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Content Uniformity (content + uniformity)

Distribution by Scientific Domains

Medical Sciences	40%

Selected Abstracts

Is there variability in drug release and physical characteristics of amiodarone chloride from different commercially available tablets?

INTERNATIONAL JOURNAL OF PHARMACY PRACTICE, Issue 4 2010
Possible therapeutic implications
Abstract Objectives, Amiodarone is a low-solubility, high-permeability drug with a narrow therapeutic index and reported bioavailability problems associated with switching formulations. The aim of this study was to identify whether there is variability in drug release and physical characteristics of different commercially available amiodarone hydrochloride formulations in Australia. Methods, Four available formulations (innovator Cordarone (COR) and generic products G1, G2 and G3) were tested for drug dissolution, content uniformity, hardness, weight variation, friability and disintegration in accordance with the US Pharmacopeia specifications. Key findings, The tested formulations exhibited variable dissolution behaviours: G1 and G3 exhibited the fastest dissolution, G2 dissolution was the slowest and Cordarone showed a medium dissolution. After 3 months' exposure to high temperature (40 ± 2°C) and relative humidity (75 ± 5%), the products exhibited a higher degree of disparity, with drug-release profiles of the generics being markedly different from that of Cordarone. This suggests possible implications on bioequivalence for patients who live in warm/tropical regional areas. Most products met the US Pharmacopeia specifications for drug-content uniformity and other test physical characteristics. Conclusions, The results suggested that variability in drug release profiles in vitro of amiodarone formulations might be a potential indicator of compromised bioavailability, causing possible interference with the therapeutic response of the drug. [source]

Quality by design, part I: Application of NIR spectroscopy to monitor tablet manufacturing process

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 9 2008
Simin Hassannejad Tabasi
Abstract To monitor tableting production using near infrared (NIR) spectroscopy, chemometric models were developed to analyze peak compression force, crushing strength and content uniformity. To measure tablet content uniformity, orbifloxacin tablets with drug content ranging from 60 to 90 mg were made and analyzed using ultraviolet (UV) and NIR spectroscopy. To assess the compression force and crushing strength, several batches of tablets were made on a Stokes B2 rotary tablet press and compression force was varied from 360 to 3500 lb. Principal component analysis (PCA) was used to identify tablets with regular and capped tablets breakage patterns. Comparison of statistical parameters showed that partial least squares (PLS) models gave better fit than the multiple linear regression (MLR) models. The best fit PLS models had a standard error of calibration (SEC) and a standard error of prediction (SEP) for content uniformity of 1.13 and 1.36 mg; for compression force of 69.86 and 59.48 lb and for crushing strength 0.55 kP and 0.57 kP, respectively. NIR spectroscopy in combination with multivariate modeling is a rapid and nondestructive technique that could reliably predict content uniformity, compression force and crushing strength for orbifloxacin tablets. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:4040,4051, 2008 [source]

Adduction of amiloride hydrochloride in urea through a modified technique for the dissolution enhancement

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 3 2008
Seema Thakral
Abstract Amiloride hydrochloride is a potassium-sparing diuretic since it favors sodium excretion and potassium reabsorption. In the present study, urea, a well-known adductor for linear compounds was successfully employed for inclusion of amiloride hydrochloride,a substituted cyclic organic compound through a modified technique. Formation of urea inclusion compounds was confirmed by FTIR, DSC and XRD. The minimum amount of rapidly adductible endocyte (RAE) required for adduction of amiloride hydrochloride in urea was estimated by a modified Zimmerschied calorimetric method. Urea,AH,RAE inclusion compounds containing varying proportions of guests were prepared and their thermal behavior studied by DSC. The inclusion compounds were also found to exhibit high content uniformity and markedly improved dissolution profile as demonstrated by increased dissolution efficiency. Studies reveal the possibility of exploiting co-inclusion of the drug in urea host lattice for the dissolution enhancement. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:1191,1201, 2008 [source]

Epinephrine for the treatment of anaphylaxis: do all 40 mg sublingual epinephrine tablet formulations with similar in vitro characteristics have the same bioavailability?

BIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 9 2006
Mutasem M. Rawas-Qalaji
Abstract Epinephrine autoinjectors are underutilized in the first aid emergency treatment of anaphylaxis in the community; so non-invasive sublingual epinephrine administration is being proposed. In order to determine the effect of changing excipients on the bioavailability of sublingual epinephrine, four distinct fast-disintegrating epinephrine 40 mg tablet formulations, A, B, C and D, were manufactured using direct compression. All formulations were evaluated for tablet hardness (H), disintegration time (DT) and wetting time (WT). In a prospective 5-way crossover study, four sublingual formulations and epinephrine 0.3 mg i.m. as a control were tested sequentially in a validated rabbit model. Blood samples were collected before dosing and at intervals afterwards. Epinephrine plasma concentrations were measured using HPLC-EC. All tablet formulations met USP standards for weight variation and content uniformity, and resulted in similar mean H, DT and WT (n=6). The area under the curve (AUC), maximum concentration (Cmax) and time at which Cmax was achieved (Tmax) did not differ significantly after the sublingual administration of formulation A and epinephrine 0.3 mg i.m. The AUC after B, C and D were significantly lower (p<0.05) than after epinephrine 0.3 mg i.m. These results suggest that the selection of excipients used in these tablet formulations can affect the bioavailability of sublingually administered epinephrine. Copyright © 2006 John Wiley & Sons, Ltd. [source]