Tomoji Ono,
Satoru Morishita,
Chikako Fujisaki,
Motoyasu Ohdera,
Michiaki Murakoshi,
Norio Iida,
Hisanori Kato,
Kazuo Miyashita,
Masaaki Iigo,
Toshihide Yoshida,
Keikichi Sugiyama and
Hoyoku Nishino
Abstract
We showed that enteric-coated bovine LF tablets can decrease visceral fat accumulation, hypothesising that the enteric coating is critical to the functional peptides reaching the visceral fat tissue and exerting their anti-adipogenic activity. The aim of the present study was to assess whether inges...
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PMID: 20854698
PDF is available here.
Abstract
Lactoferrin (LF), a multifunctional glycoprotein in mammalian milk, is reported to exert a modulatory effect on lipid metabolism. The aim of the present study was to elucidate whether enteric-coated LF (eLF) might improve visceral fat-type obesity, an underlying cause of the metabolic syndrome. Usin...
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PMID: 20691130
PDF is available here.
Harvey H White,
Claes C Held,
Ralph R Stewart,
David D Watson,
Robert R Harrington,
Andrzej A Budaj,
Ph Gabriel PG Steg,
Christopher P CP Cannon,
Susan S Krug-Gourley,
Janet J Wittes,
Trupti T Trivedi,
Elizabeth E Tarka and
Lars L Wallentin
Abstract
STABILITY will assess whether direct inhibition of Lp-PLA(2) with darapladib added to the standard of care confers clinical benefit to patients with CHD.
Copyright © 2010 Mosby, Inc. All rights reserved....
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PMID: 20934559
PDF is available here.
Abstract
There is scarce information about the effects of different doses and enteric-coated preparation of aspirin on platelet function, especially in Asian people, evaluated by the measurement of urinary 11-dehydrothromboxane B2 (dTXB2). The objective of the present study was to assess the effects of diffe...
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PMID: 20689403
PDF is available here.
Abstract
Mycophenolate mofetil, an immunosuppressant approved for the prevention of transplant rejection, has been used in patients with lupus nephritis. Lertdumrongluk et al. suggest that mycophenolic acid exposure may predict therapeutic responses in severe lupus nephritis, and their initial results confir...
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PMID: 20671734
PDF is available here.
Abstract
Three types of annular bed flow patterns were identified. Plug flow gave the best coat uniformity followed by global and localized fluidization. Plug flow may be advantageous for high spray-rate conditions, large-scale coating and prevention of particle segregation. Plug flow could be differentiated...
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PMID: 20204472
PDF is available here.
Abstract
We utilized water-miscible organic solvents such as acetone and ethanol, which are considered safe class 3 solvents according to the ICH guideline. We deemed such an approach suitable for safe scale up and for enteric coating application to other compounds of a similar lipophilicity.
The resulting m...
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PMID: 19929567
PDF is available here.
Abstract
For TDM in SLE patients with GFR > 60 ml/min/1.73 m(2), C(12h) after MMF ingestion could predict MPA AUC(0-12h), while an LSS around T(max) should be used for patients on EC-MPS....
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PMID: 20210680
PDF is available here.
Abstract
Short-term administration of low-dose enteric-coated aspirin was associated with visible small bowel damage in the majority of users. We could not prove that aspirin-induced small bowel mucosal injury was prevented by GGA....
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PMID: 19968611
PDF is available here.
Abstract
In this small study in healthy Pakistani male subjects, there were significant differences in the bioavailability and pharmacokinetic parameters of the enteric- and film-coated tablet formulations of flurbiprofen. Thus, the 2 formulations could not be considered bioequivalent. Both formulations were...
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PMID: 20399997
PDF is available here.
Abstract
Low-density lipoprotein cholesterol and plasma triacylglycerol levels were significantly lower in the group fed live bacteria, by 42% and 32%, respectively (P<0.05), and fecal bile acid excretion was accelerated (+45%). Expression of the low-density lipoprotein receptor and 3-hydroxy-3-methylglutary...
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PMID: 19695834
PDF is available here.
Abstract
Adequate early mycophenolic acid (MPA) exposure is an important determinant for effective rejection prophylaxis. This pharmacokinetic study investigated whether an intensified dosing regimen of enteric-coated mycophenolate sodium (EC-MPS) could achieve higher mycophenolic acid (MPA) exposure early af...
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PMID: 20150450
PDF is available here.
Abstract
Besides coating on placebo cores it was possible to determine the amount of active ingredient in the film when coated onto cores containing the same active ingredient. In addition, the method is even applicable when varying the process parameters and measurement conditions within a restricted range....
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PMID: 19778159
PDF is available here.
Abstract
Importantly, none of the investigated conditions had a noteworthy impact on the release of freely water-soluble diltiazem HCl or slightly water-soluble theophylline from pellets coated with ethylcellulose containing small amounts of PVA-PEG graft copolymer. In particular, the presence of significant...
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PMID: 19747068
PDF is available here.
Abstract
The presence of either film coating on the guaifenesin-containing tablets was found to prolong the onset time of drug crystallization. The coating polymer was the most important factor determining the delay in the onset of crystallization, with the more hydrophilic polymer, hypromellose, having a hi...
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PMID: 19877992
PDF is available here.
Abstract
There was a fourfold increase (18 versus 75 minutes) in lag time when the same amount of ethylcellulose (4 g) was dissolved in 100 mL of ethanol instead of 160 mL. When the same amount of drug and ethylcellulose solution was applied on the acrylic coated beads as multiple layers coating, the lag tim...
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PMID: 20070184
PDF is available here.
Abstract
The results from both the immediate release and delayed release case studies support the assertion that continuous coating processes are capable of applying aqueous film coatings with significant improvements in coating uniformity and reduction in product loss....
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PMID: 19954403
PDF is available here.
Abstract
Results showed that Acryl-EZE enteric coating systems provide excellent performance in both media (0.1N HCl and acetate buffer pH 4.5) for monolithic and multiparticulate dosage forms....
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PMID: 20070183
PDF is available here.
Abstract
Enteric-coated tablets containing mycophenolate sodium have been developed to reduce gastric toxicity. The objective of this study was to compare 2 enteric-coated formulations containing 360 mg of mycophenolate sodium: the innovator product, Myfortic, and an agent that recently became available in M...
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PMID: 20172348
PDF is available here.
Abstract
The dissolution profiles of formulations demonstrated similar disposition in biorelevant medium in both USP apparatus 2 and 3. The dissolution profiles were described by f2 model in apparatus 2 and Weibull's function in apparatus 3. The vitro-in vivo relationship analysis showed that the formulation...
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PMID: 20184226
PDF is available here.
Abstract
These studies were conducted in order to assess the bioequivalence of two film-coated formulations containing 250 mg and 1000 mg of valacyclovir (INN: valaciclovir; CAS 124832-26-4), which is the L-valyl ester and a pro-drug of the antiviral drug acyclovir (INN: aciclovir). In the study with valacyc...
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PMID: 20533765
PDF is available here.
Abstract
A stability indicating reversed-phase liquid chromatography method is developed and validated for the determination of norfloxacin in a new formulation of extended-release tablets. The LC method is carried out on a Luna C(18) column (150 x 4.6 mm) maintained at 40 degrees C. The mobile phase is comp...
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PMID: 19835680
PDF is available here.
Abstract
In this study, EC-MPS had a similar incidence of GI complications and dose manipulations compared with MMF. Despite similar GI complication rates and dose manipulations, treatment with EC-MPS seemed to result in a lower incidence of BPAR. Based on these observations, more studies need to be conducte...
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PMID: 19696634
PDF is available here.
Abstract
Despite the potential tolerability advantage of enteric-coated mycophenolate sodium (EC-MPS), no prospective, randomized trial has evaluated whether conversion from mycophenolate mofetil (MMF) to EC-MPS permits mycophenolic acid dose to be increased or gastrointestinal side-effects to be ameliorated...
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PMID: 19386081
PDF is available here.
Abstract
OBJECTIVE: To prepare enteric coated pellets containing panax notoginseng saponins. METHOD: Panax notoginseng saponins loaded pellets were prepared by Extrusion-Spheronization method, and coated by Eudragit L30D-55 using Glatt fluid bed with the bottom spray process, central composite design was use...
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PMID: 19771862
PDF is available here.
Abstract
OBJECTIVE: To prepare the gastric retenting and chronopharmacologic drug delivery tablets containing sinomenine hydrochloride as a model drug, evaluate the effects of the coating layers formulation and technics on drug release behavior, and to elucidate the mechanism of drug release based on obtaine...
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PMID: 19526781
PDF is available here.
Abstract
From serum data, the obtained values for test and reference products were 593.05 +/- 84.85 and 607.92 +/- 67.07 ng/ ml for Cmax; 1756.71 +/- 287.29 and 1786.90 +/- 280.17 ng-h/ml for AUC0-24; 1889.26 +/- 286.46 and 1929.18 +/- 284.33 ng-h/ml for AUC0- yen, respectively. No statistically significant...
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PMID: 19281731
PDF is available here.
Abstract
In this study EC-MPS at a dose of 720 mg twice daily for 6 months has proven to be an effective and well-tolerated treatment for patients with severe, recalcitrant AD....
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PMID: 19120337
PDF is available here.
Abstract
Evaluation of: Machnicki G, Ricci JF, Brennan DC, Schnitzler MA. Economic impact and long-term graft outcomes of mycophenolate mofetil dosage modifications following gastrointestinal complications in renal transplant recipients. Pharmacoeconomics 26(11), 951-967 (2008). This commentary discusses fin...
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PMID: 19371175
PDF is available here.
Abstract
We undertook a 12-month, multicenter, open-label pilot study in which 16 de novo renal transplant patients aged 5-16 years received EC-MPS with cyclosporine A microemulsion (CsA-ME), steroids, and anti-interleukin-2 receptor antibody induction. The mean dose of EC-MPS was 916 +/- 93 mg/m(2) per day...
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PMID: 18985393
PDF is available here.
Abstract
The purpose of the study is to perform the in vitro and in vivo evaluation of multi-layer film coatings for omeprazole. The system consists of drug-layered or drug-containing core pellets coated with salt (sodium chloride and disodium hydrogen phosphate), hydroxypropyl methyl cellulose (HPMC), and e...
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PMID: 19182399
PDF is available here.
Hiroaki Nema,
Mototsugu Kato,
Takehiko Katsurada,
Youichi Nozaki,
Akihiko Yotsukura,
Izumi Yoshida,
Katsuhiko Sato,
Yuko Kawai,
Yasushi Takagi,
Takanori Okusa,
Shunichi Takiguchi,
Masayuki Sakurai and
Masahiro Asaka
Abstract
As endoscopy frequently reveals gastroduodenal disorder among low-dose aspirin users, both administration of BA and of enteric-coated aspirin warrant concern for gastroduodenal ulcer....
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PMID: 18779739
PDF is available here.
Abstract
A novel double-coating enteric system was developed to accelerate drug release in conditions resembling the upper small intestine. The system comprises an inner coat (partially neutralised EUDRAGIT L 30 D-55 and organic acid) and an outer coat (standard EUDRAGIT L 30 D-55). Prednisolone tablets were...
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PMID: 18930772
PDF is available here.
Abstract
The purpose of this study was to formulate budesonide (BUD) compression-coated tablets for colonic specific delivery. Pectin and guar gum were used as enzyme-dependent polymers. For comparison purposes, both pH- and time-dependent polymers were also tried. In vitro release studies were carried out a...
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PMID: 19199041
PDF is available here.
Abstract
The aim of present study was to develop a time- and pH-dependent system for delivering mesalamine to the colon. The system consists of the core tablet of mesalamine which is compression coated with hydroxypropyl methylcellulose (HPMC K4M) (time-dependent factor). This is then coated with pH-dependen...
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PMID: 18802844
PDF is available here.
Abstract
The aim of the present study was to investigate the influence of Eudragit E PO on the drug release mechanism of Eudragit L 100-55 film coatings applied to theophylline tablets by a dry powder coating technique. The process was entirely liquid-free. Calculation of the Flory-Huggins interaction parame...
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PMID: 19883252
PDF is available here.
Abstract
The purpose of this research work was to develop venlafaxine hydrochloride-coated and layered matrix tablets using hypromellose adopting wet granulation technique. The granules and the tablets were characterized. The monolithic tablets were coated with different ratios of ethyl cellulose and hyprome...
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PMID: 19883254
PDF is available here.
Abstract
By 12 weeks, ERr 731 caused a highly significant reduction of the MRS total score from 27.0 +/- 4.7 points to 12.4 +/- 5.3 points when compared to the placebo-induced decrease from 27.0 +/- 5.3 points to 24.0 +/- 6.2 points (P < .0001). A significant reduction in each individual MRS item score, in h...
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PMID: 19161045
PDF is available here.
Abstract
The dry coating process was evaluated in terms of storage stability investigating drug release and agglomeration tendency of the different coated oral dosage forms; hydroxypropyl methylcellulose acetate succinate (HPMCAS) was used with triethylcitrate (TEC) as plasticizer and acetylated monoglycerid...
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PMID: 19883250
PDF is available here.
Abstract
The bioavailability and bioequivalence of two different film coated tablets containing ethinylestradiol (CAS 57-63-6) and chlormadinone acetate (CAS 302-22-7) (Bellissima as test and the respective preparation from the originator as reference) were investigated in 20 healthy female volunteers after...
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PMID: 20108652
PDF is available here.
Abstract
Omeprazole (CAS 73590-58-6) effectively suppresses the gastric acid secretion in the parietal cells of the stomach and is a widely prescribed proton pump inhibitor in Bangladesh. The increasing number of omeprazole containing products available in the market raises questions of therapeutic equivalen...
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PMID: 19517893
PDF is available here.
Abstract
The arithmetic means of AUC(0-tlast) and Cmax were 3,656.01 pg x h/ml and 1970.22 pg/ml for the test formulation and 3771.51 pg x h/ml and 1756.52 pg/ml, respectively, for the reference formulation. The mean tmax was 1.16 h for the test and 1.13 h for the reference formulation. The point estimators...
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PMID: 19634511
PDF is available here.
Abstract
Pharmacokinetic parameters of PAS-Akri coated tablets (Akrikhin, Russia) were investigated. The tablets contain paraaminosalicylic acid (PAS) as sodium dihydrate in an amount of 1000 mg. The single oral dose of the drug for healthy volunteers in the trial was 6, 9 or 12 tablets. In 7 days the dosage...
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PMID: 19499713
PDF is available here.
Abstract
Trileptal oral suspension formulation and film-coated tablets are bioequivalent in healthy Chinese males....
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PMID: 18826868
PDF is available here.
Abstract
The major challenges in targeting drug to various parts of the gastrointestinal tract include control of drug release with respect to its environment and transit time. These two variables should be taken into consideration in designing a rational colonic drug delivery system. To this end, a swelling...
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PMID: 18812022
PDF is available here.
Abstract
We describe the microencapsulation of the model enzyme bile salt hydrolase (Bsh) using whey protein-gum arabic microencapsulates for food-grade and targeted enzyme delivery in the proximal region of the small intestine. Furthermore, the efficacy of enteric coating microencapsulates for site-specific...
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PMID: 18729459
PDF is available here.
Abstract
It has been shown in adult kidney transplant recipients that a conversion from MMF to EC-MPS significantly reduced the GI related symptom burden. No such study exists on children with GI problems while receiving MMF therapy. Ten paediatric kidney transplant recipients (mean age 14.5 yr, s.d. 4.5) re...
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PMID: 18798359
PDF is available here.
P Darji,
R Vijayaraghavan,
C M Thiagarajan,
R K Sharma,
B Subbarao,
R Pishardy,
K V Dakshinamurthy,
R Vijaykumar,
G Abraham,
S Bhaskar,
L Agarwal,
B Shah,
A Abraham,
M John,
K Sampathkumar,
T Das,
L Umesh,
S Sundar,
H Ballal,
S Jasuja,
S Saxena and
T K Saha
Abstract
Of 154 patients screened, 118 fulfilled the inclusion or exclusion criteria. Eighty-five men and 33 women with a mean age of 41.6 years participated in this study. Median time since transplantation was 12 months. Mean (SD) dose of MMF reported at baseline was 1209.4 (422.89) mg/d. More than 50% of p...
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PMID: 18790208
PDF is available here.
Abstract
The relationship of gastric motor activity and gastric emptying of 0.7 mm caffeine pellets with their absorption was investigated in the fed state in healthy human subjects by simultaneous monitoring of antral motility and plasma concentrations. A kinetic model for gastric emptying-dependent absorpt...
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PMID: 18434110
PDF is available here.
Abstract
Pellet cores containing modified starch (high-amylose, crystalline and resistant starch) as the main excipient were enteric-coated with an Eudragit L30 D-55 based dispersion. The polymer weight gain was from 15% to 30% (w/w). Pellet cores were prepared using piroxicam (2.5% w/w, poor water solubilit...
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PMID: 18579353
PDF is available here.
Abstract
Renal function remained unchanged after conversion. Serum hemoglobin (Hb) increased in 18/21 (86%) of patients after conversion. Endogenous erythropoietin level decreased from a median of 28.3 (11.5-374) to 16.6 (3.1-78.8) mIU/mL, (P<0.001); and the erythropoietin:Hb ratio dropped from 2.7 (0.7-34.3...
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PMID: 18724224
PDF is available here.
Abstract
Recently, there has been concern by regulatory authorities of the risk of alcohol-induced dose dumping of oral modified release (MR) formulations. The aim of this work was to use in vitro dissolution methodology to investigate the vulnerability of MR products to alcohol under different physiological...
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PMID: 18547758
PDF is available here.
Abstract
Being a sustained release dosage form, pellets allow ofloxacin to exhibit improved release and absorption profiles. In this paper, the centrifugal granulation method was employed to prepare ofloxacin pellets. Then the pellets were subjected to a coating process with methacrylic acid copolymers to pr...
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PMID: 18538518
PDF is available here.
Abstract
Our studies showed that dissolution rate of EZ were distinctively increased in the solid dispersion system compared to that in pure EZ or physical mixtures. The increase of dissolution rate was obviously related to the ratio of EZ to PEG4000. The solid dispersion system (EZ/PEG4000=1/8, w/w) gave th...
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PMID: 18495389
PDF is available here.
Abstract
In vivo performance of "pH-responsive" dosage forms is complex and influenced by a multitude of factors other than just in situ pH....
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PMID: 18465212
PDF is available here.
Abstract
Layering of pellets with recombinant Lactococcus lactis Thy 12 was optimised for the production of a dosage form with a high load of viable recombinant L. lactis. Shear stress induced during the atomisation and the type of carrier used for the layering process did not influence the viability. A 5% l...
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PMID: 18423993
PDF is available here.