Description:FORM 2
THE PATENTS ACT 1970
(39 of 1970)
&
The Patent Rules 2003
COMPLETE SPECIFICATION
(See sections 10 & rule 13)
1. TITLE OF THE INVENTION
“AN ANTI-GLYCEMIC FORMULATION AND METHOD OF PREPARATION THEREOF”
2. APPLICANT (S)
NAME NATIONALITY ADDRESS
MAYONS PHARMACEUTICALS PRIVATE LIMITED Indian Octroi No. 4, Old Kamptee Road, Kalamna Basti, Kalamna, Nagpur 440026, Maharashtra, India.
3. PREAMBLE TO THE DESCRIPTION
COMPLETE SPECIFICATION
The following specification particularly describes the invention and the manner in which it is to be performed.

FIELD OF THE INVENTION
The present invention relates to the field of pharmaceutical formulation. In particular, the invention relates to an anti-glycemic tablet formulation comprising Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract, and Morus nigra extract, in combination with pharmaceutically acceptable inert excipients for the management of blood sugar level. The invention also provides a method for preparing the same.
BACKGROUND OF THE INVENTION
Diabetes mellitus is a chronic metabolic disorder characterized by elevated blood glucose levels resulting from defects in insulin secretion, insulin action, or both. Persistently high blood sugar levels lead to serious complications such as cardiovascular disease, neuropathy, nephropathy, retinopathy, delayed wound healing, and increased susceptibility to infections. Globally, the prevalence of diabetes is rising at an alarming rate due to sedentary lifestyles, unhealthy dietary habits, obesity, and genetic predisposition. The growing incidence among younger populations and in developing countries has become a significant public health concern.
Conventional treatment strategies, including oral hypo-glycemic agents and insulin therapy, are effective in managing blood sugar levels but are often associated with side effects such as hypoglycemia, gastrointestinal disturbances, weight gain, and long-term resistance. Moreover, many patients struggle with compliance due to the cost of treatment, adverse effects, and the need for lifelong medication.
In recent years, increasing attention has been directed toward plant-based alternatives for the management of diabetes and regulation of blood glucose levels. A wide variety of medicinal plants contain bioactive compounds such as flavonoids, alkaloids, terpenoids, polyphenols, and glycosides, which have demonstrated anti-glycemic, antioxidant, and anti-inflammatory properties. These natural agents can act by stimulating insulin secretion, enhancing glucose uptake, modulating carbohydrate metabolism, or protecting pancreatic β-cells from oxidative damage.
Plant-derived formulations are generally considered safer, more biocompatible, and cost-effective compared to conventional synthetic drugs. They are also widely accepted among patients due to their natural origin, lower side-effect profile, and suitability for long-term use. Consequently, plant-based anti-glycemic formulations are emerging as promising therapeutic options or adjuncts to conventional treatment for effective diabetes management.
A marketed product “Cephalandra indica 30” by BM Homoeopathy discloses C. indica use in the management of Diabetes mellitus, Diabetes insipidus, skin affections, jaundice, and dropsy, highlighting its traditional therapeutic applications in homeopathic practice.
Another marketed product “SYZ-Cephalandra” by Best made Natural Products discloses a homeopathic formulation comprising Cephalandra indica, Gymnema sylvestre, Momordica charantia, and Syzygium jambolanum to support general metabolic well-being and balanced living.
An article entitled “Effect of homeopathic preparations of Syzygium jambolanum and Cephalandra indica on gastrocnemius muscle of high fat and high fructose-induced type-2 diabetic rats” by Sampath et al. in the journal Homeopathy (2013), discloses the homeopathic preparations of S. jambolanum and C. indica exhibited antidiabetic effects by improving insulin action through activation of insulin signaling molecules in skeletal muscle of type-2 diabetic rats.
An article entitled “A detailed review of various herbal treatment options for potentially curing or ameliorating pain in diabetic neuropathy” by Wal et al. in the journal Current Traditional Medicine (2022) discloses the effects of Momordica charantia in alleviating pain associated with diabetic neuropathy.
Given the rising concerns over increasing blood sugar levels in individuals, there is a pressing need for safe, effective, and affordable therapeutic alternatives or adjuncts that can regulate glucose levels, enhance patient compliance, and minimize the risk of long-term complications associated with diabetes.
SUMMARY OF THE INVENTION
It is an object of the present invention to provide an anti-glycemic formulation for the effective management of blood sugar level.
It is an object of the present invention to provide an anti-glycemic tablet formulation comprising Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract, and Morus nigra extract, in combination with pharmaceutically acceptable inert excipients.
It is yet another object of the present invention to provide an anti-glycemic formulation that enhances targeted delivery while minimizing systemic side effects.
It is another object of the present invention to provide a method for preparation of an anti-glycemic tablet formulation.
The aforesaid objects are achieved by the present invention. All the said objects are achieved by providing an anti-glycemic tablet formulation comprising Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract, and Morus nigra extract, in combination with pharmaceutically acceptable inert excipients for the effective management of blood sugar level.
In an embodiment, the present invention relates to an anti-glycemic formulation, comprising:
a) Cephalandra indica extract;
b) Syzgium jambolanum extract;
c) Gymnema slyvestre extract;
d) Momocardia charantia extract;
e) Morus nigra extract; and
f) Pharmaceutically acceptable inert excipients.
In an aspect of the embodiment, the extracts Cephalandra indica, Syzgium jambolanum, Gymnema slyvestre, Momocardia charantia and Morus nigra are present in an equal ratio of 1:1:1:1:1.
In an aspect of the embodiment, the pharmaceutically acceptable inert excipients comprise a filler, a disintegrant, a binder, a lubricant and a glidant.
In an aspect of the embodiment, the filler is lactose.
In an aspect of the embodiment, the disintegrant is sodium starch glycolate.
In an aspect of the embodiment, the binder is polyvinylpyrrolidone.
In an aspect of the embodiment, the lubricant is magnesium stearate.
In an aspect of the embodiment, the glidant is hydrous magnesium silicate.
In an embodiment, the present invention relates to an anti-glycemic tablet formulation, comprising:
a) Cephalandra indica extract in a concentration range of 1-3 % w/w;
b) Syzgium jambolanum extract in a concentration range of 1-3 % w/w;
c) Gymnema slyvestre extract in a concentration range of 1-3 % w/w;
d) Momocardia charantia extract in a concentration range of 1-3 % w/w;
e) Morus nigra extract in a concentration range of 1-3 % w/w;
f) Lactose as a filler, in a concentration range of 80-90 % w/w;
g) Sodium starch glycolate as a disintegrant, in a concentration range of 1-3 % w/w;
h) Polyvinylpyrrolidone as a binder, in a concentration range of 1-3 % w/w;
i) Magnesium stearate as a lubricant, in a concentration range of 0.3-0.9 % w/w; and
j) Hydrous magnesium silicate as a glidant, in a concentration range of 0.1-0.7 % w/w;
wherein the percentages are with respect to total weight of the formulation.
In an embodiment, the present invention is further directed to a method for preparing an anti-glycemic formulation, the method comprising the steps:
a) Mixing Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract and Morus nigra extract in equal ratios to obtain a mother tincture;
b) Mixing filler with binder solution to form a mixture;
c) Adding the mother tincture to the mixture to obtain a wet mass;
d) Granulating the wet mass obtained in step c) by passing through a sieve to form granules;
e) Drying the granules obtained in step d) in a tray dryer to obtain dried granules;
f) Sieving the dried granules to obtain sieved granules; and
g) Blending the sieved granules obtained in step f) with disintegrant, lubricant and glidant in a blender to obtain an anti-glycemic formulation.

BRIEF DESCRIPTION OF DRAWINGS
Reference will be made to embodiments of the invention, examples of which may be illustrated in accompanying figures. These figures are intended to be illustrative, not limiting. Although the invention is generally described in the context of these embodiments, it should be understood that it is not intended to limit the scope of the invention to these particular embodiments.
Figure 1 illustrates histological assessment of the pancreatic tissue in (a) control group, (b) STZ-induced diabetic control group, (c) standard treatment group, and (d) anti-glycemic formulation treatment groups.
Figure 2 illustrates histological assessment of the hepatic tissue in (a) control group, (b) STZ-induced diabetic control group, (c) standard treatment group, and (d) anti-glycemic formulation treatment groups.
Figure 3 illustrates histological assessment of the renal tissue in (a) control group, (b) STZ-induced diabetic control group, (c) standard treatment group, and (d) anti-glycemic formulation treatment groups.
DETAILED DESCRIPTION OF THE INVENTION
The following description with reference to the accompanying drawings is provided to assist in a comprehensive understanding of exemplary embodiments of the invention. It includes various specific details to assist in that understanding but these are to be regarded as merely exemplary. Accordingly, persons skilled in the art will recognize that various changes and modifications to the embodiments described herein can be made without departing from the scope and spirit of the invention. In addition, descriptions of well-known functions and constructions are omitted for clarity and conciseness.
The terms and words used in the following description are not limited to the bibliographical meanings and are merely used to enable a clear and consistent understanding of the invention. Accordingly, it should be apparent to the person skilled in the art that the following description of exemplary embodiments of the present invention is provided for illustration purpose only.
The term "a" and "an" refers to one or to more than one (i.e., to at least one) of the grammatical object of the article. The information provided in this document, and particularly the specific details of the described exemplary aspects, is provided primarily for clearness of understanding and no unnecessary limitations are to be understood from there.
The terms "comprising" (and any form of comprising, such as "comprise", "comprises", and "comprised"), "having" (and any form of having, such as "have" and "has"), "including" (and any form of including, such as "includes" and "include"), or "containing" (and any form of containing, such as "contains" and "contain"), are inclusive or open-ended and do not exclude additional, unrecited elements or method steps.
As used herein, the term ‘about’ means that the numerical value is approximate and small variations would not significantly affect the practice of the disclosed embodiments. Where a numerical limitation is used, unless indicated otherwise by the context, ‘about’ means the numerical value can vary by ±10% and remain within the scope of the disclosed embodiments.
The terms "treat," "treated," or "treating" mean both therapeutic treatment or prophylactic or preventative measures wherein the object is to prevent or slow down (lessen) an undesired physiological condition, disorder or disease, or obtain beneficial or desired clinical results. For purposes of this invention, beneficial or desired clinical results include, but are not limited to, alleviation of symptoms; diminishment of extent of condition, disorder or disease; stabilized (i.e., not worsening) state of condition, disorder or disease; delay in onset or slowing of condition, disorder or disease progression; amelioration of the condition, disorder or disease state or remission (whether partial or total), whether detectable or undetectable; an amelioration of at least one measurable physical parameter, not necessarily discernible by the patient; or enhancement or improvement of condition, disorder or disease.
As used herein ‘Anti-glycemic formulation’ refers to a pharmaceutical composition comprising one or more active agents capable of lowering, regulating, or stabilizing elevated blood glucose levels. The formulation includes plant extracts as bioactive agents, alone or in combination with pharmaceutically acceptable excipients, and is intended for use in the management, prevention, or treatment of hyper glycemia and diabetes-related complications.
As used herein ‘Tablet formulation’ is a solid pharmaceutical dosage form prepared by compressing one or more active pharmaceutical ingredients (APIs) together with pharmaceutically acceptable excipients such as binders, diluents/fillers, disintegrants, super-disintegrants, lubricants, and glidants. Tablet formulations are designed to ensure accurate dosing, ease of administration, stability during storage, and appropriate disintegration and dissolution to release the active ingredients at the desired rate and site of action.
As used herein ‘Pharmaceutically acceptable inert excipients’ refers to any of the components of a pharmaceutical formulation other than the active and which are approved by regulatory authorities or are generally regarded as safe for human or animal use. A combination of excipients may also be used.
The present invention aims to develop an anti-glycemic tablet formulation comprising Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract, and Morus nigra extract, in combination with pharmaceutically acceptable inert excipients for the management of blood glucose level. The formulation enhances targeted delivery while minimizing systemic side effects.
In an embodiment, the present invention relates to an anti-glycemic tablet formulation, comprising:
a) Cephalandra indica extract;
b) Syzgium jambolanum extract;
c) Gymnema slyvestre extract;
d) Momocardia charantia extract;
e) Morus nigra extract; and
f) Pharmaceutically acceptable inert excipients.
Cephalandra indica is a perennial climbing plant of the Cucurbitaceae family, is traditionally employed in Ayurvedic and homeopathic systems of medicine for the management of diabetes and related complications. The plant, including its roots, fruits, and leaves, comprises bioactive constituents such as alkaloids, flavonoids, and triterpenes, which exhibit pronounced hypo-glycemic activity. Additionally, it restores antioxidant enzyme activities (superoxide dismutase, catalase) and reduces lipid peroxidation.
Syzygium jambolanum, commonly known as Jamun or Indian blackberry, is a medicinal plant traditionally used in the management of diabetes and metabolic disorders. The seeds, bark, and leaves are rich in bioactive compounds such as alkaloids, flavonoids, tannins, anthocyanins, ellagic acid, and jamboline, which are reported to exhibit anti-hyperglycemic, antioxidant, and anti-inflammatory activities. Seed extracts of S. jambolanum have been shown to enhance insulin secretion, improve glucose tolerance, and protect pancreatic β-cells against oxidative stress.
Gymnema sylvestre is a slow growing, perennial, medicinal woody climber found in central and peninsular India. It is a potent antidiabetic plant and used in folk, ayurvedic and homeopathic systems of medicine. It is also used in the treatment of asthma, eye complaints, inflammations and snakebite. In addition, it possesses antimicrobial, anti-hypercholesterolemic, hepatoprotective and sweet suppressing activities. It also acts as feeding deterrents to caterpillar, prevent dental caries and is used in skin cosmetics.
Momordica charantia, known as bitter melon or bitter gourd, is a tropical and subtropical vine widely cultivated in Asia, Africa, and the Caribbean for its edible, bitter fruit. The plant contains various beneficial compounds, including saponins, flavonoids, and triterpenes, which are linked to its diverse health benefits. It is used for treating diabetes and other health conditions.
Morus nigra is a genus of flowering plants in the Moraceae family, widely distributed across subtropical regions of Asia, North America, and Africa. The plant is rich in bioactive compounds such as flavonoids, stilbenes, benzofurans and polyhydroxylated alkaloids. The plant has demonstrated diverse pharmacological activities, including antioxidant, anti-inflammatory, antidiabetic, anti-obesity, and antimicrobial effects.
In an aspect of the embodiment, the extracts Cephalandra indica, Syzgium jambolanum, Gymnema slyvestre, Momocardia charantia and Morus nigra are present in an equal ratio of 1:1:1:1:1.
In an aspect of the embodiment, the pharmaceutically acceptable inert excipients comprise a filler, a disintegrant, a binder, a lubricant and a glidant.
Fillers, also known as diluents, are used to increase the bulk of a formulation, making it easier to handle and manufacture, especially when the active pharmaceutical ingredient is present in small amounts. Fillers aid in the manufacturing process by providing structural integrity and improving the stability of tablets, capsules, or powders without affecting the efficacy of active ingredients.
In an aspect of the embodiment, the fillers are selected from the group comprising lactose, sucrose, magnesium stearate, glucose, plant cellulose, calcium carbonate, and mixtures thereof.
In preferred aspect of the embodiment, the filler is lactose.
Lactose was used as a filler to provide the required bulk to the formulation, especially since the active ingredients alone were insufficient in weight for convenient compression. It is widely preferred for its excellent compressibility, flow properties, and compatibility with most APIs. Lactose also contributes to consistent tablet weight, uniform distribution of the actives, and acceptable mouthfeel, making it one of the most reliable excipients in solid dosage forms.
Disintegrants facilitate the breakup of tablets or capsules into smaller fragments upon contact with gastrointestinal fluids, thereby promoting drug dissolution and absorption. This disintegration process is vital for drug dissolution and subsequent absorption into the body, ultimately affecting the drug's effectiveness.
In an aspect of the embodiment, the disintegrants are selected from the group comprising carboxymethylcellulose calcium, carmellose sodium, croscarmellose sodium, alginic acid, bentonit, cellulose, sodium starch glycolate and mixtures thereof.
In preferred aspect of the embodiment, the disintegrant is sodium starch glycolate.
Sodium starch glycolate was incorporated as a superdisintegrant to ensure rapid disintegration of tablets after administration. It absorbs water quickly and swells extensively, thereby facilitating the breakup of the tablet matrix into smaller fragments. This mechanism enhances the dissolution of active ingredients and promotes faster absorption, which is essential for achieving the desired therapeutic response in antidiabetic therapy.
Binders are excipients that impart cohesive properties to powders, allowing them to form granules and maintain the integrity of tablets. They are critical during wet or dry granulation processes. Binders contribute to the mechanical strength and durability of tablets during handling and storage.
In an aspect of the embodiment, the binders are selected from the group comprising polyvinylpyrrolidone (PVP), hydroxypropyl cellulose, microcrystalline cellulose, polyethylene glycol, gelatin, starch, carbomers, sodium carboxymethyl cellulose and mixtures thereof.
In preferred aspect of the embodiment, the binder is polyvinylpyrrolidone.
Polyvinylpyrrolidone served as a binder to provide cohesiveness to the formulation. It ensured that the powder blend remained intact during compression, producing tablets with adequate hardness and mechanical strength. PVP is highly versatile and soluble, which helps in achieving uniform distribution of actives and improves tablet durability while minimizing friability and dusting during handling.
Lubricants reduce friction between the tablet or granules and the equipment during manufacturing, preventing sticking and ensuring smooth ejection from the tablet press. Lubricants help improving pharmaceutical operations by reducing the adhesion forces between powder/equipment as well as particle/particle in terms of wall friction and inter-particle friction.
In an aspect of the embodiment, the lubricants are selected from the group comprising boric acid, magnesium stearate, sodium oleate, stearic acid and mixtures thereof.
In preferred aspect of the embodiment, the lubricant is magnesium stearate.
Magnesium stearate was employed as a lubricant to minimize friction between the tablet blend and the tooling surfaces during compression. It improved powder flow into the dies and ensured smooth ejection of tablets, preventing sticking or picking issues. Being highly effective at low concentrations, magnesium stearate contributed to improved process efficiency; however, its content was carefully controlled to prevent potential delays in disintegration or dissolution.
Glidants reduce interparticle friction and improves the flowability of powders during the manufacturing process. The use of glidants minimizes weight variability and enhances the reproducibility of dosage.
In an aspect of the embodiment, the glidants are selected from the group comprising colloidal silicon dioxide, hydrous magnesium silicate, starch and magnesium trisilicate and mixtures thereof.
In preferred aspect of the embodiment, the glidant is hydrous magnesium silicate.
Hydrous magnesium silicate, commonly known as talc, was included as a glidant and anti-adherent. It enhanced the flow properties of the powder blend, reducing interparticulate friction and aiding in uniform die filling during compression. Talc also acted as an anti-adherent by preventing tablets from sticking to punches, ensuring smooth surfaces and consistent tablet quality. Its use contributed to both manufacturing ease and the overall elegance of the final dosage form.
In an embodiment, the present invention relates to an anti-glycemic tablet formulation, comprising:
a) Cephalandra indica extract in a concentration range of 1-3% w/w;
b) Syzgium jambolanum extract in a concentration range of 1-3% w/w;
c) Gymnema slyvestre extract in a concentration range of 1-3% w/w;
d) Momocardia charantia extract in a concentration range of 1-3% w/w;
e) Morus nigra extract in a concentration range of 1-3% w/w;
f) Lactose as a filler, in a concentration range of 80-90 % w/w;
g) Sodium starch glycolate as a disintegrant, in a concentration range of 1-3 % w/w;
h) Polyvinylpyrrolidone as a binder, in a concentration range of 1-3 % w/w;
i) Magnesium stearate as a lubricant, in a concentration range of 0.3-0.9 % w/w; and
j) Hydrous magnesium silicate as a glidant, in a concentration range of 0.1-0.7 % w/w;
wherein the percentages are with respect to total weight of the formulation.
In an embodiment, the present invention is further directed to a method for preparing an anti-glycemic formulation, the method comprising the steps:
a) Mixing Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract and Morus nigra extract in equal ratios to obtain a mother tincture;
b) Mixing filler with binder solution to form a mixture;
c) Adding the mother tincture to the mixture to obtain a wet mass;
d) Granulating the wet mass obtained in step c) by passing through a sieve to form granules;
e) Drying the granules obtained in step d) in a tray dryer to obtain dried granules;
f) Sieving the dried granules to obtain sieved granules; and
g) Blending the sieved granules obtained in step f) with disintegrant, lubricant and glidant in a blender to obtain an anti-glycemic formulation.
In an aspect of the embodiment, the anti-glycemic formulation is formulated into the desired dosage form such as tablets, capsules, powders, granules, films, sprays, gels, and liquids to ensure uniformity, stability, and bioavailability.
In preferred embodiment, the anti-glycemic formulation is in a tablet form.

EXAMPLES
EXAMPLE 1 - Preparation of an Anti-glycemic Formulation according to the invention:
The components and their concentrations utilized for preparing an anti-glycemic formulation for the management of blood glucose level is outlined in the table below:
Table 1- Composition of the Anti-glycemic Formulation
Sr. No. Ingredient/ Phase Concentration (%)
01 Cephalandra indica 2.0
02 Syzgium jambolanum 2.0
03 Gymnema slyvestre 2.0
04 Momocardia charantia 2.0
05 Morus nigra 2.0
06 Lactose 85.0
07 Sodium Starch Glycolate 2.0
08 Polyvinylpyrrolidone 2.0
09 Magnesium Stearate 0.6
10 Hydrous Magnesium Silicate 0.4
• Preparation Methodology:
1. The active pharmaceutical agents, 2.0 mg Cephalandra indica, 2.0 mg Syzgium jambolanum, 2.0 mg Gymnema slyvestre, 2.0 mg Momocardia charantia, 2.0 mg Morus nigra were mixed to obtain a mother tincture.
2. 85.0 mg of Lactose was mixed with 2.0 % of Polyvinylpyrrolidone (PVP K-30) solution to obtain a mixture.
3. The mother tincture was gradually added to the mixture and mixed thoroughly to obtain a wet mass.
4. The wet mass was passed through a #20 sieve to obtain granules of uniform size.
5. The granules obtained in step 4 were dried in a tray dryer at a temperature not exceeding 60 °C for 30–45 minutes, or until the loss on drying (LOD) was reduced to below 5% to form dried granules.
6. The dried granules were passed through a #40 sieve to obtain sieved granules.
7. The sieved granules were blended with 0.6 mg magnesium stearate and 0.4 mg hydrous magnesium silicate (talc) for 5 minutes using a blender to obtain an anti-glycemic formulation.
8. The anti-glycemic formulation was compressed into tablets of uniform weight and hardness using a rotary tablet press.
EXAMPLE 2- Characterization of Anti-glycemic Tablet Formulation:
The anti-glycemic formulation was subjected to standard evaluation studies to assess its physicochemical and quality attributes.
The parameters evaluated included individual weights of randomly selected tablets, hardness to determine crushing strength, friability to assess resistance to abrasion and chipping, moisture content (LOD) to measure loss on drying, disintegration time to determine breakdown under physiological conditions, and TLC (thin layer chromatography) to confirm the presence of lactose in the formulation.
Table 2- Evaluation Parameters of Anti-glycemic Formulation
Parameter Recommendation Observation Remarks
Appearance White round biconvex tablet Complies Pass
Weight variation (20 tablets) ±5% for tablets >250 mg 248–252 mg Pass
Hardness 2–4 kg/cm² 3.5 kg/cm² Pass
Friability NMT 1.0% 0.32% Pass
Moisture content (LOD) NMT 5.0% 3.8% Pass
Disintegration Time NMT 5 min 2 min 30 sec Pass
TLC for Lactose NLT 94% lactose 95% Pass
NMT-Not more than; NLT-Not less than

EXAMPLE 3 - In-vivo Evaluation of Anti-glycemic Tablet Formulation
An in-vivo study was conducted to evaluate the anti-glycemic potential of the formulation using streptozotocin (STZ) induced diabetic rat model. The study assessed the impact of the formulation on blood glucose, lipid profile, liver and renal function parameters, and histopathological assessment of the pancreas, liver, and kidney.
Materials and Methods
Test Item: Anti-glycemic tablet formulation
Intended Use: Management of blood sugar level
Diabetes Disease Inducer: Streptozotocin (STZ)
Standard Drug: Glimepiride
Animal Model: Sprague Dawley albino rats, 8-10 weeks old, weighing 180 -200 grams
Grouping: Fifty-four animals were randomly divided into nine groups (n=6 per group
• Induction of Diabetes Mellitus
Diabetes mellitus was induced by a single intraperitoneal injection of streptozotocin (STZ) at a dose of 60 mg/kg body weight, prepared in 0.1 M citrate buffer (pH 4.5), administered to overnight-fasted rats. Post-STZ administration, rats received a 20% glucose solution overnight to mitigate initial hypoglycemic effects. Blood glucose levels were measured after three days; rats with glucose levels exceeding 250 mg/dL were considered diabetic. Control rats received an injection of 0.2 mL of the vehicle alone (0.1 M citrate buffer, pH 4.5) to discern effects attributable specifically to STZ administration.
Table 3- Treatment groups for in-vivo study

Group Treatment No. of Animals Dosage mg/kg
I Control (non-treated) 6 0.9% saline (0.5 mL)
II Disease control 6 Streptozotocin (60 mg/Kg)
III Standard 6 Glimepiride (3 mg/kg) once daily + Streptozotocin (60 mg/Kg)
IV Anti-glycemic formulation 6 Anti-glycemic formulation (100 mg/kg) twice daily + Streptozotocin (60 mg/Kg)
V Cephalandra indica extract (2 % w/w) 6 Cephalandra indica extract (100 mg/kg) twice daily + Streptozotocin (60 mg/Kg)
VI Syzgium jambolanum extract (2 % w/w) 6 Syzgium jambolanum extract (100 mg/kg) twice daily + Streptozotocin (60 mg/Kg)
VII Gymnema slyvestre extract (2 % w/w) 6 Gymnema slyvestre extract (100 mg/kg) twice daily + Streptozotocin (60 mg/Kg)
VIII Momocardia charantia extract (2 % w/w) 6 Momocardia charantia extract (100 mg/kg) twice daily + Streptozotocin (60 mg/Kg)
IX Morus nigra extract (2 % w/w) 6 Morus nigra hydroalcoholic extract (100 mg/kg) twice daily + Streptozotocin (60 mg/Kg)

EXAMPLE 3A - Effect of Anti-glycemic Tablet Formulation on Blood Glucose Level of Streptozotocin-Induced Diabetic Rats
Animals were subjected to an 18-hour fasting period prior to blood glucose estimation. Blood samples were collected from each group on days 7, 14, 21, and 28 post-treatments. Glucose levels were determined using standard enzymatic method to evaluate the effect of the formulation on glycemic control.
Administration of the anti-glycemic formulation resulted in a marked reduction in blood glucose levels in STZ-induced diabetic rats. Among the treatment groups, Group IV (anti-glycemic formulation) demonstrated the highest percentage reduction in glucose levels between days 14 and 21. A significant decline (p < 0.001) in blood glucose was observed in group IV compared with the diabetic control group II on days 21 and 28, underscoring its strong antihyperglycemic potential. Beyond day 21, no significant difference was noted between the glimepiride-treated group III (standard) and the formulation-treated group IV, further supporting the comparable antidiabetic efficacy of the test formulation. In contrast, the individual extracts tested failed to produce any significant reduction in glucose levels. Based on these findings, subsequent studies were carried out with four groups: Group I (Control), Group II (Diabetic control), Group III (Standard), and Group IV (Anti-glycemic formulation).
Table 4- Blood glucose levels in control and treatment groups of streptozotocin-induced diabetic rats
Group Treatment Blood Glucose Level (mg/dl)
Day 0 Day 1 Day 7 Day 14 Day 21 Day 28
I Control
(non-treated) 64.667 ± 1.256 69.167 ± 0.946 70.56 ± 0.224 69.167 ± 0.654 75.676 ± 0.333 71.75 ± 2.55
II Disease control 67.987 ± 2.887 269.500 ± 26.876 *** 287.000 ± 8.303 292.167 ± 15.063‡ 311.00 ± 16.509 ‡ 295.00 ± 10.509 ‡
III Standard 60.331 ± 5.761 269.167 ± 17.132 *** 199.333 ± 17.128 ‡ 129.113 ± 0.003‡ 74.50 ± 0.764 ‡ 71.50 ± 3.75 ‡
IV Anti-glycemic formulation 70.113 ± 0.643 374.600 ± 13.075*** 223.800 ± 32.152‡ 175.400± 29.209‡ 89.0± 17.530 n.s 80.5± 12.53 n.s
V Cephalandra indica extract (2 % w/w) 60.547 ± 1.546 252.253 ± 16.245 *** 257.654 ± 10.453 252.257 ± 18.263 251.523 ± 17.315 255.35 ± 10.629
VI Syzgium jambolanum extract (2 % w/w) 62.987 ± 4.85 231.325 ± 17.176 *** 227.563 ± 10.251 222.317 ± 17.213 239.056 ± 16.219 225.235 ± 13.259
VII Gymnema slyvestre extract (2 % w/w) 61.678 ± 4.765 251.156 ± 18.153 *** 257.054 ± 16.423 252.357 ± 17.143 251.075 ± 23.759 255.342 ± 18.531
VIII Momocardia charantia extract (2 % w/w) 63.865 ± 3.862 245.764 ± 20.254 *** 249.075 ± 12.313 242.245 ± 18.163‡ 241.217 ± 15.439 235.175 ± 16.354
IX Morus nigra extract (2 % w/w) 65.135 ± 4.758 240.132 ± 21.204 *** 237.056 ± 15.413 241.347 ± 25.213 233.186 ± 18.542 230.231 ± 13.459
***P<0.001 when diabetic control, standard and test compared with normal indicating successful induction of diabetes. ‡P<0.001 when standard and test anti-glycemic formulation compared with diabetic control indicating significant reduction in blood glucose level on day 7, 14, 21 and 28. n.s indicates insignificant difference (P>0.05) between standard and test 1 on day 21 and 28.
Table 5- Estimation of HbA1c levels in control and treatment groups in Streptozotocin -induced diabetic rats
Groups Treatment Serum HbA1c level (%)
I Control (non-treated) 4.01 ± 0.35
II Disease control 8.04 ± 0.57
III Standard 5.0 ± 0.41
IV Anti-glycemic formulation 4.25 ± 0.02

EXAMPLE 3B - Effect of the Anti-glycemic Tablet Formulation on Lipid Profile in Streptozotocin-Induced Diabetic Rats
To evaluate the impact of the treatment groups on the lipid profile, the animals were euthanized at the end of 30 days of treatment, and blood samples were collected for the estimation of lipid profile.
The Anti-glycemic formulation showed significant modulation of serum lipid levels after 30 days of treatment in diabetic rats. Administration of the Anti-glycemic formulation in group IV led to a marked reduction in total cholesterol and triglycerides, indicating its potential to alleviate dyslipidemia associated with streptozotocin-induced diabetes. These results highlight the potential of the formulation in both glycemic regulation and lipid management, thereby suggesting it as a promising treatment for the diabetes mellitus.
Table 6- Lipid profile assessment in control and treatment groups in Streptozotocin-induced rats
Groups Treatment Serum Total cholesterol level (mg/dl) HDL level (mg/dl) Serum Total glycerides level (mg/dl)
I Control (non-treated) 61.215 ± 0.441 40.065 ± 0.616 93.884 ± 1.429
II Disease control 124.586 ± 2.309 27.977 ± 1.008 244.651 ± 12.408
III Standard 76.634 ± 0.906 ‡ 40.687 ± 0.391 100.025 ± 0.896 ‡
IV Anti-glycemic formulation 79.545 ± 0.477‡ 18.167 ± 0.0.171 79.551 ± 0.473‡
‡P<0.001 when standard and test formulation compared with diabetic control, indicates significant reduction in total cholesterol and glyceride levels.

EXAMPLE 3C- Effect of the Anti-glycemic Tablet Formulation on Liver and Renal Function in Streptozotocin-Induced Diabetic Rats
To evaluate the impact of the treatment groups on the lipid profile, the animals were euthanized at the end of 30 days of treatment, and blood samples were collected for the estimation of liver and renal function parameters.
Evaluation of liver and renal function tests showed a significant elevation in serum glutamate pyruvate transaminase (SGPT) and serum glutamate oxaloacetate transaminase (SGOT) activities in streptozotocin (STZ)-induced diabetic rats, reflecting liver dysfunction associated with diabetes. Treatment with the anti-glycemic formulation (Group IV) resulted in a marked and significant reduction (p < 0.001) in SGPT and SGOT levels compared to the diabetic control (Group II). In addition, a significant decline in serum creatinine was observed in Group IV, indicating that the anti-glycemic formulation confers both hepatoprotective and renoprotective effects in STZ-induced diabetic rats.
Table 7: Liver and Renal function test performed in control and treatment groups in Streptozotocin-induced rats.
Groups Treatment SGPT level (mg/dl) SGOT level (mg/dl) Serum Creatinine level (mg/dl)
I Control (non-treated) 45.072 ± 4.898 49.417 ± 4.776 0.635 ± 0.022
II Disease control 86.281 ± 1.123 130.136 ± 4.108 1.520 ± 0.072
III Standard 44.873 ± 0.490‡ 62.631 ± 0.636 ‡ 0.846 ± 0.015 ‡
IV Anti-glycemic formulation 54.637 ± 0.462‡ 42.323 ± 0.366‡ 0.940 ± 0.008 ‡
‡P<0.001 when standard and test formulation compared with diabetic control, indicates significant reduction in SGPT, SGOT and Creatinine levels.
EXAMPLE 3D - Effect of Anti-glycemic Tablet Formulation on Pancreatic, Hepatic and Renal Histopathology
At the end of 30 days of treatment, the rats were euthanized, and the pancreas, liver, and kidneys were dissected, fixed in 10% formalin, embedded in paraffin, sectioned, and stained with hematoxylin and eosin for microscopic examination.
Histopathological examination revealed normal pancreatic, hepatic, and renal architecture in control rats (Group I), while STZ-induced diabetic (Group II) rats exhibited cell degeneration, necrosis with vacuolization, and glomerular shrinkage with tubular damage. The anti-glycemic formulation (Group IV) demonstrated marked preservation and restoration of cellular integrity, indicating both hepatoprotective and renoprotective effects (Figures 1-3).

 
We Claim:
1. An anti-glycemic formulation, comprising:
a) Cephalandra indica extract;
b) Syzgium jambolanum extract;
c) Gymnema slyvestre extract;
d) Momocardia charantia extract;
e) Morus nigra extract; and
f) Pharmaceutically acceptable inert excipients.

2. The anti-glycemic formulation as claimed in claim 1, wherein the extracts Cephalandra indica, Syzgium jambolanum, Gymnema slyvestre, Momocardia charantia, and Morus nigra are present in an equal ratio of 1:1:1:1:1.

3. The anti-glycemic formulation as claimed in claim 1, wherein the pharmaceutically acceptable inert excipients comprise a filler, a disintegrant, a binder, a lubricant and a glidant.

4. The anti-glycemic formulation as claimed in claim 3, wherein the filler is lactose.

5. The anti-glycemic formulation as claimed in claim 3, wherein the disintegrant is sodium starch glycolate.

6. The anti-glycemic formulation as claimed in claim 3, wherein the binder is polyvinylpyrrolidone.

7. The anti-glycemic formulation as claimed in claim 3, wherein the lubricant is magnesium stearate.

8. The anti-glycemic formulation as claimed in claim 3, wherein the glidant is hydrous magnesium silicate.

9. An anti-glycemic tablet formulation, comprising:
a) Cephalandra indica extract in a concentration range of 1-3% w/w;
b) Syzgium jambolanum extract in a concentration range of 1-3% w/w;
c) Gymnema slyvestre extract in a concentration range of 1-3% w/w;
d) Momocardia charantia extract in a concentration range of 1-3% w/w;
e) Morus nigra extract in a concentration range of 1-3% w/w;
f) Lactose as a filler, in a concentration range of 80-90 % w/w;
g) Sodium starch glycolate as a disintegrant, in a concentration range of 1-3 % w/w;
h) Polyvinylpyrrolidone as a binder, in a concentration range of 1-3 % w/w;
i) Magnesium stearate as a lubricant, in a concentration range of 0.3-0.9 % w/w; and
j) Hydrous magnesium silicate as a glidant, in a concentration range of 0.1-0.7 % w/w;
wherein the percentages are with respect to total weight of the formulation.

10. A method for preparing an anti-glycemic tablet formulation, the method comprising the steps:
a) Mixing Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract and Morus nigra extract in equal ratios to obtain a mother tincture;
b) Mixing filler with binder solution to form a mixture;
c) Adding the mother tincture to the mixture to obtain a wet mass;
d) Granulating the wet mass obtained in step c) by passing through a sieve to form granules;
e) Drying the granules obtained in step d) in a tray dryer to obtain dried granules;
f) Sieving the dried granules to obtain sieved granules; and
g) Blending the sieved granules obtained in step f) with disintegrant, lubricant and glidant in a blender to obtain an anti-glycemic formulation.

Dated this: 13th September 2025

Vijaykumar Shivpuje
IN/PA-1096
Agent for the Applicants
To,
The Controller of Patents
The Patent Office, Mumbai.

 
ABSTRACT
“AN ANTI-GLYCEMIC FORMULATION AND METHOD OF PREPARATION THEREOF”
The present invention relates to the field of pharmaceutical formulation. In particular, the invention relates to an anti-glycemic tablet formulation comprising Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract, and Morus nigra extract, in combination with pharmaceutically acceptable inert excipients for the management of blood sugar level. The invention also provides a method for preparing the same.

, Claims:We Claim:
1. An anti-glycemic formulation, comprising:
a) Cephalandra indica extract;
b) Syzgium jambolanum extract;
c) Gymnema slyvestre extract;
d) Momocardia charantia extract;
e) Morus nigra extract; and
f) Pharmaceutically acceptable inert excipients.

2. The anti-glycemic formulation as claimed in claim 1, wherein the extracts Cephalandra indica, Syzgium jambolanum, Gymnema slyvestre, Momocardia charantia, and Morus nigra are present in an equal ratio of 1:1:1:1:1.

3. The anti-glycemic formulation as claimed in claim 1, wherein the pharmaceutically acceptable inert excipients comprise a filler, a disintegrant, a binder, a lubricant and a glidant.

4. The anti-glycemic formulation as claimed in claim 3, wherein the filler is lactose.

5. The anti-glycemic formulation as claimed in claim 3, wherein the disintegrant is sodium starch glycolate.

6. The anti-glycemic formulation as claimed in claim 3, wherein the binder is polyvinylpyrrolidone.

7. The anti-glycemic formulation as claimed in claim 3, wherein the lubricant is magnesium stearate.

8. The anti-glycemic formulation as claimed in claim 3, wherein the glidant is hydrous magnesium silicate.

9. An anti-glycemic tablet formulation, comprising:
a) Cephalandra indica extract in a concentration range of 1-3% w/w;
b) Syzgium jambolanum extract in a concentration range of 1-3% w/w;
c) Gymnema slyvestre extract in a concentration range of 1-3% w/w;
d) Momocardia charantia extract in a concentration range of 1-3% w/w;
e) Morus nigra extract in a concentration range of 1-3% w/w;
f) Lactose as a filler, in a concentration range of 80-90 % w/w;
g) Sodium starch glycolate as a disintegrant, in a concentration range of 1-3 % w/w;
h) Polyvinylpyrrolidone as a binder, in a concentration range of 1-3 % w/w;
i) Magnesium stearate as a lubricant, in a concentration range of 0.3-0.9 % w/w; and
j) Hydrous magnesium silicate as a glidant, in a concentration range of 0.1-0.7 % w/w;
wherein the percentages are with respect to total weight of the formulation.

10. A method for preparing an anti-glycemic tablet formulation, the method comprising the steps:
a) Mixing Cephalandra indica extract, Syzgium jambolanum extract, Gymnema slyvestre extract, Momocardia charantia extract and Morus nigra extract in equal ratios to obtain a mother tincture;
b) Mixing filler with binder solution to form a mixture;
c) Adding the mother tincture to the mixture to obtain a wet mass;
d) Granulating the wet mass obtained in step c) by passing through a sieve to form granules;
e) Drying the granules obtained in step d) in a tray dryer to obtain dried granules;
f) Sieving the dried granules to obtain sieved granules; and
g) Blending the sieved granules obtained in step f) with disintegrant, lubricant and glidant in a blender to obtain an anti-glycemic formulation.