Double-blinded, Controlled, Randomized Study of Dihydrocodeine Tartrate vs Codeine Phosphate in Treating Cancer Pain

To compare the effects and adverse reactions of dihydrocodeine tartrate andcodeine phosphate in treating moderate cancer pain. Methods: Sixty-nine cases of cancer patientswith moderate pain were treated with dihydrocodeine tartrate or codeine phosphate respectively bydouble-blind, controlled randomized methods and the effects and adverse reactions were observed.Results: After administration of dihydrocodeine tartrate or codeine phosphate, in treatment group orcontrol group, the total effective rate was 86.6% and 93.6%, and common adverse symptoms includedconstipation (31.3%/12.9%), nausea (18.8%/19.7%), gastric trouble (18.8%/19.7%), skin pruritus(12.5%/10%), vomit (9.3% and 6.5%) with the difference being not significant. Conclusion: Theeffects of dihydrocodeine tartrate in treating moderate cancer pain are similar to codeinephosphate. Both them can be used to treat moderate cancer pain.

Determination of ephedrine and codeine in human urine by cation-selective exhaustive injection and sweeping micellar electrokinetic chromatography

A sensitive method for the determination of ephedrine and codeine in human urine by capillary electrophoresis （CE） was described. In order to improve the sensitivity, two online concentration techniques including cation-selective exhaustive injection （CSEI） and sweeping micellar electrokinetic chromatography （sweeping-MEKC） were used. Under the optimum conditions, the detection limits （S/N = 3） were 0.10 μg/L for ephedrine and 0.80 μg/L for codeine. This method was successfully applied to real urine sample analysis.

Comparison of the Efficacy of Oral Oxycodone and Oral Codeine in the Treatment of Post-Craniotomy Pain—A Randomized, Double-Blind Trial

Background: Post-craniotomy pain has been reported to be moderate to severe. Management of post-craniotomy pain is often inadequate, yet limited by the side effects of opioids. We aim to find out the efficacy of oral oxycodone as compared to oral codeine for the treatment of post-craniotomy pain in our institution. Methods: A randomized, double-blinded controlled trial was used to evaluate the efficacy of oral oxycodone versus oral codeine. 40 patients were randomized to the control group of codeine (n = 20) or the experimental group receiving oxycodone (n = 20) in addition to regular oral paracetamol for both groups of patients. Results: There was no difference in the visual analogue scale scores at 24 hours (2.78 versus 1.85, p = 0.11) or side effects in the oxycodone group compared with the codeine group. Conclusions: Oral oxycodone had similar efficacy as oral codeine in the management of post-craniotomy pain.

Separation and characterization of degradation/interaction products of codeine phosphate in ibuprofen arginate/codeine phosphate combination formulation by HPLC coupled with MS analysis

A simple HPLC method was developed and validated according to the ICH guidelines to detect and quantify the related substances of codeine phosphate in the raw material and in its combination formulation with ibuprofen before and after forced degradation. These products were further identified by using HPLC-TOF/MS and MS/MS techniques. Good separations were obtained on a C18 （250 min×4.6 mm, 5 μm） column maintained at 50 ℃ with linear gradient elution by a mixture of mobile phase A （ammonium acetate （pH 6.0 regulated with acetic acid, 0.04 M）-acetonitrile （92：8, v/v）） and mobile phase B （acetonitrile） at a flow rate of 1 mL/min. UV detection was set at 245 nm. Codeine was found to be instable under oxidation with the production of mainly two stereoisomers of codeine N-oxide. A new degradation product, not reported previously, was detected under alkaline hydrolysis, which was identified as 6-hydroxy-3-methoxy-17-methyl-7,8-didehydromorphinan-5-ol and shortly named as deshydrolevomethorphandiol. The esterification of codeine by ibuprofen occurred in very small amount and only under acidic stress. These results contribute to the understanding of the degradation behavior of codeine and its interaction with ibuprofen. The developed method is sensitive and precise and could be applied for the quality control of codeine bulk drug, preparations of codeine phosphate, and its combination with ibuprofen.

Antitussive activity of Triclisia dictyophylla of the family Menispermecae

Objective:To verify through a scientific mean the therapeutic use of the plant as an anti-tussive agent,by traditional medicine healers and also aid in the search for new drugs developments from plants.Methods:The roots of Triclisia dictyophylla were investigated for their antitussive properties.The plant was uprooted in the month of June 2003 at Igbodo,Delta State,Nigeria and was taken to the university of Nigeria Nsukka for taxonomy. The roots were chopped,ground and immersed in pure drinking water for 24 hours.After filtration, extraction was carried out using a Rotary evaporator,preliminary phytochemistry and acute toxicity studies were carried out.Antitussive study was carried out using a total of 42 young rats of average weight of 72.2 g.The rats were housed in standard animal house of the university and were allowed access to feeds and water but, were fasted for 12 hours prior to commencement of experiment.Specific and appropriate dosage of the crude extract and Codeine re - dissolved in water were administered orally 30 minutes prior to induction of cough. Cough was induced by exposing the animals to Sulphure dioxide gas for 3- minutes.Coughing was taken as number of Head-nods per minute,Stethoscope aided audible sounds and,or tears secretion.Percentage cough inhibition for crude extract and,or Codeine treated rats were compared with reference to control animals.Results were subjected to statistical analysis using SPSS 13.0.Results:A 10.2%extraction yield was got from a starting root initial weight of 320 g.The preliminary phytochemistry of the aqueous root extract revealed the presence of alkaloids,saponins,flavonoids,proteins,reducing sugars,steroids,resins fats/oils and glycosides. The Median lethal dose(LD_(50)) based on Lorke's 1983 method was 548 mg/kg The aqueous root extract at concentrations of 10 mg/kg,50 mg/kg,100 mg/kg and 200 mg/kg orally administered,inhibited cough in rats induced by sulphure dioxide gas by 16.67%,33.33%,50.00%and 83.33%respectively.While Codeine phosphate,a standard antitussive agent,at oral concentrations of 10 mg/kg and 20 mg/kg inhibited cough in rats induced by sulphure dioxide gas by 33.33%and 60.67%respectively.Conclusion:Earlier works by some authors had led to isolation of Morhinian Alkaloids from Triclisia dictyophylla thus most probably linking its mechanism of antitussive activity to that likable of Morphine.This study justifies the use of the plant in treatment of cough by Traditional Medicine Healers.

Studies of Active Ingredients in Cough Syrup by Capillary Zone Electrophoresis with Amperometric Detection

The present paper covers a simple, reliable and reproducible method, based on capillary zone electrophoresis(CZE) with amperometric detection(AD), for the separation and the determination of ephedrine hydrochloride, promethazine hydrochloride and codeine phosphate. Under the optimal conditions, the three analytes were base-line separated completely within 16 min. Good linear relationships between the peak heights and the concentrations of the three analytes were obtained with the correlation coefficients better than 0 9993. The method was directly applied to the determination of the active ingredients in pharmaceutical preparations and the assay results were satisfactory.

Bioinspired Scalable Total Synthesis of Opioids

As one of the largest and most representative families of natural medicines harvested from plants,the mass production of opioids legitimately occupies large,worldwide farmland cultivation of opium poppies,causing severe regulation limitations and supply uncertainty.Due to their complex structures,the chemical synthesis of opioids has been criticized as infeasible for large-scale production in view of lengthy synthetic steps and overall low efficiency.