WO2026019379A1 - A pharmaceutical composition comprising vitamin b - Google Patents

Abstract

The present invention relates to over the counter (OTC) film coated tablet compositions comprising one or more types of vitamins. Specifically, the invention focuses on formulations that include B vitamins, such as thiamine (B1), riboflavin (B2), nicotinamide (B3), pantothenic 5 acid (B5), pyridoxine (B6), biotin (B7), folic acid (B9), and cobalamin (B12). These vitamin- enriched tablets are intended for dietary supplementation to support various bodily functions, including energy metabolism, nervous system health, and the maintenance of healthy skin, hair, and eyes.

Description

DESCRIPTION A PHARMACEUTICAL COMPOSITION COMPRISING VITAMIN B Field of Invention The present invention relates to over the counter (OTC) film coated tablet compositions comprising one or more types of vitamins. Specifically, the invention focuses on formulations that include B vitamins, such as thiamine (B1), riboflavin (B2), nicotinamide (B3), pantothenic acid (B5), pyridoxine (B6), biotin (B7), folic acid (B9), and cobalamin (B12). These vitamin- enriched tablets are intended for dietary supplementation to support various bodily functions, including energy metabolism, nervous system health, and the maintenance of healthy skin, hair, and eyes. Background of the Invention Vitamin B complex supplements are widely used to address deficiencies and promote overall health. The B vitamins play crucial roles in energy production, brain function, and cell metabolism. Despite their importance, many individuals do not get sufficient amounts of these vitamins from their diets alone, leading to the need for supplementation. Vitamin B1 (thiamine) is essential for glucose metabolism and nerve, muscle, and heart function. Vitamin B2 (riboflavin) supports energy production and cellular function, growth, and development. Vitamin B3 (niacin) aids in DNA repair and stress responses. Vitamin B5 (pantothenic acid) is critical for synthesizing coenzyme A, which is involved in fatty acid metabolism. Vitamin B6 (pyridoxine) is important for amino acid metabolism, red blood cell production, and the creation of neurotransmitters. Vitamin B7 (biotin) supports metabolic functions and the health of skin, hair, and nails. Vitamin B9 (folic acid) is necessary for DNA synthesis and repair, red blood cell formation, and fetal development during pregnancy. Vitamin B12 (cobalamin) is vital for neurological function and DNA synthesis. Traditional tablet formulations of B vitamins can face challenges such as poor stability, unpleasant taste, and the need for multiple dosages to achieve desired levels. Innovations in formulation can enhance the stability, bioavailability, and user acceptability of these supplements. 1    The present invention addresses these issues by providing a comprehensive tablet formulation that combines multiple B vitamins in a single dosage form. This approach ensures that individuals can conveniently meet their nutritional needs without the inconvenience of taking multiple pills. Additionally, the invention may include advanced formulation techniques to improve the stability and taste of the vitamins, making the supplements more pleasant and easier to consume. In view of the foregoing, there is a need to improve stability and high patient compliance in film coated tablet compositions comprising vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B7, vitamin B9, vitamin B12, inositol, one or more pharmaceutically acceptable excipient and film coating. The present invention provides a solution to these problems by providing novel compositions comprising vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B7, vitamin B9, vitamin B12, inositol, one or more pharmaceutically acceptable excipient and a film coating wherein the film coating comprising hypromellose and pearlescent amber. These solutions will be described in detail. Brief Description of the Invention The present invention provides a film coated tablet compositions comprising vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B7, vitamin B9, vitamin B12, inositol, zinc, one or more pharmaceutically acceptable excipient and film coating wherein film coating comprises hypromellose and pearlescent amber and film coating material is free of titanium dioxide. The film coated pharmaceutical composition comprises film coating wherein said film coating can be comprises, 50.00-70.00% by weight hypromellose, 20.00-30.00% by weight Pearlescent Amber. The film coated tablet compositions of the present invention can be comprises below: ^ 4.00% - 8.00% by weight vitamin B1, ^ 4.00% - 8.00% by weight vitamin B2, ^ 4.00% - 8.00% by weight vitamin B3, ^ 4.00% - 8.00% by weight vitamin B5, ^ 1.00% - 3.00% by weight vitamin B6, ^ 0.01% - 0.50% by weight vitamin B7, 2    ^ 4.00% - 8.00% by weight inositol, ^ 4.00% - 8.00% by weight zinc, ^ 0.01% - 0.50% by weight vitamin B12, ^ 1.00% - 5.00% by weight film coating, and ^ up to %100 by weight one or more pharmaceutically acceptable excipients, and wherein film coating material is free of titanium dioxide. In other aspect of the present invention a process for preparing film coated tablet compositions can be comprises below steps a. Sieving and mixing Vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B8, inositol, zinc, vitamin B9, vitamin B12, zinc and one or more pharmaceutically acceptable excipient, b. Compressing the tablets, c. Coating with hypromellose, pearlescent amber and one or more film coating agent. Detailed Description of the Invention The aspects and disclosures according to the present invention, in particular the film coated tablet compositions, methods and uses, refer to film coated tablet compositions comprising the Vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B8, inositol, vitamin B9, vitamin B12, zinc, one or more pharmaceutically acceptable excipient and film coating wherein film coating comprises hypromellose and pearlescent amber, defined hereinbefore and hereinafter. The present invention provides a film coated tablet compositions comprising vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B7, vitamin B9, vitamin B12, inositol, zinc, one or more pharmaceutically acceptable excipient and film coating wherein film coating comprises hypromellose and pearlescent amber and film coating material is free of titanium dioxide. Excipients used in a formulation may adversely affect physicochemical and pharmacokinetic properties. These excipients can interact with the active ingredient. For this reason, while developing the formulation, the substances to be used in addition to the active substance must be carefully and consciously selected. 3    Preferably, the present invention relates to the film coated tablet compositions comprising Vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B8, inositol, vitamin B9, vitamin B12, zinc and one or more pharmaceutically acceptable excipient, wherein the excipients are selected from the group including, but are not limited to diluents, lubricants, glidants, binders, disintegrants, antioxidants, solubility increasing agents, preservatives, buffering agents, solvents, flavoring agent, stabilizers, sweetening agent, mixtures thereof. and other materials known to one of ordinary skill in the art and the mixtures thereof. Preferably, the present invention relates to the film coated tablet compositions comprising Vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B8, inositol, vitamin B9, vitamin B12, zinc and one or more pharmaceutically acceptable excipient, wherein the excipients are selected from the group including, but are not limited to diluents, lubricants, glidants, binders, disintegrants, antioxidants, solubility increasing agents, preservatives, buffering agents, solvents, flavoring agent, stabilizers, sweetening agent, mixtures thereof. and other materials known to one of ordinary skill in the art and the mixtures thereof. Diluents are essential components in film coated tablet compositions, serving to increase the volume of the formulation, ensuring uniform distribution of the active pharmaceutical ingredient (API), and enhancing the stability and manufacturability of the product. They help achieve consistent dosing, improve the flow properties of powders, and ensure that tablets and capsules reach a practical size for handling and administration. Diluents also contribute to the appearance and taste of the final product, thereby enhancing patient compliance and acceptability. In tablet formulations, they provide the necessary bulk for compression, while in capsules, they fill the dosage unit to the desired weight and volume. For injectable formulations, diluents help maintain isotonicity and stability. Commonly used diluents in film coated tablet compositions include lactose, which is valued for its compressibility and compatibility with most APIs; microcrystalline cellulose (MCC), known for its excellent binding properties; and dicalcium phosphate (DCP), which offers good flowability. Starch is used for its binding and disintegration properties, while mannitol and sorbitol are favored for their pleasant mouthfeel and sweet taste, respectively. Calcium carbonate is commonly used in antacid formulations, sodium chloride is used in small amounts in injectable formulations, and sucrose is used in chewable tablets and lozenges for its sweetness. Additionally, povidone serves as both a binder and diluent, particularly in solid dosage forms. Microcrystalline cellulose (MCC) is highly regarded for its exceptional binding 4    properties and ability to enhance the hardness and stability of tablets. It also improves the flow properties of powder blends, making it a versatile diluent in various solid dosage forms. In preferred embodiment in the present invention amount of diluent can be between 40.00-80.00% (w/w). In preferred embodiment in present invention diluent can be microcrystalline cellulose. In preferred embodiment in the present invention amount of microcrystalline cellulose can be between 40.00-80.00% (w/w). Lubricants are crucial excipients in film coated tablet compositions, primarily used to reduce friction during the tablet manufacturing process. They help prevent the tablet blend from sticking to the equipment, ensuring a smooth and efficient production process. Lubricants improve the flow of the tablet mixture through the machinery, enhancing the uniformity and consistency of the final product. Additionally, they aid in the ejection of tablets from the die cavity, preventing damage and ensuring the integrity of the tablets. Commonly used lubricants in film coated tablet compositions include magnesium stearate, stearic acid, talc, sodium stearyl fumarate, colloidal silicon dioxide, and polyethylene glycol (PEG). In preferred embodiment in the present invention amount of diluent can be between 0.5- 2.0% (w/w). In preferred embodiment in present invention lubricant can be magnesium stearate. In preferred embodiment present invention amount of lubricant can be between 0.5-2.0% (w/w). In film coated tablet compositions, flow enhancers are used to improve the flow properties of powders and granules during the manufacturing processes. These substances are added to formulations to ensure that mixtures flow freely and consistently during tablet or capsule production, preventing blockages and irregular distributions. Flow enhancers are particularly important in formulations with high doses of active ingredients, which often have poor flow properties. In preferred embodiment in the present invention amount of flow enhancer can be between 0.5-2.0% (w/w). Examples of flow enhancers include colloidal silicon dioxide (Aerosil), talc, magnesium stearate, microcrystalline cellulose, stearic acid, calcium silicate, dicalcium phosphate, glyceryl behenate, precipitated silica, and corn starch. These substances help achieve more 5    homogeneous mixtures during pharmaceutical manufacturing, enhancing the quality and effectiveness of the final product. In preferred embodiment flow enhancer in present invention compositions can be colloidal silicon dioxide (Aerosil). Disintegrants play a crucial role in the formulation of pharmaceutical compositions, primarily by facilitating the breakup of the tablet or capsule content into smaller fragments upon contact with gastrointestinal fluids. This process significantly enhances the dissolution and absorption of the active pharmaceutical ingredients, ensuring rapid onset of action. Disintegrants are particularly important for ensuring the bioavailability of the drug, making them indispensable in the design of immediate-release formulations. Commonly utilized disintegrants include, but are not limited to, sodium starch glycolate, croscarmellose sodium, crospovidone, alginic acid, carboxymethyl cellulose, and various modified cellulose derivatives. These agents are chosen based on their efficiency, compatibility with other excipients, and the nature of the active ingredient. A combination of these disintegrants can also be employed to achieve the desired disintegration profile and improve patient outcomes. In preferred embodiment in the present invention amount of disintegrant can be between 4.00-8.00% (w/w). In preferred embodiment disintegrant in present invention compositions can be croscarmellose sodium. In further embodiment tablet compositions in present invention can be comprise film coating. In further embodiment tablet compositions in present invention can be comprise film coating and film coating material is free of titanium dioxide. Film coating agents play an essential role in the formulation of pharmaceutical tablets by providing a protective layer that enhances the tablet's appearance, stability, and patient acceptability. These coatings protect the active ingredients from environmental factors such as light, moisture, and oxygen, which can degrade the drug over time. Additionally, film coatings can mask unpleasant tastes or odors, making the medication more palatable. They also facilitate easier swallowing and can be used to control the release profile of the active ingredient. In 6    preferred embodiment, tablet composition in present invention can be comprised of AquaPolish F brown 080.79 G as a film coating agent. In other embodiment AquaPolish F brown 080.79 comprising hypromellose, pearlescent amber, macrogol, riboflavin and Brillant Blue FCF (Blue 1) Al-Lake HD. In other embodiment AquaPolish F brown 080.79 comprising 50.00% - 70.00% by weight hypromellose, 20.00% - 30.00% by weight pearlescent amber, 5.00% - 12.00% by weight macrogol, 1.00% - 5.00% by weight riboflavin and at most 1.30% by weight Brillant Blue FCF (Blue 1) Al-Lake HD. Advantages In particular, it is very difficult to coating process of a product with vitamin B content. Because B Vitamins are odorous, dominantly coloured and stable materials that can remove their colour on the coating. Suppressing the dark yellow colour of vitamin B with coating, preventing the odour from reaching the patient and preventing stability problems is the most challenging part of the formulation. These problems can be solved by using film coating material comprising hypromellose and Pearlescent Amber. There is an obligation to use titanium free coating materials in food supplements. The requirement to use titanium free materials complicates both the choice of coating material and the coating process. Coating materials without titanium content are very difficult to opacify. With a minimum coating content of 5%, the core tablet surface can be covered. In some cases, even 5% coating content may not be sufficient for coverage / opacity. Both physical and chemical stability problems can be observed in titanium-free coating materials. The coating processes of coatings made using titanium-free coating materials are both time- consuming and difficult. Non-opacity, adhesion, discolouration and inhomogeneity of colour may be observed during the coating process. The inventors surprisingly have found that the tablet compositions comprising Vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B8, inositol, vitamin B9, vitamin B12, zinc, one or more pharmaceutically acceptable excipient and film coating wherein the film coating comprising hypromellose and pearlescent amber improves tablet compositions chemical physical stability, increase patient compliance. 7    With the use of Pearlescent Amber in the coating content, both physical and chemical stability is ensured. While the coating processes performed on titanium-free materials reach 4-5 hours; with the use of Pearlescent Amber in the coating content, the desired coating weight was reached with a process time of 1 hour. This is very important and advantageous in terms of process efficiency. In the coating process, non-opacification, adhesion, discolouration and inhomogeneous colouring problems can be observed. With the use of Pearlescent Amber in the coating content, opacification was achieved even with only 1% coating. The tablet composition of the present invention comprises below: ^ 4.00% - 8.00% by weight vitamin B1, ^ 4.00% - 8.00% by weight vitamin B2, ^ 4.00% - 8.00% by weight vitamin B3, ^ 4.00% - 8.00% by weight vitamin B5, ^ 1.00% - 3.00% by weight vitamin B6, ^ 0.01% - 0.50% by weight vitamin B7, ^ 4.00% - 8.00% by weight inositol, ^ 4.00% - 8.00% by weight zinc, ^ 0.01% - 0.50% by weight vitamin B12, ^ 1.00% - 5.00% by weight film coating, and ^ up to %100 by weight one or more pharmaceutically acceptable excipients, and wherein film coating material is free of titanium dioxide. In other embodiment, the tablet composition of the present invention comprises below: ^ 4.00% - 8.00% by weight vitamin B1, ^ 4.00% - 8.00% by weight vitamin B2, ^ 4.00% - 8.00% by weight vitamin B3, ^ 4.00% - 8.00% by weight vitamin B5, ^ 1.00% - 3.00% by weight vitamin B6, ^ 0.01% - 0.50% by weight vitamin B7, ^ 4.00% - 8.00% by weight inositol, ^ 4.00% - 8.00% by weight zinc, 8    ^ 0.01% - 0.50% by weight vitamin B12, ^ 1.00% - 5.00% by weight coating material of AquaPolish F brown 080.79, and ^ up to %100 by weight one or more pharmaceutically acceptable excipients, and wherein film coating material is free of titanium dioxide. In other aspect of the present invention a process for preparing film coated tablet composition can be comprises below steps a. Sieving and mixing Vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B8, inositol, vitamin B9, vitamin B12, zinc and one or more pharmaceutically acceptable excipient, b. Compressing the tablets, c. Coating with hypromellose, pearlescent amber and one or more film coating agents. In preferred aspect of the present invention a process for preparing film coated tablet compositions can be comprises below steps a. Sieving and mixing Vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B8, inositol, vitamin B9, vitamin B12, zinc, microcrystalline cellulose, croscarmellose sodium, kollidon VA 64, aerosil, magnesium stearate, b. Compressing the tablets, c. Coating with film AquaPolish F brown 080.79 G. In other aspect of a pharmaceutical composition of the present invention for use in the supplementation to support various bodily functions, including energy metabolism, nervous system health, and the maintenance of healthy skin, hair, and eyes. Experiments Stability Results The stability of the product was monitored under the following three conditions. During the stability period, the product was found to meet the specifications. 25°C ± 2°C / %60 RH ± %5 RH 30°C ± 2°C / %65 RH ± %5 RH 40°C ± 2°C / %75 RH ± %5 RH 9   

Claims

CLAIMS 1. A film coated pharmaceutical composition comprising vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B7, vitamin B9, vitamin B12, inositol, zinc and one or more pharmaceutically acceptable excipient, characterized in that film coating comprises hypromellose and Pearlescent Amber, and film coating material is free of titanium dioxide. 2. The film coated pharmaceutical composition according to claim 1 wherein said film coating comprises, 50.00-70.00% by weight hypromellose, 20.00-30.00% by weight Pearlescent Amber. 3. The film coated tablet compositions according to claim 1, wherein said composition comprises: ^ 4.00% - 8.00% by weight vitamin B1, ^ 4.00% - 8.00% by weight vitamin B2, ^ 4.00% - 8.00% by weight vitamin B3, ^ 4.00% - 8.00% by weight vitamin B5, ^ 1.00% - 3.00% by weight vitamin B6, ^ 0.01%-0.50% by weight vitamin B7, ^ 4.00%-8.00% by weight inositol, ^ 4.00%-8.00% by weight zinc, ^ 0.01%-0.50% by weight vitamin B12, ^ 1.00%-5.00% by weight film coating, and ^ up to %100 by weight one or more pharmaceutically acceptable excipients, and wherein film coating material is free of titanium dioxide. 4. A process for preparing film coated tablet compositions according to claim 1, comprising the steps of a. Sieving and mixing vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin 6, vitamin B8, inositol, vitamin B9, vitamin B12, zinc and one or more pharmaceutically acceptable excipient, b. Compressing the tablets, c. Coating tablets with hypromellose, pearlescent amber and one or more film coating agents, and wherein film coating material is free of titanium dioxide. 10