Chiral Separation of Chlorpheniramine by Capillary Electrophoresis *L

Aim To study the chiral separation of chlorpheniramine(Chp) by using a mixture of β CD and glutamate β CD as the chiral additive in CE. Methods Mixture of β cyclodextrin and glutamate β cyclodextrin was used as a chiral selector to the separation of chlorpheniramine. The effects of the concentrations of β cyclodextrin and glutamate β cyclodextrin, the voltage and the pH of buffers on the separation of chlorpheniramine were studied. Results The chiral recognization of the mixed chiral selector was better than that of a single selector. At pH below 4, the pH of buffers did not affect the separation and the separation of chlorpheniramine had good reproducibility. Conclusion Using a mixture of β CD and Glu β CD as chiral selector is useful for the enantioseparation of Chp in CE.

Near-infrared chemical imaging for quantitative analysis of chlorpheniramine maleate and distribution homogeneity assessment in pharmaceutical formulations

Near infrared chemical imaging(NIR-CI)combines conventional near infrared(NIR)spectros-copy with chemical imaging,thus provides spectral and spatial information simult aneously.It could be utilized to visualize the spatial distribution of the ingredients in a sample.The data acquired using NIR CI instrument are hyperspectral data cube(hypercube)containing thousands of spectra.Chemometric methodologies are necessary to transform spectral information into chemical information.Partial least squares(PLS)method was performed to extract chemical information of chlorpheniramine maleate in pharmaceutical formulations.A series of samples which consisted of different CPM concentrations(w/w)were compressed and hypercube data were measured.The spectra extracted from the hypercube were used to establish the PLS model of CPM.The results of the model were R^(2)_(val)0.981,RMSEC 0.384%,RMSECV 0.483%,RMSEP 0.631%,indicating that this model was reliable.

Synergistic action of famotidine and chlorpheniramine on acetic acid-induced chronic gastric ulcer in rats

AIM： To assess the synergistic action of famotidine （FMD） and chlorpheniramine （CPA） on acetic acid-induced chronic gastric ulcer in rats. METHODS： Chronic gastric lesions were induced in male Sprague-Dawley （SD） rats by serosal application of the acetic acid. Forty SD rats were randomly divided into blank group （n = 8）, control group （n = 8）, FMD group （n = 8）, CPA group （n = 8）, and FMD＋CPA group （n = 8）. Each group was given intraperitoneally （i.p.） 0.5 mL/100 g distilled water, 9 g/L NaCl saline, 4 mg/kg FMD, 10 mg/kg CPA, 4 mg/kg FMD＋10 mg/kg CPA, respectively, daily for 10 d, On d 10, ulcer area was determined by planimetry, The level of myeloperoxidase （MPO） in the liver homogenation was determined by biochemical methods and the plasma levels of 6-ketoprostaglandin F1 alpha （6-keto-PGFla）and IL-8 were determined by radioimmunoassay. RESULTS： The synergistic effects of FMD＋CPA group on the lesion, IL-8, 6-keto-PGFla and MPO were confirmed. The effect of FMD＋CPA group was significantly different as compared to the control and FMD groups. The lesion （mm2） was reduced from 40.18±2.6 in control group to 6.83±2.97 in PMD＋CPA group, P〈0.01, and from 32.9 ±3.27 in FMD group to 6.83±2.97 in PMD＋CPA group, P〈0.01. The plasma levels of IL-8 decreased from 0.69± 0.11 ng/L in control group to 0.4±0.04 ng/L in PMD＋CPA group, P〈0.01, and from 0.51±0.08 ng/L in FMD group to 0.4±0.04 ng/L in PMD＋CPA group, P〈0.05. The level of 6-keto-PGF1, increased from 7.55±1.65 ng/L in control group to 16.62±0.97 ng/L in PMD＋CPA group,P〈0.01, and from 13.15±1.48 ng/L in FMD group to 16.62±0.97 ng/L in PMD＋CPA group,P〈0.05. The levels of MPO in the liver homogenate decreased from 9.12±2.05 u/Lin control group to 4.33±0.95 u/L in PMD＋CPA group, P〈0.01, and from 8.3±1.29 u/L in FMD group to 4.33±0.95 u/L, P〈0.01. CONCLUSION： The synergistic action of FMD and CPA on acetic acid-induced chronic gastric ulcer in rats decreases the incidence of ulcer and also enhances the healing of ulcer.

Inhibitory Effects of Chlorpheniramine and Astemizolum on Contraction of Isolated Rat and Rabbit Uteri Induced by Oxytocin and PGF_(2α)

The contraction of isolated rat and rabbit uteri induced by oxytocin and PGF2α was markedly inhibited by chlorpheniramine (Chl) and astemizolum (Ast) , both of which also decreased the resting tension of uteri, and their spontaneous contraction. The inhibitory effects of both drugs were dose-dependent. At high concentrations , Chl 7. 4 × 10-4 mol/L and Ast 10-4 mol/L could counteract the contraction of the uteri induced by Oxy and PGF2α, and their spontaneous contraction as well. They decreased the resting tension to the lower level. The mechanism of their non-special relaxed action on uteri could not be completely explained only by their H1-receptor blocking action. Whether they act by blocking calcium channel or by inhibiting calmodulin (CaM) remains to be further explored.

Characterization and Biodegradation Studies for Interpenetrating Polymeric Network (IPN) of Chitosan-Amino Acid Beads

The paper describes the synthesis of pH sensitive interpenetrating polymeric network (IPN) beads composed of chi-tosan, glycine, glutamic acid, cross linked with glutaraldehyde and their use for controlled drug release. The drug was loaded into beads by varying their composition such as, amount of crosslinker glutaraldehyde, ratio of chitosan, glycine and glutamic acid. The beads were characterized by fourier transform infrared (FTIR) spectroscopy to confirm the cross linking reaction and drug interaction with crosslinked polymer in beads, Scanning Electron Microscopy (SEM) to understand the surface morphology and Differential scanning calorimetry (DSC) to find out the thermal stability of beads. X-Ray Diffraction (XRD) investigation was carried out to determine the crystalline nature of drug after loading into chitosan-glycine-glutamic acid IPN beads. Results indicated amorphous dispersion of chlorpheniramine maleate (CPM) in the polymeric matrix. The swelling behavior of the beads at different time intervals was monitored in solutions of pH 2.0 and pH 7.4. The release experiments were performed in solutions of pH 2.0 and pH 7.4 at 37oC using chlorpheniramine maleate (CPM) as a model drug. The swelling behavior and release of drug were observed to be dependent on pH, degree of cross linking and their composition. The results indicate that the cross linked IPN beads of chitosan-glycine-glutamic acid might be useful as a vehicle for controlled release of drug. The kinetics of drug release from beads was best fitted by Higuchi’s model in which release rate is largely governed by rate of diffusion through the matrix.

Square Wave Voltammetric Behavior of N,N-DiethyI-P-Nitroso Aniline an Indirect Method for Determination of Chlorpheniramin Maleate, Application of Pharmaceutical Formulations

The electrochemical behavior of N,N-diethyl-p-nitroso aniline was carried out using SWV （square wave voltammetric） at HMDE. A well defined reduction peak was observed at （-0.214） volt versus the reference electrode （Ag/AgC1/sat. KCI）, calibration curve was constructed in phosphate buffer （pH = 7.0）, the relationship is linear within the concentration range 1.283 × 10.5 M - 3.66 × 10.5 M with the correlation （R = 0.9923）. The serial addition ofCPM （chlorpheniramine maleate） leads to the decrease in the reduction current peak （Ip）, quantitatively, the plot of Alp （Ip - Ip） where, Ip： Peak current of N, N-diethyl-p-nitroso aniline alone, lp： peak current of N,N-diethyl-p-nitroso aniline in the presence of CPM, versus concentration is linear within the concentration range 0.984 × 10-6 M - 9.756 × 10-6 M, the correlation coefficient was 0.9954. The method was successfully applied to determine CPM in different types of pharmaceutical formulations, and compared with standard method from British Pharmacopeia [1].