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Methocarbamol is a central nervous system depressant with skeletal muscle relaxant properties indicated to treatspasms. During the synthesis of methocarbamol from guaifenesin, both potential known and an unknown impurity(0.05%–0.1%), high performance liquid chromatography) were observed. The later was separated using preparativeliquid chromatography. Upon the findings of the 1H nuclear magnetic resonance, Mass, and IR spectral analysis, theunknown impurity was designated as a β-isomer of methocarbamol [1-hydroxy-3-(2-methoxy phenoxy) propan-2-ylcarbamate]. The impurity isolation, its structure elucidation, and the potential formation mechanism are discussed.
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Abstract: In the countryside, the use of halogenated anesthetics is difficult, therefore the use of injectable agents is an essential tool in anesthetic practice. This study aimed to compare two multimodal injectable anesthesia protocols and to determine the appropriate protocol to perform a medial laparotomy and embryo recovery in sheep. 16 healthy adult creole sheep were used. Animals were randomized to receive xylazine 0.2 mg/kg PC IM and ketamine 10 mg/kg PC IV (XK group), or a continuous infusion of 5% solution of xylazine (50 mg), ketamine (500 mg), and guaifenesin (500 mL) at a rate of 2.2 mL/kg/h IV (XKG group). Heart and respiratory frequency, rumen motility, and body temperature were evaluated before anesthesia, after induction, and during recovery. Induction was assessed by muscle spasms, nystagmus, and limb movement. Anesthesia was evaluated based on time, mandibular relaxation, skin sensitivity, and reflexes. Recovery was evaluated on a scale for anesthetic agent (0-10). Cardiorespiratory parameters decreased below baseline after induction of anesthesia in both groups. Between the groups, there was a significant difference in decubitus time (XK: 9.06 ± 0.73 min; XKG: 7.81 ± 0.53 min) and recovery (XK: 53.13 ± 5.3 min; XKG: 98.38 ± 5.71 min). Changes in the cardiopulmonary system were similar in both anesthetic regimens, and they were within acceptable clinical range. It is concluded that, in short surgical procedures, xylazine-ketamine anesthesia provides rapid induction, maintenance of physiological parameters within optimum limits, and rapid recovery.
Resumen: En el campo, el uso de anestésicos halogenados es difícil, por lo que el uso de agentes inyectables es una herramienta esencial de la práctica anestésica. El objetivo del presente estudio fue comparar dos protocolos de anestésicos inyectables multimodales y determinar el adecuado protocolo para realizar una laparatomía medial y recuperar embriones en ovejas. Se utilizaron 16 ovejas criollas adultas y sanas. Los animales se asignaron al azar para recibir xilazine 0,2 mg/kg PC IM y de ketamina 10 mg/kg PC IV (XK grupo) o una infusión continua de solución al 5 % de xilazine (50 mg), ketamina (500 mg) y de guaifenesina (500 mL) a una tasa de 2,2 mL/kg/h IV (grupo XKG). Frecuencia cardiaca y respiratoria, motilidad del rumen y temperatura corporal se evaluaron antes de la anestesia, después de la inducción y durante la recuperación. La inducción se evaluó según los espasmos musculares, nistagmo y movimiento de las extremidades. La anestesia se valora en función del tiempo, relajación mandibular, sensibilidad cutánea y reflejos. La recuperación se evaluó a una escala de agente anestésico (0-10). Los parámetros cardiorrespiratorios disminuyeron por debajo de los valores basales después de la inducción de anestesia en ambos grupos. Entre los grupos, hubo una diferencia significativa en el tiempo de decúbito (XK: 9,06 ± 0,73 min; XKG: 7,81 ± 0,53 min) y la recuperación (XK: 53,13 ± 5,3 min; XKG: 98,38 ± 5,71 min). Los cambios en el sistema cardiopulmonar fueron similares en ambos regímenes anestésicos, y estaban dentro de rangos clínicos aceptables. Se concluye que, en intervenciones quirúrgicas cortas, la anestesia xilacina-ketamina proporciona una rápida inducción, el mantenimiento de los parámetros fisiológicos dentro de los límites óptimos y una recuperación rápida.
Resumo: O uso de anestésicos halogenetos é difícil em campo, razão pela qual o uso de agentes injetáveis é uma ferramenta essencial da prática anestésica. O objetivo do presente estudo foi comparar dois protocolos de anestésicos injetáveis multimodais e determinar o protocolo adequado para realizar uma laparatomia medial e recuperar embriões em ovelhas. Se utilizaram 16 ovelhas domésticas adultas e saudáveis. Os animais foram designados aleatoriamente ao azar para receber 0,2 mg/kg PC IM de xilazina e 10 mg/kg PC IV de cetamina (XK grupo) ou uma infusão contínua de solução ao 5 % de xilazina (50 mg), cetamina (500 mg) e de guaifenesin (500 mL) a um índice de 2,2 mL/kg/h IV (grupo XKG). A frequência cardíaca e respiratória, motilidade do rumem e temperatura corporal foram avaliaram antes da anestesia, após a indução e durante a recuperação. A indução é avaliada se avaliou segundo os espasmos musculares, nistagmo e movimento das extremidades. A anestesia foi medida em função do tempo, relaxamento mandibular, sensibilidade cutânea e dos reflexos. A recuperação se avaliou com uma escala do agente anestésico (0-10). Os parâmetros cardiorrespiratórios diminuíram abaixo dos valores basais apósa indução do anestesia em ambos os grupos. Entre os grupos, houve uma diferença significativa no tempo de decúbito (XK: 9,06 ± 0,73 min; XKG: 7,81 ± 0,53 min) e a recuperação (XK: 53,13 ± 5,3 min; XKG: 98,38 ± 5,71 min). As mudanças no sistema cardiopulmonar foram similares em ambos os regimes anestésicos, e estavam dentro de rangos clínicos aceitáveis. Conclui-se que, em intervenções cirúrgicas curtas, a anestesia xilazina-cetamina proporciona uma rápida indução, a manutenção dos parâmetros fisiológicos dentro dos limites ótimos e uma recuperação rápida.
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OBJECTIVE:To establish a method for the dissolution determination of Pentoxyverine citrate and guaifenesin tab-lets,and to compare the difference of preparations from different manufactures. METHODS:The paddle method was used to deter-mine the dissolution,using water as medium with medium volume of 1000 mL and rotation speed of 75 r/min,sampling at 45 min. HPLC method was used to determine the accumulative dissolution of pentoxyverine citrate and guaifenesin:CAPCELL PAK C18 MGⅡ S-5 column;mobile phase of acetonitrile-triethylamine phosphoric buffer solution(pH 2.6±0.05)(33:67,V/V),flow rate of 1.0 mL/min,detection wavelength of 215 nm(pentoxyverine citrate)and 275 nm(guaifenesin),column temperature of 35 ℃,sample size of 20 μL. RESULTS:The linear range of pentoxyverine citrate and guaifenesin were 5.0916-50.9155 μg/mL(r=0.9999)and 29.9995-299.9952 μg/mL(r=0.9999),respectively. RSDs of precision,stability and reproducibility tests were all lower than 2.0%. Average recoveries were 97.90%-100.68%(RSD=0.95%,n=9)and 97.09%-101.85%(RSD=1.32%,n=9). Average accu-mulative dissolution of pentoxyverine citrate in 6 manufactures of samples were 12%,98%,66%,97%,91%,32%(n=3);those of guaifenesin were 8%,95%,68%,90%,93%,18%(n=3),respectively. CONCLUSIONS:The method is simple,ac-curate,sensitive,specific and suitable for the dissolution determination of Pentoxyverine citrate and guaifenesin tablets. The dissolu-tion of samples between different manufactures and the same manufactures different batches are quite different.
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A simple and sensitive HPLC method for simultaneous quantification of guaifenesin, ambroxol and loratidine in bulk and liquid dosage form was developed and fully validated. The separation and quantification was performed using a Kromasil C8 (250 × 4.6 mm, particles 5 μm) HPLC column. Isocratic elution mode with a flow rate of 1.2 mL/min was used, and the injection volume was 10 μL. The detector was set to a wavelength of 290 nm and the column oven was maintained at 30 °C. Orthophosphoric acid (0.1%) and acetonitrile in the ratio of 60:40 v/v was used as the mobile phase. Guaifenesin, ambroxol and loratidine were eluted with retention time of 3.045 min, 5.489 min and 13.981 min, respectively. The method was validated in accordance with ICH guidelines and the results of all the validation parameters were found to be within the acceptable limits. The calibration plots were linear over the concentration ranges from 50-150 μg/mL, 30-90 μg/mL and 5-15 μg/mL for guaifenesin, ambroxol and loratidine, respectively. Developed method was successfully applied for the quantification of the above three drugs in liquid dosage form. The excipient did not interfere with drug peaks.
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OBJECTIVE: To identify and analyze the potential impurities of methocarbamol on the basis of its synthetic route and starting materials.
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Objective:To establish an HPLC method for the determination of two components and the preservative in compound dextromethorphan hydrobromide syrups. Methods:An Agilent Zobax SB-C18 column(250 mm × 4. 6 mm,5 μm) was used with meth-anesulfonic acid solution (adding 4. 8g methanesulfonic acid and 10ml triethylamine into 750ml water,and adjusting the pH value to 3. 5 by phosphoric acid)-acetonitrile (75∶25) as the mobile phase at the flow rate of 1. 0 ml·min-1 and 280nm as the detection wave-length. Results:The calibration curve was linear within the range of 102-1 025μg·ml-1 for guaifenesin,15-619μg ·ml-1 for dextro-methorphan hydrobromide and 10-407μg·ml-1 for benzoic acid. The average recovery of guaifenesin, dextromethorphan hydrobromide and benzoic acid was 100. 0% (RSD=0. 35%), 100. 1%(RSD=0. 77%)and 100. 8%(RSD=0. 49%), respectively. Conclusion:The method is simple,rapid and accurate,and suitable for the quality assessment of compound dextromethorphan hydrobromide syrups.
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Guaifenesin and Phenylephrine possess greater water solubility but lower permeability and bioavailability. The aim of this study is to develop a microemulsion to overcome these issues. Castor oil, Oleic acid and Emu oil were selected as oil phase. Tween 80 and Span 80 were selected as surfactants.2-propanol and ethanol were selected as co-surfactants. Optimization of co-surfactant was done by taking a series of O/W microemulsions which were formulated by titration method. 32 formulations were formed initially and based on various physical parameters like clarity, Stability, density, viscosity, pH and electrical conductivity, 17 formulations were narrowed down. The particle size study was carried out by zeta analysis and the results proved that the formulations were nano sized. FTIR studies proved that there was not much interaction between the drugs in the formulation. In-vitro dissolution studies were performed for all the 17 formulations individually for both the drugs was found. The optimum formulation where sustained release for both the drugs was found to be in the combination of Oleic acid: Tween 80: Water: 2-propanol (1:3:5:9). This formulation was subjected to ex-vivo diffusion study and the permeation through the membrane was found.
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OBJECTIVE: To study influence of humidity on granule flowability, explore relationship between flowability and quality of guaifenesin sustained tablet, give a basis for industrialization. METHODS: By hygroscopicity study, CRH was measured. After 10 days in RH 33%, 60%, 75%, 84%, 92.5%, flowability of granule and quality index of tablet, such as appearance, extremum of weighty friability was measured and compared with result of 0 d. Functional relationship between micromeritics parameter and quality index of tablet was fitted. RESULTS: CRH of granule is between RH 67%-68%. When relative humidity is above RH 60%, flow-ability and quality of tablet is changed obviously. Used compressbiliity as X1, repose angle as X2, extremum of tablet weight as Y1, friability as Y2, linear relationship of them is Y1 = 0.192X1+ 0.092X2- 7.398 (r = 0.9921), Y2= 0.069X1 + 0.087X2 - 3.505 (r = 0.9881), when P < 0.001, the equations had statistical significance in the range of observation. CONCLUSION: Relative humidity of production and storage of granule should less than RH 60%. Functional relationship between micromeritics parameter of granule (compressbiliity and repose angle) and quality index of tablet (extremum of weighty friability) had statistical significance in the range of observation. Copyright 2012 by the Chinese Pharmaceutical Association.
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OBJECTIVE: To establish an RP-HPLC method for the determination of aminophylline,eyhedrine and guaifenesin in Xiaoer kechuan oral solution.METHODS: The determination was performed on Hypersil ODS column(150 mm?4.6 mm,5 ?m).The mobile phase consisted of acetonitrile-0.015 mol?L-1 KH2PO4(0.1% triethylamine and pH value of phosphoric acid adjusted to 2.7)(10 ∶ 90) with a flow rate of 1.6 mL?min-1 and detection wavelength of 254 nm and 209 nm.RESULTS: The linear ranges were 356.4～712.8 ?g?mL-1 for aminophylline,88～176 ?g?mL-1 for eyhedrine and 106～212 ?g?mL-1 for guaifenesin(r=0.999 9).The average recovery rates were 101.0%(RSD=0.73%,n=9),99.7%(RSD=1.00%,n=9),98.3%(RSD=0.44%,n=9),respectively.CONCLUSIONS:The method is simple and accurate for quality control of Xiaoer kechuan oral solution.
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OBJECTIVE:To investigate the internal quality of 31 batches of Compound Glycyrrhiza oral solutions from different manufacturers.METHODS:The contents of Morphine and Guaifenesin in Compound Glycyrrhiza oral solutions were determined by HPLC,and the pH value of the solution was detected as well.RESULTS:Of the total 31 batches of samples,13 was unqualified in Morphine content,1 was unqualified in Guaifenesin content,and 1 was unqualified in pH value.CONCLUSION:The manufacturers should strictly obey the standards recorded in China Pharmacopoeia in respect of quality control to ensure the safety and efficacy of clinical medication.
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OBJECTIVE:To evaluate the clinical efficacy and safety of guaifenesin,pseudoephedrine hydrochloride- codeine phosphate oral solution in relieving cough,eliminating phlegm,relieving nasal stuffiness and other cold symptoms. METHODS:A total of 240 patients with cold symptoms(120 cases in trial group and another 120 cases in control group) were enrolled in our multicenter,randomized,double-blinded and parallel controlled study and treated with guaifenesin-pseudoephedrine hydrochloride-codeine phosphate oral solutionI or compound codeine phosphate liquor 10mL tid for(5?2)d.RESULTS:227(112 in trial group and 115 in control group) were the valid cases with completed trial.Compared with pre-treatment,both of the 2 groups had a significant improvement in symptoms including cough,expectoration and nasal stuffiness after treatment(P
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OBJECTIVE:To evaluate the cough-relieving and sputum-eliminating efficacy and safety of Guaifenesin Pseudoephedrine Hydrochloride-Codeine Phosphate Oral Solution.METHODS:By a randomized control study,a total of 60 patients characterized by nonproductive cough andlittle sputum were randomly assigned to receive Guaifenesin Pseudoephedrine Hydrochloride-Codeine Phosphate Oral Solution(Trial Group)or Ambroxol Hydrochloride Oral Solution(Control Group)l0 mL tid for 5～7 d.RESULTS:Both groups had a significant improvement in symptoms including cough and expectoration after treatment(P0.05).CONCLUSION:Guaifenesin Pseudoephedrine Hydrochloride-Codeine Phosphate Oral Solution is more effective in relieving cough than Ambroxol Oral Solution,and it has certain effect in eliminating phlegm.In addition,it is safe and has little adverse reaction.
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OBJECTIVE: To establish xiaochuan oral oral solution quality control method.METHODS: Three kinds of main components' contents in xiaochuan oral solution were determined by HPLC.RESULTS: The prepared oral solution was brown liquid,with identification and tests all up to the standards specified in Chinese Pharmacopeia(2005 edition).The linear ranges of guaifenesin,ephedrine hydrochloride,and aminophylline(theophylline) were 7～13 ?g?mL-1(r=0.999 9),4.55～8.45 ?g?mL-1(r=0.999 8),and 10.64～19.76 ?g?mL-1(r=0.999 9),respectively,with the average recoveries at 99.35%(RSD=0.97%),100.40%(RSD=1.02%),and 100.57%(RSD=1.08%),respectively.CONCLUSION: The established quality control method could be used for quality control of it.