Composition of vitamin C and elderberry extract in a prolonged-release system for improved immune function

Abstract

Composition of vitamin C and elderberry extract in a prolonged-release system for enhanced immune support, comprising: a) 400 mg vitamin C (ascorbic acid), b) 150 mg elderberry extract standardized to anthocyanins, c) 15 mg zinc gluconate, d) 100 mg echinacea extract standardized to polysaccharides, e) 100 mg quercetin, f) 300 mg hydroxypropyl methylcellulose, g) 50 mg microcrystalline cellulose, h) 30 mg cross-linked polyvinylpyrrolidone, i) 5 mg magnesium stearate, j) 5 mg of a black pepper extract standardized to piperine, and k) 20 mg of an enteric coating agent.

Description

The present invention relates to an extended release formulation containing vitamin C and Holunderberries extract which serves to improve immune function by sustained release of drugs.In recent years, interest has grown in natural dietary supplements to enhance the immune system, especially formulations that combine strong antioxidants such as vitamin C with traditional drugs such as Holunder extract. Vitamin C is a known antioxidant that promotes immune function by protecting cells from oxidative damage and promoting activity of immune cells. Holunderberry extract derived from Sambucus nigra is known for its antiviral and anti-inflammatory properties and contributes to the general durability of the immune system. Despite these advantages, conventional formulations of these ingredients are often insufficient because they are rapidly metabolized and excreted from the body, so frequent dosing is required to maintain effectiveness.A major problem with conventional vitamin C and Holunderberries preparations is their short half-life in blood, which results in varying plasma levels and limits their sustained efficacy. This results in users having to take several doses distributed throughout the day to ensure continuous support of the immune system, which may be inconvenient and lead to poor compliance with the augmentation scheme. Moreover, the rapid degradation of these compounds in the gastrointestinal tract can decrease their bioavailability, impairing their overall efficacy.To solve these problems, there is a need for a novel formulation that enables uniform release of vitamin C and Holunderberries extract over a longer period of time. Such a delivery system could improve the bioavailability and duration of action of these compounds and provide prolonged support to the immune system without requiring multiple doses. Thus, an extended release delivery system would optimize the therapeutic benefit of both ingredients and make it more convenient and effective for daily maintenance of the immune system.An object of the present disclosure is to provide the prolonged release formulation which allows uniform release of vitamin C and Holunderberries extract, thus providing continuous support to the immune system throughout the day.Another object of the present disclosure is the controlled release system improves bioavailability of the two active agents to ensure they remain longer in the body and are more effectively utilized.Another object of the present disclosure is that users need not take multiple doses in a sustained release mechanism, which increases convenience and promotes better compliance with the augmentation program.Another object of the present disclosure is, by controlling vitamin C release, the formulation reduces the likelihood of gastrointestinal discomfort, sometimes associated with high doses of vitamin C at a time.Another object of the present disclosure is to have both synergistic effects by combining vitamin C and Holunderberries extract in a single prolonged release system, thereby maximizing their antioxidant, anti-inflammatory and immune enhancing properties.Another object of the present disclosure is to maintain stable plasma levels of vitamin C and Holunderberry compounds, thereby avoiding the peak and trough values that may reduce the efficacy of conventional dietary supplements.Another object of the present disclosure is that once daily or less frequent dosing enhances user compliance and makes it easier for humans to incorporate the supplement into their daily routine.Another object of the present disclosure is that the formulation can help reduce the frequency and severity of common diseases and support general well-being through consistent support of the immune system.The present invention relates to a unique immunopotentiating tablet formulation specifically designed to improve immune function by a synergistic combination of active ingredients. This formulation contains vitamin C, Holunderextract, zinc gluconate, Echinaceaextract and Retin, all of which are known for their individual immune supporting properties. To optimize the release of these drugs, hydroxypropyl methylcellulose is used as a prolonged release polymer that provides long lasting bioavailability. In addition, adjuvants such as microcrystalline cellulose, crosslinked polyvinylpyrrolidone and magnesium stearate are used to facilitate tablet formation, stability and ease of use. The addition of black pepper extract standardized for piperin increases the bioavailability of the active ingredients and thus improves their effectiveness. This formulation aims to provide a convenient and effective dietary supplement that supports the health of the immune system and offers an approach to boost the body's natural defenses against diseases and promote general well-being.EXAMPLE 1: CompositionThe immuno-strengthening tablet formulation contains several important active ingredients and adjuvants to improve its effectiveness and utility. It contains 400 mg vitamin C (ascorbic acid) which serves as a strong antioxidant and promotes immune function. The formulation contains 150 mg of Holunder extract which is standardized and contains anthocyanins known for their immune enhancing properties. In addition, it contains 15 mg of zinc gluconate, a mineral which is essential for the maintenance of a robust immune response.To further aid the health of the immune system, the formulation contains 100 mg of Echinaceaextract standardized on polysaccharides and 100 mg of Crosscetine, a flavonoid with anti-inflammatory activity. Hydroxypropyl methylcellulose in an amount of 300 mg acts as a prolonged release polymer and provides sustained release of the active agents. Microcrystalline cellulose is contained in an amount of 50 mg and serves as a binder, while 30 mg of cross-linked polyvinylpyrrolidone as a disintegrant ensures the proper disintegration of the tablet.The formulation also contains 5 mg of magnesium stearate which serves as a lubricant in tablet compression and provides smooth preparation. Black pepper extract standardized on piperine is added in an amount of 5 mg to increase the bioavailability of the active ingredients. Finally, an optional enteric coating is included in an amount of 20 mg to protect the ingredients from gastric acid and thus increase the overall stability and effectiveness of the formulation.EXAMPLE 2: Preparation of Holder ExtractTo obtain Holunderberries extract, first grind 200 g of dried Holunderberries (Sambucus nigra) to a coarse powder. The powder is placed in an extraction glass and covered with 1 litre of 70% ethanol solution (prepared by mixing 700 ml of ethanol with 300 ml of distilled water), taking care that the powder is completely submerged in order to achieve a solids-to-solvent ratio of 1:5. Seal the vessel and macerate the mixture for 24-48 hours at room temperature, shaking it occasionally to improve extraction. After maceration, filter the solution to remove plant material and pass the filtrate to a rotary evaporator. The ethanol is evaporated at 40-50°C under reduced pressure until a concentrated extract is obtained. To further dry the extract, it is placed in a vacuum oven set at 40°C to obtain a semi-solid or powdered form which yields about 20-25 g of concentrated Holunderber's berry extract. Store the extract in an air-tight sealed container protected from light and moisture to contain the bioactive components, particularly the anthocyanins that support the immune system.EXAMPLE 3: Extraction of Echinacea Extract (Standardized on Polysaccharides)To extract a standardized Echinaceaextract rich in polysaccharides, first 100 g of dried Echinacearoot or air parts are weighed and ground into a coarse powder. The pulverized material is placed in a beaker, and 500 ml of 70% ethanol (v / v) is added while thoroughly stirring to ensure saturation. Macerate the mixture at room temperature (20-25°C) for 24-48 hours, occasionally stir. After maceration, filter the mixture with filter paper or vacuum filtration equipment to separate the liquid extract from the solid plant material. If desired, the extract is concentrated by evaporating the ethanol at a reduced pressure of about 500 mmHg and a temperature of 40-50°C with a rotary evaporator. For standardization of the extract, polysaccharide content is quantified by analytical methods such as phenol-sulfuric acid method or high performance liquid chromatography (HPLC), using a known polysaccharide standard for calibration. For long term storage, the concentrated extract may be freeze dried to remove residual moisture and to obtain the active ingredients. The extract should be stored in airtight containers at 2-8°C and protected from light and moisture until it can be used for the formulation.EI GAME 4: Preparation of a tabletTo prepare the immuno-strengthening tablet formulation, they first measure the required amounts of the individual ingredients: 400 mg vitamin C, 150 mg Holunderberries extract (standardized on anthocyanins), 15 mg zinc gluconate, 100 mg Echinacea extract (standardized on polysaccharides), 100 mg Crosscetine, 300 mg hydroxypropylmethyl cellulose (for prolonged release), 50 mg microcrystalline cellulose (as binder), 30 mg cross-linked polyvinylpyrrolidone (as disintegrant), 5 mg magnesium stearate (as lubricant), 5 mg black pepper extract (standardized on piperine to improve bioavailability) and 20 mg of an optional enteric coating agent. Place the powdered ingredients into a mixing container and mix them for about 10-15 minutes until a homogeneous mixture is formed. Then add the lubricant and bioavailability enhancer and mix gently for an additional 3 to 5 minutes. If necessary, they carry out a wet granulation step to improve the handling and uniformity of tablets. Subsequently, the mixed powder is compressed into tablets by a tablet compression machine, an approximate weight of 1000 mg per tablet being aimed for. If an enteric coating is used, prepare the coating solution and apply it uniformly to the tablets.EXAMPLE 5: Physicochemical evaluationTo evaluate the physicochemical properties of the immunoamplifying tablets, they begin with weight uniformity by weighing 20 tablets on an analytical balance to ensure that each tablet weighs about 1000 mg. For the hardness test, using a tablet hardness tester, measure the force required to break 10 tablets, tending to have a hardness of between 4-8 kg. Conduct a friability test by placing 20 tablets in a friabilator and subjecting them to 100 revolutions at 25 U / min. The weight loss should not exceed 1%. Ensure that all measurements are made at room temperature (20-25 °C).The results show that the evaluation of the weight uniformity revealed that the average weight of the tablets was 1002 mg, with a standard deviation of 5 mg, indicating uniform production. The hardness test results gave an average hardness of 6 kg for the tablets, which is within the acceptable range. The friability test gave a weight loss of only 0.5%, which is well below the 1% limit. These results show that the tablets have sufficient mechanical strength and uniformity, which is critical to ensuring product stability during handling and transport.EXAMPLE 6: Disintegration and dissolution testTo perform disintegration tests, six tablets are placed in simulated gastric fluid (pH 1.2, 37°C) in a disintegrator to monitor the disintegration time and ensure that they disintegrate within 30 minutes. For dissolution testing, they use a USP dissolution apparatus (type II) with simulated intestinal fluid (pH 6.8, 37°C) and a stirring speed of 50 U / min. Take samples at specific intervals (e.g., 15, 30, 60, 120 minutes) and analyze the release of the drugs to ensure that at least 80% of vitamin C, Holunderberries extract, and Crosscetine are released within the indicated time.The disintegration test showed that all tablets dissolved in simulated gastric fluid within 25 minutes and thus fulfilled the specification of ≤30 minutes. Dissolution tests showed that 85% of vitamin C, 80% of the Holunder extract and 90% of the Crosscetine were released within 60 minutes in simulated intestinal fluid. This rapid disintegration and dissolution profile emphasizes the effectiveness of the formulation in the rapid release of the active ingredients, which is critical for maximizing the immune enhancing effect shortly after administration.EXAMPLE 7: Evaluation of bioavailabilityTo evaluate bioavailability, in vitroabsorption studies are performed with Caco-2 cell lines cultured in 24-well plates. Prepare test samples by dissolving a tablet in 5 mL PBS (pH 7.4) and placing it on the apical side of the cells. Incubate for 2 hours at 37 °C. Measure the concentration of released drugs by HPLC to evaluate absorption efficiency. Moreover, the absorption of the formulation is compared with and without 5 mg black pepper extract (piperin) to determine the enhancing effect.In vitroabsorption studies with Caco-2 cell lines showed an absorption rate of 50% for vitamin C and 45% for perpendicularine after 2 hours. When the formulation contained black pepper extract (piperin), the absorption rates increased to 65% for vitamin C and 60% for perpendicularine. These results indicate that the addition of piperine markedly increases the bioavailability of the principal active ingredients, which is critical for achieving optimum therapeutic effects in the immuno-strengthening formulation.EXAMPLE 8: Stability TestConduct accelerated stability studies by storing the tablets in stability compartments at 40°C and 75% relative humidity for 3 months. At the end of this period, changes in physical properties (color, odor, appearance) and chemical stability (drug concentration by HPLC) are to be evaluated. For long term stability tests, store the tablets at controlled room temperature (25°C) and humidity and evaluate their properties after 0, 6, 12 and 24 months.Accelerated stability studies showed no significant changes in physical properties after 3 months at 40° C. and 75% relative atmospheric humidity, with all active ingredients remaining above 90% of their original concentration. Long term stability tests conducted at 25°C showed that the tablets maintained their integrity and efficacy for 12 months with the drug concentration slightly decreasing to 95%. These results indicate that the formulation is stable under both accelerated and long term storage conditions and provides sustained efficacy.EXAMPLE 9: Microbial AssaysPerform microbiological threshold tests by removing 10 tablets and testing for the total number of aerobic microorganisms, the total number of yeasts and moulds, and specific pathogens (e.g. Salmonella, E. coli). Bake the samples in suitable nutrient media at 30-35°C for 48-72 hours for aerobic germination number and at 20-25°C for 5-7 days for yeast and mold count. Ensure that all tests conform to the pharmacopoeia standards and sterility is maintained throughout the process.The microbial limit tests confirmed that the total aerobic microbial count was below 10 CFU / tablet and no pathogenic organisms (e.g. Salmonella, E. coli) were detected in the samples. The total number of yeasts and moulds, <5 CFU / tablet, was also within acceptable limits. These results show that the formulation is microbiologically safe and meets regulatory standards, thus minimizing the risk of contamination.Although the particular features of the preferred embodiment have been particularly pointed out herein, it will be understood that many additional features may be added and many changes may be made to the preferred embodiment without departing from the principles of the disclosure. These and other changes in the preferred embodiment of the disclosure will be apparent to those skilled in the art from the present disclosure, and it is to be clearly understood that the foregoing descriptions are intended to be illustrative of the disclosure and not limiting.Examples1 A composition of vitamin C and Holunderberries extract in an extended release system for enhanced immune strengthening comprising: a) 400 mg vitamin C (ascorbic acid), b) 150 mg Holunder extract standardized to anthocyanins, c) 15 mg zinc gluconate, d) 100 mg Echinacea extract standardized to polysaccharides, e) 100 mg Crosscetine, f) 300 mg hydroxypropyl methylcellulose, g) 50 mg microcrystalline cellulose, h) 30 mg cross-linked polyvinylpyrrolidone, i) 5 mg magnesium stearate, j) 5 mg of a piperine standardized black pepper extract, and k) 20 mg of an enteric coating agent.

Claims

A composition of vitamin C and Holunderberries extract in an extended release system for enhanced immune strengthening comprising: a) 400 mg vitamin C (ascorbic acid), b) 150 mg Holunder extract standardized to anthocyanins, c) 15 mg zinc gluconate, d) 100 mg Echinacea extract standardized to polysaccharides, e) 100 mg Crosscetine, f) 300 mg hydroxypropyl methylcellulose, g) 50 mg microcrystalline cellulose, h) 30 mg cross-linked polyvinylpyrrolidone, i) 5 mg magnesium stearate, j) 5 mg of a piperine standardized black pepper extract, and k) 20 mg of an enteric coating agent.The vitamin C and holonder extract composition in an extended release delivery system of claim 1, wherein the holonder extract is derived from Sambucus nigra and contains at least 20% anthocyanin.The vitamin C and Holunder extract composition in an extended release system according to claim 1, wherein the Echinacea extract is derived from Echinacea purpurea and contains at least 4% polysaccharides.The composition of vitamin C and Holunder extract in an extended release system according to claim 1, wherein the extended release polymer, hydroxypropyl methylcellulose, is present at a concentration that causes delayed release of the active agents over 8 to 12 hours.The vitamin C and holunder extract composition in an extended release delivery system of claim 1, wherein the crosscetine is from natural sources selected from the group consisting of onion extract and citrus peel extract.The vitamin C and Holunder extract composition in an extended release delivery system of claim 1, wherein the zinc gluconate is contained in the formulation at a concentration effective to promote immune function and prevent zinc deficiency.The composition of vitamin C and Holunder extract in an extended release system according to claim 1, wherein the formulation is provided in a tablet form coated for enteric release, enabling protection from gastric acid.