PHARMACEUTICAL AIDS : aA FULL NOTE FOR STUDENTS

 PHARMACEUTICAL AIDS.

·       Oragnoleptic character—Oragnoleptic character mainly based on the sensory organs. Oragnoleptic character involves color, odor, taste, flavor etc.

·       Pharmaceutical aids: - The substances which are essentially used in manufacturing or compounding of various pharmaceutical dosages form is called as pharmaceutical aids. It helps in masking the unpleasant odor, taste, and flavour of any dosages form and made to more elegant during the dosages administration.

·       Drugs are the preparation which contains the active pharmaceutical ingredients and excipients (coloring, flavouring, sweetening agents, preservatives etc). Excipients are also known as the pharmaceutical aids.

·       Pharmaceutical aid or excipients shown no or little pharmaceutical effect but it play an important role to modifying the drugs dosages form (tablets, capsule, syrups, emulsion, solution etc). Example of pharmaceutical aids contains— coloring agents, sweetening agents, emulsifying agent, suspending agents, flavouring agents, diluents, lubricants etc.

·       Importance/Application of pharmaceutical aids—

 

·       It helps in masking the unpleasant odor, taste, and color etc.

·       It insures safe, efficiency, reproducible, and convenient manner of drug delivery.

·       Pharmaceutical aids increase the shelf life of the drugs.

·       It protects the chemical changes and microbial action of main API, they include antibacterial agents and antioxidants.

·       Due to involvement of the pharmaceutical aids we design the different form of shape, size of the dosages form.

·       It is overcomes the patients inconvenience and helps in manufacturing, to design attractive dosages form.

·       Ideal characteristics of the pharmaceutical aids—

 

·       It does not change chemical nature of the drugs.

·       It is does not cause any toxic effects.

·       Masking the unpleasant color, odor, and taste.

·       During administration it does not cause any allergic reactions.

·       Overcomes the patient inconvenience.

·       It prevents the microbial activity or contamination in the pharmaceutical products.

·       It improves the shelf life of the products.

·       It works on low concentration.

·       Cheap and easily available

Pharmaceutical aids, also known as pharmaceutical excipients or inactive ingredients, are substances other than the active pharmaceutical ingredient (API) that are included in a pharmaceutical formulation. They serve various functions in pharmaceutical products, contributing to their stability, bioavailability, appearance, taste, and ease of administration. Here are some key points about pharmaceutical aids:

1. Function: Pharmaceutical aids perform several roles in pharmaceutical formulations, including:

   a. Enhancing Stability: They can protect the active ingredient from degradation due to factors such as light, moisture, or pH changes.

   

   b. Improving Solubility and Bioavailability: Some aids can enhance the solubility and dissolution rate of poorly soluble drugs, thereby improving their bioavailability.

   

   c. Aiding in Formulation and Manufacturing: Pharmaceutical aids can help in the formulation process, ensuring uniform mixing, flowability, and ease of tableting or capsule filling.

   

   d. Providing Color, Flavor, and Appearance: They are often used to enhance the product's aesthetic appeal, taste, or odor, making it more acceptable to patients.

   

   e. Ensuring Drug Delivery: Certain aids can control the release or delivery of the active ingredient in the body, allowing for sustained or targeted drug action.

   

2. Types of Pharmaceutical Aids: There is a wide range of pharmaceutical aids available, and their selection depends on the specific formulation requirements. Common types of pharmaceutical aids include:

   

   a. Fillers and Diluents: These aids provide bulk to formulations, ensuring accurate dosing and facilitating tablet or capsule formation.

   

   b. Binders and Adhesives: They help in tablet compression by providing cohesion and ensuring the tablet's integrity.

   

   c. Disintegrants: Disintegrants promote the breakup of tablets or capsules in the gastrointestinal tract, facilitating drug release and absorption.

   

   d. Lubricants and Glidants: These aids prevent sticking of formulations to the equipment during manufacturing and improve tablet flowability.

   

   e. Preservatives: Preservatives are added to prevent microbial growth and ensure product shelf-life.

   

   f. Coatings and Film Formers: Coatings provide protection, taste masking, or modified release properties to tablets or capsules.

   

   g. Flavors, Sweeteners, and Colors: These aids improve the taste, appearance, and palatability of oral formulations.

   

3. Safety and Regulatory Considerations: Pharmaceutical aids undergo rigorous safety testing and regulatory evaluation. They should be safe for consumption, compatible with the active ingredient, and not interfere with its therapeutic effects. Regulatory authorities, such as the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA), establish guidelines and specifications for pharmaceutical aids to ensure their quality, purity, and appropriate use.

Pharmaceutical aids play a crucial role in the formulation, stability, and administration of pharmaceutical products. They contribute to the overall quality, effectiveness, and patient acceptability of medications, ensuring that they can be safely and effectively used for therapeutic purposes.

 

·       Coloring agent

 

·       Colorants or coloring agents are mainly used to improve the distinctive appearance of pharmaceutical dosages form, which are helps in the identification during manufacturing and increase the patient acceptance towards the pharmaceutical dosages form.

·       In pediatric and geriatrics coloring agents play a major role and attract the consumer by providing the aesthetic appearance to dosages form.

·       Classification of coloring agents—

 

·       On the basis their origin it is divided into two parts—

o   Synthetic—Tartrazine, Azorubine, brilliant blue, erythrosine.

o   Natural—Animal—carmine,      tyrian purple.                                                Plants—Annatto, caramel, lycopene Mineral—malachite, cinnabar, aragonite.

·       On the basis of their solubility it is divided into two categories—

·       Colorant dyes (soluble in the medium) —Indigo carmine, brilliant blue, caramel.

·       Pigments (insoluble in the medium) — Cadmium pigment, chromium pigment, cobalt pigment.

·       Uses/Applications of coloring agents—

 

·       Coloring agent provide the suitable color to formulation and helps in the identification.

·       Increase the consumer acceptance.

 

§  Flavouring agents

 

·       Flavourants or flavouring agents are mainly used for masking the unpleasant or unacceptable odor from formulation and provide more pleasant taste or flavour.

·       There are four basic taste sensations are salty, sweet, bitter, and sour. Flavour added to drug solutions can make a medicine more acceptable to take especially if the drug has an unpleasant taste. In the pediatrics dosages form flavour play a key role for administration of the drugs.

·       Flavouring agents are more sensitive against the heat (thermolabile nature) so it cannot be added prior to an operation involving heat, they

are often mixed with the granules as an alcohol solution. In market many coating tablet are present for masking the flavour.

·       Classification of flavouring agents—

 

·       It is classify into two categories—

·       Natural    flavouring    agents—Citrus    fruit (lemon,     orange),          spice (cinnamon, peppermint, ginger, onion), fruits (apple, banana).

·       Synthetic             flavouring            agents—Benzaldehyde,    cinnamic aldehyde,coumarin,ethyl methyl ketone.

·       Uses/Applications of flavouring agents—

 

·       Masking the unpleasant taste or flavour and provide suitable flavour.

·       Increase the consumer acceptance.

§  Sweetening agents

 

·       Sweetening agents or sweeteners are mainly used for masking the undesirable or bitter taste of any drug formulation and increase the patient acceptance towards pharmaceutical dosages form. In pediatric dosages form it is widely used because children prefer more the sweetening drugs.

·       In Homeopathic medication, small sugar pills are used during the drug delivery. Recently it is widely used in the Ayurvedic medicine also.

·       Sugar is the most widely used sweetening agent, due to its viscosity nature it also used as preservative for liquid preparation.

·       Classification of sweetening agents—

 

·       It is divided into two categories—

·       Natural    sweetening    agent—Glucose,    fructose,           sucrose,                     dextrose, sorbitol.

·       Artificial coloring agent—sucralose, aspartame, saccharin.

 

·       Uses/Applications of sweetening agents—

 

·       Sweetening agent masking the undesirable or bitter taste.

·       Increase the consumer acceptance.

 

 

 

§  Presevative

 

·       Preservative are the chemical agent which prevents the product contamination or product decomposition by the action of any contaminant (environmental or biological). Preservative commonly add in the pharmaceutical and various food products for enhancing their stability and shelf life. Phenolic compounds like sodium benzoate are highly used as preservative during the manufacturing.

·       Classification of preservative—

 

·       On the basis of mechanism of action it is divided into three categories—

o   Antimicrobial agents—that agent which prevents the contamination (gram positive and gram negative) and degradation by microbes is called as antimicrobial agents. These agents are active in low concentration.Example- phenolic compounds, parabens,                              propylene glycol,BHT,BHA.

§  On the basis of their activity it is further divided into two parts.

·       Microbiostatic—that inhibits the growth and multiplication of the microbes.

·       Microbiocidal—that agent direct kills the microbes.

o   Antioxidants agents—those agents which prevents the products oxidation or degradation in the presence of molecular oxygen. Generally API is more reactive towards the oxygen, so antioxidants are mix with the product and overcome the product reactivity.

§  Example— ascorbic acid, citric acid, tocoferols, BHA, BHT.

o   Chelating agents—those agents which form the cyclic compounds or complexes with the pharmaceutical ingredients and prevent the degradation of pharmaceutical formulation

§  Example—EDTA, polyphosphates.

·       On the basis of sources it is divided into two parts—

·       Natural preservatives—vinegar, honey, castor oil, salt, sugar.

·       Synthetic preservatives—sodium benzoate, BHA,BHT.

 

·       Uses/Application of preservatives—

 

·       Preservative enhance the stability and shelf life of the products, so it maintain the product activity for long time.

·       It prevents the product by any microbial contamination increase their resistance power against the microbial growth.

·       Many    environmental     factors    effect    the products                               property,              for overcoming this activity preservative are also used.

·       It also mixes with the food preparation for prevention their oxidation.