Paracetamol Drugs Research Articles

Acute Renal Failure Secondary to Paracetamol Intoxication: A Case Report

Renal damage secondary to paracetamol intoxication is rare, estimated between 1% and 2% of intoxication cases. Its pathophysiology is still debated, the clinical involvement consisting in an acute tubular necrosis with a good prognosis if it is rapidly treated. Renal damage can sometimes occur without prior hepatic damage, and the onset of renal manifestations is generally between the 2nd and 7th day after taking paracetamol. If its management remains exclusively symptomatic, its late onset can sometimes lead to serious metabolic complications. It is therefore important to systematically monitor renal function following paracetamol drug intoxication. We report the case of a 60-year-old male subject hospitalized for the management of voluntary drug intoxication (VDI) with paracetamol complicated by acute hepatocellular failure and acute renal failure. His management required extrarenal purification (hemodialysis) and the evolution was favorable with recovery ad integrumof renal function. Conclusion: Although less known and of unelucidated physiopathology, nephrotoxicity secondary to voluntary drug intoxication with paracetamol is a reality and can lead in extreme cases to the use of extrarenal purification technique (hemodialysis).

Assessment of Psychology, Behaviour and Self-Medication Potential Among Indian People During CovID-19 Pandemic

Aim: This research work was done during the Indian festive season of 2020 to assess the attitude, mentality and psychological pattern of Indians. Also, the effect of yoga and meditation in combating the Covid-19 pandemic related stress was analyzed in the present research work. As Paracetamol and Diclofenac are OTC medications which are widely available without doctor’s prescription, the potential of self-medication for these drugs amidst the pandemic need to be studied, this study further attempted to analyze the rate and extent of self-medication of these drugs among Indians. Materials and Methods: An e-questionnaire survey bearing questions on pandemic-related mental stress, sleep duration, yoga, meditation practice, and extent of self-medication in combating the pandemic was floated to the residents of Bengaluru to collect their response. The collected data were analyzed using Statistical Package for the Social Sciences software version 17. Results: A mixed response regarding their stress, anxiety, and fear expressed on a higher scale was the same before or during Covid could be perceived. The sleep pattern before and during CoVid had no significant variation (p>0.05) and appeared the same. All the respondents agreed that they spend considerable time with electronic gadgets during the Covid lockdown period. Most of the respondents (60%) practice yoga and meditation occasionally or daily. The high rate of self-medication with Paracetamol and Diclofenac drugs among Indian people in the current pandemic situation shows they are OTC and readily available. The self-medication practice is of real concern as it may cause a long-term impact on the consumers.

Effect of pediatric drugs on solubility of restorative materials used in primary teeth

Background: Pleasant tasting syrups have a long history of use in pediatric practice to aid compliance with medication. Pharmaceutical firms sweeten liquid drug preparations with sucrose to increase the palatability which causes dental caries and erosion in children. In pediatric population, the commonly used esthetic restorative materials are glass ionomers, compomers or composites. Hence solubility of dental restorative materials are of considerable clinical importance and cannot be overlooked. Aims and objectives of current study were to evaluate the effect of commonly used pediatric drugs on the surface solubility of pediatric restorative materials.Methods: The study was conducted on 40 disc shaped specimens of GIC and composite immersed in artificial saliva and pediatric drugs, at 370C for 7 days to determine the solubility in pediatric drug formulations. The solubility of the specimens was calculated by a given formula by comparing the initial and final masses of the specimens.Results: In both GIC and Composite groups higher solubility was seen with paracetamol drug formulations. The mean solubility value of GIC was 0.14±0.02 and that of composite was 0.07±0.035, in paracetamol drug formulations.Conclusions: From the above experimental study it can be concluded that the solubility of restorative materials were comparatively higher in pediatric liquid medications with low pH. Among the drugs paracetamol showed increased erosive effects leading to solubility.

Fasted intestinal solubility limits and distributions applied to the biopharmaceutics and developability classification systems

After oral administration, a drug’s solubility in intestinal fluid is an important parameter influencing bioavailability and if the value is known it can be applied to estimate multiple biopharmaceutical parameters including the solubility limited absorbable dose. Current in vitro measurements may utilise fasted human intestinal fluid (HIF) or simulated intestinal fluid (SIF) to provide an intestinal solubility value. This single point value is limited since its position in relation to the fasted intestinal solubility envelope is unknown. In this study we have applied a nine point fasted equilibrium solubility determination in SIF, based on a multi-dimensional analysis of fasted human intestinal fluid composition, to seven drugs that were previously utilised to investigate the developability classification system (ibuprofen, mefenamic acid, furosemide, dipyridamole, griseofulvin, paracetamol and acyclovir). The resulting fasted equilibrium solubility envelope encompasses literature solubility values in both HIF and SIF indicating that it measures the same solubility space as current approaches with solubility behaviour consistent with previous SIF design of experiment studies. In addition, it identifies that three drugs (griseofulvin, paracetamol and acyclovir) have a very narrow solubility range, a feature that single point solubility approaches would miss. The measured mid-point solubility value is statistically equivalent to the value determined with the original fasted simulated intestinal fluid recipe, further indicating similarity and that existing literature results could be utilised as a direct comparison. Since the multi-dimensional approach covered greater than ninety percent of the variability in fasted intestinal fluid composition, the measured maximum and minimum equilibrium solubility values should represent the extremes of fasted intestinal solubility and provide a range. The seven drugs all display different solubility ranges and behaviours, a result also consistent with previous studies. The dose/solubility ratio for each measurement point can be plotted using the developability classification system to highlight individual drug behaviours. The lowest solubility represents a worst-case scenario which may be useful in risk-based quality by design biopharmaceutical calculations than the mid-point value. The method also permits a dose/solubility ratio frequency distribution determination for the solubility envelope which permits further risk-based refinement, especially where the drug crosses a classification boundary. This novel approach therefore provides greater in vitro detail with respect to possible biopharmaceutical performance in vivo and an improved ability to apply risk-based analysis to biopharmaceutical performance. Further studies will be required to expand the number of drugs measured and link the in vitro measurements to in vivo results.

Design of chitosan based acrylic polymer as a carrier for water soluble drug

Study of drug release from polymeric systems has a significant role in drug formulation and in pharmaceutical dosage determination. Chitosan based membranes have been developed by grafting polymerization of vinyl monomers including acrylic acid (AA) and 2-hydroxyethylmethacrylate (HEMA) onto chitosan using potassium persulphate (K2S2O8), and sodium bisulphite (NaHSO3) as redox chemical initiation system. The grafting polymerization of vinyl monomers onto chitosan was confirmed by Fourier Transform-Infrared Spectroscopy (FTIR) and Scanning Electron Microscope (SEM). Release profile of Paracetamol drug from chitosan grafted vinyl polymers were investigated using gastric and intestinal medium (pH 1.2 and 7.4 respectively) followed by studying the kinetic data for Paracetamol drug release using Koresmeyer – peppas, Higuchi, Zero order and First order equations where the data confirmed that the drug diffusion from chitosan was related to Higuchi model and reached to 90 % drug release at pH value 7.4 for a sample containing high amount of acrylic acid.

Bio-fabrication of multifunctional nano-ceria mediated from Pouteria campechiana for biomedical and sensing applications

The present study focuses on the synthesis of size-controlled nano-ceria (CePC NPs) from aqueous extract of Pouteria campechiana via self-propagating solution combustion synthesis. The extract volume is varied to know the influence of extract on the physical, optical and surface properties of CePC NPs. The p-XRD study revealed the size-controlled synthesis of CePC NPs from 11.46 to 15.59 nm. The nano-regime size is having a definite effect on the biomedical and sensing applications of the NPs. The specific surface area of 34.04 m2g−1, with a maximum pore diameter of 24.33 nm was observed for CePC NPs with a size 11.46 nm. The antioxidant behaviour was maximum with 71.73% of DPPH inhibition at concentration 500 μg/mL. In vitro A546 cancer suppressive activity of CePC NPs reveals that phytochemicals functionalized by highest volume during synthesis showed a low IC50 value of 118.92 μg/mL despite the large size. The bio-derived NPs shows RBC membrane protection above ∼93%, owing to its non-toxic behaviour. The CePC NPs exhibits suitable antibacterial applications against Bacillus subtilis, Staphylococcus aureus, Pseudomonas syringae and Pseudomonas aeruginosa. The bio-fabricated samples exhibited the best hydrogen diffusion value of 1.035 × 10−5. The Rct values of the CePC NPs are comparable with each other (∼73.03–90.39 Ω) with high capacitance, and hence the bio electrodes have superlative efficiency in sensing the Paracetamol drug.

Computational studies of the encapsulation of ibuprofen and paracetamol into cucurbit[7]uril

Herein, theoretical methods were used to study the cucurbit[7]uril (CB[7]) as a possible carrier agent for the poor water soluble drugs ibuprofen (IBF) and paracetamol (PCT). These drugs form a stable inclusion complex with the CB[7] during 50 ns of molecular dynamics simulation preserving its solvation shell. Likewise CB[7], both complexes are soluble in water with calculated solvation enthalpy of –131 and –133 kcal/mol for isolated CB[7]. The binding free energy, obtained from the potential of mean force calculations, reveals that the IBF@CB[7] complex is more stable (–16.7 kcal/mol) than the PCT@CB[7] complex (–11.7 kcal/mol). Correspondingly, the binding energies obtained in DFT-D3/B3LY/6-31G(d,p) calculation are –30.07 and –24.51 kcal/mol for IBF@CB[7] and PCT@CB[7], respectively. The high energy gap of complexes implies their chemical stability. Our results indicate that the CB[7] can be a new carrier agent for IBF and PCT, improving their solubility and chemoprotection in aqueous media.

Пирексия и антипиретическая терапия у больных при критических состояниях

Повышение температуры ядра тела является одним из наиболее часто встречающихся аномальных признаков у пациентов, поступивших в ОИТ, и это связано с увеличением смертности среди некоторых групп пациентов с тяжелыми заболеваниями. Повышенная температура тела обнаруживается примерно у 50 % взрослых пациентов, поступивших в отделение интенсивной терапии (ОИТ). Повышенная температура тела классифицируется как пирексия или гипертермия. Пирексия (также ее называют лихорадкой) рассматривается как адаптивный ответ на физиологический стресс, который регулируется через эндогенные пирогенные и антипиретические пути и связан с увеличением гипоталамического заданного значения. Гипертермические синдромы включают: гипертермию окружающей среды, в том числе тепловой удар; гипертермию, вызванную лекарственными средствами; нейролептический злокачественный синдром; синдром серотонина и эндокринные причины, включая тиреотоксикоз, феохромоцитому и надпочечниковый криз. Многие эпизоды пирексии вызваны инфекциями. Наиболее распространенными источниками инфекции являются нижние дыхательные пути, внутрибрюшные инфекции, инфекции мочевых путей и другие, которые включают инфекцию кожи и мягких тканей, костей или суставов, центральной нервной системы, этмоидных и верхнечелюстных пазух. Пирексия из-за неинфекционной этиологии также является распространенной причиной лихорадки у пациентов в ОИТ. Для борьбы с пирексией могут использоваться антипиретики, главным образом парацетамол и нестероидные противовоспалительные препараты, а также физические методы охлаждения. Лечение с помощью жаропонижающих препаратов распространено в ОИТ. Было показано, что исследования жаропонижающей терапии, которые включали как септических, так и несептических пациентов, не обнаружили значительного улучшения 28-дневной госпитальной летальности у взрослых критических пациентов с сепсисом или без него. Дополнительные исследования улучшат понимание патофизиологии пирексии и будут способствовать развитию данного направления.

مروری بر داروهای مورد استفاده در درمان درد رنال کولیک در مقالات چاپ شده به زبان فارسی؛ یک مطالعه مروری روایتی

Introduction: Renal colic is the most common clinical manifestation of urinary stones and one of the most common urological emergencies that is very agonizing for the patient due to excruciating pain. Different therapeutic interventions are performed for relieving the pain in patients with renal colic. This narrative review study was performed, aiming to evaluate the medications used for pain management in patients with renal colic. Methods: The present study is a narrative review. In this study, to find related articles, researchers conducted a computer search in SID, Magiran, and Google Scholar databases using Persian keywords meaning renal colic and kidney colic. Studies were searched in Persian language databases without any time limit. Results: In reviewing the articles, various studies were performed on different drugs for controlling pain in patients with renal colic. Most of the studied drugs were opioids (morphine, buprenorphine, tramadol, and pethidine) and non-steroidal anti-inflammatory drugs (NSAIDs) (paracetamol, diclofenac, and ketorolac). Additionally, drugs such as ketamine, desmopressin, aminophylline, and intradermal administration of distilled water were also evaluated. Conclusion: Although narcotics are most effect for relieving pain in patients with renal colic, but the development of side effects such as inhibition of the respiratory center in the medulla and activation of the vomiting center (chemoreceptor trigger zone; CTZ) has limited the use of narcotics. Due to having analgesic effects similar to opioids and fewer side effects, it is recommended to use NSAIDs (Ketorolac) as the first line of treatment for renal colic patients.

Systematic study of paracetamol powder mixtures and granules tabletability: Key role of rheological properties and dynamic image analysis

The aim of this systematic study was to analyze the granulometric and rheological behavior of tableting mixtures in relation to tabletability by single tablet and lab-scale batch compression with an eccentric tablet machine. Three mixtures containing 33, 50, and 66% of the cohesive drug paracetamol were prepared. The high compressibility of the powder mixtures caused problems with overcompaction or lamination in the single tablet compression method; due to jamming of the material during the filling of the die, the lab-scale batch compression was impossible. Using high shear granulation, the flow properties and tabletability were adjusted. A linear relationship between the span of granules and the specific energy measured by FT4 powder rheometer was detected. In parallel, a linear relationship between conditioned bulk density and the tensile strength of the tablets at lab-scale batch tableting was noted. The combination of dynamic image analysis and powder rheometry was useful for predicting the tabletability of pharmaceutical mixtures during the single tablet (design) compression and the lab-scale batch compression.

Microfluidic Electrochemistry Meets Trapped Ion Mobility Spectrometry and High-Resolution Mass Spectrometry-In Situ Generation, Separation, and Detection of Isomeric Conjugates of Paracetamol and Ethoxyquin.

Over the last 3 decades, electrochemistry (EC) has been successfully applied in phase I and phase II metabolism simulation studies. The electrochemically generated phase I metabolite-like oxidation products can react with selected reagents to form phase II conjugates. During conjugate formation, the generation of isomeric compounds is possible. Such isomeric conjugates are often separated by high-performance liquid chromatography (HPLC). Here, we demonstrate a powerful approach that combines EC with ion mobility spectrometry to separate possible isomeric conjugates. In detail, we present the hyphenation of a microfluidic electrochemical chip with an integrated mixer coupled online to trapped ion mobility spectrometry (TIMS) and time-of-flight high-resolution mass spectrometry (ToF-HRMS), briefly chipEC-TIMS-ToF-HRMS. This novel method achieves results in several minutes, which is much faster than traditional separation approaches like HPLC, and was applied to the drug paracetamol and the controversial feed preservative ethoxyquin. The analytes were oxidized in situ in the electrochemical microfluidic chip under formation of reactive intermediates and mixed with different thiol-containing reagents to form conjugates. These were analyzed by TIMS-ToF-HRMS to identify possible isomers. It was observed that the oxidation products of both paracetamol and ethoxyquin form two isomeric conjugates, which are characterized by different ion mobilities, with each reagent. Therefore, using this hyphenated technique, it is possible to not only form reactive oxidation products and their conjugates in situ but also separate and detect these isomeric conjugates within only a few minutes.

Toxic effects of a mixture of five pharmaceutical drugs assessed using Fontinalis antipyretica Hedw.

The potential health risks associated with the pharmaceuticals released into the environment through effluents from sewage treatment plants have become a major cause for concern. Owing to the lack of effective indicators, monitoring the concentration of these pollutants in the aquatic environment is challenging. The aim of this study was to assess the toxicity of a mixture of five pharmaceutical drugs (paracetamol, carbamazepine, diclofenac, irbesartan, and naproxen) using the aquatic moss Fontinalis antipyretica as a bioindicator and bioaccumulator. We examined the effects of the drug mixture on the cellular antioxidant system, chlorophyll content, and morphological traits of F. antipyretica. The plant was exposed for 5 months to three concentrations of the mixture, including the environmental concentration (MX1), and 10- (MX10) and 100-times (MX100) the environmental concentration. The results showed that only carbamazepine and irbesartan were accumulated by the species. The bioconcentration level increased with exposure time, with the maximum uptake at the 4th month of exposure. The increase in bioaccumulation with exposure time was more evident in plants exposed to MX100. Analysis of the activity of antioxidant enzymes showed that superoxide dismutase (SOD, EC 1.15.1.1.) and catalase (EC 1.11.1.6.) were highly sensitive to the drug mixture. The activity of the enzymes was significantly higher in plants exposed to MX100; however, the activity of guaiacol peroxidase (GPX, EC 1.11.1.7.) was not significantly affected. Plants exposed to MX10 and MX100 had significantly lower total chlorophyll content and chlorophyll a/b ratio compared with those of plants in the control group; however, photosynthetic activity was restored after 5 months of exposure. The morphological characteristics of F. antipyretica were less sensitive to the treatment conditions.

Comparison of Efficacy of Oral Ibuprofen versus Paracetamol for PDA Closure in Preterm Neonates

Objective: The aim of this study is to compare the efficacy of oral ibuprofen versus paracetamol for PDA closure in preterm neonates. Study Design: Randomized Control trial Place and Duration: The study was conducted at Neonatology department North West General Hospital, Peshawar for duration of three years from April 2018 to March 2021. Methods: Total one hundred and fifty preterm neonates were included in this study. Patients’ detailed demographics including gestational age, gender; birth and diameter were recorded after taking informed written consent from the parents. Patients were equally divided into two groups, I and II. Group I had 75 patients and received paracetamol for closure for patent ductus arteriosus and group II received oral ibuprofen for closure of PDA. Outcomes among both groups were calculated in terms of effectiveness, mortality and post-operative complications. Data was analyzed by SPSS 22.0 version. Results: Mean gestational age of the patients in group I was 29.12±7.44 weeks and in group II mean gestational age was 30.09±4.66 weeks. 45 (65%) male in group I and in group II 40 (53.3%) were male babies. Mean ductal diameter in group I was 3.02±1.13 and in group II mean diameter was 2.98±0.16 mm. In group I cesarean birth was found in 50 (66.7%) and in group II 48 (64%) cesarean birth was found. Mean duration of closure was lower in group I 4.24±1.03 days as compared to group II 5.01±0.03 days. PDA closure rate was higher in group I 62 (82.7%) and in group II its frequency was 58 (77.3%). Re-opening of ductus was found in 6 (8%) in group I and 8 (10.7%) in group II. Adverse outcomes were renal failure, hyperbilirubinemia and gastrointestinal bleeding among both groups. Mortality rate in ibuprofen group was higher 7 (9.3%) as compared to group I 4 (5.3%). Conclusion: We concluded in this study that the use of drug paracetamol is effective for the closure of PDA in preterm neonates as compared to oral ibuprofen with less adverse outcomes and mortality rate. Keywords: PDA, Neonates, Paracetamol, Ibuprofen, Complications, Mortality

Evaluation of two novel co-processed excipients for direct compression of orodispersible tablets and mini-tablets

Pediatric, geriatric, and other patients who suffer from swallowing difficulties represent a special patient group, where an increased need in appropriate formulation development is required. To overcome these mostly swallowability linked issues, orodispersible tablets (ODTs) and orodispersible mini-tablets (ODMTs) can be seen as a suitable alternative to improve compliance. Orodispersible tablets are oral solid dosage forms which rapidly disintegrate after contact with saliva, leaving a liquid dispersion, which can be easily swallowed. To fulfil the required quality criteria and optimize the formulations regarding tensile strength and disintegration time, co-processed excipients (CPE) based on mannitol are frequently used in the manufacturing of orodispersible tablets. This study aimed to systematically compare two new CPEs, namely Granfiller-D® and Hisorad® and evaluate their potential in future OD(M)T formulations with already marketed products. The performance of the CPEs was examined in combination with three different APIs. Disintegration time, sufficient mechanical strength and content uniformity for low dosed formulation were chosen as main quality aspects. Conventionally sized tablets (9 mm) with 50% drug load of ibuprofen and paracetamol were produced with each CPE. Low dosed OD(M)Ts with a drug load of 4% enalapril maleate were manufactured to study content uniformity. Large differences were visible in the formulations containing ibuprofen and only Hisorad® allowed to compress ODT fulfilling the specifications of Ph.Eur. and FDA regarding disintegration times (180 s and 30 s, respectively). For the poorly binding model drug paracetamol, none of the studied excipients showed a satisfactory performance, with maximum tensile strengths < 1 MPa. To reach content uniformity in low dosed ODMTs, Ludiflash® seems to be the most preferable alternative, as the formulation showed the lowest acceptance values (AV) according to Ph.Eur. (<4) as well as the smallest coefficient of variation (CV) in API content (CV < 2%). In conclusion, the study revealed that none CPE is the ideal choice for all approaches, but different CPEs should be selected dependent on different challenges during formulation development of OD(M)Ts.

Bio-fabrication of multifunctional quasi-spherical green α-Fe2O3 nanostructures for paracetamol sensing and biomedical applications

Green metal oxide nanostructures with various diverse properties are synthesized to find solutions to various problems arising in the field of medicine and technology. The present study includes cost-effective, eco-friendly synthesis of α-Fe2O3 nanoparticles (ISD NPs), using varied volumes of extract of Scoparia dulsis as a reducing agent via Solution combustion synthesis. The extract influences the size, shape of quasi-spherical, bandgap positions, surface area to volume ratio of the nanoparticles prepared. The structural purity is ascertained via p-XRD studies, with nano regime size in the range of 27–37 nm. The optical energy gap (1.90–2.23 eV) and the mesoporous nature of the biogenic NPs have attributed by UV-DRS and surface area studies. The characterization findings reveal the “symbiotic association” of bio reducing agents and metal to influence the pronounced activity in biomedical and electrochemical studies. The controlled size and morphology give explicit results in in-vitro assays performed. The free radical scavenging hunt was maximum with DPPH inhibition of 71.88% and also exhibited depreciated cell viability of adenocarcinoma human alveolar basal epithelial cells to 39.88% with a lower IC50 value. The inherent stabilization behavior of ISD NPs towards human RBC's is appreciated (71.43%) owing to its bio-compatibility nature. The antidiabetic property via pancreatic α-amylase inhibition was in the range of 60–82%. The distinct electrochemical activities of the ISD NPs showed a higher proton diffusion coefficient (D) with 8.21 × 10−6 cm2s−1, low charge resistance (85.27 Ω) and increased capacitance (5.3 × 10−4 F). The electrochemical studies indicate that the ISD NPs as bio electrodes are a promising sensor for paracetamol drug detection.

In Vitro and in Vivo Evaluation Of Pharmacological Activites of Pouzolzia Sanguinea

Pouzolzia sanguinea grows in tropical and sub-tropical regions of Bangladesh, used for a variety of purposes including pain, rheumatoid kidney diseases in traditional medicine. The crude ethanolic leaf extract of P. sanguinea with its different fractions (ethanol, n-hexane, and chloroform) was investigated for phytochemical constituents, in vitro antioxidant, anti-inflammatory effects, in-vivo analgesic and antipyretic activities. Preliminary phytochemical constituents were identified by chemical group test. P. sanguinea fractionated extracts contain alkaloids, glycosides, tannins, flavonoids, saponins, gums, and amides. Antioxidant activity test was performed by both qualitative (TLC and Rf value) and quantitative tests (inhibition of DPPH free radical scavenging). Extracts exhibited significant (p &lt;0.001, p &lt;0.0001) inhibition of DPPH free radical scavenging activity as compared to the standard drug ascorbic acid at similar doses. In vitro anti-inflammatory activity was determined by protein denaturation of egg albumin method. The percent inhibition of protein denaturation in the experiment of ethanol extract was found significantly higher (p &lt;0.0001) compared with chloroform and n-hexane extracts. In addition, in vivo analgesic and antipyretic effects were determined in mice by acetic acid-induced writhing and yeast-induced pyrexia methods. The ethanol extracts of P. sanguinea exhibited inhibition of writhing reflex on mice by 71.58% at the dose of 500 mg/kg body weight which had greater analgesic activity than other n-hexane and chloroform extracts. In the anti-pyretic test, fractional extracts ethanol, chloroform, and n-hexane at a dose of 500 mg/kg body weight significantly (p &lt;0.05) decreased pyrexia in mice up to 3 h as compared with the positive control paracetamol drug at a dose of 150 mg/kg body weight. In our in vitro and in vivo study models, it is evident that Pouzolzia sanguinea fractionated extracts showed significant antioxidant, anti-inflammatory, analgesic, and antipyretic activities. J. Bio-Sci. 29(2): 31-42, 2021 (December)

Paracetamol/ naproxen co-crystals; a simple way for improvement of flowability, tableting and dissolution properties

Background: The poor solubility of drugs is one of the most important limitations in formulating drugs into suitable dosage forms. In addition, the mechanical properties are the main obstacles in formulating tablet dosage form by direct compression method. This study aims to investigate the possible improvement in mechanical properties, solubility performance, and tableting properties of drug-drug co-crystals of paracetamol and naproxen. Material and Methods: The three paracetamol/naproxen co-crystals investigated the pre-compression parameters (Angle of repose, Carr’s index, and Hausner’s ratio) of the three paracetamol/naproxen co-crystals were investigated. Moreover, the solubility of the co-crystals was tested as well. In addition, the three paracetamol/naproxen co-crystals were formulated as oral tablets by direct compression method using microcrystalline cellulose and magnesium stearate. The prepared co-crystals were compressed into tablet dosage forms and the dissolution profiles were monitored. Results: The results showed an enhancement in flowability and compressibility of the prepared co-crystals when compared with paracetamol or naproxen alone. The poor tableting properties of prepared paracetamol tablets were very clear and it is in opposite to the co-crystals prepared tablets, which met all the pharmacopeial requirements. The in vitro dissolution study was conducted to compare the dissolution profiles of the prepared co-crystals tablets with marketed paracetamol tablets (Piodol®) and marketed naproxen tablets (Napron®). The dissolution profile of (1 to 2) co-crystal prepared tablets showed a superior dissolution rate with more than 50 % of the paracetamol drug dissolved within the first 5 minutes of dissolution rate. The dissolution study resulted in a better dissolution of the prepared paracetamol/naproxen tablets due to the co-crystal formation. Conclusion: It could be concluded that the prepared paracetamol/naproxen co-crystals represent a promising way for improving flowability and compression properties, enabling the formulation of the co-crystals as oral tablets by direct compression method with a clear enhancement in the dissolution rate.

Impact of Selenium on Structural Changes Induced by Hypothyroidism In Adult Male Rat ׳s Testis

Background: The poor solubility of drugs is one of the most important limitations in formulating drugs into suitable dosage forms. In addition, the mechanical properties are the main obstacles in formulating tablet dosage form by direct compression method. Aim of this research: To investigate the possible improvement in mechanical properties, solubility performance, and tableting properties of drug-drug co-crystals of paracetamol and naproxen. Methods: The pre-compression parameters (Angle of repose, Carr’s index, and Hausner’s ratio) of the three paracetamol/naproxen co-crystals were investigated. Moreover, the solubility of the co-crystals was tested as well. In addition, the three paracetamol/naproxen co-crystals were formulated as oral tablets by direct compression method using microcrystalline cellulose and magnesium stearate. The prepared co-crystals were compressed into tablet dosage forms and the dissolution profiles were monitored. Results: The results showed an enhancement in flowability and compressibility of the prepared co-crystals when compared with paracetamol or naproxen alone. The poor tableting properties of prepared paracetamol tablets were very clear and they are in opposite to the co-crystals prepared tablets, which met all the pharmacopeial requirements. The in vitro dissolution study was conducted to compare the dissolution profiles of the prepared co-crystals tablets with marketed paracetamol tablets (Piodol®) and marketed naproxen tablets (Napron®). The dissolution profile of (1 to 2) co-crystal prepared tablets showed a superior dissolution rate with more than 50 % of the paracetamol drug dissolved within the first 5 minutes of dissolution rate. The dissolution study resulted in a better dissolution of the prepared paracetamol/naproxen tablets due to the co-crystal formation. Conclusion: It could be concluded that the prepared paracetamol/naproxen co-crystals represent a promising way for improving flowability and compression properties, enabling the formulation of the co-crystals as oral tablets by direct compression method with a clear enhancement in the dissolution rate.

Acute Liver Failure: Indian Perspective.

Acute Liver Failure: Indian Perspective.

Gambaran Pengobatan Pasien Suspek Covid-19 Rawat Inap RS Brayat Minulya Surakarta Periode Maret - Oktober 2020

Treatment therapy for suspected COVID-19 is an important factor in the recovery of patients with suspected COVID-19. This study aims to determine the characteristics and description of the treatment of patients with suspected COVID-19. This research is a non-experimental research which was conducted retrospectively and analyzed descriptively. The sampling technique was saturated sampling on 55 patients with suspected COVID-19 in inpatient isolation at Brayat Minulya Hospital for the period March-October 2020. The results showed that most of the patients with suspected COVID-19 more dominated by female patients as many as 31 patients (56.36%), in the age group&gt; 65 years as many as 15 patients (27.27%), with the most frequent diagnosis of moderate symptoms as many as 43 patients (78%), with comorbidities dyspepsia. as many as 5 patients (11.90%). Treatment features mostly used the 10.22% Levofloxacin antibiotic group, 6.98% vitamin C group, 1% Oseltamivir antiviral group, 2.74% multivitamin Neurobion, 0.50% zinc supplement, and the symptomatic drug Paracetamol 8.47. %, Omeprasole 6.48%, Ondancentron 4.98%, Ambroxol 4.98%, Methylprednisolone 1.50%, Trifed and Rhinos SR 0.25%, Combivent respule 0.50%, Enoxaparin 1%, Colcichin 0.25 %, Ketorolac 0.25%, comorbid drugs such as Novorapid 1.99%, Amlodipine 1.50%, Isosorbid dinitrate 0.75%, Renxamin 0.50%, Aminoral 0.50%, Haessteril 0.25%, and citicholin 0.25%.