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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.

The aim is to study the effect and safety of using the antispasmodic and synbiotic (Lactobacillus paracasei CNCM I-1572 in combination with fructooligosaccharides) in patients with irritable bowel syndrome with constipation.Materials and methods — prospective randomized controlled trial of 80 patients with irritable bowel syndrome with constipation. Patients in the main group (40 people) took mebeverine hydrochloride 200 mg 2 times a day and synbiotic (5x109 CFU Lactobacillus paracasei CNCM I-1572 and 5.2 g fructooligosaccharides) during 28 days. Patients in the control group (40 people) received mebeverine hydrochloride 200 mg 2 times a day during 28 days. Before and after treatment, patients underwent the GSPS questionnaire.Results — in control group clinical remission was achieved in 52.6% of patients. In the main group clinical remission was established in 92.3%, the increase was 39.7% (p Conclusion — the results of study demonstrate a significant increase in the effectiveness of therapy in patients with irritable bowel syndrome with constipation with the combined use of antispasmodic and synbiotic.

Physicians tend to prescribe brand-name medicines for treating specific diseases. This might be due to the better clinical effects of these medicines compared to the generic ones. The aim of the pr...

International audience; The removal efficiency of the pharmaceutical drug Mebeverine Hydrochloride (MEB) from solutions by an activated carbon (AC) prepared from dates stems was investigated in the present research work. The surface properties of the activated carbon were investigated by elementary analysis, BET surface area, SEM, FTIR and pH(pzc). The operating parameters effect on the MEB adsorption efficiency was investigated by using batch experiments. The adsorption isotherms study indicated that the experimental data were well described by Freundlich and DR isotherms, with the maximum adsorption capacity (q(max)) of 4105 mg/g. This result suggests the multilayer adsorption of MEB on the activated carbon. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s40201-021-00658-1.

The paper presents information on modern functional disorders of the gastrointestinal tract and biliary system, based on the recommendations of the Rome IV. Own studies on the effectiveness of treatment of biliary functional disorders with Niaspam (mebeverine hydrochloride) are presented. We studied 30 patients with biliary pain and functional disorders of the gallbladder. As a result of studies, it was found that the symptoms of biliary dysfunction stop in 83.3 % of patients, the contractility of the gallbladder is restored in 86.7 %. No side effects have been reported.

A simple, precise, rapid, accurate and economic reverse phase high performance liquid chromatographic method has been developed for the estimation of mebeverine hydrochloride in bulk and tablet dosage form. The separation was achieved by using kinetex column C18 (150×4.6mm, 5µ) and 15mM ammonium acetate and methanol in proportion of 30:70 v/v as mobile phase, at a flow rate of 1.0mL/min. The detection was carried out at 230nm. The retention time of mebeverine was found to be 3.346 minutes.The limit of detection and limit of quantitation were found to be 0.005µg/mL and 0.016µg/mL, respectively. The reliability of the proposed method was ascertained by evaluating various validation parameters like linearity, precision, accuracy and specificity according to ICH guidelines. The proposed method applies LC-MS compatible buffers which increases the life time of column and can be used as lc-ms compatible method. This method acts as a quality control tool for routine analysis of mebeverine hydrochloride in bulk and tablet dosage forms.

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.

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.

The main objective of this paper is to develop and validate flow injection method, a precise, accurate, simple, economic, low cost and specific turbidimetric method for the quantitative determination of mebeverine hydrochloride (MbH) in pharmaceutical preparations. A homemade NAG Dual & Solo (0-180º) analyser which contains two identical detections units (cell 1 and 2) was applied for turbidity measurements. The developed method was optimized for different chemical and physical parameters such as perception reagent concentrations, aqueous salts solutions, flow rate, the intensity of the sources light, sample volume, mixing coil and purge time. The correlation coefficients (r) of the developed method were 0.9980 and 0.9986 for cell 1 and 2 respectively and showed the linearity of response against concentration over the range of 1.0 to 6.5 and 0.7-6.5mmol/L for cell 1 & 2 respectively. The limit of detections (LOD) for cell 1 and cell 2 were 0.28 and 0.21 mmol/L respectively. The intra-day and inter-day precision for two serial estimations of 3.5 and 5.5 mmol/L of MBH exhibited a relative standard deviation of 0.46%, 0.28%, 0.23%, 0.26% and 0.39%, 0.79%, 0.14%, 0.05% for cell 1 & 2 respectively. The accuracy of the developed method has expressed a recovery percentage (Rec %) and error % which was between 99.22 to 101.13 and 99.39 to 101.17 for cell 1 and cell 2 respectively. The ICH guidelines were followed for method validation. The developed method was successfully applied for the determination of MbH in pure and pharmaceutical preparations and the method can be conveniently used for routine analysis in laboratory as a quality control method since the method permits quantitively determination of 60 samples/h.

A validated method for the estimation of the mebeverine hydrochloride, an anti-spasmodic agent, was developed which was simple, precise, rapid and accurate. A clear separated chromatographic peak was achieved on Apollo C18 (4.6x250 mm), 5-μm column. Mobile phase used in this separation was the mixture of methanol and water in the ratio of 90:10% v/v with a flow rate of 0.9 μL/min at ambient temperature. The detection was achieved at a wavelength of 265 nm. At the retention time of 3.9 min and tailing factor of 1.09, chromatographic peak was observed. As per the guidelines of ICH, the method was developed and was validated with respect to accuracy, linearity, specificity, precision and robustness. Correlation co-efficient obtained shows a good linear relationship of more than 0.998 in the concentration range of 5 μg to 30 μg. Mean % recovery of 99.2% was seen and %RSD for repeatability and intermediate precision was less than 2%. Therefore, the developed method can be used for the quantitative determination of mebeverine hydrochloride successfully in pharmaceutical dosage forms.

By using precipitation polymerization, liquid electrodes of polymers imprinted with Mebeverine hydrochloride and metronidazole benzoate were created whereas the imprinted polymer (MIP) and non imprinted (NIP) polymers were prepared by using Mebeverine hydrochloride and Metronidazole benzoate qua a template. In the polymerization process, 2-Acrylamido-2-methyl-1-propane Sulphonic acid (AMPS) or 1-Vinylimidazole (VIZ) was used qua monomer, pentaerythritol triacrylate (PETRA) or Divinylbanzene (DVB) was used qua a cross-linker while benzoyl peroxide (BPO) was used as an initiator. The MIP membranes and the membranes of NIP were created by using Dibutyl Sebacate (DBS) and Tris(2-ethylhexyl)phosphate(TEHP) qua plasticizers in PVC matrix. The response time of the liquid electrodes was 1min. whereas their slopes and detection limits reached to 19.62 – 57.36 mV per decade and 1.2 x 10-6 – 2.0 x 10-5 M, respectively. Filling with standard solution of drug (0.1M), the liquid electrodes response -with suitable No.( selectivity for numerous of species - was suitable No.( since pH reached to 1.5 – 12. The developed electrodes were successfully applied for the analyte determination in preparation pharmaceutical sample without any time consuming pretreatment steps.

In different applications, pharmaceutical products are widely distributed and frequently released into the environment. The adsorption of Mebeverine hydrochloride (MB.HCl) on chitosan polymer was studied under certain conditions. The Adsorption Isotherms can be well defined using the Freundlich and Temkin equations. The pH of the solution significantly influences the adsorption potential of chitosan, the adsorption of chitosan increased from the initial pH of 1.1 and then decreased over the (2-10) pH range. Adsorption is sensitive to the change in ion strength, indicating that electrostatic attraction is an important mechanism for the sorption process. Adsorption of chitosan to MB.HCl is defined as endothermic adsorption by enthalpy change (ΔH). The value of the (ΔG) is negative at all the temperatures studied, which suggests the spontaneous trend to adsorb MB.HCl to chitosan. The value of (ΔG) decreased when the temperature rose from 5°C to 25°C, indicating higher adsorption of MB.HCl at an increased temperature. The positive value of (ΔS) represents chitosan’s attraction to drugs as well as that randomness on its solid-solution interface.

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.

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.

The introduction of sustainable development concepts to analytical laboratories has recently gained interest, however, most conventional high-performance liquid chromatography methods do not consider either the effect of the used chemicals or the amount of produced waste on the environment. The aim of this work was to prove that conventional methods can be replaced by greener ones with the same analytical parameters. The suggested methods were designed so that they neither use nor produce harmful chemicals and produce minimum waste to be used in routine analysis without harming the environment. This was achieved by using green mobile phases and short run times. Four mixtures were chosen as models for this study; clidinium bromide/chlordiazepoxide hydrochloride, phenobarbitone/pipenzolate bromide, mebeverine hydrochloride/sulpiride, and chlorphenoxamine hydrochloride/caffeine/8-chlorotheophylline either in their bulk powder or in their dosage forms. The methods were validated with respect to linearity, precision, accuracy, system suitability, and robustness. The developed methods were compared to the reported conventional high-performance liquid chromatography methods regarding their greenness profile. The suggested methods were found to be greener and more time- and solvent-saving than the reported ones; hence they can be used for routine analysis of the studied mixtures without harming the environment.

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 o C/60 % RH and 40 o 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. Keywords: Mebeverine hydrochloride, Buccal, Mucoadhesive tablet, Swelling index, Bioadhesive strength, Local anesthetic

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).

WOS: 000278921800022, PubMed ID: 20101482, Gel formulations of mebeverine hydrochloride (MbHCl) containing hydroxypropylmethylcellulose (HPMC), metolose (MTL), and poloxamer 407 (PLX) were prepared to be used in the treatment of different oral painful conditions. HPMC was used as a mucoadhesive gel base while MTL and PLX were used to prepare sol-gel thermosensitive gels. MTL and PLX formulations showed proper sol-gel transition temperature for intraoral application. Formulations were evaluated in terms of their viscosity, mechanical properties, mucoadhesivity, stability, and in vitro drug release. The formulation prepared with 2% of HPMC K100M provided the highest viscosity at room temperature. However, the viscosity of HPMC-PLX mixture showed a significant increase at body temperature. The greatest mucoadhesion was also noted in HPMC PLX combinations. Texture pro. le analysis exhibited the differences of the adhesion, hardness, elasticity, cohesiveness, and compressibility of the formulations. The release profiles of MbHCl were obtained, and non-Fickian release was observed from all the formulations. The formulations were stored at different temperature and relative humidity. No significant changes were observed at the end of the 3 months. HPMC-PLX formulation of MbHCl was chosen for in vivo studies, and it remained longer than dye solution on the rabbit's intraoral mucosal tissue. It was found worthy of further clinical evaluation.

Simple, sensitive, rapid and cost effective extraction spectrophotometric methods are described for the assay of mebeverine hydrochloride (MBH) in bulk samples and pharmaceutical formulations. These two methods (Bromophenol blue and Erichrome Black-T) are based on the formation of chloroform soluble ion-pair complexes of MBH with Bromophenol blue (BPB) and with Erichrome Black-T (EBT), to form yellow and pink colored chromogen in a Glycine-HCl buffer of pH 2.4 (BPB) and in a KCI-HCl buffer of pH 1.4 (EBT) with absorbance maximum at 416 nm and at 524 nm for BPB and EBT respectively. The calibration graph is found to linear over 0.2-20 μg/mL (BPB) and 0.2-20 μg/mL (EBT), with molar absorptivity values of 1.8295 x 10 4 1 moL -1 cm -1 and 1.5896 x 10 4 1 moL -1 cm -1 , respectively. The LOD (Limit of Detection) were found to be 0.090 μg/mL and 0.084 μg/mL and LOQ (Limit of Quantification) were 0.2997 μg/mL and 0.2730 μg/mL for the BPB and EBT method, respectively. The results of analysis for the two methods have been validated statistically and by recovery studies. The results are compared with those obtained with reported method. The proposed methods are simple, sensitive, accurate and suitable for quality control applications.

Two accurate, precise and simple spectrophotometric methods had been developed and validated for the determination of mebeverine hydrochloride (MEB) and chlordiazepoxide (CHL). The first method was used for the determination of MEB in the range of 5-81 μg/mL and CHL in the range of 0.5-4 μg/mL, MEB was determined by second derivative spectrophotometric determination by measuring the peak amplitude at 234.8 nm (zero value of CHL) whereas CHL was determined by first derivative spectrophotometric method by measuring the peak amplitude at 280.4 nm (zero value of MEB). In the second method, three chemometric methods were evaluated for simultaneous assay of MEB and CHL. The developed methods were successfully applied to the analysis of the cited drugs in laboratory prepared mixtures and tablets with good recoveries. The validity of the proposed methods was further assessed by applying the standard addition technique. The validation was carried out following the International Conference on Harmonization (ICH) guidelines.

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.

The efficiency of the well known antispasmodic drug mebeverine-hydrochloride, as a local anaesthetic was evaluated. The drug was formulated into different ointment and gel bases. The prepared topical applications were evaluated for the in vitro release of the drug and for the local anaesthetic effect on the rabbit's eye. The release profile agreed with the first order kinetics, the release rate and the duration of action of the drug was found to be a function of type of base. Carbopol 934 gel gave the longest duration of action (113 minutes), the polyethylen glycol base gave a moderate duration (50 minutes), while the shortest duration of action (15 minutes) was achieved in case of hydrophilic petrolatum.

In this study Eudragit RS PM and RL PM were evaluated as carriers for the preparation of prolonged release solid dispersions of mebeverine hydrochloride by solvent and melting methods. The prepared tablets were examined for dissolution at pH 1.2 and 7.4, Eudragit RS PM and RL PM were found satisfactory as potential slow release carriers. The solid dispersion prepared by the solvent method showed a slow release pattern. Drug release appeared to fit both, first order and Higuchi matrix model kinetics. However, on application of the differential rate treatments, the evidence supported the Higuchi matrix model. Effect of temperatures on dissolution rate was studied for thermodynamic consideration.The drug release was pH-independent until pH 7.4.As the pH increased, the release was significantly reduced due to solubility problem.

Double emulsions (w/o/w) were prepared by two steps emulsification procedure using isopropyl myristate as the oily phase. The influence of the inner aqueous phase volume and emulsifier concentration on the release characteristics of either caffeine or mebeverine hydrochloride from the prepared emulsions was studied. For the purpose of comparison, the release of each drug from either o/w or w/o emulsion was investigated. The results showed that the release of both drugs from w/o/w emulsions was independent on the inner aqueous phase volume. The release of mebeverine hydrochloride was sustained from either w/o/w or w/o emulsions while that of caffeine was not significantly retarded as indicated by the amount released after 24 hours. Increasing the concentration of the hydrophilic emulsifier (Tween 20) had a little effect on the release of both drugs from w/o/w emulsions. On the other hand, the release of mebeverine hydrochloride was more prolonged on increasing the concentration of the lipophilic emulsifier (Span 80), while the release of caffeine was not significantly retarded.

Mebeverine hydrochloride suppositories were prepared using Witepsol H15 suppository base. The effect of different concentrations of various enhancers (surfactants, amino acids and osmotic modifiers) on the drug release form the prepared suppositories was studied. The results showed that mebeverine hydrochloride suppositories containing Brij 35 (2%) and urea (10%) were superior to the other formulations containing the tested enhancers. These formulae showed the highest release rates (K = 0.083 ± 0.004 min-1 and 0.111 ± 0.005 min-1 , respectively) that followed first-order kinetics with t50% of 8.35 ± 0.45 min and 6.24 ± 0.33 min, respectively. Therefore, these two formulae with the control suppositories were subjected to in vivo study in albino rabbits compared to the commercial Duspatalin® tablets and intravenous injection. Higher Cmax (1770.26 ± 165.46 ng.ml-1) within shorter Tmax (0.75 ± 0.20 h) was observed after rectal administration of the control suppositories compared to that of commercially available film-coated tablets (Duspatalin® – 135 mg). A significant difference (p≤0.05) between the absolute bioavailability of Duspatalin® tablets (27.09 ± 3.80%) and control suppositories (46.66 ± 1.72%) was detected. Statistically (p≤0.05), the mean residence time (MRT) after oral administration of Duspatalin® tablets (3.16 ± 0.30 h) was significantly longer than that after the rectal administration of control suppositories (2.73 ± 0.30 h). suppositories containing 2% Brij 35 showed higher plasma levels of the drug (2766.11± 339.50 ng.ml-1) with an absolute bioavailability of 70.50 ± 10.51% compared to 27.09 ± 3.80% for Duspatalin® tablets.

Two methods are described for the simultaneous determination of mebeverine hydrochloride (MB) and sulpiride (SU) in their combinations. The first method depends on the first derivative of the ratio spectra by measurement of the amplitudes at 263.7 and 234.9 nm for MB and SU, respectively. The linear ranges and detection limits are 4.0-40.0 and 0.72 microg/ml for MB and 1.0-10.0 and 0.34 microg/ml for SU. In the second case, a chemometric (classical least squares) method was developed. The concentration data matrices were obtained by using different concentrations of pure drugs in 0.1 M HCl. The absorbance data matrix corresponding to each concentration data matrix was obtained by the measurements of absorbances in the range 200-300 nm in their zero order spectra; then calibration was obtained by using the absorbance data matrix and the concentration data matrix for the prediction of the unknown concentrations of MB and SU in their mixture. The numerical values were calculated by using Matlab R12 version 6.0 and Origin 5.0 software. The procedures do not require any separation steps. These two methods were successfully applied for assaying the pharmaceutical formulation, of Colona tablets.

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 I�m. 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.

First- and second-derivative spectrophotometric methods have been proposed for the determination of glibenclamide, mebeverine hydrochloride and clopamide with their corresponding degradation products. Solutions of these drugs were analysed by measuring the first- and second-derivative spectral response at certain wavelengths where the respective degradation products exhibit no contribution. Also, clopamide can be determined in a mixture with reserpine and dihydroergocristine by utilising the second-derivative method. Kinetic investigation of the alkaline degradation rate of these drugs revealed that the proposed methods were stability indicating. The different pharmaceutical preparations were assayed and were found to give results of the same accuracy and reproducibility as the corresponding official method or “maximum absorbance” methods of assay.

Mebeverine hydrochloride (Duspatalin†), synthesized during the course of a study on a series of reserpine derivatives, was found to be an active smooth muscle relaxant.