Pharmacognostic screening and antiemetic evaluation of the ethanol extract of the leaves of Morinda lucida benth. (rubiaceae)

Emesis is a common side and adverse effect associated with many illnesses, even drugs. It is the act or process of vomiting. Causes vary from pregnancy, morning sickness, motion sickness, chemotherapy and so on. Emetics are drugs or substances that induce vomiting. Antiemetics are agents given to stop vomiting and to stop the nauseous feeling. Morinda lucida, Benth. family, Rubiacae. It is commonly known as brimstone tree. It is about 24m long, the branches are fibrous in nature and does not break easily, the tree bark is brown to grey, the leaves are green with green fruits. This project is focused on the pharmacognostic evaluation and antiemetic activities of the ethanol extract of the leaves of Morinda lucida. The plants were properly collected and identified by a taxonomist, then, air dried at room temperature, blended using an electric miller. The ethanol leaf extract of the plant was obtained using cold maceration, filtered and concentrated using rotary evaporator. The extract was used for antiemetic evaluations, pharmacognostic and chromatographic (thin layer chromatography) evaluations. The LD50 was determined using Lorkes method. Pharmacognostic evaluation shows the presence of, lignin, cellulose, saponin, tannis, alkaloids flavonoids. The LD50 shows that there was no death recorded. The result of the research shows that the ethanol extract of Morinda lucida on 2 weeks old chickens exhibited antiemetic effect. It can therefore be concluded that the ethanol extract of Morinda lucida possess antiemetic activity as claimed and the result of these findings can be of great importance to the development of new antiemetic drug.

Statistical Modeling of Antiemetic Activity of Chemical Compounds

A model has been built linking the molecular structure of drugs with their antiemetic activity. It is shown that the bioactivity of drugs depends on the pseudopotential of the molecule, the information function of the molecule, and the geometric size of the substituents. The critical conditions for the emergence of effective antiemetic activity of molecules have been established. The optimal sizes of the substituents were determined, which correspond to the maximum bioactivity of the drugs. The mechanism of the threshold action of substituted benzamides was revealed.

A Photo Stability Indicating HPLC technique for Validation of Netupitant and Palonosetron in Bulk and Formulations

Analytical chemistry is the science that seeks ever improved means of measuring the chemical composition of natural and artificial materials.Netupitant Delayed emesis has been largely associated with the activation of tachykinin family neurokinin 1 receptors. Palonosetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally and peripherally in turn inhibits the visceral afferent stimulation of the vomiting center.The mobile phase used was orthophosphoric and acetate 70% buffer pH 3 and 30% methanol.The assay of Netupitant and Palanosetron was performed with tablets and the % assay was found to be 100.08 and 100.04, The linearity was found to be linear with a correlation coefficient of 0.999, the precision 0.8 and 0.3 for Netupitant and Palanosetron which shows that the method is precise.The validation of developed method shows that the accuracy is well within the limit, which shows that the method is capable of showing good accuracy and reproducibility. The LOD and LOQ for Netupitant were found to be 3.02 and 9.98 and LOD and LOQ for Palanosetron was found to be 3.00 and 10.00. Thus, it shows that the method is stability indicating, sensitive, accurate, robust and precise. Hence, the developed HPLC method can be successfully applied to the pharmaceutical dosage form and can be used for routine analysis.

Study on the antiemetic property of methanolic stem extract of Swertia chirata using chick emesis model

Background: Swertia chirata has been an important herb known for centuries for its various medicinal uses and bitter taste. The stem of the plant is used as a traditional medicine in an array of diseases including the treatment of vomiting. Therefore, the study was undertaken to explore the possible antiemetic property of methanolic extract of its stems by using chick emesis model.Methods: 25 male chicks of four days old weighing 25 to 35 grams were fed with copper sulfate anhydride at 50mg/kg body weight to induce emesis. The chicks were grouped into 5 with each group bearing 5 chicks (n=5). Group I (control) received 10ml/kg normal saline; group II (standard) received 150mg/kg chlorpromazine; group III (experimental-1), group IV (experimental-2) and group V (experimental-3) received 50, 100 and 150mg/kg respectively of the extract. All doses are given intraperitoneally. Assessment of antiemetic activity was done by calculating the percentage of inhibition of the number of retches in the chicks.Results: All the three doses of the extract showed antiemetic activity. The dose of 50 mg/kg showed activity comparable to chlorpromazine, while dose of 100 mg/kg and 150mg/kg showed greater activity than chlorpromazine. Highest antiemetic activity (79.26% inhibition) was shown by a dose of 150mg/kg and lowest (42.22% inhibition) by 50mg/kg.Conclusions: Methanolic extract from the stems of Swertia chirata has excellent anti-emetic property which can be further investigated for development of potential antiemetic medicines.

Studies of Degradation Kinetics of a 5-HT3 Antagonist, Ramosetron Hydrochloride: Effects of Temperature

Ramosetron hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT3) receptor antagonist with potential antiemetic activity. Upon administration, ramosetron selectively binds to and blocks the activity of 5-HT subtype 3 (5-HT3) receptors located in the vagus nerve terminal and the vomiting center of central nervous system (CNS), suppressing chemotherapy-induced nausea and vomiting. Degradation of Ramosetron HCl was conducted with 0.1N NaOH at 60°C, 70°C and 80°C to study the reaction kinetics. The reaction rate constants (k) for degradation at 60°C, 70°C and 80°C were -2.2680 molL-1s-1 , -3.3714 molL-1s-1 and -5.3686 molL-1s-1 for zero order and -1.05 x 10-2s-1, -1.60 x 10-2s-1 and -2.70 x 10-2s-1 for first order kinetics, respectively. The activation energy of Ramosetron HCl was found as 10.05 kcalmol-1 by using Arrhenius equation. Dhaka Univ. J. Pharm. Sci. 17(2): 167-173, 2018 (December)