Antibacterial drugs in conventional and dispersible forms. What to choose?
Jurga Knašienė
LSMU MA Geriatrics clinic
The results of drug treatment depend not only on the ingredients but also on the optimal selection of the drug form and method of administration. One of the most common obstacles when taking conventional forms of medication is the inability to swallow a tablet due to mechanical gastrointestinal obstruction or impaired swallowing. There are people, usually children and the elderly, who are generally reluctant to take tablet forms, afraid to swallow overly large or small tablets, dissatisfied with the color, coating, and other physical properties of the tablet.
It is difficult for patients who have experienced a stroke, suffer from Parkinson's or other progressive neurological diseases, oncological, cardiovascular, respiratory system diseases to swallow a conventional form of medication.
The danger of breaking the integrity of tablets or capsules
PSA QLD Pharmacy Research Trust report states that crushed tablets and opened capsules are unsuitable for treatment. Changing the pharmaceutical form of a drug causes it to lose all its pharmacological properties and potentially become dangerous to health, as it is difficult to predict its therapeutic effect. Inhaling crushed drug particles or powders can also be dangerous, as they can damage the mucous membranes or even cause respiratory tract obstruction.
It has been proven that altering the established drug form changes its pharmacological properties, increases the toxicity of the drug, reduces effectiveness, safety, and bioavailability. In 70% of cases, the dosage of the active substance decreases, which raises doubts about the treatment with such drugs.
Breaking the coating of tablets not only changes the appearance of the drug but also its absorption properties. The coating of the drug is not intended to improve the cosmetic appearance of the drug but to protect the active substance from moisture, sunlight, temperature changes, thereby improving the taste properties of the active substance. In modern preparations, the coating plays a significant role in the rate of drug release or the release of the active substance in a specific location of the gastrointestinal tract, protecting it from the aggressive effects of stomach juices, which should reach the small or large intestine. By damaging the coating, the active substance may be released too quickly and in excessive amounts, causing local reactions such as irritation or ulcers in the gastrointestinal tract.
When selecting a drug form, the doctor must anticipate the patient's problems related to swallowing a tablet.
It is recommended to pay attention if patients complain of:
• discomfort when chewing and swallowing;
• dry mouth;
• coughing before, during, and after swallowing;
• changes in voice, hoarseness;
• sensation of a lump in the throat (obstruction);
• regurgitation of undigested food;
• recurrent aspiration pneumonia;
• unexplained rapid weight loss;
• throat pain.
In such cases, alternative drug forms are recommended for the patient, such as chewable, buccal, sublingual, transdermal, rectal, intranasal, and injectable drug forms.
Dispersible forms of antibacterial drugs are superior
The success of drug treatment depends on several factors, such as: individual drug selection for each patient according to indications, drug dosage and regimen, as well as the optimal selection of the drug form and route of administration. Sometimes it is difficult to comply with the latter condition, as half of the patients have difficulty swallowing conventional oral forms of medication.
It has been revealed that many patients, in order to swallow tablets more easily, crush them into pieces or even crush them into powder, which can make treatment unsuccessful or even dangerous. When surveyed, it was found that they still trust liquid oral forms of medication more. However, due to the requirement to maintain an optimal "antibiotic/stabilizer ratio," high concentration suspensions cannot be created, so the latter forms of drugs are used only in pediatric practice and cannot be adapted for adult treatment. Meanwhile, dispersible drug forms, unlike conventional effervescent tablets, have important pharmacokinetic advantages.
Medicines Ospamox GDT (orodispersible tablets) and Amoksiklav GDT are manufactured using patented technology. The essence of this technology is the production of three-phase tablets with uniform pharmacokinetic properties both when swallowed and dispersed (dissolved) in water.
Advantages of Ospamox and Amoksiklav dosage forms:
• ensures a constant concentration of clavulanic acid and maximum protection of amoxicillin;
• wide absorption area ensuring a steady increase in drug concentration in the blood serum;
• stable absorption;
• minimal impact on intestinal microflora;
• easy administration: when preparing for administration, dispersible tablets need to be thoroughly mixed in a small amount of water, taken with food to minimize the risk of gastrointestinal side effects and ensure optimal absorption of amoxicillin/clavulanic acid;
• ensures increased fluid intake, preventing the development of acidosis.
• in cases of sore throat, difficulty swallowing, the dispersible dosage form ensures convenient and effective treatment
Summary
When evaluating literature data, it is important to emphasize that successful drug treatment depends not only on the active ingredients but also on the optimal selection of the dosage form and method of drug administration. Most patients find it easier to swallow tablets by crushing them into pieces or even into powder. The same problems arise when taking capsules: patients simply open the capsule and swallow the powder, which can make the treatment ineffective.
Case Study I
In November 2013, a 10-year-old boy J. K. was treated for 3 days of persistent fever, sore throat, swallowing difficulties, general weakness, and drowsiness. Consulted with an ENT specialist, diagnosed with bacterial tonsillopharyngitis, treatment included antipyretics, fluids, and antibiotic therapy with Amoxicillin tablets. After three days, the fever intensified, and the child's swallowing difficulties worsened due to pain. The pediatrician was called to the house again, who, after examining the tonsils, decided to change the antibiotic treatment. The treatment was changed to amoxicillin with clavulanic acid twice a day, but it was ineffective. Upon further investigation of the medical history, it was discovered that the child's mother was crushing the tablets for easier swallowing. The pediatrician, recognizing the situation and the ineffective antibiotic treatment due to poor drug absorption from incorrect administration, prescribed special dispersible doses of Amoksiklav.
After 3 days of treatment, the child's condition improved, the fever subsided, the tonsils decreased in size, and the fever and throat pain gradually subsided.
Case Study II
A 12-year-old patient V. Š. sought medical attention for acute rhinitis, fever up to 38.5°C, sore throat, and cough. From the medical history - the girl constantly suffers from upper respiratory tract infections. At home, she drank warm fluids, teas, performed nasal lavages, and took 200 mg of ibuprofen once. However, as the symptoms progressed, she sought medical help.
Upon examination, the patient had a temperature of 37.5°C, reddened tonsillar arches, and purulent nasal discharge. Tenderness was noted in the left cheekbone area upon palpation. Bilateral vesicular breathing in the lungs.
In the general blood test, a mild leukocytosis up to 15 thousand, deviation to the left, and an increased C-reactive protein of 80 mg/l were observed. Acute sinusitis was diagnosed. The girl was prescribed a broad-spectrum antibiotic in dispersible tablets because she couldn't swallow the tablets due to painful swallowing. The antibiotic course lasted for 14 days, after which the patient recovered.
Discussion of Clinical Situations
One of the problematic groups includes children weighing 40 kg or more who require antibacterial treatment and have a sore throat, making it difficult for them to swallow a tablet. In this case, it is best to prescribe dispersible tablets, as they are easier to take, increasing the likelihood that the child will swallow them. Evaluating clinical situations, treating physicians timely identified the possible cause of treatment failure and prescribed appropriate treatment, which helped avoid more serious disease complications.
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