Formulation and Process Development Articles

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Singapore Attracts Pharmaceutical Manufacturing Investment

Pharmaceutical and biopharmaceutical manufacturing and research and development represent an important part of Singapore's economic base. Several major projects were announced in 2007 as Singapore, along with Ireland and Puerto Rico, compete for investment in the life sciences.

Pharmaceutical manufacturing output

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Pharmaceutical Technology, Jan 2, 2008

The Importance of Leachables and Extractables Testing for a Successful Product Launch

The FDA Guidance for Industry, Container Closure Systems for Packaging Human Drugs and Biologics (1) addresses the review and evaluation of packaging requirements. According to this document, each New Drug Application (NDA) or Abbreviated New Drug Application (ANDA) should contain enough information to demonstrate that a proposed container closure system and its components are suitable for its intended use.

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Pharmaceutical Technology, Jan 2, 2008

How to Build a Better Outsourcing Relationship

So you've decided to hire a contract manufacturing organization (CMO) to produce your clinical-trial materials (CTM). Or you've just signed a deal to provide your services to a top-tier pharmaceutical company. But how do you ensure that the project goes smoothly? Which factors will guarantee that the job is completed successfully? CMOs, pharmaceutical companies, and consultants offered Pharmaceutical Technology some interesting answers.

All sides agree that accurate and timely communication is a big requirement for a successful outsourcing relationship. "Transparency is key in building good information flow," according to Scott Houlton, chief operating officer of Aptuit (Greenwich, CT), a contract drug-development services company. Partners must be readily available to answer questions and offer details about the work at hand. This way, CMOs are sure to understand the project's specifications, and pharmaceutical companies will know about problems that arise.

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Pharmaceutical Technology, Jan 2, 2008

Pharmaceutical and Biopharmaceutical Manufacturing Advances in Ireland

Like its counterparts in Puerto Rico and Singapore, Ireland is seeking to diversify its base in the life sciences. It has embarked on a plan of not only attracting investment in its traditional strength in bulk pharmaceutical and finished-product manufacturing, but also investment in earlier drug-development from basic research to process development to clinical trial management. In pursuing research, the Irish government has agreed support, including financial support for several significant collaborations between academia and life science companies. These companies include Genzyme (Cambridge, MA), Schering Plough (Kenilworth, NJ), GlaxoSmithKline (London), Beckman Coulter (Fullerton, CA), Janssen (Titusville, NJ), Pfizer (New York, NY), Eli Lilly (Indianapolis, IN), Merck Sharp & Dohme, the affiliate of Merck and Co. (Whitehouse Station, NJ), and Helsinn (Lugano, Switzerland).

Pharmaceutical strength

Journal: 
Pharmaceutical Technology, Jan 2, 2008

Enhancement of Iontophoretic Transport of Diphenhydramine Hydrochloride Thermosensitive Gel by Optimization of pH, Polymer Conce

The purpose of the present study was to explore the passive and electrically assisted transdermal transport of diphenhydramine hydrochloride (DPH) by iontophoresis. For better bioavailability, better patient compliance, and enhanced delivery of DPH, an iontophoretic drug delivery system of a thermosensitive DPH gel was formulated using Lutrol F-127. The study was conducted using silver–silver chloride electrodes across hairless pig skin. The effects of pH, polymer concentration, electrode design, and pulse rate on the DPH permeation were investigated. The relationship between temperature, viscosity, and conductance of DPH was correlated using conductometry. Iontophoretic transport of DPH was found to increase with a decrease in the pH of the medium and an increase in the surface area of the electrode. Viscosity measurements and flux calculations indicated the suitability of the Lutrol gel for transdermal iontophoretic delivery of DPH.

Journal: 
AAPS PharmSciTech ,Volume 8, Issue 4 ,2007

Formulation and Development of Floating Capsules of Celecoxib: In Vitro and In Vivo Evaluation

The objective of the present study was to develop a hydrodynamically balanced system for celecoxib as single-unit floating capsules. Various grades of low-density polymers were used for formulation of these capsules. The capsules were prepared by physical blending of celecoxib and the polymer in varying ratios. The formulation was optimized on the basis of in vitro buoyancy and in vitro release in citrate phosphate buffer pH 3.0 (with 1% sodium lauryl sulfate). Capsules prepared with polyethylene oxide 60K and Eudragit RL100 gave the best in vitro percentage release and were used as the optimized formulation. By fitting the data into zero-order, first-order, and Higuchi models, we concluded that the release followed zero-order kinetics, as the correlation coefficient (R value) was higher for zero-order release. For gamma scintigraphy studies, celecoxib was radiolabeled with technetium-99m by the stannous reduction method.

Journal: 
AAPS PharmSciTech ,Volume 8, Issue 4 ,2007

Studies on a Novel Doughnut-Shaped Minitablet for Intraocular Drug Delivery

The objective of this study was to evaluate the effect of 2 independent formulation variables on the drug release from a novel doughnut-shaped minitablet (DSMT) in order to optimize formulations for intraocular drug delivery. Formulations were based on a 32 full-factorial design. The 2 independent variables were the concentration of Resomer (% wt/wt) and the type of Resomer grade (RG502, RG503, and RG504), respectively. The evaluated response was the drug release rate constant computed from a referenced marketed product and in vitro drug release data obtained at pH 7.4 in simulated vitreous humor. DSMT devices were prepared containing either of 2 model drugs, ganciclovir or foscarnet, using a Manesty F3 tableting press fitted with a novel central-rod, punch, and die setup. Dissolution data revealed biphasic drug release behavior with 55% to 60% drug released over 120 days.

Journal: 
AAPS PharmSciTech ,Volume 8, Issue 4 ,2007

Influence of Selected Formulation Variables on the Preparation of Enzyme-entrapped Eudragit S100 Microspheres

The aim of this work is to study the influence of formulation parameters in the preparation of sustained release enzyme-loaded Eudragit S100 microspheres by emulsion solvent diffusion technique. A 32 full factorial experiment was designed to study the effects of the amount of solvent (dichloromethane) and stabilizers (Tween 20, 40, or 80) on the drug content and microsphere size. The results of analysis of variance test for both effects indicated that the test is significant. The effect of amount of stabilizer was found to be higher on both responses (SSY1 = 45.60; SSY2 = 737.93), whereas solvent concentration comparatively produced significant effect on the size of microspheres (SSY1 = 0.81; SSY2 = 358.83). Scanning electron microscopy of microspheres with maximum drug content (2.5 mL dichloromethane and 0.1 mL Tween 80) demonstrated smooth surface spherical particles with mean diameter of 56.83 ± 2.88 µm.

Journal: 
AAPS PharmSciTech ,Volume 8, Issue 4 ,2007

Estimation of the Percolation Thresholds in Lobenzarit Disodium Native Dextran Matrix Tablets

The objective of the present work is to estimate for the first time the percolation threshold of a new series of dextran (native dextran of high molecular weight [B110-1-2, Mw = 2 × 106]), in matrices of lobenzarit disodium (LBD) and to apply the obtained result to the design of hydrophilic matrices for the controlled delivery of this drug. The formulations studied were prepared with different amounts of excipient in the range of 20% to 70% wt/wt. Dissolution studies were performed using the paddle method (100 rpm) and one face water uptake measurements were performed using a modified Enslin apparatus. The Higuchi, zero-order, and Hixson-Crowell models as well as the nonlinear regression model were employed as empiric methods to study the release data. Values of diffusion exponent 0.563 < n < 0.786 (Korsmeyer equation) for dissolution profile and water uptake mechanism 0.715 < n < 1 (Davidson and Peppas equation) suggested anomalous or complex mechanisms.

Journal: 
AAPS PharmSciTech ,Volume 8, Issue 4 ,2007

Production of Cromolyn Sodium Microparticles for Aerosol Delivery by Supercritical Assisted Atomization

The purpose of this study was to produce cromolyn sodium (CS) micrometric particles with controlled particle size (PS) and PS distribution (PSD) suitable for aerosol delivery, using a supercritical fluids–based process. CS was micronized using the supercritical assisted atomization (SAA) technique at different solute concentrations in water and different precipitation temperatures. Two techniques were used to measure PS and PSD of produced particles: scanning electron microscopy image analysis and laser scattering analysis. The 2 techniques were compared to provide a complete description of the powder obtained. High-performance liquid chromatography analysis was used to verify the absence of degradation of CS after micronization; differential scanning calorimetry, thermogravimetric analysis (TGA), and X-ray analysis were performed to study the effect of operative conditions on the crystalline structure and on the water content of SAA micronized particles.

Journal: 
AAPS PharmSciTech ,Volume 8, Issue 4 ,2007

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