Comparison of the in vitro dissolution properties and in vivo steady-state pharmacokinetics of two sustained-release theophylline preparations

1988 ◽  
Vol 10 (1) ◽  
pp. 17-21 ◽  
Author(s):  
J. H. G. Jonkman ◽  
W. J. V. Van Der Boon ◽  
G. Grasmeijer
Keyword(s):  
Steady State ◽  
Sustained Release ◽  
In Vitro Dissolution ◽  
Dissolution Properties ◽  
Sustained Release Theophylline

In-vitro dissolution and in-vivo absorption of marketed sustained release theophylline preparations

1990 ◽  
Vol 65 (3) ◽  
pp. R5-R8 ◽  
Author(s):  
A.A. Al-Angary ◽  
S.H. Khidr ◽  
G.M. Mahrous ◽  
M.W. Gouda
Keyword(s):  
Sustained Release ◽  
In Vitro Dissolution ◽  
In Vivo Absorption ◽  
Sustained Release Theophylline

Formulation Design of an HPMC-Based Sustained Release Tablet for Pyridostigmine Bromide as a Highly Hygroscopic Model Drug and its In Vivo/In Vitro Dissolution Properties

2007 ◽  
Vol 33 (11) ◽  
pp. 1183-1191 ◽  
Author(s):  
Yuh-Tyng Huang ◽  
Tong-Rong Tsai ◽  
Chun-Jen Cheng ◽  
Thau-Ming Cham ◽  
Tsun-Fwu Lai ◽  
...  
Keyword(s):  
Sustained Release ◽  
Pyridostigmine Bromide ◽  
In Vitro Dissolution ◽  
Formulation Design ◽  
Sustained Release Tablet ◽  
Dissolution Properties ◽  
Model Drug ◽  
Release Tablet

In Vitro Conditions for the Study of the In Vivo Performance of Sustained-Release Theophylline Matrix Tablets Administered in Fasted Conditions and with a High-Fat Diet

1999 ◽  
Vol 25 (11) ◽  
pp. 1199-1203 ◽  
Author(s):  
M. T. Andonaegui ◽  
J. L. Barría ◽  
A. M. Thielemann ◽  
C. Seitz ◽  
M. N. Gai
Keyword(s):  
Sustained Release ◽  
High Fat Diet ◽  
Matrix Tablets ◽  
High Fat ◽  
Sustained Release Theophylline

Improving of the accuracy of in vitro-in vivo linear correlation using kinetic models for ultra sustained release theophylline tablets

2003 ◽  
Vol 28 (4) ◽  
pp. 301-307 ◽  
Author(s):  
E. Karasulu ◽  
S. Aktogu ◽  
H. Y. Karasulu ◽  
A. Aydogdu ◽  
I. Tuglular ◽  
...  
Keyword(s):  
Sustained Release ◽  
Linear Correlation ◽  
Kinetic Models ◽  
Sustained Release Theophylline

scholarly journals Development of Risperidone PLGA Microspheres

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Susan D’Souza ◽  
Jabar A. Faraj ◽  
Stefano Giovagnoli ◽  
Patrick P. DeLuca
Keyword(s):  
Steady State ◽  
Sustained Release ◽  
Sustained Delivery ◽  
Plga Microspheres ◽  
Sprague Dawley ◽  
Multiple Dosing ◽  
Duration Of Action ◽  
Sprague Dawley Rats

The aim of this study was to design and evaluate biodegradable PLGA microspheres for sustained delivery of Risperidone, with an eventual goal of avoiding combination therapy for the treatment of schizophrenia. Two PLGA copolymers (50 : 50 and 75 : 25) were used to prepare four microsphere formulations of Risperidone. The microspheres were characterized by several in vitro techniques. In vivo studies in male Sprague-Dawley rats at 20 and 40 mg/kg doses revealed that all formulations exhibited an initial burst followed by sustained release of the active moiety. Additionally, formulations prepared with 50 : 50 PLGA had a shorter duration of action and lower cumulative AUC levels than the 75 : 25 PLGA microspheres. A simulation of multiple dosing at weekly or 15-day regimen revealed pulsatile behavior for all formulations with steady state being achieved by the second dose. Overall, the clinical use of Formulations A, B, C, or D will eliminate the need for combination oral therapy and reduce time to achieve steady state, with a smaller washout period upon cessation of therapy. Results of this study prove the suitability of using PLGA copolymers of varying composition and molecular weight to develop sustained release formulations that can tailor in vivo behavior and enhance pharmacological effectiveness of the drug.

scholarly journals Development and Optimization of Floating Microspheres in Amethopterin

2021 ◽  
Vol 14 (4) ◽  
pp. 1538-1543
Author(s):  
Raghav Mishra
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Patient Compliance ◽  
Drug Loading ◽  
Practical Significance ◽  
In Vitro Dissolution ◽  
Minimal Risk ◽  
Gastric Residence Time

Due to the complexity of gastric emptying, as well as its considerable variability, the in vivo efficacy of drug delivery devices cannot be predicted. When it pertains to drugs with an absorption window in the upper small intestine, a controlled drug delivery system with a longer residence period in the stomach may be of considerable practical significance. Recent developments have shown that floating microspheres are particularly well suited for mixing sustained and delayed releases to achieve a variety of release models with a minimal risk of dumping. The aim of present investigation is to develop and analyze the floating microspheres of amethopterin, which after oral administration could increase the gastric residence time and enhance the bioavailability of the drug by sustained release and minimize the dose dependent side effects as well as improves patient compliance. Floating microspheres of ethyl cellulose, Polyvinyl alcohol and polyvinyl pyrrolidone-K90 were formulated by emulsification solvent evaporation technique. The various parameters of prepared microspheres were studied for SEM, flow properties, buoyancy, yield, percent drug loading, in vitro dissolution studies, stability in different pH and FTIR studies. Microspheres prepared with different concentrations of polymers were spherical in shape with smooth surface. The size of microspheres was in range of 256.02 µm and 362.84 µm. Good drug entrapment and buoyancy were observed for formulation F2. The in vitro drug release after 6h was found to be in range from 58.15% to 96.28%. It was established that the newly created floating microspheres of Amethopterin provide an appropriate and practical solution for the sustained release of medication over a longer period of time, resulting in increased oral bioavailability, effectiveness, as well as better patient compliance.

scholarly journals In vitro dissolution profile and in vivo absorption study of sustained-release tablets containing chlorpheniramine maleate with water-insoluble glucan.

1984 ◽  
Vol 32 (9) ◽  
pp. 3720-3723 ◽  
Author(s):  
KEN MASUMOTO ◽  
KUMIKO MATSUMOTO ◽  
AKIYOSHI YOSHIDA ◽  
SHINICHI HAYASHI ◽  
NAOKI NAMBU ◽  
...  
Keyword(s):  
Sustained Release ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Absorption Study ◽  
Chlorpheniramine Maleate ◽  
Sustained Release Tablets ◽  
In Vivo Absorption ◽  
Insoluble Glucan

Excipient-Excipient Interaction in the Design of Sustained-Release Theophylline Tablets: In Vitro and In Vivo Evaluation

2001 ◽  
Vol 27 (6) ◽  
pp. 499-506 ◽  
Author(s):  
Mohsen A. Bayomi ◽  
Saleh A. Al-Suwayeh ◽  
Abdel-Rehim M. El-Helw
Keyword(s):  
Sustained Release ◽  
In Vivo Evaluation ◽  
Sustained Release Theophylline

In vitro Dissolution and in vivo Bioequivalence Evaluation of Two Brands of Isosorbide 5-mononitrate Sustained Release Tablets

2012 ◽  
Vol 62 (12) ◽  
pp. 576-582
Author(s):  
Y.-H. Kim ◽  
K.-S. Choi ◽  
S.-H. Kam ◽  
K.-H. Lee ◽  
J.-S. Park
Keyword(s):  
Sustained Release ◽  
In Vitro Dissolution ◽  
Sustained Release Tablets

scholarly journals Formulation of Lipid-Based Tableted Spray-Congealed Microparticles for Sustained Release of Vildagliptin: In Vitro and In Vivo Studies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2158
Author(s):  
Khaled H. Al Zahabi ◽  
Hind Ben tkhayat ◽  
Ehab Abu-Basha ◽  
Al Sayed Sallam ◽  
Husam M. Younes
Keyword(s):  
Sustained Release ◽  
Oral Drug Delivery ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Once Daily ◽  
Significant Difference ◽  
In Vivo Pharmacokinetics

Spray-congealing (SPC) technology was utilized to prepare lipid-based microparticles (MP) capable of sustaining the release of Vildagliptin (VG) for use as a once-daily treatment for type 2 diabetes mellitus. VG microparticles were prepared using Compritol® and Gelucire®50/13 as lipid carriers in the presence of various amounts of Carbomer 934 NF. The lipid carriers were heated to 10 °C above their melting points, and VG was dispersed in the lipid melt and sprayed through the heated two-fluid nozzle of the spray congealer to prepare the VG-loaded MP (VGMP). The microparticles produced were then compressed into tablets and characterized for their morphological and physicochemical characteristics, content analysis, in vitro dissolution, and in vivo bioavailability studies in mixed-breed dogs. The VGMP were spherical with a yield of 76% of the total amount. VG was found to be in its semicrystalline form, with a drug content of 11.11% per tablet and a percentage drug recovery reaching 98.8%. The in vitro dissolution studies showed that VG was released from the tableted particles in a sustained-release fashion for up to 24 h compared with the immediate-release marketed tablets from which VG was completely released within 30 min. The in vivo pharmacokinetics studies reported a Cmax, Tmax, T1/2, and MRT of 118 ng/mL, 3.4 h, 5.27 h, and 9.8 h, respectively, for the SPC formulations, showing a significant difference (p < 0.05)) from the pk parameters of the immediate-release marketed drug (147 ng/mL, 1 h, 2.16 h, and 2.8 h, respectively). The area under the peak (AUC) of both the reference and tested formulations was comparable to indicate similar bioavailabilities. The in vitro–in vivo correlation (IVIVC) studies using multiple level C correlations showed a linear correlation between in vivo pharmacokinetics and dissolution parameters. In conclusion, SPC was successfully utilized to prepare a once-daily sustained-release VG oral drug delivery system.

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