ABSTRACT

The need of the day is to produce the product that meets customer requirements. As pharmaceuticals are related to health care this should be vital part of industry to produce a product such as tablets, capsules, ointments, creams, gels and emulsions etc. with minimum variation satisfying the needs of customer. Customer requirements are translated into ‘Critical to Quality’ (CTQ) characteristics of the products that they are about to produce by the formulation scientists.  As example, hardness, thickness, uniformity of weight, assay, dissolution etc are CTQ characteristics of tablets, Content uniformity, viscosity, density are CTQ characteristics of a gel etc.  There are various sources of variation which can be monitored by the Quality by Design i.e., QbD approach. Process should be monitored and controlled by using statistical process control which includes six sigma approach, process capability and control charts. Some of the more frequently used indices are Cp and Cpk. Cp represents process capability while Cpk is the process capability index which are determined between USL and LSL which signifies upper specification limit and lower specification limit. Cpk of at least 1.33 is desired, and 1.5 is excellent and if there are not more than 3.4 defects per million units, then six sigma is achieved.

Keywords: Quality by design, Cpk, Cp, Customer requirements, variation

ABSTRACT

The colon is the terminal part of the GIT which has gained increased importance not just for the delivery of the drugs for both local and systemic administration. The delivery of drug for the treatment of local diseases associated with the colon like Crohn’s disease, ulcerative colitis, etc. but also for the systemic delivery of proteins, therapeutic peptides, anti-asthmatic drugs, antihypertensive drugs and anti-diabetic agents. To achieve successful colon targeted drug delivery, a drug need to be protected from degradation, release and absorption in the upper portion of the GI tract and then to be ensured abrupt or controlled release in the proximal colon and that system refers to delivery of drug in to lower part of the GI tract, mainly large intestine. When this is the most important delivery of those drug which are normally inactivated in the upper parts of the gastrointestinal tract (GIT). This review mainly compares the primary approaches for CDDS (Colon Specific Drug Delivery) namely prodrugs, pH and time dependent systems, and microbial triggered systems, which achieved limited success and had limitations as compared with newer CDDS namely pressure controlled colonic delivery capsules, CODESTM, and osmotic controlled drug delivery (ORDS-CT) which are unique in terms of achieving the in vivo site specificity, and feasibility of manufacturing process for the CDDS. These treatments could be more effective if it is possible for drug to be directly delivered to colon. This review article discusses introduction of colon, need and approaches of colonic drug delivery, factor effecting colonic transition, colonic diseases and the novel and emerging technologies for advanced colon targeting for site specific drug delivery to colon. It is a challenging area for future research and holds lots of promises for novel and efficient approach for targeted drug delivery system.

Keywords: Colon targeted drug delivery, newly developed approaches, future prospect for CDDS.

ABSTRACT

As obesity remains the center of concern from many decades but yet there is no exact treatment, mostly you have to prefer the surgical method such as gastric bypass, which remains the only therapeutic treatment and the anti-obesity pharmacotherapy remains very limited therefore the priority is to discover or develop more potent drugs. The only potential strategy is to achieve weight loss it can be done by either reducing energy intake or by stimulating anorexigenic signals or by blocking orexegenic signals and to increase energy expenditure. This can be achieved by stimulating the Oxm, peptide PYY, GLP, GLP-1 receptor, and fat cells derived hormone like Leptin and Obestatin these reduces obesity by reducing food intake as seen in mice and humans by stimulating satiety signals, and by regulating the glucose homeostasis, by secreting glucose dependent insulin.

Keywords: Oxyntomodulin, Obestatin, Leptin, anti-obesity

ABSTRACT

Type 2 Diabetes Mellitus is the most prevalent disease, affecting majority of the world’s population. There are plenty of antidiabetics available in the market helping in achieving glycaemia control. The use of DPP-4 inhibitor is one the effective approach for treating the disease. Alogliptin is the latest analogue to the DPP-4 inhibitor class, approved in 2013. It is a highly selective, oral inhibitor of DPP-4 enzyme. Along with Alogliptin, FDA approved the fixed dose combinations of Alogliptin with Metformin and Pioglitazone, in the same year. Clinical data demonstrate that administering Alogliptin alone or in combination, leads to reduction in mean HbA1c and Fasting Plasma Glucose (FPG) level. Mean reduction of HbA1c is about 0.5% to 0.6% with Alogliptin alone and on combination with Metformin and Pioglitazone, the mean HbA1c reduce approximately by 0.6% and 1.8% respectively. The drug also reduces the Fasting Plasma Glucose (FPG) level by 10mg/dl to 20mg/dl and in combination with Metformin and Pioglitazone, the FPG level reduce by 20mg/dl and 50mg/dl respectively. Alogliptin is a drug with suitable tolerance and high safety profile. The drug shows no incidence of hypoglycemia and is weight neutral. Hence, Alogliptin benzoate is the preferred choice of the drug to treat type 2 diabetes mellitus.

Keywords: Type 2 Diabetes mellitus; Alogliptin; DPP-4 inhibitors; Incretin based therapy.

ABSTRACT

The patients who undergo Coronary Artery Bypass Graft surgery or Percutaneous Transluminal Coronary Angioplasty have co-morbid conditions that could negatively influence their survival. Diabetes Mellitus, COPD, Rheumatoid Arthritis, Anxiety and Depression could affect the outcome. Diabetes Mellitus is a risk factor for coronary artery disease. COPD patients could experience pneumonia and atrial fibrillation as complications. Rheumatoid arthritis patients are highly prone to inflammatory process which is the underlying pathology for atherosclerosis and can be a prognostic factor for CAD as well as chances for increased re-occlusion in patients undergoing coronary revascularising procedures. Anxiety and depression are negative emotions that adversely affect the outcome of patients. The co-morbid conditions should be effectively evaluated and managed.

Keywords: Coronary artery bypass grafting, Percutaneous trans-luminal coronary angioplasty, diabetes mellitus, chronic obstructive pulmonary disease, rheumatoid arthritis, anxiety.

ABSTRACT

The poor aqueous solubility and dissolution rate of API is one of the main challenge in pharmaceutical development. The improvement of solubility and dissolution profiles of these lipophilic drug molecules without altering the molecular structure is a particular challenge for the successful development of pharmaceutical products. Pharmaceutical cocrystals are molecular complexes of an API and one or more cocrystal formers, which are solids at room temperature, interacting through hydrogen bonding, π-stacking or van der Waals forces. A crystalline form of the API is strongly preferred because of their relative ease of isolation, and the physico-chemical stability that the crystalline solid state affords. The vast majority of APIs occur as solids; these include, salts, polymorphs, cocrystals and hydrates/solvates. Cocrystallization as a method of obtaining new forms of Active Pharmaceutical Ingredients (APIs) with improved physicochemical properties like solubility, stability, and melting point has gained much attention in recent years and is a promising alternative to so far employed preparation of salts, hydrates, solvates and other forms. Cocrystallization improves physicochemical properties of drug without affecting their pharmacological properties. There are various methods for preparation of cocrystals like solvent evaporation, solution crystallization, antisolvent addition, kneading etc. The characterization methods includes FTIR, DSC, PXRD, NMR, Raman spectroscopy etc.

Keywords: Co-crystals, solubility, dissolution, stability, characterization etc.

ABSTRACT

Obesity can lead to a complex range of diseases including diabetes, hypertension, osteoarthritis, certain types of cancer, and heart disease. It is now identified as the second leading preventable cause of death after cigarette smoking. Obesity and overweight occurs due to imbalance between calories consumed and calories utilized. Weight loss drugs, also called anti-obesity medications that help to reduce weight. Obesity drugs may be used in adult patients at medical risk from obesity BMI 30 or greater, or overweight patients with established BMI 27. The ideal anti-obesity drug would produce sustained weight loss with minimal side effects. These drugs alter one of the fundamental processes of the human body, weight regulation, by altering either appetite, or absorption of calories. In past years, numerous drugs have been approved for the treatment of obesity. However, most of them have been withdrawn from the market because of their adverse effects. Hopefully, more effective and better tolerated anti-obesity drugs will be developed through an improved understanding of the multiple mechanisms and complex physiological systems targeting appetite.

Key words: Obesity, anti-obesity drugs, weight loss, side effects.

ABSTRACT

Fluvoxamine is an antidepressant which is extremely utilized in our psychiatric practice. Sexual dysfunctions like erectile dysfunction, decreased libido and delayed ejaculation are well known side effects of this drug. However upsetting and painful sexual side effects like Priapism induced by Fluvoxamine has not been reported till yet through any literature. Here we are endeavoring to demonstrate a case of Fluvoxamine induced Priapism.

Keywords: Fluvoxamine, Priapism, Antidepressants.

ABSTRACT

Single unit floating effervescent matrix tablets of Dipyridamole were successfully prepared with hydrophilic polymers like HPMC K4M , HPMC K15M and HPMC K100M with 10% NaHCO₃ by Simple direct compression method with drug: polymer ratio of 1:1.5,1:2,1:2.5:1.3. FT-IR studies were conducted between drug, polymer and various excipients used in the formulations. Evaluation parameters of powder blend like Hausner’s ratio, Compressibility index, Angle of repose were carried out and results showed that the powder has good flow properties. Formulated tablets gave satisfactory results for various evaluation parameters like tablet hardness (5-6 Kg/cm²), weight variation (±10%), Friability (<0.9%), content uniformity (90%-110%), thickness (4-5mm) in vitro buoyancy properties and in vitro drug release. The floating lag time was found to be less for the formulations FS2, FS5, with 50sec, 48sec, respectively. Even the total floating time was found to be more than 12hrs for FS2, FS5, formulations with more than 90%drug release upto 12hrs. The swelling studies were carried for 24 hrs. The results indicate that the selected polymers were of swellable type and HPMC K4M has marginally more swellability than HPMC K15M and HPMC K100M matrices.  In vivo radiographic studies in fed condition the single unit matrix tablets (FS5) showed a gastric residence time of more than 6hrs. Indicated that the tablets remained in the stomach for 6hrs, which indicates the increase in the GRT is due to floating and swelling principle.

Keywords: Dipyridamole, Radiographic Studies, Hydrophilic Polymers, Floating Effervescent Matrix Tablets.

ABSTRACT

Two series of substituted phenothiazine derivatives were synthesized in order to obtain better antimicrobial agents.  The titled compounds 3a_, 3b_, 3c_, 3d_, 3e_, 3f and 3g, 3h, 3i, 3j were obtained by using o-chlorobenzoic acid and m-dichlorobenzene as starting material respectively. These compounds were synthesized according to Ullmann and Mannich base reaction. The structures of all these compounds were confirmed by spectral analysis. The titled compounds were screened for antibacterial and antifungal activities. Except 3e all compounds have shown good antibacterial activity against gram-positive and gram-negative bacteria. However, all these compounds have shown good antifungal activity against A. niger. The compound 3g has shown greater antifungal activity than the standard.

Keywords: Phenothiazine; o-Chlorobenzoic acid; Antibacterial; Ullmann; Mannich.

ABSTRACT

UV-Spectrophotometric method was developed for the simultaneous determination of Silybin (SIL) and Resveratrol (RES) from pharmaceutical (In-house) gel formulation (SIL-RES hydrogel). The in-house SIL-RES hydrogel was formulated by using carbopol as gelling agent. The UV spectrophotometric method involves formation of Q-absorbance equation at 218nm (isoabsorptive point) and at 288 nm, using methanol as a solvent. The linearity for both Silybin and Resveratrol was in the range of 2-12 μg/ml and 1-6 μg/ml respectively. The % recovery was found to be 99-100% for both Silybin and Resveratrol indicating proposed method is accurate and precise for simultaneous estimation of Silybin and Resveratrol in gel.

Keywords: Silybin, Resveratrol, Q-Analysis, UV-Spectrophotometry, In-house gel, Isoabsorptive point

ABSTRACT

Methotrexate is considered as the standard drug treatment for Rheumatoid arthritis. The purpose of this study is to find out the incidence of Adverse Drug Reactions (ADR), and possible risk factors in patients of rheumatoid arthritis administering methotrexate. And to determine the possibility of any new adverse drug reaction that is not well explored in previous studies. An observational follow up study designed and conducted using Naranjo scale to identify the adverse drug reactions in rheumatoid arthritis patients administering methotrexate in KIM’s Hospital.  The objective is to identify the dose dependent adverse drug reactions in rheumatoid arthritis patients and identify possible risk factors associated adverse drug reactions of methotrexate of methotrexate. Toxic effects may occur hours, to days to weeks after methotrexate administration and or overdose, the purpose of this study is to determine the relation between the dose and the occurrence of adverse drug reaction of methotrexate. During the study period clinically relevant adverse drug reaction have been presented by the patients taking methotrexate who attended hospital for their regular checkup. For example, the most commonly reported adverse drug reaction is abnormal taste for food and other less commonly presented adverse drug reaction include diarrhea, constipation, nausea, vomiting, and alopecia. In female patient’s 20-49 age group reported adverse drug reaction like amenorrhea, dysmenorrhea. Methotrexate toxicity develops due to increased patient susceptibility during the treatment.

Keywords: Rheumatoid Arthritis, Methotrexate, Adverse drug reaction (ADR), Naranjo scale.

ABSTRACT

Bioavailability may be considered as one aspect of drug product quality that links the in-vivo performance of the drug product used in clinical trials with studies demonstrating evidence of safety and efficacy. In the present study, the bioavailability was performed for the qualitative evaluation of the L-lysine produced by modified Corynebacterium glutamicum. Thirty 3-week-old male Sprague-Dawley rats weighing 45-55 g were used. The animals were divided into three groups. The first group was kept on a protein free basal diet which was supplemented with the biotechnologically modified L-lysine from Corynebacterium glutamicum. The second group comprised of animals which were fed the same basal diet but supplemented with a marketed preparation of L-lysine. The third group was kept on a regular protein diet which served as a control. The animals were fed ad libitum for 13 days, during which weight gain and food consumption were recorded and food conversion efficiency (FCE; weight gained/weight food eaten) was calculated. Ratios of means were calculated using the (least-square means)LSM for untransformed and ln-transformed FCE. The bioavailability was estimated by measuring the pharmacological activity (weight gained) and compared with that of the marketed preparations of L-lysine under similar conditions. For the study reference and test samples,-s the 95% confidence interval fell within the range of 97.72 and 103.61, which was the indication of bio similarity for biological activity of both the samples.

Keywords: Bioavailability, L-lysine, Corynebacterium glutamicum.

ABSTRACT

The present work was designed to investigate the anti-ulcer activities of methanolic extract of artocarpusaltilis [breadfruit] on alcohol induce ulcer in male albino rats. Animals were administered orally with a single dose of 98‰ alcohol [depending on the animals’ weight] to induce ulcer. This resulted in significant increase in ulcer occurrence [exacerbation]. Both the induced and normal rats were divided into six groups of 5 rats each. Group 1 was the control group [induced but not treated] while group 2 received 100mg/kg dose of aqueous extract of artocarpusaltilis. Group 3 and 4 received 200mg/kg and 300mg/kg dose of aqueous extract of artocarpusaltilis respectively. Group 5 received 10mg/kg per oral dose of omeprazole [standard drug]. Administration of methanolic extract of artocarpusaltilis produce a decrease in ulcer occurrence in induced rats. The decrease in ulcer occurrence was significant [p‹0.005] with all the groups treated with methanolic extract of artocarpusaltilis when compared to the control group. But group 3 and 4 exclusively showed same potency when compared to group 5 [standard drug]. The decrease in ulcer incidence when compared to the control group [ulcer induced but not treated] and for exhibiting same potency with the standard drug shows that the extract of artocarpusaltilis  is effective in controlling ulcer and can be used as a substitute for the standard drug in managing or treating/controlling ulcer. Conclusively, methanolic extract of artocarpusaltilis has tremendous beneficial anti-ulcer values in the treatment of ulcer following oral administration.

Keyword: Artocarpusaltilis, Omeprazole, anti-ulcer activities, gastric ulcer, ulcer index.

ABSTRACT

Drug utilization study is one of the fundamental watchtowers of promoting rational use of medicine for the treatment of various diseases. Often drugs are not used keeping in mind their safety and efficacy. To study the drug utilization pattern of psychotropic drugs in psychiatric outpatient department of Government General Hospital, Kakinada. A  Descriptive observational study was carried out in psychiatric outpatient department for duration of 3months.patients of either sex and ages in between 15-80years suffering from a psychiatric illness and started on atleast one psychotropic drug were selected. Patients below 15years age, pregnant and lactating women, patients who are not willing to co-operate, patients with intellectual disability were excluded from the study. 202 patients were enrolled for 3months study. The most affected gender was females (59.4%).commonly affected age group was between 26-35 years(30.6%).the average number of drugs per encounter for males is 3.158 and for females is 3.291.the percentage of drugs supplied form hospital pharmacy and percentage of drugs prescribed by generic names was 95.4%.all the drugs were prescribed from National Essential List Of Medicines (100%). Schizophrenia was the most commonly diagnosed psychiatric disorders followed by mood disorders. Antipsychotics (35.7%) are most commonly prescribed class of drugs followed by Benzodiazepines (21.2%), Olanzapine (19.2%) was most commonly prescribed antipsychotic drug. All the psychotropic drugs were prescribed from National Essential List Of Medicines. Atypical antipsychotics were prescribed more often than typical antipsychotics Owing to their fewer incidences of extra pyramidal side effects. Among atypical antipsychotics olanzapine was commonly prescribed.

Keywords: Drug utilization, psychotropic drugs, rational prescribing.

ABSTRACT

The purpose of this study was to formulate a stable parenteral formulation of Palonosetron HCl 0.05 mg/mL which is pharmaceutically equivalent to Reference Drug Product. Preformulation study was performed to evaluate the compatibility of product with materials which come in contact with the product during manufacturing. Compatibility study was carried out with metal, silicon tubes, PVDF filters and stoppers. Thermal cycling and photostabilty study were also performed to ensure the stability of the product. Palonosetron injection was formulated by dissolving the API and excipients in WFI in a S.S vessel under continuous stirring. Stability studies at different conditions were also performed. Compatibility study results indicate that drug product was compatible with the product contact materials. Thermal cycling and photostabilty data indicates that there was no significant degradation in the formulation. As a part of Sterilization cycle development, terminal sterilization was performed at 121⁰C for 15, 20 and 30 minutes time intervals and finalized cycle was 20 minutes. A stable Palonosetron Injection was developed and evaluated. Compatibility and accelerated stability studies at different conditions were performed and it can be concluded that the product is compatible with product contact materials, thermal and photostable.

Keywords: Palonosetron Hydrochloride, Compatibility Study, Thermal Cycling, Terminal Sterilization, Stability Study.

ABSTRACT

Hospitals are always acted as a source of infection to patients admitted to them. The terms hospital infection, hospital-acquired infection or nosocomial infection are applied to infections developing in hospitalized patients, not present or in incubation at the time of their admission. Such infection may become evident during their stay in hospital or, sometimes, only after their discharge. Approximately 5-10 % of patients admitted to acute care hospitals in developed countries, and more than 25% of such patients in developing countries, have been found to acquire infections which were not present or incubating at the time of admission. Such hospital-acquired, or nosocomial infections add to the morbidity, mortality, and costs that one might expect from the underlining illness alone. To fight these infections hospital personals employs many techniques and treatments to minimize the risk of certain infections. One of them is the use of antibiotics (like Meropenem) to prevent or control the spreading of such infections. Meropenem is an ultra-broad spectrum injectable antibiotic  used to treat a wide variety of infections. It is a beta lactum and belongs to the subgroup of carbapenem, similar to imipenem and ertapenem. Most hospital acquired pathogens show both sensitive and resistant results for Meropenem. So it is necessary to evaluate the minimum inhibitory concentration (MIC) of Meropenem which would help the doctors to treat the patients infected by hospital acquired pathogens in a distinctive manner. So for the evaluation of MIC of Meropenem we are using the E-Strip Method which is useful for quantitative determination of susceptibility of bacteria to antibacterial agents. The system comprises of a predefined quantitative gradient which is used to determine the Minimum Inhibitory Concentration (MIC) in mcg/ml of different antimicrobial agents against microorganisms as tested on appropriate agar media, following overnight incubation. Thus by this experiment we will be able to provide satisfactory data to the hospital personals for the treatment of hospital acquired infections using Meropenem.

Keywords: Minimum Inhibitory Concentration, Meropenem, E-Strip Method.

ABSTRACT

The present study was designed to investigate the neuroprotective effect of a flavonoid Morin Hydrate in 3-nitropropionic acid induced model of Huntington's disease.3-Nitropropionic acid was used to induce symptoms similar to that of Huntington’s disease in male wistar rats. Rats were treated with Morin (50 mg/kg and 100 mg/kg) for 14 days. Body weight, brain weight, behavioural parameters, biochemical parameters were assessed and brain samples were sent for histopathology.3-nitropropionic acid administration for 14 days significantly induced symptoms such as reduced body weight, impaired gait, locomotor activity, muscle grip strength and also caused oxidative stress in striatum. The treatment with Morin 50 mg/kg was less effective as compared to that of Morin 100 mg/kg. Morin (100 mg/kg)showed slightly reduced oxidative stress as well as motor coordination deficits. Histopathology results also revealed reduced neuronal degeneration in Morin (100 mg/kg) samples as compared to Huntington control (HC) rats. This evidence suggest flavonoid Morin might have protective effect against 3-Np induced huntington’s disease or disease like symptoms, and further studies on higher doses are needed to explore the usefulness of flavonoid Morin in HD.

Keywords: Huntington’s disease, 3-Nitropropionic acid, Morin Hydrate, Antioxidant, Neuroprotective

ABSTRACT

A novel polymer based on azobenzene-4,4’-diacetic allyl ester as core linker polycondensated with methyl methacrylate and n-butyl methacrylate was conveniently synthesized for the purpose of targeting colonic drug delivery. The cross linker was characterized by infrared spectroscopy, nuclear magnetic resonance and mass spectroscopy. The synthesized polymers (PMB) showed good film forming. Comparative study of synthesized polymers was done using In-vitro drug release pattern of budesonide from polymer coated capsule formulation in colonic media. Budesonide capsules coated with PMB1:1:2: B and PMB1:1:3: B showed maximum drug release in colon in a sustained release manner.

Keywords: colon specific drug delivery, azoreductase, diazo linker, allyl ester, budesonide.

ABSTRACT

Bioanalytical methods of Reverse Phase-High performance liquid chromatography (HPLC) was developed and validated for simultaneous estimation of Isoniazid (INH) and Ciprofloxacin Hydrochloride (CIP HCl) encapsulated in lipid polymeric hybrid nanoparticles (LPNs) in plasma and in organ homogenates of lung, liver, spleen and kidney of mice. Chromatographic separation was done using Agilent® C18 bonded silica column of dimensions 150 × 4.6 mm, 5μmwith flow rate 1.0 ml/min, injection volume 20 µland column temperature 40°C. The mobile phase consists of a mixture of 70 volumes of 0.1 percent v/v of trifluoroacetic acid(TFA) and 30 volumes of acetonitrile (ACN). The results indicated that the developed method was linear and selective for all matrices studied. Analysis of accuracy and precision showed adequate values, with relative standard deviation values lower than 5, which are in accordance with USFDA guidelines for bioanalytical method validation. Isoniazid (INH) and Ciprofloxacin Hydrochloride (CIP HCl) were stable in plasma and tissue homogenates under different storage and processing conditions. This method was applied to study the pharmacokinetic and biodistribution profile of both drugs in free form and in bound state with lipid nanoparticles. The results showed that polymeric nanoparticles showed higher drug accumulation in the target site i.e. lung as compared to non-target organs fulfilling our aim of developing a HPLC method for the simultaneous estimation of both drugs and their application in determination of pharmacokinetic and pharmacodynamic potential of the lipid nanoparticles.

Keywords: HPLC, bioanalytical, Tuberculosis, Stability, LOD

ABSTRACT

A simple and sensitive stability indicating HPTLC method has been developed and validated for estimation of Palonosetron hydrochloride. Separation of the drug was carried on aluminium plates precoated with silica gel 60 F₂₅₄ using Ethyl acetate: Methanol: Triethylamine (6:3:1 v/v/v) as mobile phase. The retention factor (R_f) for Palonosetron hydrochloride was found to be 0.50 ± 0.04. The detection was carried at 242 nm. Stress testing of Palonosetron hydrochloride was carried out according to the International conference on harmonization (ICH) guideline Q1A (R2). The drug was subjected to acid, base, neutral hydrolysis, oxidation, thermal degradation and photolysis. Palonosetron hydrochloride showed considerable degradation under oxidative condition. The method was successfully validated according to ICH guidelines Q2 (R1). The data of linear regression analysis indicated a good linear relationship over the range of 250–1500ng/band concentrations with correlation coefficient 0.994. The accuracy of the method was established based on the recovery studies. The LOD and LOQ were 11.81ng/band and 35.78ng/band respectively.

Keywords: Palonosetron hydrochloride, High Performance Thin Layer Chromatography (HPTLC), Validation, Stability-Indicating Method.

ABSTRACT

Diclofenac sodium (DF) niosomes was formulated by sonication method using various proportions of tween 40, span 40 and cholesterol. Each formulation (F1, F2 and F3) was evaluated for vesicle size, drug entrapment efficiency, release of drug, osmotic and rheological properties. F1 with high surfactant level 20 µmol % of each surfactant tween 40 and span 40 has high entrapment efficiency (90.1%), high retention for DF during storage at 4˚C, 304 nm vesicle size and 96% release for 12 hours. All formulations have shear thinning flow and membrane rigidity due to presence of cholesterol in their bilayer membrane. Hence, using niosomes as an oral drug delivery system for DF is feasible approach.

Keywords: DF; entrapment efficacy; niosomes; Vesicle diameter and Diclofenac.

ABSTRACT

Cefadroxil is a first generation cephalosporin antibiotic intended for oral administration. In the Present investigation, an attempt has been made to increase the therapeutic efficacy to reduce the frequency of administration and to improve the patient compliance by developing the sustained release matrix tablets of Cefadroxil by using direct compression method. Excipients like Xanthun gum, HPMC K 15 M, PVP K 30 are used as matrix polymers. MCC used as diluents, magnesium stearate as lubricant, and talc act as a glidant. The different excipients were tested for their compatibility with the drug Cefadroxil by using FTIR and DSC, which revealed that there was no chemical and physical interaction occurred. Then the Preformulation parameters like bulk density, tapped density, compressibility index, and Hauser’s ratio were analyzed for prepared powder before compression. The thickness of best formulation CF9 is 3.5mm, hardness of best formulation CF9 is 3.6kg/cm², friability of best formulation CF9 is 0.66%, weight variation of best formulation CF9 is 499±0.39.The In-vitro drug release were performed in the USP Apparatus (basket) using 0.1 N HCL as dissolution media at 50 rpm speed. The sample was done at periodic intervals of 1hr, 2hr, 3hr, 4hr, 5hr, and 6hrs and was replaced with equal volume of dissolution media to maintain the sink condition. The best In-vitro release shown by formula CF9 that is 95% .The results indicate that the selected formulation was stable during the period of accelerated stability studies. The optimized formulation CF9 compared with the marketed sample Cetil-500mg. Marketed sample in-vitro drug release is 98.85%. All evaluated formulations results were found to be satisfied.

Keywords: Cefadroxil, sustained release matrix tablets, xanthan gum, HPMC K15M, PVP K 30.

ABSTARCT

Solanum spirale is a tribal medicinal food plant which is used among the Adi tribes of Arunachal Pradesh, India. The methanol extract of shoot and berry were studied for their total phenolic (Folin-Ciocalteu’s method) and total flavonoid contents (colorimetric method) to study antioxidant potential ((DPPH & ABTS). The extracts were recorded to contain considerable amounts of phenolic content (18.64±2.12 mg GAE/g) in shoot and 11.72±1.42 mg GAE/g) in mature berry and flavonoid content of (5.29±1.01 µM RE/g) in shoot&50.52±1.03 µM RE/g) in mature berry and antioxidant potentials were calculated as 29.85±1.25 µM/g in the ABTS assay of shoot and38.27±1.33µM/g in the ABTS assay of berry while 45.4±0.37µM/g in the DPPH assay of shoot and 52±0.92 µM/g in the DPPH assay of mature berry respectively. This work also discourse traditional use of Solanum spirale among Adi tribes of Arunachal Pradesh.

Keywords: Solanum spirale, total phenolic, flavonoid content, antioxidant potential, tribals, medicinal food, ethnobotany.

ABSTRACT

The aim of the study was to prepare and evaluate topical gels incorporating liposomes of Dexamethasone base. Multilamellar vesicular (MLVs) liposomes were prepared using thin film hydration method. By subjecting MLVs to sonication using Ultra homogenizer, SUVs were formed. Liposomes were composed of soya lecithin, cholesterol, and dexamethasone. Using these method different concentrations of dexamethasone liposomes were prepared and were successfully incorporated in 1% carbopol gels. Liposomes were characterized for their particle size using zeta sizer and entrapment efficiency by dialysis method. SUVs were evaluated for in vitro release. Viscosity of gel formulations was measured using Brookfield viscometer, Drug lipid compatibility was performed using FTIR spectroscopy. Liposomal gels were evaluated for in vitro release studies, ex-vivo permeation studies and pharmacodynamic studies (Anti-inflammatory activity). Results showed more localized and sustained effect with Liposomal dexamethasone gels than dexamethasone gel formulation.

Keywords: Dexamethasone, Liposomal gel, Multilamellar vesicles, Small unilamellar vesicles, Anti-inflammatory activity.

ABSTRACT

Skin is the protective layer of the body exposed to environmental pollution hence, it is essential to protect the skin .The skin on face can be protected by applying various cosmetics intended specially for facial application. It can be a cream, lotion, face mask or peel off mask etc. Peel off mask can be used as the remedy to treat facial skin related problems such as wrinkles, ageing, acne and it can also be used to close the pores. The open pores can cause deposition of dust and result in white heads. Peel off mask can be used for cleansing and moisturizing the skin. Most of the face peel off mask is prepared by polymers which can form thin layer on face. Peel off mask is available in gel form and as dry form. Dead skin cells can be removed by applying peel off mask. Mask can remain on the face for 5-30 minutes, the duration can be varied depending on the ingredients used. Some peel off mask required whole night for better result. It can be prepared with synthetic and herbal ingredients. In this work, the peel off mask was prepared with herbal ingredients such as apple, apricot, orange peel, cucumber, beetroot and other ingredients like polyvinyl alcohol, propylene glycol, polyethylene glycol 400, methyl paraben, lactic acid and water. The preparation was evaluated for its physical characteristics and it was found to have the entire desired characteristics of a peel off mask.

Keywords: Peel off mask, herbal, Acne, apple, walnut, cucumber, orange peel.

ABSTRACT

The present study was designed to assess the blood electrolytes (Sodium, potassium, chloride, calcium and phosphate) values in healthy volunteers and some malaria patients of males and females categories and to compare between them. The study aimed to examine possible changes in electrolyte levels of healthy volunteers and malaria patients in University of Port Harcourt Teaching Hospital. The subjects were 120 healthy staff and student adults between 18-50 years of the University community and 120 patients of the University teaching hospital randomly selected. 5mls of blood sample were collected separately from ante cubital vein of each of the study subjects. The serum electrolytes determined were sodium, potassium and chloride (Ion Selective Electrode method); calcium (Randox method) and phosphorus (Phosphomolybdate method).  Measurements of results were analyzed using statistical data analysis. The mean values of Sodium, potassium, chloride and calcium in healthy volunteers were higher compared to those of malaria patients. Phosphorous were higher in the malaria patients compared to the healthy volunteers. The results obtained showed a significant difference at p < 0.05 significant level between healthy and malaria individuals for various blood electrolytes. We can thus conclude that healthy volunteers and malaria patient blood electrolytes is significantly different.

Keywords: Electrolytes, serum, malaria

ABSTRACT

A sensitive static headspace gas chromatographic method using flame ionization detector was developed and validated for the estimation of Allylamine in Sevelamer hydrochloride tablet dosage form. The chromatographic separation was achieved on capillary column Rtx-5 Amine (30m×0.53mm×1.0μm) with 5% diphenyl/95% dimethyl polysiloxane stationary phase. The critical experimental parameters such as, diluents, columns and sample preparations were studied and optimized. The method was validated as per United States Pharmacopoeia (USP) and International Conference on Harmonization (ICH) guidelines in terms of detection limit, quantification limit, linearity, precision, accuracy, specificity, solution stability and robustness. The method was found to be linear in the range between 10 μg/mL and 75 μg/mL with a correlation coefficient (r2) of 0.99984. The detection and quantification limits obtained for Allylamine were 3.3 μg/mL and 10.0 μg/mL w.r.t sample concentration respectively. The recovery obtained for Allylamine was between 100.0% and 110.0%. The developed method was applied successfully for the estimation of Allylamine in Sevelamer hydrochloride tablet dosage form.

Keywords: GC-HS, Allylamine, Validation, Sevelamer hydrochloride tablets.

ABSTRACT

Sthaulya simply is the increased physical Guruta of body. It is Kaphaj Nanatmaj Vyadhi. Sthaulya can be described as “Medo roga, Medovriddhi, Medasvi and Ati- Sthaulya. Sthaulya can be described as having heaviness and bulkiness of body due to extensive growth or abnormal increase of Medodhatu resulting in to pendulous appearance of buttocks, belly, and breast with decrease in energy level.  Yogratnakar had described the Tryushanaadi Lauha in the management of Sthaulya. A clinical trial was done with Tryushanaadi Lauha on randomly selected 15 clinically diagnosed patients of Sthaulya to know the efficacy of trial drug. Tryushanaadi Lauha has highly significant result in Sthaulya.

Keywords: Kapha Dosha, Sthaulya, Tryushanaadi Lauha

ABSTRACT

Mycobacterial enoyl acyl carrier protein reductase (InhA) is a clinically validated target for the treatment of tuberculosis infection, a disease that still causes the death of at least a million people annually. The current study aims to design and explore the possible mechanism of action of various furfuraldehyde formazans as direct inhibitors of InhA through molecular docking studies. A series of furfuraldehyde formazans were computationally designed and energy minimized. These compounds were docked into the active site of InhA (PDB code, 2NSD) using software Glide from the suite of Schrödinger. These compounds were identified as potential inhibitors of InhA on the basis of Glide Score (G-Score), hydrogen bonding (H-bond) and van der Waals (vdw) interaction between ligand and the receptor. Ten furfuraldehyde formazans displayed G-Scores (-7.351 to -9.148) higher than that of isoniazid (-7.250). These compounds have good hydrogen bonding and hence good affinity for the enzyme, when compared with isoniazid. Further, we plan to synthesize these compounds and screen them for antimycobacterial and enzyme inhibitory activity.

Keywords: Tuberculosis, InhA, Furfuraldehyde, Formazans, Glide.

ABSTRACT

The present study is a simple, fast, precise, selective and accurate RP-HPLC method was developed and validated for the simultaneous determination of Irbesartan and Atorvastatin from bulk and formulations. The proposed method was developed by HPLC Shimadzu Separation Module with PDA/UV detector connected to Empower-2 software using Inertsil C₁₈ ODS (4.6 x 250mm, 5mm) with an injection volume of 20 µl was injected and eluted with a mobile phase composition of Methanol: Acetonitrile (50:50), which is pumped at a flow rate of 0.8ml/min and detected by PDA detector at 245nm. Ambient column temperature has maintained. The total run time was 10mins.The retention time of Irbesartan and Atorvastatin were found to be 2.9 min. and 4.1 min respectively. Linearity was observed in the concentration range of 0.2-0.8mg/ml for Irbesartan and Atorvastatin respectively with correlation coefficient 0.999 for both the drugs. Percent recoveries obtained for both the drugs were98.0-101.50%, respectively. The method was validated according to the ICH guidelines with respect to specificity, linearity, accuracy, precision and robustness. The method developed IRB be used for the routine analysis of Irbesartan and Atorvastatin from their combined dosage form.

Keywords: Irbesartan and Atorvastatin; Isocratic Elution; RP- HPLC Method; Forced degradation studies; PDA Detector; Tablet dosage forms.

ABSTRACT

In the present study we have developed a non-effervescent gastro retentive dosage form containing pantoprazole sodium by emulsion solvent diffusion method. A 2³ full factorial design was used for the optimization process and the various responses obtained were evaluated by fitting in the binomial equations. Formulations ERS 1-8 were made utilizing three independent variables such as amount of crospovidone (%), Eudragit^®E100 (mg) and Eudragit^®RS100 (mg) which were varied at low and high levels and are evaluated for percentage buoyancy, entrapment efficiency and cumulative drug release after 5 h in buffer pH 2.2. The experimental values of the optimized formulation ERS-O coincides well with the predicted values obtained from optimization technique. Design expert 9.0.3 predicts responses as % buoyancy of 75.04±0.05, % entrapment efficiency of 87.57±0.21 and cumulative drug release after 5 h of 97.93±0.15 which were close to the actual values validates the design. The optimized formulation were in size range 20-120 µm with spherical shape, internal hollow cavity and porous boundary wall, moreover only physical cross-linking occurred with zero order release pattern and the in vivo analysis through ethanol induced ulceration method gave better ulcer healing orally than the intravenous route.

Keywords: Emulsion solvent diffusion method; Non effervescent; Gastro retentive drug delivery; Gastric residence time; Anti-ulcer activity

ABSTRACT

Novel pyrano quinolone derivatives were synthesized by the treatment of p-methyl acetanilide upon treatment with DMF and POCL₃ at 0⁰ C it undergone cyclization reaction which gives 2-chloro-6-methyl quinolone-3-carbaldehyde and further treated the reaction with 4M HCL gives 2-hydroxy-6methyl quinolone-3-carbaldehyde is formed. The above reaction further treated with ethyl aceto acetate and piperidine by using grind stone technique with the elimination of ethanol and water gives 3-acetyl-7-methyl-2H- Pyrano[2,3-b] quinolone-2-one. The above reaction was further treated with 40% KOH and ethanol with different substituted aldehyde to give novel pyrano quinoline derivatives. Compounds which are synthesized are identified by MP and TLC as well as characterized by IR, ¹HNMR and MASS spectroscopy. Docking studies were performed for anti-malarial activity using Plasmodium falciparum lactate dehydrogenase for a selected compounds shows good binding energy when compared to Chloroquine which is used as standard.

Keywords: Vilsmeier Hacck reagent, pyrano quinolones, docking.

ABSTRACT

The objective of the study is to compare the analytical performance in terms of precision and accuracy of three methods viz., Immunoturbidimetry (IT), Capillary Electrophoresis (CEP) and High Performance Liquid Chromotography (HPLC) for the measurement of glycosylated haemoglobin (HbA1c). A total of 40 routine patients samples were used for the estimation of HbA1c using the three methods and the results obtained were correlated between the three methods. The correlation coefficient ‘r’ obtained between IT & CEP, IT& HPLC and CEP & HPLC were 0.96, 0.95 & 0.99 respectively, indicating that an ‘r’ value of 0.99 obtained between CEP & HPLC is in agreement with the CLIA guidelines value of > 0.98,while poor ‘r’ values of 0.96 and 0.95 were obtained when IT method was compared with both CEP and HPLC methods. As per this study both CEP & HPLC methods gave good precision and accuracy for Bio-Rad controls. Further, CEP and HPLC methods have provisions to identify interference by Haemoglobin variants present in patient sample. The outcome this study recommends the use of one of the two methods viz., CEP and HPLC for routine measurement of HbA1c.

Keywords: HbA1c, Immunoturbidimetry, Capillary Electrophoresis, HPLC.

ABSTRACT

Two novel methods having requisite precision, accuracy, specificity and robustness were developed and validated for quantitative determination of Apixaban in pharmaceutical dosage forms. The first method was based on isocratic reverse phase liquid chromatography using Sunfire C18, 150mm×4.6mm, 5µ and mobile phase consists of Buffer: acetonitrile (60:40) at a flow rate 1ml/min and detection was achieved photodiodide array detector set at 280 nm. The response was linear range of 5-50 µg/ml (R² =0.9998). The second spectrophotometric method involves detection at 280 nm. The calibration curve range between 5-50 µg/ml (R² =0.9999). Validation of method was carried out fulfilling ICH guidelines. Both the methods were applied without any interference from excipients, for determination of drug in coated tablets. It is suggested that the proposed HPLC and UV spectrophotometric methods could be used routine quality control and dosage form assay of Apixaban.

Keywords: HPLC, UV Spectrophotometry, Apixaban, Method development, Validation.

ABSTRACT

Poisonous plants may be a threat to the health and safety of people and animals. It makes crucial to have knowledge about surrounding poisonous plants. Information gathered by generating database of poisonous materials from any particular region may be life saving. Chemical analysis of these plants is another important aspect especially for forensic experts solving crime cases involving poisonous plants. Therefore this paper has also conducted Thin Layer Chromatographic separation of poisonous plants. A wide diversity of plants could be seen in and around Rohtak city of Haryana but literature survey didn’t reveal any significant information about the poisonous plants from this area. Therefore, the present study has inspected occurrence of some poisonous plants throughout Rohtak city and their chromatographic analysis. Importantly the results have been of great utility. Morphological examination identified ten poisonous plants vis. Thevetia peruviana, Nerium odoratum, Calotropis procera, Ricinus communis, Datura fastusa, Argemone mexicana, Ipomea marginate, Crinium asiaticum, Plumeria obtuse and Abrus precatorius from different localities of the selected area.  A new single solvent system chromatographically separating all these poisonous plant extracts has also been developed.

Keywords: Poisonous plants, Thin Layer Chromatography, Forensic science.

ABSTRACT

Several 1-aryl-5-hepta-O-benzoyl-β-D-lactosyl-2-S-benzoyl-2, 4-isodithiobiurets have been synthesized by the interaction of hepta-O-benzoyl-β-D-lactosyl isothiocyanate with several 1-aryl-S-benzyl isothiocarbamides. These compounds were screened for their antibacterial and antifungal activities against–Escherichia coli, Proteus vulgaris, Staphylococcus aureus, Salmonella typhimurium, Klebsiella pneumonie, Psudomonasaeruginosa, Aspergillus niger and Candida albicance.  The newly synthesized compounds have been characterized by analytical and IR, ¹H NMR and Mass spectral studies. These compounds show appreciable activity towards these microorganisms.

Keywords: Lactosyl isothiocyanate, 1-aryl-S-benzyl isothiocarbamides, isodithiobiurets and antimicrobial activity.

ABSTRACT

Phytochemical are compounds derived from natural source play important role in mankind health system with various physiological activities such as antioxidant and thrombolytic activity. Borago officinalis leaves have been assessed for quantity of antioxidant compounds comprise in estimation of total phenolic, total flavonoid and total tannin contents, and thrombolytic activity of hydrolacholic leaves extract at different concentration ranges. The hydroalcholic extract of leaves showed low phenolic contents about (26.45 ± 0.126 mcg GAE\g DW) with approximately similar quantity of total flavonoid and total tannin contents about (212 ± 0.278 mcg QE\g DW) and (216 ± 0.521 mcg GAE\g DW), respectively. Leaf extract exhibited a dose dependent manner thrombolytic activity ranges between (8.346± 0.669 - 44.6697±1.1076) considered significant in comparison with control negative distilled water (p value < 0.0001) and moderate activity in comparison with control positive streptokinase. Borago officinalis leaf was a good source for antioxidant compounds and open a venue for production of thrombolytic agents from the leaf with less side effects in comparison to the conventional drugs.

Keywords: Borago officinalis, thrombolytic activity, total phenolic content, total flavonoid contents, total tannin contents.

ABSTRACT

Development of amphiphilic drug-lipid complexes is a potential approach for improving delivery of the drugs by increasing solubility, release profile and oral bioavailability. Rutin, a polyphenolic flavonoid, shows several biological effects like capillary protectant, anti-oxidant, anti-inflammatory, anti-aging, cardio-protective, anti-thrombotic and neuroprotective, but its use is limited due to its low aqueous solubility. To overcome this limitation, phospholipid complex of Rutin was developed to improve its aqueous solubility for better absorption through the gastrointestinal tract and this might result in improved bioavailability. The Rutin phytosomes prepared by solvent evaporation method using different ratios of Rutin and Soybean phosphatidylcholine (1:1, 1:2 and 1:3) was evaluated for percentage yield, compatibility studies by infra-red spectroscopy, particle size, poly dispersity index, zeta potential, drug content and were found to be within the acceptable range. Surface morphology by scanning electron microscopy, solubility studies, in-vitro drug release and stability studies also were carried out. The phospholipid complex of Rutin was found to be fluffy and porous with rough surface. The water solubility of Rutin was improved from 0.058mg/ml to 0.475 mg/ml in the prepared Phytosomes. The in-vitro drug release studies showed that there is no drug release from pure drug and F1 formulation up to 120min in acidic buffer pH 1.2; while in phosphate buffer pH 7.4 showed releases about 49.3% and 92.85% respectively, which indicates the significant enhancement of dissolution of Rutin phytosomes compared to pure drug. Stability studies suggested that the formulations were stable. In this study, Phytosomes could be successfully tailored for Rutin with improved dissolution characteristics which is promising for lowering the influence of exogenous factors and increasing drug delivery.

Keywords: Rutin, Soybean phosphatidylcholine, Phytosomes, Solubility.

ABSTRACT

The purpose of the study was to prepare and evaluate liposomes containing Artemether, a lipophilic drug having short half life of 2-3hrs after oral administration. Thin film hydration method was used for the preparation of artemether-encapsulated conventional and PEGylated liposomal suspensions using various drug: lipid ratio and their characteristics, such as particle size, zeta potential, encapsulation efficiency, and in vitro drug release were investigated. The drug encapsulation efficiency of PEGylated liposomes was high when compared to conventional liposomes. The average particle size of both conventional and PEGylated liposomes was obtained in nanometers with PDI ranging from 0-0.356. Zeta potential of conventional liposomes was found to be more negative when compared to PEGylated liposomes. In-vitro drug diffusion studies was carried for period of 16 hrs where PEGylated liposomal formulation showed more sustained release compared to conventional liposomes. The conventional and PEGylated liposomal formulations followed zero order and Higuchi kinetics respectively. The artemether containing liposomes were successfully formulated and evaluated.

Keywords: Artemether, thin film hydration, liposomes, conventional, PEGylated.

ABSTRACT

Ayurveda, being as ancient system of medicine, which comprises hundreds of Kalpanas of pharmaceutical preparations but only few of these Kalpanas are in practice. In this modern era many good preparations have been extinguished in the passage of time among these, Varti Kalpana is main one. Now-a-days, when human life is very fast, we should be ready to make necessary changes in our science according to the need of hour. In present study Nimbadi Yonivarti is selected for the management of Swetapradara which has been mentioned as Anubhuta Yoga by Vd. Devisharan Garga Ayurveda Upadhyaya in “Nari Roganak. The present study was aimed at setting up a standard profile of Nimbadi Yonivarti which was prepared using pharmacognostically authenticated raw drugs followed by subjecting it to detailed pharmacognostical, physicochemical and phytochemical (including Thin Layer Chromatography) analysis as per standard protocol. The observations were systematically recorded. Pharmacognostical findings (crystals, epicarp cells, trichom, etc.) confirm the ingredients present in the finished product. Identified phytochemical components (Carbohydrates, tannins, fanolic compound, glycosides, steroids, flavonoids.etc.) support the intended action of the formulation in vaginal discharge.

Keywords: HPTLC, Pharmacognosy, Phytochemistry, Nimbadi Yonivarti, Shwetapradara.

ABSTRACT

In the present study a series of 3-(2-Hydroxy-3, 5-dichlorophenyl)-5-(4-chloro phenyl) isoxazole (8a) and 3-(2-Hydroxy-3, 5-dichlorophenyl)-5-(2, 4-chloro phenyl) isoxazole (8b) have been synthesized by refluxing the chalconedibromide (6a) and (6b) with hydroxyl amine hydrochloride in ethanol containing catalytic amount of piperidine. The formation of the above synthesized compounds was confirmed on the basis of their chemical tests and spectral analysis. The synthesized heterocycles then screen for their antimicrobial activity against some kahrip plant pathogens viz. AlternariaMacrospor, XanthomonasCampestris, Pseudomonas syringae and Fusarium Spp. From the above study the result revealed that isoxazole derivatives shows good to moderate antimicrobial activity against plantpathoges.

Keywords: Chalcones, chalconedibromide, plant pathogens, antimicrobial activity, isoxazole.

ABSTRACT

The present study was undertaken to evaluate the hydroalcoholic extract of seeds of Citrullus lanatus for its protective effect on gentamicin-induced nephrotoxicity in rats. The eight study groups contained six rats in each group. Nephrotoxicity was induced in male Wistar rats by subcutaneous administration of gentamicin 80 mg/kg.bd. wt. for nine days. Based on acute toxicity studies, doses of extract selected were 200 and 400mg/kg bd.wt. and administered orally for ten days. Effect of hydroalcoholic extract on gentamicin induced nephrotoxicity was determined using blood urea nitrogen, serum creatinine, serum total protein levels and urinary total proteins and urinary creatinine as indicators of kidney damage. Anti-oxidant studies were carried out and histological studies were also conducted in kidney tissue. Gentamicin induced nephrotoxicity which was indicated by increased levels of blood urea nitrogen, serum creatinine, serum total proteins, urinary total proteins and urinary creatinine levels. Extract alleviated the gentamicin-induced effects on serum markers and urinary functional parameters. Dose dependent decrease in LPO levels and increased levels of catalase, superoxide dismutase, glutathione also supported the nephroprotector activity of extract. In histopathological studies gentamicin induced nephrotoxicity was indicated by degenerative changes in kidney tissues, congestion with hemorrhages where as marked regenerative changes were observed in kidney sections of animals which received higher dose of the extract. Present study reveals that the hydroalcoholic extract of seeds of Citrullus lanatus attenuated the nephrotoxicity induced by Gentamicin in rats.

Keywords: Citrullus lanatus, Gentamicin, Nephroprotector activity, Anti-oxidants.

ABSTRACT

The aim of this study is to develop and characterize a solidified self-emulsifying formulation of glimepiride, and to compare its in vitro drug release profile to a commercially available tablets. Several self-emulsifying formulations (SEF) were prepared by selecting different combination from constructed pseudoternary phase diagram. Selected formulations SEF1, SEF2 and SEF3 were solidified using crospovidone and evaluated. Following emulsification, the optimized formula was selected to have the smallest mean particle size and the highest absolute zeta potential, which should yield the formation of a stable emulsion and its superiority in dissolution characteristics. Particle size and distribution of SEF1, SEF2 and SEF3 were 423.36nm, 159.128nm and 115.899nm respectively. Zeta potential analysis revealed  that SEF3 had highest zeta potential – 43.78mV followed by -39.2mV (SEF2) and -39.08mV (SEF1). In vitro drug release in 30 min of formulation SEF1, SEF2 and SEF3 were 75.31%, 83.48% and 93.03% respectively. Which indicated superiority of SEF3. In vitro studies were also performed to compare the optimized formula, SEF3, to a commercially available Betaglim tablet. T_50% of glimepiride in SEF3 and betaglim was found to be 7 min and 22 min respectively. Which indicated a significant improvement in glimepiride release characteristics. SEF3 was found to be stable under stressed conditions. However slightly increased globules size of sample stored at accelerated storage condition for 12 weeks was observed.

Keywords: Self-emulsifying drug delivery system, glimepiride, crospovidone, in vitro.

ABSTRACT

Qualitative analysis of phytochemical screening of P. florida and P. djamor mushroom fruit body was studied. Nine solvents viz: 20% Methanol, Ethanol, chloroform, Ethyl acetate, Petroleum ether, Acetone, Hexane, Benzene, and Water were used to obtain extracts from fruit body powders of mushroom parts. The extracts were subjected to qualitative phytochemical screening using standard procedures. Result showed that nine phytochemicals screened were present. They are alkaloids, Carbohydrates and Proteins, present in all extract of both sample. However Tannins, Oxalate, phenols, quinones, were absent in both sample in all extracts. Flavonoids, sterols present in 3 extracts (i.e) methanol, ethanol, acetone and 2 types of sample solvent extracts. The diversity of phytochemicals found present suggests that P. florida and P. djamor could serve as a source of useful drugs.

Key words: Pleurotus florida, Pleurotus djamor ,phytochemical, different solvent extracts.

ABSTRACT

Biochemical changes during in vitro root formation in Tribulus terrestris were investigated in the callus derived from nodal explants on Murashige and Skoog’s (MS) medium supplemented with 1.0 mg/l 2,4-D+ 0.5 mg/l Kinetin. The callus maintained on MS medium fortified with 2.0 mg/l 2, 4-dichlorophenoxy acetic acid (2,4-D) + 0.5 mg/l Kinetin. The above callus subcultured on Murashige and Skoog’s (MS) medium + 2.0 mg/l α-naphthalene acetic acid (NAA). Metabolites like starch and total; soluble sugars decreased while reducing sugar, total phenol and total protein increased during root differentiation in callus. Enzyme activity viz. α-amylase, acid invertase, peroxidase and acid phosphatase increased during root differentiation.

Keywords: Tribulus terrestris Linn, Biochemical changes, Rhizogenesis, Callus.

ABSTRACT

Present study circumspects synthesis of some 2, 4, 5-triaryl substituted analogues of imidazole and their spectral characterization by means of IR and ¹H NMR. The compounds were screened for antibacterial activity against standard strains of both Gram positive and Gram negative bacteria. Results obtained establishes compounds IM3 and IM4 to be significantly responsive against different bacterial strains and as such these compounds can pave the way for development of potent antibacterial agents.

Keywords: Imidazole, Aryl aldehydes, Antibacterial, Cup-plate method

ABSTRACT

Michelia champaca, a healthful plant and it's normally utilized in people medication to treat varied diseases. The aim of the study was to evaluate the hepatoprotective & invivo antioxidant activities of Michelia champaca against carbon tetrachloride induced liver injury in rats. The methanol extract of Michelia champaca at dose of 250 and 500 mg/kg were administered orally once daily for seven days. Serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), total bilirubin (TB), alkaline phosphatase (ALP), lactate dehydrogenase (LDH) and total protein (TP) were estimated from serum. In-vivo antioxidant activity of methanol extract of Michelia champaca was evaluated by various assays including catalase (CAT), superoxide dismutase (SOD), reduced glutathione, glutathione peroxidase (GPx), glutathione reductase (GRD) and malondialdehyde (MDA) levels in liver tissues. Histopathological examination of the liver sections was carried out to support the induction of hepatotoxicity. The results of the study indicated that, methanol extract of Michelia champaca 500 mg/kg showed a major decrease in SGPT, SGOT, TB, ALP, LDH levels that were all elevated within the carbon tetra chloride treated group. The Michelia champaca extract showed considerably redoubled the degree of CAT, SOD, GSH, GPx, GRD and reduce the degree of MDA. Michelia champaca leaves extract therapy also protective effects against histopathological alterations. From the above study it can be concluded that methanol extract of Michelia champaca had hepatoprotective & antioxidant activities against carbon tetra chloride induced hepatic damage in experimental animals.

Keywords: Michelia champaca, carbon tetra chloride, hepatoprotective, antioxidant activity.

ABSTRACT

The concept of the sintering technique in the pharmaceutical sciences is relatively new.The objective of the present study was to prepare and evaluate thermally sintered gastro retentive floating matrix tablets of Atazanavir sulphate. The formulations were prepared by direct compression method using EC N100 and HPMC K100 as polymer. The prepared tablets were exposed at two different temperatures like 50⁰C and 60⁰C for two different periods like 1.5 hr and 3 hr in a hot air oven. Effects of sintering conditions were studied on in vitro dissolution studies, hardness, friability, floating lag time and total floating time. The sintering temperature and the sintering time markedly affected the drug release properties. The release rate of the drug was inversely related to the sintering temperature and the sintering time. The hardness was increased with increase in sintering temperature and duration of sintering; but friability of tablets was found to be decreased with increasing sintering time. Floating lag time was inversely proportional to the sintering temperature and sintering time, whereas total floating time was directly proportional to the sintering temperature and sintering time. The formulation F2 sintered at 60⁰ for 3 h was selected as an optimized formulation based on the drug retarding properties and the optimized formulation followed Fickian diffusion mechanism with Korsmeyer-Peppas release kinetics. FTIR and DSC studies were used to characterize the optimized formulation and those studies showed no evidence on interaction between the drug and polymer used.

Keywords: Sintering, Gastro retentive, Floating, Atazanavir sulphate (ATZ).

ABSTRACT

Nimesulide is a selective Cyclooxygenase - 2 enzyme inhibitor useful in inflammatory conditions. It belongs to class 2 of Biopharmaceutical classification system (BCS), which has very low water solubility leading to low oral bioavailability. The objective of present study was to enhance the solubility and dissolution rate of poorly soluble model drug, nimesulide. For the same purpose, two approaches were used. First approach includes Electrospinning technique, and the second approach is co-grinding technique. In Electrospinning technique, the solution containing drug and polymer (PVP K-90) dissolved in an organic solvent was taken and made in to nanofibers of different drug- polymer ratios (1:1, 1:2, 1:3, 1:4, 1:5) using electro-spinning apparatus. In the co-grinding technique, mixtures with different ratios (1:1, 1:3, 1:5, 1:7, 1:9) of drug and carrier were prepared employing potato starch, lactose, microcrystalline cellulose, sodium starch glycolate and treated agar as carriers. Of the two approaches, nanofibers provided a better solubility enhancement when compared to co-grinding mixtures and pure drug. The optimized formulation (nanofibers) was characterized by Fourier transform infrared spectroscopy (FTIR), Scanning electron microscopy (SEM), Differential scanning calorimetry (DSC) and the in-vitro dissolution rate studies. The optimized nimesulide nanofiber formulation displayed nearly 50- fold faster dissolution compared to the pure drug and the optimized co-ground mixture. It has also shown two to three- fold greater anti-inflammatory activity in Wistar albino rats as compared to pure drug. Hence, nanofibers produced by electrospinning technique provided a scope for enhancing the solubility and dissolution rate by encapsulating poorly water soluble drugs within the polymeric matrix leading to potential bioavailability enhancement through the oral or topical routes.

Keywords: Electro-spinning, Nimesulide, Dissolution rate enhancement, nanofibers.

ABSTRACT

A simple, accurate and stability indicating high performance liquid chromatographic (HPLC) method was developed for the simultaneous estimation of Torsemide and Spironolactone in combined dosage form. Isocratic RP-HPLC separation was achieved on Kromasil RP- C18 column (250mm×4.6mm; 5µm) using methanol: acetonitrile: water in the ratio of 50:30:20 (v/v), pH6.8, at flow rate of1.0ml/min at ambient temperature. Quantization was achieved by UV detection at 235nm over the concentration range of 10-60μg/ml for torsemide and 25-150μg/ml for spironolactone with percentage recoveries of range 99.688-101.792 and 98.282-101.811for torsemide and spironolactone respectively. Different stress degradation studies like acidic, alkaline, peroxide, thermal etc were measured for both standard drugs and results found that the stress degradation conditions doesn’t affect the elution of the both the drugs and hence the developed method was found to be stability indicating method.

Keywords: Torsemide, Spironolactone, RP-HPLC estimation, forced degradation studies.

ABSTRACT

The research involve formulation and evaluation of three different ophthalmic solutions of Ketorolac tromethamine with three different amino acid transporters. The prepared formulations were subjected to ex-vivo transcorneal permeation and cornea hydration studies through excised goat cornea and the results were compared with those of a prepared standard Ketorolac tromethamine ophthalmic solution. The trans corneal permeation studies were carried out by using an all glass Franz diffusion cell. The non-steroidal anti-inflammatory drug Ketorolac tromethamine ophthalmic solution is indicated for the temporary relief of ocular itching due to seasonal allergic conjunctivitis and also for the treatment of inflammation following cataract surgery. In the study, the three amino acid transporters used were Lysine, Phenylalanine and Valine which are responsible for protein synthesis and play a significant role in the process of maintaining structural and functional integrity of conjunctiva and retina. The results obtained from the permeation studies of conjugated physical mixtures of Ketorolac tromethamine with different amino acid transporters across the excised goat cornea were observed to exhibit enhanced permeation when compared with the permeation of Ketorolac tromethamine from the standard formulation.

Keywords: Ex-vivo, corneal permeation, conjugation, transporters and Ketorolac Tromethamine.

ABSTRACT

A simple, economic, rapid, high range and accurate stability indicating RP-HPLC method was development for simultaneous estimation of Azithromycin and Ambroxol Hydrochloride in their combined tablet dosage form. This method was carried out by using Isocratic peak HPLC instrument with kromasil C-18 Column (250 mm X 4.6mm,5um) with mobile phase consisting a mixture of Methanol: Acetonitrile: Phosphate buffer in the ratio of 70:20:10 (v/v), at a flow rate of 1.1 ml/min with UV detection at 221nm . The retention time for Azithromycin and Ambroxol Hydrochloride are 9.08 and 5.39min respectively. Suitability, specificity, linearity, accuracy, precision, stability, and sensitivity of this method for the quantitative determination of the drugs were proved by validation in accordance with the requirements laid down by International Conference on Harmonization (ICH) Q2 (R1) guidelines. To establish stability indicating nature of the LC method, forced degradation of drug substances was performed under stress conditions like thermal, oxidation, peroxide, UV light, acid and base hydrolysis) The limit of quantification (L.O.Q) for Azithromycin and Ambroxol Hydrochloride are found to be 0.70ug/ml 1.00ug/ml.Then the limit of detection (L.O.D) for Azithromycin and Ambroxol Hydrochloride are found to be 0.15ug/ml and 0.3ug/ml respectively. The results of the study showed that the proposed method is reliable and robust and can be used as quality control tool for the estimation of these drugs in combined pharmaceutical solid dosage forms.

Keywords: Azithromycin, Ambroxol Hydrochloride, RP-HPLC method, Validation.

ABSTRACT

The present research has been undertaken with the aim to formulate and evaluate the low cost herbal gel containing Rubia cordifolia root extract. The gel formulation was designed by using ethanolic extract of Rubia cordifolia root in varied concentrations (750 mg, 1000 mg&1250 mg) and evaluated using physiological measurements. The gel was prepared by using various polymer bases (HPMC K4, HPMC K15, and Carbopol 934). Among them Carbopol 934 has given better gel formation. The gel was prepared by using Carbopol 934, Rubia cordifolia root extract, Propylene glycol 400, Methyl paraben, Propyl paraben and required amount of distilled water. Then skin pH (6.8-7) was maintained by drop wise addition of triethanolamine. The physiochemical parameters of formulations (pH, viscosity, spreadability etc.) were determined. Stability studies have carried out as per ICH guidelines for 3 months at different temperatures and humidity. The results showed that formulation containing 750 mg Rubia cordifolia root extract have better stability than other formulation. Further all formulations have studied for skin irritation on animal model (Rabbit) and result showed that there was no skin irritation to animals.

Keywords: Rubia cordifolia, root extract, Carbopol 934, Gel and ICH guidelines.

ABSTRACT

A sensitive and selective RP-HPLC method is described for the determination of stability in Acetaminophen and Tramadol dosage forms. Chromatographic separation was achieved on a C₁₈ column using mobile phase consisting of a mixture of mixed Phosphate buffer pH: 3.4 Acetonitrile (30:70v/v/v), with detection of 236nm and flow rate at 1mL/min. Linearity was observed in the range 100-300 µg /ml for Acetaminophen (r² =0.994) & 10-30µg /ml for Tramadol (r² =0.994) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim. No chromatographic interference from tablet excipients was found. The proposed methods were validated. The force degradation of the drugs was assessed by different environmental conditions. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.

Keywords: Stability indicating, RPHPLC, Acetaminophen, Tramadol.

ABSTRACT

Lornoxicam is a non steroidal anti-inflammatory drug of oxicam class and it has the same side effects of this group when taken orally and has a relatively short plasma half-life (3 to 4 h) which makes it a good candidate for colon targeting. It could avoid the systemic side effects, enhance its low oral bioavailability due to hepatic first pass metabolism and delay drug release to target the colon. Eighteen tablet formulations of lornoxicam were prepared by wet granulation and coated with different polymers (pectin, chitosan, ethyl cellulose, cellulose acetate phthalate, eudragit L-100 and eudragit L-100-55), each at three concentration. The tablets were evaluated for their physical characters, in–vitro dissolution in gradient pH, as well as, mathematical modeling using DDSolver software package. The dissolution data best fitted to first order with T_lag model with Krosmyer Pepas (n) values around unity suggesting erosion mechanism for all tablets except pectin coated ones which showed Fickian diffusion mechanism. Fitting the release data to the different erosion models suggested heterogeneous erosion mechanism. Lornoxicam tablets coated with 6% Eudragit L-100 were successfully delivered to the colon with a relative bioavailability of 531.96% compared to the conventional commercial tablets in rabbits.

Keywords: Lornoxicam, Colon targeting, Tablet, Eudragit L-100.

ABSTRACT

The present study attempted to evaluate acyclovir loaded PLGA nanoemulsions for ocular delivery. The acyclovir loaded PLGA nanoemulsions were prepared by spontaneous emulsification method. Five batches were prepared and labeled as NE-1, NE-2, NE-3, NE-4 and NE-5 by changing the concentration of PLGA polymer. The prepared nanoemulsions were subjected for its physico-chemical characterization, in-vitro diffusion, release kinetics and stability studies. FT-IR and DSC shown the drug and polymer were compatible with each other and no change in their chemical nature. The morphology of nanoemulsion shows spherical in shape with smooth surfaces. The particle size and zeta potential and Poly dispersity index were determined by malvern instrument and the results shown that the prepared nanoemulsion has significant ranges of particle size (164.67 - 244.43nm), zeta potential (-33.20 to -37.60) and poly dispersity index (0.256-0.499). Drug entrapment efficiency and % practical yield ranges between (54.97-79.67) and (46.83-58.01) respectively. The in-vitro % drug release of acyclovir indicates formulation NE-4 has significant sustained release compared with other formulations. The release kinetic data of all formulations are fitted with Higuchi’s model and non-fickian diffusion mechanism. The stability study indicates 5°C±3°C and 25°C±2°C/60%±5% RH is ideal storage condition for nanoemulsion for longer period. Thus it can be conclusively stated that the acyclovir loaded PLGA nanoemulsions may be considered as an improved ophthalmic drug delivery system for the treatment of ocular viral infections.

Keywords: Acyclovir, PLGA polymer, Nanoemulsion, Ocular delivery, Spontaneous emulsification method.

ABSTRACT

The goal of this study was to develop and optimize the Capecitabine loaded chitosan nanoparticles (CS-NPs)for improved colon cancer therapy, by enhancedsurface area, sustained drug release, reduced dose and hence, most importantly, reduced toxicity. Capecitabine loaded Chitosan nanoparticles were prepared by 3² full factorial designs, using ionotropic gelation method by cross-linking of chitosan (CS) with sodium tripolyphosphate (TPP). CS-NPs were prepared by dissolving chitosan in 1% (w/v) acetic acid solution under magnetic stirring at room temperature. The CS solution was diluted with deionized water to produce different concentration. The capecitabine was dissolved in CS solution using sonication and aqueous TPP solution was added drop wise using syringe to the mixture with moderate stirring for 30 min. The prepared nanoparticles were characterized by FT-IR spectroscopy and DSC to confirm the cross linking reaction between CS and cross-linking agent. From the % entrapment of capecitabine, nanoparticles were optimized using regression analysis, contour plots and check point analysis.Particle size of the optimized batch (CS-NPs-8) was found to be 87 nm. The Polydispersity index of the nanoparticles was found to be 0.113. The nanoparticles formed were spherical in shape with high zeta potentials, -35mV. In vitro release studies in phosphate buffer saline (pH 7.4) showed an initial burst effect and followed by a slow drug release. The drug release followed first order kinetics and was found to be diffusion controlled. Optimized formulation was also showing more % inhibition than drug alone in In-vitro anticancer study. From the accelerated study of optimized batch, it was found to be stable.

Keywords: Capecitabine, Colon cancer, Chitosan-TPP nanoparticles, HT-29.

ABSTRACT

Peptic ulcer and Depression are managed by co-administering number of drugs for long duration. Hence, drug-drug interactions which are important cause of antagonistic drug reaction and may lead to amplified risk of hospitalization and amplified care cost. The study was piloted to find the impact of pantoprazole which is generally used for primary peptic ulcer disease in humans on the pharmacokinetic and antidepressant activity of fluoxetine. The influence of pantoprazole on pharmacokinetic parameters of fluoxetine was studied in healthy male albino rabbits. The effect of pantoprazole on antidepressant activity was studied using four animal models. The serum concentration of fluoxetine was estimated by HPLC. And the antidepressant activity was studied using despair swim test, compulsive gnawing test, serotonin syndrome and tail suspension test. After treating with pantoprazole for 7 days the concentration of serum fluoxetine was significantly decreased at 2nd, 4th, 8th, 16th and 24th hour. Pantoprazole treatment for one week exhibited significantly changes in the pharmacokinetic parameters like AUC, AUMC, t1/2 and Cmax of fluoxetine in healthy albino rabbits. The immobility time significantly decreases after pantoprazole treatment for one week by despair swim and tail suspension test in rats and mice respectively. Compulsive gnawing test and serotonin syndrome also shows decrease in the effect after pantoprazole treatment. When both drugs are co-administered together dose of fluoxetine should be increased.

Key words: Depression; Fluoxetine; Pantoprazole; Drug-drug interaction; Tail Suspension test; Despair Swim Test.

ABSTRACT

The present research work focuses on improving the bioavailability of the anti osteoporotic drug Risedronate Sodium. This drug belongs to BCS class III which implies that it is permeability rate limited. Hence an attempt was made to reduce the particle size to nano dimensions using ionotropic gelation technique. In this technique, chitosan was used as the polymer and sodium Tri poly Phosphate was used as the cross linking agent. The resulting nanoparticles were optimized using 3² full factorial design and characterized for their entrapment efficiency, percent yield, in vitro diffusion studies. The particle size and zeta potential was found out and surface morphology was studied using Scanning electron microscopy. The in vivo studies clearly showed a marked improvement in the bioavailability of the nanoparticles as compared to the plain drug suspension.

Keywords: Risedronate Sodium, Nanoparticles, Bioavailability.

ABSTRACT

Pollution has become a global problem and the results are implied in high levels of contaminations reported for soil, water, air, plants and animals. In the present study, Al-Nahrawan is one of the most known industrial regions in Iraq. Samples of soil, water and air were taken for study. These samples were contaminated by different heavy metals like Pb, Cr, Cu, Fe and Zn that were characterized with low pH when compared with normal non industrial regions. The present results indicate that Al-Nahrawan region is affected widely by heavy metals contamination in soil, water and air as a result of industrial activities.

Keywords: Heavy metals, Al-Nahrawan, Pollution, industrial activity.

ABSTRACT

A rapid, accurate, linear, and sensitive RP-HPLC method has been developed and validated for estimation of febuxostat in the bulk drug and marketed tablet formulation. The chromatographic separation was achieved on Kromasil C18 Column (250 mm × 4.6 mm, 5 μm particle size) using solvent methanol:water(65 : 35 v/v, pH 3.0 adjusted with OPA)as a mobile phase at flow rate of 1.0 ml/min and25°C column temperature was maintained and analysis were carried out at detection wavelength316 nm. The linearity study was studied in the concentration range 10-50 μg/ml for febuxostat and correlation coefficient was found to be 0.999. The percentage purity of febuxostat was found in the range of 98-101%. The limit of detection and limit of quantification were found to be1.22μg/ml and3.58μg/ml. The method was validated for linearity, precision, accuracy, specificity and selectivity. The obtained results indicates that the proposed method allows selective analysis of febuxostat, in the presence of their degradation products formed under a variety of stress conditions. The developed procedure is also applicable for the determination of instability of the drugs in commercial products.

Keywords: Febuxostat; Validation; Force degradation studies; HPLC-DAD.

ABSTRACT

In the present study, an attempt was made to develop the transdermal drug delivery systems of Fluvastatin sodium using transfersomes incorporated in a gel, which will control the release of drug, increasing the bioavailability of the drug and thus decreasing the dosing frequency of the drug.  It was designed by encapsulating the drug in various transfersomal formulations composed of various ratios of Soya Lecithin: Span 80 or Tween 80 or sodium deoxycholate. The transfersomes were prepared by rotary evaporation sonication method. Lipid:surfactant ratio of 90:10 is  found to be more effective when compared to other ratios . Experimental results of the present study showed that deformable lipid vesicles improve the transdermal delivery, prolong the release, and improve the site specificity of the Fluvastatin sodium. The drug diffusion studies showed that the prepared transferosome vesicle follows zero order kinetics and mechanism of drug diffusion follows peppas model.

Keywords: Transfersomes, Anti-hyperlipidemic, Controlled release, Lipid, Surfactant.