Abstract：
:Aqueous wet massing of stable anhydrous theophylline (A) with polyvinylpyrrolidone (PVP) resulted in its complete transformation to theophylline monohydrate (M). Drying at 45 degrees C, resulted in the formation of metastable anhydrous theophylline (A*) which then transformed to A. PVP, a known crystallization inhibitor, was effective in inhibiting the A* --> A transition. The higher molecular weight polymer, PVP K90, was more effective in inhibiting the A* --> A transition as compared to PVP K17. The disappearance of M, and the formation of A* and A was simultaneously monitored by XRD. An increase in the drying temperature from 45 to 55 degrees C accelerated the A* --> A transition. In granules prepared by the high-shear process, approximately 50% of theophylline existed as A and the rest as A*. In contrast, the fluid-bed granulation process yielded granules containing only A. Thus, the physical form of theophylline in tablets was influenced by the molecular weight of the binding agent, the granulation method, and the drying temperature. Using A as the starting material, tablets were manufactured by high-shear aqueous wet granulation process and the A* content was quantified. These tablets were stored under various relative humidity (RH) conditions at 25 degrees C for 2 weeks. Storage at RH >or= 33% caused complete A* --> A conversion accompanied by a pronounced decrease in the initial dissolution rate indicating that phase transitions during processing and storage can have a significant influence on product performance.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Tantry JS,Tank J,Suryanarayanan Rdoi
10.1002/jps.20746subject
Has Abstractpub_date
2007-05-01 00:00:00pages
1434-44issue
5eissn
0022-3549issn
1520-6017pii
S0022-3549(16)32242-0journal_volume
96pub_type
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journal_title：Journal of pharmaceutical sciences
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更新日期：1987-02-01 00:00:00
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更新日期：2011-11-01 00:00:00
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doi：10.1002/jps.2600700818
更新日期：1981-08-01 00:00:00
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更新日期：1986-04-01 00:00:00
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doi：10.1002/jps.2600801207
更新日期：1991-12-01 00:00:00
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更新日期：2002-03-01 00:00:00
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更新日期：2018-05-01 00:00:00
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abstract：:The in vitro antifungal activity of a novel series of cis- and trans-5-([aryl or aryloxy (or thio)]methyl)-3-(1H-imidazol-1-ylmethyl)-3- (2-thienyl)-2-methylisoxazolidines (13-24) was evaluated and compared with ketoconazole. The title series of compounds was prepared via a 1,3-dipolar cycloaddition reaction of 1-(2-t...
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更新日期：1988-12-01 00:00:00
abstract：:A method for the measurement, in human plasma, of all tertiary and secondary tricyclic antidepressants prescribed in the United States is described. The method uses electron beam ionization GLC-mass spectrometry, employing a computer-controlled multiple-ion detector. This method, mass fragmentography, is used with int...
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更新日期：1976-02-01 00:00:00
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abstract：:Ambrisentan is a nonsulfonamide, ET(A)-selective endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH), and tadalafil is a phosphodiesterase type 5 (PDE-5) inhibitor under investigation for treatment of PAH. Due to the potential combination use, the pharmacokinetic (P...
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pub_type： 杂志文章,随机对照试验
doi：10.1002/jps.21789
更新日期：2009-12-01 00:00:00
abstract：:The transdermal delivery of 2 fluorescent probes with similar molecular weight but different lipophilicity, into and through the skin from 2 commercially available transdermal bases, pluronic lecithin organogel, and Lipoderm® has been evaluated. First, in vitro penetration of fluorescein sodium and fluorescein (free a...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2017.09.008
更新日期：2018-02-01 00:00:00
abstract：:The solubility of phenacetin was determined at five temperatures in solvent mixtures of aprotic-amphiprotic mixtures of dioxane and water. Enthalpy-entropy compensation analysis is used to study the effect of changing polarity of the medium on the solute. The apparent heats of solution and free energies of solution ar...
journal_title：Journal of pharmaceutical sciences
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更新日期：1996-10-01 00:00:00
