Ravi

The present investigation has been undertaken with aim to formulation and evaluation of etoricoxib gel with different gelling agent and different penetration enhancer. Etoricoxib is highly selective cyclooxygenase-2 (COX-2) inhibitor. In this present study gel with carbopol, HPMC and Na-CMC as gelling agent prepared with different penetration enhancer like propyl glycol, oleic acid. Menthol oil. Formulation were evaluated for pH, stability study, spreadibilty, extrudabilty, bioadhesive (ex-vivo), skin irritation, viscosity, appearance and In-vitro drug diffusion. The formulation of Etoricoxib topical gel was prepared using carbopol, HPMC and Na-cmc in three batches A, B and C. With the consideration of all formulation characteristic and parameter we selected batch-A formulation for further study of anti-inflammatory and anti-analgesic activity. It was concluded that the Etoricoxib gel formulation containing carbopol with increase concentration of propyl glycol 10% and 2% oleic acid (OA) was suitable for topical application and it shows comparable result with market product and shows much better result of formulation, anti-inflammatory and anti-analgesic activity.

Eye is a window to the outside world and hence it becomes an important part of our body. Various diseases occurring in the eye cavity are difficult to treat. Some diseases require continuous use of medicine and other requires surgery. Lacrisert, Vitrasert, Mydriasert, Prosert etc. are patented technologies useful in the treatment of eye disorders. In this article brief description of various patented technologies such as Eyegiene kit, Ophtha coils, Versidoser, Microneedle, Implantable MEMS ocular drug delivery system, Ocuseal liquid bandage, Filter paper strips is given.

Ophthalmic drug delivery is one of the most interesting and challenging endeavors facing the pharmaceutical scientist. The anatomy, physiology and biochemistry of the eye render this organ highly impervious to foreign substances. The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid pre-corneal elimination of the drug may be overcome by the use of in situ gel forming systems that are instilled as drops into the eye and then undergo a sol-gel transition in the cul-de-sac. The purpose of the present work was to develop an ophthalmic drug delivery system of Pefloxacin mesylate for in situ gelling system byusing ion sensitive gelling agent (Gelrite) and viscofying agent (HPMCK4M). Optimization by 22 factorial design using Design expert software 8.0 version was applied to the formulations. Formulation with Gelrite (gellan gum) and HPMC K4M shows percent drug content of 99.83%, viscosity of 1864 cp at 20 rpm and in-vitro drug release of 88.32% which shows formulation is good. The developed formulation was found to be stable and provided sustained release of the drug over 8 hours.

Liquid chromatography-mass spectrometry (LC-MS) is sensitive technique that is affected by matrix effect. It arises due to phospholipids, proteins or metabolites present in biological fluids. It either increases or decreases the ionization of sample and affects detection limits. By careful evaluation of matrix effect on the drugs and their ionization in LC-MS the sensitivity could be improved. Evaluation of matrix effect for bio estimation of prasugrel hydrochloride is done by sample preparation methods, chromatographic conditions, internal standard and mass spectrometric conditions. A LC-MS method was developed for prasugrel hydrochloride with mobile phase consisted of ammonium formate (5mM, pH 7.5): acetonitrile (30:70, %v/v) at 1 mL/min flow rate and PDA detection at 220 nm. The mass detection method was after ionization with ESI probe, CDL temperature 230°C, detector voltage-1.5 Kv, nebulisation gas flow-1.5 L/min and column temperature was 30.5°C. The molecular ion peak was identified at m/z of 410 and product ion peak at m/z 374. The plasma spiked with prasugrel was subjected to each evaluation process and matrix effect was studied.  In sample preparation technique, the extraction efficiency and process efficiency were also calculated. The study results have shown that the matrix effect could be reduced systematically by the procedures performed and the sensitivity of LC-MS in the detection and quantification was increased to detect 20 ng/mL of Prasugrel from plasma.

A simple, specific, sensitive, precise and stability-indicating reversed phase high performance liquid chromatographic method was developed and validated for the simultaneous determination of thiocolchicoside and aceclofenac, using a RP-18 column and a mobile phase composed of 0.1% trifluoroacetic acid: acetonitrile (45:55). The retention time of thiocolchicoside and aceclofenac were found to be 2.35 and 13.2 min, respectively. Linearity was established for both thiocolchicoside and aceclofenac in the range of 0.08-0.8 and 1-10 µg/ml. Both the drugs were subjected to acid, alkali and neutral hydrolysis, oxidation, dry heat, and photolytic degradation. The degradation studies indicated that both thiocolchicoside and aceclofenac were susceptible to acid, alkaline and neutral hydrolysis. The degradation products of thiocolchicoside and aceclofenac were well resolved from the pure drugs with significant differences in the retention time values. This method can be successfully employed for simultaneous quantitative analysis of thiocolchicoside and aceclofenac in bulk drugs and formulations.

A simple, rapid and specific Second order derivative spectroscopic method with good sensitivity was developed and validated for the simultaneous determination of Desloratidine and Pseudoephedrine HCl in pharmaceutical dosage form. In Ethanol, the quantitative determination of both drugs carried out using second derivatives values measured at 268 and 271 nm for Desloratidine and Pseudoephedrine HCl respectively using a Shimadzu UV-Visible spectrophotometer. In this proposed method both drugs obeyed linearity within the concentration range of 5-30 µg/ml and 80-800 µg/ml for Desloratidine and Pseudoephedrine HCl respectively. The low RSD values indicate good precision and high recovery values indicate accuracy of the proposed method. The proposed method has been applied to the determination of drugs in commercial formulations. Assay results were in good agreement with label claim. The method was validated as per ICH guidelines. The developed method was simple, accurate, precise, specific, sensitive and reproducible which can be efficiently and easily applied to pharmaceutical dosage forms.

A simple, accurate, precise, specific, sensitive, reproducible and Reliable RP- HPLC Method was developed for Quantitative Estimation of Metaxalone and Diclofenac potassium in Pharmaceutical Dosage Form. The developed RP- HPLC method with the mobile phase Methanol: Water (80: 20) and Qualisilgold-C18 (250Χ4.6mm, 5μm particle size) as stationary phase with a flow rate of 1.0 mL/minute by using λmax 275nm and PDA detector. Proposed method was found to be linear in the concentration range of 8.0 to 80.0 μg/mL for Metaxalone and 1.0 to 10.0 μg/mL for Diclofenac potassium respectively, and the correlation coefficient was found to be 0.9991 for both the drugs. Precision study showed that the % RSD was within the range of acceptable limits (< 2), and the % Recovery was found to be in the range of 99.29%-101.28% for Metaxalone and 99.98%-102.45% for Diclofenac potassium. The proposed method has been validated as per ICH guidelines.

There are various approaches for the delivery of therapeutic substance to the target site in a controlled release fashion. One such approach is using microspheres as carriers for drugs or active pharmaceutical compound. However, the success of this drug delivery system is limited due to their short residence time at the site of absorption. Mucoadhesive microspheres can be tailored to adhere to any mucosal tissue including those found in stomach, thus offering the possibilities of localized as well as systemic controlled release of drugs. This article presents the  advantages of Mucoadhesive microsphere, mechanism, theories involved in mucoadhesion, factor that affect the mucoadhesion, polymer in Mucoadhesive drug delivery system, methodology of preparation of Mucoadhesive microsphere, method of evaluation and their applications in drug delivery. Mucoadhesive drug delivery systems promises several advantages that arise from localization at a given target site, prolonged residence time at the site of drug absorption and an intensified contact with the mucosa increasing the drug concentration gradient.

The present investigation was aimed at estimating the effectiveness of the edible mucilage of Borassus flabellifer fruit as a polymer in the development of a gastric floating dosage form of ranitidine HCl. Borassus flabellifer fruit mucilage, was shown to aid in the formulation of floating tablets. In the present study, it was used as a pharmaceutical excipient and its efficiency was compared with HPMC in the formulation of ranitidine HCl floating tablets. Sodium bicarbonate was used as a gas-generating agent, ranitidine HCl  tablets were prepared by direct compression method. The prepared tablets were evaluated for physicochemical parameters and found to be within range viz. hardness, swelling index, floating capacity, thickness, and weight variation. Further, tablets were evaluated for in vitro release characteristics for 12 hrs. All in all, the formulation F3 manifested a prolonged release of the active ingredient. The optimized formulation F3 followed higuchi’s mechanism. Based on the diffusion exponent (n) value, the drug release was found to be diffusion controlled. From the study, it was evident that the mucilage manifested all the characteristics of a good pharmaceutical excipient that can be used for the formulation of floating tablets.

A simple validated high performance thin layer chromatographic method was developed for the determination of Aceclofenac in presence of its degradant. Separation of Aceclofenac from the degradant could be achieved using aluminium backed silica gel 60 F254 plate with toluene: ethyl acetate: glacial acetic acid, (6:4:0.02v/v) as mobile phase. Densitometry analysis was carried out at 282 nm. The method showed high sensitivity with good linearity over the concentration range of 0.5 – 4 µg/spot. The method was successfully applied to the analysis of pharmaceutical formulation containing Aceclofenac with excellent recovery. The LOD and LOQ were found to be 0.1 and 0.5 µg/spot. Aceclofenac was subjected to hydrolytic, oxidative, thermal and photolytic degradation. It was found that the drug was highly susceptible to acid hydrolysis. Kinetic investigation of the drug followed pseudo-first order reaction. From the Arrhenius plot the activation energy was found to be 13.19 kcal/mole. Statistical analysis revealed that the developed method is accurate and reliable. Hence it can be used for routine quality control analysis of Aceclofenac in tablet formulation.