Chlorpheniramine Maleate Tablets Research Articles

Evaluation of modified Cenchrus americanus starch as disintegrant in formulation of chlorpheniramine maleate tablets

The aim of this research was to investigate the disintegrant properties of modified Cenchrus americanus starch (MCS) in chlorpheniramine maleate tablets formulation. The matured seeds of C. americanus were steeped in 4 L of 0.25 % w/v sodium hydroxide at 5 °C for 24h, washed, soaked in distilled water (30 ± 2 °C) for 24 h, and wet milled. The slurry was washed with distilled water through a 200 mesh screen, and the filtrate left undisturbed for 18 h. The top layer sediment was scrapped off, and the starch re-suspended with water. Further washing and sedimentation was done until the top layer of the starch became white. The starch was dried at 40 °C, defatted using Petroleum-Ether, air dried, sized (125µm) and characterized using standard methods. The MCS was used at 5, 10 and 15 % w/w as disintegrant in the formulation of chlorpheniramine maleate granules using the wet granulation method. Primogel at similar concentrations was used as comparing standard. Characterization of the granules for densities and flowability were done. Chlorpheniramine maleate tablets compressed from these granules were evaluated for uniformity of weight, hardness, disintegration time, assay and dissolution. Results showed poor flow properties for the MCS powder while the chlorpheniramine granules exhibited good flow. The tablets showed minimal variation in weight, good hardness (6.06±0.10 - 8.07±1.31 kgF), disintegration time (< 7 min), friability (< 1 %), and dissolution of more than 80 % within 30 min. The MCS compared favourably with primogel as disintegrant in chlorpheniramine tablets formulation and met with British Pharmacopoeia set limits.

Evaluation of modified Cenchrus americanus starch as disintegrant in formulation of chlorpheniramine maleate tablets

Evaluation of modified Cenchrus americanus starch as disintegrant in formulation of chlorpheniramine maleate tablets

Non-Destructive Analysis of Chlorpheniramine Maleate Tablets and Granules by Chemometrics-Assisted Attenuated Total Reflectance Infrared Spectroscopy.

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

Application of microcrystalline cellulose obtained from Gossypium herbaceum in direct compression of chlorpheniramine maleate tablets

The flow, tableting and in vitro release properties of directly compressed chlorpheniramine maleate (CPM) tablets containing fluid bed dried and lyophilized microcrystalline cellulose (MCC) obtained from Gossypium herbaceum (GH) were investigated. Delignification of dried GH linters was done through the soda process to obtain alpha cellulose which was hydrolyzed with 2.0 N hydrochloric acid to get MCC. The MCC was washed with water until neutral. Drying was done by either fluid bed method or lyophilization to obtain MCC-GossF and MCC-GossL respectively. Chlorpheniramine tablets containing 20, 30 and 40% of the MCCs were prepared by direct compression method. Avicel PH102 (AVH-102) served as comparing standard. Using standard methods, evaluation of the powders and the tablets was done. The evaluated parameters of the powders and tablets conformed to the British Pharmacopoeia specifications. The CPM tablets containing MCC-GossF (coded CGF) had better flow but were not mechanically as strong as those containing MCC-GossL (coded CGL). The hardness and disintegration times of the tablets were in the order of CGF < CGL and the friability was in the order of CGF > CGL. Similar parameters of DCL compared well with CPM tablets containing AVH-102 (coded DAV). The MCC obtained from GH had dilution potential up to 40% except in CGF-4 tablets. The in vitro dissolution showed > 80% CPM release from all the batches within 30 min. The release kinetics were of mixed order while the mechanism of drug release was Fickian. The MCCs served as good directly compressible binder for chlorpheniramine maleate.

Application of microcrystalline cellulose obtained from Gossypium herbaceum in direct compression of chlorpheniramine maleate tablets

Application of microcrystalline cellulose obtained from Gossypium herbaceum in direct compression of chlorpheniramine maleate tablets

Validation of an UV-Visible spectrophotometry assay method for the determination of chlorpheniramine maleate tablets without prior extraction

Methods proposed by pharmacopeias to check the quality of chlorpheniramine maleate tablets are multi steps methods which involve extraction and present issues with repeatability. An alternative method is proposed with a sensitive, reliable, simple and rapid UV-VISIBLE spectrophotometry method developed for the determination without extraction of chlorpheniramine maleate in tablets. The method was validated using the accuracy profile approach with an accuracy ranging from 99.70 to 100.46%. Analysis was done using 0.25 mol/L sulfuric acid, distilled water, and raw material in a room at 23 °C for 25 to 30 minutes. Chlorpheniramine maleate concentration varied from 0.018 to 0.03 mg/mL. The method was found to be specific with the appearance of the corresponding maxima at 265 nm and a correlation coefficient (R2 ) of 0.9993. Limits of detection and quantification were respectively 1.39 × 10-4and 2.26 × 10-3 mg/mL. The tolerance limits for the different concentration levels (75, 100 and 125%) were respectively: 88.37; 92.74 and91.62% for lower limits and 111.03; 108.17 and 108.02% for upper limits. It was observed that the tolerance limits were within the limits of acceptability set at 20%. Consequently, the method was declared valid and reliable for routine analysis of chlorpheniramine maleate in tablets containing chlorphenamine as active principle.Keywords : Chlorpheniramine maleate, tablets, accuracy profile, assay method without extraction, validation

Determination and stability testing method of chlorpheniramine maleate in the presence of tartrazine using HPLC

The single-component CPM tablet mostly used sodium tartrazine as the yellow coloring agent. Sodium tartrazine is soluble in solvents used to extract CPM from tablet and suspected interference CPM determination especially after forced degradation for stability indication testing of CPM tablets. This study aimed to develop a selective, accurate and precise method for determination and stability testing of chlorpheniramine maleate (CPM) in the presence of tartrazine in the tablet. A µBondapak ® C18 column (3.9 x 300 mm, 10 µm) with diode array detector was used for separation. The mobile phase was a mixture of methanol and 0.2% triethylamine (90:10) with a flow rate of 2 mL/minutes. The validated HPLC method was used for CPM determination in tablet samples that had been forced degraded using dry heat at 105 o C, UV radiation of 254 nm, hydrolysis with 1N NaOH, 1N HCl and oxidation using 5% H 2 O 2 . The HPLC chromatogram showed that CPM split into chlorpheniramine (CP) and maleic acid (MA). Resolution (Rs) among CP and the other analytes especially with the products resulting from the forced degradation by heat, UV radiation, HCl, and H 2 O 2 were good. The CPM hydrolysis using NaOH caused the CP not completely separated from the degradation product due to tailing or overlapping peaks. The proposed HPLC method was valid for the determination of CPM in tablets containing tartrazine. Even though the stability-indicating method was inadequate especially for the result of the CPM hydrolysis process using NaOH.

Process quality control of the manufacturing of Chinese Materia Medica by process analysis technology

Process quality control is essential for the manufacturing of Chinese Materia Medica. Non-destructive monitoring is still a challenge for the quality control of Chinese Materia Medica manufacturing. As the commonly used non-destructive process analysis technology, near infrared spectroscopy, near infrared chemical imaging, and laser-induced breakdown spectroscopy have been applied to the quality control of Chinese Materia Medica manufacturing. The characteristic near infrared bands of 29 natural chemical components have been assigned. Ten spectral pre-processing methods and five variable selection methods have been optimized, respectively. Given the interrelationship among modeling parameters, a system modeling concept was put forward to establish a global model. Accuracy Profile was further proposed as the validation method of models. In addition, the homogeneity of chlorpheniramine maleate tablets from six brands was successfully visualized by near infrared-chemical imaging. As and Hg variation in An-Gong-Niu-Huang Wan have been rapidly monitored by laser-induced breakdown spectroscopy. A systematic modeling method (model establishment, evaluation, and validation) and the non-destructive technology of homogeneity visualization and toxic element detection have been developed for quality control of Chinese Materia Medica manufacturing, which is shown in Figure 1 of the article. These achievements have greatly promoted the research and application of process analysis technology in Chinese Materia Medica manufacturing, laying a solid foundation for the development of intelligent Chinese pharmaceutical industry.

Direct Compression and in vitro Release of Chlorpheniramine Maleate from Tablets Containing Fluid Bed Dried and Lyophilized Microcrystalline Cellulose Derived from Cocos nucifera

Aims: To investigate the mechanical and in vitro release properties of chlorpheniramine maleate (CM) tablets formulated with fluid bed dried and lyophilized microcrystalline cellulose (MCC) derived from the fruit husk of Cocos nucifera (CN).
 Study Design: Experimental design.
 Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka from January, 2015 to December, 2016.
 Methods: Chips of matured (CN) fruit husk were de-lignified by soda treatment methods to obtain alpha cellulose which was hydrolyzed with mineral acid (Hydrochloric acid) to obtain CN-MCC. A portion of the damp CN-MCC was fluid bed dried at 60°C for 2 h (coded MCCF-Cocos) and the remaining CN-MCC was lyophilized at -45°C for 3 h (coded MCCL-Cocos). The MCC powders were blended with 20, 30 and 40% w/w CM and directly compressed at 9.81 mega Pascal (mPa). The CM tablets containing MCCF-Cocos (coded CM-CF) and MCCL-Cocos (coded CM-CL) were evaluated using standard methods.
 Results: Both batches had tablets with minimal weight variation; CM-CL tablets were mechanically stronger (P = .037) and less friable than CM-CF tablets. CM-CL tablets took a longer time to disintegrate than CM-CF tablets. Comparatively, CM tablets containing AVC-102 (coded CM-AV) were mechanically stronger, less friable and had a longer disintegration time than CM-CL and CM-CF tablets. The dilution potential of CM-AV was greater than CM-CL and CM-CF tablets. CM release was faster in CM-CF. There was more than 80 % release of CM from CM-CF, CM-CL and CM-AV tablets within 30 min. Although CM-CL tablets were mechanically stronger than CM-CF, the data for all batches of the tablets obtained fell within the British Pharmacopoeia set limits for uncoated tablets.
 Conclusion: Chlorpheniramine maleate tablets containing fluid bed dried and lyophilized microcrystalline cellulose obtained from C. nucifera had good mechanical and in vitro release properties.

The effect of binder concentration and dry mixing time on granules, tablet characteristics and content uniformity of low dose drug in high shear wet granulation

High shear mixers are classically used for wet granulation because they provide granules with a high density and a high strength in a short granulation time. In this study, the high shear wet granulation process was employed using chlorpheniramine maleate as a model drug, since it represents an example of low dose drug employing 32 randomized full factorial design and optimized in terms of different properties using Response Surface Methodology (RSM) approach. The effect of binder concentration (X1) and dry mixing time (X2) at three levels on the granules and tablet properties was studied. Chlorpheniramine maleate tablets were prepared from the produced granules to evaluate the impact of dry mixing time and the binder concentration on the produced granules and tablet properties as well as tablet content uniformity. The results show that both evaluated variables had an impact on the produced granules and tablets as well as tablet content uniformity. The high shear mixer is found to be an efficient mixer for dry blending prior to the wet massing of a low dose drug formulation when impeller speed and chopper speed were carefully selected. The results of RSM optimization indicated that formulation containing 4.46% Binder concentration at a dry mixing time of 5 min, gave the most desirable properties for the produced granules and tablets. The observed results of the optimized formula were: Carr's Index:12.72%, Hausner Rati:1.14, angle of repose: 35.18°, hardness: 5.5 Kp, friability: 0.42%, disintegration time: 60 s, average of content uniformity: 112.18% with RSD: 4.6%, and d (0.9): 982 μ which are in consistence with the predicted results, having low values of standard error.

Stabilitty indicating method development and validation for the quantification of chlorphenamine maleate related subtances using hplc technique

Chlorpheniramine Maleate (CPM) is an antihistamine used for the treatment of allergic disorders and common cold since, the method for determination of CPM related substances in pharmaceutical products is not described in current pharmacopoeias; the aim of this work was to develop and validate a precise, accurate and robust method. Separation was achieve on a RP C-18 column (250 x 4.6 mm, 5 µm particle size), column temperature kept at 40°C. The mobile phase content A: 80 volumes buffer solution (pH 3.00) and Mobile phase B 20 volumes of Acetonitrile, and UV detection wavelength at 225nm. The method was validated by ICH guidelines and validation studies proved that the method is stability indicating and used for determination of related substances of CPM tablets.

Rapid Discrimination of Chlorpheniramine Maleate and Assessment of Its Surface Content Uniformity in a Pharmaceutical Formulation by NIR-CI Coupled with Statistical Measurement

This study demonstrated that near infrared chemical imaging (NIR-CI) was a rapid and nondestructive technique for discrimination of chlorpheniramine maleate (CPM) and assessment of its surface content uniformity (SCU) in a pharmaceutical formulation. The characteristic wavenumber method was used for discriminating CPM distribution on the tablet surface. To assess the surface content uniformity of CPM, binary image and statistical measurement were proposed. Furthermore, high-performance liquid chromatography (HPLC) was used as reference method for accurately determining volume content of CPM in the sample. Moreover, HPLC was performed to assess volume content uniformity (VCU) of CPM in whole region and part region of the tablets. The NIR-CI result showed that the spatial distribution of CPM was heterogeneous on the tablet surface. Through the comparison of content uniformity of CPM determined by NIR-CI and HPLC, respectively, it demonstrated that a high degree of VCU did not imply a high degree of SCU of the samples. These results indicate that HPLC method is not suitable for testing SCU, and this has been verified by NIR-CI. This study proves the feasibility of NIR-CI for rapid discrimination of CPM and assessment of its SCU, which is helpful for the quality control of commercial CPM tablets.

In Vitro Drug Release Studies of Metronidazole Topical Formulations Through Cellulose Membrane

The present work reports on the mucoadhesive and mechanical properties of the water-soluble gum obtained from Entandophragma angolense when incorporated in oral tablets. Flat-faced chlorpheniramine maleate tablets containing the gum were formulated. The potential for chemical interaction between the gum and drug was evaluated by UV spectroscopy. The mucoadhesive, mechanical and release properties of the tablets were evaluated. The rates of water uptake and erosion were determined for the tablets. The detachment time for the tablets increased from 78.71 ± 0.43 to 84.28 ± 0.75 min, and from 33.57 ± 0.48 to 79.27 ± 4.7 min as the amount of gum per tablet was increased from 2.5 to 10.0% w/w, respectively. The drug release time for all tablets increased with binder concentration. UV spectroscopy suggested the absence of chemical interactions. The novel natural gum compared favourably with established mucoadhesive polymers namely hydroxypropylcellulose and gelatin. The mucoadhesive, mechanical and release properties were a function of polymer concentration. Key words : Entandophragma angolense, chlorpheniramine maleate tablets, mucoadhesion, mechanical properties

Influence of processing parameters and formulation factors on the drug release from tablets powder-coated with Eudragit ® L 100-55

The aim of this study was to develop a dry powder coating process for chlorpheniramine maleate (CPM) tablets using Eudragit ® L 100-55 as the delayed release polymer. Powder coating, a water and organic solvent-free process, was investigated as a method to prevent the migration of an ionizable, highly water soluble model drug into the polymeric film during the coating process. Eudragit ® L 100-55 was pre-plasticized with triethyl citrate (TEC) using hot-melt extrusion at levels of 20%, 30%, and 40%, based on the polymer weight. The extrudate was subsequently cut into pellets and cryogenically ground into a fine powder. Talc was incorporated into the coating powder as an anti-tack agent. PEG 3350 was used as a primer for the powder coating of tablets with pre-plasticized Eudragit ® L 100-55. The addition of polyethylene glycol 3350 (PEG 3350) to the pre-plasticized Eudragit ® L 100-55 was necessary to enhance the adhesion of the coating powder to the tablet cores. PEG 3350 also improved film formation and coalescence of the polymeric particles due to its plasticization effects on the acrylic polymer. For comparison, theophylline tablets were also coated with pre-plasticized Eudragit ® L 100-55. Theophylline was selected as a less water soluble model drug. The powder coating process was performed in a modified laboratory scale spheronizer. The drug release rate was dependent both on TEC content and the coating level. The stability of the powder-coated CPM tablets was confirmed at 25 °C/60% RH over a storage time of 12 weeks.

Influence of a lipophilic thermal lubricant on the processing conditions and drug release properties of chlorpheniramine maleate tablets prepared by hot-melt extrusion

The objective of this study was to investigate the influence of a lipophilic thermal lubricant on the processing conditions and properties of chlorpheniramine maleate (CPM) tablets prepared by hot-melt extrusion. CPM tablets containing Eudragit RS PO, triethyl citrate (TEC) and glyceryl monostearate (GMS) were prepared by hot-melt extrusion. An investigation of the thermal stability of CPM, Eudragit RS PO, TEC and GMS as determined by thermogravimetric analysis (TGA) showed that CPM and the excipient components of the extruded tablets were stable at the thermal processing temperatures. The incorporation of either TEC or GMS into the powder blend decreased the drive AMPS and the torque values during the hot-melt extrusion process. The glass transition temperature of Eudragit RS PO and the melting point of GMS were determined using differential scanning calorimetry (DSC) from a physical mixture, and the results demonstrated that these two materials were not miscible in the molten state. These results were in agreement with findings from scanning electron microscopy (SEM) and X-ray diffraction studies. An increase in the thermal lubricant (GMS) level in the Eudragit RS PO system resulted in an increase in the rate of drug release from the tablets. Both TEC and GMS facilitated thermal processing. While TEC lowered both the glass transition temperature and the melt viscosity of the acrylic polymer, GMS only decreased the melt viscosity of the acrylic polymer and had no effect on the glass transition temperature.

Solid-state plasticization of an acrylic polymer with chlorpheniramine maleate and triethyl citrate

The influence of in situ plasticization of chlorpheniramine maleate (CPM) on Eudragit® RS PO from hot-melt extruded matrix tablets, and from compressed granules prepared by thermal processing was investigated. CPM was studied as both a model drug substance and as a solid-state plasticizer for the acrylic polymer. Triethyl citrate (TEC) was incorporated into the polymer blend as a liquid plasticizer for the polymer. The influence of TEC and CPM concentration on the dissolution properties of CPM tablets was investigated. The glass transition temperature ( T g) of the samples was determined by modulated differential scanning calorimetry (MDSC). The morphologies of the granules formed by hot-melt extrusion and hot-melt granulation processes were investigated by scanning electron microscopy. The addition of 12% TEC to the polymer reduced the T g by 32.5 °C, while the reduction in the T g for the same level of CPM was 16.4 °C. The effect of TEC levels on drug release was dependent on the tablet preparation method. At high TEC levels, the release rate of CPM decreased in tablets prepared by direct compression and tablets made from compressed granules that had been prepared by high shear hot-melt granulation. However, the CPM release rate increased from hot-melt extruded tablets with increasing blends of plasticizer in the extruded tablets. An increase in the CPM content in the tablets resulted in an increase in the drug release rate. During high shear hot-melt granulation, the model drug adhered to the polymer to form a porous discontinuous structure. Following hot-melt extrusion, the drug was distributed at a molecular level in the continuous polymeric structure. The influence of both CPM and TEC levels on the drug release rate from these polymeric drug delivery systems was shown to be a function of whether the granules or tablets were formed by either hot-melt granulation or hot-melt extrusion, as well as the plasticization effects of both TEC and CPM on the acrylic polymer.

Influence of Thermal Processing on the Properties of Chlorpheniramine Maleate Tablets Containing an Acrylic Polymer

The purpose of this investigation was to determine the effects of thermal processing and post-processing thermal treatment on the release properties of chlorpheniramine maleate (CPM) from matrix tablets containing Eudragit® RS PO and triethyl citrate (TEC). CPM tablets containing Eudragit RS PO with and without TEC were prepared by direct compression (DC), high shear hot-melt granulation (HMG), and hot-melt extrusion (HME). X-ray diffraction patterns showed that the CPM was distributed in Eudragit RS PO at the molecular level following HME. The thermogravimetry analysis (TGA) profiles of CPM, Eudragit RS PO, and TEC demonstrated that these materials were thermally stable during both the high shear HMG and HME processes. The tablets were subjected to post-processing thermal treatment by storing the tablets at 60°C in open containers for 24 hr. Tablets prepared by DC showed the highest drug release rate constant of 36.2%hr−1/2. When 4% TEC was incorporated into the formulation, the drug release rate constant for the directly compressed tablets decreased to 32.4%hr−1/2. After high shear HMG and HME of the powder blend containing 4% TEC, the drug release rate constant decreased to 30.8 and 13.8%hr−1/2 for the respective processes. The drug release rate constants for all tablets decreased following post-processing thermal treatment. The reduction in release rate was due to an increase in the intermolecular binding and entanglement between drug molecules and polymer molecules that occurred during thermal processing. Post-processing thermal treatment of the hot-melt extrudates had a minimal effect on the drug release rate since the HME process enhanced the drug and polymer entanglement to a greater extent.

Comparative Study of Aqueous and Organic Enteric Coatings of Chlorpheniramine Maleate Tablets

AbstractTwo acrylic polymers (Eudragit® L 12.5 P and L 30 D) and a cellulosic polymer (cellulose acetate trimellitate, CAT) in organic and aqueous formulations were used in order to obtain an enteric coating on tablets containing clorpheniramine maleate as a water-soluble model drug. The coating of tablets was executed in a coating pan in similar conditions for each kind of solvent. The coated tablets were tested according to the delayed-release test of USP 23 (Method A). In our experimental conditions different amounts of polymers were needed to obtain an enteric coating. The lowest amount was in the case of Eudragit L 30 D (aqueous), after which appeared Eudragit L 12.5 P (organic), CAT (organic), and finally, CAT (aqueous) as the polymer that needed to be of the highest amount. During the dissolution test differences in the size and aspect of the tablets were observed according to the polymers. Acrylic polymers did not show changes in size and aspect, but CAT polymers showed a notable increase in size....

Chitosan as a tablet binder

AbstractChitosan was evaluated as a binder for chlorpheniramine maleate tablets in comparison with other cellulose binders such as sodium carboxymethylcellulose, hydroxypropylmethylcellulose and methylcellulose. The effects of binder concentration on the mechanical properties of granules and tablets as well as on disintegration time and dissolution profiles were studied. Results showed that granules prepared with methylcellulose had lowest percentage of fines and friability. Chitosan tablets showed best dissolution profiles. The rank order correlation for binder efficiency was: hydroxypropylmethylcellulose > chitosan > methylcellulose > sodium carboxymethylcellulose.

Preparation of ethyl cellulose pseudolatex and studies on suitability of it as a binder for granulation

AbstractEthyl cellulose pseudolatices were prepared by an emulsion-solvent evaporation technique, which consisted of dissolving the polymer in a blend of benzene and ethyl alcohol, followed by the addition of adjuvants. The organic, solvents were removed from the emulsion using vacuum distillation. Physical evaluation of the dispersions and the cast films was carried out.On the basis of characteristics of cast films selected formulations were fused as granulating agents for preparing chlorpheniramine maleate tablets. Good correlation was observed between total solid in the granulating dispersion and the drug release. The possible mechanisms for the drug release from the tablets are suggested.