ABSTRACT

Nanotechnology belongs to the production and utilization of materials at the nanoscale up to 100nm in size. Nanotechnology is emerging technique has application in biology and biotechnology as well as medical technology. It is expected to provide reasonable products by this technology in various fields of application. Novel nanodevices, nano and bio-materials are fabricated by nanotechnology. Paramagnetic nanoparticles, nanoshells, quantum dots, nanosomes are some of the nanoparticles used in diagnosis. These are the targeted drug delivery system. It provides therapeutically active drug molecule only to the site of action, without affecting other tissues, at comparatively lower doses. The prospective medical applications are in detection, diagnosis, monitoring and treatment of disease. It is effective in the treatment of cancer, tuberculosis, Alzheimer’s disease, Parkinson’s disease and heart diseases. The clinical applications are in dentistry, ophthalmology, tissue engineering and surgery are discussed. The purpose is to improve the health by amplifying the safety and efficacy of nanodevices. Nanotechnology will have global impact in the development of future health systems.

Keywords: Nanotechnology, Nanoparticles, Nano-devices, Applications.

ABSTRACT

Obesity is a chronic and highly prevalent medical condition associated with increased risk of developing numerous comorbidities such as hypertension, type 2 diabetes, stroke, and heart disease. Obesity is a state of excess adipose tissue mass or characterized by excessive accumulation of fat in the subcutaneous and deep tissue of the body, usually 20% or more of an individual’s body weight. The current clinical definition of obesity, as defined by expert committees, is based on body mass index (B.M.I) which is simply derived by dividing weight by height in meters squared. It results from an excessive intake of calories in relation to energy expenditure over a long period of time. Obesity is more prevalent in developed than developing countries. It has been increasing at an alarming rate throughout the world  over  the past two decades to the extent that it a now a pandemic, affecting millions of people globally, and it is the second leading cause of preventable death in the United States. As per unani philosophy, Siman Mufrit is a balghami disease.  Khilte balgham predominates in the body of obese persons and hence is considered the predisposing factor in the causation of obesity because shahem and sameen(fats) are having barid ratab mizaj. The people having barid mizaj have a slower metabolic rate and finally suffer from obesity. Unani system of medicine recommends different regimens and a large number of drugs that can be successfully used in the treatment of obesity. Some single drugs as well as compound formulations mentioned by unani physicians are being used in the treatment of obesity, particularly the drugs which are endowed with properties like  mufatteh sudad, musakhin,mudir, muhazzil and mulattif.

Keywords: Siman Mufrit, Obesity, Unani medicine.

ABSTRACT

Purines and pyrimidine derivatives are the important class of compounds in medicinal chemistry. Pyrimidine – a totally unsaturated six membered ring containing nitrogen at 1,3-position. They represent the diazine family with urazil and thymine being the constituents of ribonucleic acid (RNA) and deoxyribonucleic acid (DNA) and with cytosine. The work highlights one pot synthesis of some 1,3-dihydro pyrimidine derivatives from different substituted aldehydes. All the synthesized derivatives were screened for antibacterial activity using  gram positive (Bacillus subtilis, Staphylococcus aureus) and gram negative (Pseudomona aeruginosa, Escherichia coli) organisms at concentrations of 400μg/disc and 200μg/disc. The compound 5b (p-dimethyl aminophenyl derivative) was found to be sensitive in all strains. The structure of compound 5b was confirmed by IR spectral studies.

Keywords: Dihydropyrimidine, substituted aldehydes, antibacterial, IR spectra 

ABSTRACT

A simple, rapid and sensitive liquid chromatography / electro spray ionization tandem mass spectrometry (LC–ESI–MS/MS) assay method has been proposed for the determination of apremilast in human plasma samples using apremilast d₅ as internal standard (IS). Analyte and the IS were extracted from the 200 µL of human plasma via simple solid–phase extraction. The Chromatographic separation was obtained on a C₁₈ column operating at a flow rate of 1.0 mL/min by using a mobile phase comprising of mixture of 5mm ammonium acetate in 0.2% formic acid buffer (15:85, v/v) and acetonitrile. A linear (r² ³ 0.99) of the calibration curve was obtained over the concentration range of 2.03–808 ng/mL.  As per FDA guidelines method validation was performed and the results met the acceptance criteria. The intra–day and inter–day precision (%CV) and accuracy results in five validation batches across five concentration levels were well within the acceptance limits. To analyze the more number of samples in short time, thus increasing the productivity a short run time of 2.25 min for each sample was applied and this was made possible. The method was successfully applied to a pharmacokinetic study in humans.

Keywords: Apremilast, human plasma, solid–phase extraction, LC–ESI-MS/MS, Pharmacokinetics.

ABSTRACT

We deliver chemistry of multicomponent reaction (MCR) for 2-Benzyl-5-(2-benzyloxycarbonylamino-3-Phenyl-propylamino)-4-(2-chloro-quinoline-3yl)-5-(2,2,2-trifluoro acetoxy)-pentanoic acid methyl ester (6a-g) by flexible Ugi multi-component approach, through commercially available amino acid,  aldehydes, isocyanides and amino acid ester in one pot. Further, the binding activity with CT DNA and nucleus property with pUC 19 DNA were studied by absorption spectra (K_b constant is= 4.2 × 10^-4 M^-1). The DNA binding results explored that the new molecule bind to DNA through interaction and also an efficient nucleus agent.

Keywords: Multicomponent synthesis, Ugi reaction, Quinolines, DNA Binding, Photonuclease activity.

ABSTRACT

A perforation duodenal ulcer occurs when an area of erosion eats right through the gut wall in the part of the digestive system leading from the stomach, knows as the duodenum .the life threatening condition known as peritonitis may follow, where inflammation and infection spread rapidly into the abdominal cavity affecting the entire major organ. Ulcer usually has a history of indigestion perhaps involving reflux ,where stomach acid pass up into the throat .with a perforated duodenal ulcer there may be sudden pain in the centre of the chest just below the breast bone, become more generalized abdominal pain and emergence surgery is generally required to repair the gut. Study of parental antibiotics used in post operative perforation duodenal ulcer in surgery department Prospective observation study, all the patients admitted in surgery ward in RMMCH during in 4 month study period from October 2016 to January 2017 who has compliance with inclusion and exclusion criteria. The total number of 40 patients. The male (85%) patients are mostly affected when compared to female patients (15%) with duodenal ulcer. Among the study population more patients with duodenal perforation were the under age group of 51-61 years. Followed by elderly patient with age group above sixty. The majority of the parenteral antibiotics mostly prescribed in metronidazole >amikacin >cefotaxim > ciprofloxacin > gentamycin > cefixime.

Keywords: surgery, paranteral antibiotics, Pharmaco therapy.

ABSTRACT

The objective of this research work was to formulate and evaluate the floating drug delivery system containing Risperidone drug, to improve oral bioavailability by increasing gastric residence time. Gastroretentive drug delivery system was developed by using Gum karaya & HPMC K 200M polymers. Formulations were prepared by using direct compression method. Optimization study was performed by using 3²  full factorial design. The formulated floating tablets batches were evaluated for physicochemical parameters like hardness, thickness, weight variation, friability, drug content, floating lag time and swelling index. All prepared batches shown good in-vitro buoyancy studies and acceptable result of  for various parameters. Comparing the all the formulations, formulation R6 was considered as optimized formulation which exhibited 99.41% of drug release in 12 hours, floating lag time of 2.14 ± 2.0 minutes total floating time of over 12 hours.

Keyword: Floating, hardness, floating lag time, drug release.

ABSTRACT

To develop and evaluate Push Pull Osmotic tablets of ketorolac Tromethamine (KT). Core tablets of KT were formulated by wet granulation method using polymers (HPMC K4M, K15M) , coated with semipermeable membrane (cellulose acetate), plasticizer (PEG 400) , pore former (D- sorbitol) and osmogen (sodium chloride). Compatibility studies were carried out using Differential Scanning Calorimetry(DSC), no incompatibility between the drug and polymers observed. The Physical properties of tablets were evaluated for thickness, hardness, friability, drug content, effect of osmotic agent, percentage of pore former, pH, agitational intensity, weight gain, osmotic pressure and in vitro drug release for 12 hours. Release studies best fitted to zero order pattern, indicating drug release was non-Fickian, independent of pH and agitational intensity. The system is simple, cost effective and alternative to conventional osmotic pump since sophisticated laser drilling technique is not required.

Keywords: Core tablets, Osmogen, DSC, Physical properties, zero order drug release

ABSTRACT

A rapid and sensitive stability indicating RP-HPLC method was developed for simultaneous estimation of salbutamol, carbocisteine and theophylline in combined tablet formulations. Chromatography was carried out on a Discovery HS C18 HPLC Column at 35 °C (250 x 4.6 mm; 5m) by eluting with a mobile phase consisting of a 50:50 v/v mixture of acetonitrile and 0.1 % orthophosphoric acid in water at a flow rate of 1.0 mL/ min. The detection wavelength was set at 215 nm. Accuracy was assessed by using standard addition method. The developed HPLC method was validated with respect to precision, specificity, accuracy, linearity and robustness. Forced degradation studies on the formulation were conducted by adopting the proposed method to assess the stability of the analytes under acid, base, peroxide, thermal and photolytic conditions and suitability of the method to resolve the degradation products.

Keywords: Salbutamol, Carbocisteine, Theophylline, RP-HPLC, Forced degradation, Method validation.

ABSTRACT

The present study was aimed to evaluate the wound healing activity of extract of seeds of Swietenia macrophylla. It is well-known plant in Asian traditional medicines. On the basis of traditional use and literature references, this plant was selected for wound healing potential. The ethanolic extract of seeds of Swietenia macrophylla was examined for wound healing activity in the form of ointment in the excision wound model using Albino rats. The extract ointments showed efficient response in the excision wound model as comparable to the group treated with standard drug Betadine ointment and control group in terms of wound contracting ability, wound closure time and epitheliallization period. Histological analysis was also consistent with the proposal that Swietenia macrophylla seed extract exhibits significant wound healing. Swietenia macrophyllan was found to possess significant wound healing property. This was evident by decrease in wound closure (P<0.005) and epitheliallization period.

Keywords: Swietenia macrophylla, Wound healing, Betadine, ethanolic extract

ABSTRACT

Current study was undertaken to improve solubility and bioavailability of poorly water soluble drug, Olmesartan. A mixed hydrotropic method was used to prepare the hydrotropes of Olmesartan. On the basis of screening Sodium Benzoate, Potassium Acetate and Tri Sodium Citrate hydrotropes were selected to prepare various hydrotropic solid dispersions of Olmesartan using selected hydrotropic agent in different ratio with the drug. The prepared solid dispersions were evaluated for solubility analysis, Drug Content Estimation, Fourier Transformed Infrared Spectroscopy, Differential Scanning Calorimetry, and In-vitro Dissolution Study of hydrotropes. From the study the results revealed that solubility was increased by using certain ratio (1:1:1:0.5) of drug with hydrotropic agents alone as well as in the combination. In the present study an attempt was made to prepare hydrotropes of a poorly water soluble drug Olmesartan to enhance the solubility and bioavailability of drug. The screening of different hydrotropic agents was performed to evaluate the best suited agent for drug hydrotrophs. On the basis of solubility analysis, the Sodium Benzoate, Potassium Acetate and Tri Sodium Citrate agents   have the ability to enhance the solubility of the drug more than 3 times of its original solubility. The method is economical and simple, to enhance the solubility of Olmesartan.

Keywords: Hydrotropy Method, Co solvent, Olmesartan, Physicochemical property, Sodium Benzoate, Potassium Acetate, Tri Sodium Citrate.

ABSTRACT

The preparation was to be started with the preparation of successive extract of plant leaves of Ficus Carica Linn. (Moraceae) in petroleum ether and ethanol respectively followed by pharmacological investigations including Organoleptic property and photochemical investigation i.e. test for triterpenoids, Glycosides, Alkaloids, Flavonoids, and Tannins. The % yield values for ethanolic leaves extract and petroleum ether leaves extract were found to be 3.6 & 5.4%. The anti-ulcer effect of ethanolic leaves extract of Ficus Carica Linn. Studied in Pylorus ligation and chemical (HCl-Alcohol) induced ulcer in albino rats. The extract at dose of 250, 500 mg/kg produced significant inhibition of gastric lesion by chemical and Pylorus ligation induced ulcer in rats and omeprazole and Sucralfate used as a standard drug. The extract reduced ulcerative lesion, gastric volume, free and total acidity but raised the P^H of gastric juice in Pylorus ligation& chemical induced model. The obtained result for the  anti-ulcer activity of ethanolic leaves  extract were confirmed, and reduced ulcerative lesion, gastric volume, free acidity and total acidity  with the comparison of standard drug. The all significant were shows the ulcerative index, free & total acidity, percentage of protection, hemorrhage, streaks, as compared to control and also p^H raised up to 3.5 respectively.

Keywords: Anti-ulcer, Ficus Carica L., Albino Rats, Sucralfate, Omeprazole.

ABSTRACT

Hirschsprung’s disease is a rare motor disorder of the gut which is characterized by the absence of ganglia in distal colon resulting in a functional obstruction. We report a case of a male baby of 15days of life presented with abdominal distension, vomiting, passage of stools in small amounts, greenish gastric aspirate. Physically facial puffiness, rough dry skin and cold peripheries were noticed. On abdominal examination, there were prominent veins, visible intestinal peristalsis and mild hepatospleenomegaly. Ultrasound abdomen shows dilated bowel loops suggesting intestinal obstruction. X-ray abdomen (ERECT) reveals cecal volvulus with intestinal obstruction. Histopathology report shows the impression – features consistent with Hirschsprung’s disease. The treatment for Hirschsprung’s disease is surgery.

Keywords: Hirschsprung’s disease, intestinal obstruction.

ABSTRACT

A simple and reliable high performance thin layer chromatographic (HPTLC) method has been developed and validated for the study of fingerprint chromatograms of the hexane , chloroform, ethyl acetate and aqueous extracts of leaves of Hemigraphis colorata (blume) H.G. Hallier .HPTLC separation of the all extracts was performed and scanned  at ultraviolet absorbance at 254 nm. A mobile phase composed of toluene: ethyl acetate: formic acid :methanol (3:6:1.6:0.4).The chromatogram obtained and the peak profile of the components collected by scanning could  made up the fingerprint of the  various  extracts from leaves of  Hemigraphis colorata and compared with antioxidants markers of flavonoids and phenolic acids. The fingerprint chromatograms had a good stability, precision, and reproducibility. The method is suitable for differentiation of extracts from the leaves of Hemigraphis colorata, and can be used as a quality control method for this plant.

Keywords: Hemigraphis colorata, ethyl acetate extract, rutin ,quercetin ,Gallic acid

ABSTRACT

The main objective of the present investigation is to evaluate the analgesic activity of hydro-alcoholic extract of Acacia Senegal pod on mice. Analgesic activity of hydro-alcoholic extract of Acacia Senegal pod at a dose of 200 mg/Kg, 400 mg /Kg and 800 mg /Kg were evaluated against drug pentazocine at a dose of 17.5 mg/Kg. Adult albino mice and rats of either sex of six numbers in each group were under taken for study and evaluated by eddy’s hot plate and tail immersion method. The all doses of Acacia Senegal pod crude hydro-alcoholic extract were found to produce significant (P<0.05) analgesic activity. In eddy’s hot plate and tail immersion, both method showed significant activity (P<0.05) after 30 minutes. The result showed significant analgesic activity against stimuli.

Keywords: Acacia senegal pod, Crude hydro-alcoholic extract, Eddy’s hot plate method, Tail immersion method, Pentazocine.

ABSTRACT

The aim and objective of the present work is to design and develop fast disintegrating tablets of Amlodipine Besylate to improve the patient compliance and  desired bioavailability by selected delivery system by following immediate release mechanism. The drawbacks of the tablets can be overcome using methods involved in modified dissolving tablets, oral  dissolving  tablets (MDT) or orally disinter grating tablets (ODT) ; which started as an alternative oral dosage forms. To achieve successful delivery of drug , it  needs to be protected from degradation,  drug release to be improved and increase absorption. For this objective and to have the rapid  uptake of drug in solution form by rapid disintegrating formulation to be expected to have better  Therapeutic effect of both drugs in the gastrointestinal tract. The research objective   of the present work understands the novel advancements that are made in oral fast disintegration preparations incorporated anti hypertensive drug like Amlodipine Besylate using combination of super disintegrants.

Keywords: Amlodipine Besylate, Disintegration, Anti - Hypertensive, Bioavailability.

ABSTRACT

Clarithromycin drug in the form tablet was formulated with different polymers. The object of the present work is preparing floating tablets in controlled fashion. The gas generating agent, sodium bicarbonate was added in different concentrations with varying amount of retardation polymers. Different grades of HPMC polymers HPMC K4M, K15M & K100M were used as retarding polymers. The formulation blend was evaluated for various physicochemical properties and all the parameters were found to be within limits. The formulations F1-F9 were formulated and evaluated for various quality control parameters. All the formulations were passed the tests and the results were within limits. From the dissolution data it was evident that formulation F7 was found to be best with maximum percent drug release of 96.90% upto 24 hours.

Keywords: Clarithromycin, HPMCK4M, HPMCK15M, HPMCK100M, Floating tablets.

ABSTRACT

Nonionic surfactant vesicles (niosomes) were formulated with an aim of enhancing the oral bioavailability of Decitabine, an anti-cancer drug. Niosomes were formulated by conventional thin film hydration technique with different molar ratios of surfactant, cholesterol and dicetyl phosphate. The formulated niosomes were found spherical in shape, ranging from 2.95 𝜇m to 10.91 𝜇m in size. Vesicles with 1 : 1 : 0.1 ratios of surfactant : cholesterol : dicetyl phosphate with each grade of span were found to have higher entrapment efficiencies, which were further selected for in vitro studies. Vesicles formulated with sorbitan monostearate were found to have maximum drug release (99.091%) at the end of 24 hours and followed zero order release kinetics. In conclusion, noisome could be a promising delivery for Decitabine with improved oral bioavailability and prolonged release profiles.

Keywords:  Niosomes, Decitabine, Non-Ionic Surfactants.

ABSTRACT

The assumption on colon-specific drug delivery system suffers from minor inherent problems. The development of novel into pH dependent and microbially triggered compression enteric  coated  tablets  was  done.  Capecitabine was used as a model drug. The core tablet was coated with acid soluble coating, Eudragit®S-100 which was compression coated with immediate release blend of drug containing microbial triggering polysaccharide, guar gum. Different combinations of polymers were selected to achieve drug targeting to the colon for the treatment  of  colorectal cancer. The novel – CODES successfully showed resistance to the gastric environment and exhibited no drug release in simulated intestinal fluid. In-vitro release studies for prepared  tablets  were carried out for 2 hours in 0.1 N HCl, 3 hours in pH 7.4 phosphate buffer and remaining in 6.8 pH phosphate buffer. In vitro studies revealed that it have limited drug release in stomach, small intestine and released maximum drug in the colonic environment.

Keywords: pH dependent, time delayed, microbially triggered, compression coating, CODESTM.

ABSTRACT

The main aim of the present study was to develop and validate a simple, rapid and sensitive assay method for sildenafil citrate in pharmaceutical dosage forms by reverse phase high performance liquid chromatography method. Determination Of Sildenafil Citrate was determined by reverse phase HPLC using Potassium dihydrogen phosphate Buffer (pH 7.0):ACN(45:55) and column  Inertsil ODS-3V 5μ (150*4.6mm) as a stationary phase and  the chromatogram of Sildenafil Citrate has shown in figure 10 and peak was observed at 228 nm which was selected as a wavelength for quantitative estimation. After development of the method, it was validated for system suitability, specificity, linearity, precision, accuracy, robustness and solution stability studies. The results system suitability was found to be within the limits. The limit were not more than RSD <2%. Precision RSD was found to be 0.43 for Sildenafil Citrate. The precision was found to be within the limits. The limit were not more than RSD <2%. Precision RSD was found to be 0.3 for Sildenafil Citrate. The accuracy was found that recovery value of pure drug from the reanalyzed solution of formulation were between 98.0 % to 102% which indicates that the method is accurate and also reveals that commonly used excipients. Theoretical plate for Sildenafil Citrate was found to be not less than 4500. Retention time was nearer to 5.0. In Robustness parameter in both conditions the R.S.D. was less than 2%. (-10 and +10) Hence this method was better for pharmaceutical formulations Analysis. In Solution Stability parameter the R.S.D. was less than 2%. Both Standard and Sample solution was stable up to 48 Hrs.

Keywords: Sildenafil Citrate, system suitability, specificity.

ABSTRACT

In the present research work an attempt was made to formulate and evaluate  CR tablets of Ranolazine by using different polymers, polymers namely HPMC Phthalate and Eudragit S 100. Drug polymer interaction studies were carried out by using FTIR analysis which confirmed that there were no interactions between the drug and excipients. All the physical parameters of Drug & Drug – excipients (wet granules) carried out. The results indicate that all formulations were within the pharmacopoeial  specifications. The various formulations of CR tablets of Ranolazine were formulated by using various concentration different polymers HPMC Phthalate and Eudragit S 100. The tablets were evaluated for pre compression and post compression parameters and In-vitro dissolution. The results indicated that the, physical parameters of formulated tablets were within the Pharmacopeial specifications. The controlled release tablets of Ranolazine formulations was optimized on the basis of different physical parameters and mainly with the comparison of formulations on the basis of in-vitro dissolution study and the optimized formulation F4 were found to be 97.0 % drug release within 24 hours. The kinetic studies To know the kinetic drug release, the data was treated according to different model. The drug release data of F1-F5 fitted to Higuchi plots were best fit into Higuchi equation and diffusion mechanism. The zero order plots for all formulation were found linear. The result shows that, drug release rate for the F4 formulation follow the zero order mechanism. The accelerated stability studies of selected formulation (F4) showed that there were no significant changes.

Keywords:  Ranolazine, HPMC Phthalate and Eudragit S 100.

ABSTRACT

The burden of Chronic Kidney Disease (CKD) is increasing in alarming proportion all over the world.  According to World Health organization (WHO), CKD is 12^th leading cause of death and 17^th cause of disability. In India, an estimated 100-120 per million population reach Chronic kidney disease stage-V. In India due to lack of financial resources, lack of trained manpower & infrastructure leads to severe strain on existing health policies in the light of the increasing burden of  Chronic kidney disease. Maintenance dialysis is a well-recognized modality of treating patients having end stage renal disease. Good quality of life and survival on maintenance dialysis depends on various factors but unfortunately in our country, the quality of dialysis delivered to patients can vary from center to center that may affect  the health  of hemodialysis patients. This study was undertaken to analyze the post hemodialysis effects in patients with ESRD.A Prospective observational study was conducted on total of 150 out-patients undergoing maintenance hemodialysis, in order to find out the post hemodialysis effects in chronic renal failure patients and patient information was collected accordingly. In this study most of the patients undergoing hemodialysis experienced hepatitis, arthropathy and disequilibrium effects after repeated hemodialysis process. We observed that people undergoing hemodialysis experiences severe side effects which can be minimized by creating awareness so that the life expectancy of the hemodialysis patients can be increased.

Keywords: End stage renal disease (ESRD), Chronic kidney disease (CKD), Hemodialysis  (HD),  Arteriovenous fistula (AV).

ABSTRACT

The synthesis of Nitrogen base heterocycles particularly highly substituted piperidine are very important structural motif which is present in numerous natural alkaloids including piperine, nicotine, coniine etc and non-natural substances too. The piperidine is extracted from black pepper^1,2, Psilocaulon absimile (Aizoaceae)³ and Petrosimonia monandra⁴.   The functionalized piperidine derivatives are ubiquitous building block in synthesis of pharmaceuticals and fine chemicals, consequently it attract interest, both for their synthetic challenges,⁵ and also their value in synthetic chemistry⁶ and diverse biological activity.⁷ The present work includes the synthesis of highly functionalized piperidine derivatives using the Oximation of Michael adducts (scheme 3). The target product was oxime for further reaction but instead of the required oxime as product the side product with six member heterocylic product was formed as major product. The yield of side product was depends on time and thermodynamic conditions. Owing to the new results which were confirmed by singe crystal X-rays and NMR data, we have developed this methodology which gives easy access to the synthesis of highly substituted piperidine (Scheme 3). This strategy is very simple and efficient to have 2,3,4,6 substituted nitrogen containing heterocycle as Piperidine.

Keywords: Piperidine, Heterocyclic compound, Oximation, Michel adduct.

ABSTRACT

The present study was designed to develop simple accurate, precise, reproducible and validating of a stability indicating reverse phase high performance liquid chromatographic (RP-HPLC) method for the simultaneous estimation of azithromycin, ornidazole and fluconazole in bulk and its pharmaceutical dosage forms. Chromatographic separation of the three drugs was performed on a Phenomenex C₁₈ column (250X4.6mm 5μm) as stationary phase with a mobile phase comprising of 20mM potassium dihydrogen phosphate : Acetonitrile (pH 4.8) in the ratio 30:70% v/v at a flow rate of 1ml/min and peak monitored at 254nm using PDA detector. The retention time of azithromycin, fluconazole, ornidazole and procaine hydrochloride (internal standard) was Rt1-2.8, Rt2-5.0, Rt3-6.3 and Rt-3.8minutes respectively. The linearity of azithromycin, fluconazole and ornidazole were in the range of 20-100μg/ml, 3-15μg/ml and 15-75μg/ml with an internal standard, procaine hydrochloride 5µg/ml respectively. The accuracy of the method was found to be 98-102% and %RSD was found to be less than 2% indicating high degree of accuracy and precision of the proposed HPLC method. The limit of detection for azithromycin, fluconazole and ornidazole was found to be 0.34, 2.80 and 0.76μg/ml respectively whereas, the limit of quantification was found to be 1.05, 8.6 and 2.31μg/ml respectively. Forced degradation studies were conducted to know the stability of the drug samples under various stress conditions like acid, base, peroxide and photolytic degradation according to ICH guidelines. Results are validated statistically as per ICH guidelines.

Keywords: RP-HPLC, Azithromycin, fluconazole, ornidazole estimation, Forced degradation study, validation.

ABSTRACT

The objective of the present investigation was to prepare colon targeted piroxicam loaded Eudragit S 100 microspheres and evaluate its properties. The microspheres were prepared by using "O/O solvent evaporation" technique. The formulation was optimized by investigating the influence of various process variables like stirring speed, drug: polymer ratio and percentage of emulsifier on the fabrication and the prepared microspheres were evaluated for in vitro properties. Piroxicam loaded Eudragit S 100 microspheres were successfully prepared using "O/O solvent evaporation" method. Microspheres prepared using 1:5 drug: polymer ratio, with a stirring speed of 1000 rpm, and 1.0% w/v concentration of emulsifying agent was selected as an optimized formulation. In vitro drug release were performed in pH 1.2 (0.1N HCl) for 2h and in pH 6.8 phosphate buffer for next 2h followed by 7 pH phosphate buffer up to 24 h. The release pattern of drug was slow at low pH values and increased on rise in pH. The drug release followed Higuchi model.

Keywords: Emulsion solvent evaporation method; Piroxicam loaded Eudragit microspheres.

ABSTRACT

The present research work describes the  improvement of  bioavailability of Isradipine through buccal delivery. Isradipine buccal tablets were prepared with β cyclodextrin which improved the photostability of the drug. Buccal formulations were evaluated for in vitro release, moisture absorption, mechanical properties, and bioadhesion, and optimized formulation was subjected for bioavailability studies in healthy human volunteers and compared with marketed tablet. The pharmacokinetic parameters C_max, t_max and AUC_o-t of test formulation were calculated and compared with the reference i.e., marketed product. It was observed from the study that the drug release from the test formulation could be sustained and it was concluded that the test formulation was able to sustain the drug release as compared to reference marketed product with 1.672 fold increase in extent of absorption i.e., AUC_0-t.

Keywords: buccal delivery, Isradipine, bioadhesion, photostability, bioavailability