PREPARATION AND EVALUATION OF METOLAZONE SOLID DISPERSIONS AND FAST DISSOLVING TABLETS USING STERCULIA FOETIDA SEED STARCH AND PLASDONE K-29/32 AS SUPERDISINTEGRANTS

Objective: The objective of the current study is to improve the solubility of the Biopharmaceutical Classification System (BCS) Class-II drug, Metolazone, using various superdisintegrants. Methods: Starches were extracted from Sterculia foetida seed powder by water and alkali techniques i.e., sodium hydroxide at 0.1%, 0.25% and 0.5% concentrations. Several phytochemical and physicochemical parameters were evaluated on the extracted starches. Solid dispersions of Metolazone were prepared by the solvent evaporation technique using plasdone K-29/32 alone and by mixing plasdone K-29/32 with Sterculia foetida seed starch. Various physical parameters were evaluated for the prepared solid dispersions. Tablets were prepared using Metolazone solid dispersions and varying concentrations of Sterculia foetida seed starch by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization using Scanning Electron Microscopy (SEM) and stability studies. Results: Phytochemical tests showed the presence of starch in all extracts. Starch prepared from 0.1% sodium hydroxide (SFS2) showed best physicochemical properties. In vitro dissolution studies revealed that solid dispersion MS4 containing Metolazone and plasdone K-29/32 in 1:3 ratios showed better drug release. Formulation MPT6 containing MS5 solid dispersion with 15% w/w of SFS2 showed enhanced drug release. SEM studies revealed no major interactions between drugs and excipients. Accelerated stability studies showed that all tablets were stable. Conclusion: Sterculia foetida seed starch and plasdone K-29/32 have enhanced the solubility of Metolazone

In-Vivo Evaluation of Some Novel Chromen- 2 One Based on Pharmacological Activity of Antipsychotic Drug

Most neuroleptics block the emesis hyper activity and aggression induced by apomorphine and other dopaminergic agonists. In higher doses, most neoroleptics induce characteristic cataleptic immobility that allows the animal to be placed in abnormal postures that persists, the aim of this project work was to carry out preliminary pharmacological screening of 2-[(4-methyl-2-oxo-2H-chromen-7-yl) oxy-(aryl)] acetamide. preliminary pharmacological screening of the synthesized compounds for the antipsychotic activity. The screening was limited to in vivo models only. The synthesized compounds were converted to their hydrochloride salts in order to make them water-soluble. These hydrochloride salts were used for the pharmacological testing purpose. The experiments were performed on Swiss albino mice (male) and the route of administration was intra peritoneal

FORMULATION AND EVALUATION OF FEBUXOSTAT FAST DISSOLVING TABLETS USING ENTADA SCANDENS SEED STARCH AND POLOXAMER-188 AS SUPERDISINTEGRANTS

Objective: The present study focused on solubility enhancement of the Biopharmaceutical Classification System (BCS) Class-II drug, Febuxostat using various super disintegrants. Methods: Starches were extracted from Entada scandens seed powder by alkali method i.e., sodium hydroxide at 0.1%, 0.25% and 0.5% concentrations and water. Starches were evaluated for various phytochemical and physicochemical tests. Solid dispersions of Febuxostat were prepared by fusion method using poloxamer-188 alone and by mixing poloxamer-188 with Entada scandens seed starch. Various physical parameters were evaluated for these solid dispersions. Tablets were prepared using Febuxostat solid dispersions and varying concentrations of Entada scandens seed starch by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) and stability studies. Results: Phytochemical tests revealed the presence of starch in all extracts. Starch prepared from 0.5% sodium hydroxide (ESS4) showed best physicochemical properties. In vitro dissolution studies revealed that solid dispersion F4 containing Febuxostat and poloxamer-188 in 1:3 ratios showed better drug release. Formulation FE5 containing F4 solid dispersion with 12.5% w/w of ESS4 showed enhanced drug release. FT2 tablets having 12.5% w/w of ESS4 showed better drug release when compared to others. FTIR and DSC studies revealed no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Accelerated stability studies showed that all tablets were stable. Conclusion: The super disintegrant property of Entada scandens seed starch was evaluated

PREPARATION AND EVALUATION OF DOLUTEGRAVIR SOLID DISPERSIONS

Objective: The current work mainly focuses on solubility enhancement of dolutegravir which is a BCS (Biopharmaceutical Classification System) class-II drug using various excipients. Methods: Solid dispersions of dolutegravir were prepared by solvent evaporation and fusion methods using carriers like poloxamer-188 and plasdone K-29/32 in different ratios (1:0.5 to 1:3.0). The amount of dolutegravir used was kept constant and the polymer concentrations were increased. Various physical parameters like angle of repose, carr’s index, Hausner’s ratio were calculated for the prepared solid dispersions. They were also evaluated for particle size and drug content uniformity along with in vitro drug release. Characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD) were also done. Results: Dolutegravir solid dispersions showed good to excellent flow properties. From in vitro dissolution studies, it was observed that the solid dispersion formulation DF3 containing dolutegravir and poloxamer-188 in 1:1.5 ratios prepared by fusion method showed better dissolution rate when compared with other formulations. The dissolution parameters were also evaluated. DF3 showed a higher drug release of 86.33% in 60 min. FTIR and DSC studies revealed that there were no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Conclusion: The solid dispersions prepared using poloxamer-188 by fusion method has enhanced the solubility of dolutegravir

PHYTOCHEMICAL AND PHARMACOLOGICAL EVALUATION OF COMMIPHORA MUKUL FOR ANTIDEPRESSANT ACTIVITY IN ALBINO MICE

Objective: The main aim and objective of the present study is to investigate the effect of Commiphora mukul (Family: Burseraceae), on depression in mice using tail suspension test (TST) and forced swim test (FST).Methods: The oleo-gum resin of guggul was extracted with alcohol and fractionated with ethyl acetate and petroleum ether. All the fractions were subjected for preliminary phytochemical screening, using various qualitative tests. Till date, no scientific data were available on the antidepressant activity of this plant. So, in the present investigation, TST and FST are selected as animal models for evaluation of antidepressant activity in albino mice.Results: The preliminary phytochemical screening of guggul has revealed the presence of carbohydrates, proteins, tannins, and flavonoids in hydroalcoholic fraction. Ethyl acetate fraction showed positive results toward flavonoids, alkaloids, proteins, and steroids. Hydroalcoholic, ethyl acetate, and petroleum ether fractions (50 and 100 mg/kg p.o.) of guggul administered orally for 14 successive days had decreased the immobility periods significantly in a dose-dependent manner in both TST and FST, showing significant antidepressant-like activity. The activities of the fractions were found to be comparable to imipramine in both FST and TST.Conclusions: Although a number of synthetic drugs are being used as standard treatment for clinically depressed patient, they have adverse effects that can compromise the therapeutic treatment. In the traditional systems of medicine, many plants and formulations have been used to treat depression for thousands of years. The results of this study indicate the potential for the use of guggul as an adjuvant in the treatment of depression.Keywords: Guggul, Commiphora mukul, Antidepressant activity, Forced swim test, Tail suspension test, Depression

Eisenmenger syndrome in a patient with ventricular septal defect: a case report

Eisenmenger Syndrome (ES) represents Pulmonary Arterial Hypertension (PAH) associated with Congenital Heart Defects (CHD). Although patients survive until their third or fourth decades of life, the symptoms include dyspnea, cyanosis, fatigue, dizziness, and syncope. In addition, cardiac arrhythmias, a late complication are causing sudden death in patients with ES. Treatment options have been limited; however, recent successes have been achieved with the use of therapies targeted against the pathophysiological pathways that underlie PAH. The dual endothelin receptor antagonist and prostacyclins demonstrated to improve hemodynamics of the patients. This is the case of a 16 year old young female with ventricular septal defect that was admitted with increasing shortness of breath and cyanosis with clubbing which are clinical features of Eisenmenger syndrome. She was medicated with Furosemide, Sildenafil which improved her functional status

Penicillin induced toxic epidermal necrolysis with secondary impetiginization: a rare case

Drug induced allergic reactions can be categorized into IgE-mediated and non-IgE mediated hypersensitivity reactions. Symptoms of IgE-mediated reactions are angioedema, bronchospasm, anaphylaxis, and urticaria that appears within 72 hours and those which are Non-IgE mediated hypersensitivity reactions include morbilliform eruptions, interstitial nephritis, hemolytic anemia, serum sickness, thrombocytopenia, and erythema multiforme, after 72 hours. TEN is defined as an extensive detachment of full-thickness epidermis most often related to an adverse drug reaction. We report a rare case of penicillin induced toxic epidermal necrolysis with Secondary Impetigination in a 38-year-old male patient with complaints of rashes all over the body, chest pain and dry tongue since seven days. Based on history and clinical examination patient was diagnosed as of penicillin induced toxic epidermal necrolysis with secondary impetigination and was successfully treated with antihistamines, parenteral antibiotics and corticosteroids.

Bilateral thalamic infarcts presenting oculomotor nerve palsy: case report

Bilateral thalamic infarctions are rare; oculomotor nerve palsy can be the result of direct or indirect damage to the oculomotor nerve. We report a case of oculomotor nerve palsy associated with changes in visual pattern and speech disturbances. There is no loss of consciousness. A computed tomography scan of brain showed acute bilateral thalamic infarct. Oculomotor nerve palsies with pupillary involvement warrant thorough investigation and there is no treatment to re-establish function of the weak nerve other than the body’s own healing process

Phenobarbital induced Stevens-Johnson syndrome: a case report

Stevens-Johnson Syndrome (SJS) is a life-threatening acute hypersensitive reaction affecting the skin and mucous membranes. We report a case with SJS likely induced by phenobarbitone during the switch of sodium valproate and phenobarbitone regimen. The patient reported fever with fluid-filled lesions all over the body and redness and burning sensation of both the eyes. Peeling of the skin due to rupture of the fluid-filled lesions and pigmentation on the skin for 10 days. Based on a physical examination and laboratory findings, he was diagnosed with Phenobarbital induced Stevens-Johnson syndrome. The patient was administered systemic steroid therapy and treated symptomatically and finally replaced with phenobarbitone and sodium valproate. During the hospital stay, the patient appeared normal and the skin lesions disappeared, after two weeks of treatment

Chlordiazepoxide induced Stevens-Johnson syndrome in acute pancreatitis

Stevens-Johnson Syndrome (SJS) is an acute hypersensitive reaction and a life-threatening condition affecting both skin and mucous membranes. We report a case with SJS likely induced by Chlordiazepoxide. The patient undergoing treatment for acute pancreatits is prescribed with Chlordiazepoxide after administering the patient reported mild pyexia with lesions all over the body with redness. Mild peeling of the skin due to rupture of the lesions and pigmentation on the skin was observed for 3 days. Based on these finding he was diagnosed with Chlordiazepoxide induced Stevens-Johnson syndrome. The patient was administered systemic steroid therapy and treated symptomatically. Here we describe a case of Chlordiazepoxide induced SJS in acute pancreatitis patient