An active film-coating approach to enhance chemical stability of a potent drug molecule

  title={An active film-coating approach to enhance chemical stability of a potent drug molecule},
  author={Divyakant S. Desai and Venkatramana M. Rao and Hang Guo and Danping Li and Daniel Stein and Frank Y. Hu and Chris Kiesnowski},
  journal={Pharmaceutical Development and Technology},
  pages={227 - 235}
Peliglitazar, a PPAR α/γ agonist, was found to undergo acid as well as base catalyzed degradation. The acid catalyzed degradation led to the formation of benzylic alcohol and glycine carbamate and the base catalyzed degradation led to formation of p-hydroxyanisole and an amine degradant. In capsule formulations, the capsules with the lowest drug-loading exhibited maximum instability even at 25°C/60% RH storage condition. Incorporation of pH-modifiers to maintain ‘micro-environmental pH’ acidic… 
Effect of coating excipients on chemical stability of active coated tablets
Higher stability of triacetin systems over PEG systems was attributed to lower solubility and mobility of peliglitazar in HPMC compared with the PVA-based coating, while for the same plasticizer/detackifier, higher stability of H PMC over PVA, based on the overall stability for the film-forming polymer-plasticizer/ Detackifier combination.
Reactive Impurities in Excipients
Reactive impurities in pharmaceutical excipients can affect drug product instability, leading to decreased product performance, loss in potency, and/or formation of potentially toxic degradants. The
An evaluation of process parameters to improve coating efficiency of an active tablet film-coating process.
Objective: Quantification of degradation products in drug substances and products is the most challenging tasks in pharmaceutical industries nowadays. Systematic study on the degradation products of
Pharmaceutical application and development of fixed-dose combination: dosage form review
This review provides discussions of the FDC application in variety of disease using various formulation technologies that consider characteristics of each active pharmaceutical ingredient (API) in FDC to maximize the benefits and overcome the challenges of developing FDC products.
Reactive Impurities in Excipients: Profiling, Identification and Mitigation of Drug–Excipient Incompatibility
In this review paper, excipient impurity classes are categorized into six major classes, including reducing sugars, aldehydes, peroxides, metals, nitrate/nitrite, and organic acids, and the potential reactions with drug candidates of these impurities are reviewed.
Formulation design, challenges, and development considerations for fixed dose combination (FDC) of oral solid dosage forms
An overview to pharmaceutical scientists about recent trends in the formulation development of the FDC products is given and decision trees to select most optimum formulation development strategy are provided.
Optimization of Critical Quality Attributes in Tablet Film Coating and Design Space Determination Using Pilot-Scale Experimental Data
The results indicate that all the process responses are affected by changing the inlet air flow rate, temperature, and suspension spray rate, which facilitates the quality by design implementation of continuous pharmaceutical manufacturing.
A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms
Abstract This paper proposes the development of a drug product Manufacturing Classification System (MCS) based on processing route. It summarizes conclusions from a dedicated APS conference and


Effect of different acids on solid-state stability of an ester prodrug of a IIb/IIIa glycoprotein receptor antagonist.
Adding acids to blends containing DMP 754 and anhydrous lactose improved the stability at 40 degrees C/75% relative humidity and decreased the rate of hydrolysis of the amidine group and this effect was more pronounced with stronger acids.
Chemical stability of an ester prodrug of a glycoprotein IIb/IIIa receptor antagonist in solid dosage forms.
Although the compression process resulted in enhanced degradation of the binary blend of DMP 754 and anhydrous lactose, tablets manufactured by the wet granulation process were more stable than capsules manufactured bythe same process.
Effect of Processing and Formulation Variables on the Stability of a Salt of a Weakly Basic Drug Candidate
This study shows that selection of the proper manufacturing process, in conjunction with the appropriate pH modifier, could be critical to dosage form stability, suggesting that a higher microenvironmental pH than that provided by sodium bicarbonate is needed to maximize stability.
Stable extended release oral dosage composition
PURPOSE: Provided is a film-coated extended release solid oral dosage composition containing a nasal decongestant, for example, pseudoephedrine in a controlled release core and a film outer coating
Selection of solid dosage form composition through drug-excipient compatibility testing.
A drug-excipient compatibility screening model was developed by which potential stability problems due to interactions of drug substances with excipients in solid dosage forms can be predicted and selection of dosage form composition by using this model would lead to reduction of "surprise" problems during long-term stability testing of drug products.
Moisture sorption and permeability characteristics of polymer films: implications for their use as barrier coatings for solid dosage forms containing hydrolyzable drug substances.
Moisture sorption and permeability characteristics of polymer films were studied and their effectiveness to protect a hydrolyzable drug assessed. Cast films were prepared from Eudragit L30 D-55,
Drug-Excipient Incompatibility Studies of the Dipeptide Angiotensin-Converting Enzyme Inhibitor, Moexipril Hydrochloride: Dry Powder vs Wet Granulation
It was found that most of the commonly used fillers, disintegrants, lubricants,ubricants, glidants, and coating agents were incompatible with 1 in dry powder mixtures; moisture and basic agents were determined to be the dominant destabilizing factors.
Stabilization of a new antiulcer drug (Lansoprazole) in the solid dosage forms
AbstractIn the previous study, we clarified that enteric granules were appropriate dosage forms of lansoprazole. The establishment of these formulations, however, was difficult because some of the
Modeling of pan coating processes: Prediction of tablet content uniformity and determination of critical process parameters.
An engineering model for predicting the active pharmaceutical ingredient (API) content uniformity (CU) for a drug product in which the active is coated onto a core using a perforated coating pan demonstrated that good correlation between the model predictions and the experimental results for the API CU was achieved.