Sanjay

The objective of present study was to prepare and evaluate Zaltoprofen (ZLT) enteric coated oral mucoadhesive sustained release (SR) tablet in order to improve its GI residence time and improve its bioavailability by using natural biopolymers like xanthan gum and semisynthetic polymer HPMC for its safe use in rheumatoid arthritis, osteoarthritis, ankylosing spondylitis condition. The sustained release polymers, hydroxypropyl methylcellulose (HPMC) of different viscosities and xanthan gum evaluated in different proportions as a major matrix material. Drug-polymer compatibility studies by FTIR and DSC gave confirmation about their purity and showed no interaction physically between drug and selected polymers. ZLT matrix tablets were prepared by wet granulation.  The effect of polymer concentration on the drug release profile and in-vitro bioadhesion of the matrix tablets was studied. A 32 full factorial design was utilized in the optimizing the levels of HPMC and Xanthan gum. Concentration of HPMC K4M and the concentration of xanthan gum per tablet were used as the independent variables.  The dependent variables were the bioadhesive strength, percent drug dissolved at 2, 6 and 10 hours. The data obtained were fit to a model and polynomial equations were generated. Response surface graph was generated based on these equations. Formulation composition with desired release characteristics and bioadhesive strength were found to be predictive using this model. The optimized factorial batch was further given the coating of Opadry® enteric (94 series) polymer in order to avoid GI disturbances. The Z-22 tablets were kept for stability study at 40°C ±2°C and 75% ± 5% RH for a period of 6 months according to ICH guidelines. The formulation was found to be stable after 6 months of study. The pharmacokinetic parameters Cmax, Tmax, Mean Residence Time (MRT) and Area under Curve (AUC) of developed SR tablet were found to be improved with significant difference (p

The study aims at developing novel extended release pellets of venlafaxine. The main objective of the work was to develop robust extended release formulations of Venlafaxine (test formulation) for regulated markets having comparable in-vitro dissolution profile with Innovator product - Effexor® XR (Reference Product). Venlafaxine spheroids were made using extrusion spheronization technique. The release of the drug from the spheroids was controlled by applying a coating comprising ethyl cellulose as rate controlling polymer. The coated pellets were then encapsulated in the hard gelatin capsules. The in-vitro dissolution studies were conducted to evaluate the release of the drug venlafaxine from the coated spheroids contained in capsule at pH 6.8 using phosphate buffer. The in-vitro dissolution profile of the test compositions was compared with Reference Product Effexor XR. The results obtained showed that the test formulations had higher percentage release of venlafaxine in initial time period. Therefore, a better control on the release was desired. During the manufacturing of spheroids, it was observed that more fines were generated during the extrusion spheronization, which is not suitable for large scale production of the formulation. Accordingly batches were optimized using different types of binder and coating composition. Effect of the binder and percentage coating was studied. The drug release of venlafaxine using Povidone K30 as binder, Ethyl cellulose and Acryl-EZE MP 93018508 white as release control polymers was compared with innovator’s drug release and was found to be equivalent. From the results, it was concluded that use Povidone K30 as binder during extrusion spheronization process results on generation of less fines, thus increases the yield of the product. Also, the formulation containing dual coating of Ethyl cellulose and Acryl-EZE MP 93018508 on the spheroids containing Povidone K30 as binder showed the dissolution profile similar to that of the Reference Product Effexor XR.

A simple UV-Visible spectrophotometric method is developed for the simultaneous determination of Ebastine and Phenylephrine hydrochloride in pharmaceutical dosage form using  the  first order derivative spectrophotometric method. The determination of both the drugs is based on the respective zero crossing point (ZCP) of their first order derivative spectra obtained in methanol. The first order derivative spectra were obtained using methanol as a solvent and the determinations were made at 241.0 nm (ZCP of Phenylephrine HCl) for Ebastine and 232.0 nm (ZCP of Ebastine) for Phenylephrine hydrochloride. The linearity was obtained in the concentration range of 4-24 μg/ml for both drugs and correlation coefficient (r2) were found to be 0.9994 and 0.9991 for Ebastine and Phenylephrine hydrochloride respectively. The percentage purity of drugs in combined tablet dosage form was found to be 100.02 % for Ebastine and 99.89 % for Phenylephrine hydrochloride. The % recoveries were found to be 99.88% for Ebastine and 99.24% for Phenylephrine hydrochloride.  The method was found to be simple, accurate and precise and was applicable for the simultaneous determination of Ebastine and Phenylephrine in tablet dosage form.

Increase in anal resting pressure (ARP) is considered as the primary cause of chronic anal fissure (CAF). Reduction in ARP is the primary objective in treatment of CAF. Topical diltiazem is considered as first-line treatment option in CAF as surgical treatment may be associated with several post operative complications including permanent incontinence in some cases. Few studies have reported that lidocaine alone is inferior to anal dilators for pain relief in CAF which suggest that relief of internal anal sphincter is required for effective symptomatic management. The aim of this study was to evaluate whether combined treatment with diltiazem and lidocaine has any significant advantage over diltiazem monotherapy in patients with CAF. To evaluate this, 150 patients were enrolled and randomized to either treatment group. ARP, pain intensity and adverse events were recorded at various time points over 20 days study period. Fall in the mean ARP from baseline was comparable in both the study groups. However, significantly greater fall in pain intensity from baseline was observed with combined treatment with diltiazem and lidocaine, which can be attributed to the additional local anesthetic effects of lidocaine with combination treatment. No patient had any systemic or local adverse effects. Global assessment by patients and investigator was also favourable for combination treatment. We conclude that combined treatment with topical diltiazem and lidocaine is safe and effective option for pharmacological treatment of CAF, and addition of lidocaine to diltiazem significantly increases the pain relief achieved with diltiazem alone.

Immunomodulators are natural or synthetic substances that help in regulation or normalize or modify the immunity of an individual to favor a particular immunological response. Immunomodulator corrects immune systems that are out of balance. Natural immunomodulators are less potent than prescription immunomodulators. Synthetic immunomodulators medications, work by suppressing immune system and decreasing inflammation in the digestive tract in people with inflammatory bowel disease, ulcerative colitis etc. The benefits of immunomodulators are from their ability to stimulate natural and adaptive defense mechanisms, such as cytokines, which enables the body to help itself. Two types of immunomodulators: Immunosuppressants; agents which suppress immune system and used for the control of pathological immune response in autoimmune disease and Immunostimulants; agents which used to enhance body's resistance against infections. A large number of disorders such as immunodeficiency state, autoimmune disease, cancer and viral infection can be treated with immunostimulants drugs.

Nanotechnology can be defined as the manipulation, precision-placement, modeling and manufacture of material at the nanometer scale. The purpose of this review is to discuss the impact of nanotechnology in the treatment of the major health threats including cancer, infectious diseases, metabolic diseases, autoimmune diseases, and inflammations. Indeed, during the past 37 years, the explosive growth of nanotechnology has burst into challenging innovations in pharmacology. Although the introduction of nanotechnology obviously permitted to step over numerous milestones toward the development of the magic bullet proposed a century ago by the immunologist Paul Ehrlich. Cancer cells have unique properties that can be exploited by nanoparticles. They can be used very effectively for drug delivery. Normally, drugs work through the entire body before they reach the disease-affected area. Using nanotechnology, the drug can be targeted to a precise location which would make the drug much more effective and reduce the chances of possible side-effects. A great advantage of using nanotechnology for drug delivery is that the amount and time of drug release can be easily controlled by predetermination of nanoparticle. Nanotechnology is still in its early stages. The applications discussed in this review have already been developed and are already helping patients all over the world. Keywords- Nanoparticle, Cancer, Alzheimer's disease, TDDS

A simple, precise, accurate and stability-indicating reverse phase high performance liquid chromatography (RP-HPLC) method is developed for estimation of Levosalbutamol sulphate and Budesonide in bulk and suspension for inhalation 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 40:60 (%v/v). The flow rate was 0.8 ml/min and effluent was monitored at 266 nm. Retention time was found to be 3.16 min., 17.94 min. and 20.90 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 be 0.43, 0.72, 0.97 and 1.24 µg/ml respectively. No chromatographic interference from placebo and degradants were found. The proposed method was successfully used for estimation of Levosalbutamol sulphate and Budesonide in bulk and suspension for inhalation dosage forms.

The phytochemical analysis was carried out for standardization of fruits of Opuntia elatior Mill. The fruits were preliminary evaluated by estimation of proximate analysis. Presence of betacyanin was confirmed by spectrophotometric and high performance liquid chromatography coupled with mass spectroscopy techniques. The average weight of fruit was 24.568 ± 7.134 g/unit and the percentage of peel and seed was very low compared to the edible portion. Phytochemical analysis indicated the presence of color pigment betacyanin as an active principle and sugar content in high amount and low acidity of fruit which make it very sweet and delicious. The total betacyanin content (47.10 mg/100 ml) equivalent to betanin obtained from fruits of Opuntia elatior Mill. was higher as compared to Opuntia ficus-indica and Opuntia undulata Griff. while lower as compared to Opuntia stricta Haw. 

A simple, rapid and precise Reverse Phase High Performance Liquid Chromatographic method was developed for simultaneous estimation of Eperisone hydrochloride and Diclofenac sodium in pharmaceutical dosage form by reverse phase Pinnacle DB C-18 column (250 mm, 4.6 mm, and 5 μm). The sample was analyzed using 50mM ammonium acetate buffer containing 0.2% triethylamine (pH-4.0 adjusted with glacial acetic acid): Acetonitrile (40:60, v/v), as a mobile phase at a flow rate of 1.0 ml/min. and detection at 273 nm. The retention time for Eperisone hydrochloride and Diclofenac sodium was found to be 3.07 min and 5.56 min, respectively. The linearity of developed method was achieved in the range of 10-100 μg/ml for Eperisone hydrochloride and 10-100 μg/ml for Diclofenac sodium. The method was validated in terms of accuracy, precision, linearity, limit of detection, limit of quantitation, robustness and ruggedness as per ICH guidelines.

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical second derivative spectrophotometric method for the simultaneous determination of Paracetamol and Pamabrom in dosage form. The derivative spectrophotometric method was based on the determination of both the drugs at their respective zero crossing point (ZCP). The second order derivative spectra were obtained in dist. water and the determinations were made at 268.2 nm (ZCP of Pamabrom) for Paracetamol and 225.0 nm (ZCP of Paracetamol) for Pamabrom. The linearity was obtained in the concentration range of 4-18 μg/ml for Paracetamol and 2-16 μg/ml for Pamabrom The method was found to be simple, sensitive, accurate and precise and was applicable for the simultaneous determination of Paracetamol and Pamabrom in pharmaceutical tablet dosage form.