Carbamazepine Tablets Research Articles

Pharmaceutical residues in plastic tablet containers: Impacts on recycling and the environment

High-density polyethylene tablet containers are potentially very suitable for recycling, but no data are publicly available on active pharmaceutical ingredients’ (API) residues in empty containers and if they affect the recyclability of pharmaceutical packaging. Plastic tablet containers represented 15 % of pharmaceutical primary packages sold in Finland in 2020 and 2021, equalling 350 tons of plastic per year. We studied the residues of six APIs remaining or adsorbed inside plastic tablet containers. The effects of tablet coating and usage in dose-dispensing services versus households on the API residues, and rinsing water’s ability to remove the residues were evaluated. Up to 940,000 µg/kg of carbamazepine was detected in a container of uncoated carbamazepine tablets. The residues from coated tablets containing the other five APIs were 2.4–6,100 µg/kg. Ten times higher paracetamol residues were obtained in containers from household use than from a dose-dispensing unit. Rinsing can remove most API residues, but it leads to environmental emissions. For example, rinsing water can double carbamazepine emissions from a Finnish wastewater treatment plant where plastic packaging waste effluents are processed. Considering the API concentrations, decreasing residues by rinsing and dilution with other plastic packaging waste, the residues of the studied APIs are not considered an obstacle to the recycling of plastic tablet containers. However, further research is needed on more toxic APIs and the fate of APIs in the plastics recycling process.

Formulation, Development and Evaluation of Extended- Release Tablets of Carbamazepine

The current work sets out to design and develop a carbamazepine (CBZ) extended-release tablet in the treatment of epilepsy using wet granulation technology. The tablets were prepared using HPMC K 100M and ethyl cellulose as hydrophilic and hydrophobic polymers, respectively. The effect of the concentration of the polymer was studied. The studies indicated that the drug release can be modulated by varying the concentration of the polymer. Tapped density, bulk density, angle of repose, Hausner's ratio, and Carr's index were all calculated for powder blends. The prepared trial batches of tablets were first characterized for hardness, friability, weight variation, and drug content to select an optimized batch. An in-vitro dissolution study of the optimized batch (F4) was carried out in distilled water using a USP Type I (basket type) dissolution apparatus at 100rpm. The optimized formulation (F4) showed a drug content of 99.51%. In-vitro drug release of optimized formulation was found to be 88.10% in 24hours. The optimised formulation demonstrated release for up to 24 hours. The optimised formulation's stability was studied for three months at 40±2ºC/75±5% RH, 30±2ºC/65±5% RH, and 25±2ºC/60±5% RH, and the prepared tablets showed no remarkable effect from the stability study. The results suggest that the developed extended-release tablets of CBZ (400 mg) could perform as therapeutically equivalent alternatives to conventional dosage forms, leading to better patient compliance.

In vitro comparative quality evaluation of different brands of carbamazepine tablets commercially available in Dessie town, Northeast Ethiopia

BackgroundGood-quality drugs that fulfill the regulatory parameters and are produced per the current good manufacturing practice (cGMP) standards are very critical for the best therapeutic outcomes. However, the variety of branded drugs circulation in the market often put clinicians and pharmacists in a difficult situation of choice due to the possibility of interchangeability among brands, so we should ascertain the quality of the various brands of drugs, available in the drug market. The purpose of the study was to evaluate the quality and physicochemical equivalence of six brands of carbamazepine tablets that are commercially available in Dessie town, Northeast Ethiopia.MethodsAn experimental study design was used. Six different brands of carbamazepine tablets were purchased from community pharmacies in Dessie town, Northeast Ethiopia, which were selected using simple random sampling methods. Identification, weight variation, friability, hardness, disintegration, dissolution test, and assay for the content of active ingredients were evaluated according to the procedures described in the United States Pharmacopeia (USP) and British Pharmacopeia (BP), and the results were compared with USP and BP standards. The difference (f1) and similarity (f2) factors were calculated to assess in vitro bioequivalence requirements.ResultsThe identification test results revealed that all samples contained the stated active pharmaceutical ingredients and all brands of carbamazepine tablets complied with the official specification for weight variation, friability, and hardness tests. The percentage concentration of carbamazepine was found in the range of 97.85 to 102.09, which met the USP specification of 92% to 108% of the stated amount. Similarly, all samples fulfilled disintegration time (i.e., ≤ 30 min) except brand CA1 (34.183 min) and dissolution tolerance limits (i.e., Q ≥ 75% at 60 min), which was found in the range of 91.673% -97.124%. The difference factor (f1) values were < 15 and the similarity factor (f2) values were > 50 for all the tested brands of carbamazepine tablets.ConclusionThe present study revealed that all brands of carbamazepine 200 mg tablets met the quality control parameters as per pharmacopoeial specifications except the disintegration test of brand CA1, and could be used each brand interchangeably to achieve the desired therapeutic effect.

Development Optimization and Evaluation of Fast Disintegrating Tablets of Antiepileptic Drug Carbamazepine

Background: The main objective of present research work is to formulate the Carbamazepine as Fast Disintegrating tablets to give fast relief and an increase in the patient compliance. Carbamazepine, an antiepileptic, belongs to BCS Class-II and used to control some types of seizures in the treatment of epilepsy and Neuropathic Pain by blocking use-dependent sodium channels.&#x0D; Methods: The powdered materials were compressed by direct compression technique using super disintegrants like sodium starch glycollate, croscarmellose sodium and starch, Magnesium Stearate and Di Calcium Phosphate are used as lubricant and diluents/fillers respectively.&#x0D; Result and Discussion: Totally nine formulations were designed and are evaluated for hardness, friability, thickness, assay, wetting time, Disintegration time, in-vitro drug release. From the Results concluded that all the formulation were found to be with in the Pharmacopeial limits and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) &amp; regression coefficient (r) were calculated. The optimized formulation was characterized with the help of Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FTIR) studies show no interaction between the drug and the excipients. The stability study was conducted as per the ICH guidelines and the formulations were found to be stable, with insignificant changes in hardness, drug content and disintegration time.&#x0D; Conclusion: These results revealed that fast disintegrating tablets of the poorly soluble drug, carbamazepine, showing enhanced dissolution and, hence, better patient compliance.

Impact of drug release in USP II and in-vitro stomach on pharmacokinetic: The case study of immediate-release carbamazepine tablets

The in-vitro reproduction of the real physiological conditions that occur along the gastrointestinal (GI) tract would be the optimum for the dissolution and release testing of pharmaceutical formulations for oral intake. In this study a method for the automated reproduction of the real pH conditions that occurs in the gastric cavity and a device that mimics the same forces exerted by the internal walls of the stomach are presented. Commercial immediate-release carbamazepine tablets were tested in conventional (USP II) and unconventional apparatuses. The gastric pH and the fluid dynamic conditions are factors to be carefully considered since they both affect the drug release profiles. Finally, a PBPK model was used to predict the evolution of plasma drug concentrations knowing the experimental in-vitro GI release behavior. It was found that, for immediate-release carbamazepine tablet, the gastric drug release does not have a major impact on the plasmatic drug concentration.

Formulation and development of paediatric orally disintegrating carbamazepine tablets

Carbamazepine is a medicine used to manage epilepsy and partial or tonic-clonic seizures. This study aimed at formulating and obtaining carbamazepine orodispersible tablets for paediatric use at a 50 mg dose, with a diameter not greater than 6 mm and a tablet weight of 80 mg, through a direct compression process. The SeDeM pre-formulation/formulation method was used to define the characteristics of both carbamazepine and the selected excipients for direct compression. This study succeeded in formulating and obtaining the proposed tablets. Following the application of the SeDeM method, the tablets met the mass uniformity test and showed appropriate hardness values for orodispersible tablets. The tablets also met the United States Pharmacopeia (USP) test specifications at t = 60 min. The orodispersible tablets obtained may improve compliance with paediatric treatment with carbamazepine, ensuring the safety and effectiveness of the medicine.

Chicken-claw needling at Xiaguan (ST 7) combined with intradermal needling on negative emotions in primary trigeminal neuralgia of phlegm obstruction and blood stasis: a randomized controlled trial

To observe the clinical effect of chicken-claw needling at Xiaguan (ST 7) combined with intradermal needling on negative emotion in primary trigeminal neuralgia (PTN) of phlegm obstruction and blood stasis. Sixty cases of patients with PTN of phlegm obstruction and blood stasis were randomly divided into an observation group and a control group, 30 cases in each group. The observation group was treated with chicken-claw needling at Xiaguan (ST 7) combined with intradermal needling (acupoints Sibai [ST 2], Yuyao [EX-HN 4], Hegu [LI 4], Taichong [LR 3] and auricular points Xin [CO15], Shenmen [TF4], Pizhixia [AT4], etc.), once a day, 6 d as a course of treatment, rest 1 d between courses, a total of 2 courses of treatment; and the control group was given oral carbamazepine tablets for 13 days. Before and after treatment, the pain visual analogue scale (VAS), TCM syndromes, self-rating anxiety scale (SAS) scores and the contents of serum neurotransmitter (β-endorphin [β-EP], substance P [SP] and 5-hydroxytryptamine [5-HT]) were compared, and the clinical efficacy was evaluated. After treatment, the VAS, SAS, TCM syndrome scores and the contents of serum SP in the two groups were lower than those before treatment (P<0.05), and the above indexes in the observation group was lower than those in the control group (P<0.05). The contents of serum β-EP and 5-HT in the two groups were higher than those before treatment (P<0.05), and the above indexes in the observation group were higher than those in the control group (P<0.05). The total effective rate in the observation group was 93.3% (28/30), which was higher than 83.3% (25/30) in the control group (P<0.05). Chicken-claw needling at Xiaguan (ST 7) combined with intradermal needling can relieve pain symptoms and negative emotions in patients with primary trigeminal neuralgia of phlegm obstruction and blood stasis, which may be related to the regulation of serum neurotransmitter levels.

Are There Differences in the Homogeneity of the Parts of Tablets Obtained after Subdivision?-A Preliminary Assessment Using an X-ray Microtomography.

Aim: The study aimed to analyze the weight and homogeneity of the parts of tablets containing carbamazepine and tablets with trazodone hydrochloride, obtained after subdivision with a kitchen knife. X-ray microtomography was used for homogeneity analysis. Methods: 30 tablets with carbamazepine and 30 tablets with trazodone hydrochloride were analyzed in terms of weight uniformity after subdivision. Then, seven tablets of each type were analyzed using an X-ray microtomography (Phoenix vǀtomeǀx, General Electric). The absorption of X-rays by an object is proportional to its density. In turn, measurement of the density of the analyzed object in a microtomographic image is the grayscale level. Based on the correlation between the grayscale value and the reference density, from the calibration phantom, we were able to determine the density of any area of the tablet’s scan. Results: During the subdivision, the weight loss exceeded 3% for two carbamazepine tablets, while for trazodone tablets, none lost more than 3%, which is the limit recommended by Food and Drug Administration (FDA). As to the density of the tablets resulting from the microtomographic analysis, two of the whole tablets containing trazodone hydrochloride had a significantly higher density than the remainder (p < 0.001). Similarly, some differences in density were observed in the analysis of the density of tablets of carbamazepine (p = 0.008). Parts of one of the analyzed tablets with trazodone obtained after subdivision differed in terms of pixel brightness, thus density. On the other hand, the uniform density was observed for parts of the split tablets containing carbamazepine. Conclusions: Parts of the trazodone hydrochloride tablets obtained after subdivision differed in terms of homogeneity and weight. Microtomographic methods may be an interesting and useful method for evaluating the uniformity of compounds in solid dosage forms.

The Study of Polymorphism in Pharmaceutical Operating Processes: Granulation Technique for Carbamazepine Tablets

The Study of Polymorphism in Pharmaceutical Operating Processes: Granulation Technique for Carbamazepine Tablets

The Study of Polymorphism in Pharmaceutical Operating Processes: Granulation Technique for Carbamazepine Tablets

The Study of Polymorphism in Pharmaceutical Operating Processes: Granulation Technique for Carbamazepine Tablets

Do Thickening Agents Used in Dysphagia Diet Affect Drug Bioavailability?

Swallowing oral solid dosage forms is challenging in patients with dysphagia who are at risk of aspiration or choking. The most common method to facilitate drug administration in dysphagia patients is to mix the powdered drug with a small amount of thickened water, however little is known about the effects of this method on in vivo bioavailability of drugs. This study aimed to evaluate the impact of thickened liquids on dissolution rate and bioavailability of levetiracetam as a model drug. Powdered commercial tablets of levetiracetam, carbamazepine, atenolol and cefixime were mixed with water thickened with two commercial thickeners, modified maize starch (MS) and xanthan gam (XG), at three thickness levels: nectar, honey and pudding in test groups, and mixed with only water in the control group. At the first stage, the effects of thickened water on in vitro drug release of 4 drugs (levetiracetam, carbamazepine, atenolol and cefixime) were tested by using dialysis membrane method. Addition of both thickeners significantly reduced the release of three drugs compared to the control group, except carbamazepine. Levetiracetam which had the highest solubility was chosen as the model drug for in vivo experiments. In the second stage, New Zealand albino female rabbits (n=24) were divided into two groups as: control group (water+drug, n=6) and test group (thickened water+drug, n=18). Powdered levetiracetam tablets were mixed with water thickened with XG (n=9, 1.2%, 2.4%, 3.6%) and MS (n=9, 4%, 6%, 8%) at three thickness levels and administered to the rabbits by intragastric gavage. Blood samples were collected at 9 time points following administration. After two-weeks of wash-out, test groups were crossed over and sample collection was repeated. Blood samples were analysed using liquid chromatography with tandem mass spectrometry (LC-MS/MS). An in vitro-in vivo correlation (IVIVC) model was developed using in vitro drug dissolution (%) and in vivo plasma concentrations of levetiracetam for control group and test groups. The peak plasma concentration (Cmax) was lower and time to reach Cmax (tmax) was relatively higher in test groups compared to control group. The lowest Cmax was detected at the highest thickness level, however, the differences between groups were not statistically significant (p=0.117 and p=0.495 for Cmax and tmax, respectively). No significant difference in total amount of levetiracetam absorbed (AUC) was found between groups (p=0.215 and p=0.183 for AUCinfinity and AUClast, respectively). The comparisons according to the type of thickener also revealed that pharmacokinetic parameters did not significantly differ between groups, except for a significantly lower Cmax when drug was mixed with MS-thickened water at nectar consistency (1.2%) compared to drug mixed with XG (4%) at the same thickness level (p=0.038). A good correlation was observed between in vitro and in vivo data, which was characterized by higher r2 values as the concentration of the thickening agents was increased, but not for all thickness levels studied, indicating an inability of this in vitro model to fully predict the in vivo response. These results suggest that regardless of the thickness level, the administration of levetiracetam with two commercial thickening agents commonly used in dysphagia for safe swallowing, do not affect the pharmacokinetic efficiency and thus, the bioavailability of the drug.

Carbamazepine Induced Ataxia: A Case Report in Pediatrics

Ataxia is a manifestation which is characterized by lack of coordination in the movement of different muscles in the body due to variety of diseased conditions. Carbamazepine is used as an antiepileptic and for pain disorders and a range of psychiatric diagnoses that shows ataxic symptoms in a dose-dependent manner. Toxic effects are due to the drug’s anti-cholinergic activity, sodium channel blockade, CNS depression and myocardial depressant properties. Even at therapeutic doses, patient might show mild signs of toxicity and hence serum drug concentration needs to be monitored regularly. In case of mild to moderate toxicity, treatment is not required. This is a common yet rarely reported case report of carbamazepine induced ataxia in a pediatric patient of 6 years old male child who was presented with chief complaints of headache, stiffness of body, generalized weakness and nausea since one week. He had 2 episodes of vomiting at morning and stiffening of body which lasted for few seconds on the day of admission. He had history of ingestion of 3 tablets of carbamazepine of strength 100mg for headache. Supportive treatment was provided and was closely monitored by a multi-disciplinary team for clinical features of ataxia which was reversed after 3 days of hospital stay.

Comparative Study of Different Products of Carbamazepine Tablets Available in Iraqi Market

Carbamazepine (CBZ) is a widely used antiepileptic drug to control grand mal epilepsy, as well as for the treatment of peripheral neuralgia. According to the biopharmaceutical classification system (BCS), CBZ is considered a class II drug. CBZ is characterized by a slow and irregular gastrointestinal absorption, with irregular oral bioavailability; due to its low water solubility. Therefore, the release of the drug from the dosage form (tablets in this study) and the subsequent step of dissolution represent the most important parameters that decide whether a sufficient plasma concentration will be achieved or not. In the current study, the FTIR study for the pure API, CBZ, and the different commercially available brands of CBZ conventional tablets, available in the Iraqi drug market (Mosul city as an example), were examined. Subsequently, various quality control parameters such as the weight variation, content uniformity, friability, and hardness of the conventional CBZ tablets were conducted. Moreover, the disintegration and the dissolution tests of the different brands of CBZ available in the Iraqi drug market were performed.&#x0D; Keywords: Antiepileptic Drug, Bioequivalence; Epilepsy; Generic; Brand vs generic; IVIVC; QC

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Carbamazepine.

Literature relevant to assessing whether BCS-based biowaivers can be applied to immediate release (IR) solid oral dosage forms containing carbamazepine as the single active pharmaceutical ingredient are reviewed. Carbamazepine, which is used for the prophylactic therapy of epilepsy, is a non-ionizable drug that cannot be considered "highly soluble" across the range of pH values usually encountered in the upper gastrointestinal tract. Furthermore, evidence in the open literature suggests that carbamazepine is a BCS Class 2 drug. Nevertheless, the oral absolute bioavailability of carbamazepine lies between 70 and 78% and both invivo and invitro data support the classification of carbamazepine as a highly permeable drug. Since the therapeutic and toxic plasma level ranges overlap, carbamazepine is considered to have a narrow therapeutic index. For these reasons, a BCS based biowaiver for IR tablets of carbamazepine cannot be recommended. Interestingly, in nine out of ten studies, USP dissolution conditions (900mL water with 1% SLS, paddle, 75rpm) appropriately discriminated among bioinequivalent products and this may be a way forward to predicting whether a given formulation will be bioequivalent to the comparator product.

Analysis of the effect of sodium valproate sustained release tablets on epilepsy control and cognitive improvement in elderly patients

Background: To study the effect of sodium valproate sustained release tablets on epilepsy control and cognitive function improvement in elderly patients.Methods: Study was conducted from January 2018 to December 2019, the elderly epilepsy patients admitted in our center were prospectively collected and divided into experimental group and control group according to the method of random number table. The experimental group was treated with sodium valproate sustained-release tablets, and the control group was treated with carbamazepine tablets. The epilepsy control rate and cognitive function improvement of the two groups were observed.Results: total of 71 patients entered the study, including 36 in the experimental group and 35 in the control group; the epilepsy control rate (p = 0.03) and the improvement of cognitive function (p = 0.01) in the experimental group were better than those in the control group.Conclusions: Sodium valproate sustained-release tablets can improve the epilepsy control rate and cognitive function of elderly epilepsy patients, but it needs further large samples and external data validation.

Formulation and Evaluation of Carbamazepine Tablets using Biosurfactant in Ternary Solid Dispersion System

Abstract: Objectives: The present study is aimed to develop and evaluate Carbamazepine tablets using ternary solid dispersed product. Carbamazepine belongs to BCS class II having low solubility. Ternary system was formulated with biosurfactant and water-soluble polymers to enhance dissolution rate and bioavailability. Methods: Binary and ternary solid dispersion was prepared using hydroxyl propyl methyl cellulose (HPMC) K-100, Polyvinyl pyrolidine (PVP) K-30 and Poly ethylene glycol (PEG) 6000 as a polymer and biosurfactant respectively by solvent evaporation method and evaluated for drug content uniformity and in-vitro dissolution study. Carbamazepine tablet were prepared by incorporation of ternary solid dispersed product along with other excipients by direct compression technique. Prepared formulations were evaluated for pre-compression and post-compression parameters. Oral toxicity study of biosurfactant was performed using female wistar rats. Results: In-vitro dissolution profile of optimized tablet formulation OF1 and OF2 showed 75.14% and 71.26% release in 1.2 pH respectively and similarly at 6.8 pH buffer 64.33% and 58.96% respectively. Pre-compression and postcompression values of formulated tablets were within the specified acceptable limits. In-vivo dissolution study of optimized formulation OF1 showed an increase in dissolution rate in accordance with pure drug. Oral toxicity study of biosurfactant was safe at 2000 mg per kg body weight of rat. Short term stability of the optimized formulation was stable without deviations at room temperature. Conclusion: Addition of biosurfactant in ternary solid dispersion system proved to be promising excipient in formulation of carbamazepine tablet for enhanced dissolution rate, dose reduction and bioavailability. Key words: Carbamazepine, Solid dispersion, Ternary system, Biosurfactant, in-vivo oral toxicity.

Spectrophotometric Determination of Carbamazepine in Pharmaceutical Formulations Based on its Reaction with a Brominating Agent

Two accurate spectrophotometric methods described for the estimation of carbamazepine (CBZ) in both pharmaceutical and pure form. These methodologies are attached to the bromination of CBZ by bromine formed in instantly from the bromate-bromide reaction. The general procedure includes the additional of a known amount of bromate-bromide reagent in an acidic mediocre to CBZ. After the reaction is integrated, the unreacted bromine was reacted with a steady amount of methylene blue, and the absorbance was measured at 665 nm (method A) or, cresol red could be used for the reaction and the absorbance moderated at 517 nm (method B). Beer’s law was submitted from 0.45 to 15.00 μg/mL CBZ with a molar absorptivity of 4.93 × 103 L/mol.cm for method A and from 0.50 to 12.00 μg/mL CBZ with a molar absorptivity of 1.37 × 104 L/mol.cm for method B. The proposed methods were effective for the determination of CBZ in tablets with great precision and accuracy.

Evaluation of the efficacy of carbamazepine and gabapentin in the management of trigeminal neuralgia: A clinical study

Background: Trigeminal neuralgia (TN) is a syndrome of unilateral, paroxysmal, stabbing facial pain, originating from the trigeminal nerve. Carbamazepine still remains as the gold standard drug in terms of efficacy in TN. Over the time, several other drugs are also used as alternatives for TN such as oxcarbazepine, baclofen, lamotrigine, levetiracetam, gabapentin, valproate, botulinum toxin A injection. Objective: To Evaluate the efficacy of Carbamazepine and Gabapentin in the management of Trigeminal Neuralgia. Materials and Methods: A total of 42 patients with a mean age of 52.78 years included in the study were randomly divided into two groups A and B and were given the tablets of carbamazepine in the dose range of 400mg to 1200 mg and gabapentin in the dose range of 600mg to 1800mg and recalled after 3rd day, 15th day, 1 month and 3 month period to evaluate the response to the drugs. The collected data was subjected to statistical analysis. Results: The therapeutic effectiveness of carbamazepine recorded as good response in 52.38% of patients of group A after 72 hours of recall while 28.57% patients had an average response and 19% patients had not relieved off pain attacks at the dose of 400mg of carbamazepine. The therapeutic effectiveness of gabapentin recorded as good response in 52.38% of group B patients after 72 hours of recall while 42.8% patients had an average response at the dose of 600mg of gabapentin. Conclusion: The study suggests that gabapentin can be effective as first or second line treatment of trigeminal neuralgia, even in cases resistant to traditional treatment modalities.

IN VITRO RELEASE STUDIES OF CARBAMAZEPINE TABLETS AND BENZOYL METRONIDAZOLE SUSPENSIONS USING THE FLOW-THROUGH CELL APPARATUS AND SIMULATED GASTROINTESTINAL FLUIDS

Objective: To characterize the in vitro release of carbamazepine tablets and benzoyl metronidazole suspensions using the flow-through cell apparatus and simulated gastrointestinal fluids.Methods: Tegretol® tablets, Flagyl® suspension, and generic formulations of each were tested. Release studies were performed using an automated flow-through cell apparatus. Simulated gastric fluid (with and without pepsin) and simulated intestinal fluid (without pancreatin) at 16 ml/min and fasted state simulated intestinal fluid at 8 ml/min, all at 37.0±0.5 °C, were used as dissolution media. The quantity of dissolved carbamazepine and benzoyl metronidazole was determined at 5-min intervals until 60 min at 285 and 278 nm, respectively. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values, and t10%, t25%, t50% and t63.2% were calculated. Mean values for all parameters were compared between the reference and generic formulations using Studentʼs t-test. Dissolution data were fitted to different kinetic models.Results: Simulated gastric fluid without pepsin showed no discriminative capability for carbamazepine tablets. Significant differences were observed between the reference and generic formulations for almost all parameters (*P&lt;0.05). In some cases, the logistic model best described the in vitro release of both drugs.Conclusion: Using an apparatus and media that best simulates the gastrointestinal environment, we identified differences in the rate and extent of dissolution of both drugs that could help to optimise the design of interchangeable formulations. Based on the physicochemical characteristics of carbamazepine and benzoyl metronidazole and the conditions in which the formulations were tested, these differences could be of clinical relevance.

ВИБІР ДОПОМІЖНИХ РЕЧОВИН З МЕТОЮ ОТРИМАННЯ ТАБЛЕТОК НА ОСНОВІ КАРБАМАЗЕПІНУ З ТІОТРИАЗОЛІНОМ МЕТОДОМ ВОЛОГОЇ ГРАНУЛЯЦІЇ

Мета роботи. Обгрунтувати доцільність створення комбінованого лікарського засобу на основі карбамазепіну з тіотриазоліном. Вивчити вплив ДР на процес пресування, якість поверхні та однорідність маси таблеток на основі карбамазепіну з тіотриазоліном, які отримували методом вологої грануляції.Матеріали і методи. Діючі речовини - карбамазепін з тіотриазоліном (1,5:1), допоміжні речовини (наповнювачі, розпушувачі, зв’язуючі, змазуючі). Таблетки пресували методом вологої грануляції. Вплив ДР речовин на таблетки карбамазепіну з тіотриазоліном вивчали за такими показниками: процес пресування, зовнішній вигляд поверхні таблеток після виготовлення, однорідність дозування маси таблеток.Результати й обговорення. За результатами дисперсійного аналізу експериментальних даних було встановлено, що на процес пресування, зовнішній вигляд поверхні таблеток після виготовлення та однорідність дозування маси таблеток карбамазепіну з тіотриазоліном впливає природа наповнювача, розпушувача, зв’язуючих та змазуючих ДР Так, на процес пресування таблеток серед наповнювачів найкращий вплив має МКЦ 101, серед розпушувачів лідером є крохмаль преджелатанізований.На якість поверхні таблеток карбамазепіну з тіотриазоліном після виготовлення серед розпушувачів найбільший позитивний вплив має крохмаль картопляний. На однорідність дозування маси таблеток серед змазуючих речовин лідером є кислота стеаринова, серед розпушувачів перевага на боці крохмалю преджелатанізованого, серед наповнювачів лідером є МКЦ 101, серед зв’язуючих найбільший вплив має 2 % розчин ГПМЦ.Висновки. Вивчено вплив чотирьох груп допоміжних речовин на процес пресування, зовнішній вигляд та однорідність дозування таблеток карбамазепіну з тіотриазоліном. Більшість із вивчених 16-ти ДР придатна для отримання таблеток карбамазепіну з тіотриазоліном методом вологої грануляції. За дослідженими показниками (процес пресування, якість поверхні таблеток, однорідність дозування) побудовані діаграми переваг рівнів вивчених факторів.