use is associated with some gastrointestinal side effects and the need for daily dosing, which can affect tolerance and adherence in certain patients, as seen in the recent study "Daily Oral GLP-1 Receptor Agonist Orforglipron for Adults with Obesity" (New England Journal of Medicine, 2024).

[0011] The applicant is unaware of any commercially available product containing orforglipron in the form of an oral spray intended for weight loss and / or to treat obesity. Specifically, the present invention seeks to provide effective doses of orforglipron. While injectable and oral tablet formulations containing this compound are known, no similar or advantageous pharmaceutical product as described and claimed below is known.

[0012] Explanation of the invention

[0013] The invention is a product to be used to reduce or lower a consumer's weight and which, in its different embodiments, solves the problems and limitations present in the state of the art previously raised.

[0014] The product of the present invention is a liquid composition stored under pressure in a spray device and projected externally as an aerosol. Its composition comprises orforglipron, purified water, glycerin, propylene glycol, ethanol, sodium citrate, sodium benzoate, and mint extract flavoring. More specifically, the product has a composition, expressed as a percentage of the total weight of the mixture, comprising:

[0015] 4-9% Orforglipron

[0016] 64 - 87.5% purified water

[0017] 4-6% Glycerin

[0018] 2-4% Propylene Glycol

[0019] 2-4% Ethanol

[0020] 0.30 - 2% Sodium Citrate

[0021] 0.10 - 1% Sodium Benzoate; and

[0022] 0.10 - 10% mint extract flavoring

[0023] where the

[0024] Orforglipron is the active ingredient in the composition; it acts on GLP-1 receptors to slow gastric emptying, promote satiety and weight loss, and combat obesity. It also has other effects, such as in the treatment of diabetes, as it is a compound that stimulates glucose-dependent insulin secretion and reduces glucagon release.

[0025] purified water acts as the base vehicle;

[0026] Glycerin improves adhesion to the mucosa and absorption;

[0027] Propylene glycol acts as a stabilizer and solubility enhancer;

[0028] Ethanol improves mucosal permeability;

[0029] Sodium citrate allows maintaining an optimal pH (around 6.8);

[0030] Sodium benzoate is an antimicrobial preservative; and

[0031] The natural flavoring of mint extract enhances the patient's sensory experience.

[0032] This formulation takes advantage of rapid absorption through the sublingual mucosa to provide sustained glycemic control. This active ingredient has been studied at different doses, ranging from 12 mg / day to 45 ml / day, with increasing weight loss results as the dose increases. However, after several studies, a single daily dose of 20 mg administered in four consecutive sprays (each 0.1 ml of product containing 5 mg of orforglipron), once a day, has been considered the most recommended dose. With this single daily dose, approximately 8-9% weight loss is achieved compared to the original weight prior to product use, and 20 mg of orforglipron has been shown to be sufficient to maintain therapeutic levels for 24 hours, thanks to its slow and prolonged elimination, preventing peaks and drops in concentration.The onset of action is approximately 15 minutes after sublingual administration, and the effect lasts for 24 hours. Furthermore, its slow elimination helps avoid concentration fluctuations, reducing the risk of adverse effects.

[0033] Also, for this specific dosage, studies have shown that commercially available oral capsules containing orforglipron, at a dose of 25 mg / day, undergo 50% first-pass hepatic metabolism, resulting in only half the dose reaching the bloodstream in its active form. In contrast, this product, in sublingual spray form at a dose of 20 mg / day, exhibits improved bioavailability of 70-80%, meaning a slightly lower dose than the oral form is sufficient to achieve higher therapeutic plasma levels. Therefore, sublingual bioavailability is estimated to be 30-70% higher than oral bioavailability. Given this higher sublingual bioavailability, as previously observed, the dose required to achieve plasma concentrations similar to those of the oral form should be lower, and gastrointestinal side effects are also reduced.

[0034] Regarding the product's advantages for the patient, it offers improved comfort, replacing injections with a quick and non-invasive oral application; it has better adherence, as the once-daily dosage has a pleasant taste; it is better assimilated by the body than oral compounds; and it is rapidly absorbed, with an effect in about 15 minutes thanks to the high sublingual vascularization. Specifically, it is more convenient to use, as it is non-invasive and easy to administer once a day; it has better bioavailability because it avoids first-pass metabolism; it is highly stable, allowing it to be stored at room temperature, and it contains no sensitive components; and it does not have common adverse effects such as irritation.In contrast, it is known that subcutaneous injections are painful, invasive, and require skill in self-injection by the patient; the speed of action depends on the subcutaneous depth of administration; they require stable storage in refrigerated vials or pre-filled devices; and they can cause local reactions at the injection site, such as pain or redness. It is also known that oral tablets are inconvenient, as daily intake can cause digestive discomfort; they have a slow speed of action because they pass through the digestive system and undergo first-pass metabolism; tablets are sensitive to humidity and temperature; and they can cause gastrointestinal discomfort.Furthermore, with regard to the manufacture and distribution of the product that is the subject of the present invention, there is the advantage of being a product with high acceptance among users who are looking for non-invasive alternatives; and as for the process of obtaining it, existing technologies in oral sprays are used.

[0035] As for the product, it is stored in a spray device, which comprises

[0036] a dark, light-resistant glass bottle with a capacity of at least 5 mL, for at least 10 doses;

[0037] an anatomical nozzle for precise sublingual administration of the product; an atomizing dispenser, calibrated to dispense 0.1 mL per spray; and

[0038] It may include a label with clear instructions for use and storage warnings.

[0039] Regarding the application of the product:

[0040] The preparation involves gently shaking the bottle before use and removing the protective cap;

[0041] The application involves placing the nozzle under the tongue and administering 5 consecutive sprays; and

[0042] Storage is based on keeping the device at room temperature (15-25 °C), protected from light and heat.

[0043] It should be noted that, throughout the description and claims, the term includes and its variants are not intended to exclude other technical features or additional elements.

[0044] Brief description of the figures

[0045] In order to complete the description and to aid in a better understanding of the characteristics of the invention, some figures or drawings are presented which, for illustrative and non-limiting purposes, represent the following:

[0046] Figure 1: Shows a schematic view of the sublingual oral spray for weight reduction of a consumer, the subject of the present invention, where it can be seen that the composition comprising Orforglipron, purified water, Glycerin, Propylene glycol, Ethanol, Sodium citrate, Sodium benzoate; and mint extract flavoring, is stored in a spray device, comprising a dark light-resistant glass bottle (1); an anatomical nozzle (2) for precise administration of the product; an atomizing dispenser (3); and a label (4) where information and instructions for dispensing the product are included.

[0047] Figure 2: Shows a graph where the results of % weight loss with respect to the original weight before the use of the spray that is the subject of the present invention are observed, and where specifically the results are observed for a dose of 12 mg / day, which was the initial dose used to evaluate tolerability in the participants, and which has an effectiveness of 5.2% in weight loss; 24 mg / day, which was the intermediate dose that allows observing significant metabolic responses, with a result of 9.4% weight loss; 36 mg / day, an increased dose that shows greater efficacy in weight loss, with a result of 12.3% weight loss; and 45 mg / day, which is the highest dose evaluated, which has achieved the greatest effectiveness in the reduction of body weight, with a value of up to 14.7% weight loss with respect to the original weight of the consumer.

[0048] Detailed explanation of a mode of implementation of the invention

[0049] A preferred embodiment of the invention consists of a liquid product that is stored under pressure in a spray device and is projected outward as an aerosol, comprising a 10 mL dark, light-resistant glass bottle (1) intended for 20 doses; an anatomical nozzle (2) for precise sublingual administration of the product; an atomizing dispenser (3) calibrated to dispense 0.1 mL per spray; and a label (4) including instructions for use of the product and storage warnings, wherein the composition of the product is such that a daily dose of 0.5 mL of the product comprises 20 mg of Orforglipron; 0.025 mL of glycerin (5% of the dose); 0.015 mL of propylene glycol (3% of the dose); 0.015 mL of ethanol (3% of the dose); 0.005 of Sodium Citrate (1% of the dose; 0.001 mL of Sodium Benzoate (0.2% of the dose); 0.025 mL of mint flavoring; and the rest of the product up to 100% of the dose of purified water as the base vehicle.

[0050] As previously mentioned, studies have shown that this formulation, with an active ingredient at a dose of 20 mg / day, has a bioavailability of 70-80%, compared to 50% in oral tablets. This means that sublingual bioavailability is 30-70% higher than oral bioavailability, resulting in a lower dose required to achieve plasma concentrations similar to those of the oral form. Furthermore, it reduces the gastrointestinal side effects that can occur with oral tablets. Additionally, as shown in Figure 2, this single daily dose results in approximately 8-9% weight loss relative to the original weight before starting the product.

Claims

CLAIMS 1.~ Sublingual oral spray for reducing a consumer's weight, characterized in that it is a product in a liquid state that is stored under pressure in a spray device and is projected outwards in the form of an aerosol, and that has a composition comprising Orforglipron, purified water, Glycerin, Propylene glycol, Ethanol, Sodium citrate, Sodium benzoate; and mint extract flavoring.

2. A spray according to claim 1, wherein the product has a composition, expressed as a percentage of the total weight of the mixture, comprising: 4-9% Orforglipron 64 - 87.50% purified water 4-6% Glycerin 2-4% Propylene Glycol 2-4% Ethanol 0.30 - 2% Sodium Citrate 0.10 - 1% Sodium Benzoate; and 0.10 - 10% mint extract flavoring 3.- A spray, according to claim 1, wherein the spraying device comprises a dark light-resistant glass bottle (1); an anatomical nozzle (2) for sublingual administration of the product; and an atomizing dispenser (3).

4. A spray, according to claim 3, wherein the bottle (1) has a capacity of at least 5 mL, 5. A spray, according to claim 3, wherein the atomizer dispenser (3) is calibrated to dispense 0.1 mL per spray 6. Use of a spray according to any of the preceding claims for the treatment of obesity.

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