Bioequivalence of generic drugs of loratadine

Loratadine, analogues of which contain the active substance Loratadinum, is intended to relieve allergic reactions. The complex chemical formula helps block H1 histamine receptors and makes this drug vital. All loratadine substitutes are long-acting drugs.

The active substance of synthetic origin is a whitish powder, insoluble in water. Once in the body, it is absorbed in the small intestine and selectively blocks H1-histamine receptors. Loratadine prevents histamine from affecting smooth muscles and blood vessels, reduces capillary permeability, and slows down exudation.

The effect after taking the tablet begins to appear 2 hours after the drug reaches the intestines and begins to be absorbed. The effect of the drug does not depend on food intake. The activity of one dose reaches a maximum after 8 hours and lasts for at least a day. Therefore, it is enough to take one tablet a day to alleviate the condition of allergic reactions of various types.

Tavegil - general information

This drug belongs to the first generation antiallergic drugs, and has existed on the pharmacological market for about seventy years. In terms of its properties, it is in many ways reminiscent of the well-known diphenhydramine, and although it has greater effectiveness and duration of action, its cost is noticeably more expensive, and therefore it is used somewhat less frequently.

While showing good effectiveness against various forms of allergies, Tavegil at the same time has a large number of side effects characteristic of the first generation of antihistamines. The main ones are the following: drowsiness, lethargy, feeling tired, decreased reaction speed, dry mouth, headache, coordination disorders, nausea, constipation. In rare cases, the drug itself can cause allergic reactions. Affects the ability to drive vehicles, mental and physical activity.

DIAZOLIN

Name:

Artyom Kim
Review:
A fairly effective and affordable drug. It has been used for a long time and with benefit.

Name:

Bombay travel
Review:
Disgusting medicine! I took it for the swelling of my face and as an antihistamine (my wisdom tooth was coming out and hurting) So the allergy pill caused such an Allergy that they barely took me to the hospital!!!!! After 15 min. after taking: Itching of the skin, redness, blisters, then hives, all over the body, with huge spots like a leopard! Only a dexamethosone injection saved me!!!!! PPC is an allergy pill that causes allergies!!!!!! Do not buy! Better than Parlazin or Tavegil! But it’s not Diazolin that causes such reactions that you can die from anaphylactic shock!

Name:

Seryozha GRU
Review:
This is because it is unnecessary to drink anything without a doctor’s prescription! And here we are all doctors of medical sciences, and then we are surprised at mutant viruses that do nothing...

Name:

Belkin
Review:
I haven’t drunk yet, although the doctor prescribed it for tooth inflammation (exudate)... I’ll probably abstain, I’ll be healthier!

Name:

Yulia Groznykh (Zhavoronkova)
Review:
I am allergic to diazolin, I remember almost dying from it

Name:

MiHallna
Review:
Twenty years ago, I started working after college as a district nurse, a pediatrician, a very competent doctor by vocation, and explained about some of its properties: with long-term use and the correct dosage (minimum), an immunomodulatory (or stimulating) effect develops. Has anyone encountered this? Or did I remember wrong? After all, 20 years have passed

Name:

Anastasia Lutsenko
Review:
I took the course after implantation, everything is fine, alive and well

Name:

Tatyana Parfenova
Review:
The reaction was the opposite, I couldn’t sleep all night!

Name:

Antonina Maksimova
Review:
I drink it and I’m glad that I found a way out of hives, it helps a lot

Name:

Andrey Tremba
Review:
suprastin did not help, but diazolin helped with urticaria

Name:

Nikita
Review:
an excellent drug, quickly relieves swelling, makes breathing easier, the whole family uses it.

Loratadine - general information

This is a much “younger” medicine that appeared on the pharmaceutical market in the eighties of the last century. Refers to second-generation antihistamines, which do not have the listed disadvantages and frequent side effects. Only in rare cases can undesirable symptoms occur, but still their severity is much weaker than that of Tavegil.

At the same time, the disadvantage of second-generation antiallergic drugs, which include Loratadine, is their cardiotoxic effect , as a result of which they are not recommended for patients with cardiovascular pathologies.

The duration of the therapeutic effect of Loratadine is long - up to 24 hours , as a result of which it is usually prescribed once a day.

Bioequivalence of generic drugs of loratadine

In connection with the expansion of the pharmaceutical market due to generics, questions arise about assessing the identity of their action in comparison with original drugs and the need to conduct research to determine their interchangeability, since the effectiveness, safety, as well as the severity of side effects of generic drugs can vary significantly. The main reasons for this are differences in pharmaceutical technology for drug production, excipients (EX) used, properties of substances, drug packaging, storage conditions, transportation, etc.

Most of the antihistamines used have a number of specific pharmacological properties that characterize them as a separate group.

In terms of their chemical structure, most of them belong to fat-soluble amines, which have a similar structure. The core is represented by an aromatic or heterocyclic group and is linked via a nitrogen, oxygen or carbon molecule to an amino group. The core determines the severity of antihistamine activity and some of the properties of the substance. Knowing its composition, one can predict the strength of the drug and its effects, for example, the ability to penetrate the blood-brain barrier.

Recently, 2nd generation antihistamines have been created, which have significant selectivity and act only on peripheral H1 receptors. These drugs do not cross the blood-brain barrier and therefore do not cause central nervous system side effects.

Claritin is deservedly considered the most promising oral antihistamine (the “gold” standard of therapy).

Loratadine (Claritin) is the most frequently prescribed “new” antihistamine, does not have a sedative effect, does not have significant drug interactions, including interactions with alcohol, and is recommended for use by patients of all age groups, available without a doctor’s prescription.

Generic drugs are cheaper than the original drug, therefore they are in greatest demand among a wide range of consumers. But the issue of bioequivalence of generic drugs is relevant both for people suffering from allergies and for doctors.

The purpose of the study is to conduct quality control of generics of loratadine and the original drug Claritin.

Research objectives:

1. Consider the pharmacological properties of loratadine
2. Carry out quality control of loratadine preparations
3. Conduct an analysis of the bioequivalence of generic drugs.

The object of the study is generic drugs of loratadine.

Subject of the study – Medicines with the active ingredient loratadine: “Claritin” Schering-Plough Labo NV (Belgium), “Loratadine Stada” NIZHFARM (Russia); manufacturer: MAKIZ-PHARMA (Russia), Loragexal tablets Salutas Pharma GmbH (Germany), Lomilan Lek (Slovenia).

Hypothesis: generic drugs are bioequivalent to the original drug.

Research methods:

1. Solubility of drugs containing the active substance loratadine.
2. Chemical method of analysis of loratadine using quantitative determination of the substance of loratadine
3. Dissolution test

When drugs arrive at a pharmacy, they are initially subject to acceptance control. It involves assessing its quantitative characteristics: acceptance of goods, as well as establishing quantitative losses of goods and the reasons for their occurrence.

The legal basis for conducting quantitative analysis is the Civil Code of the Russian Federation (Articles 465, 466, 483, 521), as well as the “Instructions for the acceptance of industrial and technical products and consumer goods by quantity.” Quantitative analysis during acceptance control includes the following operations:

— selection of containers for opening; opening the container; counting the number of units (if necessary, weighing goods); reconciliation with shipping documents.

The supplier delivered the goods to the K-10 pharmacy of Amur Pharmacies LLC in Svobodny, packed in boxes, sealed and sealed, the head of the pharmacy on all copies of invoices, according to the number of places, confirmed with her signatures and seal the fact of receipt of the goods. In case of a discrepancy (if any) between the actual availability of goods and the invoice data, a mark is made on the start and end times of goods acceptance, confirming the fact of acceptance. In our case there was no discrepancy.

The quantity of medicines corresponds to that indicated in the delivery note No. 2936/15

Documentary analysis was carried out on the basis of the invoice.

The pharmacy received medications according to delivery note No. 2936/15 dated May 15, 2015.

In accordance with the delivery note, the drug name, quantity, and serial number correspond to the stated requirements.

I carried out acceptance control of the drug for quality; it consisted of checking: the integrity of the transport container, the absence of obvious defects in the secondary consumer packaging; availability of a complete set of documents confirming the quality of the delivered batch of drugs (declaration of conformity of the quality of this drug, certificate of conformity of the quality of the drug, manufacturer’s passport, analysis protocol, etc.); compliance of the remaining shelf life of the medications taken with the terms of the contract.

If the organization accepting medicines has accepted a declaration of conformity of the quality of medicines based on the quality management certificate of the manufacturer, as third-party evidence, the acceptance of medicines for quality includes checking for compliance with the requirements of the RD for the following indicators: “Description”, “ Packaging", "Marking".

Requirements for labeling and packaging of medicines for medical use are established by Article 46 of the Law “On the Circulation of Medicines”.

Medicines have primary and secondary packaging.

On the primary packaging, in a clearly readable font in Russian, the names of the medicinal products (Active substance), batch number, and expiration date are indicated. On the secondary packaging, in a clearly readable font in Russian, the names of the medicinal products (Active substance), the name of the manufacturer of the medicinal product, batch number, registration certificate number, expiration date, methods of use, dosage form, dispensing conditions, storage conditions, and warning labels are indicated.

Tablets Claritin, Laminal, Loragexal, Loratadine Stada are an industrially produced drug. They are obtained by pressing loratadine and excipients and belong to solid dosage forms.

The drugs are used orally as an antihistamine.

Control of packaging and labeling. Tablets are produced in blister packaging made of polymer material and aluminum foil or in blister-free packaging.

Labeling of tablets should include: the name of the enterprise, its trademark, address, name of the drug in Russian, INN (metamizole sodium) dosage, number of tablets, batch number, registration number, expiration date, bar code, storage conditions.

Organoleptic control is a mandatory type of control and consists of checking the dosage form according to the following indicators: appearance, smell, homogeneity of mixing, absence of mechanical inclusions in liquid dosage forms. Dosage forms intended for children are selectively tested for taste.

Control of shape and appearance : Claritin tablets should be white or almost white, free of foreign inclusions, oval, on one side there is a line mark, the trademark “Cup and Flask” and the number “10”, the other side is smooth.

Conclusion: The tablets are white, do not contain foreign inclusions, oval, on one side there is a line mark, the trademark “Cup and Flask” and the number “10”, the other side is smooth.

2.3 Dissolution of drugs containing the active ingredient loratadine

According to the pharmacopoeial article, Solubility (OPS 42-0049-07), in the pharmacopoeial analysis the concept of solubility is given as a characteristic of the approximate solubility of a medicinal substance at a temperature from 15 to 25 degrees. C. The test should be carried out at a fixed temperature, typically 20 +/- 2 degrees. C, unless otherwise indicated in the private monograph.[5]

It is recommended to use solvents of different polarities (usually three); The use of low boiling, flammable (eg diethyl ether) or highly toxic (eg benzene, methylene chloride) solvents is not recommended. A substance is considered dissolved if no particles of the substance are detected in the solution when observed in transmitted light. The solution may contain trace amounts of physical impurities such as filter paper fibers and others. For substances that form cloudy solutions when dissolved, the corresponding indication must be given in the private pharmacopoeial monograph.

We know from the Global Fund that loratadine is insoluble in water, but soluble in acetone, alcohol, and chloroform.[5]

Studies were conducted on Claritin and its generics.

Dissolving Claritin in acetone:

Add 1.0 ml of acetone to 1.00 g of ground claritin substance and shake continuously for 10 minutes. at 20 C. The substance did not dissolve completely, we continue the experiment by adding 1.0 ml of acetone to 100 mg of ground claritin substance and carry out the dissolution, claritin is completely dissolved, it is easily soluble.

Dissolving Claritin in alcohol:

To 1.00 g of ground claritin substance add 1.0 ml of 96% alcohol and shake continuously for 10 minutes. at 20 deg. C. Claritin has dissolved completely, it is easily soluble.

Dissolving Claritin in chloroform:

Add 1.0 ml of chloroform to 1.00 g of ground claritin substance and shake continuously for 10 minutes. at 20 C. Claritin did not dissolve completely, we continue the experiment by adding 1.0 ml to 100 mg of claritin. chloroform and carry out dissolution, claritin is not completely dissolved. Add 2.0 ml of chloroform and continue dissolution. Claritin has completely dissolved, it is soluble.

Dissolving Claritin in water:

Add 1.0 ml of water to 1.00 g of ground claritin substance and shake continuously for 10 minutes. at 20 C. Claritin has not completely dissolved, we continue the experiment by adding 1.0 ml to 100 mg of claritin. water and carry out dissolution, claritin is not completely dissolved. Add 2.0 ml of water and continue dissolving. Claritin has not completely dissolved, add 7.0 ml of water and continue dissolving. Claritin did not dissolve completely. Then we take 10 mg of Claritin powder, add 10.0 ml of water and dissolve, it does not dissolve completely. We continue the experiment, add 100 ml of water to 10 mg of claritin and dissolve it. Claritin did not dissolve completely; it is practically insoluble in this solvent.

Similarly, “Loratadin Shtad” NIZHFARM (Russia) was dissolved; manufacturer: MAKIZ-PHARMA (Russia), Loragexal tablets Salutas Pharma GmbH (Germany), Lomilan Lek (Slovenia).

During the study, we found that loratadine is insoluble in water, easily soluble in acetone and alcohol, and soluble in chloroform.

To determine the authenticity of loratadine, physicochemical methods (IR and UV spectroscopy) are currently used mainly, purity is controlled by thin layer chromatography, and UV spectrophotometry is used to analyze dosage forms. The UV absorption spectrum of the drug solution prepared for quantitative determination in the region from 220 nm to 290 nm should have a maximum at a wavelength of 246 nm.

The determination is carried out by thin layer chromatography using silica gel F254 R as a thin layer.

To a sample of mixed powder of crushed tablets, equivalent to 10 mg of loratadine, add 5 ml of glacial acetic acid, shake for 20 minutes and settle. 10 μl of the test solution and 10 μl of the reference solution are applied to the starting line of the chromatographic plate. The plate with the applied samples is dried in air for 10 minutes and placed in a chromatographic chamber with a solvent system. When the solvent front passes 10 cm from the starting line, the plate is removed from the chamber, dried in a stream of cold air and viewed under UV light at a wavelength of 254 nm. The chromatogram of the test solution should show a main spot at the level of the main spot on the chromatogram of the reference solution, corresponding to it in size and absorption intensity.

In a college setting, a chemical method for analyzing loratadine is available by quantifying the loratadine substance.

Quantitative determination is carried out by non-aqueous titration. About 0.1 g (exactly weighed) of the substance is dissolved in a mixture of 5 ml of glacial acetic acid and titrated with a 0.1 M solution of perchloric acid until color appears (indicator - 0.1 ml of 0.1% phenolphthalein).

1 ml of 0.1 M perchloric acid solution corresponds to 38.288 mg C22H23ClN2O2 x HCl.

Dissolution test. Loratadine drugs are widely used for acute and chronic allergic diseases. Used in oral dosage forms, they have high bioavailability. However, differences in therapeutic efficacy are often observed, which in some cases are due to differences in the release of the active substance from the generic dosage form. Confirmation of the biequivalence of generic drugs using the “Dissolution” test is considered one of the current approaches to this problem.

When assessing the bioequivalence of loratadine, a dissolution test is recommended.

It is known that the release of medicinal substances is influenced by 2 groups of factors: the physicochemical properties of the substance (its solubility, particle size, crystalline state) and factors depending on the dosage form (manufacturing technology, excipients).

The FDA's industry guidance on the dissolution test for solid dosage forms recommends a biopharmaceutical classification of drugs, proposed in 1995, based on the solubility of the drug substance and its absorption in the gastrointestinal tract.

According to accepted opinion, a substance is “highly soluble” if at pH values ​​of 1-8 in 250 ml. buffer dissolves the entire dose of the active substance. It is also considered that a substance is “well absorbed” if at least 80% of the dose is absorbed from the gastrointestinal tract.

In accordance with these criteria, 4 groups of substances are distinguished:

Dissolves well + is well absorbed

Poorly dissolved + well absorbed

Well dissolved + poorly absorbed

Poorly dissolved + poorly absorbed

The presence of a main center in the loratadine molecule, the aromatic pyridine nitrogen atom, determines the good solubility of this compound in solutions of mineral acids. Loratadine is practically insoluble in water.

It is obvious that in the environment of gastric juice, which has a pH value from 1 to 4, the main nitrogen atom is predominantly in an ionized state, which determines the good solubility of loratadine. At the same time, the tembioavailability of loratadine when administered orally is quite high. Therefore, this drug can be classified as group 1 according to the biopharmaceutical classification.

The objects of the study were tablets containing loratadine of various Schering-Plough Labo NV (Belgium), “Loratadine Stada” NIZHFARM (Russia); Manufacturer: MAKIZ-PHARMA (Russia), Loragexal tablets Salutas Pharma GmbH (Germany), Lomilan Lek (Slovenia).

The “Dissolution” test is carried out in accordance with GPM 42-0003-04 - “Dissolution” [18] on a SOTAX AT 7 smart device, a “paddle stirrer” apparatus. The volume of the dissolution medium is 900 ml, the temperature is –37°C. The rotation speed of the paddle mixers is 50 rpm. A hydrochloric acid solution with pH 1.0 was used as a dissolution medium.

The preparation of the medium pH was controlled using a pH meter.

The study is carried out on 6 samples of tablets for each drug. Sampling time: 5, 15, 25, 45, 60 minutes after the start of the test. Sample volume – 10 ml. After selection, the dissolution medium was replenished in the appropriate volume. Samples were diluted with dissolution medium and then filtered through a white ribbon paper filter, discarding the first portion of the filtrate.

In college conditions, an imitation of the “shovel stirrer” device was carried out. Dissolution volume - 900 ml. temperature -37 degrees. Rotation speed 50 rpm. A hydrochloric acid solution with pH 1.0 was used as a dissolution medium.

The study was conducted on 6 samples of tablets for each drug.

Sampling time - after 5, 15, 25, 45, 60 minutes. after the start of the test. Sample volume 10 ml.

After sampling, the dissolution medium was replenished in the appropriate volume. Samples were diluted with dissolution medium and then filtered through a white ribbon paper filter, discarding the first portion of the filtrate.

Release profiles of loratadine from tablets were obtained and subjected to quantitative analysis. According to the analysis of the data obtained, loratadine quickly goes into solution: after 15 minutes, at least 70% of the active substance is released.

Release profiles of loratadine at pH 1.0

Calculations were also made for Loragexal, Lominal, and Loratadine STADA. According to the analysis of the data obtained, the most significant differences between the release profiles were observed at the beginning of the test at the 5 min point.

Based on the results of the “Dissolution” test, we can conclude that in 60 minutes in a medium of 0.1 M hydrochloric acid, the tablets are almost completely dissolved; at least 80% of the drug substance passes into the solution, which meets the requirements of General Pharmacopoeia Monograph 42-0003-04 (Dissolution) .

Thus, tablets produced by Loratadin Shtada NIZHFARM (Russia); Manufacturer: MAKIZ-PHARMA (Russia), Loragexal tablets Salutas Pharma GmbH (Germany), Lomilan Lek (Slovenia). are bioequivalent in comparison with the standard analogue - Claritin tablets (Belgium).

Conclusion

In recent years, much attention has been paid to the production of generic drugs and generic replacement of original drugs during pharmacotherapy. The use of high-quality generics significantly reduces government health care costs and at the same time ensures good quality of treatment.

The use of generics is beneficial both for the individual patient and for healthcare as a whole only if they have reliable evidence of equivalence and interchangeability with respect to the original drug. Therefore, checking generics for all types of equivalence during their registration helps solve the problem of availability of drugs with proven interchangeability.

Assessment of bioequivalence (“pharmacokinetic equivalence”) of medicines is the main type of medical and biological control of reproduced (generic) medicines that do not differ in dosage form and content of active ingredients from the corresponding original medicines; bioequivalence studies allow one to make informed conclusions about the quality of compared drugs in relation to to a smaller volume of primary information and in a shorter period of time than during clinical trials, however, these studies do not evaluate the effectiveness of the drug with its long-term use. There is also information about a greater number of side effects among generics compared to original drugs. A number of publications provide data that when replacing original drugs with generics, the budget for drug supply can be reduced by approximately 11%. At the same time, large pharmaceutical companies involved in the development of new drugs indirectly incur losses, and accordingly, this may hinder new developments.

According to literature sources, most doctors believe that generics are inferior in effectiveness to original drugs.

Our study, using the example of Claritin and its generics, shows that the quality of generic drugs supplied to pharmacies meets regulatory requirements.

Generics of loratadine are bioequivalent, i.e. interchangeable. The highest price was set for claritin, the lowest price for loragexal.

Conclusions:

1. Description, packaging and labeling and organoleptic control of the study drugs comply with regulatory requirements.
2. Based on the results of the “Dissolution” test, we can conclude that in 60 minutes in a medium of 0.1 M hydrochloric acid, the tablets are almost completely dissolved; at least 80% of the drug substance passes into the solution, which meets the requirements of OFS 42-0003-04 (Dissolution ).
3. Thus, tablets produced by Loratadin Shtada NIZHFARM (Russia); manufacturer: MAKIZ-PHARMA (Russia), Loragexal tablets Salutas Pharma GmbH (Germany), Lomilan Lek (Slovenia) are bioequivalent in comparison with the standard analogue - Claritin tablets (Belgium).

Recommendations:

1. Buyers who want to achieve quick action to relieve an allergic reaction should be offered the drugs Claritin, Loragexal, because after 5 minutes their bioavailability is 70%.
2. Recently, most buyers are buying generics of loratadine. People are interested in drugs of good quality, but at a more social and attractive price. In the current economic crisis, people have begun to save money, but they are equally concerned about quality drugs. Loratadine shtada, lominal, and loragexal have these qualities. These drugs are of high quality and have a reasonable price.
3. At the patient’s request to offer him a modern antihistamine, the pharmacist can first of all offer the original drug Claritin with a convenient once-daily dosage form, without a hypnotic effect.

List of used literature:

1. Belikov V.G. Pharmaceutical chemistry. At 2 o'clock / V.G.Belikov. – M.: MEDpress-informa, 2007.
2. Gaevy M.D. Pharmacology / M.D. Gaevy, V.I. Petrov, L.M. Gaevaya. Ed. IN AND. Petrova. – M.: ICC “MarT”, 2008.
3. Glushchenko N.N. Pharmaceutical chemistry. / N.N. Glushchenko, T.V. Pleteneva, V.A. Popkov; edited by T.V. Pleteneva. – M.: Academy, 2004.
4. State Pharmacopoeia XI. Issue 1. General methods of analysis. M.: Medicine, 1987. –6. Vikulova, S.O. Bioequivalence and generics: created for each other / S.O. Vikulova // Remedium. - 1999. - No. 12.

Similarities between the two drugs

Tavegil and Loratadine, for all their dissimilarity, have a number of common properties.

The first thing that these two popular medications have in common—no matter how trivial it may sound—is their anti-allergy effect. Both are antihistamines, used for a variety of allergic conditions, and have generally the same scope of use.

Another common property that is worth noting is their high efficiency . Both drugs exhibit a pronounced effect and give tangible results in various forms of allergies.

The next similarity is that they are both long-acting antihistamines. The duration of their effect reaches 12-24 hours (Loratadine is slightly longer).

Finally, it should be noted that both drugs are widely used not only in adults, but also in pediatric practice (contraindicated in children under 1 year of age). For children they are available in the form of syrup.

When are analogues used?

The instructions for use recommend the use of any antihistamine drug that contains the active ingredient loratadine in the following cases:

• acute atopic conjunctivitis;
• allergic rhinitis;
• rhinitis, nasopharyngitis and pharyngitis of unknown etiology;
• asthma;
• atopic dermatitis;
• hives;
• angioedema;
• unspecified allergic reactions.

After taking it for 24 hours, a single dose of the drug will work in the human body and create the following effect:

• antiallergic;
• antihistamine;
• antiexudative;
• antipruritic.

Instructions for use do not recommend taking analogues for:

• hypersensitivity to the active substance;
• during breastfeeding;
• children under 2 years old.

Treatment of pregnant women with the active ingredient loratadine is possible only on the recommendation of an allergist. The doctor may prescribe one of the drugs if the expected benefit to the patient outweighs the potential risk to the fetus.

What is the difference between Tavegil and Loratadine?

Despite a number of common properties, it would probably not be a mistake to say that there are even more differences between these two popular medications.

Their main distinctive features that should be taken into account when prescribing are the following:

1. Tavegil often produces various side symptoms, while Loratadine does so only in rare cases.
2. Tavegil causes drowsiness, weakness, lethargy, and decreased performance. Such side effects are not typical for Loratadine.
3. Both drugs have good effectiveness and duration of action, but for Loratadine these indicators are slightly higher.
4. Loratadine, unlike Tavegil, in the vast majority of cases does not affect the ability to drive a car or engage in active physical and mental activity.

How to take the pills?

It’s worth saying right away that this medicine is prescribed to children over 12 years of age and adults . When treating allergic conditions, they are prescribed 1 tablet once a day before meals. When treating young patients whose age ranges from 2 to 12 years , the amount of medication taken depends largely on the child’s body weight. If the baby's weight does not exceed 30 kg, then in this case he should take half a tablet every day. If the child’s weight is more than 30 kg, then the norm for taking the medicine is 1 tablet per day.

How does Loratadine ointment work?

When an allergy occurs, a person experiences sneezing and tearing. In addition, as the painful condition develops, he develops rhinitis and swelling. Also, rashes, itching, and skin irritation on the skin. In order to combat the painful condition, you should use Loratadine in the form of an ointment or cream.

Antihistamines produced in this form are subject to a certain set of requirements that are mandatory:

• their intake should lead to a reduction in inflammation present on the skin;
• Treatment with these agents should lead to the elimination of dryness, burning, redness and itching of the skin.
• drugs should provide protection of the skin from infection during the next contact with an irritant substance.

It is worth saying that the drug Loratadine in the form of an ointment has all these properties. When a patient is treated with this medicine, in addition to it, he also takes other antihistamines. For effective treatment, it is mandatory to follow a diet, and in addition to this, use an ointment that eliminates allergy symptoms that have arisen on the skin.

Pharmacokinetics

Loratadine is quickly and completely absorbed from the gastrointestinal tract. The time to reach maximum concentration in blood plasma is 1.3 - 2.5 hours. Eating increases the time to reach maximum concentration by 1 hour. In elderly people, the maximum concentration in plasma increases by 50%; in alcoholic liver damage, the maximum concentration increases with increasing severity of the disease. Protein binding - 97%. Loratadine is metabolized in the liver to form the active metabolite descarboethoxyloratadine with the participation of cytochrome p450 isoenzymes CYP3A4 and, to a lesser extent, CYP2D6. Equilibrium concentrations of loratadine and metabolite in plasma are achieved on the fifth day of administration. The half-life varies from 3 to 20 hours (average 8.4 hours), the active metabolite - 8.8 - 92 hours (average 28 hours); in elderly patients, respectively - 6.7 - 37 hours (average 18.2 hours) and 11 - 38 hours (17.5 hours). In alcoholic liver damage, the half-life increases with increasing severity of the disease. Excreted from the body with urine and bile. In patients with chronic renal failure and during hemodialysis, the pharmacokinetics of loratadine remain virtually unchanged.