Sahilhusen I. Jethara

Optimizing Oral Controlled Release Drug Delivery Systems usingExperimental Designs

The number of literature reports on the use of design of experiments optimization in development of drug delivery technology has been piling up steadily. This review article provides an updated bird’s eye view survey account on the publications and optimization techniques of different novel controlled release delivery designs for use in oral applications. Such systematic techniques find their use in every type of conventional dosage form and novel drug delivery system. The drug delivery devices investigated for optimization using various designs include oral controlled release tablet. The present manuscript deal with various steps involved in design of experiments optimization methodology using diverse experimental designs. It also deals with a variety of showing literature findings as well as the potential application of such design of experiments procedures on optimization of assorted drug delivery systems. Such an explicit and updated review on drug delivery optimization has not been published anywhere else in the recent past.

Enhanced Solubility and Dissolution Rate of Aceclofenac by Using SprayDrying Techniques

The present study deals with improvement in aqueous solubility of aceclofenac using HPMC K-15M, PVP-K30 and Eudragit RS-100 in varying ratio by spray-drying at optimized condition. The samples of solid dispersion were subjected to fourier transform infra-red spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction morphology (PXRD), scanning electron microscopy (SEM), in vitro drug release and stability studies. A decrease in the melting enthalpy in DSC indicates conversion of crystalline to amorphous state. The results were supported by PXRD, FTIR and SEM data revealed a characteristic decrease in crystallinity. The dissolution studies demonstrated a marked increase in the dissolution rate in comparison with pure drug. The considerable improvement in the dissolution rate of aceclofenac from spray drying, decreased drug crystallinity, altered surface morphology and micronization. The optimized co-crystals exhibited excellent stability on six month storage at accelerated conditions of 40°C and 75% relative humidity. Thus, the solid dispersion obtained by spray drying is a potential tool for improving drug solubility in water.

Development and Evaluation of Bilayer Tablet of Metoclopramide HCl and Aceclofenac

Bilayer tablets are basically used to administer a dosage form with dual release effect or to formulate two incompatible drugs. The main objective of the present research work was to prepare bilayer tablet of Metoclopramide hydrochloride (MTH) and Aceclofenac (ASF) for separate layers to avoid the degradation of the drug, with the desired release pattern and thus to maximize the efficacy of both drugs in combination for the effective treatment of migraine. MTH and ACF were formulated as immediate and conventional release layer respectively. ASF was formulated as conventional release layer using PVP K-30 and MCC as binder and disintegrants respectively. MTH was formulated as immediate release layer by using various disintegrants like Sodium starch glycolate (SSG), Cross carmellose sodium (CCS) and Pre-gelatinized starch (PGS). Mixture design technique was used to find out the optimized quantity of the super disintegrants. Disintegration time (DT) and drug release at 15 min (Rel15min) were taken as dependent variables while quantity of super disintegrants was taken as independent variable. SSG and CCS in a concentration of 7.5% and 4.5% respectively gave a DT of 9 sec, and 98.67% release at 15 min (Rel15min). Stability studies of bilayer tablets as well as physical mixture were carried out and the samples were evaluated with DSC, FT-IR and % content of drug. Bi-layer tablet was suitable for preventing direct contact of these two drugs and thus to maximize the efficacy of combination of two drugs for migraine.

Recent Patents Survey on Self Emulsifying Drug Delivery System

Self-Emulsifying Drug Delivery System is a unique feasible approach to overcome low oral bioavailability problem which is associated with the hydrophobic drugs due to their unparalleled potential as a drug delivery with the broad range of application. The estimated 40% of active pharmaceuticals are poorly water soluble. Now recently, formulation containing oral SEDDS has received much interest as it solve problems related to oral bioavailability, intra and inter-subject variability and lack of dose proportionality of hydrophobic drugs. Now a days, it is the first way to investigate the development of any kind of innovative dosage forms. Many important in-vitro characteristics such as surfactant concentration, oil/surfactant ratio, emulsion polarity, droplet size and zeta potential play an important role in oral absorption of drug from SEEDS. It can be orally administered in the form of SGC or HGC and also enhances bioavailability of drugs to increase solubility and minimizes the gastric irritation. After administration the drug remains entrapped in the oily droplets (inside the droplet or in the surfactant`s film at the interface) of the emulsion that are formed in the GIT upon self-emulsification process. It is also a bit problematic to say that the drug is being released from SMEDDS, it would be more precise to say that it diffuses out of oily droplets into the GIT media resulting in the formation of an equilibrium between the drug dissolved in oily droplets and the outer dispersed media (e.g. GIT fluids). Many of the application and preparation methods of SEDDS are reported by research articles and patents in different countries. We present an exhaustive and updated account of numerous literature reports and more than 150 patents published on SEDDS in the recent period. This current patent review is useful in knowledge of SEDDS for its preparations and patents in different countries with emphasis on their formulation, characterization and systematic optimization strategies, thus paving the way for accelerated progress into the SEDDS application in pharmaceutical research as well as patents on SEDDS methods.

Recent Survey on Nanosuspension: A Patent Overview

The major goals of designing nanosuspension of nanosize materials are increasing due to their tremendous potential as a drug delivery system with the wide range of applications. Nanosuspension is a unique tool for improving the bioavailability of poorly soluble drugs. Nanosuspension drug delivery has wide range of application like oral, injectable, transdermal, inhalation, peroral, ocular, pulmonary and topical etc. by improviing the bioavailability, reducing the dose, gastric irritation, decreasing intra subject variability and increasing adhesivness with intestinal membrane. Recently, nanosuspension has been received much interest as a way to resolve solubility and stability problem because of their cost-effectiveness and technical simplicity compare to other liposome and colloidal drug carriers. Nanosuspensions are engaged to control particle size, surface properties and release of pharmacologically active agents in order to achieve the site-specific action of the drug at the therapeutically optimal rate, improve the bioavaibility of drug with poor solubility and dose regimen. Application and preparation method of nanosuspension has been reported by research articles and patented in different countries. Most of the marketed nanosuspensions are in preclinical and clinical based study for its application. More than 100 patents have been published on nanosuspensions by the recent days. This patent reviews covers different methods of pharmaceutical preparation and applications in drug delivery as well as the recent marketed published or granted patent surveys. This patent review is useful in enhance the knowledge of controlled drug delivery and applications.