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Mebeverine hydrochloride is an important drug to treat irritable bowel syndrome. The solubility of this drug in supercritical carbon dioxide was measured at temperatures from 35 to 65 °C and pressures from 12 to 30 MPa. Results were between 2.16 and 30.2 ppm by mole. The data were correlated with density‐based models (K‐J, MST, Chrastil, Garlapati and Madras, Bartle et al., and Sparks et al.) and equations of state (Peng‐Robinson, Soave, and Estévez et al. models). The mean relative deviation and corrected correlation coefficient were used to assess the goodness of the models. Based on all ten models, Sparks et al. performed best according to average absolute relative deviation (5.64 %), and Bartle et al. was the best according to Radj (0.997). However, this contribution's main merit is the reported experimental data. [ABSTRACT FROM AUTHOR]

A novel and highly sensitive flow injection method was developed for the determination of Mebeverine. The method is based on the formation of an ion pair compound between Mebeverine hydrochloride and calcium hexacyanoferrate in an ammonium chloride medium, resulting in the formation of a whitish-yellow precipitate complex. The analysis was performed using a homemade NAG-4SX3-3D triple flow cell CFIA Analyzer. The experimental parameters were studied to optimize both the chemical and physical aspects of the method. The linear working range was obtained to be 0.01-40 mM, with an impressive correlation coefficient (r) of 0.9907. The limit of detection (LOD) was determined to be 0.349 µg/150 µl, and the repeatability of the method (RSD%) was demonstrated to be less than 1.5%. To further evaluate the performance of the newly proposed method, a comparison was conducted using the standard addition method in conjunction with a classical method. Overall, the developed flow injection method offers simplicity, sensitivity, and reliable analytical performance for the determination of Mebeverine, making it a promising alternative to the classical method. [ABSTRACT FROM AUTHOR]

Background: To assess the effectiveness and safety of a fixed-dose combination (FDC) of mebeverine hydrochloride 135 mg and chlordiazepoxide 5 mg in the management of irritable bowel syndrome (IBS) in Indian patients. Methods: This was an 8-week, prospective, open-label, observational study. Patients (n = 60, age: 18–60 years) newly diagnosed with IBS and having anxiety symptoms (score ≥18 on Hamilton Anxiety Rating Scale [HAM-A]), who were prescribed the study drug as a part of routine practice were included. Results: All 60 enrolled patients completed the study. Patients' mean standard deviation (SD) age was 37.45 (11.00) years; most were male (73.33%). The mean (SD) IBS-symptoms severity scale (IBS-SSS) score at baseline was 182.72 (84.39) indicating moderate symptom severity; the mean change at week 8 was 85.50 (82.69), P < 0.0001 (primary endpoint), and at week 4 was 64.70 (58.44), P < 0.0001. The mean (SD) IBS-36 score was 78.33 (41.87) at baseline and decreased at week 8 by 45.88 (34.92), P < 0.0001. At week 8, majority of patients achieved a ≥50-point improvement in IBS-SSS score (73.33%), and a ≥10-point improvement in IBS-36 scores (88.33%). The mean (SD) HAM-A total score was 26.97 (6.72) at baseline and decreased to 10.45 (8.99) at week 8, P < 0.0001. Three adverse drug reactions unlikely to be related to study drug were reported in two patients (nausea n = 1, headache n = 2). Good tolerability to study drug was reported by all patients and investigators at week 8. Conclusion: The FDC of mebeverine hydrochloride and chlordiazepoxide was effective in the treatment of IBS and was well tolerated. [ABSTRACT FROM AUTHOR]

Background: The remarkable properties of nickel oxide (NiO) and cerium oxide (CeO2) nanostructures have attracted considerable interest in these nanocomposites as potential electroactive materials for sensor construction. Methods: The mebeverine hydrochloride (MBHCl) content of commercial formulations was determined in this study using a unique factionalized CeO2/NiO-nanocomposite-coated membrane sensor. Results: Mebeverine-phosphotungstate (MB-PT) was prepared by adding phosphotungstic acid to mebeverine hydrochloride and mixing with a polymeric matrix (polyvinyl chloride, PVC) and plasticizing agent o-nitrophenyl octyl ether. The new suggested sensor showed an excellent linear detection range of the selected analyte at 1.0 × 10−8–1.0 × 10−2 mol L−1 with regression equation EmV = (−29.429 ± 0.2) log [MB] + 347.86. However, the unfunctionalized sensor MB–PT displayed less linearity at 1.0 × 10−5–1.0 × 10−2 mol L−1 drug solution with regression equation EmV = (−26.603 ± 0.5) log [MB] + 256.81. By considering a number of factors, the applicability and validity of the suggested potentiometric system were improved following the rules of analytical methodological requirements. Conclusion: The created potentiometric technique worked well for determining MB in bulk substance and in medical commercial samples. [ABSTRACT FROM AUTHOR]

Additive technologies have undoubtedly become one of the most intensively developing manufacturing methods in recent years. Among the numerous applications, the interest in 3D printing also includes its application in pharmacy for production of small batches of personalized drugs. For this reason, we conducted multi-stage pre-formulation studies to optimize the process of manufacturing solid dosage forms by photopolymerization with visible light. Based on tests planned and executed according to the design of the experiment (DoE), we selected the optimal quantitative composition of photocurable resin made of PEG 400, PEGDA MW 575, water, and riboflavin, a non-toxic photoinitiator. In subsequent stages, we adjusted the printer set-up and process parameters. Moreover, we assessed the influence of the co-initiators ascorbic acid or triethanolamine on the resin's polymerization process. Next, based on an optimized formulation, we printed and analyzed drug-loaded tablets containing mebeverine hydrochloride, characterized by a gradual release of active pharmaceutical ingredient (API), reaching 80% after 6 h. We proved the possibility of reusing the drug-loaded resin that was not hardened during printing and determined the linear correlation between the volume of the designed tablets and the amount of API, confirming the possibility of printing personalized modified-release tablets. [ABSTRACT FROM AUTHOR]

Background: The remarkable properties of nickel oxide (NiO) and cerium oxide (CeO2) nanostructures have attracted considerable interest in these nanocomposites as potential electroactive materials for sensor construction. Methods: The mebeverine hydrochloride (MBHCl) content of commercial formulations was determined in this study using a unique factionalized CeO2/NiO-nanocomposite-coated membrane sensor. Results: Mebeverine-phosphotungstate (MB-PT) was prepared by adding phosphotungstic acid to mebeverine hydrochloride and mixing with a polymeric matrix (polyvinyl chloride, PVC) and plasticizing agent o-nitrophenyl octyl ether. The new suggested sensor showed an excellent linear detection range of the selected analyte at 1.0 × 10−8–1.0 × 10−2 mol L−1 with regression equation EmV = (−29.429 ± 0.2) log [MB] + 347.86. However, the unfunctionalized sensor MB–PT displayed less linearity at 1.0 × 10−5–1.0 × 10−2 mol L−1 drug solution with regression equation EmV = (−26.603 ± 0.5) log [MB] + 256.81. By considering a number of factors, the applicability and validity of the suggested potentiometric system were improved following the rules of analytical methodological requirements. Conclusion: The created potentiometric technique worked well for determining MB in bulk substance and in medical commercial samples.

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The photocatalytic degradation of the Mebeverine hydrochloride (MEB) by ZnO and the combined ZnO-Activated Carbon (ZnO-AC) under solar light has been investigated in batch mode. The AC was prepared from dates stems using ZnCl2 as chemical activation agent. The effect of some operating parameters on the MEB degradation efficiency such as: photocatalyst dose, solution pH and initial MEB concentration has been examined. The results revealed that the surface reaction on ZnO plays a crucial role in the MEB photo-degradation as confirmed by UV-Visible spectrophotometry. The photocatalytic efficiency of the mixture ZnO-AC is dependent on the mass ratio ZnO/AC, which was optimized for a value of 15 wt%. The MEB degradation kinetics follows a pseudo first order model and the Langmuir-Hinselwood (L-H) model fit adequately the experimental data. Besides, our results show that the combined system (adsorption/photocatalysis) is effective for the MEB degradation than the photocatalysis process alone. A comparative study with the literature indicated the benefits of coupling ZnO-AC under the solar light (93 mW cm−2). [ABSTRACT FROM AUTHOR]

Additive technologies have undoubtedly become one of the most intensively developing manufacturing methods in recent years. Among the numerous applications, the interest in 3D printing also includes its application in pharmacy for production of small batches of personalized drugs. For this reason, we conducted multi-stage pre-formulation studies to optimize the process of manufacturing solid dosage forms by photopolymerization with visible light. Based on tests planned and executed according to the design of the experiment (DoE), we selected the optimal quantitative composition of photocurable resin made of PEG 400, PEGDA MW 575, water, and riboflavin, a non-toxic photoinitiator. In subsequent stages, we adjusted the printer set-up and process parameters. Moreover, we assessed the influence of the co-initiators ascorbic acid or triethanolamine on the resin’s polymerization process. Next, based on an optimized formulation, we printed and analyzed drug-loaded tablets containing mebeverine hydrochloride, characterized by a gradual release of active pharmaceutical ingredient (API), reaching 80% after 6 h. We proved the possibility of reusing the drug-loaded resin that was not hardened during printing and determined the linear correlation between the volume of the designed tablets and the amount of API, confirming the possibility of printing personalized modified-release tablets.

Mebeverine hydrochloride (MVH) is a potent direct antispasmodic agent acting mainly on the smooth muscles of the gastrointestinal tract (GIT) and is used to treat irritable bowel syndrome and reducing the abdominal spasm. Herein, hydrogels of dextran using acrylic acid (monomer) and N,N-methylenebisacrylamide (crosslinker) followed by further modification using isopropylamine were prepared as vehicles for the delivery of MVH. Synthesized hydrogels were evaluated for drug loading and types of interaction involved in drug loading. Drug release study was performed in pH 2.2 and pH 7.4 to mimic the pH of simulated gastric fluid and simulated intestinal fluid, respectively, to evaluate the effect of structural factor on drug release. Different kinetic models were applied to drug release data in order to evaluate drug release mechanisms and kinetics. Criteria for selecting the most appropriate model were based on the linearity basis (coefficient of correlation). [ABSTRACT FROM AUTHOR]

Objective: Mebeverine hydrochloride is an antispasmodic agent that has a direct musculotropic action on the smooth muscles of the gastrointestinal tract; especially the colon. Therefore, the current study aimed at formulating and optimizing colon targeted mebeverine hydrochloride microspheres for treatment of chronic gastrointestinal disorder. Methods: Mebeverine hydrochloride-loaded chitosan microspheres were formulated adopting emulsion cross-linking method using glutaraldehyde as a cross linking agent. A 3³ Box Behnken design was utilized in formulating the microspheres and investigating the effect of different formulation factors such as drug: polymer ratio (X1), stirring speed (X2) and the surfactant concentration (X3) on particle size (Y1), the entrapment efficiency percentage (Y2) and the cumulative release percentage of mebeverine hydrochloride after 8 h (Y3). Result: The particle size and entrapment efficiency were significantly affected by tested formulation parameters. The release of mebeverine hydrochloride from optimized formula was pH dependent. In simulated gastric fluid, less than 10% of entrapped mebeverine hydrochloride was released, while, a relatively high amount of the drug (> 65%) was released in simulated colonic fluid (pH 7.4). The in vivo pharmacokinetic study revealed that the optimized formula of microspheres exhibited increased oral absorption of mebeverine hydrochloride, compared to free drug (Cmax 168.51±20.05 ng/ml vs. 126.45±29.46 ng/ml, respectively). In addition, the optimized formula exerted a remarkably higher systemic bioavailability, compared to the free drug. Conclusion: These results underscore the applicability of cross-linked chitosan microspheres as a promising carrier for colon targeted delivery of mebeverine hydrochloride for treating diseases associated with the colon such as irritable bowel syndrome. [ABSTRACT FROM AUTHOR]

Herein, a feasible chemical reduction method followed by intensive mixing was applied for the preparation of an attractive material based on graphite studded with cuprous oxide nanoparticle-based cubes (Cu2ONPs–C@G). Transmission electron microscope (TEM), scanning electron microscope (SEM), X-ray diffraction (XRD) and cyclic voltammetry (CV) were utilized for characterization. Cuprous oxide nanoparticles (Cu2ONPs), with a diameter range mainly distributed from 4 to 20 nm, aggregate to form microcubes (Cu2ONPs–C) with an average diameter of about 367 nm. Paste electrode was prepared using Cu2ONPs–C@G (Cu2ONPs–C@G/PE) for voltametric quantification of the musculotropic antispasmodic drug: mebeverine hydrochloride (MEB). The electrochemical behavior of MEB was studied using CV, and the optimum analytical parameters were investigated using square wave adsorptive anodic stripping voltammetry (SWAdASV). Moreover, density functional theory (DFT) was used to emphasize the ability of MEB to form a complex with Cu2+, confirming the suggested electrochemical behavior of MEB at Cu2ONPs–C@G/PE. With good stability and high reproducibility, SWAdASV of Cu2ONPs–C@G/PE shows successful quantification of MEB over the concentration range of 5.00 × 10−11–1.10 × 10−9 M with lower limit of detection (LOD) and lower limit of quantification (LOQ) values of 2.41 × 10−11 M and 8.05 × 10−11 M, respectively. Finally, accurate quantification of MEB in dosage forms (tablets) and biological fluids (spiked human urine and plasma samples) was achieved using Cu2ONPs-C@G/PE.

Irritable bowel syndrome (IBS) is one of the most common functional bowel diseases. What is more, a number of digestive diseases are characterized by symptoms similar to those observed in IBS. The principles of treatment of IBS and IBS-related disorders are same. The key symptom of IBS - abdominal pain - is developed as a result of spasmodic or hyperkinetic dyskinesia, so the main group of drugs to be used in the treatment are antispasmodics. Preference is given to selective antispasmodics. Sparex is a national generic of the selective intestinal antispasmodic mebeverine hydrochloride which has been known since 1965, and is characterized by the most affordable price among analogues. The study which included 48 patients demonstrated high efficacy of Sparex administered for 4 weeks in a dosage of 200 mg twice daily for relief of pain, flatulence and stool normalization both in IBS and IBS-related disorders. Good and satisfactory results evaluated by a 3-point scale were achieved in 87.5% of patients. The results allowed to conclude that the medicine, apart from its strong antispasmodic effect, also provided a eukinetic action - normalization of the transit of chyme in the intestine both in constipation and diarrhea. Normalization of stool was observed in 77.2% of patients with both constipation and diarrhea, and in the rest of patients the severity of stool disorders decreased by more than 1 point. In the course of the study, no side effects were observed while taking Sparex.

Selective myotropic spasmolytics are the most effective modern correction means for pain at irritable bowel syndrome. Currently various drugs of mebeverine hydrochloride are represented in the domestic market, the dosage of the active substance in which is identical but they are produced by various technologies. We established that in patients with the irritable bowel syndrome administration of the drug Niaspam (Sun Pharmaceutical Industries Ltd.) at standard dosages for 2 weeks showed high effectiveness in arresting pain syndrome and intestinal dyskinesias. Niaspam statistically reliably reduces the relative intensity of intestinal contractions, normalizes the contraction rythmicity but effective predominantly in lower parts of the gastrointestinal tract. Peculiarities of the production technology allow gradual mebeverine release from the capsule, which is extremely important in therapy of intestinal dyskinesias.

Purpose: To formulate and evaluate an antispasmodic drug, mebeverine hydrochloride (Mbv-HCl), as a local anesthetic mucoadhesive buccal tablet. Methods: Mbv-HCl loaded tablets were formulated, using a direct compression technique, with varying polymer concentrations including carbopol 934P alone, carbopol 934P/hydroxypropyl methylcellulose (HPMC) mixture, or carbopol 934P/chitosan mixture. The tablets were evaluated for physicochemical characteristics, in-vitro drug release, bioadhesive strength, swelling, ex-vivo residence time, ex-vivo permeation, drug permeation through the buccal membrane of sheep, and stability. Results: The results indicate that formulation F4, which contains HPMC/carbopol 934P (3:1), showed the best in-vitro drug release profile. The release kinetics for all the formulations fitted well with Hixson-Crowell kinetic model. Bioadhesive strength, surface pH, and swelling index of F4 were 41.52, 6.36, and 231.2 %, respectively. Maximum residence time ex-vivo was exhibited by formulation F4, showing a maximum residence time of about 330 min with 80 % of Mbv-HCl permeated in 6 h ex-vivo. F4 was stable after storage for 60 days at 25 °C/60 % RH and 40 °C/75 % RH, with non-significant change (p < 0.05) in drug content, bioadhesive strength and in vitro release. Conclusion: The optimized mucoadhesive buccal formulation is promising for delivery of Mbv-HCl, and displays high bioadhesion and adequate permeability through sheep buccal membrane to achieve a local anesthetic action. [ABSTRACT FROM AUTHOR]

Electrospinning was used to prepare core/shell fibers containing the active pharmaceutical ingredients indomethacin (IMC) or mebeverine hydrochloride (MB-HCl). The shell of the fibers was fabricated from the pH sensitive Eudragit S100 polymer, while the drug-loaded core was based on the mucoadhesive poly(ethylene oxide) (PEO). Three different drug loadings (from 9 to 23% (w/w) of the core mass) were prepared, and for MB-HCl two different molecular weights of PEO were explored. The resultant fibers generally comprise smooth cylinders, although in some cases defects such as surface particles or flattened or merged fibers were visible. Transmission electron microscopy showed all the systems to have clear core and shell compartments. The drugs are present in the amorphous physical form in the fibers. Dissolution tests found that the fibers can effectively prevent release in acidic conditions representative of the stomach, particularly for the acidic indomethacin. After transfer to a pH 7.4 medium, sustained release over between 6 and 22 h is observed. Given the mucoadhesive nature of the PEO core, after dissolution of the shell the fibers will be able to adhere to the walls of the intestinal tract and give sustained local drug release. This renders them promising for the treatment of conditions such as irritable bowel disease and colon cancer. [ABSTRACT FROM AUTHOR]

A novel electrochemical sensor for the selective determination of mebeverine hydrochloride (MEB) in drug substance, products, and human plasma was introduced. The prepared nanoparticle sensor was based on a carbon paste electrode chemically modified with silica and gold nanoparticles. The surface morphology of the modified electrode was characterized by scanning electron microscope. Several parameters such as pH, scan rate, and accumulation time were optimized in order to determine the best conditions for analysis. A good linear response was obtained in the range of 4.0 × 10−1 × 10 mol L with detection limit of 1.5 × 10 mol L. The obtained results are in good agreement with those obtained by official method. The method was applied for determination of mebeverine hydrochloride in different pharmaceutical dosage forms containing MEB alone or in mixtures with sulpiride or chlordiazepoxide as well as in human plasma. The developed method was simple, rapid, economic, and challenging to green chemistry. [ABSTRACT FROM AUTHOR]

Both fast dissolving and sustained release drug delivery systems (DDSs) comprising mebeverine hydrochloride ( MB- HCl) embedded in either povidone ( PVP) K60 or Eudragit® L 100-55 nanofibers have been prepared by electrospinning. The fibers are found to have cylindrical morphologies with smooth surfaces, except at high drug loadings that appear to induce surface roughness ( PVP) or fragmentation ( Eudragit). There is a general increase in fiber diameter with drug loading. Differential scanning calorimetry and X-ray diffraction demonstrate that the drug exists in an amorphous state in the fibers. Infrared spectroscopy data indicate that the drug has good compatibility with the polymer, whereas nuclear magnetic resonance spectroscopy and high-performance liquid chromatography analyses confirmed that the MB- HCl was not degraded during the spinning process. In vitro dissolution tests of the PVP fiber mats show them to dissolve within 10 s, an improved dissolution profile over the pure drug. The Eudragit fibers show p H-dependent drug release profiles, with only very limited release at p H 2.0 but sustained release over approximately 8 h at p H 6.8. The Eudragit nanofibers have the potential to be developed as oral DDSs for localized drug release in the intestinal tract, whereas the PVP materials may find the application as buccal delivery systems or suppositories. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:283-292, 2014 [ABSTRACT FROM AUTHOR]

Performance of partial least squares regression (PLSR) is enhanced in the presented work by three multivariate models, including weighted regression PLSR (Weighted-PLSR), genetic algorithm PLSR (GA-PLSR), and wavelet transform PLSR (WT-PLSR). The proposed models were applied for the stability-indicating analysis of mixtures of mebeverine hydrochloride (meb) and sulpiride (sul) in the presence of their reported impurities and degradation products. The work introduced in this paper aims to compare these different chemometric methods, showing the underlying algorithm for each and making a comparison of analysis results. For proper analysis, a 6-factor, 5-level experimental design was established resulting in a training set of 25 mixtures containing different ratios of the interfering species. A test set consisting of 5 mixtures was used to validate the prediction ability of the suggested models. Leave one out (LOO) and bootstrap were applied to predict number of PLS components. The GA-PLSR proposed method was successfully applied for the analysis of raw material (test set 101.03% ± 1.068, 101.47% ± 2.721 for meb and sul, respectively) and pharmaceutical tablets containing meb and sul mixtures (10.10% ± 0.566, 98.16% ± 1.081 for meb and sul). Copyright © 2011 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Abstract: A comparison between support vector regression (SVR) and Artificial Neural Networks (ANNs) multivariate regression methods is established showing the underlying algorithm for each and making a comparison between them to indicate the inherent advantages and limitations. In this paper we compare SVR to ANN with and without variable selection procedure (genetic algorithm (GA)). To project the comparison in a sensible way, the methods are used for the stability indicating quantitative analysis of mixtures of mebeverine hydrochloride and sulpiride in binary mixtures as a case study in presence of their reported impurities and degradation products (summing up to 6 components) in raw materials and pharmaceutical dosage form via handling the UV spectral data. For proper analysis, a 6 factor 5 level experimental design was established resulting in a training set of 25 mixtures containing different ratios of the interfering species. An independent test set consisting of 5 mixtures was used to validate the prediction ability of the suggested models. The proposed methods (linear SVR (without GA) and linear GA-ANN) were successfully applied to the analysis of pharmaceutical tablets containing mebeverine hydrochloride and sulpiride mixtures. The results manifest the problem of nonlinearity and how models like the SVR and ANN can handle it. The methods indicate the ability of the mentioned multivariate calibration models to deconvolute the highly overlapped UV spectra of the 6 components’ mixtures, yet using cheap and easy to handle instruments like the UV spectrophotometer. [Copyright &y& Elsevier]

A simple, economic, and time-efficient stability-indicating, reverse-phase ultra-performance liquid chromatographic (RP-UPLC) method has been developed for analysis of mebeverine hydrochloride in the presence of both impurities and degradation products generated by forced degradation. When mebeverine hydrochloride was subjected to acid hydrolytic, oxidative, base hydrolysis, photolytic, and thermal stress, degradation was observed only in base hydrolysis. The drug was found to be stable to other stress conditions. Successful chromatographic separation of the drug from impurities formed during synthesis and from degradation products formed under stress conditions was achieved on a Waters Acquity C18, 50 mm x 2.1 mm, 1.7 µ particle size column, UV detection at 225 nm and a gradient elution of orthophosphoric acid and acetonitrile as the mobile phase. The method was validated for specificity, precision, linearity, accuracy, and robustness and can be used for quality control during manufacture and for assessment of the stability samples of mebeverine hydrochloride. To the best of our knowledge, a validated stability indicating UPLC method that separates all the six impurities disclosed in this investigation has not been published elsewhere. Total elution time was about 8 min which allowed quantification of more than 100 samples per day. [ABSTRACT FROM PUBLISHER]

Abstract: Validated sensitive and highly selective stability indicating methods are adopted for simultaneous quantitative determination of sulpiride and mebeverine hydrochloride in presence of their reported impurities and hydrolytic degradates whether in pure forms or in pharmaceutical formulation. The first method is High Performance Liquid Chromatography, where the mixture of sulpiride and mebeverine hydrochloride together with the reported interferents plus metopimazine as internal standard are separated on a reversed phase cyano column (5 μm ps, 250 mm × 4.6 id) using acetonitrile: water (70:30 v/v) adjusted to pH = 7 as a mobile phase. The drugs were detected at 221 nm over a concentration range of 5–40 μg ml−1 and 5–60 μg ml−1 with mean percentage recoveries 99.75% (S.D. 0.910) and 99.99% (S.D. 0.450) for sulpiride and mebeverine hydrochloride respectively. The second method is High Performance Thin Layer Chromatography, where sulpiride and mebeverine hydrochloride are separated on silica gel HPTLC F254 plates using absolute ethanol:methylene chloride:triethyl amine (7:3:0.2 by volume) as mobile phase and scanning of the separated bands at 221 nm over a concentration range of 0.4–1.4 and 0.2–1.6 μg band−1 with mean percentage recoveries 101.01% (S.D. 1.991) and 100.40% (S.D. 1.868) for sulpiride and mebeverine hydrochloride respectively. [ABSTRACT FROM AUTHOR]

Mebeverine hydrochloride is known to suffer from extensive first pass effect. In an attempt to improve its oral bioavailability and possibility to restrict its absorption only to the colon, mebeverine microspheres were prepared by emulsion solvent evaporation method. Four formulations were prepared with varying drug and polymer ratio. These formulations were subjected to various evaluation parameters like percent practical yield, entrapment efficiency, particle size, in vitro drug release, in vivo activity. Practical yield of the microspheres was up to 89.59% with encapsulation efficiency up to 79.4%. Scanning electron microscopy confirmed that the microsphere structures were smooth, spherical, and discrete and the particles were of the size range 200 to 300 µm. In vitro release of the drug showed biphasic release pattern with non-Fickian diffusion release in 12 h. On the basis of drug content, particle size, in vitro release and in vivo studies, formulation F-3 was found to be optimal. Antiirritable bowel syndrome activity was performed in colorectal distention in rat, which is a model for constipation-induced irritable bowel syndrome. The formulations F-2 and F-3 showed significant effect in fecal output when compared to the control as well as the marketed preparation in the constipation-induced irritable bowel syndrome in rats. [ABSTRACT FROM AUTHOR]

The antispasmodic drug mebeverine hydrochloride was formulated into a film-forming gel to be used as a topical local anesthetic. A mixture of cellulose derivatives was used as a base. Additives were used to enhance the release as well as the residence time. Formulations were characterized in terms of drug release, mucoadhesion and rheology. Clinically, the selected formula has shown faster onset (p = 0.0156), longer duration (p = 0.0313), better film residence (p = 0.0313), and no foreign body sensation (p = 0.0313) in comparison to Solcoseryl® dental paste. Histopathological examination showed no change in inflammatory cells count, concluding that this topical anesthetic is efficacious and safe orally. [ABSTRACT FROM AUTHOR]

Abstract: Four PVC membrane electrodes for the determination of mebeverine hydrochloride (MvCl) were fabricated and fully characterized in terms of composition, life span, usable pH range, working concentration range and temperature. The membranes of these electrodes consist of mebeverinium-silicotungstate (Mv-ST), silicomolybdate (Mv-SM), phosphotungstate (Mv-PT), or phosphomolybdate (Mv-PM) ion-associations dispersed in PVC matrix with dibutyl phthalate plasticizer. The electrodes showed near-Nernstian response over the concentration range of 4.0 × 10-6 to 1.0 × 10-2M MvCl and were applied to the potentiometric determination of mebeverinium ion in pharmaceutical preparations, serum and urine in steady state and flow injection (FI) conditions with average recoveries of 96.4–102 % and relative standard deviations of 0.132–1.86%. The electrodes exhibit good selectivity for MvCl with respect to a large number of inorganic cations, organic cations, sugars and amino acids. The sensitivities of these electrodes are high enough to measure as low as 1.86μg/ml of MvCl which permit the determination of the Ksp values of the ion-associates used. The proposed potentiometric methods offer the advantages of simplicity, accuracy, automation feasibility and applicability to turbid and colored sample solutions. [Copyright &y& Elsevier]

Two simple and sensitive methods are described for the quantitative determination of mebeverine hydrochloride as single ingredient. The first method depends on the application of quantitative 1H-NMR spectroscopy using deuterated chloroform and hexamine as an internal reference standard. The second method is based on measuring the native fluorescence of mebeverine hydrochloride in 0.1 N sulphuric acid at 360 nm with excitation at 290 nm. Furthermore simultaneous determinations of two component mixtures, mebeverine hydrochloride with sulpiride and isopropamide iodide with trifluoperazine hydrochloride are presented using first-derivative and second-derivative UV-spectrophotometry, respectively. The proposed methods have been successfully applied to the determination of the cited drugs in commercial tablets. Compared with the reference methods, the proposed methods are more sensitive, with good accuracy and reproducibility. [ABSTRACT FROM AUTHOR]

Three simple, sensitive and reproducible visible spectrophotometric methods (A-C) for the determination of mebeverine hydrochloride (MVH) in bulk samples and pharmaceutical formulations are described. Methods A and B are based on the formation of ion-association complexes between the drug and fast green FCF (FGFCF, λmax 625 nm) or bromothymol blue (BTB, λmax 405 nm). Method C is based on the formation of a molecular complex between the drug and cobalt thiocyanate (CTC, λmax 625 nm). Regression analysis of Beer's plots showed good correlation in the concentration ranges 2–40, 2–25 and 100–600 μg/ml for methods A, B and C respectively. No interference was observed from the usually existing additives in pharmaceutical formulations and the applicability of the methods was examined by analysing tablets containing MVH. Standard deviations were typically ⩽ 0.75 mg per dose (RSD: 0.25–0.5%). Recoveries were 99.0–100.2%. [ABSTRACT FROM AUTHOR]

Herein, a feasible chemical reduction method followed by intensive mixing was applied for the preparation of an attractive material based on graphite studded with cuprous oxide nanoparticle-based cubes (Cu2ONPs–C@G). Transmission electron microscope (TEM), scanning electron microscope (SEM), X-ray diffraction (XRD) and cyclic voltammetry (CV) were utilized for characterization. Cuprous oxide nanoparticles (Cu2ONPs), with a diameter range mainly distributed from 4 to 20 nm, aggregate to form microcubes (Cu2ONPs–C) with an average diameter of about 367 nm. Paste electrode was prepared using Cu2ONPs–C@G (Cu2ONPs–C@G/PE) for voltametric quantification of the musculotropic antispasmodic drug: mebeverine hydrochloride (MEB). The electrochemical behavior of MEB was studied using CV, and the optimum analytical parameters were investigated using square wave adsorptive anodic stripping voltammetry (SWAdASV). Moreover, density functional theory (DFT) was used to emphasize the ability of MEB to form a complex with Cu2+, confirming the suggested electrochemical behavior of MEB at Cu2ONPs–C@G/PE. With good stability and high reproducibility, SWAdASV of Cu2ONPs–C@G/PE shows successful quantification of MEB over the concentration range of 5.00 × 10−11–1.10 × 10−9 M with lower limit of detection (LOD) and lower limit of quantification (LOQ) values of 2.41 × 10−11 M and 8.05 × 10−11 M, respectively. Finally, accurate quantification of MEB in dosage forms (tablets) and biological fluids (spiked human urine and plasma samples) was achieved using Cu2ONPs-C@G/PE. [ABSTRACT FROM AUTHOR]

• Mebeverine hydrochloride, being a hydrophilic drug, is unable to penetrate the skin. • Encapsulation of Mebeverine hydrochloride improves drug skin penetration. • Encapsulation of Mebeverine hydrochloride energizes its local anesthetic action. Mebeverine hydrochloride (MBH) is an antispasmodic drug that holds the potential to exert a local anesthetic action via blocking voltage operated sodium channels. However, its local anesthetic activity was not yet exploited due its poor skin permeability. Nanocarriers have emerged as efficient vehicles for delivering both lipophilic and hydrophilic drugs through the stratum corneum. In this study, therefore, the efficacy of ethosomes for delivering MBH via skin for local anesthetic effect was investigated. The ethosomes were formulated, optimized and characterized for particle size, zeta potential, entrapment efficiency and in vitro permeation studies. Then, the optimized formula was incorporated into Carbopol 940® gel and evaluated for skin irritation and in vivo local anesthetic action. Ethosomes were spherical in shape with vesicle sizes varied from 308.2 ± 18.2 nm to 78.8 ± 8.6 nm and entrapment efficiencies of 18–65%. In vitro drug permeation across rabbit ear skin revealed enhanced drug permeation and higher transdermal flux with ethosomal formulations, compared to aqueous drug solution. In addition, an ethosomal gel of optimized formula showed a potent local anesthetic effect as manifested by a 2.3-fold increase in the area under the efficacy curve (AUEC) of MBH loaded ethosomal gel, compared to the MBH gel. Furthermore, skin irritation experiments demonstrated that MBH ethosomal gel induced neither erythema nor edema upon application to rabbit skin. Collectively, MBH loaded ethosomal vesicles might represent a promising delivery vehicle for safe and efficient local anesthetic effect. [ABSTRACT FROM AUTHOR]