Mebeverine HCl Research Articles

QbD: A novel approach for formulation and optimization of colon targeted drug delivery system containing mebeverine HCl

The aim of the work is to study the programmed release of model antispasmodic drug Mebeverine HCl based on pulsatile principle to target colon proximity. Compression coated tablets included core tablet consisting of Croscarmellose as super disintegrant and pulsatile layer comprising impermeable Ethocel cup and mixture of Keltone, Eudragit S100, Ethocel as swellable and rupturable layer. The prepared core tablet was evaluated for weight variation, hardness, thickness, friability, drug content, disintegration time and in vitro dissolution studies. For optimization Box-Behnken design was employed to study the effect of independent variables viz., weight ratio of Keltone (X1), Eudragit S100 (X2), Ethocel (X3) on dependent variables viz., t10 (Y1), t50 (Y2) and Q12 (Y3). Results revealed positive influence of independent factors on responses. The data were statistically analyzed using ANOVA and were found to be statistically significant (P < 0.05). Mathematical modeling for kinetic studies revealed that the release profile after lag time followed first order kinetics. The results concluding that a successful pulsatile drug delivery system of Mebeverine HCl was developed.

Development and validation of simple, precise UV spectrophotometric methods for the quantification of Mebeverine HCl in API and Marketed Products

Simple, rapid, economic and sensitive UV spectrophotometric methods using three solvent mediums viz., 0.1N HCl, Phosphate buffer pH 6.8 and Phosphate buffer pH 7.4 were developed and validated for the estimation of Mebeverine HCl in active pharmaceutical form, Marketed tablets and capsules. The developed methods were validated in terms of linearity, accuracy, precision, and specificity, limit of detection and limit of quantification as per ICH guidelines. The purity of Mebeverine HCl was characterized by melting point and FTIR. At determined absorption maxima of 263 nm for all solvents proved to be linear in the range of 1-50 µg/ml and exhibited good correlation coefficient (R2 = 0.9999, 0.9992, 0.9999) and recovery of (99.00 – 104.55%). This method is applied for two marketed Mebeverine HCl brands and results were in good agreement with label claim. The methods were validated statistically and by recovery studies for linearity, precision, repeatability, and reproducibility. The obtained results proved that the method can be employed for the routine analysis of Mebeverine HCl in active pharmaceutical form as well as in the commercial marketed formulations viz., tablets and capsules.

Formulation and in vitro evaluation of compression coated mebeverine HCl tablets for colon targeting

The aim of the study was to develop colon targeted compression coated Mebeverine HCl (MEB) tablets using pH dependent, swellable and rupturable polymers for effective treatment of irritable bowel syndrome (IBS). The MEB loaded core tablets were prepared by direct compression method using CCM and CP as super disintegrating agents at different concentrations and evaluated for pre compression and post compression parameters. The optimized core tablets were further used to fabricate compression coated tablets using different ratios of Eudragit L100, Eudragit S100 as pH- dependent polymers, Keltone and Ethocel as swellable and rupturable polymers by modified compression method. Drug compatibility with excipients was checked by FTIR studies and results indicate no interaction. The precompression and post compression studies were within acceptable limits. In vitro dissolution studies were done for compression coated tablets to find out the lag phase, burst drug release and retard drug release The findings of this study concludes that the lag time of compression coated tablet can be modulated by combining with EL 100, ES 100, Keltone and Ethocel in different weight ratio. These designed tablet system was found to be satisfactory in terms of release of the drug after the predetermined lag time, thus the system can be target to release in the colon proximity. The compression coating technique can be successfully applied for MEB for colon targeting to treat IBS.

Mebeverine HCl-loaded sodium carboxymethyl gum ghatti-chitosan microparticles: In vitro-in vivo evaluations

The current research attempted to design a sustained releasing microparticles made of chitosan and carboxymethylated derivative of gum ghatti (CMGG) via polyelectrolyte complexation. CMGG was synthesized by conventional Williamson ether synthesis method, where degree of substitution was found 0.40 ± 0.04%. The synthesized CMGG and chitosan was used to formulate mebeverine HCl (M-HCl) loaded CMGG-chitosan microparticles by means of crosslinking using glutaraldehyde (covalent crosslinker). The particle sizes and DEE (%) of these M-HCl loaded microparticles were within 34.40 ± 1.06 to 46.00 ± 1.05 μm and 75.85 ± 1.20% to 51.44 ± 0.25%, respectively. The formulated M-HCl loaded CMGG-chitosan microparticles were instrumentally characterized using SEM, DSC and FTIR analyses. In vitro, M-HCl loaded microparticles in gastric pH were observed to have a greater M-HCl releasing rate than those at alkaline pH. Korsmeyer–Peppas model with the Fickian diffusion phenomena were found to be followed by these newly developed microparticles in in vitro drug releasing. In addition, in vivo pharmacodynamic activity of M-HCl loaded CMGG-chitosan microparticles in healthy rabbits was evaluated and a higher correlation coefficient indicated the existence of excellent in vitro-in vivo correlation.

Design and Evaluation of Mebeverine Hydrochloride Microspheres with Novel Timed Release Polymers

Drugs having the shorter half life are needed to be administered frequently in order to maintain the required therapeutic concentrations. One of the strategies to overcome the frequent administration is by developing the controlled release formulations. Microspheres including the micro particles and microcapsules (having a core of the drug) of 1-1000 μm in diameter are one of the emerging controlled drug delivery systems that can eliminate the frequent drug administration. Hence, in the present study an effort was made to formulate microsphere of Mebeverine HCl by using different delayed-released polymers at different concentrations. Different formulations were prepared using guar gum and glutaraldehyde as delayed release polymers and evaluated for the properties like the effect of polymer concentrations on the microsphere formation, particle size, muco-adhesion etc. Also, the prepared microspheres were evaluated for flow properties along with the drug release rates. From the results, it was observed that higher concentrations of polymer resulted in better microsphere formation compared to low concentrations. Projection Microscopic images of optimized formulation showed that the microspheres have rough surface. In vitro drug release studies showed that the optimized formulation showed 96.26 percent Mebeverine HCl release at the end of 13 hours. Overall, it can be concluded that the preparation of Mebeverine HCl microspheres can eliminate the need for frequent administration thereby providing the better therapeutic compliance compared to the conventional dosage forms.

Development of Mebeverine HCl Prolonged release Mini-tablets by thermoplastic granulation technique

Mebeverine HCl is a BCS class-I drug and thus it possesses high solubility in aqueous media across the biological pH range. The marketed reference product is a multi-unit particulate system (MUPS) containing prolonged release pellets filled in hard gelatin capsule. In conventional manufacturing process, a huge quantity of solvents (aqueous and/or organic) is used to manufacture such dosage form. Additionally, it demands more processing time and efforts. Therefore, a prolonged release capsules dosage form of Mebeverine HCl was formulated using thermoplastic (melt) granulation technique without usage of any solvent. Prolonged release minitablets sized 2 mm in diameter were developed as per quality by design principles. A 23 full-factorial design of experiment was applied to optimize levels of drug release controlling ingredients which includes a hydrophobic meltable binder (hydrogenated castor oil) cum matrixing agent, a hydrophilic meltable binder (polyethylene glycol) which may act as pore former also, and a release controlling polymer (ethyl cellulose). The optimized formulation was found stable. Dissolution profiles of the optimized formulation were found similar to the marketed reference product in different media across the physiological pH range. In conclusion, the explored solvent less process was capable to manufacture the MUPS dosage form of Mebeverine HCl prolonged-release capsules, which is stable and pharmaceutically equivalent with the reference product. The developed process is more beneficial to small and medium scale industry, as it does not require any special and costly equipment, significantly decreases manufacturing cost and increases productivity compared to conventional process, which is mentioned in literature.

Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl.

To prolong the residence time of dosage forms within the gastrointestinal tract until all drug is released at the desired rate is one of the real challenges for oral controlled-release drug delivery systems. This study was designed to develop a controlled-release floating matrix tablet and floating raft system of Mebeverine HCl (MbH) and evaluate different excipients for their floating behavior and in vitro controlled-release profiles. Oral pharmacokinetics of the optimum matrix tablet, raft system formula, and marketed Duspatalin® 200 mg retard as reference were studied in beagle dogs. The optimized tablet formula (FT-10) and raft system formula (FRS-11) were found to float within 34±5 sec and 15±7 sec, respectively, and both remain buoyant over a period of 12 h in simulated gastric fluid. FT-10 (Compritol/HPMC K100M 1:1) showed the slowest drug release among all prepared tablet formulations, releasing about 80.2% of MbH over 8 h. In contrast, FRS-11 (Sodium alginate 3%/HPMC K100M 1%/Precirol 2%) had the greatest retardation, providing sustained release of 82.1% within 8 h. Compared with the marketed MbH product, the Cmax of FT-10 was almost the same, while FRS-11 maximum concentration was higher. The tmax was 3.33, 2.167, and 3.0 h for marketed MbH product, FT-10, and FRS-11, respectively. In addition, the oral bioavailability experiment showed that the relative bioavailability of the MbH was 104.76 and 116.01% after oral administration of FT-10 and FRS-11, respectively, compared to marketed product. These results demonstrated that both controlled-released floating matrix tablet and raft system would be promising gastroretentive delivery systems for prolonging drug action.

SIMULTANEOUS DETERMINATION OF 2-CHLORO METHYL PROPIONATE, 1,4-DI-BROMO BUTANE AND PARA ANISIC ALDEHYDE IN MEBEVERINE HYDROCHLORIDE API BY GAS CHROMATOGRAPHY-MASS SPECTROMETRIC WITH SELECTED-ION-MONITORING MODE

<p>ABSTRACT<br />Objective: To develop an accurate, precise and linear gas chromatography-mass spectrometric (GC-MS) selected-ion-monitoring (SIM) method for<br />quantitative estimation of 2-chloro methyl propionate (2-CMP), 1,4-dibromo butane and para anisic aldehyde (PAA) as an genotoxic impurities in<br />mebeverine HCl API (MEB) at ppm level and validated as per International Council of Harmonization (ICH) guidelines.<br />Methods: This method used in SIM mode mass selective detection was developed and validated for the trace level analysis of three impurities. All<br />these three impurities are simultaneously determined by a GC-MS method using VF-624 Capillary column (60 m×0.32 mm×1.80 µm) with Helium as<br />carrier gas and a flow rate of 2.0 mL/minutes. Chromatographic separation of 2-CMP, 1,4-DBB, and PAA was achieved in 7.91, 13.69, 18.45 minutes<br />and m/z values were 63, 55, 135 on SIM mode.<br />Results: The method was linear for 2-CMP, 1,4-DBB and PAA in mebeverine HCl 1.90 µg/ml to 7.5 µg/ml, respectively. The coefficient of correlation<br />(r<br />) for the 2-CMP, 1,4-DBB and PAA was better than 0.999. The limit of detection obtained was 0.28, 0.35, 0.22 µg/ml and the limit of quantification<br />(LOQ) obtained was 0.85, 1.06, 0.66 µg/ml. The method was fully validated, complying Food and Drug Administration, ICH and European Medicines<br />Agency guidelines. Furthermore, verified precision, accuracy, LOQ precision, LOQ accuracy, ruggedness, and robustness.<br />2<br />Conclusion: The proposed method is specific, accurate, precise, linear, rugged and robust for the determination of the three genotoxic impurities in<br />API of mebeverine HCl, and hence, is of wide applicability in pharmaceutical industries.<br />Keywords: 2-chloro methyl propionate, 1,4-dibromo butane, Para anisic aldehyde, Mebeverine HCl, Gas chromatography-mass spectrometric, Method<br />development, Method validation.</p>

Method Development and Validation of Mebeverine HCl in Bulk Drugs by Using Spectrophotometric Method

In the present research a simple, accurate, precise and cost effective UV-Vis spectrophotometric method for the estimation of Mebeverine HCl in bulk was illustrated. The absorption maxima of the drug was found to be 220 nm in 0.1 N HCl. A linear response was observed in the range of 5-15 µg/ml with a regression coefficient of 1.0. Validation parameters were carried out as per the guidelines of International Conference for Harmonization. This method can be used in the industries for determination of Mebeverine HCl to analyze the quality of Mebeverine HCl without any interference.

Simultaneous HPLC Determination of Chlordiazepoxide and Mebeverine HCl in the Presence of Their Degradation Products and Impurities

A simple, rapid, and sensitive RP-HPLC method was developed and validated for the simultaneous determination of chlordiazepoxide (CDO) and mebeverine HCl (MBV) in the presence of CDO impurity (2-amino-5-chlorobenzophenone, ACB) and MBV degradation product (veratric acid, VER). Separation was achieved within 9 min on a BDS Hypersil phenyl column (4.5 mm × 250 mm, 5 µm particle size) using a mobile phase consisting of acetonitrile: 0.1 M potassium dihydrogen phosphate: triethylamine (35 : 65 : 0.2, v/v/v) in an isocratic mode at a flow rate of 1 mL/min. The pH of the mobile phase was adjusted to 4.5 with orthophosphoric acid and UV detection was set at 260 nm. A complete validation procedure was conducted. The proposed method exhibited excellent linearity over the concentration ranges of 1.0–100.0, 10.0–200.0, 2.0–40.0, and 2.0–40.0 µg/mL for CDO, MBV, VER, and ACB, respectively. The proposed method was applied for the simultaneous determination of CDO and MBV in their coformulated tablets with mean percentage recoveries of 99.75 ± 0.62 and 98.61 ± 0.38, respectively. The results of the proposed method were favorably compared with those of a comparison HPLC method using Studentt-test and the variance ratioF-test. The chemical structure of MBV degradation product was ascertained by mass spectrometry and IR studies.

Photoinduced oxidation of a tris(2,2'‐bipyridyl)ruthenium(II)–peroxodisulfate chemiluminescence system for the analysis of mebeverine HCl pharmaceutical formulations and biological fluids using a two‐chip device

A new method for the analysis of mebeverine hydrochloride (MEB) has been developed using a two-chip device. The method is highly selective, sensitive, rapid and consumes minute amount of reagents. The developed method is free of interference from the degradation products of MEB and from common ingredients present in pharmaceutical formulations. The limit of detection was 0.043 µg/mL, and the limit of quantification was 0.138 µg/mL. The short analysis time per sample (20 s) allowed a large number of analyses to be performed within a very short time. Various samples were analyzed, including two different pharmaceutical formulations and a uniformity of content analysis for 20 tablets from a known batch and two biological samples at different concentrations. In addition, the method was compared with a validated high-performance liquid chromatography (HPLC) method and the results clearly indicated the suitability of the developed method for routine analyses. A new mechanism for the tris(2,2'-bipyridyl)ruthenium(II) (Ru(bpy)3 (2+) )-peroxodisulfate (S2 O8 (2-) ) chemiluminescence (CL) system has also been proposed. The mechanism is based on photoinduced oxidation of Ru(bpy)3 (2+) to Ru(bpy)3 (3+) via the formation of Ru(bpy)3 (2+) * upon irradiation with visible light. S2 O8 (2-) then oxidizes Ru(bpy)3 (2+) * to Ru(bpy)3 (3+) and the analyte subsequently reduces the resultant Ru(bpy)3 (3+) to Ru(bpy)3 (2+) *, which then produces the CL signal.

Simultaneous determination of some antiprotozoal drugs in different combined dosage forms by mean centering of ratio spectra and multivariate calibration with model updating methods.

BackgroundMetronidazole (MET) and Diloxanide Furoate (DF), act as antiprotozoal drugs, in their ternary mixtures with Mebeverine HCl (MEH), an effective antispasmodic drug. This work concerns with the development and validation of two simple, specific and cost effective methods mainly for simultaneous determination of the proposed ternary mixture. In addition, the developed multivariate calibration model has been updated to determine Metronidazole benzoate (METB) in its binary mixture with DF in Dimetrol® suspension.ResultsMethod (I) is the mean centering of ratio spectra spectrophotometric method (MCR) that depends on using the mean centered ratio spectra in two successive steps that eliminates the derivative steps and therefore the signal to noise ratio is enhanced. The developed MCR method has been successfully applied for determination of MET, DF and MEH in different laboratory prepared mixtures and in tablets. Method (II) is the partial least square (PLS) multivariate calibration method that has been optimized for determination of MET, DF and MEH in Dimetrol ® tablets and by updating the developed model, it has been successfully used for prediction of binary mixtures of DF and Metronidazole Benzoate ester (METB) in Dimetrol ® suspension with good accuracy and precision without reconstruction of the calibration set.ConclusionThe developed methods have been validated; accuracy, precision and specificity were found to be within the acceptable limits. Moreover results obtained by the suggested methods showed no significant difference when compared with those obtained by reported methods.Graphical

Application of Fourier Function to Double Divisor Ratio Spectra Curves for Analysis of Some Amoebicide Drugs in Their Ternary Mixtures

This work concerns with development of spectrophotometric methods for analysis of Metronidazole, Diloxanide Furoate and Mebeverine HCl. Method (I) is double divisor ratio spectra derivative method (DDRD) which depends on using derivative signals of the ratio spectra using double divisor. Method (II) is hybrid double divisor ratio spectra (HDDR) which depends on convolution of the double divisor ratio spectra using trigonometric Fourier functions. The developed HDDR method showed better selectivity than DDRD due to its higher resolution power. The methods have been applied for analysis of the studied drugs in their commercial tablets and the results obtained from the analysis of the market sample by the proposed methods were statistically compared with those obtained by manufacturer RP-HPLC method.

Quantitative HPLC analysis of mebeverine, mesalazine, sulphasalazine and dispersible aspirin stored in a Venalink monitored dosage system with co-prescribed medicines

An HPLC method for the quantitative analysis of mebeverine HCl, 5-aminosalicylic acid (5-ASA), sulphasalazine and dispersible aspirin has been developed and then applied to these specific medicines when stored, with other medications, in Venalink blister packs (monitored dosage system) for periods of up to 35 days. Chromatographic separation was achieved on a reversed-phase C12 column with an isocratic mixture of methanol, water and acetic acid as the mobile phase. The method was validated regarding: accuracy, precision, detection limits, quantification limits, specificity and robustness.

Validated HPLC Determination of the Two Fixed Dose Combinations (Chlordiazepoxide Hydrochloride and Mebeverine Hydrochloride; Carvedilol and Hydrochlorothiazide) in Their Tablets

Simple, rapid, and selective RP-HPLC methods with UV detection were developed for simultaneous determination of chlordiazepoxide hydrochloride and mebeverine hydrochloride (Mixture I) and carvedilol and hydrochlorothiazide (Mixture II). The chromatographic separation in both mixtures was achieved by using an RP-C8 (octylsilyl) analytical column. For Mixture I, a mobile phase composed of acetonitrile-0.05 M disodium hydrogen phosphate-triethylamine (50 + 50 + 0.2, v/v/v), pH 2.5, was used; the detector wavelength was 247 nm. For Mixture II, the mobile phase consisted of acetonitrile-0.05 M disodium hydrogen phosphate (50 + 50, v/v), pH 4.0, and the detector was set at 220 nm. Quantification of the analytes was based on measuring their peak areas. Both mixtures were resolved in less than 6 min. The reliability and analytical performance of the proposed HPLC procedures were statistically validated with respect to linearity, range, precision, accuracy, selectivity, robustness, LOD, and LOQ. The linear dynamic ranges were 2.5-150 and 2.5-500 microg/mL for chlordiazepoxide HCI and mebeverine HCI, respectively, and 0.25-200 and 0.25-150 microg/mL for carvedilol and hydrochlorothiazide, respectively. The validated HPLC methods were successfully applied to the analysis of their commercial tablet dosage forms, for which no interfering peaks were encountered from common pharmaceutical adjuvants.

Preparation and in vitro evaluation of mebeverine HCl colon-targeted drug delivery system

Mebeverine HCl is a water soluble drug commonly used to treat irritable bowel syndrome by acting directly on the smooth muscles of the colon. This work was aimed at the formulation and in vitro evaluation of a colon-targeted drug delivery system containing mebeverine HCl. Matrix tablets were prepared using ethyl cellulose (EC), Eudragit RL 100 either solely or in combination by wet granulation technique. Dissolution was carried out in 0.1 N HCl for 2 h followed by pH 6.8 phosphate buffer for eight hours. Uncoated forms released more than 5% drug in 0.1 N HCl therefore, Eudragit L100 was used as a coat. The results indicated very slow release profile. As a result, single retardant was used to prepare the matrix and coated by Eudragit L 100. The matrix containing 7% Eudragit RL 100 and 6% of binder was subjected to further studies to assess the effect of different coats (Eudragit L 100-55 and cellulose acetate phthalate) and different binders (pectin and sodium alginate) on the release profile. Eudragit L 100 and pectin were the best coating agent and binder, respectively. The final formula was stable and it can be concluded that the prepared system has the potential to deliver mebeverine HCl in vivo to the colon.

Design and formulation of mebeverine HCl semisolid formulations for intraorally administration.

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 profile 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.

Quantitative determination of mebeverine HCl by NMR chemical shift migration

Quantitative 1H NMR spectroscopic methods are not frequently reported, but current NMR instrumentation allows ready access to such data. Mebeverine HCl is an attractive molecule for NMR spectroscopy teaching purposes as it possesses a variety of simple but significant functional groups; we fully assign its 1H and 13C NMR spectra. Using mebeverine HCl, we show that concentration changes, in water as a solvent, can lead to significant changes in the 1H chemical shifts of non-exchangeable aromatic protons and to a lesser extent to aromatic methoxy protons. An important observation is that different protons migrate to different extents as the concentration of the solute is varied, and thus the 1H NMR spectra are concentration-dependent across a useful range. This chemical shift variation of selected protons was therefore analyzed and applied in the quantitative determination of mebeverine HCl in a medicine (Colofac IBS) formulated as a tablet. Self-association phenomena in water could account for these observed chemical shift migration effects as shown by determining the hydrodynamic radius from the modified form of the Stokes–Einstein equation, and thence the apparent hydrodynamic volume, V H, for mebeverine HCl in D 2O solution which is 10-fold greater than that seen in either CDCl 3 or CD 3OD.

Spectrophotometric determination of benzydamine HCl, levamisole HCl and mebeverine HCl through ion-pair complex formation with methyl orange

A simple, rapid and sensitive spectrophotometric method has been proposed for the assay of benzydamine HCl (BENZ), levamisole HCl (LEV) and mebeverine HCl (MBV) in bulk and pharmaceutical formulations. The method based on the reaction of the selected drugs with methyl orange (MO) in buffered aqueous solution at pH 3.6. The formed yellow ion-pair complexes were extracted with dichloromethane and measured quantitatively with maximum absorption at 422 nm. The analytical parameters and their effects on the reported systems are investigated. The extracts are intensely colored and very stable at room temperature. The calibration graphs were linear over the concentration range of 2–10 μg ml −1 for BENZ, 6–24 μg ml −1 for LEV and 4–14 μg ml −1 for MBV. The stoichiometry of the reaction was found to be 1:1 in all cases and the conditional stability constant ( K f) of the complexes have been calculated. The proposed method was successfully extended to pharmaceutical preparations-tablets. Excipients used as additive in commercial formulations did not interfere in the analysis. The proposed method can be recommended for quality control and routine analysis where time, cost effectiveness and high specificity of analytical technique are of great importance.

Formulation of an antispasmodic drug as a topical local anesthetic

Mebeverine hydrochloride, a spasmolytic agent on GIT smooth muscles, was reported to have a local anesthetic effect. Thus, it was desired in this study to formulate mebeverine HCl into a gel that could be used locally in the treatment of different oral painful conditions. Poloxamer 407 (P-407) was used as the base for this gel. Different additives were used to enhance drug release from the preparation while others were used to enhance the residence time for the preparation. Different formulae were characterized in terms of drug release and mucoadhesion. The formula which has shown the best compromise between the aforementioned parameters was selected for clinical evaluation in comparison to Lidocaine HCl gel ® and rheologically examined. The best drug release enhancer was cetrimide (0.005%, w/w), while hydroxypropylcellulose (0.5%, w/w) as a mucoadhesive additive has shown the best compromise between fast drug release and mucoadhesion. The gel formula (G) has shown a better pain reduction efficiency ( p = 0.0078) and longer duration ( p = 0.0313) than Lidocaine HCl gel ®. Histopathological examination has shown no change in the inflammatory cells count of rat oral mucosa. Therefore, it could be concluded that (G) is very promising as a local anesthetic preparation for the treatment of different oral painful conditions.