Sustained-release of Cyclosporin A pellets: preparation, in vitro release, pharmacokinetic studies and in vitro–in vivo correlation in beagle dogs

2015 ◽  
Vol 42 (7) ◽  
pp. 1174-1182 ◽  
Author(s):  
Dongmei Jiang ◽  
Jin Zeng ◽  
Yuan Zhu ◽  
Guanghui Zhou ◽  
Wenwen Deng ◽  
...  
Keyword(s):  
Sustained Release ◽  
Cyclosporin A ◽  
In Vitro Release ◽  
Pharmacokinetic Studies ◽  
Beagle Dogs ◽  
Vitro Release

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

In vitro release and in vivo absorption in beagle dogs of meloxicam from Eudragit® FS 30 D-coated pellets

2006 ◽  
Vol 322 (1-2) ◽  
pp. 104-112 ◽  
Author(s):  
Chunsheng Gao ◽  
Jian Huang ◽  
Yan Jiao ◽  
Li Shan ◽  
Yan Liu ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Beagle Dogs ◽  
In Vivo Absorption ◽  
Vitro Release

scholarly journals Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 168
Author(s):  
Md. Khalid Anwer ◽  
Essam A. Ali ◽  
Muzaffar Iqbal ◽  
Mohammed Muqtader Ahmed ◽  
Mohammed F. Aldawsari ◽  
...  
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Janus Kinase ◽  
Hybrid Nanoparticles ◽  
Polymer Hybrid ◽  
Vitro Release

Baricitinib (BTB) is an orally administered Janus kinase inhibitor, therapeutically used for the treatment of rheumatoid arthritis. Recently it has also been approved for the treatment of COVID-19 infection. In this study, four different BTB-loaded lipids (stearin)-polymer (Poly(d,l-lactide-co-glycolide)) hybrid nanoparticles (B-PLN1 to B-PLN4) were prepared by the single-step nanoprecipitation method. Next, they were characterised in terms of physicochemical properties such as particle size, zeta potential (ζP), polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL). Based on preliminary evaluation, the B-PLN4 was regarded as the optimised formulation with particle size (272 ± 7.6 nm), PDI (0.225), ζP (−36.5 ± 3.1 mV), %EE (71.6 ± 1.5%) and %DL (2.87 ± 0.42%). This formulation (B-PLN4) was further assessed concerning morphology, in vitro release, and in vivo pharmacokinetic studies in rats. The in vitro release profile exhibited a sustained release pattern well-fitted by the Korsmeyer–Peppas kinetic model (R2 = 0.879). The in vivo pharmacokinetic data showed an enhancement (2.92 times more) in bioavailability in comparison to the normal suspension of pure BTB. These data concluded that the formulated lipid-polymer hybrid nanoparticles could be a promising drug delivery option to enhance the bioavailability of BTB. Overall, this study provides a scientific basis for future studies on the entrapment efficiency of lipid-polymer hybrid systems as promising carriers for overcoming pharmacokinetic limitations.

scholarly journals Formulation and Evaluation of Parenteral Sustained Release Microspheres of Diclofenac Sodium

2003 ◽  
Vol 71 (2) ◽  
pp. 101-111
Author(s):  
C. Sajeev ◽  
R. Archna ◽  
V. Gupta ◽  
A. Sobti ◽  
R. Saha
Keyword(s):  
Sustained Release ◽  
Response Time ◽  
Diclofenac Sodium ◽  
In Vitro Release ◽  
Tail Flick ◽  
Duration Of Action ◽  
Sustained Release Formulation ◽  
Vitro Release

The aim of this study was to formulate and evaluate microsphere based depot type parenteral sustained release formulation of diclofenac sodium (DFS). Drug was formulated in the form of microspheres, using varying proportion of ethylcellulose (EC) as the retardant material to extend the release, by phase separation-coacervation technique. The in vitro release pattern of the designed formulations was studied using modified Franz diffusion cell. In vivo pharmacodynamic study was carried out by determining the index of analgesia (increase in response time to thermal stress as percentage of basal response time). Tail flick method was employed to measure both the degree of analgesia and its duration of action. The prepared microspheres were white, free flowing, and spherical in shape with a mean particle size of 50 μm. In vitro release study of the micro-spheres in aqueous media was found to extend the release of DFS beyond 24 hours with DFS and EC ratio 1:3. The plot of log percentage remaining to be released vs. time gave a linear relationship indicating first-order release kinetics. The in vitro release rate constant (Kr) for different microspheres varied between 0.1448 hr-1 and 0.0256 hr-1. A good correlation was obtained between K, and proportion of EC in the microspheres. In vivo pharmacodynamic studies indicated that the duration of analgesic action is prolonged beyond 24 hrs in case of microsphere products of 1:3 ratio of DFS to EC, whereas administration of marketed parenteral preparation showed activity only up to 11hrs. Also, a good correlation was obtained between analgesic activity in vivo and cumulative percentage of drug release from the formulations.

scholarly journals New Technology of Thermoplastic Coating for Osmotic Pump Tablets: Study on in vivo Drug Release

2020 ◽  
Vol 02 (01) ◽  
pp. e1-e10
Author(s):  
Chun Ping Yuan ◽  
Hui Min Hou ◽  
Zhi Hong Cheng ◽  
Qing Hua Ge ◽  
Ding Zhong Song ◽  
...  
Keyword(s):  
Drug Release ◽  
New Technology ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Metformin Hydrochloride ◽  
Beagle Dogs ◽  
Coating Technology ◽  
Vitro Release

Abstract Aim The in vivo pharmacokinetics of thermoplastic-coated tablets prepared by a new technology of thermoplastic coating in Beagle dogs were studied, and the correlation between in vitro release and in vivo absorption was analyzed. Methods The in vitro release profiles of metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets were investigated. The single-dose pharmacokinetic study of these tablets in Beagle dogs was performed, and the obtained results were separately compared with the data of conventional osmotic pump tablets reported in the literature. Results Metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets displayed controlled drug-release characteristics and had a good in vivo–in vitro correlation in Beagle dogs, respectively. The literature-compared results further demonstrated that both thermoplastic-coated tablets had release characteristics of osmotic pump tablets in vivo. Conclusion The thermoplastic-coated tablets could control drug release in vivo and it was further confirmed that the new thermoplastic coating technology could replace the spray coating of osmotic pump controlled-release tablets. This study provides a theoretical basis and practical support for the industrialization and clinical application of the new thermoplastic coating technology.

Development, in vitro release and in vivo bioavailability of sustained release nateglinide tablets

2020 ◽  
Vol 55 ◽  
pp. 101355 ◽  
Author(s):  
D. Nagasamy Venkatesh ◽  
S.N. Meyyanathan ◽  
R. Shanmugam ◽  
A. Zielinska ◽  
J.R. Campos ◽  
...  
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Development In Vitro ◽  
Vitro Release

Reliability of a Single β-Thromboglobulin Measurement in a Diabetic Population : Importance of PGE1 in Anticoagulant Mixture

1987 ◽  
Vol 57 (02) ◽  
pp. 201-204 ◽  
Author(s):  
P Y Scarabin ◽  
L Strain ◽  
C A Ludlam ◽  
J Jones ◽  
E M Kohner
Keyword(s):  
In Vitro Release ◽  
Mean Value ◽  
Reliable Estimate ◽  
Diabetic Patients ◽  
Single Measurement ◽  
Diabetic Population ◽  
The Difference ◽  
Vitro Release

SummaryDuring the collection of samples for plasma β-thromboglobulin (β-TG) determination, it is well established that artificially high values can be observed due to in-vitro release. To estimate the reliability of a single β-TG measurement, blood samples were collected simultaneously from both arms on two separate occasions in 56 diabetic patients selected for a clinical trial. From each arm, blood was taken into two tubes containing an anticoagulant mixture with (tube A) and without (tube B) PGE!. The overall mean value of B-TG in tube B was 1.14 times higher than in tube A (p <0.01). The markedly large between-arms variation accounted for the most part of within-subject variation in both tubes and was significantly greater in tube B than in tube A. Based on the difference between B-TG values from both arms, the number of subjects with artifically high B-TG values was significantly higher in tube B than in tube A on each occasion (overall rate: 28% and 14% respectively). Estimate of between-occasions variation showed that B-TG levels were relatively stable for each subject between two occasions in each tube. It is concluded that the use of PGEi decreases falsely high B-TG levels, but a single measurement of B-TG does not provide a reliable estimate of the true B-TG value in vivo.

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