Search Results (12)

Chlorpheniramine maleate (CPM) is a first-generation antihistamine that is frequently used to treat allergic reactions. However, excessive consumption presents potential health risks. Therefore, it is crucial to develop a quick and precise technique for identifying CPM levels. In this study, nickel cobalt phosphide (NiCoP), a binary metal phosphide, was successfully incorporated into carbon nanofibers. This involved creating a pore structure by adding polyvinylpyrrolidone (PVP) as a pore-forming template to a polyacrylonitrile (PAN) substrate via electrostatic spinning. An innovative electrochemiluminescent sensor for CPM detection was constructed using NiCoP/PVP/PAN carbon nanofibers (NiCoP/PVP/PAN/CNFs). Under optimal conditions, the electrochemical behavior of CPM was studied using NiCoP/PVP/PAN/CNF-modified working electrodes. These findings demonstrate that the three-dimensional porous network architecture of NiCoP/PVP/PAN/CNFs enhances the conductive properties of the material. Consequently, an electrochemical optical sensor fabricated using this structure exhibited remarkable performance. The linear detection range of the sensor was 1 × 10⁻⁸–7 × 10⁻⁵ mol/L, and the detection limit was 7.8 × 10⁻¹⁰ mol/L. When human urine and serum samples were examined, the sensor was found to have a high recovery rate (94.35–103.36%), which is promising for practical applications. Full article

This work presents an innovative application of the sugar templating method to fabricate highly porous floating tablets based on cellulose derivatives for gastroretentive drug delivery systems (GRDDS). Ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC) were utilized to develop formulations that optimize porosity, buoyancy, and drug release. Among the tested formulations, E₁₀H₅/CPM, consisting of 10% w/w EC and 5% w/w HPMC loaded with chlorpheniramine maleate (CPM), exhibited the most favorable properties, including high porosity (94.4%), uniform pore distribution, immediate buoyancy, and over 24 h of floating time. E₁₀H₅/CPM tablets demonstrated superior drug release performance compared to an EC-only formulation (E₁₀/CPM), attributed to the presence of HPMC, which facilitated improved hydration and diffusion. The in vitro release study showed that E₁₀H₅/CPM achieved a cumulative release of 79.01% over 72 h, following a Fickian diffusion mechanism. However, a limitation was noted in drug loading, with E₁₀H₅/CPM incorporating 6.40 mg of CPM, compared to 8.72 mg in E₁₀/CPM. Future work should focus on enhancing drug load and further optimizing polymer composition to improve the release profile. Overall, this study underscores the potential of sugar templating in developing cost-effective, scalable floating tablet formulations for improved gastric retention and localized drug delivery. Full article

Chlorphenamine maleate is a prohibited additive found in herbal teas and health foods. Excessive intake of this substance can result in adverse health effects. In this study, two novel haptens, PEM and bepotastine (PB1), mimicking chlorphenamine maleate structure were designed and synthesized based on molecular simulation for developing two corresponding polyclonal antibodies (PEM-Ab and PB1-Ab), respectively. Afterward, an indirect competitive enzyme-linked immunosorbent assay (ic-ELISA) was developed to quickly and accurately detect chlorphenamine maleate in herbal teas using PB1-Ab, which has a high sensitivity and specificity. For chlorphenamine maleate, the half-maximal inhibitory concentration (IC₅₀) and limit of detection (LOD) of PB1-Ab under ideal circumstances were found to be 1.18 µg/L and 0.07 µg/L, respectively. Besides, an environmentally friendly sample pre-treatment strategy was employed that allowed easy and effective elimination of complex matrices. The ic-ELISA method observed the average recovery rate from 87.7% to 94.0% with the variance coefficient (CV) ranging from 2.2% to 9.4%. Additionally, the identification of 25 commercially available herbal teas using liquid chromatography-tandem mass spectrometry (LC-MS/MS) further confirmed the validity of our detection. The results of the two methods are consistent. Overall, the proposed ic-ELISA could be an ultrasensitive and reliable method for chlorphenamine maleate adulterated in foods or exposure to the environment. Full article

Loratadine (LRD), a non-sedating and slow-acting antihistamine, is often given in combination with short-onset chlorpheniramine maleate (CPM) to increase efficacy. However, LRD has poor water solubility resulting in low bioavailability. The aim of this study was to improve LRD solubility by preparing co-amorphous LRD-CPM. However, the obtained co-amorphous LRD-CPM recrystallized rapidly, and the solubility of LRD returned to a poor state again. Therefore, co-amorphous LRD-CPM solid dispersions using polyvinylpyrrolidone (PVP) as a carrier were prepared. The obtained solid dispersions were characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR). The solubility, dissolution, and mechanism of drug release from the LRD-CPM/PVP co-amorphous solid dispersions were studied and compared with those of intact LRD, LRD/PVP solid dispersions, and co-amorphous LRD-CPM mixtures. The results from XRPD and DSC confirmed the amorphous form of LRD in the co-amorphous solid dispersions. The FTIR results indicated that there was no intermolecular interaction between LRD, CPM, and PVP. In conclusion, the obtained LRD-CPM/PVP co-amorphous solid dispersions can successfully increase the water solubility and dissolution of LRD and extend the amorphous state of LRD without recrystallization. Full article

The purpose of the study is to develop and assess mucoadhesive in situ nasal gel formulations of loratadine and chlorpheniramine maleate to advance the bioavailability of the drug as compared to its conventional dosage forms. The influence of various permeation enhancers, such as EDTA (0.2% w/v), sodium taurocholate (0.5% w/v), oleic acid (5% w/v), and Pluronic F 127 (10% w/v), on the nasal absorption of loratadine and chlorpheniramine from in situ nasal gels containing different polymeric combinations, such as hydroxypropyl methylcellulose, Carbopol 934, sodium carboxymethylcellulose, and chitosan, is studied. Among these permeation enhancers, sodium taurocholate, Pluronic F127 and oleic acid produced a noticeable increase in the loratadine in situ nasal gel flux compared with in situ nasal gels without permeation enhancer. However, EDTA increased the flux slightly, and in most cases, the increase was insignificant. However, in the case of chlorpheniramine maleate in situ nasal gels, the permeation enhancer oleic acid only showed a noticeable increase in flux. Sodium taurocholate and oleic acid seems to be a better and efficient enhancer, enhancing the flux > 5-fold compared with in situ nasal gels without permeation enhancer in loratadine in situ nasal gels. Pluronic F127 also showed a better permeation, increasing the effect by >2-fold in loratadine in situ nasal gels. In chlorpheniramine maleate in situ nasal gels with EDTA, sodium taurocholate and Pluronic F127 were equally effective, enhancing chlorpheniramine maleate permeation. Oleic acid has a better effect as permeation enhancer in chlorpheniramine maleate in situ nasal gels and showed a maximum permeation enhancement of >2-fold. Full article

In many parts of the world, water resources are scarce or even extremely scarce, and the reuse of water resources has become mainstream in today’s world. Many regions use treated wastewater for agricultural irrigation, aquaculture, and other activities. However, in recent years, wastewater has been found to contain large amounts of pharmaceuticals and personal care products (PPCPs). Therefore, there is a potential risk of PPCPs being transported in the environment and affecting human health. In this study, we compared the uptake, transport, and accumulation of 27 PPCPs in three types of sprouts (radish, buckwheat, and okra).The bioaccumulation of amantadine, diphenhydramine, chlorpheniramine maleate, sibutramine, hemosibutramine, chlorosibutramine, N-monomethyl sibutramine, N, N-desmethyl sibutramine, and carbamazepine was found to be significantly higher in plants grown for 12 days in media containing 0.5, 5.0, and 50.0 ng/mL PPCPs. With increasing concentration of PPCPs in the culture solution, the amount of PPCPs absorbed by plants and the degree of accumulation also showed an increasing trend. At the same time, it was demonstrated that there was an obvious uptake transfer phenomenon of PPCPs by plants, and the trend of uptake transfer became more and more obvious as the concentration of external environmental pollutants increased. In addition, amantadine, chlorpheniramine maleate, carbamazepine, N, N-desmethyl sibutramine, hemosibutramine, and chlorosibutramine showed more active translocation in some plants (TF > 1.0). Full article

One of the most prevalent over-the-counter cold and cough medications is the chlorpheniramine maleate (CPM)–ibuprofen (IBF) combination. A reversed-phase high-performance liquid chromatography (RP-HPLC) method was effectively optimized and developed for the simultaneous detection of chlorpheniramine maleate and ibuprofen in a pharmaceutical formulation. The mobile phase for the RP-HPLC method was an isocratic combination of acetonitrile and 0.01 M acetate buffer at pH 3.8 (55:45; v/v) on an Eclipse Plus C18 reversed phase column. An ultraviolet (UV) detector with a wavelength of 225 nm was used to detect the analytes at a flow rate of 1.0 mL/min. CPM and IBF were satisfactorily eluted, with mean retention times of 2.09 and 6.27 min, respectively. The approach was shown to be linear (R² > 0.9998 for CPM and 0.9992 for IBF), precise (% RSD 3.02% for CPM and 3.48% for IBF), accurate (% recoveries 97.7–98.9% for CPM and 101–104.5% for IBF), specific, easy to use, sensitive, quick, and robust. Limits of detection (LODs) were found to be 10 and 27 μg/mL for CPM and IBF, respectively. Without interference from excipients, the validated method could be utilized in regular quality control analysis of various dosage combinations of hard gelatin capsules containing CPM and IBF. Full article

Non-destructive analysis of chlorpheniramine maleate (CPM), pharmaceutical tablets, and granules was conducted by chemometrics-assisted attenuated total reflectance infrared spectroscopy (ATR-IR). For tablets, an optimum PLSR model with eight latent factors was obtained from area-normalized and standard normal variate (SNV) pretreated ATR-IR spectral data with correlation coefficients (R²) of calibration and cross-validation of 0.9716 and 0.9602, respectively. The model capability for the 42 test set samples was proven with R² between the reference and model prediction values of 0.9632, and a root-mean-square error of prediction (RMSEP) of 1.7786. The successive PLSR model for granules was constructed from SNV and first derivative pretreated ATR-IR spectral data with two latent factors and correlation coefficients (R²) of calibration and cross-validation of 0.9577 and 0.9450, respectively. Full article

The polyelectrolyte poly(sodium 4-styrenesulfonate) undergoes aromatic–aromatic interaction with the drug chlorpheniramine, which acts as an aromatic counterion. In this work, we show that an increase in the concentration in the dilute and semidilute regimes of a complex polyelectrolyte/drug 2:1 produces the increasing confinement of the drug in hydrophobic domains, with implications in single chain thermodynamic behavior. Diafiltration analysis at polymer concentrations between 0.5 and 2.5 mM show an increase in the fraction of the aromatic counterion irreversibly bound to the polyelectrolyte, as well as a decrease in the electrostatic reversible interaction forces with the remaining fraction of drug molecules as the total concentration of the system increases. Synchrotron-SAXS results performed in the semidilute regimes show a fractal chain conformation pattern with a fractal dimension of 1.7, similar to uncharged polymers. Interestingly, static and fractal correlation lengths increase with increasing complex concentration, due to the increase in the amount of the confined drug. Nanoprecipitates are found in the range of 30–40 mM, and macroprecipitates are found at a higher system concentration. A model of molecular complexation between the two species is proposed as the total concentration increases, which involves ion pair formation and aggregation, producing increasingly confined aromatic counterions in hydrophobic domains, as well as a decreasing number of charged polymer segments at the hydrophobic/hydrophilic interphase. All of these features are of pivotal importance to the general knowledge of polyelectrolytes, with implications both in fundamental knowledge and potential technological applications considering aromatic-aromatic binding between aromatic polyelectrolytes and aromatic counterions, such as in the production of pharmaceutical formulations. Full article

The present study describes the use of two taste-masking polymers to fabricate a formulation of chlorpheniramine maleate for paediatric administration. Co-axial electrospinning was utilized to create layered nanofibres; the two polymers, Eudragit^® E PO and Kollicoat^® Smartseal, were alternated between the core and the shell of the system in order to identify the optimum taste-masked formulation. The drug was loaded in the core on all occasions. It was found that the formulation with Kollicoat^® Smartseal in the core with the drug, and Eudragit^® E PO in the shell showed the most effective taste-masking compared to the other formulations. These fibres were in the nano-range and had smooth morphology as verified by scanning electron microscopy. Solid-state characterization and thermal analysis confirmed that amorphous solid dispersions were formed upon electrospinning. The Insent E-tongue was used to assess the taste-masking efficiency of the samples, and it was found that this formulation was undetectable by the bitter sensor, indicating successful taste-masking compared to the raw version of the drug. The E-tongue also confirmed the drug’s bitterness threshold as compared to quinine HCl dihydrate, a parameter that is useful for formulation design and taste-masking planning. Full article

Jellies for oral administration have been suggested as alternative dosage forms to conventional tablets for improved palatability and compliances for pediatric and geriatric patients. To evaluate the effect of jelly formulation on the bioavailability of cold medicines, two types of jellies were prepared for a fixed-dose combination of acetaminophen (AAP), chlorpheniramine maleate (CPM), dextromethorphan hydrobromide (DMH), and dl-methylephedrine hydrochloride (MEH). Jelly-S and Jelly-H were fabricated using carrageenan and locust bean gum in the absence and presence of xanthan gum, respectively. In vitro dissolution and in vivo absorption of the four drugs in the jellies were compared with other conventional formulations, a syrup and two types of immediate-release (IR) tablets with different hardness, Tablet-S (15 kPa) and Tablet-H (20 kPa). All the formulations exhibited more than 80% dissolution rate within 2 h even though the syrup, Jelly-S, and Tablet-S showed higher 30-min dissolution compared to Jelly-H and Tablet-H. The dissolution rates from the jellies decreased with increasing pH, which resulted in the slowest dissolution in pH 6.8 compared to the syrup and IR tablets. When administered orally to beagle dogs, all five formulations were determined not to be bioequivalent. However, Jelly-S and Jelly-H showed 0.82–1.05 of the geometric mean ratios (GMRs) of AUC_0-t for all four drugs compared to the syrup suggesting comparable absorption. In two IR tablets, GMRs of AUC_0-t were in a range of 0.55–0.95 indicating a tendency of lower absorption than the syrup and jellies. In conclusion, jelly can be a patient-centered formulation with comparable bioavailability to syrup. Full article

Separation of nine commonly used active ingredients in cold medicines, were demonstrated by micellar electrokinetic chromatography. The ingredients included paracetamol, chlorpheniramine maleate, diphenhydramine hydrochloride, triprolidine hydrochloride, phenylpropanolamine hydrochloride, dextromethorphan hydrobromide, loratadine, aspirin and caffeine. Effects of buffer concentrations, pH, organic modifiers and capillary length were investigated. The optimum conditions were achieved in 10 mM sodium dihydrogenphosphate-sodium tetraborate buffer, pH 9.0, containing 50 mM sodium dodecyl sulfate and 28% v/v acetonitrile using the effective length of 50 cm, the separating voltage of +15 kV and the capillary temperature of 30°C. Separation of all peaks was obtained within 28.4 min with a resolution of 1.2. Full article