Loratadine Capsules are a widely used over-the-counter medication, belonging to the second generation of antihistamines. The main ingredient is loratadine, and it also contains some excipients such as starch, lactose, magnesium stearate, etc. These excipients help with the shaping, stability, and administration of the drug. After the human body comes into contact with allergens, the immune system releases chemicals such as histamine. Histamine binds to histamine receptors on the cell surface, causing a series of allergic symptoms such as sneezing, runny nose, nasal congestion, skin itching, rash, etc. Loratadine can selectively block peripheral H1 receptors, competitively inhibit the binding of histamine to H1 receptors, thereby preventing histamine from exerting its biological effects and achieving the goal of relieving allergic symptoms. Compared with the first generation antihistamines, loratadine is less likely to cross the blood-brain barrier, resulting in weaker central inhibitory effects and less impact on normal human activities. Patients with liver and kidney dysfunction should adjust their dosage under the guidance of a doctor; Elderly people should also be cautious when taking medication and closely monitor for adverse drug reactions. During medication, one should avoid driving motor vehicles, operating machinery, or working at heights to prevent accidents caused by adverse reactions such as drowsiness; If you are using other medications, please consult a physician or pharmacist before using this product.
At the same time, our company not only provides pure powders, but also tablets and injections. If needed, please feel free to contact us at any time.
Additional information of chemical compound:
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Loratadine COA
Loratadine capsules are a widely used second-generation antihistamine drug, mainly used to alleviate symptoms of allergic diseases such as allergic rhinitis and chronic urticaria. It occupies an important position in the pharmaceutical market due to its significant therapeutic effect and relatively small side effects. Understanding the production method of loratadine capsules is of great significance for ensuring drug quality, meeting clinical medication needs, and promoting the development of the pharmaceutical industry.
Preparation before production
Selection and inspection of raw materials and auxiliary materials
Main drug loratadine
Quality standard: It should comply with the provisions of the Chinese Pharmacopoeia or relevant international pharmacopoeias, and the purity is generally required to be above 98.0%. The appearance should be white or off white crystalline powder, odorless and tasteless.
Inspection items: including characteristics, identification, related substances, content determination, etc. Identification can be achieved through methods such as infrared spectroscopy and high-performance liquid chromatography; Strict control of impurity content is required for substance inspection to ensure that it does not exceed the prescribed limit; Accurate determination of the content of loratadine is required to ensure that it meets the requirements of the labeled amount.
Auxiliary materials
Starch: commonly used as a filler to increase the volume and weight of capsule contents. White, odorless, and impurity free starch should be selected, with a moisture content generally not exceeding 12%. The inspection items include characteristics, moisture, ash content, etc.
Lactose: It is also a commonly used filler with good fluidity and compressibility. It should comply with the quality standards stipulated in the pharmacopoeia, and the inspection items include properties, acidity, sulfate, heavy metals, etc.
Magnesium stearate: As a lubricant, it can prevent particles from adhering to the surface of the die during the tablet pressing process, ensuring smooth demolding of the tablet. White, odorless and tasteless magnesium stearate should be selected, and its content should comply with regulations. The inspection items include properties, heavy metals, arsenic salts, etc.
Preparation and commissioning of equipment and instruments
Crushing equipment: such as a universal crusher, used to crush raw materials and some auxiliary materials of loratadine to achieve the appropriate particle size. Before use, it is necessary to check the cleanliness of the equipment to ensure that there are no residues from the previous production; Check whether the cutting tools of the crusher are sharp and operate normally.
Screening equipment: A vibrating screen is a commonly used screening equipment used to screen crushed materials, remove oversized or undersized particles, and ensure uniform particle size of the materials. During debugging, it is necessary to select the appropriate mesh size based on the characteristics of the material and process requirements, and check the integrity and tension of the mesh.
Mixing equipment: such as a V-type mixer, used to evenly mix loratadine and various excipients. Before use, clean the interior of the equipment to ensure there are no impurities; Check the sealing performance of the mixer to prevent material leakage; Set appropriate mixing time and speed to ensure the mixing effect.
Granulation equipment: Wet granulation machine can mix the mixed materials with adhesive to make wet granules. When debugging, it is necessary to select the appropriate stirring blade and granulation knife speed according to the properties of the material, control the amount of water added and granulation time, and ensure that the wet particles produced are uniform in size and moderately elastic.
Drying equipment: Hot air circulation oven is used for drying wet particles. Before use, check if the temperature control system of the oven is functioning properly to ensure accurate control of the drying temperature; Check if the ventilation system is unobstructed to ensure that hot air can evenly pass through the material layer.
Granulation equipment: The swing granulator can round the dried particles to make them more uniform in size. When debugging, it is necessary to choose the appropriate mesh size, control the speed and force of the whole particle, and avoid particle breakage or fine powder production.
Capsule filling equipment: The fully automatic capsule filling machine can accurately fill the whole granules into the capsule shell. Clean the equipment and install suitable capsule molds before use; Debug the filling amount and filling speed of the equipment to ensure that the difference in capsule loading meets the specified requirements.
Packaging equipment: such as aluminum-plastic blister packaging machine, used for packaging filled capsules. When debugging, appropriate packaging materials and molds should be selected according to the specifications of the capsule, and the heat sealing temperature and pressure should be adjusted to ensure the sealing and aesthetic properties of the packaging.
Production process
01
Pre treatment of raw materials and auxiliary materials
Crushing and screening of loratadine: The raw material of loratadine is crushed in a universal crusher, and the crushed material is screened through a vibrating screen to select particles with the required particle size (generally required to pass through an 80-100 mesh screen) for later use.
Processing of excipients: Starch, lactose and other excipients also need to be crushed and screened to make their particle size similar to that of loratadine granules. Magnesium stearate generally does not need to be crushed, but it needs to be sieved to remove clumps.
02
mix
Dry mixing: Mix the sieved loratadine granules with appropriate amounts of starch, lactose, and other excipients in a certain proportion into a V-type mixer. Turn on the mixer and mix at an appropriate speed for 15-20 minutes to achieve initial and uniform mixing of the materials.
Wet mixing: Prepare an appropriate amount of adhesive, such as 10% starch slurry. Slowly add the adhesive to the dry mixed material, while starting the wet granulation machine for stirring and granulation. During the feeding process, attention should be paid to controlling the feeding speed and the amount of adhesive used, so that the material can be evenly wetted and form moderately sized wet particles. The general wet granulation time is 3-5 minutes.
03
Granulation
After wet granulation is completed, transfer the wet particles to a hot air circulating oven for drying. The drying temperature is generally controlled at 60-70 ℃, and the drying time depends on the moisture content of the wet particles and the performance of the drying equipment, usually 2-3 hours. Regularly flip the material during the drying process to ensure even drying. The moisture content of the dried particles should be controlled between 3% and 5%.
04
Whole grain
Dry the particles and use a swing granulator to round them. Choose a suitable sieve (usually 14-20 mesh) to remove particles that are too large or too small, making the particle size more uniform. The whole particle should be loose and free of lumps.
05
Total mixing
Add the whole granules and magnesium stearate to a V-type mixer for total mixing, with a mixing time of 10-15 minutes. The purpose of blending is to evenly distribute magnesium stearate on the surface of the particles, providing lubrication and further ensuring the uniformity of the material.
06
Capsule filling
Selection of capsule shell: Choose the appropriate capsule shell based on the specifications and loading requirements of loratadine capsules. The quality of the capsule shell should comply with relevant standards and be free from defects such as damage and deformation.
Filling operation: add the total mixed particles into the hopper of the automatic capsule filling machine, adjust the filling amount and filling speed, and start the equipment for capsule filling. During the filling process, it is necessary to regularly check the differences in capsule filling volume and appearance quality to ensure compliance with regulatory requirements.
07
package
Aluminum plastic blister packaging: Place the filled capsules into the mold of the aluminum plastic blister packaging machine, and seal the capsules between the aluminum foil and plastic blister through heating, pressure, and other processes. During the packaging process, attention should be paid to controlling the heat sealing temperature and pressure to ensure the sealing of the packaging.
Outer packaging: Put the capsules packaged in aluminum-plastic blister packs into paper boxes or plastic bottles, label them with the drug name, specifications, batch number, expiration date, and other information. The outer packaging should be sturdy, aesthetically pleasing, and able to protect the medication from damage.
Observing the effect of Loratadine Capsules on acetylcholinesterase activity in a rat model, and clarifying the changes in acetylcholinesterase activity in rats treated with different doses of Loratadine. Through this study, on the one hand, it can enrich the understanding of the pharmacological effects of Loratadine and provide a more comprehensive theoretical basis for its rational application in clinical practice; On the other hand, it also helps to reveal the interaction mechanism between drugs and the acetylcholinesterase system, providing reference for the development of new drugs or the discovery of new drug targets.
Materials and Methods
Experimental animals: Select healthy adult SD rats with a weight range of 200-250g, half male and half female. Rats are kept in a standard animal room with an ambient temperature controlled at 22-25 ℃ and a relative humidity of 40% -60%. They are kept in a cycle of 12 hours of light and 12 hours of darkness, and are free to eat and drink. Allow the rats to adapt to the environment for one week before the experiment begins.
Experimental drugs and reagents: Loratadine raw material, purchased from a well-known drug supplier, has been tested for purity and meets the experimental requirements. Loratadine was prepared into solutions of different concentrations using an appropriate amount of physiological saline, namely low-dose group (5mg/kg), medium dose group (10mg/kg), and high-dose group (20mg/kg). Acetylcholinesterase and butyrylcholinesterase activity assay kits were purchased from a professional biological reagent company and stored and used according to the instructions.
Experimental instruments: mainly including electronic balance (used for accurate weighing of drugs and rat body weight), high-speed freeze centrifuge (used for separating components in serum and tissue samples), spectrophotometer (used for measuring cholinesterase activity), constant temperature water bath (providing appropriate reaction temperature), etc.
Experimental grouping and treatment: SD rats adapted to the environment were randomly divided into four groups, with 10 rats in each group: control group, low-dose Loratadine group, medium dose Loratadine group, and high-dose Loratadine group. The control group rats were given an equal volume of physiological saline by gavage, while the low, medium, and high-dose groups rats were given corresponding concentrations of Loratadine solution by gavage once a day for 28 consecutive days.
Sample Collection and Processing: After 28 days of administration, anesthetize the rats and collect blood samples by cardiac blood collection. Place the blood in a centrifuge tube, let it stand for 30 minutes, centrifuge at 3000r/min for 10 minutes, separate the serum, and store it in a -20 ℃ refrigerator for future use. At the same time, quickly remove the liver tissue of rats, rinse it with pre cooled physiological saline, absorb the surface moisture, weigh a certain weight of liver tissue, add an appropriate amount of physiological saline to make a 10% tissue homogenate, then centrifuge at 3000r/min for 15 minutes at 4 ℃, take the supernatant, and store it in a -20 ℃ refrigerator for testing.
Acetylcholinesterase activity determination: The activities of acetylcholinesterase and butyrylcholinesterase in serum and liver tissue were measured using the method provided by the reagent kit. The specific operation steps are strictly in accordance with the instructions of the reagent kit. The absorbance value is measured at a specific wavelength using a spectrophotometer, and the enzyme activity unit is calculated based on the standard curve.
Statistical analysis: Use professional statistical software to process experimental data. Quantitative data is expressed as mean ± standard deviation, and one-way ANOVA is used for comparison between multiple groups. If there is homogeneity of variance, LSD method is further used for pairwise comparison; If the variances are uneven, Dunnett's T3 method is used for pairwise comparison. The difference is considered statistically significant with P<0.05.
result
Effect of Loratadine on serum acetylcholinesterase activity in rats
Compared with the control group, the low-dose Loratadine group showed a slight decrease in serum acetylcholinesterase activity in rats, but the difference was not statistically significant (P>0.05); The serum acetylcholinesterase activity in the medium dose Loratadine group was significantly reduced, and the difference was statistically significant (P<0.05); The high-dose Loratadine group showed a more significant decrease in serum acetylcholinesterase activity compared to the control group, with a highly significant difference (P<0.01).
Effect of Loratadine on serum butyrylcholinesterase activity in rats
There was no significant change in serum butyrylcholinesterase activity in the low-dose Loratadine group compared to the control group (P>0.05); The serum butyrylcholinesterase activity in the medium dose group decreased, and the difference was statistically significant (P<0.05); The high-dose group showed a more significant decrease in serum butyrylcholinesterase activity compared to the control group, with a highly significant difference (P<0.01).
Effect of Loratadine on Acetylcholinesterase Activity in Rat Liver
In liver tissue, there was no significant difference in acetylcholinesterase activity between the low-dose Loratadine group and the control group (P>0.05); The activity of acetylcholinesterase in the liver of the medium dose group was significantly reduced (P<0.05); The high-dose group showed a greater decrease in liver acetylcholinesterase activity compared to the control group, with a highly significant difference (P<0.01).
Effect of Loratadine on the activity of butyrylcholinesterase in rat liver
Low dose Loratadine had little effect on the activity of butyrylcholinesterase in rat liver, and there was no significant difference compared with the control group (P>0.05); The activity of liver butyrylcholinesterase was slightly reduced in the medium dose group (P<0.05); The high-dose group showed a significant decrease in liver butyrylcholinesterase activity, with a highly significant difference compared to the control group (P<0.01).
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