Quick Links

FORMULATION AND EVALUATION OF OPTIMIZED BATCH IN SITU GEL OF ONDANSETRON HYDROCHLORIDE

Ankit Kushwaha*, M. K. Gupta, Anandiya Goswami

Nasal route for drug delivery is the route which has been utilized from ancient times for recreational purpose. The main advantage of this route is the presence of highly permeable monolayer epithelium and rich vascularised submucosa, By this route hepatic first pass metabolism is avoided and also drug can be easily administered to brain by crossing blood brain barrier, but the main drawback of these routes is that a very low volume can be instilled (0.25 to 0.5 ml) in droplet form therefore drug loading becomes a major problem in exploring and utilizing this route. Present study aims to overcome this problem of drug loading by utilization of novel concept of mixed solvency and minimizing the drug clearance by formulating in situ mucoadhesive gel. By this concept the solubility of this drug can be easily increased at nasal cavity. pH and a higher drug loading is also expected. As the drug loading of these antiemetic drugs isincreased at nasal pH, the amount of drug crossing the olfactory region and blood brain barrier (BBB = highly lipophilic) will be increased. More amount of drug will reach brain’s CTZ centre and will help in prevention and treatment of emesis.


PREPARATION, CHARACTERIZATION, EVALUATION AND SOLUBILITY ENHANCENMENT STUDY OF DRY POWDER FOR INJECTION OF LAMOTRIGINE USING MIXED SOLVENCY TECHNIQUE

Chetan kumar Patil*, M. K. Gupta, Anandiya Goswami, Ramlakhan Patel

Lamotrigine is an anti-epileptic drug used in the treatment of epilepsy and bipolar disorder. An effort was made to formulate the dry powder for injection of lamotrigine with the help of mixed solvency technique. In this technique for poorly soluble drugs to reduce concentration of individual solubilizers and to minimize the toxic effect of solubilizers. Formulation SB-6 shows maximum solubility while other shows less solubility. Formulation SB-1 shows maximum stability as compared to other formulations.


DESIGN AND EVALUATION OF ZERO ORDER ONCE DAILY ENTERIC EXTENDED RELEASE MATRIX TABLET CONTAINING OXYBUTYNIN HYDROCHLORIDE

Rashad, Amira Ahmed* *, El-Gazayerly, Omaima Naim, Abd El Rehem, Randa Tag

Oxybutynin Hydrochloride is antimuscarinic drug used for the management of urinary incontinence. Being a freely water soluble drug, with half-life approximately three hours, making it a good candidate for controlled-release formulations. Enteric Extended-release hydrophilic matrix tablets were prepared by direct compression using a number of hydrophilic polymers. All the compressed formulations were evaluated. Kinetic analysis of the release was performed. Pharmacokinetic parameters of Oxybutynin HCl from the optimized zero order tablet formula (F#24L) was compared to the immediate release innovator "Ditropan®" in human volunteers using a randomized crossover design on a release profile over 48 hours. The optimized tablet formulation was F#24L (containing 50% CMC Na 2000 cps) with sub-coat and enteric coat.


PREPARATION AND CHARACTERIZATION OF SELF EMULSIFYING DRUG DELIVERY SYSTEM OF TELMISARTAN

Manoj Goyal*1, Vikas Rathore 2, Ashutosh Dubey

Improvement of bio-availability of poorly water soluble drugs presents one of the further most challenges in drug formulations. One of the most admired and commercially viable formulation approaches for this challenge is selfemulsifying drug delivery system (SEDDS). There are many techniques to convert liquid SEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop SEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to SEDDS by adsorbing it on Aerosil 200. Prepared SEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and exvivo intestinal permeability study. Results showed that prepared SEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 µm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of SEDDS with less aggregation. Drug releases from SEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from SEDDS than that of suspension of plain TEL. Study concluded that SEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.


STRUCTURE BASED DRUG DESIGN: A REVIEW

Pratyosh Shamra and Jagdish K. Sahu*

The field of structure-based drug design is a rapidly growing area in which much advancement has occurred in recent years. The outburst of genomic, proteomic, and structural information has provided hundreds of new targets and opportunities for future drug lead finding. This review condenses the process of structure-based drug design and comprises, primarily, the choice of a target, the evaluation of a structure of that target, the essential queries to consider in choosing a method for drug lead discovery, and evaluation of the drug leads.