Formulation and Evaluation of Herbal Tablet Dosage Form as a Slimming Product

The seeds of Syzygium cumini (L), widely recognized as Java plum or black jamun, are a significant indigenous species that originated in India and Indonesia. This species is commonly found in tropical and subtropical regions and is a member of the Myrtaceae family[1] India possesses a rich legacy of medicinal practices, supported by a diverse array of plant species that are crucial for the herbal remedies employed in various healthcare systems. This includes the Siddha and Unani systems, as well as other esteemed Indian medical traditions [2] Numerous pharmacological benefits of this herb are recognized, such as its antibacterial, anti-inflammatory, anti-obesity, and antioxidant properties. In traditional Ayurvedic medicine, different components of the plant, such as the bark, dried seeds, leaves, and fruits, have been utilized to treat various health concerns [3] Obesity is an escalating health issue worldwide, leading to a rising demand for safe and effective weight loss products. Herbal remedies, especially, have become more popular because of their perceived safety and effectiveness. Java plum seed powder, which is abundant in phytochemicals, has been traditionally utilized for its potential benefits in weight loss and anti-obesity effects. The powder made from Java plum seeds has been known to exhibit anti-obesity effects by reducing fat cell formation and promoting fat breakdown. Nonetheless, its effectiveness and bioavailability as a weight loss product are constrained because of its low solubility and stability. Enhancing the efficacy of strategies aimed at the prevention, management, and treatment of obesity has been prioritized within the framework of global public health Globally, there is a rising trend in the number of adults diagnosed with obesity. In 2020, it was estimated that there were 810 million cases, and projections suggest that this figure could escalate to 1.53 billion by 2035[4] The potential of jamun seeds as a new resource for the food and pharmaceutical industries is shown by an analysis of their nutritional and phytochemical characteristics. The health advantages of jamun seeds and their use as a component in the creation of functional foods are highlighted in this review. Furthermore, it discusses the safety aspects related to the consumption of jamun seeds, thereby promoting additional research focused on the development of various functional foods that can safely include jamun seeds or their extracts within permissible limits [5] Obesity, characterized by an excessive buildup of fat, especially in the abdominal area, results from an imbalance between energy intake and expenditure. A larger intake of meals high in energy density, a lower intake of foods high in micronutrients and bioactive substances, and a decrease in physical activity are some of the variables that contribute to this imbalance., and additional influences including early-life nutrition and hormonal factors, as well as genetic, cultural, environmental, and economic considerations. As a result, tackling obesity poses a complex health challenge. The detrimental effects of an unhealthy lifestyle on obesity development are well acknowledged. A diet high in fats and sugars, combined with inadequate physical activity, contributes to weight gain and, ultimately, obesity. Thus, dietary intervention is a vital component of lifestyle changes and is recognized as an effective approach to address obesity and its related health concerns. Specifically, increasing the intake of fruits and vegetables has been identified as an effective dietary strategy for reducing the risk of obesity-related diseases, such as cardiovascular diseases, cancer, and diabetes mellitus [6]

• Aim and Objectives:

Aim:

This study aims to develop and assess a herbal tablet formulation utilizing Java plum seed powder as a weight loss product, while also evaluating its effectiveness and safety in decreasing body weight and body mass index (BMI)^[7]

Objectives

Formulation of herbal tablets: To formulate herbal tablets using Java plum seed powder and other excipients, and to optimize the formulation to achieve desired physical and chemical characteristics.

1. Evaluation of physical and chemical characteristics: To evaluate the physical and chemical characteristics of the formulated tablets, including hardness, friability, disintegration time, and dissolution rate.
2. Stability studies: To ascertain the shelf-life and storage conditions of the prepared tablets, stability tests will be carried out.
3. Development of a herbal tablet dosage form that is stable and bioavailable. Assessment of the physical and chemical properties of the prepared tablets.
4. Evaluation of the effectiveness and safety of the prepared tablets in decreasing body weight and BMI.

• Need and Significance of Herbal Tablet Dosage Form:

The Need of Herbal Weight Loss Products ^[7]

1. Rising obesity prevalence: The global surge in obesity underscores the necessity for effective and safe weight loss alternatives.
2. Adverse effects of synthetic weight loss solutions: Man-made weight loss products may lead to detrimental side effects, including cardiovascular issues and psychological dependency.
3. Increasing demand for herbal alternatives: There is a growing consumer preference for natural and herbal weight management products, driven by their perceived safety and effectiveness.

The Significance of Herbal Weight Loss Products ^[7]

1. Practical and easily obtainable: Tablets provide a practical and readily available method of administration, making them especially appropriate for weight loss supplements.
2. Consistent dosing: Tablets provide a standardized dosage of the herbal extract, ensuring reliable effectiveness and safety.
3. Durability and longevity: Tablets exhibit a longer shelf-life and improved stability in comparison to other dosage forms, such as liquids or powders.

• Plan of work:

1. Literature survey.
2. Collection & Authentication of herbal ingredient
3. Selection of excipients.
4. Pre-evaluation parameters:

• Angle of repose
• Bulk density
• Tapped density
• Hausner’s ratio
• Compressibility index
• Percent Compressibility index

5. Formulation Development:

• Selection of manufacturing technique
• The direct compression method

6. Post-Evaluation Parameters:

• Weight of Tablet
• Hardness
• Friability
• Thickness
• Disintegration time
• pH Determination
• Dissolution time

• Drug and Excipient profile:

Plant profile:

1. Flavonoids ^[15]

The important class of naturally occurring polyphenolic compounds known as flavonoids is known for its anti-inflammatory, anti-allergic, anti-diabetic, and antioxidant qualities. Some flavonoid derivatives may also have antiviral effects. These compounds included myricetin rhamnoside, myrigalone-G pentoside, quercetin galloyl-pentoside, and cryptostrobin, ellagic acid and caffeic acid in the leaf extract, and the bark extract. Of the 28 chemicals found in the ethanolic extract of S. formosum leaves, 11 flavonoids, such as catechin, myricetin, and quercetin.

Quercetin

Myricetin

1. Phenols ^[15]

 S. cumini, exhibits a restricted range of phenolic compounds in its different parts, such as fruit extracts (particularly gallic acid), bark extracts (including 3,3-di-O-methyl ellagic acid and 3,3,4-tri-O-methyl ellagic acid), seed extracts (like ferulic acid), flower extracts, and leaf extracts (like ellagic acid and caffeific acid)

Tannins:^[15]

The polyphenolic macromolecules known as tannins have anti-inflammatory, anti-cancer, anti-nutritional, antioxidant, and cardioprotective properties. The methanol extract of S. aqueum leaves contained galloylquinic acid and other tannin components in trace amounts. In contrast, S. cumini contained very little tannin components in any of the plant's sections, including the leaf extract's nilocetin and corilagin in the seed extract like Hydrolysable tannins.

Hydrolysable Tannins

Terpenoids:^[15]                                

The hepatoprotective, anti-inflammatory, antibacterial, analgesic, and immunomodulatory properties of terpenoids are well-known. In different plant sections, S. cumini exhibited a restricted presence of triterpenoid chemicals.

Citronellol

Alkaloids:^[15]

Natural organic substances known as alkaloids are identified by the presence of at least one nitrogen atom. Many pharmacological characteristics, including antibacterial, anticancer, analgesic, antihyperglycemic, and antimalarial activities, are possessed by these substances. According to studies, S. cumini seeds contain the alkaloid jambosine, which has antidiabetic effects.

Quinine

Glycosides:^[15]

The formation of a glycosidic link between a sugar molecule and another functional group characterizes glycosides. A lot of plants store things as inactive glycosides. These substances have antihyperglycemic and antiarrhythmic actions, among other pharmacological effects. S. aromaticum flower buds have yielded a novel acetophenone, 2,4,6-Trihydroxy-3-methylacetophenone-2-O-β-d-glucoside. Jambolin, also known as antimellin, is a glycoside found in S. cumini seeds that prevents the enzymatic conversion of starch to sugar and has antidiabetic properties. Several chemicals have been found in various areas of S. species, such as S. polyanthum and S. cumini.

Anthraquinone

Drug profile:

Java Plum seed powder:

• Synonyms: Syzygium cumini, Jambolan, Black plum, Indian black berry, Jamun
• Biological source: Eugenia jambolana Lam/Syzygium jambolanum DC/Syzygium cumini (linn.) Skeels Syn. This fast-growing tree is found in Bangladesh, Pakistan, India and Shri-lanka
• Family: Myrtaceae
• Plant part used: Seed powder

Fig No. 1 Java Plum Seed Powder

• Scientific Classification ^[2]

Kingdom: Plantae

Unranked: Angiosperms

Unranked: Eudicots

Unranked: Rosids

Order: Myrtales

Family: Myrtaceae

Genius: Syzygium

Species: Cumini

Bionamial Name: Syzygium Cumini (L) Skeels

• Uses:

Because of its anti-inflammatory and antioxidant qualities, Java plum (Jamun) seed powder, which is derived from the seeds of the Syzygium cumini fruit, has long been used to help control blood sugar levels, enhance digestion, management of obesity, and promote general health.

Excipients:

• Lubricant
• Binder
• Disintegrant

METHODOLOGY:

Direct compression technique is applied to Herbal Tablet Dosage Form.

Procedure:

1. Collect and clean all the apparatus properly.
2. Determine the tablet composition of the herbal (Java Plum seed) powder, excipients and other additives.
3. Choose suitable excipients such as binder, lubricant, disintegrant (Methyl cellulose, Talc and Maize starch) to enhance the tablets physical and chemical properties.
4. Prepare the tablet mixture by mixing the herbal seed powder with the choosen excipients by using the mortar and pestle.
5. Pass the mixture through the sieve (size 60 no.)
6. Use a press to compress the tablet mixture into the tablet. By using the Tablet punching machine using 10nm dye.
7. Conduct physical test such as weight variation, thickness, hardness, friability and disintegration time to evaluate tablet physical properties.
8. Package the tablets into a suitable container and label the package with relevant information.

Fig No. 2 Tablet Punching Machine

• RESULT AND DISCUSSION:

1. Test for phytochemical constituents of the Herbal powder (Java Plum seed powder):

Benedict's test is used to detect the presence of reducing sugars, such as glucose, fructose, and sucrose, in the herbal powder. By looking for a reddish-brown tint or precipitate when heated, Millon's test, which is employed in phytochemical analysis of herbal tablets, finds proteins, particularly those that include the phenolic amino acid tyrosine.  Brontrager's test is used to detect the presence of saponins in herbal powders ^[10]

Batches of Herbal tablet dosage formulation:

• Batch no.:1 (F3)

The herbal tablet dosage form prepared by using this particular batch has not formulated or evaluated properly. The tablet prepared are breakable.

• Batch no.:2 (F9)

The herbal tablet dosage form prepared by using this particular batch has formulated properly but the evaluation of this dosage form are inaccurate its disintegration time and hardness is not in the given range.

• Batch no.:3 (F6)

 The herbal tablet dosage form prepared by using this particular batch has formulated and evaluated properly. The evaluation parameters of the herbal tablet dosage form by using this batch are accurate to the standard one.

Pre-evaluation studies:

For the above formulation we have concern the pre-evalution parameters of the API. We have taken the angle of repose by using the formula, ? = tan^-1(h/r). Bulk density  by using the formula, BD = Mass/Bulk volume. Tapped density by using formula, TD = Mass/Tapped volume. Compressibility index by using formula, CI= Tapped density-Bulk density/Tapped density. Also, we have concern the % compressibility index by using formula, %CI =CI × 100 and also, the Hausner’s ratio by using formula, HR =Tapped density/bulk density.

Angle of repose:

When a pile of powder is poured onto a level surface, the angle formed between the slope and the horizontal surface is known as the angle of repose. It is used to evaluate the flowability of granular materials and measures how easily a powder flows.

The angle of repose of the herbal powder is done for the formulation of the herbal tablet for several reasons:

Assessing Flowability, Predicting Tablet Quality, Determining Powder Characteristics, and Optimizing Tablet Formulation ^[12]

1. Bulk density:

The mass of a powder sample divided by its volume, which includes the interparticulate void volume between particles, is known as the bulk density.  The bulk density of the herbal powder is done for the formulation of the herbal tablet for several reasons: Assessing Powder Flowability, Determining Compressibility, Optimizing Tablet Formulation, and Predicting Tablet Quality ^[13]

2. Tapped density:

Tapped density refers to the density of a powder that has undergone a mechanical tapping method to compact its particles and minimize the spaces between them. The tapped density of the herbal powder is done for the formulation of the herbal tablet for several reasons: Assessing Powder Compressibility, Determining Powder Flowability, Optimizing Tablet Formulation, and Predicting Tablet Quality ^[14]

3. Compressibility index:

The Compressibility Index (CI), often referred to as Carr's Index, evaluates how a powder compresses when subjected to pressure and is derived from both bulk and tapped densities; smaller values signify improved flow characteristics, whereas larger values indicate less favorable flow properties. The compressibility index of the herbal powder is done for the formulation of the herbal tablet for several reasons: Assessing Powder Compressibility, Determining Powder Flowability, Optimizing Tablet Formulation, and Predicting Tablet Quality ^[15]

4. % Compressibility index:

The % compressibility index of the herbal powder is done for the formulation of the herbal tablet for several reasons: Assessing Powder Compressibility, Determining Powder Flowability, Optimizing Tablet Formulation, and Predicting Tablet Quality^[15]

5. Hausner’s ratio:

The Hausner ratio (HR) is a measure of powder flowability, calculated by dividing the tapped bulk density by the poured (loose) bulk density.  The Hausner's ratio of the herbal powder is done for the formulation of the herbal tablet for several reasons: Assessing Powder Flowability, Determining Powder Compressibility, Optimizing Tablet Formulation, and Predicting Tablet Quality ^[12]

The outcomes for the pre-evaluation parameter results are as follows;

• Angle of repose: 0.044°
• Bulk density: 0.5g/ml
• Tapped density: 0.71g/ml
• Compressibility index: 0.295
• % Compressibility index: 29.5%
• Hausner’s ratio: 1.42

2. Post-evaluation studies ^[11]

1. Weight of tablet:

The weight of the tablet is done after the formulation of the herbal tablet for several reasons: Uniformity of dosage form, Quality control, Content uniformity, and Detection of variation.

Hardness:

The hardness of the tablet is done after the formulation of the herbal tablet for several reasons:

Ensuring Mechanical Strength, Predicting Tablet Performance, Detecting Formulation Issues, and Ensuring Patient Compliance.

1. Friability:

The friability of the tablet is done after the formulation of the herbal tablet for several reasons: Ensuring Mechanical Strength, Predicting Tablet Performance, Detecting Formulation Issues, and Ensuring Patient Compliance.

2. Thickness:

The thickness of the tablet is done after the formulation of the herbal tablet for several reasons: Ensuring Uniformity, Predicting Tablet Performance, Detecting Formulation Issues, and Ensuring Patient Compliance.

3. Disintegration time:

The disintegration time of the tablet is done after the formulation of the herbal tablet for several reasons: Ensuring Rapid Release of Active Ingredients, Predicting Bioavailability, Detecting Formulation Issues, and Ensuring Patient Compliance.

4.  pH Determination:

The pH determination of the tablet is done after the formulation of the herbal tablet for several reasons: Ensuring Stability and Efficacy, Predicting Bioavailability, Detecting Formulation Issues, and Ensuring Patient Safety.

5. Dissolution time:

The dissolution time of the tablet is done after the formulation of the herbal tablet for several reasons: Ensuring Release of Active Ingredients, Predicting Bioavailability, Detecting Formulation Issues, and Ensuring Patient Compliance.

Fig No. 3 Prepared Herbal Tablet Dosage Form