MOUTH ULCER TREATMENT GEL FORMULATION AND RELATED METHODS

Abstract

ABSTRACT A mouth gel formulation is designed for the treatment of mouth ulcers, incorporating Carbopol 934P polymer, lignocaine hydrochloride, gallic acid, propylene glycol, and preservatives. The formulation aims to alleviate irritation from food materials and prevent severe conditions associated with mouth ulcers, such as carcinogenicity. The preparation method involves soaking Carbopol 934P in water, mixing with lignocaine hydrochloride and gallic acid in propylene glycol, and adding preservatives to form a drug mixture. The mixture is then combined with the Carbopol solution and adjusted to the desired pH with triethanolamine to achieve gel consistency.

Specification

Description:TECHNICAL FIELD
[0001] The invention relates to a pharmaceutical formulation designed to enhance the healing process of mouth ulcers by providing a protective gel that reduces irritation and inflammation.

BACKGROUND
[0002] Mouth ulcers, also known as canker sores, are a common oral health issue that can cause significant discomfort and pain. These ulcers can be triggered by a variety of factors, including stress, injury, food sensitivities, and underlying health conditions. The healing process for mouth ulcers is often slow, primarily due to the constant irritation from food and beverages, which can exacerbate pain and inflammation. This persistent irritation not only prolongs healing but can also lead to more severe complications if not managed effectively.
[0003] The management of mouth ulcers typically involves the use of topical treatments to alleviate pain and promote healing. However, many existing treatments may not provide adequate protection against the continuous exposure to irritants, leading to prolonged discomfort for the patient. There is a need for more effective formulations that can offer both pain relief and a protective barrier to enhance the healing process. Such advancements could significantly improve the quality of life for individuals suffering from recurrent mouth ulcers and reduce the risk of complications associated with chronic inflammation.

SUMMARY
[0004] In accordance with embodiments, a mouth gel formulation is provided for treating mouth ulcers. The formulation comprises a Carbopol 934P polymer in an amount ranging from about 0.5% to about 2% by weight of the total formulation, lignocaine hydrochloride in an amount of 2% w/v, gallic acid in an amount of 3% w/v, propylene glycol in an amount ranging from about 5% to about 15% by weight of the total formulation, and preservatives in an amount ranging from about 0.05% to about 1% by weight of the total formulation.
[0005] In accordance with other embodiments, the mouth gel formulation includes the Carbopol 934P polymer present in an amount of about 1% by weight of the total formulation.
[0006] In yet other embodiments, the mouth gel formulation includes propylene glycol present in an amount of about 10% by weight of the total formulation.
[0007] In further embodiments, the mouth gel formulation includes preservatives comprising methyl parabens and propyl parabens.
[0008] In additional embodiments, the mouth gel formulation includes methyl parabens present in an amount ranging from about 0.1% to about 0.3% by weight of the total formulation and propyl parabens present in an amount ranging from about 0.01% to about 0.1% by weight of the total formulation.
[0009] In accordance with other embodiments, the mouth gel formulation has a volume of about 50 ml.
[0010] In yet other embodiments, the mouth gel formulation avoids irritation from food material.
[0011] In further embodiments, the mouth gel formulation prevents severe conditions associated with mouth ulcers, wherein the severe conditions include carcinogenicity.
[0012] In accordance with embodiments, a method of preparing a mouth gel formulation for treating mouth ulcers is provided. The method comprises soaking a Carbopol 934P polymer in water, wherein the Carbopol 934P polymer is present in an amount ranging from about 0.5% to about 2% by weight of the total formulation, mixing the Carbopol 934P polymer with a mechanical stirrer to prevent lump formation, adding lignocaine hydrochloride in an amount of 2% w/v and gallic acid in an amount of 3% w/v to propylene glycol, wherein the propylene glycol is present in an amount ranging from about 5% to about 15% by weight of the total formulation, adding preservatives to the lignocaine hydrochloride and gallic acid mixture to form a drug mixture, wherein the preservatives are present in an amount ranging from about 0.05% to about 1% by weight of the total formulation, adding the drug mixture to the Carbopol 934P polymer mixture with constant stirring to form the mouth gel formulation, and adjusting the pH of the mouth gel formulation with triethanolamine to achieve a gel consistency.
[0013] In additional embodiments, the method includes soaking the Carbopol 934P polymer in water overnight in an amount of about 1% by weight of the total formulation, the propylene glycol is present in an amount of about 10% by weight of the total formulation, and the preservatives comprise methyl parabens in an amount ranging from about 0.1% to about 0.3% by weight of the total formulation and propyl parabens in an amount ranging from about 0.01% to about 0.1% by weight of the total formulation.


BRIEF DESCRIPTION OF THE DRAWINGS
[0014] FIG. 1 illustrates, in a flowchart, the process of formulating a mouth gel using specific ingredients and methods.
[0015] FIG. 2 illustrates in-vitro release profile.

DETAILED DESCRIPTION
[0016] In the formulation of a mouth gel for treating mouth ulcers, a variety of components may be utilized to achieve the desired therapeutic and physical properties. The Carbopol 934P polymer may be employed as a gelling agent, which can be soaked in water to facilitate its dispersion and prevent lump formation. This process may be enhanced by the use of a mechanical stirrer, which can ensure uniformity in the gel formulation. The addition of triethanolamine may be used for adjusting the pH, thereby achieving a gel-like consistency suitable for the application of the gel.
[0017] Lignocaine hydrochloride and gallic acid may be incorporated into the formulation to provide analgesic and antioxidant properties, respectively. These components may be mixed with propylene glycol, which can act as a solvent and humectant, aiding in the solubilization and stability of the active ingredients. The preservatives, including methyl parabens and propyl parabens, may be added to the formulation to prevent microbial growth, thereby extending the shelf life of the product.
[0018] The process of combining these ingredients may involve constant stirring to ensure a homogeneous mixture. The final mixture may be adjusted to a specific volume with water, and the pH may be fine-tuned with triethanolamine to achieve the desired consistency. This formulation process may be designed to address the slow healing rate of mouth ulcers by providing a protective barrier that minimizes irritation from food materials, potentially preventing severe conditions such as carcinogenicity. The formulation may be evaluated for its drug release profile to ensure effective delivery of the active ingredients.
[0019] FIG. 1 is a flowchart illustrating a method in step 100 for preparing a mouth gel formulation for treating mouth ulcers, according to an embodiment. At step 100, the process may begin with the soaking of Carbopol 934P in water. This action may involve the use of Carbopol 934P polymer, which may be soaked overnight in water to ensure proper hydration and preparation for subsequent mixing. The soaking process may be important for achieving the desired consistency and effectiveness of the gel formulation. The Carbopol 934P polymer may be present in an amount of about 1% by weight of the total formulation, which may be necessary for maintaining the structural integrity and viscosity of the gel. This step may be followed by the mixing of the soaked Carbopol 934P with a mechanical stirrer to prevent lump formation, ensuring a smooth and uniform gel base. The mechanical stirring may facilitate the even distribution of the polymer within the aqueous medium, which may be vital for the stability and homogeneity of the final product. The preparation of the mouth gel formulation may be further enhanced by the addition of lignocaine hydrochloride and gallic acid to propylene glycol, which may serve as a solvent and stabilizer. The propylene glycol may be present in an amount of about 10% by weight of the total formulation, which may contribute to the solubilization of active ingredients and the overall texture of the gel. The incorporation of preservatives, such as methyl parabens and propyl parabens, into the lignocaine hydrochloride and gallic acid mixture may form a drug mixture that may be added to the Carbopol 934P polymer mixture with constant stirring. This action may ensure the preservation and efficacy of the formulation by preventing microbial growth and degradation. The preservatives may be present in specific amounts to achieve optimal preservation without compromising the safety and effectiveness of the gel. The final step in the preparation process may involve adjusting the pH of the mouth gel formulation with triethanolamine to achieve a gel consistency. This adjustment may be necessary to ensure the gel's stability and compatibility with the oral environment, enhancing its therapeutic potential for treating mouth ulcers. The pH adjustment may also play a role in optimizing the release and activity of the active ingredients within the gel matrix.
[0020] In the context of the mouth gel formulation process, step 102 may involve the mixing of the Carbopol 934P polymer with a mechanical stirrer. This action may be important to prevent the formation of lumps, which can ensure a uniform consistency in the gel. The mechanical stirrer may facilitate the even distribution of the polymer particles within the mixture, potentially enhancing the overall quality and effectiveness of the mouth gel. The use of a mechanical stirrer may be seen as a method to achieve a homogeneous mixture, which can be necessary for the subsequent steps in the formulation process. This step may be integral to the preparation of the mouth gel, as it may lay the foundation for the addition of other components, such as lignocaine hydrochloride and gallic acid, in later stages. The prevention of lump formation may also contribute to the stability and efficacy of the final product, as a smooth gel consistency may be more desirable for application and therapeutic purposes.
[0021] In the process of formulating the mouth gel, lignocaine hydrochloride and gallic acid may be added to propylene glycol. This step may involve the careful measurement of lignocaine hydrochloride at a concentration of 2% w/v and gallic acid at 3% w/v, which may then be combined with propylene glycol. The propylene glycol may be present in an amount of about 10% by weight of the total formulation. This combination may be achieved through constant stirring to ensure a homogeneous mixture. The addition of these components may serve to integrate the active ingredients into the gel matrix, potentially enhancing the therapeutic efficacy of the formulation. The lignocaine hydrochloride may provide local anesthetic effects, while the gallic acid may contribute to the overall stability and effectiveness of the gel. The propylene glycol may act as a solvent and humectant, facilitating the dispersion of the active ingredients and maintaining the moisture content of the gel. This step may be important in ensuring that the active ingredients are evenly distributed throughout the gel, which may be necessary for the consistent delivery of therapeutic effects when applied to mouth ulcers.
[0022] In the context of the mouth gel formulation process, the step involves the addition of preservatives to a mixture containing lignocaine hydrochloride and gallic acid to form a drug mixture. This step may be important in ensuring the stability and preservation of the active ingredients within the formulation. The preservatives, which may include methyl parabens and propyl parabens, are potentially added in specific concentrations to achieve the desired preservation effect. The methyl parabens may be present in an amount ranging from about 0.1% to about 0.3% by weight of the total formulation, while the propyl parabens may be present in an amount ranging from about 0.01% to about 0.1% by weight of the total formulation. This precise addition may help in maintaining the efficacy and safety of the mouth gel over time. The process of combining these components with constant stirring may ensure a uniform distribution of the preservatives throughout the mixture, which may be necessary for the consistent performance of the mouth gel. The integration of these components may also contribute to the overall formulation preparation, aligning with the intended purpose of treating mouth ulcers. The careful selection and incorporation of these preservatives may play a role in the formulation's ability to prevent severe conditions associated with mouth ulcers, such as carcinogenicity, by maintaining the integrity and effectiveness of the active ingredients.
[0023] In the context of step 108, the process may involve the integration of the drug mixture with the Carbopol 934P polymer mixture, potentially under continuous stirring, to facilitate the formation of the mouth gel formulation. The drug mixture, which may include lignocaine hydrochloride, gallic acid, and preservatives such as methyl parabens and propyl parabens, can be combined with the pre-prepared Carbopol 934P polymer mixture. This action may be important in ensuring the homogeneity and consistency of the gel formulation. The continuous stirring may serve to maintain uniform distribution of the components, thereby enhancing the stability and efficacy of the mouth gel. The formulation process may be designed to address the treatment of mouth ulcers by leveraging the therapeutic properties of the included active ingredients. The integration of these components may be aimed at achieving a gel consistency that is suitable for application, potentially providing relief from the symptoms associated with mouth ulcers. The process may also involve considerations for the preservation of the formulation, ensuring its longevity and effectiveness.
[0024] In the context of the mouth gel formulation process, the step of adjusting the pH of the mouth gel formulation with triethanolamine to achieve a gel consistency may be considered. This step may involve the careful addition of triethanolamine to the mixture, which may serve to modify the pH level of the formulation. The adjustment of pH is important as it may influence the gel-like consistency of the final product, ensuring that the formulation attains the desired texture and stability. The triethanolamine may interact with the other components of the formulation, such as the Carbopol 934P polymer, lignocaine hydrochloride, gallic acid, propylene glycol, and preservatives, to facilitate the formation of a stable gel matrix. This interaction may be necessary for the therapeutic efficacy of the mouth gel, as it may ensure the proper release and activity of the active ingredients. The process of pH adjustment may be conducted with precision to avoid any adverse effects on the formulation's performance. The potential for achieving a gel consistency through this method may highlight the role of triethanolamine in the formulation process, as it may contribute to the overall effectiveness and usability of the mouth gel for treating mouth ulcers.

EXAMPLES
Example 1: Mouth Gel Formulation for the Treatment of Mouth Ulcers

Ingredients Concentration
Carbopol 934P Polymer 0.5% to about 2%
Lignocaine Hydrochloride 2% w/v
Gallic Acid 3% w/v
Propylene Glycol 5% to about 15%
Methyl Paraben 0.05% to about 1% w/w
Propyl Paraben 0.05% to about 1% w/w
Triethanolamine q.s. to adjust pH
Water q.s. up to 100%

EXAMPLE 2- IN VITRO DRUG RELEASE STUDY
[0025] The in vitro drug release study was conducted to assess the release profile of the active ingredients, gallic acid and lignocaine hydrochloride, from the formulated mouth gel. The study utilized the dialysis bag diffusion method, where approximately 1 g of the gel, containing 30 mg of gallic acid and 20 mg of lignocaine hydrochloride, was placed inside a dialysis membrane with a molecular weight cut-off of 8-12 kDa. The membrane was immersed in 50 ml of Phosphate Buffered Saline (PBS, pH 6.8) and incubated at 37.5°C with constant stirring at 150 rpm. Samples were collected at specific intervals, and the release of the drugs was analyzed using High-Performance Liquid Chromatography (HPLC). Over a period of 2.5 hours, the gel demonstrated a gradual drug release, with approximately 86% of both active ingredients being released by the end of the study. The initial rapid release provided immediate therapeutic effects, followed by a sustained release, ensuring prolonged drug availability at the ulcer site. This controlled release profile, facilitated by the Carbopol 934P polymer matrix, makes the formulation effective for pain relief and enhanced healing of mouth ulcers. The same is shown in Fig 2.

EXAMPLE 3- STABILITY DATA FOR MOUTH GEL FORMULATION
Parameter Initial Accelerated (40°C/75% RH, 3 months) Real-Time (30°C/65% RH, 6 months) Long-Term (25°C/60% RH, 12 months)
Appearance Clear, homogenous gel No change No change No change
Viscosity (cps) 185,400 ± 1.78 183,000 ± 2.12 182,500 ± 2.04 181,700 ± 1.95
pH 6.87 ± 0.23 6.80 ± 0.15 6.82 ± 0.18 6.81 ± 0.20
Gallic Acid Content (%) 100 98.5 98.3 97.8
Lignocaine Content (%) 100 99.2 98.9 98.5
Microbial Contamination None detected None detected None detected None detected
In Vitro Drug Release (%) 86% in 2.5 hours 85.5% in 2.5 hours 85.2% in 2.5 hours 84.8% in 2.5 hours

[0026] The mouth gel formulation exhibited excellent physical, chemical, and microbial stability over the evaluated time periods and conditions, with only minimal changes in viscosity, pH, drug content, and release profile, all within acceptable limits. This confirms that the formulation is stable for at least 12 months under long-term storage conditions.

EXAMPLE 4- ORGANOLEPTIC EVALUATION DATA FOR MOUTH GEL FORMULATION
Parameter Evaluation Criteria Initial Observation After 3 Months (Accelerated Stability, 40°C/75% RH) After 12 Months (Long-Term Stability, 25°C/60% RH)
Appearance Visual clarity, color, homogeneity Clear, colorless, uniform gel No change No change
Odor Smell (neutral or pleasant) Neutral, mild odor No change No change
Texture Smoothness, absence of grittiness Smooth, non-gritty Smooth, non-gritty Smooth, non-gritty
Taste Acceptability, bitterness, sweetness Mildly bitter, acceptable No change No change
Spreadability Ease of application on mucosa Easily spreadable No change No change
Color Visual color assessment Colorless Colorless Colorless


, Claims:CLAIMS
We claim:
1. A mouth gel formulation for treating mouth ulcers, comprising:
a Carbopol 934P polymer in an amount ranging from about 0.5% to about 2% by weight of the total formulation;
lignocaine hydrochloride in an amount of 2% w/v;
gallic acid in an amount of 3% w/v;
propylene glycol in an amount ranging from about 5% to about 15% by weight of the total formulation; and
preservatives in an amount ranging from about 0.05% to about 1% by weight of the total formulation.

2. The mouth gel formulation as claimed in claim 1, wherein the Carbopol 934P polymer is present in an amount of about 1% by weight of the total formulation.

3. The mouth gel formulation as claimed in claim 1, wherein the propylene glycol is present in an amount of about 10% by weight of the total formulation.

4. The mouth gel formulation as claimed in claim 1, wherein the preservatives comprise methyl parabens and propyl parabens.

5. The mouth gel formulation as claimed in claim 4, wherein the methyl parabens are present in an amount ranging from about 0.1% to about 0.3% by weight of the total formulation and the propyl parabens are present in an amount ranging from about 0.01% to about 0.1% by weight of the total formulation.

6. The mouth gel formulation as claimed in claim 1, wherein the mouth gel formulation has a volume of about 50 ml.

7. The mouth gel formulation as claimed in claim 1, wherein the mouth gel formulation avoids irritation from food material.

8. The mouth gel formulation as claimed in claim 1, wherein the mouth gel formulation prevents severe conditions associated with mouth ulcers, wherein the severe conditions include carcinogenicity.

9. A method of preparing a mouth gel formulation for treating mouth ulcers, the method comprising:
soaking a Carbopol 934P polymer in water, wherein the Carbopol 934P polymer is present in an amount ranging from about 0.5% to about 2% by weight of the total formulation;
mixing the Carbopol 934P polymer with a mechanical stirrer to prevent lump formation;
adding lignocaine hydrochloride in an amount of 2% w/v and gallic acid in an amount of 3% w/v to propylene glycol, wherein the propylene glycol is present in an amount ranging from about 5% to about 15% by weight of the total formulation;
adding preservatives to the lignocaine hydrochloride and gallic acid mixture to form a drug mixture, wherein the preservatives are present in an amount ranging from about 0.05% to about 1% by weight of the total formulation;
adding the drug mixture to the Carbopol 934P polymer mixture with constant stirring to form the mouth gel formulation; and
adjusting the pH of the mouth gel formulation with triethanolamine to achieve a gel consistency.

10. The method as claimed in claim 9, wherein the Carbopol 934P polymer is soaked in water overnight in an amount of about 1% by weight of the total formulation, the propylene glycol is present in an amount of about 10% by weight of the total formulation, and the preservatives comprise methyl parabens in an amount ranging from about 0.1% to about 0.3% by weight of the total formulation and propyl parabens in an amount ranging from about 0.01% to about 0.1% by weight of the total formulation.

Dated this 29th October, 2024

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