Medicinal candy – why do we need dispersible tablets?

Pharmacy is a constantly developing industry, looking for new formulas and forms. The creation of fundamentally new medicinal substances is associated with enormous time and material costs. On average, it takes 12–14 years to bring a new drug to market, and the share of potentially effective molecules in the total mass is 1:10,000 [1]. There is a second way of development - the use of well-known substances in new dosage forms with increased effectiveness, improved bioavailability and minimized side effects. We decided to dwell in more detail on this innovative side of the pharmacological industry and highlight it in a series of materials about modern dosage forms that are already in our pharmacies or are about to appear in stock. And we will begin our immersion into the interesting world of modern pharmaceutical technologies with a concept that is already familiar to pharmacists and pharmacists - modified release of medicinal substances.

What are dispersible tablets?

Most medications in tablet form are intended to be taken orally and must be swallowed and washed down with water. Dispersed tablets are distinguished by the fact that they dissolve in the mouth without additional effort. That is, you just need to put them under your tongue and wait a little, and everything else will happen on its own.

According to regulatory documents, the dissolution rate of dispersible tablets should be no more than 30 seconds.

For the first time, such a drug was developed in 1996 by American scientists, and replaced buccal (cheek) tablets, which had many disadvantages. The product consists of molecules and filler, which form a special microsphere, and under the influence of saliva break down into microscopic components.

The filler retains the active substance and protects it from the destructive effects of hydrochloric acid. They pass through the digestive tract and enter the duodenum, from where the active component penetrates the blood and immediately begins to act.

Where's the active ingredient, Lebowski?

Probably the earliest attempt to create a controlled-release dosage form (DF) was the work of Professor Israel Lebowski, who in 1938 proposed the use of oral pellets coated with a coating that provides prolonged release of the active substance. Just like modern pharmacologists, Lebowski wanted to create an ideal drug that quickly penetrates the zone of action in an optimal concentration and remains in the required dose for a certain period of time sufficient to achieve a therapeutic effect [2]. Of course, technology has come a long way since the 30s of the last century, but the principle declared by Lebowski has remained unchanged.

Modern modified-release drugs are characterized primarily by a change in the mechanism and nature of drug release. They can be intended for different routes of administration - oral, parenteral, implantation, transdermal, inhalation and others.

Modified-release oral dosage forms may be referred to by various English and Russian terms [1].

Table 1: Terms for modified-release dosage forms

Benefits of the drugs

Due to the special release form and mechanism of action, dispersed tablets have advantages over conventional preparations for oral use.

1. Increased bioavailability
   . Dispersed tablets, unlike conventional drugs, are fast-acting. They are not subject to the destructive effects of hydrochloric acid and are better absorbed into the blood.

2. Minimal number of side effects
   . The drugs do not irritate the gastrointestinal mucosa, so they do not have a negative effect on the stomach.
3. Pronounced effect
   . The effectiveness of treatment with dispersible tablets is not inferior to therapy with injection solutions.
4. Ease of use
   . To take medications you do not need to constantly carry water with you, and the pleasant taste completely eliminates discomfort.

Dispersible drugs can be taken by any category of patients. These include young children, people who have problems swallowing (dysphagia), patients with mental disorders, kidney dysfunction, paralysis, etc. For infants, tablets can be dissolved in water or breast milk.

Instantly soluble medications in dentistry

We have already managed to figure out what the word “dispersible” means in the oral cavity. It is worth knowing which drugs in this dosage form can be used to treat dental diseases. Painkillers remain the most popular. When acute pain occurs, the patient wants to get rid of it as quickly as possible. The quickly dissolving product Ketorol Express will help improve your well-being before contacting a specialist. Ibuklin Junior, created on the basis of ibuprofen and paracetamol, will help relieve minor toothache.

What “orally dispersible drugs” means is worth knowing for those who have to undergo antibacterial therapy. In dentistry, drugs such as Sumamed, Amoxicillin Express, Flemoxin Solutab, Amoxiclav can be used. Only a specialist can prescribe such antibiotics.

How to take medications?

Taking dispersible drugs does not cause difficulties for patients. They need to be dissolved in any liquid (tea, milk, juice, etc.) or simply placed under the tongue.

The amount of liquid varies from 50 ml to 1-2 glasses, depending on the content of the active substance. Eating usually does not affect the absorption and bioavailability of the drug, but it is better to clarify this point in the manufacturer’s instructions.

List of dispersible drugs

Most often, antibiotics, vitamins and painkillers are produced in the form of dispersible tablets, but their list is constantly growing. Recently, pharmaceutical companies have begun to produce anxiolytic and antiparkinsonian drugs, as well as ACE inhibitors, in a similar form.

They are used in certain categories of patients who may have difficulty taking medications, and with the advent of drugs in dispersed form, therapy is greatly facilitated.

Antibacterial drugs

Antibacterial agents based on amoxicillin and azithromycin are produced in the form of dispersible tablets, which include:

• Flemoklav Solutab;
• Flemoxin;

• Amoxiclav Quiktab;
• Sumamed.

Antibiotics from this list are used to treat respiratory infections, ENT organs, skin, soft tissues, and genitourinary tracts. They have a wide spectrum of activity and rarely cause side effects - the most common are headaches and digestive system disorders. The dosage depends on the clinical course of the disease, the severity of symptoms, age and characteristics of the patient’s body. No dose adjustment is required in the elderly, as well as in patients with mild to moderate hepatic and renal dysfunction.

Anxiolytic Phenazepam

The anxiolytic drug Phenazepam is considered the most common drug used to treat neurological and psychoemotional disorders, depression, anxiety, etc. It has pronounced therapeutic activity and quickly eliminates unpleasant symptoms.

The key advantage of Phenazepam is that it causes virtually no drowsiness, so it can be used during the daytime.

Phenazepam dispersible tablets can be taken anywhere and at any time if you need to quickly stop a panic attack.

The disadvantage of the oral form of the drug is that it began to act only 1-2 hours after administration. This caused some inconvenience to patients, especially those suffering from panic attacks. After the appearance of Phenazepam in the form of lozenges, this drawback was eliminated - the therapeutic effect of the drug appears 15-20 minutes after administration.

Madopar tablets

Madopar is another popular drug used to treat Parkinson's disease and restless legs syndrome.

It contains the active substance levodopa, which has pronounced therapeutic activity. People diagnosed with Parkinson's disease often suffer from dysphagia and akinesia, conditions that make it difficult to take oral tablets and suspensions.

In addition, most of them are in old age, when the absorption and digestibility of the active components slows down. Madopar in the form of dispersible tablets makes treatment effective and comfortable - the patient does not have to make an effort to swallow the medicine, and the therapeutic effect appears faster and lasts longer.

Prestarium drug

The drug Prestarium belongs to the category of ACE inhibitors, has a vasodilator and hypotensive effect. It is used for chronic heart failure, coronary heart disease and arterial hypertension of any severity.

The active ingredient in perindopril, arginine, lowers blood pressure, normalizes the functioning of the heart and blood vessels, and reduces the load on the myocardium.

Prestarium is recommended for use in patients who suffer from paresis, paralysis and other disorders after strokes to prevent relapses.

Prestarium dispersible tablets are taken once a day, preferably in the morning before meals. You just need to put them on your tongue, wait until they dissolve, and swallow them with saliva. The therapeutic effect begins 15-20 minutes after administration, reaches a maximum after an hour and lasts about a day.

Nise remedy

Nise dispersible tablets are a non-steroidal anti-inflammatory drug based on the active substance nimesulide. It has a pronounced antipyretic, analgesic and anti-inflammatory effect, and is used for any diseases accompanied by fever and pain. Unlike other NSAIDs, Nise does not destroy the gastric mucosa, so it can be used with caution in diseases of the gastrointestinal tract, kidneys and liver. The dosage is prescribed individually, the course of treatment is no more than 7-10 days.

Free drug table:

Despite the fact that dispersible tablets have advantages over traditional drugs, it is better to consult a doctor and study the instructions before use.

Each drug has contraindications and side effects that should be considered before taking. It is especially important to exercise caution when using medications in certain categories of patients - children, pregnant women, people with chronic diseases.

Types of modified release

Modified-release dosage forms differ according to a number of criteria:

• According to the degree of control of the release process - controlled, prolonged (or slow) release.
• According to the kinetics of release - continuous, intermittent, delayed, pulsating.
• By modification of the therapeutic effect - the time of onset of the effect, its duration, severity.

Controlled-release formulations tend to vary the release time of the active ingredient according to the characteristics of the therapeutic effect. Drugs with this release form must meet the following requirements:

• the process of release of the active substance must be described by a known type of mathematical relationship;
• the release of the active ingredient must take place according to a given program at a predetermined speed;
• release should not depend on the action of various physiological and pathological factors - food intake, the action of digestive enzymes, and so on.

When all these conditions are met, the release process becomes predictable, precise in speed, duration and location of release, which allows the therapeutic effect to be predicted. If any of these conditions are not met, the dosage form is prolonged.

Pulsatile or intermittent release dosage forms release the drug at a specific time or over a period of time at the required location and dosage. As a rule, such forms have a reservoir type device, and the release mechanism is provided by shells, osmotic systems and other technological methods. The release period is controlled by the thickness, porosity of the shell or the properties of the polymer “plug”.

In modified pulsatile release systems, a layer of polymer is injected under a semi-permeable outer shell to provide a plateau period of a specified duration (approximately 4-5 hours) and a delayed time of action of the drug. To ensure repeated release, multi-layer or multi-pellet systems are used.

Regular tablets or dispersible

Dispersible preparations are easy to use, have high bioavailability and a pronounced therapeutic effect. They are recommended for use in the treatment of children, people with mental illness, dysphagia, paralyzed patients and those who suffer from serious chronic pathologies.

Despite the fact that their cost is higher than that of conventional tablets, they have advantages and cause less harm to the body. If your doctor recommends taking dispersible agents, it is better to pay more but reduce the likelihood of discomfort during treatment and the development of side effects.

Who can be prescribed medications in this form?

What does “orally dispersible tablets” mean? This question arises among those patients who are prescribed drugs in this form. Specialists have to use medications of this type when the patient, for a number of reasons, cannot take classical medications.

Dysphagia is a disease characterized by impaired swallowing. Pathology can be either congenital or acquired. People often face this problem after a stroke. The patient cannot independently form a food bolus and move it towards the throat. In this case, the use of classical medications becomes impossible. The doctor has to explain to relatives what “oral dispersible tablets” mean and how to give them correctly to the patient.

Medicines in this form are widely used to treat children under 3 years of age. It is possible to carry out therapy in infants without any particular difficulties. In this case, the medication is given to the baby immediately before breastfeeding.

Travelers should know what “orally dispersible tablets” mean. The drug, which dissolves quickly, can be taken while driving. Even if there is no glass of water nearby, the treatment process will not be complicated. The tablet just needs to be placed under the tongue.