ABSTRACT

The current review article describe on the principles of mucoadhesive buccal drug delivery systems based on adhesion to biological surfaces that are covered by mucus. The delivery of drugs through the buccal mucosa has attracted and numerous approaches, both conventional and complex, have been developed in an attempt to deliver a variety of pharmaceutical compounds via the buccal route. Buccal delivery involves the administration of the desired drug through the buccal mucosal membrane lining of the oral cavity. Buccal transmucosal delivery helps to bypass first- pass metabolism by allowing direct access to the systemic circulation, maintaining the drug concentration between the effective and toxic levels, inhibiting the dilution of the drug in the body fluids, and allowing targeting and localization of a drug at a specific site. It is a complex phenomenon which involves wetting or swelling and interpenetration of polymer chains, it can be of Matrix or Reservoir types. This article aims at reviewing the numerous techniques that has been designed till date for optimizing novel transmucosal buccal drug delivery system.

Keywords: transmucosal delivery, buccal delivery, complexation, first-pass effect

ABSTRACT

Centellaasiatica of the family Umbelliferae is commonly found in the parts of India, Asia and Middle East & commonly known as Mandookaparni. It is a perennial, herbaceous creeper growing upto 30 cm in height with fan-shaped leaves. It contains glycosides, alkaloids and triterpine acids. Toxicological study of asiaticoside showed that subcutaneous injection of asiaticoside in doses of 0.04 to 0.05 gm / kg in rat and rabbit was found toxic. The oral dose of 1 gm / kg was well tolerated. The plant is bitter, acrid, sweet, cooling, soporific, cardiotonic, nervine tonic, stomachic, carminative, antileprotic, diuretic and febrifuge. It is used as a brain tonic for promoting brain growth and improving memory. Ayurvedic medicines has effectively used it in the treatment of inflammation, anemia, asthma, blood disorders, bronchitis, fever, urinary discharge and splenomegaly. Reported activity of Centellaasiatica are cardiovascular acivity, antioxidant activity, antimicrobial activity, antifilarial activity, anxiolytic activity,antidiabetic and antihyperlipidemic activity, radioprotective activity, antiprolifirative activity, anticonvulsant activity, memory enhancement activity, antinociceptive activity, anti-inflammatory activity, antiulcer activity, antifertility activity, antitumor activity, wound healing activity and anti-immune activity.

Keywords: Centellaasiatica, Mandookaparni, Asiaticoside, Brain tonic.

ABSTRACT

Virosomal Drug Delivery System is the novel drug delivery system available which has been a great revolutionary technology in drug delivery in recent years. Virosomes are the immunogenic compositions that include methods of eliciting an immune response. Virosomes are spherical, unilammellar phospholipid bilayer vesicle with a mean diameter of range 120-180nm. These represent reconstituted empty influenza virus envelopes, which contain 70% phosphatidylcholine and remaining 30% neuraminidase (NA) and haemagglutinin (HA) glycoproteins. A virosome can include at least one viral surface envelope glycoprotein expressed on the surface of the virosome. The virosome can also optionally include at least one adjuvant molecule expressed on the surface of the virosome. A virosome is a drug or vaccine delivery mechanism incorporating virus derived proteins to allow the virosome to fuse with the target cell. Virosomes cannot replicate but are pure fusion active vesicles. Virosomal drug delivery depends on the methods used to prepare the encapsulated bioactive material their incorporation into the virosomes and followed by the characterization and formulation of the finished preparations. All these features allow us to consider influenza virosomes as a promising model for antigen and molecular delivery, which could be helpful for the development of new vaccines or immunotherapeutic protocols that combine safety with immunogenicity and their applicability in different fields of medical research. This technology can potentially be used to deliver peptides, nucleic acids or genes, and drugs like antibiotics, anticancer agents, and steroids. In this paper reviewed about the challenges in drug delivery, advantages of virosomes in successful delivery of immunogens, formulation, Virosomal Technology and its various approaches.

Keywords: Virosomes, influenza virus, liposomes, hemagglutinin and Neuraminidase.

ABSTRACT

Rheumatoid arthritis is a common inflammatory disease characterized by progressive bone and cartilage destruction, A full cure for rheumatoid arthritis  is yet to be discovered but  Microemulsion containing NSAID can be used as best option for the management of pain in Rheumatoid arthritis because of their potential to incorporate a wide range of drug molecules (hydrophilic and hydrophobic) due to the presence of both lipophilic and hydrophilic domains.  Association of drugs with Microemulsion is normally noncovalent, based on collective strength of weak binding forces which are broken to release drug. The small droplets of Microemolsion provide better adherence to membranes and transport NSAID molecules in a controlled fashion for the pain management of Rheumatoid Arthritis. These adaptable delivery systems provide protection against oxidation, enzymatic hydrolysis and improve the solubilization of lipophilic drugs and hence enhance their bioavailability.

Keywords: Rheumatoid arthritis, Microemulsion, NSAID, Lipophilic domain,  Hydrophilic domains.

ABSTRACT

The Rapid growing area for the last few decades in the pharmaceutical industry, are the Oral Disintegrating Tablets. They effortlessly dissolve or disintegrate in saliva within 60 seconds. Here, disintegration plays a critical role, disintegrants or superdisintegrants in the dosage forms are included for advancement of solid orals. The Excipients used in the formulation of ODT’s allow quick release of the drug, with faster dissolution. The innovations in the platform of formulating ODTs are aimed at both increasing the performance of the dosage form by decreasing the disintegration time and increasing the patient compliance. These achievements require constant promotion of formulation variables as well as techniques in the production of dosage forms. An attempt is made by this article to divulge the strategies which are used by inventors for improving the performance and acceptability of ODTs.

Keywords: Zydis Technology, Orasolv Technology, Super Disintegrants, Fast Dissolving.

ABSTRACT

In the last decade, poorly soluble drugs have been an area of concern for all the researchers in the field of pharmacy. A number of researches have been carried out to enhance the solubility and dissolution properties of such drugs. This study deals with a comprehensive review of liquisolid technique carried out mainly for biopharmaceutical classification system (BCS) class II & IV drugs. These drugs are having problems of poor solubility, dissolution and thus poor bioavailability. Various studies conducted on a number of drugs so far, have been reviewed. A variety of techniques such as micronization, salt formation, complexation, solid solutions, and liquisolid technique etc. have been used to overcome such problems. It has been observed that liquisolid technique is the most promising way for solubility and dissolution enhancement of such drugs. It can be concluded that liquisolid technique results in increased solubility, dissolution and thus bioavailability.

Keywords: Liquisolid, dissolution, solubility, bioavailability.

ABSTRACT

The transfer of analytical procedure (TAP), also referred to as method transfer, is the documented process that qualifies a laboratory (the receiving unit) to use an analytical test procedure that originated in another laboratory (the transferring unit), thus ensuring that the receiving unit has the procedural knowledge and ability to perform the transferred analytical procedure as intended. Method Transfer enables to adapt method to new facility or instrument and to meet new facility validation requirements and also helps to maintain validated state of method. It gives documented guidance in principle and provides general recommendations on the necessary activities that should be addressed to conduct a successful intra- or inter- site transfer. It applies to all dosage forms such as sterile products, metered-dose aerosols and clinical trial supplies. There are many approaches to Method Transfer such as Comparative Testing, Co-validation between two laboratories, Revalidation, Transfer waiver.

Keywords: Method Transfer, transferring unit, receiving unit, validation.

ABSTRACT

Erectile dysfunction is the sexual dysfunction characterized by inability to maintain an erection of penis during sexual performance. Oral phosphodiesterase type 5 inhibitors drugs are successful for treatment of impotence such as sildenafil, vardenafil, tadalafil, alprostadil and avanafil. Clinical trials reveals that avanafil have faster onset of action as well as higher specificity for phosphodiesterase type 5 inhibitors with fewer side effects in comparision of other oral phosphodiesterase type 5 inhibitors drugs. In case of analytical method only LC-MS/MS method has been done. There may be chances of analytical study of avanafil will be done in future by using various spectroscopy method.

Keywords: Avanafil, Erectile dysfunction, Clinical Study, Analytical Approach

ABSTRACT

Mucoadhesive dosage forms may be designed to enable prolonged retention at the site of application, providing a controlled rate of drug release for better therapeutic results. Mucoadhesive drug delivery systems are used to prolong the residence time of the dosage form at the site of application or absorption and to facilitate intimate contact of the dosage form with the underlying absorption surface to improve and enhance the bioavailability of drug. Some of the promising plymers that have been commonly used in these systems include polycarbophil, carbopol, lectins, chitosan, carboxymethylcellulose, pectin, carragenan, alginic acid, polylysine, polybrene, polyethylene glycol, polyvinyl pyrrolidone , dextran etc. Now  scientists are developing mucoadhesive micro and nanoparticulate systems by using  novel mucoadhesive polymers for better therapeutic results and site specific targeting with lesser side effects. Improvements in mucoadhesive based oral delivery and, in particular, the development of novel, highly-effective and mucosa-compatible polymers, are creating new commercial and clinical opportunities for delivery of narrow absorption window drugs at the target site to maximize their efficacy. This review is an effort to provide information on such mucoadhesive drug delivery systems that are developed for oral, buccal, nasal, rectal and vaginal routes for both systemic and local effect.

Keywords: Mucoadhesive; gastroretentive; bioavailability; micro and nanoparticulte; polymers.

ABSTRACT

For the past few decades, there has been a considerable research interest in the area of drug delivery using particulate delivery systems as carriers for small and large molecules. Particulate systems like nanoparticles have been used as a physical approach to alter and improve the pharmacokinetic and pharmacodynamic properties of various types of drug molecules.  Nanoparticles promise to revolutionize medicine and increasingly used in drug delivery. The purpose of this review is to explore the design, development of nanotechnology, different method of preparation and application. By making the drug into nanoparticles by using different method of preparation, which may alleviate the manifestations of disease with minimal dose and less toxicity. These drug delivery systems can be potentially translated into targeted cellular and tissue-specific clinical applications designed to achieve maximal therapeutic efficacy with minimal side effects.         

Keywords: nanotechnology, methods of preparation, applications in drug delivery.

ABSTRACT

Abuse, misuse and diversion of drug substance are one of the most growing problems of United States and all over the world. The most critical challenge in combating the problem of drug abuse is to balance the control of prescription drugs along with continued access for legitimate use. To overcome the increasing problem of drug abuse, development of abuse deterrent formulation can prove an effective tool. This review provides an overview of abuse, modes of abuse, drugs with abuse potential, and different approaches for development of abuse deterrent formulations. Due to high mortality and morbidity, Opioids are the drug of choice for development abuse deterrent formulation. Hence draft guidance of US F.D.A. (US Food and Drug administration) for evaluation and labeling of abuse deterrent Opioid formulations are also under the scope of this review.

Keywords: Drug abuse, FDA, deterrent, formulations

ABSTRACT

Carrier technology offers an intelligent approach for drug delivery by coupling the drug to a carrier particle such as microspheres, nanoparticles, liposomes etc. which modulates the release and absorption characteristics of the drug Microspheres constitute an important part of these particulate drug delivery system by virtue of their small size and efficient carrier characteristics. However, the success of these novel drug delivery system is limited due to their short residence time at the site of absorption. It would, therefore, be advantageous to have means for providing an intimate contact of the drug delivery system with the absorbing membranes. It can be achieved by coupling bioadhesion characteristics to microspheres and developing novel delivery systems referred to as “bioadhesive microspheres” This article contain the bioadhesive microspheres which have been developed for oral, buccal, nasal, ocular, rectal and vaginal routes for either systemic or local effects. This presents study include the spectrum of potential applications of bioadhesive microspheres in controlled drug delivery ranging from the small molecules, to peptides, and to the macromolecular drugs such as proteins, oligonucleotides and even DNA some Research Work on Bioadhesive Microspheres and Microcapsules. Various patent related to bioadhesive microsphere and Developments in the techniques for in vitro and in vivo evaluation of bioadhesive microspheres have also been discussed. From this study concluded that the bioadhesive microsphere can be efficiently used as controlled or targeted drug delivery.

Keywords: Bioadhesive Microspheres; Controlled release drug delivery; Site Specific Bioadhesive Polymer, Application.

ABSTRACT

Eye is the most exclusive organ of the body and various drug delivery systems are used to deliver drug into eye. Eye diseases are commonly encountered in day to day life, which are cured or prevented through the conventionally used dosage forms like eye drops, ointments. Delivery to the internal parts of the eye still remains troublesome due to the anatomical and protective structure of the eye. To improve ocular drug contact time, bioavailability and residence time, and to reduce the patient discomfort, frequency of dose, as well as to slow down the elimination of the drug there are significant efforts concentrating towards newer drug delivery systems for ophthalmic administration. This review focuses on the various new drug delivery systems applied in eye like inserts, in-situ gel, the newly developed particulate and vesicular systems like liposomes, pharmacosomes and discomes, niosomes, nanoparticles, iontophorosis, corneal shields, drug embedded contact lenses, ocular wafers etc  and the most recent advanced approaches of the ocular delivery systems like the delivery of the genes and proteins to the internal structures which were used in treating the diseases caused due to genetic mutation, along with safety evaluation of ocular drug delivery formulations with some case studies.

Keywords: Advance ocular therapy, control drug delivery systems, corneal permeability, vesicular systems, safety evaluation.

ABSTRACT

Alzheimer disease (AD) is a progressive dementia affecting a large proportion of the aging population, which is characterized by memory impairment, cognitive dysfunction, behavioral disturbances, and deficits in activities of daily living. Multiple lines of evidence demonstrate that oxidative stress is an early event in Alzheimer’s disease (AD), occurring prior to cytopathology, and therefore may play a key pathogenic role in AD. Cure of cognitive disorders such as amnesia, attention deficit and Alzheimer’s disease is still a nightmare in the field of medicine and several nootropic agents are being used to improve memory, mood and behavior, but the resulting side effects associated with these agents have made their use limited. Indian system of medicine emphasizes use of herbs, nutraceuticals and life style changes for age related neurodegenerative disorders like Alzheimer’s disease. In Ayurveda, Medhya herbs such as Centella asiatica, Bacopa monnieri, Acorus calamus and several others are beneficial in cognitive disorders including Alzheimer’s disease and if their scientific evidences and proofs are taken into consideration they make themselves a reasonably good target in finding a cure for memory and intellectual disorders.  Current review sums up the plants that have shown the beneficial and encouraging results in treating ailments like Alzheimer’s disease having antioxidant properties which play an important role in pathogenesis of Alzheimer’s disease.

Keywords: Alzheimer disease, oxidative stress, Medhya herbs,

ABSTRACT

Curcumin has been identified as a major constituent in turmeric. It has been used in traditional medicine for liver disease (jaundice), indigestion, urinary tract diseases, rheumatoid arthritis, and insect bites. Numerous studies have demonstrated the in-vitro anticancer effect of curcumin. Curcumin inhibits several different cellular targets like nuclear factor- kappa B (NF-ĸB); this in turn induces apoptosis and blocks the function of protein kinase C. The major problem associated with curcumin is its poor aqueous solubility resulting in its poor bioavailability at the tumor site. Therefore, improvement in stability, solubility and bioactivity is needed. The current review discusses the activity of curcumin on various types of cancer along with the advances in the drug delivery systems designed to improve curcumin delivery. These newly developed formulations improve the drug bioavailability and effectiveness. Numerous formulations of curcumin have been developed like microcapsules, β-cyclodextrin inclusion complexes, nanoparticles and others such drug delivery systems.

Keywords: Aqueous solubility, curcumin, cellular targets, nanoparticles, types of cancer 

ABSTRACT

Wounds are the result of injuries to the skin that disrupt the other soft tissue. Healing of a wound is a complex and protracted process of tissue repair and remodeling in response to injury. A wound can be described as a defect or a break in the skin, resulting from physical or thermal damage or as a result of the presence of an underlying medical or physiological condition. Wound healing is a complex process of cellular and biochemical interactions involving various cells such as keratinocytes, fibroblasts and endothelial cells. The in vitro assays & in vivo models can be performed to evaluate wound healing activity. In vitro models are useful, quick, and relatively inexpensive. In vivo-Small animals provide a multitude of model choices for various human wound conditions. In vitro fibroblast assay, keratinocytes assay can be performed. The wound healing efficacies of various herbal extracts have been evaluated by In vivo- models  excision models, incision models, dead space models, burn modes can be performed on small animals after getting approval from the Ethics committee. In vitro and in vivo assays are stepping stones to well-controlled clinical trials of herbal extracts. Wound healing property can be checked by measuring tensile strength of skin, measurement of wound area, percentage of contraction, collagen content, protein estimation, Period of epithilazation.

Key words: In vitro cell assays, excision models, burn wound models, incision models, dead space models

ABSTRACT

Nanoemulsions are only kinetically stable. However, the long term physical stability of nanoemulsions (with no apparent flocculation or coalescence) makes then unique and they are sometimes referred to as ‘Approaching thermodynamic stability. The inherently high colloid stability of nanoemulsions can be well understood from a consideration of their stearic stabilization (when using non-ionic surfactants and /or polymers) and how this is affected by the ratio of the adsorbed layer thickness to droplet radius. Successful ocular drug delivery has largely eluded solution due to, the physiological constraints imposed by the protective mechanisms of the eye that lead to poor absorption of drugs with very small fractions (less than 5%) of the instilled dose penetrating the cornea and reaching the intraocular tissues. Low drug contact time and poor ocular bioavailability due to drainage of solution, tear turnover and its dilution or lacrimation are the problems associated with conventional systems. Novel systems offer manifold advantages over conventional systems as they increase the efficiency of drug delivery by improving the release profile and also reduce drug toxicity. Conventional delivery systems get diluted with tear, washed away through the lacrimal gland and usually require administering at regular time intervals whereas novel emulsions are stable, have improved solubility, required reduced dosing frequency and release drug for prolonged periods of time. The aim of this review focuses on micro and nanoemulsions between 1 and 200 nm with a mean droplet size of about 40nm) for ocular drug delivery.

Keywords: Nanoemulsions, surfactant, droplet size, ophthalmic, stability

ABSTRACT

Perindopril is an angiotensin converting enzyme inhibitor. The bioavailability of Perindopril following oral administration is 20 % due to high hepatic first pass metabolism. When administered orally, frequent dosing is needed due to its short biological half-life (0.8 to 1hr). sobuccal patches are one of the better option for perindopril administration. 9 Formulations were prepared using 3² full factorial designs by solvent-casting technique to explore the effects of sodium alginate and carbopol 934 (as independent variables) on drug release, mucoadhesive strength and retention time (as dependent variables). The prepared buccal patches were also evaluated for, weight uniformity, patch thickness, folding endurance, surface pH, swelling studies, % moisture content,% drug content, tensile strength, drug release studies, mucoadhesive strength, retention time. The ex-vivo permeation studies were carried out across excised sheep buccal mucosa using modified Franz diffusion cell. Patches exhibited drug release in the range of 70.37to 96.62% in 8 hrs. Drug release from patches followed zero order and higuchi release model and the mechanism of the drug release was due to swelling and erosion of hydrophilic polymers. The formulation was optimized with desirable drug release, mucoadhesive strength and retention time by applying computer software Design Expert 8.0.7.1. Ex-vivo drug release values for the cumulative amount of the drug permeated across the sheep buccal mucosa from optimized formulation was 76.76%. The experimented values were in good agreement with expected values for the optimized formulation which demonstrate the feasibility of the model in the development of buccal patches.

Keywords: Perindopril, Mucoadhesion, Factorial design

ABSTRACT

To investigate the effect of Aluminium chloride on the activities of testicular enzymes in rat. Forty male Albino rats were divided into four groups (n=10). Treatment was given for a period of 45 days daily. Group-I Control given only distilled water, Group-II treated with aluminium chloride 50 mg/Kg body wt. Group-III treated with Vitamin E 20mg/Kg body weight. Group-IV treated with aluminium chloride+ Vitamin-E. The animals were sacrificed after 24 hours duration. Biochemical studies were observed in testis. Marker enzymes ALP, ACP and LDH, SDH activities were decreased significantly with control. Lipid peroxidation was increased significantly in aluminium chloride treated rats. The administration of AlCl₃+Vit E shows protective effect from the toxicity.

Keywords: Aluminium chloride, ALP, LDH, Marker enzymes, Vitamin-E

ABSTRACT

To increase the bioavailability and short ocular residence time of Norfloxacin eye drops, aqueous solutions of drug in chitosan/ Pluronic (poloxamer) were prepared. Mixtures of solutions of Pluronic (5-17.5% w/w) with chitosan (0.1-0.6% w/w) were prepared.  The formulations so prepared were in the liquid state at 4°C while turned into a gel at the temperature of the Cul-de-sac. Naturals polymers i.e., Poloxamer was used as the polymer which exhibited the phase transition behavior and chitosan was used to improve residence time. Norfloxacin release was determined using a membrane less dissolution model in artificial tear solution up to 8 hours and the samples were analyzed spectrophotometrically at 277nm. The rheological behavior of solutions in response to dilution or temperature changes and also the phase change temperature (PCT) were determined. Antimicrobial effect of the solutions was studied in nutrient agar in comparison to all formulations of Norfloxacin using Pseudomonas aueroginosa, Staphylococcus aureus and E.coli by the agar diffusion test using the cup-plate technique. The formulation consisted of 15% Pluronic and 0.5% chitosan, with the highest release efficiency (73.46 ± 0.876%) and an acceptable mean release time, is suggested as a suitable ophthalmic preparation for sustained release of Norfloxacin.

Keywords: Ocular drug delivery, in situ gels, chitosan, poloxamer, phase transition temperature.

ABSTRACT

In the present study, Solid Dispersion of Propranolol Hydrochloride were prepared using solvent evaporation technique using PEG 4000, PVP K-30 and PVA. However absolute bioavailability of Propranololo Hydrochloride is about 30% . To increase the solubility, solid dispersion was prepared. Preliminary solubility analysis was carried out for the selection of carriers and solid dispersion was prepared with PVA, PEG 4000, PVP-K30. These solid dispersions were analyzed for the solubility and In-vitro dissolution profile, solid dispersion of drug with PEG 4000 had shown enhanced solubility with improved dissolution rate. Further FTIR, DSC, SEM studies were carried out. Solid dispersion prepared with PEG 4000 shows the presence of amorphous form confirmed by the characterization study .The study also shows that dissolution rate of Propranolol Hydrochloride can be enhanced to considerable extent by solid dispersion technique with PEG 4000.

Keywords: Propranolol Hydrochloride, Solid dispersion, PVA, PEG 4000, PVP-K30.

ABSTRACT

Many historical limestone and sandstone monuments in Bhopal are seriously threatened by bio-deterioration and are in need of investigation and conservation. Bio-deterioration processes result from complex interactions of surface-invading microbes (such as fungi) with the surface material. The present investigation focuses on the conservation of monuments by determining the antifungal effect of azoles against the fungal isolates isolated from the monuments of Bhopal: Aspergillus niger, A. flavus, A. fumigatus, Rhizopus arrhizus and Penicillium sp.We determined the minimum inhibitory concentrations (MICs) of antimicrobial agents using the guidelines of National Committee for Clinical Laboratory Standards (M38-A). To determine MICs, the inoculums of the above isolates were exposed to itraconazole, ketoconazole, fluconazole, griseofulvin and clotrimazole. We found that the order of in vitro activity of these antifungal agents against the fungal isolates is Itraconazole> Ketoconazole >Clotrimazole = Fluconazole = Griseofulvin. This result suggests that the use of Itraconazole and Ketoconazole should be a primary consideration in the conservation of monuments. Spraying or painting with these antifungal drugs could protect the monuments from fungal biofilm development.

Keywords: Monuments, Biodeterioration, Fungi, Antifungal drugs, MIC, Conservation of Monuments.

ABSTRACT

The aim of this work was to investigate the potential of solid lipid microparticles (SLM) to offer gastroprotection and improve piroxicam’s anti-inflammatory property. The effects of NaCl and cabosil^® on the properties of the SLM were also evaluated. The SLM were prepared by the hot homogenization technique using Ultra turrax (T25 Basic digital). Phospholipon^® 90G and Capra hircus fat constituted the lipid matrix. The particle size, drug content, encapsulation efficiency, in vitro drug release, anti-inflammatory and ulcerogenic studies were carried out on the formulations. Results showed that carbosil^® significantly (p<0.05) contributed to increase in particle size of the SLM. Drug-load caused significant (p<0.05) decrease in EE % whereas significant (p<0.05) increase in EE % was associated with carbosil^®. Significant (p<0.05) reduction in drug release rate was occasioned by carbosil^®. SLM batches did not show any presence of ulcer lesions and indicated satisfactory antiinflammatory property of piroxicam. In conclusion piroxicam SLM promoted gastroprotection and satisfactory antiinflammatiory activity of piroxicam.

Keywords: Solid lipid microparticles; Piroxicam; Ulcerogenicity; Anti-inflammation.

ABSTRACT

The present study was conducted on the basis of previous chemical and biological; national and international research works on Corchorus olitorious Linn. For this, published articles, dissertations, magazines, and book reports were collected, from the past up to 2012. Aim of the work was targeted to exploit the medicinal information among both the users and non-users, benefited by this species world-wide in. Protein, lipid, calcium, iron, carotene, vitamins, folic acid and some enzymes have been reported from the leaves, still used as vegetables. Essential phytoconstituents like flavonoids, saponins, tannins, steroids, glycosides, sugars and triterpenes isolated from leaf, bark, root and seeds of the C. olitorious have been reported   for their cardiac, anti-malarial and hepato-protective activities.

Keywords: Bangladesh, biological, chemical, Corchorus olitorious L.

ABSTRACT

Gum from the peels of unripe plantain, Musa acuminata was extracted, after crushing, with distilled water and bleached with sodium hypochlorite solution. Five different granule batches of paracetamol were prepared with different concentrations of the powdered gum at concentrations of 2, 4, 6, 8, and 10 % respectively, as mucilage. The disintegrant and lubricant were maize starch and magnesium stearate at 5 and 1 % total tablet weights, respectively. The wet granulation method was used with the incorporation of the disintegrant intragranularly. Similar granulations were made with a commercial binder - sodium carboxymethylcellulose (SCMC) for comparison. The flow properties of the granules were evaluated and the granules were compressed into tablets. The physicochemical properties of the tablets were evaluated. The plantain gum was fairly white. The granules produced with plantain gum showed similar flow properties with those produced with SCMC. The tablets formulated with plantain gum were more friable that the tablets formulated with SCMC, though, the values became close with increase in adhesive concentration. The tablets formulated with plantain peel gum disintegrated and released the drug faster than those formulated with SCMC. For example, the T_30% in 0.1 N HCl was 3 mins for granulations with 6% plantain gum, and 10mins for those formulated with 6% of SCMC. The results show that the gum from fresh peels of Musa acuminata could be a good alternative binder to the commercially sourced SCMC in pharmaceutical formulations.

Keywords: Musa acuminata, binder, sodium carboxymethylcellulose, paracetamol, tablets.

ABSTRACT

A series of novel E-3- (phenyl)-2-(phenyl) prop-2-enoic acid derivatives (1a-1h and 2a-2e) have been synthesized by the base-catalyzed condensation of phenylacetic acids (1) with aryl aldehyde in the presence of triethylamine gave the series of E-3- (phenyl)-2-(phenyl) prop-2-enoic acid (1a-1h). Reaction of thionyl chloride with the E-3- (phenyl)-2-(phenyl) prop-2-enoic acid in benzene under refluxing gave the corresponding acid chlorides, which on subsequent reaction with appropriate amines, and (dialky1amino) ethanol gave compounds 2a-2e the yield of compound was found to be in the range of 60-85%.The synthesized compounds were characterized by their physiochemical properties like solubility, melting point, IR spectroscopy, ¹H NMR spectroscopy, Fab MASS and elemental analysis.

Keywords: Phenyl acetic acid, Amines, Thionyl chloride, Dialkylamino 

ABSTRACT

A Reversed-Phase Ultra Performance liquid Chromatographic (RP-UPLC) method was developed for the simultaneous determination of Ciprofloxacin HCL, Doxycycline Hyclate  and Phenazopyridine HCL in tablet dosage form. The analysis was carried out using Acquity UPLC, BEH C–18, 50 X 2.1, 1.7µ column. Mobile phase, containing 0.05 M Ammonium Acetate Buffer: Methanol (50:50) pH adjusted to 4 with Ortho-phosphoric acid was pumped at a flow rate of 1mL/min with UV-detection at 278,350,378 nm Respectively. Retention time was 0.90 ± 0.01 min, 1.60±0.02 min & 4.17±0.01 min. for Ciprofloxacin HCL, Doxycycline and Phenazopyridine HCL respectively. The method was validated for linearity, accuracy, precision, and specificity. The method showed good linearity in the range 20, 50, 80,100, 120, 150, 200 ppm. The % R.S.D for precision and accuracy of the method was found to be less than 2%. The method was validated as per the ICH guidelines. The method was successfully applied for routine analysis of Ciprofloxacin HCL, Doxycycline and Phenazopyridine HCL in combined tablet dosage form.

Keywords: Ciprofloxacin HCL (CIPRO), Doxycycline Hyclate(DOXY) , Phenazopyridine HCL(PHENA) ,Ultra performance liquid chromatography.

ABSTRACT

The synthetic seed acquaintance has been developed to use somatic embryos and/or other micropropagules as seed analogues successfully in the field or greenhouse, and their mechanical planting at a mercantile level. Synthetic seed development from somatic embryo opens up new vistas in the field of agriculture. The technology provides methods for preparation of seed analogues called synthetic seeds or artificial seeds from the micropropagules like somatic embryos, axillary shoot buds, apical shoot tips, embryogenic calli as well as protocorm or protocorm like bodies. These artificial seeds offer an important packaging system. The technique cut short lengthy choice procedure of the usual recombination breeding and can convey the advancements of biotechnology to the doorsteps of the farmer in a cost-effective manner. Synthetic seeds present a number of return, easy management, storability, compact size of propagules, and transportability. This review provided useful information for the production and utilisation of synthetic seed through encapsulation of differentiating propagules (tissue fragments with shoot primordia) for various species. The present review focuses on the technology developed, its achievements, current scenario, the limitations resisting the application of the synthetic seed technology and the future perspectives.

Keywords: Synthetic seed, Artificial seed, Micropropagation, Explants

ABSTRACT

Nateglinide is an insulin secretogogues, meglitinide anti-diabetic drug used for the treatment of type II Diabetes mellitus. Film coated means 2% coating immediate release tablets. Superdisintegrants used for the formulation of immediate release tablets to decrease the disintegration time of tablets and disaggregate the granules into fines. Current investigation aims to access the impact of gradient concentration of sodium starch glycolate, Crosscarmellose sodium on the disintegration time also drug release rate of tablets. The drug-excipients interaction study was carried out by Fourier Transform Infra-red and Different Scanning Calorimeter. The six formulations were formulated by using 2, 4, 6 % concentration of Superdisintegrants. The hardness of each formulation was in between 100 to 140 N_. The disintegration time of formulation containing 6% (F-6), 4% (F-5) and 2 % (F-4) concentration of Crosscarmellose sodium was about 7.0, 6.0 and 3.0 min respectively. The formulation having sodium starch glycolate concentration of 2% (F-1), 4% (F-2), 6% (F-3) about 8.0, 6.0 and 4.0 min respectively. As the concentration of Superdisintegrants get on increase the disintegration time was decrease. The formulation containing sodium starch glycolate had more disintegration time than Crosscarmellose sodium containing tablets.

Keywords: Secretogogues, Diabetes mellitus, Superdisintegrants.

ABSTRACT

A Simple, selective, accurate, precise and linear RP-HPLC method was developed and subsequently validated for estimation of cinacalcet in bulk & tablet dosage form. Gradient elution at a flow rate of 0.8ml/min was used for separation of drugs in reversed-phase mode using Waters HPLC 22695 model on a INERTSIL ODS C₁₈ column (150 x 4.6 mm; 5µ) at a ambient temperature. Mobile phase consisted of water: methanol: acetonitrile (20:60:20). The UV detection wavelength was 235nm 20 µl was injected. The retention time for cinacalcet was 3.7min. The percentage RSD for precision and accuracy of the method was found to be less than 2%. The % recovery was within the range between 99.73% and 99.85%. The method was validated as per the ICH guidelines.

Key words: cinacalcet, RP-HPLC, validation

ABSTRACT

Three novel Mannich bases 5-[(4-chlorophenyl)-(4-methylpiperazin-1-yl)-methyl]-pyrimidine-2,4,6-trione :CBzBAPz(NM), 5-[(4-nitrophenyl)-(4-methylpiperazin-1-yl)-methyl]-pyrimidine-2,4,6-trione: NBzBAPz(NM) and 5-[(phenyl)-(4-methylpiperazin-1-yl)-methyl]-pyrimidine-2,4,6-trione: BzBAPz(NM) are prepared by the condensation of N-methyl piperazine with p-chlorobenzaldehyde / p-nitro benzaldehyde / benzaldehyde and barbituric acid and  characterized by physico-chemical,  spectroscopic, and powder X-ray diffraction studies. Further, Cu (II), Cd (II) and Pd (II) complexes of titled ligands are synthesized and characterized. Based on the experimental results, the chelating (bidentate) behavior of the ligands is accessed. The X-band e.p.r.spectrum, electrochemical studies of the Cu (II) complex have been carried out and discussed. Three novel Mannich bases and their complexes exhibit comparable potential cytotoxicity against breast cancer cell line (MCF-7), particularly, strong cytotoxicity is observed in the case of palladium. Morphological features of cells used for the study is photographed. Use of fluorochromesacridine orange and ethidium bromide reveals apoptotic morphological features.

Keywords: barbiturates, N-methyl piperazine, anticancer activity, Mannich bases, MTT assay.

ABSTRACT

A simple, sensitive, rapid, precise, and accurate Spectrofluorimetric method has been developed for estimation of Hydroquinone (HYQ) its pharmaceutical dosage forms.HYQ showed good fluoroscence intensity in double distilled water and so Double distilled water was selected as a solvent for estimation of HYQ. The optimized excitation and emission wavelength were 290 nm and 337 nm respectively with 2.5nm slit width for HYQ determination. The linear regression data for the calibration curves shows a good linear relationship over the concentration range of 50 to 900 ng/mL for HYQ with respect to fluorescence intensity. The LOD and LOQ values were found to be 6.88 ng/mL and 20.85 ng/mL respectively. The developed method was validated in terms of linearity, precision, accuracy, limit of detection and quantification, robustness as per International Conference on Harmonization Q2 (R1) guidelines. The utility of the developed method has been demonstrated by assay of commercially available cream formulations. The developed spectrofluorimetric method can be successfully applied for routine quality control of HYQ from its formulations.

Keywords: Hydroquinone (HYQ), Double distilled water, Spectrofluorimetric method, Validation.

ABSTRACT

A series of 3-amino-5-sugarimino-1, 2, 4-thiadiazolines have been synthesized by oxidative cyclization of sugar-3-amidinothiocarbamides by using bromine. These amidino thiocarbamides were prepared by interaction of guanidine and sugar isothiocynates. Guanidine itself plays an important role as antifungal, anticancer activities when it links with glycosides its acivity increased. These newly synthesized compounds have pharmaceutical uses. The identities of these newly synthesized compounds have been established on the basis of usual chemical transformation and IR, ¹H NMR, and Mass spectral studies. The synthesized compounds were screened for their in vitro antimicrobial activities using human pathogens.

Keywords: Sugar isothiocynates, guanidine, sugar-3-amidinothiocarbamides, 1, 2, 4-thiadiazolines, antimicrobial activity.

ABSTRACT

The purpose of this research was to develop mouth dissolve tablets ofdomperidone andpantoprazole, were prepared by direct compression technique. Pantoprazole inhabits gastric acid formation and thereby it is very efficient for the treatment of gastric and duodenum ulcers. Domperidone, an antiemetic drug, has been used as an add-on treatment in adults and children. The tablets were prepared using microcrystalline cellulose as diluent and  aspartames as sweetening agent along with three different levels of disintegrant. The superdisintegrant used in this study were CCS and SSG. The tablets were evaluated for weight variation, hardness, friability, wetting time, water absorption ratio, disintegration time (DT) and dissolution study. formulation prepared with 30% of CCS showed Disintegration time of 20seconds in vitro. Also the hardness, friability, dissolution rate of prepared tablets (batch F6) were found to be acceptable according to standard limits.

Keywords: pantoprazole, Domperidone, Superdisintegrants, melt in mouth tablet, Direct compression.

ABSTRACT

A simple and sensitive reversed phase high performance liquid chromatographic (RP-HPLC) method has been developed for the simultaneous quantification of ceftriaxone and cefpodoximeproxetil in artificial mixtures of commercial formulations and spiked human plasma. The separation was carried on C₁₈ (4.6 mm x 250 mm) column with a mixture of acetonitrile and 0.03 M triethylamine (3:1 v/v) adjusted to pH 7.0, with acetic acid, as mobile phase at flow rate of 0.9 mLmin^‒1 with UV detector at 240 nm. The chromatographic peaks were recorded at detection wavelength of 240 nm. The retention times of ceftriaxone and cefpodoximeproxetil were 2.111±0.014 min and 4.053±0.013 min respectively. The concentration versus detector response (Peak height) curve is linear in the range of 0.5- 250 µg mL^‒1 for ceftriaxone (R²=0.9996), and 0.5-500 µg mL^‒1 for cefpodoximeproxetil (R²=0.9995). The limit of detection (3.3σ/S) was found to be 6.62 ng mL^‒1 and 14.2 ngmL^‒1, respectively, for ceftriaxone and cefpodoximeproxetil. Similarly limit of quantification (10σ/S) was 20 ng mL^‒1 for ceftriaxone and 42.9 ngmL^‒1 for cefpodoximeproxetil. The developed method was applied to simultaneous determination of these antimicrobials in the artificial mixtures of commercial formulations and spiked human plasma.

Keywords: Ceftriaxone; cefpodoximeproxetil; simultaneous determination; artificial mixture; commercial formulations; spiked human plasma.

ABSTRACT

A simple, precise, accurate and stability-indicating reverse phase high performance liquid chromatography (RP-HPLC) method is developed for estimation of Levosalbutamol sulphate and Ipratropium Bromide in bulk and nebulizer dosage form. The method employed, with reverse phase Inertsil® 5μ C18 (250 × 4.0 mm) column in an isocratic mode, with mobile phase of acetonitrile: buffer in the ratio 77:23 (%v/v). The flow rate was 1.3 ml/min and effluent was monitored at 210 nm. Retention time was found to be 3.05 min., and 10.59 min. The method was validated in terms of linearity, accuracy, precision, limit of detection (LOD), limit of quantification (LOQ) etc. in accordance with ICH guidelines. Linear regression analysis data for the calibration plot showed that there was good linear relationship between response and concentration in the range of 25 – 150% of the working concentration (r2 > 0.999) respectively. The LOD and LOQ values for were found to be0.72,0.43, 1.24and 0.97 and μg/ml respectively. No chromatographic interference from placebo and degradants were found. The proposed method was successfully used for estimation of Levosalbutamol sulphate and Ipratropium bromide in bulk and nebulizer dosage forms.

Keywords: Levosalbutamol sulphate, Ipratropium bromide, RP-HPLC, Validation, Stability-indicating method.

ABSTRACT

The medicinal plants are widely used by the medical practitioners for curing various diseases in their day to day practice. Caesalpinia pulcherrima (Family: Fabaceae) is one of the most valuable medicinal shrub seen throughout tropical India.   The antibacterial activities of the hot and cold methanol extracts of the stems of Caesalpinia pulcherrima was evaluated on four bacterial strains like Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Proteus vulgaris. The invitro antibacterial activity of hot and cold methanol extracts was performed by cup plate agar diffusion method at different concentration of 10mg/ml to 50mg/ml using ciprofloxacin (ciprozol-500) in dimethyl sulphoxide as a standard drug for the comparison of antibacterial activity. From the experiment done the hot methanol extract of Caesalpinia pulcherrima did produce considerable antibacterial activity than the cold maceration extract was observed. The maximum antibacterial activity of hot and cold methanol extracts was exhibited against Bacillus subtilis when compared with standard drug. In addition the preliminary phytochemicals screening of the hot and cold methanol extracts of C.pulcherrima stems revealed the presence of alkaloids, carbohydrates, glycosides, saponins, tannins and steroids. The results obtained in the present study suggest that Caesalpinia pulcherrima stems can be used in treating diseases caused by the test organisms.

Keywords: Caesalpinia pulcherrima, hot and cold methanolic extracts, ciprofloxacin, antibacterial activity.

ABSTRACT

A total of 4 compounds have been isolated from a methanol extract of Bryophyllum daigremontianum. These compounds were identified as glut-5(6)-en-3β-ol (1), mixture of α-amyrin (2a) & β-amyrin (2b) and stigmasterol (3), by extensive analysis of NMR data and by comparison with published values. The crude extract was subjected to assay for antioxidant potential through determination of total phenolic content, membrane stabilizing and thrombolytic activities, which revealed potent antioxidant and moderate membrane stabilizing activities and inhibition of clot of rat’s blood.

Keywords: Bryophyllum daigremontianum, glutenol, α- & β-amyrin, stigmasterol, antioxidant, phenolics.

ABSTRACT

A liposome is a microscopic vesicle consisting of an aqueous core enclosed in one or more phospholipid layers, used to convey vaccines, drugs, enzymes, or other substances to target cells or organs. Liposomes are bilayered structures made of amphipathic (both hydrophobic and hydrophilic) phospholipids/cholesterol that spontaneously form closed structures when hydrated in aqueous solutions. Liposomes are acceptable and superior carriers having ability to encapsulate hydrophilic and lipophilic drugs and protect them from degradation. Topical liposomes have similarity to biological membranes they can store water-soluble and lipophilic substances in their different phases. Moreover, they are similar to the epidermis with respect to their lipid composition, which enables them to penetrate the epidermal barrier to a greater extent compared to other dosage forms. According to studies performed so far liposomes are biodegradable and non-toxic. The really new aspect with liposomes is that they are thought to act not only as drug transporters but also drug localizers. Thus vehicles can transport drugs to the wanted site of action within the skin by preventing systemic absorption and consecutively unwanted effects. The liposomal semisolid formulations could perform therapeutically better effects than the conventional formulations, as prolonged and controlled release topical dosage forms, which may lead to improved efficiency and better patient compliance. Such review giving an emphasis on topically applied liposomal formulations which encompasses methods of preparation, evaluation, mechanisms for enhancement in drug delivery through the skin and regulatory requirements necessitates as topical dosage form.

Keywords: Liposomes, Carriers, Topical, Evaluation

ABSTRACT

A new series transition metal complexes of Cu(II), Co(II), Ni(II) and Zn(II)  complexes have been synthesized from 2-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)phenol (AMPT). The nature of bonding and the geometry of the complexes have been deduced from elemental analyses, magnetic susceptibility, infrared, electronic, ¹H NMR, ¹³C NMR, and EPR spectral studies. The redox behavior of copper complexes was studied by cyclic voltammetry.  The second harmonic generation (SHG) efficiency was measured by Kurtz and Perry method. The ligand and their metal complexes were screened by Well diffusion method. The interaction of complexes with CT- DNA was investigated by viscosity measurement. Results suggest that all the complexes bind to DNA via an intercalative mode. The DNA cleavage ability of all the complexes was examined on calf thymus (CT-DNA) plasmids using gel electrophoresis experiment in presence of H₂O₂. From the results it is concluded that all the complexes cleave DNA.

Keywords: 1,2,4-Triazoles, Metal complexes, SGH,  Antibacterial activity, DNA cleavage. 

ABSTRACT

Traditional healing through herbs have been the experienced of many countries since ages, as they were generally whispered to be non toxic natural products. Contemporary medicine is more concern for the cure of diseases but remnants indifferent to health conservation. There is an urgent need to combine the best elements of traditional medicine and modern medicine to improve the health care system of human kind. For the reason that of the rapid progress of herbal drug an increasing need is felt to standardize the herbal products. It is needed to develop the scientific protocols such as SOP and pharmacopoeial standards of the herbal drug. Ficus carica Linn. (Moraceae) is commonly known as edible Due to the useful effect of leaves in skin diseases, Pharmacognostical standardization of F. carica leaves was carried out. The transverse section of leaves showed upper and lower epidermis with covering and glandular trichomes and midrib showed arc shaped vascular bundle. Successive extractive value was highest (23.606%) in case of aqueous extract. Mean ash values (%) were 23.04 (total), 6.48 (acid insoluble) 12.69 (water soluble). Loss on drying was 5.9107%. Resin content was found 1.33%. Phytochemical screening leaves powder showed the presence of carbohydrates, phenolic compounds, flavonoids, steroids, tannin, resin and acidic compounds. 

ABSTRACT

This study describes the development and characterization of Enteric coated pellets of duloxetine hydrochloride that results to improve gastric stability and enhance oral systemic exposure of novel serotonin and nor-epinephrine reuptake inhibitor (SNRI), duloxetine. Duloxetine Pellets were prepared by coating drug solution on sugar sphere followed by various layering in fluidized bed Coater (FBC) with different polymers like hydroxy propyl methylcellulose (HPMC E5), Crospovidone, Hypermellose Acetate Succinate and polysorbate 80 in suitable proportion. In vitro Dissolution studies were carried out in 0.1N HCl (pH: 2) for two hours followed by Phosphate buffer (pH: 6.8) for 1.5 hours with USP (Type-II) dissolution method. Absorption studies for Optimized pellets were carried out in Rats at 5 mg/kg dose; pellets were filled in Capsule size 9 administered orally with modified gavage needle. The optimized formulation has better correlation in both In vitro and In vivo system. The systemic exposure (AUC) and maximum concentration in plasma (Cmax) of entiric coated pellets of duloxetine was significantly higher than conventional suspension formulation. Finally it can be concluded that multiparticulate approach can be used to improve the stability and systemic exposure of pH sensitive and poorly water-soluble drugs such as duloxetine.

ABSTRACT

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical Q-absorbance ratio method for the simultaneous determination of Sparfloxacin and Dexamethasone. Absorbance ratio method uses the ratio of absorbances at two selected wavelengths, one which is an isoabsorptive point and other being the λ-max of one of the two components. Sparfloxacin and Dexamethasone show an isoabsorptive point at 271.2 nm in methanol. The second wavelength used is 241.6 nm, which is the λ-max of Dexamethasone  in methanol. The linearity was obtained in the concentration range of 3-18 μg/ml for Sparfloxacin and 1-6 μg/ml  for Dexamethasone. The concentrations of the drugs were determined by using ratio of absorbances at isoabsorptive point and at the λ-max of Dexamethasone. The method was successfully applied to pharmaceutical dosage form because no interference from the preservative was found. The suitability of this method for the quantitative determination of Sparfloxacin and Dexamethasone was proved by validation. The proposed method was found to be simple and sensitive for the routine quality control application of Sparfloxacin and Dexamethasone in Eye/Ear drops. The results of analysis have been validated statistically and by recovery studies.

ABSTRACT

A new simple, accurate, precise and reproducible Reverse Phase-High Performance Liquid Chromatography  method has been developed for the simultaneous estimation of Sitagliptin and Metformin in bulk and pharmaceutical dosage form using Symmetry C18 column (4.6 x 150mm, 3.5mm, Make: XTerra) in isocratic mode. The mobile phase has been prepared by using Potassium Dihydrogen Phosphate and Acetonitrile in different ratio at different pH. Several trials have been performed and it was found that ratio 0f 65:35 of Potassium Dihydrogen Phosphate and Acetonitrile respectively was shown a good peak at pH 5.8 which has been adjusted by using Sodium Hydroxide. The detection was carried out at 254 nm. The method was linear over the concentration range for Sitagliptin 10-30ppl and for Metformin 100-300ppm. The % recoveries of Sitagliptin and Metformin were found to be 99.1 to 100.6% and 98.8 to 100.7% respectively. The validation of method was carried out utilizing International Conference on Harmonization (ICH) guidelines. The described High Performance Liquid Chromatography method was successfully employed for the analysis of pharmaceutical formulations containing combined dosage form.

ABSTRACT

This paper describes a simple, rapid and sensitive bioanalytical method based on liquid chromatography / tandem mass spectrometry (LC–MS/MS) for the determination of integrase inhibitor raltegravir in human plasma samples. Carbamazepine was used as an internal standard (IS). Analyte and the internal standard were extracted from 200 µL of human plasma via solid phase extraction. The chromatographic separation was achieved on a C₁₈ column by using a mixture of acetonitrile and 0.1% formic acid (90:10, v/v) as the mobile phase at a flow rate of 0.8 mL/min. The calibration curve obtained was linear (r² ³ 0.99) over the concentration range of 20.1–4007 ng/mL. Method validation was performed as per FDA guidelines and the results met the acceptance criteria. A run time of 2.0 min for each sample made it possible to analyze more number of samples in short time, thus increasing the productivity. The proposed method was found to be applicable to pharmacokinetic studies in humans.

ABSTRACT

The present study describes a simple, accurate, precise and cost effective UV-VIS Spectrophotometric method for the estimation of Nateglinide, an anti-diabetic drug, in bulk and pharmaceutical dosage form. The solvent used was 0.1 N HCl+ 0.5 SLS solution and the λ max or the absorption maxima of the drug was found to be 212 nm. A linear response was observed in the range of 10- 60μg/ml with a regression coefficient of 0.999. The method was then validated for different parameters such as Linearity, Accuracy, Precision, Specificity, Robustness, Ruggedness, Limit of Detection and Limit of Quantification (LOQ). This method can be used for the determination of Nateglinide in quality control of formulation without interference of the excipients. Nateglinide was subjected to stress degradation under different conditions recommended by ICH such as acid, alkali, photolytic, dry heat and oxidative. The samples so generated were used for degradation studies using the developed method.

ABSTRACT

A specific and sensitive liquid chromatography-electrospray ionization tandem mass spectrometry method was developed for the determination of zolmitriptan in human plasma. Zolmitriptan and the internal standard (IS) rizatriptan were extracted by liquid–liquid extraction and were separated on a sunfire C18 column (100 x 2.1mm and 3.5µm) with isocratic elution of mobile phase consisting of 10mM ammonium formate containing 0.1% formic acid and acetonitrile. Electrospray ionization in multiple reaction monitoring mode was used to monitor the parent and the daughter ions of the analyte and the internal standard. The response is linear over a range of 0.5 to 100.0 ng/ml concentration with a correlation coefficient (r²) greater than 0.99 and an extraction efficiency of about 95%. The validated method can be applied to pharmacokinetic, toxicokinetic and bioequivalence studies.

ABSTRACT

A novel Schiff base ligand and its metal complexes of Co(II), Ni(II), Cu(II) and Zn(II)  were synthesized and characterized. The characterization was done by using elemental analyses, molar conductivity, magnetic susceptibility, Mass, ¹H NMR, ¹³C NMR, UV-Vis and IR spectroscopy. The experimental data predict that all the complexes are mononuclear with M(II) being coordinated by a tetradentate Schiff base ligand through the deprotonated oxygen atom, nitrogen atom in thiazole ring and two azomethine nitrogen atoms. The data confirm that the complexes have the composition of [ML] Cl type. The electronic absorption spectral data of the complexes propose a square planar geometry around the central metal ion. The biological activities of the synthesized compounds were tested against bacteria by well-diffusion method.

ABSTRACT

The novel metal chelates of 2-(8-quinolinol-5-yl)–methyl amino-5 -phenyl-1, 3, 4-thiadiazole (1) has been synthesized and their antimicrobial properties were evaluated. These compounds were synthesized by reaction of 2-(8-quinolinol-5-yl)–methyl amino-5 -phenyl-1, 3, 4-thiadiazole (1) with metal acetate and characterized using IR, ¹H-NMR and elemental analysis. The synthesized compounds were screened for their in vitro antimicrobial activity against microorganism P. Expansum. B. Thiobromine, Nigras pora Sp. T. roseum, A. Niger, B. megaterium, S. aureus, P. aeruginosa and E. coli. All of the compounds are active against the microorganism in which some are exhibited moderate to good activity, whereas some were less active.

ABSTRACT

The hepatoprotective activity of a Boerrhavia diffusa of 50 % ethanolic extract  was studied using Swiss albino rats. The animals received a single intraperitoneal injection of N-nitrosodiethylamine 200mg/kg body wt followed by subcutaneous injection of CCl4 in a dose of 3 ml/kg body wt. The administration of  Boerrhavia diffusa extracts and cisplatin decreased the liver weight and average liver weight, which shows the rehabilitating capability of extracts in respect with anticancer potency in comparison with the very much effective in preventing NDEA-induced multistage hepatocarcinogenesis possibly through antioxidant and  antigenotoxic nature, which was confirmed by various liver injury and biochemical tumour markers enzymes and molecular events. Boerrhavia diffusa extract dose dependently and significantly the increase in serum hepatic enzyme levels after NDEA& CCl4 treatment compared to the toxin control group. The results of this study confirmed the antioxidant and hepatoprotective activity of the Boerrhavia diffusa extract against carbon tetrachloride& N-nitrosodiethylamine induced hepatotoxicity in Swiss albino rats. 

ABSTRACT

The pivotal motif of the present research work is to develop immediate release tablets of Fexofenadine hydrochloride. The rate of dissolution and bioavailability of the Fexofenadine HCL may be increased by using superdisintegrant in its immediate release tablets. Direct compression method was adapted to prepare the tablets by using lactose, microcrystalline cellulose as filler, crospovidone and sodium starch glycolate as superdisintegrant in different concentration (2-8%). Tablet were prepared and evaluated for Hardness, friability, weight variation, content uniformity, wetting time, disintegration time and in-vitro drug release. Disintegration time decreased with increase in the level of crospovidone. Whereas, disintegration time increased with increase in the level of sodium starch glycolate. The results indicate that the selected batch of tablet formulation containing crospovidone provides DT between 3-6 minutes with sufficient crushing strength and accepted friability. It was concluded that immediate release tablet for Fexofenadine hydrochloride can be formulated for fast treatment of allergic rhinitis

ABSTRACT

A simple, economic, accurate Absorption ratio method was developed for the simultaneous estimation of Atazanavir Sulphate and Ritonavir in bulk and tablet dosage form. 0.1M Hydrochloric acid was used as a diluent. 1% Sodium Lauryl Sulphate is used as surfactant to enhance solubility of drugs in 0.1M hydrochloric acid. The absorptions were observed at 262.8nm and 297nm which were selected based on overlap spectra of Atazanavir Sulphate and Ritonavir. The linearity range was found to be 10-20 mg/ml. The proposed method was validated. The reports was expressed that the proposed method was found to be simple, precise, accurate and rapid for the simultaneous estimation of Atazanavir Sulphate and Ritonavir in bulk and tablet dosage form using absorption ratio method. 

ABSTRACT

A selective, sensitive and rapid UPLC-MS/MS method has been developed and validated for simultaneous quantification of pramipexole, ropinirole and rasagiline in human plasma using trimetazidine as internal standard (IS). The analytes and IS were extracted from 200 µL of plasma by solid phase extraction technique using strata cartridges which offers high sensitivity, wide linearity without interferences form endogenous matrix components. Chromatographic separation was achieved in 3.00 min run time on a Synergi Polar RP column using a 5 mM ammonium acetate/methanol mobile phase in gradient mode. The quantification of target compounds was performed in a positive electrospray ionization mode and multiple reaction monitoring (MRM). The proposed method was validated over the concentration ranges of 5-50000 pg/mL for each analyte. The intra- and inter-day precision and accuracy results were acceptable as per FDA guidelines. Stability of compounds were established in a battery of stability studies, i.e. bench top, auto sampler, dry extract and long term storage stability as well as freeze-thaw cycles. The validated method has been successfully used to analyze human plasma samples for application in pharmacokinetic studies.

ABSTRACT

A new simple fast accurate and economical reverse phase high performance liquid chromatographic method was developed for the determination of Ramipril and Olmesartan in bulk and tablet dosage form. The separation was eluted on a Inertsil C₈ column (100 mm x 4.6 mm; 5µ) using a mobile phase mixture of mixed phosphate buffer 6.8 and acetonitrile in a ratio of 65:35 v/v at a flow rate of 1.0ml/min. The detection was made at 219 nm. The retention times were 2.28min for Ramipril and 3.76min for Olmesartan. Calibration curve was linear over the concentration range of 2.5-15 µg/ml for Ramipril and 10 to 60 µg/ml for Olmesartan. The propose method was validated as per the ICH guidelines parameters like Linearity, specificity, precision, accuracy, robustness and ruggedness. The method was accurate, precise, specific and rapid found to be suitable for the quantitative analysis of the drug and dosage form.

ABSTRACT

Currently there is considerable interest in the development of drugs from natural products for various diseases. The purpose of this study was to evaluate the antidepressant activity of hydroalcoholic extract of leaves of Alocasia macrorrhizos(AM), which is known to have anti-oxidant activity. In this study, mice were randomly assigned to four groups of six mice each. Group 1and 2 served as control and standard where as group 3 and 4 were treated with hydro alcoholic extract of Alocasia macrorrhizos at the doses of 250mg/kg and 500mg/kg respectively. Drugs were suspended in 1% gumacasia and administered to mice orally one hour before test procedure. After 1 hour mice were screened for its antidepressant property using two well to established models for antidepressant screening like  Forced swim test and Tail suspension test. Study result showed that Alocasia macrorrhizos at 250mg/kg and 500mg/kg significantly reduced immobility duration in both the models when compared to control group showing its antidepressant property. Further when these groups were compared to standard imipramine there was significant difference in immobility duration with AM 500mg/kg where as AM 250mg/kg values were comparable to imipramine. Hence we have concluded that hydroalcoholic extract of leaves of Alocasia macrorrhizos is having  antidepressant property which was comparable to Imipramine at 250mg/kg and significantly better results than imipramine  at 500mg/kg dose. 

ABSTRACT

A simple, accurate, precise, reproducible and economical UV spectroscopic methods for simultaneous estimation of Flupentixol and Melitracen in tablet dosage form have been developed. simultaneous equation method employs formation and solving of mathematical simultaneous equation using 254 nm and 230 nm as the λmax of Melitracen and Flupentixol respectively in 0.1N HCl. These methods were validated as per ICH norms. Calibration curves were linear over the concentration ranges of 1-10 μg/ml for Flupentixol and 10-100 μg/ml for Melitracen with mean recovery of 100.71 ± 1.53 & 100.36 ± 0.66 for Flupentixol & Melitracen respectively by Simultaneous Equation method. The validation study is statistically significant as all the statistical parameters are within the acceptance range (% RSD < 2.0 and S.D. < 2.0) for both accuracy and precision. The methods are successfully applied to pharmaceutical formulation, with no interference from excipients as indicated by the recovery study. The proposed methods are simple, rapid, economic and accurate for routine simultaneous estimation of Flupentixol and Melitracen.

ABSTRACT

The manuscript describes validated simultaneous equation method for the simultaneous estimation of Amlodipine Besylate and Indapamide in combined dosage form. Simultaneous equation method was based on the estimation of both the drugs at two wavelengths i.e. absorption maxima of both drugs. An absorption maxima of Amlodipine besylate was 240 nm and absorption maxima of Indapamide was 215 nm in methanol. The linearity was obtained over the concentration range of 10 – 30 µg/mL for amlodipine besylate and 2 – 10 µg/mL for Indapamide with mean recovery of 99.45 ± 0.84 % and 99.46 ± 0.33 % for Amlodipine Besylate and Indapamide, respectively. These methods were found to be simple, sensitive, accurate, precise and economical and applicable for the simultaneous determination of Amlodipine Besylate and Indapamide in combined dosage form.

ABSTRACT

The manuscript describes validated Reverse Phase High Performance Liquid Chromatographic (RP-HPLC) method for the simultaneous estimation of Perindopril Erbumine and Indapamide in combined dosage form. The RP-HPLC separation was achieved on Intersil ODS C₁₈ column (250 mm x 4.6 mm i.d., 5 µm particle size) at 40^oC using mobile phase Acetonitrile : Acid Phthalate Buffer (pH 3.0 ± 0.05) (50 :50, v/v) at flow rate 1.0 mL/min. Quantification was achieved with photodiode array (PDA) detection at 240 nm over the concentration range of 10 - 50 µg/mL for Perindopril Erbumine and 3 - 15 µg/mL for Indapamide with mean recovery of 100.09 ± 0.52 % and 100.13 ± 0.09 % for Perindopril Erbumine and Indapamide, respectively. These methods were found to be simple, sensitive, accurate, precise and economical and applicable for the simultaneous determination of Perindopril Erbumine and Indapamide in combined dosage form.

ABSTRACT

The world is blessed with so many closely related plant species belonging to the same family and genus that their correct identification, organoleptic, physical, pharmacological evaluation and detection of adulterants, is of paramount importance. The objective of the proposed work is to carry out the Pharmacognostic investigation, volatile oil isolation, preliminary analysis and pharmacological study of the isolated volatile oil from the plant Zanthoxylum acanthopodium DC. Organoleptic studies, determination of stomatal number, and stomatal index, powder microscopy of the fruits, proximate analysis, essential oil isolation by hydro distillation technique, preliminary analysis and anti inflammatory activity of the essential oil. The fruit powder exhibited high values of total ash and sulphated ash content indicating high quantity of carbonates and oxides whereas lower acid insoluble ash indicating less siliceous materials like earth or sand. The essential oils exhibited significant anti-inflammatory activity in experimental animals compared to the standard drug Diclofenac Sodium. These values are helpful in determining the quality and purity of crude drugs in powdered form. As proper information regarding this plant was not available this study was carried out with an effort for correct identification of the plant and evaluation of pharmacological activity of its extracted oils. The encouraging finding of the study prompts for further research on the subject.

ABSTRACT

Ibuprofen self-emulsified drug delivery system (IBSEDDS) has been prepared, characterized and optimized to release 100% drug in one hour. The optimal formulation was subjected to stability and bioavailability studies in human volunteers. The stability was conducted under different storage temperature (4^oC, room temperature and 37^oC) for 8 months and evaluated for in-vitro drug release, particle size and turbidity. Bioavailability was evaluated after administration of a single oral dose of two formulations, test (HPMC capsule containing IBSEDD) and reference (HPMC capsule containing 50 mg drug in soybean oil), by 6 health human volunteers. The results showed that IBSEDDS was stable under different storage temperatures and the drug was more stable at 4^oC. The changes in particle size and turbidity were lesser at room temperature.  The pharmacokinetic parameters for test/reference were: the C_max , 0.892/0.468 ug/ml,  the T_max, 1/1.5hr and the AUC_0-∞, 3.956/1.986 mg.hr/ml. The % RBof IBSEDDS was 199.114. In a conclusion, the IBSEDD formulation stored at 4^oC were more stable regarding drug content but samples stored at room temperature were more stable regarding particle size and turbidity. The IBSEDD formulation showed higher rate and extent of drug absorption and higher bioavailability compared to the oily drug solution.

ABSTRACT

This study was carried out to determine the polyphenolic contents and antioxidant activity of hydroalcoholic extract of Gutenbergia nigritana leaves using in vitro models. The ability of the extract to scavenge free radicals such as 2,2-diphenyl-1-picrylhydrazyl (DPPH^•), hydrogen peroxide (H₂O₂) and nitric oxide (NO) was investigated. The ferric reducing antioxidant power, total phenols and flavonoids contents of the extract were also determined using spectrophotometric methods. The result showed that the extract scavenge the radicals in a concentration dependent manner. The Free radical scavenging potentials of the extract was found to be proportional to its polyphenolic contents. Our findings revealed that the leaves of Gutenbergia nigritana contain biologically active constituents and therefore may be used as a potent antioxidant for the management of radical related diseases.

ABSTRACT

Marine Streptomyces sp.T1027 obtained from South coast of India was discovered to produce and accumulate β-carotene under the influence of light in liquid shake flask culture. The accumulation of β-carotene was growth associated and controlled by light, aeration, carbon and substrate solubility. Starch was the ideal substrate for maximum growth (4.5-6.1 g l^-1) and β-carotene accumulation (92-130 μg g^-1). Rapid extraction was done in Dimethylsulphoxide, Methanol (1:1) Solvent mixture. The organism was sensitive to a variety of antibiotics; in turn it was able to inhibit the human pathogen Corynebacterium diphtheria. Commercial substrates with high soluble starch content were found to produce maximum biomass and β-carotene production.

ABSTRACT

The article, for the first time, reports High performance liquid chromatography [HPLC] method for estimation of Dapoxetine hydrochloride [DAP] and Tadalafil hydrochloride [TAD]. The analytical method was developed for both the drugs as API and for tablet dosage form. The separation of two drugs was achieved on High quality octa decyl silane [C18 250x 4mm i.d] 5μ column. The mobile phase consists of Acetonitrile and phosphate buffer in the ratio of 45:55. Mobile phase flow rate adjusted at 1 ml/min and pH at 4.2 using ortho phosphoric acid. The detection was carried out at a wavelength 254 nm. Retention time was found 4.46 and 10.11 min respectively for TAD and DAP. The method was validated for system suitability, linearity, accuracy, and precision and solution stability as per ICH guidelines. Linearity was obeyed in the range of 8-48 mg/ml and 24- 144 mg/ml with correlation coefficient of 0.997 and 0.998 for TAD and DAP respectively. Recovery studies were found within prescribed limits that was 98.83 for TAD and 98.93 for DAP respectively. Detection and quantification limit were found to be 0.225mg/ml and 0.682mg/ml for TAD and 0.163 mg/ml and 0.494mg/ml for DAP respectively which expresses higher sensitivity of the method. Assay results were found to be 98.52 % and 98.26 % in generic brand whereas 99.03 % and 98.11 in other brand for TAD and DAP respectively.

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A specific and accurate reverse phase high performance liquid chromatographic method was developed for the simultaneous determination Ebastine (EBA) and Montelukast Sodium (MONTE) in Combined dosage forms. The analysis was carried out using Phenomenex  C_18, column (250 mm × 4.6 mm id, 5 µm particle size) with Mobile phase consisting of  Methanol : Phosphate buffer (65:35 v/v) pH 5.0+0.05 was  pumped at a flow rate was 1.0 ml/ min and  Quantification was achieved with photodiode array (PDA) detection at 261 nm over the concentration range of 10 - 50 µg/mL for ebastine & Montelukast Sodium  with mean recovery of 100.32 ± 0.85 % and 100.15 ± 0.94 % for Ebastine and Montelukast Sodium, respectively. These methods were found to be simple, sensitive, accurate, precise and economical and applicable for the simultaneous determination of Ebastine & Montelukast Sodium in combined dosage form.

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Aqueous Extract Followed By Hydroalcoholic And Alcoholic Extract Gymnema Sylvestre Roxb.^1,2 Family Asclepiadaceae And Stevia Rebaudiana Bertoni³amily Compositae. Literature survey reveals that till date, no combination of Stevia rebaudiana and Gymnema sylvestre are available in any dosage form. In the present work, the main objective is to formulate, evaluate and validate anti-diabetic liquid oral preparation of Gymnema using Stevia as sweetener. Stevia, non-caloric natural sweetener has added advantage than artificial sweetener due to number of beneficial effects Successive solvent extraction of Gymnema sylvestre and Stevia rebaudiana were carried out with the solvents like petroleum ether (60-80⁰C), ethanol, hydroalcohol and water. Phytochemical screening of aqueous extract of formulation was performed and their purity was checked by TLC of aqueous extract of Gymnema sylvestre, formulation and deacylgymnemic acid were done. While preparing liquid oral formulation, aqueous extract of Gymnema sylvestre and Stevia rebaudiana were selected, because of their maximum yield and presence of phytochemicals, which were present in alcoholic and hydroalcoholic extract. Stevia rebaudiana is a natural sweetner. In the presented formulation, stevia was used as a sweetner to make the formulation sweet. Validation of liquid oral preparation was done. Physical, chemical evaluations were carried out. The amount of deacylgymnemic acid present was found to be 22.327 mg/ml by HPLC. 

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Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, widely effective in the treatment of ophthalmic disorders like, corneal ulcers and conjunctivitis. In the present study, an attempt has been made to formulate ciprofloxacin hydrochloride as sustained release in situ gel systems utilizing the concept of ion- activated gelation using Gelrite alone and with sodium alginate in combination with HPMC E50 LV. Prepared formulations were evaluated for several parameters like drug polymer compatibility, viscosity, gelling and gel retention time, clarity, pH, drug content, antimicrobial efficacy, sterility and in vitro drug release. Among all the formulations, batches G3 containing 0.6 %w/v of Gelrite, A6 and A7 containing 1% w/w of sodium alginate with 0.5 and 0.75 % w/v of HPMC E50LV respectively were selected based on their gelling properties. The drug release of A6 extended upto 7 h and that of G3 and A7 extended upto 8 h. The formulations showed pseudo plastic behaviour after gelling. G3 showed better stability and clarity than the alginate formulations and was taken for further evaluations. It showed better antimicrobial efficacy when compared with standard. The mechanism of drug release from the best formulation was further evaluated. Hence the developed in situ system may be an alternative to conventional eye drops. 

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A simple, accurate, precise and rapid reversed-phase high performance liquid chromatographic (RP-HPLC) method has been developed and subsequently validated for the estimation of Liraglutide in bulk and Parenteral Dosage form. The proposed method is based on the separation of drugs in reversed-phase mode using Waters HPLC 22695 model, Inertsil ODS column (250 x 4.6 mm, 5µm particle size).The optimum mobile phase consisted of methanol: phosphate buffer in the ratio of 85:15 v/v(Phosphate buffer pH 5.5) was selected as a mobile phase, flow rate of 1.0 ml/min and UV detection was set at 246 nm. The retention time was 3.25.The method was validated according to ICH guidelines. It was found to be accurate and reproducible. Linearity was obtained in the concentration range of 20-80 μg/ml . The percentage RSD for precision and accuracy of the method was found to be less than 2%. The proposed method can be successfully applied in the quality control of bulk and pharmaceutical dosage forms.

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Derivative spectroscopy is one of the important technique for as resolution of multi component systems. Many of the modern pharmaceutical formulations are so complex because they contains  number of excipients such as diluents, disintegrating agents, stabilizers, coloring agents or dyes, flavors etc. along with the active ingredient. Derivative technique is becoming increasingly popular in analytical spectrophotometry as a background correction and as a resolution enhancement technique. Derivative spectroscopy is a  technique which offers an alternative approach to the enhancement of sensitivity and specificity in mixture analysis. Derivative spectrophotometry is a technique which is based on derivative spectra of a basic, zero-order spectrum. Derivative spectroscopy is widely used in different fields of the analysis.

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The aim of this work is to prepare oral liquid formulation of the non-steroidal anti-inflammatory drug mefenamic acid with sustained release property using floating in situ gelling technique. Gellan gum and sodium alginate separately were used to form the gels. Results showed the release from gellan gum was slower than that from sodium alginate in concentration dependent manner; where the drug release decreased as the amount of the gelling agent increased. Results showed that increasing the concentration of gellan gum (0.25,0.5 and 1%w/v) caused a decrease in gelation time and floating lag time with floating duration for more than 8 hours and significant decrease (p<0.05) in drug release. Increasing the concentration of sodium alginate (1, 1.5 and 2%w/v) also results in significant decrease (p<0.05) in gelation time, floating lag time and drug release with long floating duration. On the other hand increasing gas generating agent calcium carbonate (0.5, 1 and 1.5%w/v) reduces significantly floating lag time and drug release but no significant effect on gelation time. Increasing drug loading showed significant increase in drug release. Sorbitol 5%w/v was added to the selected formula as sweetening agent, which leads to decrease in the viscosity with no significant effect on drug release. Overall results indicate that drug release followed diffusion control mechanism, and were used for optimizing the liquid formulation of mefenamic acid with sustained release property, minimizing side effects and improving the bioavailability as which may reduce the dose and dosing rate with optimum effectiveness.

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Bauhinia variegata (Mountain ebony) is a well known plant in traditional medicine which belongs to the family Cesalpiniaceae. It is widely used for various ailments like skin diseases, tumour, ulcers and various infections. Against this backdrop the present study attempts to scientifically evaluate the analgesic, antifungal, anti-tumour potential of this plant. The ethanolic extract of the plant was prepared by soxhlation. Acute toxicity studies carried out on the extract revealed that it was safe at the dose of 2000 mg/kg body weight. The extract was then evaluated for its analgesic activity by eddy’s hot plate method. The antifungal evaluation was carried against Candida albicans and Aspergillus fumigatus by disc diffusion method in Sabouraud agar medium. The extract was studied for short term in-vitro cytotoxicity against DLA cell lines by Trypan blue assay method. The ethanolic extract of Bauhinia variegata bark exhibited significant analgesic activity at both the doses of 200 and 400 mg/kg body weight (p<0.05). It possesses in-vitro cell cytotoxicity against DLA cell lines (IC₅₀ 153). It also showed good antifungal activity against Aspergillus fumigatus and Candida albicans. The MIC was found to be 4.15 and 1 μg/ml respectively.

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Drug delivery of highly lipophilic molecules through the transdermal route is unsuitable when systemic effect is desired. Besides the different physical and chemical approaches for permeation enhancement, a novel method has been drawn for improvement in permeation behaviour. Here, the drug molecule was supramolecularly complexed with a phospholipid molecule to form a novel chemical entity possessing improved permeation behaviour suitable for transdermal application. Curcumin (CMN) was used as model drug for preparation of Curcumin-Phospholipid Supramolecular Complex (CPSC) and was characterized by FT-IR Spectroscopy and X-Ray Diffraction Analysis. Comparative solubility study of CPSC in water and n-octanol was performed. The prepared CPSC was incorporated in polymeric matrix films of Eudragit RL100 and Eudragit RS100 and the physicochemical compatibility was studied. The permeation kinetics and permeation parameters of the films were studied against a control batch formulation loaded with uncomplexed CMN across processed excised pig ear epidermis. Skin irritation test was perfomed on rats for safety assessment of films. Analytical reports suggested supramolecular complex formation. The solubility study showed increased hydrophilicity of the prepared CPSC. The FT-IR Spectroscopy and Differential Scanning Calorimetry (DSC) confirmed no interaction between polymers and CPSC. The formulations loaded with CPSC followed zero order and Higuchi model kinetics and possessed improved permeation parameters and a good enhancement ratio against the control batch. No skin reactions were observed during the skin irritation test. The conducted experiments suggested the supramolecular phospholipid complexation to be an effective permeation enhancement technique for transdermal route. 

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Starch from P.esculentus tubers was extracted and chemically modified using four different methods. Dextrinization of the native starch was done by heating in a hot air oven at 200^oC, while hydrolysis was achieved by HCl/ethanol hydrolysis. Gelatinization of the native starch was achieved at 90^oC while the starch xerogel was obtained by precipitation with 95% ethanol. Physicochemical characterization of these chemical forms was carried out in comparison with the native starch. These modified forms were then employed as binder/disintegrant (at 5% use level) in chloroquine phosphate tablets.  The results showed that the modified forms of the starch possessed better flow properties compared with the native starch. All batches of tablets gave maximum release of the Active Pharmaceutical Ingredient (API) within 45 min of study except tablets containing the starch xerogel or starch dextrin (200^oC). The present study indicated that the starch xerogel or dextrin may be suitable as binders in conventional tablet formulations at low concentrations and may find application as hydrophilic polymer matrices in sustained release tablet formulation.

Keywords: P. esculentus starch, disintegrant property, binder property, tablet formulation, modification, xerogelized derivative.

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Tablets of Oxaliplatin combined with Curcumin was prepared for colon specific delivery using guar gum as matrix carriers in varying concentrations from 40% to 65%. The drug concentration in the tablet was estimated by the newly developed and validated UV derivative spectroscopy method. In vitro drug release profile was studied in changing media method (0.1N HCl, phosphate buffer media, pH 7.4 and simulated colon fluid containing phosphate buffer pH 6.8 added with rat ceacal content). The drug release profiles from PB7.4 and simulated colon fluid were found to be dependent on the gaur gum concentration. Matrix tablets of Oxaliplatin and Curcumin combination showed ~65% of Oxaliplatin and 37% of curcumin release. The colon tissue homogenate studies conducted after oral administration of the optimized tablets showed the recovery of 167.5µg Oxaliplatin and 80µg. curcumin. X-ray Images of matrix tablets containing barium sulphate in Rabbit showed tablets to be intact in small intestine (3 hours after administration) but were diffused and spread out in large intestine and colon later confirming enzyme mediated erosion of the tablet in these regions.

Keywords- Oxaliplatin, Curcumin, Matrix tablets, Guar gum, Colon specific delivery, Controlled release.

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The present study deals with the formulation of multiple type floating beads of Ofloxacin to prolong gastric residence time (upto 24 hours) for slow and complete release in stomach and to provide sustained release action. Since, its solubility and absorption is better in the upper part of GI tract, so it was proposed to prepare floating beads of Ofloxacin to localize the drug at its maximum absorption site. Floating beads were prepared by drop wise addition of 3%, 4%, or 5% w/v Sodium Alginate solution containing drug and different gas forming agents or oils, into Calcium chloride solution 1% w/v in glacial acetic acid (10%) using 21 G needle.  The solution containing suspended beads were stirred with magnetic stirrer for 10 minutes to improve the mechanical strength of beads and allowed to complete the reaction to produce gas.  The fully formed beads were collected, washed with ethanol and distilled water and subsequently dried. Different oils such as Peppermint oil and Light liquid paraffin were used in the ratio of 3:5, 3:10, 3:15, and 3:20 respectively. The beads were evaluated for average diameter of beads, lag time, duration of floating drug entrapment efficiency, percent drug loading, floating time and in-vitro drug release in fasted and fed state. As we increased the concentration of polymer and oils, the diameter of beads increases taking all the parameters such as drug ratio, curing agent, curing time, needle nozzle size, dropping rate and height of needle from calcium chloride solution to be constant. The gastric retention of sodium alginate floating beads was best found to be using 20% light liquid paraffin. Also the lag time at this concentration was found to be zero thus leading to float into stomach for upto 24 hours. The drug release profile was best observed in using 4% of sodium alginate polymer and it was 92.719% in 20 hours.

Keywords-floating beads, ionotropic gelation, beads size, effervescent system, sodium alginate