ABSTRACT

A new pharmaceutical entity can cost several millions of rupees or dollars to develop. Astonishingly, even a few month deferrals in taking it to the market can have notable impact on the pecuniary status of the company. One of the major activities of the regulatory specialist is to ensure that the label of the product and related information of the patient has correctly been established and even a small error in any of the regulatory activities can make the product to be ready for recall in addition to the loss of several millions of money which is eventually bound to give rise to fall in self assurance of financiers, health experts and the patients. aRegulatory Affairs is a comparatively new profession which developed from the desire of government to protect public health by controlling the safety and efficacy of products in areas including pharmaceutical, veterinary medicines, medical device, pesticides, agrochemical, cosmetics and complementary medicines, biologics and functional foods.

Keywords- Regulatory Affairs, cosmetics, agrochemical

ABSTRACT

Keratin is a fibrous structural protein and major component of hair, horns, claws, hooves, feather, wool, hoof and outer layer of skin. These keratinous materials are formed by cells filled with keratin and are considered ‘dead tissue’. Keratin acts both as an external protective protein & internal structural protein in the cortex. It is insoluble in water and organic solvents. Keratin can be derived from the human and animal sources by the advancement in extraction, purification and characterization process. It consists of highly repetitive amino acid sequences which result in formation of various homogeneous secondary structures. Keratin has been processed in oxidized and reduced forms in term of keratose and kerateine which shows strong mucoadhesive properties in drug delivery systems .It can also be processed as keratin hydrolysate by using acid, alkali and enzyme. Especially for hair care products, skin treatment and harsh products such as detergents, shampoos, conditioners etc. As it does not contain any harmful effect, it can be used to produce variety of cosmetics and pharmaceutical products. In addition, extracted keratins are capable of forming self-assembled structures that regulate cellular recognition and behavior. These qualities of keratin led to the development of biomaterials with applications in wound healing, drug delivery, target release action, tissue engineering, trauma and medical devices. This review discusses the natural sources of keratin and their derivatives and application of keratin biomaterials in pharmaceutics and cosmetics.

Keywords: Keratin, keratin hydrolysate, Phytokeratin, Biomaterials, Drug delivery, keratin film, Nanoparticles, cosmetics.

ABSTRACT

Duchenne muscular dystrophy(DMD) one of the most severe forms of inherited muscular dystrophies. It is the most common hereditary neuromuscular disease and does not exhibit a predilection for any race or ethnic group. Mutations in the dystrophin gene lead to progressive muscle fiber degeneration and weakness. This weakness may present initially with difficulty in ambulation but progressively advances to such an extent that affected patients are unable to carry out activities of daily living and become wheelchair bound. Cardiac and orthopaedic complications are common, and death usually occurs in the twenties due to respiratory muscle weakness or cardiomyopathy. Current therapy is centred on treatment with glucocorticoids and physiotherapy to prevent orthopaedic complications. ^[1] Duchenne muscular dystrophy (DMD), an allelic X-linked progressive muscle-wasting disease, is one of the most common single-gene disorders in the developed world. Despite knowledge of the underlying genetic causation and resultant pathophysiology from lack of dystrophin protein at the muscle sarcolemma, clinical intervention is currently restricted to symptom management. In recent years, however, unprecedented advances in strategies devised to correct the primary defect through gene- and cell-based therapeutics hold particular promise for treating dystrophic muscle. Conventional gene replacement and endogenous modification strategies have greatly benefited from continued improvements in encapsidation capacity, transduction efficiency, and systemic delivery. In particular, RNA-based modifying approaches such as exon skipping enable expression of a shorter but functional dystrophin protein and rapid progress toward clinical application. Emerging combined gene- and cell-therapy strategies also illustrate particular promise in enabling ex vivo genetic correction and autologous transplantation to circumvent a number of immune challenges. These approaches are complemented by a vast array of pharmacological approaches, in particular the successful identification of molecules that enable functional replacement or ameliorate secondary DMD pathology. Animal models have been instrumental in providing proof of principle for many of these strategies, leading to several recent trials that have investigated their efficacy in DMD patients. Although none has reached the point of clinical use, rapid improvements in experimental technology and design draw this goal ever closer. Here, we review therapeutic approaches to DMD, with particular emphasis on recent progress in strategic development, preclinical evaluation and establishment of clinical efficacy. Further, we discuss the numerous challenges faced and synergistic approaches being devised to combat dystrophic pathology effectively.

Keywords: dystrophy, animal models, pharmacological, exon skipping, gene therapy, utrophin.

ABSTRACT

Elevated bioavailability is an advantage for most of the poorly soluble drugs. The present scenario of research investigation is concentrated on different techniques to alter the solubility characteristics of weakly soluble drugs and crystallization phenomenon is one amongst them. The low solubility problem can be solved by changing the crystal habit of drug. So, in the present research an attempt has been made to modify the solubility characteristics of Nifedipine, an anti-hypertensive drug, using solvent change method, Solvent evaporation technique and solvent change precipitation technique. Among them solvent change method gave a better formulation (NIF-MC-6) showing better dissolution (91.36% at the end of 240mins) as compared to pure drug and micro-crystals formulated using other methods. The formulated crystals of Nifedipine were subjected to various physico-chemical parameters like size distribution, solubility studies, in-vitro dissolution studies, drug content, FT- IR, DSC, crystallographic studies by PXRD and crystal morphology by SEM studies. The micro-crystals produced with PVPK30 and chloroform. FT-IR Results showed that there was no chemical interaction between the drug, solvent and the stabilizer. PXRD of micro-crystals showed higher peak height than pure drug indicating that crystal habit modification occurred in the micro-crystals without any polymeric changes and were found to be smaller in size than pure drug and free from any interactions. SEM studies indicated that the crystals are present in rectangular and square shape. The DSC curve showed that Nifedipine appeared an endothermic peak at about 174⁰C corresponding to its melting. However, the crystals prepared with PVP K30 shows shift of endothermic peak towards lower temperature at 170.82⁰C respectively, dictating decreased melting point of the drug in the formed crystals, which accounted for increased solubility of the drugs.

Keywords: Microcrystals, Nifedipine, PVPK30, Solvent evaporation technique, solvent change method, solvent change precipitation technique.

ABSTRACT

Alcohol is the most widely consumed chemical substance in the world. Exposure to high levels of alcohol for a long period could lead to progressive cardiac dysfunction and heart failure. Alcoholic cardiomyopathy is a cardiac dysfunction associated with chronic and excessive alcohol intake. In spite of its clinical importance, data on ACM and how alcohol damages the heart is limited. In this article, we evaluate the available data linking excessive alcohol consumption with heart failure and dilated cardiomyopathy. The study was conducted in Warangal and a total of 124 patients admitted in the hospital with DCM were included and the subjects were screened based on drinking patterns of alcohol. Alcohol without abstinence was a strong predictor of cardiac death. This suggests that a more aggressive approach to alcohol cessation is needed in these patients.

Key words: Alcohol; Alcoholic cardiomyopathy (ACM); Dilated cardiomyopathy (DCM); Heart failure

ABSTRACT

Hibiscus rosasinensis Linn are used in medicines in emollients and also it is used to treat burning sensations and skin disease. Mucilage of Hibiscus rosasinensis contains L‐rhamnose, D‐galactose, D‐galactouronic acid, and D‐glucuronic acid. The present article is trying to present an investigation is to extract the mucilage from the petals of flower of Hibiscus rosasinensis and use it in a paracetamol tablets as a binder. As the mucilage having granulating and binding properties so it is used in tablets, using paracetamol as a model drug. The Ph of mucilage was found to be 6.5 and all the physicochemical properties i.e. solubility and swelling index was studied. In this investigation wet granulation technique is used for the formation of granules using the above described mucilage which having the concentration of 2%, 5% and 7% w/v to use as a binder.’

Keywords: Hibiscus rosasinensis, Mucilage, binder, Tragacanth , Acacia

ABSTRACT

Doxorubicin is an anthracycline antibiotic widely used as a chemotherapeutic agent in the treatment of several tumors. However, its cardiac toxicity limits its use at maximum therapeutic doses. Most studies implicated increased oxidative stress as the major determinant of DOX cardiotoxicity. Thevetia peruviana known to have antioxidant activity. The aim of the current study was to explore the potential protective effects of methanolic extract of Thevetia peruviana against DOX-induced cardiotoxicity in rats. Methanolic extract of this plant showed significant cardioprotective effect by lowering the serum levels of various biochemical parameters like Creatinine  phosphokinase (CPK), Lactate dehydrogenase (LDH), Alanine transaminase (ALT) and Aspartate transaminase (AST) in the selected model. Additionally, histopathological examination indicated a protection against DOX-induced cardiotoxicity. The results also suggests that the biologically active phytoconstituents such as flavonoids, alkaloids, glycosides, carbohydrates, triterpenoids and tannins present in the methanolic extract of plant which is confirmed from the qualitative analysis may be responsible for the significant cardioprotective activity.

Keywords: Thevetia peruviana, Cardioprotective activity, Doxorubicin, Cardiotoxicity.

ABSTRACT

Yule distribution is one of the more accurate distributions for fitting the heavy tailed data, although it is difficult to get a closed formula for the parameter estimator. In Spierdijk (2007), single maximum likelihood estimator (MLE) for the Yule (ρ) parameter was found numerically. In addition, another extension of the distribution was derived and it denoted as GYule (ρ,α), generalized Yule distribution. The moment estimators were got numerically for GYule but it was difficult to get the MLE's for the parameters. [Spierdijk (2007)]. In this study, single MLE’s for GYule (ρ,α) parameters was found numerically and was applied for the same dataset used in Spierdijk (2007). GYule density function was also derived using the method of mixing distributions and then an explanation of variation was given by dividing the distribution variance into three components (randomness, liability and proneness).

Keywords: Yule distribution, generalized Yule distribution, extended Yule distribution, incomplete Beta function, mixed distributions, superstar data and the snowball effect.

ABSTRACT

Through this review we would like to introduce clean and efficient method of most conventional Friedel-Craft acylation of phenols using Ionic liquid. This method has best results of acylated phenols in terms of quality and yields are concerned. The Friedel-Craft acylation is an everyday applicable industrial synthesis. Phenols are dihydric, trihydric as well as monohydric hydrocarbons used to undergo acylation. Acetyl chloride is best suitable reagent for aromatic C-acylation. Ionic liquid [EMIM][AlCl₄] has best solvation and catalytic effect in the reaction.

Key Word: Friedel-Craft Acylation, Phenols, Ionic liquid [EMIM][AlCl₄], Acetyl Chloride

ABSTRACT

The aim of the present work was to design controlled release tablet of Tramadol hydrochloride for prolong release and it’s in vitro evaluation. Controlled tablets of Tramadol hydrochloride comprised HPMC K15M, and HPMC K100M as the release retarding polymers. These tablets were prepared by direct compression method. The seven different formulations (F1-F7) were evaluated for pre- and post-compression parameters. In vitro dissolution studies were carried out for the optimized formulation (F7). It has found that the release of drug from the sustained release layer by 99.5% in 12 h. FT-IR studies revealed that there was no interaction between the drug and polymers used in the study. The release of Tramadol hydrochloride was found to follow a pattern of Korsmeyer-Peppas, with Quasi-Fickian diffusion. Accelerated stability studies were carried out on the prepared tablets in accordance with ICH guidelines. There were no changes observed in physicochemical properties and drug release pattern of tablets. The controlled drug release pattern was successfully achieved through the formulation of controlled tablets in this study.

Keywords: Tramadol hydrochloride, HPMC K15M, HPMC K100M, Micro crystalline cellulose, direct compression, and In-vitro dissolution studies etc.  

ABSTRACT

Talinum fruticosum.L (Talinaceae) is a erect, stout, fleshy, perennial herb. It is used as a leaf vegetable. It contain rich in vitamins including vitamin A and C and minerals such as iron and calcium. The present work highlights phytochemical and antimicrobial studies of Talinum fruticosum. The whole plant were collected from Kasaragod district and subjected to successive solvent extraction. The next step the various extracts of the plant were tried to phytochemical screening. The phytochemical screening shows the presence of flavonoids glycosides carbohydrates and protein. the chloroform and methanolic extracts were subjected to phytochemical screening. The chloroform extract shown the activity against gram positive organism. The phytoconstituents like flavonoids, glycosides are responsible for this activity. The phytochemical studies gave confirmation of the above said result.

Keyword: Talinum  fruticosum. L, phytochemical, antibacterial

ABSTRACT

Ring acylations of aromatic substances are very difficult to achieve to a great extent. Nencki reaction has attempted on mono to poly hydroxy and substituted phenols have good results. Reactions are using solely acetic acid, acetic anhydride and adipic acid or mixture of acid and anhydride resulting complete consumption of phenols. The use Lewis acid freshly fused ZnCl₂ is best suitable catalyst compare to others. The essential data on phenols acylation has been studied and described as below. 

Keywords: Nencki reaction, Phenols, Acetic acid, Acetic anhydride, Adipic acid, Freshly fused ZnCl₂

ABSTRACT

The purpose of this study is to prepare Mouth dissolving tablets of Cinnarizine HCl and Domperidone Maleate by Direct compression method. In the present research study, Crosspovidone (CP) and Sodium Starch Glycolate (SSG) was taken as super disintegrant. Here the Cinnarizine HCl (H₁ anti-histaminics) and Domperidone (anti-emetic) is taken as the model drug for the study and direct compression as a method for preparation of the Mouth Dissolving Tablet. These combination of drugs are ideal for the prevention of symptoms caused by vestibular disorders and vertigo/motion sickness, nausea, dizziness, headache, vomiting, sensation of fullness when there is a delay in gastric emptying. A 3² full factorial design was applied to investigate the combine effect of two formulation variable CP(X1) and SSG(X2). Here the concentration of both Superdisintegrants was taken as independent variable, X1 and X2 respectively. I.R. and DSC study revealed that all polymers and excipients used were compatible with the drugs. All the pre and post-compression evaluation parameters shows good results and all batches are within acceptable limits. Mouths feel test gives pleasant sensation on human subjects when tablets are put it on tongue. The effect of Disintegration time (Y1) and % Drug release (Y2) were investigated as dependent parameters. From optimization data results that, among all the formulation F6 Batch was best formulation. The optimized batch obtained from the factorial design was compared with the marketed products. The stability study of the optimized batch is also done at 40ºC and 75%RH.

Keywords: 3² Full factorial design, Cinnarizine HCl, Domperidone Maleate, Crosspovidone, Sodium starch glycolate, Disintegration time, and Percentage drug release.

ABSTRACT

Slim green tea is a popular brand of tea that supports weight reduction and maintenance. High consumption of this tea in worldwide populations is a major concern to researchers and medical personnel, as regards its benefits or dangers to human health. Therefore the aim of research was to ascertain impact of slim green tea on some oxidative stress markers in heart and brain tissues, lipid profile, and cognitive functions in Wistar rats. Twenty-five (25) male Wistar rats weighing between 120g and 150g were acclimatized for 2 weeks, they were separated into 5 groups; a control Group (Group 1) and Groups (2, 3, 4 and 5) which served as test groups. Various doses of slim green tea extract (50mg/kg, 100mg/kg and 150mg/kg) and a dose of vitamin E (100mg/kg) were administered orally for four weeks to the different groups of rats (2, 3, 4 and 5) respectively, while control group received normal chaw and water ad libitum. The results indicated that slim green tea extract caused dose-dependent significant decrease (p≤0.05) on Malondialdehyde (MDA) and nitric oxide (NO) levels, and a dose-dependent significant increase (p≤0.05) on Superoxide Dismutase (SOD), Glutathione (GSH), and Catalase (CAT) levels in tissues of heart and brain in Wistar rats. The result showed high doses of slim green tea extract seemed more functional in increasing antioxidant properties in brain tissue than in heart tissue. Treatment of test groups with varied doses of tea extract on serum lipid profile demonstrated a dose-dependent significant decrease (p≤0.05) on total cholesterol and HDL levels in every group compared to control group. The extract equally caused a significant decrement on LDL level and an insignificant effect on triglyceride level when administered at 50mg/kg and 100mg/kg respectively, while dose of 150mg/kg increased LDL and triglyceride levels significantly. Results on cognitive assessment in brain showed slim green tea had no cognition-enhancing property. These findings suggest intake of slim green tea has beneficial effect especially as regard cardio-protection and neuro-oxidative protection but no effect on cognition.

Keywords: Slim green tea, Vitamin E, superoxide Dismutase, Glutathione, Catalase, cognition.

ABSTRACT

The effect of crude oil contaminated feed on cardiovascular integrity and risk factors in wistar rats was studied. 35 Wistar rats of similar weight were randomly divided into 7 groups as follows; Group 1 control (normal chow), Group 2 (Treated with 3.88g/kg crude oil mixed meal), Group 3 (Treated with 7.75g/kg crude oil mixed meal), Group 4 (Treated with 15.51g/kg crude oil mixed meal), Group 5 (Treated with 32.01g/kg crude oil mixed meal), Group 6 (Treated with 62.02g/kg crude oil mixed meal), and Group 7 (myocardial infarct-induced group). Treatments in various groups were administered for 8 weeks (exposure period) and were later withdrawn for 2 weeks (withdrawal period). The blood pressures (Systolic, diastolic blood pressure and heart rate) were recorded in both phases, 5 ml of blood was taken from all groups via cardiac puncture in both phases for analysis of lipid profiles. Cardiovascular Risk Indices (Castelli Risk index I & II, Atherogenic index of plasma, and atherogenic coefficient) were extrapolated and calculated. Results from various laboratory analyses were statistically analysed using ANOVA (SPSS) and presented in tables and charts with level of significance at P ≤0.05. Blood pressure estimates and lipid parameters all presented marked increase during the exposure phase of six weeks. Similarly, cardiovascular risk indices were aggravated significantly (P ≤0.05) during the same period. In the withdrawal phase, virtually all the above measured parameters were reversed and the corresponding biological effects ameliorated. The implications of the above extrapolates in both phases indicated that crude oil exposure could trigger lipid peroxidation, electrolyte imbalance, cellular disruptions, and can be highly detrimental and delirious to cells while withdrawal from the contaminated meal was observed to reverse the entire scenarios. In conclusion, crude oil contaminated feed on cardiovascular integrity and risk factors could be a major pre-disposing scenario for biologic derangement and down-regulation of cellular bio-functions in living organisms at estuaries and among riverine dwellers.

Keywords: Crude oil, Castelli Risk index I & II, Atherogenic index of plasma, and Atherogenic coefficient

ABSTRACT

This study investigated the behavioral and motor responses of induced fear in Wistar rats. Twenty-five wister rats used in this experiment were divided into five groups with each group comprising of five rats. Group I received low dose of glutamate receptor antagonist (GRA), Group II received high dose of GRA, Group III were given low dose of adrenaline, Group IV were given high dose of adrenaline while Group V (control group) were given normal saline. These animals were made to undergo two sets of tests viz; One, Induced Fear and Emotional Reactivity (IFER) Test using light/dark automatic reflex conditioned box to test for their threshold for fear shortly after induction using foot-shock method. The degree of passivity, grooming and escape attempt were noted and recorded and their respective cognitive recovery potentials were measured. Two, the Elevated Plus Maze (EPM) Test was employed to assess their level of fear expression under drug influence. The results and extrapolations suggested that groups administered with glutamate receptor antagonist in both low and high concentrations expressed less enhanced alertness, mental cognition and general awareness in both the light and dark compartments on a short time basis with activities characterized with passivity, grooming and  attempt to escape when compared with those sets of observations in the adrenaline-administered groups both in short and long term durations with much significant influence (p< 0.05). The results of the elevated maze plus (EPM) test followed the same pattern. The present results indicate that induced fear significantly interfered with cognitive activities and normal patterned behaviour in animals and the consequence of this psychic interference played out apparently in after-fear potential (a set of relatively new set of behavioural patterns. The cognitive recovery potential was significantly (p< 0.05) slowest in the glutamate antagonist groups and fastest (p< 0.05) in the adrenaline groups. These observations suggest that excitatory agonists like thiopental (glutamate receptor antagonist) may lack the ability to ameliorate stress-laden influence on brain cognitive circuitry but stress hormones such as adrenaline do in extremely significant fashion.

Keywords: Motor responses, glutamate receptor antagonist, emotional reactivity, foot-shock, passivity.

ABSTRACT

The impact of crude oil mixed meal on cellular status and oxidative stress markers in rat’s heart homogenates was studied. 35 Wistar rats of similar weight were randomly divided into 7 groups as follows; Group 1 control (normal chow), Group 2 (Treated with 3.88g/kg crude oil mixed meal), Group 3 (Treated with 7.75g/kg crude oil mixed meal), Group 4 (Treated with 15.51g/kg crude oil mixed meal), Group 5 (Treated with 32.01g/kg crude oil mixed meal), Group 6 (Treated with 62.02g/kg crude oil mixed meal), and Group 7 (myocardial infarct-induced group). Treatments in various groups were administered for 8 weeks (exposure period) and were later withdrawn for 2 weeks (withdrawal period). 5 ml of blood was taken from all groups via cardiac puncture in both phases for analysis for electrolytes estimations, haematological parameters, lipid profiles, and liver enzyme assay. Heart tissues were taken and homogenized and prepared for cardiac oxidative stress markers analysis, were extrapolated and calculated. Results from various laboratory analyses were statistically analysed using ANOVA (SPSS) and presented in tables and charts with level of significance at P ≤0.05. Haematological indices, electrolytes liver enzymes profile, lipid parameters and oxidative stress markers all presented marked increase during the exposure phase of six weeks. In the withdrawal phase, virtually all the above measured parameters were reversed and the corresponding biological effects ameliorated. The implications of the above extrapolates in both phases indicated that crude oil exposure could trigger, electrolyte imbalance, cellular disruptions, liver assault, and can be highly detrimental and delirious to cells while withdrawal from the contaminated meal was observed to reversed the entire scenarios. In conclusion, crude oil contaminated feed on cardiovascular integrity and risk factors could be a huge challenge and a potent pre-disposing scenario to various debilitating diseases of the heart on prolonged exposure.

Keywords: crude oil mixed meal, electrolytes, oxidative stress markers, liver enzymes, lipids.

ABSTRACT

The study was aimed to formulate solid dispersions of Manidipine by using different novel carriers like Labrafac PG, Kolliwax RH 40, Soluplus, Kolliwax GMS II, Kolliphor EL and SLS in drug carrier ratio by using solvent evaporation method. The formulations were characterized for physical appearance, solubility and in vitro dissolution studies. The optimized formulation was characterized by, Formulation SD13 was found to be optimized one based on the solubility, dissolution and other parameters using Kolliwax GMS II and SLS.  The drug release of the optimized formulation was found to be 99.41±5.38% within 90min. Powder X-ray diffraction studies performed on solid dispersion showed that Manidipine existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Additionally, scanning electron microscopy studies suggested the conversion of crystalline Manidipine to an amorphous form. Furthermore, the pharmacokinetic parameters of the optimized Manidipine solid dispersions showed increased AUC_0–t, AUC_0–∞ and C_max by 2-folds. These results suggest that the preparation of Manidipine solid dispersions using the solvent evaporation technique without might be a promising approach for improving the oral bioavailability of Manidipine. Therefore, the solid dispersions using Kolliwax GMS II as hydrophilic carrier in the combination of SLS can be successfully used for improvement of solubility and bioavailability of Manidipine.

Keywords: Manidipine, Solvent Evaporation method, Kolliwax GMS II, Hypertension, Bioavailability studies.

ABSTRACT

The objective of the present work was to formulate and evaluate novel self-nano emulsifying drug delivery system (SNEDDS) of poorly soluble drug Nateglinide. Poor water solubility and slow dissolution rate are major issues for most upcoming and existing biologically active pharmaceutical compounds. Nateglinide is Biopharmaceutical Classification System Class-II drug that has low solubility and high permeability. Surfactants and oil was selected based on solubility studies were further screened for their efficiency in formulation. Acrosyl K-135 was used as oil phase and Kolliphor RH 40 and Transcutol P were used as surfactant and co-surfactant respectively for formulation. Formulation F13 was found to be optimized formulation on the basis of in vitro dissolution studies, particle size and zeta potential. The particle size of the optimized SNEDDS formulation was found to be 74.6 nm and Z-Average was found to be 43.1 nm, indicating all the particles were in the nanometer range and the zeta potential of the optimized SNEDDS formulation was found to be -18.4 mV. The optimized formulation was then subjected to stability studies and was found to be stable after 6 months. Thus, the study confirmed that the SNEDDS formulation can be used as a possible alternative to traditional oral formulations of Nateglinide to improve its solubility.

Keywords: Nateglinide, Diabetes mellitus, SNEDDS, Solubility, Particle size & Zeta potential

ABSTRACT

Metastasis is a complex biological course that begins with detachment of tumor cells from the primary tumor, spreading into the distant tissues and/or organs, invading through the lymphovascular structures followed by their survival in the circulation. Metastatic tumors to the oro‑facial region are uncommon and account for approximately 1‑1.5% of all malignant oral tumors. Metastatic lesions can be found anywhere in the oral cavity, however, the jawbones with the molar area is the most frequently involved site. In the oral soft tissues, the gingival is the most common site, suggesting the possible role of inflammation in the attraction of metastatic deposits. Metastatic carcinomas in oral region can be the first clinical manifestation of an undiagnosed primary systemic tumor. The symptoms of metastatic carcinoma depend on the location of the tumor and can be variable, which may lead to erroneous diagnosis or may create diagnostic dilemma. Therefore, they should be considered in the differential diagnosis of inflammatory and reactive lesions that are common to the oral region. Most of the literature on oral metastases involves case reports; hence this present article is an attempt to provide a detailed review of pathogenesis, epidemiological details including clinical and radiographic presentations, microscopic features and treatment of metastatic tumors to the jaw bones and oral cavity.

Key words: metastatic tumors, jawbones, oral soft tissue.

ABSTRACT

The present study is concerned with formulation and evaluation of mucoadhesive buccal patches containing antihypertensive drug i.e. Timolol to avoid the first pass effect and to improve its bioavailability with reduction in dosing frequency and also dose related side effects. The patches were prepared by solvent casting technique with varying concentration of HPMC E15 as polymer and propylene glycol as the plasticizer and evaluate their physicochemical properties, in vitro drug release, moisture absorption, surface pH, mechanical properties, in vitro bio adhesion, and ex vivo drug permeation through porcine buccal membranes from optimized buccal patch. The physicochemical interaction between timolol and polymer was investigated by Fourier transform infrared spectroscopy. Moisture absorption, surface pH, tensile strength, elongation at break, peak detachment force and work of adhesion values of the optimized formulation F4 were found to be 124±10.59%, pH 6.61±0.28, 3.89 kg/mm², 14.16 mm², 4.92±0.06N and 0.65±0.08mJ respectively. Formulation F4 showed 68.99 ±1.67% of the drug release in in vitro condition and follows zero order kinetics and drug release mechanism follows non-fickian diffusion. Ex vivo drug permeation through porcine buccal membrane was performed and 58.52±1.59% of the drug permeated in 6 hrs with flux 0.22 mg/h/cm².The optimized formulation F4 with permeation enhancer tween 80 (1% v/w) showed drug release 64.47±1.63 % in 6 hrs with flux 0.33mg/h/cm². FTIR studies showed no evidence of interaction between the drug and polymers. Drug release from the buccal patches follows desire controlled release phenomenon as required in mucoadhesive drug delivery.

Keywords: Timolol, buccal patches, ex vivo permeation, bio adhesion.

ABSTRACT

It is well-known that Atrial Fibrillation (AF) is the commonest type of cardiac arrhythmias. The risk factors for AF have been investigated for years however, lone AF is idiopathic which means that there is no definite cause or risk factors for it. It usually affects young age groups; and because all the risk factors have been overlooked, the link between ABO system and cardiac arrhythmias in general has not been investigated yet. Based on that, we decided to set this study to figure out the link between ABO blood group and lone AF.This case series study was conducted over a period of one year (September 2016 to September 2017). A consecutive non random sampling technique was adopted by pooling all the patients with AF attended the emergency department in two main teaching hospitals (Al-Yarmouk Teaching hospital and Baghdad Medical City Teaching Hospital) during the total year data collection period. A total of 100 patient (52 females and 48 males) was collected, all were diagnosed by the cardiologist to have lone AF, their ages ranged between (20-60) years. The mean age of the study group was (40.36 +10.90) years, means of Blood parameters were as follow: for blood group A; glucose was (5.20+0.98) mmol/L, creatinine (1.15+0.28) md/dl, Sodium (146.02+4.47) meq/L and potassium (4.45+0.41)meq /L, P value <0.1. For blood group B: (4.73+0.82) mmol/L, (0.85+0.12) md/dl, (141.33+6.03) meq/L, (4.36+0.52) meq/L, P <0.2. Blood group AB: (5.14+0.96) mmol/L, (0.97+0.29) mg/dl, (145.57+5.34) meq/L, (4.17+0.51) meq/L and P <0.1. Finally blood group O results: (5.2+1.07) mmol/L, (0.99+0.29) mg/dl, (142.52+6.28) meq/L, (3.88+0.70) meq/L, P <0.1. No statistical significance was found in any of these groups.People of blood group A are at a relatively higher risk to develop lone AF than O blood group and other non O blood groups.

Key words: Lone Atrial Fibrillation, ABO blood groups, cardiac arrhythmias.

ABSTRACT

In current investigation an attempt has been made to formulate and evaluate Quinapril mouth dissolving films using HPMC 50cps, E5, E15 and in combination of Pullulan by Solvent evaporation method. Sodium starch glycolate acts as a super disintegrating agent and it is shown that as the concentration of the super disintegrates increases the disintegration time decreases. The films were evaluated for weight variation, surface pH, folding endurance, drug content, dissolving time, disintegration time, and in-vitro dissolution studies. Based on the evaluation parameters F17 was to be optimized formulation. The optimized film (F17) showed the more drug release i.e 99.40±5.30% within 7 min, lowest in vitro disintegration time 10 sec. FTIR studies proved no drug polymer interaction takes place. From in vivo bioavailability studies, C_max of the optimized formulation F17 was 72.43±0.3ng /ml, was significantly higher as compared to pure drug suspension, i.e., 42.32±0.1ng/ml. T_max of optimized formulation was decreased significantly when compared with pure drug (1.00±0.05hr, 2.00±0.1hr), AUC_0-∞ and AUC_0-t for optimized films was significantly higher (p<0.05) as compared to marketed product. These results revealed that fast dissolving films of Quinapril could be formulated for quick onset of action which is required in the efficient management of hypertension.

Keywords: Quinapril, Mouth dissolving films, Hypertension, Bioavailability studies

ABSTRACT

The present investigation deals with the formulation of mouth dissolving oral films of Rizatriptan which is used for the treatment of migraine. Rapidly dissolving films have acquired great importance in present scenario because of exclusive properties. The films of Rizatriptan were carried out using different grades of HPMCE3, E6, and E15, maltodextrin DE6, xanthan gum and other polymers by solvent casting method.  The prepared films were evaluated for film thickness, folding Endurance, Surface pH, morphological properties, %drug content and content uniformity, tensile strength, percent elongation, in vitro disintegration time and in vitro dissolution studies. The optimized formulation F24 prepared using HPMC E15 showed minimum disintegration time (9 sec), highest dissolution rate i.e. 99.6% of drug within 8 min and satisfactory physicochemical properties. The optimized film was evaluated for its bioavailability compared with pure drug as reference standard. Statistical analysis declare that no significant difference between the bioavailability parameters C_max, T_max, AUC_0–∞ and AUC_0–t of the test film (F24) and the reference product (Pure drug) indicated that they exhibited comparable plasma level-time profiles. These results revealed that the mouth dissolving film containing Rizatriptan is considered to be effectively useful for the treatment of migraine where quick onset of action is expected.

Keywords: Rizatriptan, mouth dissolving films, in vivo studies, solvent casting method.

ABSTRACT

The present work on the leaves of Argyreia speciosa Sweet (Convolvulaceae) has led to the pharmacognostical and phytochemical parameters. Macroscopical and microscopical characters, micrometry, physio-chemical constants, quantitative microscopy parameters, extractive values, carried out. The study also deals with the phytochemical screening of with various extracts. The total phenolic (TPC) and Total flavonoids contents (TFC) in leaves of Argyreia speciosa were studied with the aim of drawing the standards. The leaf is heart shaped upto 12.0-17.1-20.3 X 11.9-15.45-23.7 cm across, back with white shiny hairs on the lower surface, glabrous above, tomentose beneath and long stalked. Microscopically the leaves show cuticle, lignified xylem (3.48-5.10-7.43µ), phloem (1.45-2.85-4.25µ), starch grains, upper and lower epidermal cells were identified. Unicellular pointed tip trichomes are numerous and present on dorsal side abundantly. The palisade cells are rectangular in nature up to 10.32-13.41-16.50X1.93-2.77-3.57µ. The preliminary investigations showed that the moderate presence of terpenes, flavonoids, steroids, phenols and tannins. The TPC found to be, 173.55+0.017 mg (gallic acid equivalent/g) and TFC 134.07+0.123 mg (quercetin equivalent/g). In addition, total tannin content (TTC) determined by back titration with potassium permanganate and, was found as 087.00+0.17mg (tannin equivalent/g). In study TPC, TFC and TTC are significant and prove that, leaves are rich in estimated phytoconstituents and may have pharmacological importance.

Keywords: Argyreia speciosa, Macroscopy, Microscopy, Phenolic, Flavonoid, Tannin.

ABSTRACT

A gradient reversed phase high performance liquid chromatography (RP-HPLC) method has been developed and validated for the determination for related substances of Dapagliflozin drug substance. Chromatographic separation of Dapagliflozin from its process and degradation related substances was achieved on YMC Pack Pro C18, 250mm × 4.6mm 5m i.e A stainless steel column 250 mm long, 4.6 mm internal diameter filled with Octadecyl silane chemically bonded to porous silica particles of 5 mm diameter maintained column oven temperature at 25°C. Orthophosphoric acid buffer is mobile phase A and acetonitrile is mobile phase B. Wavelength for UV detection: 225nm, flow rate: 0.8 ml/min and Injection volume: 20µl. The developed method suitability was checked and validated as per ICH guidelines for specificity, linearity, accuracy, precision, limit of quantification, limit of detection robustness and ruggedness experiments. Dapagliflozin drug substance was subjected to stress conditions of thermal, hydrolysis, humidity, peroxide and photolytic to observe the degradation products. Limit of detection of each RS is less than 0.008%w/w indicating that the developed method is highly sensitive. The experiment results are given in detailed in this research article.

Keywords: Dapagliflozin, Related substances, HPLC, Validation

ABSTRACT

The thiol acetic acid and acetic anhydride both has been used for nucleophilic acyl substitution of phenols in two different methods. Both methods are simple and inexpensive by using aqueous NaOH base with acetic anhydride and no catalyst required for thiol acetic acid reaction. This can be a key method for identification of phenolic functional groups.

Keyword: Phenols, Thiol acetic acid, Acetic anhydride, aqueous Sodium hydroxide

ABSTRACT

The present study was performed to evaluate the anti-ulcerogenic activity of hydro-alcoholic extract of Ficus bengalensis Linn. bark against indomethacin-induced ulcers in rats and swimming stress induced ulcers in rats. Five groups of adult wistar rats were orally pre-treated respectively with carboxy methyl cellulose (CMC) solution (ulcer control group), Omeprazole 20 mg/kg (reference group), and 100, 200 and 300 mg/kg F. bengalensis Linn. bark extract in CMC solution (experimental groups), one hour before oral administration of indomethacin to generate gastric mucosal injury. Rats were sacrificed and the ulcer index, gastric volume, gastric pH, free acidity, total acidity of the gastric content was determined. Grossly, the ulcer control group exhibited severe mucosal injury, whereas pre-treatment with F. bengalensis Linn. bark extract exhibited significant protection of gastric mucosal injury in both models. Histological studies revealed that ulcer control group exhibited severe damage of gastric mucosa, along with edema and leucocytes infiltration of submucosal layer compared to rats pre-treated with F. bengalensis Linn. bark extract which showed gastric mucosal protection, reduction or absence of edema and leucocytes infiltration of submucosal layer. Acute toxicity study did not manifest any toxicological signs in rats. The present finding suggests that F. bengalensis Linn. bark extract promotes ulcer protection as ascertained grossly and histologically compared to the ulcer control group.

Key Words:  F. bengalensis Linn., Hydro-alcoholic, Gastric ulcer.