Search results for "Mace"
showing 10 items of 4713 documents
Toward Biopredictive Dissolution for Enteric Coated Dosage Forms
2016
The aim of this work was to develop a phosphate buffer based dissolution method for enteric-coated formulations with improved biopredictivity for fasted conditions. Two commercially available enteric-coated aspirin products were used as model formulations (Aspirin Protect 300 mg, and Walgreens Aspirin 325 mg). The disintegration performance of these products in a physiological 8 mM pH 6.5 bicarbonate buffer (representing the conditions in the proximal small intestine) was used as a standard to optimize the employed phosphate buffer molarity. To account for the fact that a pH and buffer molarity gradient exists along the small intestine, the introduction of such a gradient was proposed for p…
In vivo models and decision trees for formulation development in early drug development: A review of current practices and recommendations for biopha…
2018
The ability to predict new chemical entity performance using in vivo animal models has been under investigation for more than two decades. Pharmaceutical companies use their own strategies to make decisions on the most appropriate formulation starting early in development. In this paper the biopharmaceutical decision trees available in four EFPIA partners (Bayer, Boehringer Ingelheim, Bristol Meyers Squibb and Janssen) were discussed by 7 companies of which 4 had no decision tree currently defined. The strengths, weaknesses and opportunities for improvement are discussed for each decision tree. Both pharmacokineticists and preformulation scientists at the drug discovery & development interf…
Hierarchical Mass Transfer Analysis of Drug Particle Dissolution, Highlighting the Hydrodynamics, pH, Particle Size, and Buffer Effects for the Disso…
2020
Dissolution is a crucial process for the oral delivery of drug products. Before being absorbed through epithelial cell membranes to reach the systemic circulation, drugs must first dissolve in the human gastrointestinal (GI) tract. In vivo and in vitro dissolutions are complex because of their dependency upon the drug physicochemical properties, drug product, and GI physiological properties. However, an understanding of this process is critical for the development of robust drug products. To enhance our understanding of in vivo and in vitro dissolutions, a hierarchical mass transfer (HMT) model was developed that considers the drug properties, GI fluid properties, and fluid hydrodynamics. T…
Impact of uncharged and charged stabilizers on in vitro drug performances of clarithromycin nanocrystals
2018
The purpose of this study was to evaluate the effect of charge on the in vitro drug performances of clarithromycin nanocrystals. To prepare different charges of nanocrystals, media milling was employed with the use of different stabilizing systems. The uncharged nanocrystals were prepared from poloxamer 407. The negatively and positively charged nanocrystals were stabilized using a combination of poloxamer 407 with sodium lauryl sulfate (SLS) and cetyltrimethylammonium bromide (CTAB), respectively. After production, the particle size of the negatively and positively charged nanocrystals was smaller than that of the uncharged one. The similar particle size of variously charged clarithromycin…
Formulation strategy towards minimizing viscosity mediated negative food effect on disintegration and dissolution of immediate release tablets.
2017
Food induced viscosity can delay disintegration and subsequent release of API from solid dosage form which may lead to severe reduction in the bioavailability of BCS type III compounds. Formulations of such tablets need to be optimized in view of this postprandial viscosity factor. In this study, three super disintegrants, croscarmellose sodium (CCS), cross-linked polyvinylpolypyrrolidone (CPD), and sodium starch glycolate (SSG) were assessed for their efficiency under simulated fed state. Tablets containing these disintegrants were compressed at 10 and 30 KN, while taking lactose as a soluble filler. In addition to other compendial tests, disintegration force of these formulations was meas…
Retinol encapsulated into amorphous Ca2+ polyphosphate nanospheres acts synergistically in MC3T3-E1 cells
2015
Both the quality and quantity of collagen, the major structural component of the skin, decrease in aging skin. We succeeded to encapsulate retinol into amorphous inorganic polyphosphate (polyP) nanoparticles together with calcium ions ("aCa-polyP-NP"), under formation of amorphous Ca-polyP/retinol nanospheres ("retinol/aCa-polyP-NS"). The globular nanospheres are not cytotoxic, show an almost uniform size of ≈ 45 nm and have a retinol content of around 25%. Both components of those nanospheres, retinol and the aCa-polyP-NP, if administered together, caused a strong increase in proliferation of mouse calvaria MC3T3 cells. The expressions of collagen types I, II and III genes, but not the exp…
Activity–Bioavailability balance in Oral Drug Development for a Selected Group of 6‐Fluoroquinolones
2002
Abstract A nomogram is proposed to select the best candidate in drug development studies with quinolones and is intended to substitute other possible models. The nomogram is referred to as an activity–bioavailability balance (ABB) because it includes the following two criteria: ABB= 1 / gm MIC ( drug candidate ) 1 /gm MIC ( ciprofloxacin ) · F calc \( drug candidate \) F calc ( ciproflaxacin ) . The in vitro activity of a group of 4′ N ‐alkyl‐ciprofloxacin derivatives was determined together with that of ciprofloxacin, initially against some reference strains and subsequently against 159 clinical isolates of eight selected species. The inverse of the geometric mean of the lowest concentrati…
Clean method for the simultaneous determination of propyphenazone and caffeine in pharmaceuticals by flow injection Fourier transform infrared spectr…
1997
A procedure is proposed for the simultaneous FTIR determination of propyphenazone (PFZ) and caffeine (CAF) in pharmaceuticals. The method involves the dissolution of the active principles in CHCl 3 , followed by filtration of sample solutions to remove the excipients. PFZ is then determined by absorbance measurements at 1595 cm - 1 , using a baseline established between 2000 and 890 cm - 1 , and CAF by using the first-derivative values at 1712 cm - 1 , using solutions of PFZ and CAF for external calibration. The method was applied in both the stopped-flow and flow-injection modes, providing precise and accurate results for the analysis of real samples. The incorporation of a distillation un…
Mechanistic and kinetic insight into spontaneous cocrystallisation of isoniazid and benzoic acid
2015
Solid-state cocrystallisation is of contemporary interest, because it offers an easy and efficient way to produce cocrystals, which are recognized as prospective pharmaceutical materials. Research explaining solid-state cocrystallisation mechanisms is important, but still too scarce to give a broad understanding of factors governing and limiting these reactions. Here we report an investigation of the mechanism and kinetics of isoniazid cocrystallisation with benzoic acid. This reaction is spontaneous; however its rate is greatly influenced by environmental conditions (humidity and temperature) and pre-treatment (milling) of the sample. The acceleration of cocrystallisation in the presence o…