Adoption of polymeric micelles to enhance the oral bioavailability of dexibuprofen: formulation,in-vitroevaluation andin-vivopharmacokinetic study in healthy human volunteers

2013 ◽  
Vol 19 (6) ◽  
pp. 717-727 ◽  
Author(s):  
Ghada Abdelbary ◽  
Amal Makhlouf
Keyword(s):  
Oral Bioavailability ◽  
Polymeric Micelles ◽  
Healthy Human ◽  
Human Volunteers

Effect of silymarin pretreatment on the bioavailability of domperidone in healthy human volunteers

2014 ◽  
Vol 29 (4) ◽  
Author(s):  
Shravan Kumar Yamsani ◽  
Madhusudan Rao Yamsani
Keyword(s):  
Oral Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Rat Intestine ◽  
Healthy Human ◽  
P Glycoprotein ◽  
Human Volunteers ◽  
Significant Difference

AbstractThe aim of this study was to investigate the effect of silymarin pretreatment on domperidone oral bioavailability in humans.The rats were pretreated with silymarin for 7 days. The transport of domperidone across the rat intestine (duodenum, jejunum, ileum, and colon) was studied by usingIn the everted sac and non-everted sac study with silymarin pretreatment, domperidone transport increased from the duodenum, jejunum, ileum, and colon. The silymarin pretreatment increased the bioavailability of domperidone. There was a statistically significant difference in the pharmacokinetic parameters CThe significant difference in absorption of domperidone on pretreatment with silymarin is due to the inhibition of P-glycoprotein and CYP3A. Silymarin, which inhibits CYP3A4, should be contraindicated for domperidone.

EFFECT OF SILYMARIN ON THE ORAL BIOAVAILABILITY OF RANITIDINE IN HEALTHY HUMAN VOLUNTEERS

2007 ◽  
Vol 22 (2-3) ◽  
Author(s):  
B. Nageshwar Rao ◽  
Maddi Srinivas ◽  
Y. Shravan Kumar ◽  
Y. Madhusudan Rao
Keyword(s):  
Oral Bioavailability ◽  
Healthy Human ◽  
Human Volunteers

Pharmacokinetics of solid lipid Boswellia serrata particles in healthy subjects

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Preeti D. Kulkarni ◽  
Neena D. Damle ◽  
Lal Hingorani ◽  
Vaidhun H. Bhaskar ◽  
Minal R. Ghante ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Oral Bioavailability ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Maximum Plasma ◽  
Boswellic Acid ◽  
Healthy Human ◽  
Boswellia Serrata ◽  
Solid Lipid ◽  
Human Volunteers

Abstract Objectives The anti-inflammatory activity of Boswellia serrata extracts (BSE) is well known. BSE comprises boswellic acids (BA) such as 3-O-acetyl-11-keto-beta-boswellic acid (AKBA) and 11-keto-boswellic acid (KBA) as major constituents. One of the limitations of BAs is their poor oral bioavailability. The aim of the study was to prepare solid lipid particles of Boswellia serrata extract (SLBSP) to enhance the bioavailability of BAs. Methods The pharmacokinetic profile of BAs was studied in 10 healthy human volunteers following a single oral dose of 333 mg of SLBSP. Pharmacokinetic blood samples were collected at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, and 12 h post drug administration. Plasma KBA and AKBA levels were measured using a validated LC-MS/MS method. Pharmacokinetics parameters were estimated using Pheonix WinNonlin (Build 6.4.0.768) software. Results Ten healthy human volunteers were included and peak plasma concentration was achieved in 1.5 and 2.3 h for AKBA and KBA respectively. Maximum plasma concentration (C max) was 8.04 ± 1.67 ng/mL for AKBA and 23.83 ± 4.41 ng/mL for KBA whereas the corresponding area under the concentration-time curve (AUC) was 136.7 ± 56.77 ng/mL*h and 165.7 ± 24.5 ng/mL*h respectively. The elimination half-life (t 1/2) of AKBA and KBA was 6.8 ± 3.0 h and 2.45 ± 0.3 h respectively. Conclusions The SLBSP formulation of BSE showed enhanced oral bioavailability of BAs compared with historically reported data of unformulated BSE.

Pharmacokinetics of solid lipid Boswellia serrata particles in healthy subjects

2021 ◽  
Vol 36 (3) ◽  
pp. 215-221
Author(s):  
Preeti D. Kulkarni ◽  
Neena D. Damle ◽  
Lal Hingorani ◽  
Vaidhun H. Bhaskar ◽  
Minal R. Ghante ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Oral Bioavailability ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Maximum Plasma ◽  
Boswellic Acid ◽  
Healthy Human ◽  
Boswellia Serrata ◽  
Solid Lipid ◽  
Human Volunteers

Abstract Objectives The anti-inflammatory activity of Boswellia serrata extracts (BSE) is well known. BSE comprises boswellic acids (BA) such as 3-O-acetyl-11-keto-beta-boswellic acid (AKBA) and 11-keto-boswellic acid (KBA) as major constituents. One of the limitations of BAs is their poor oral bioavailability. The aim of the study was to prepare solid lipid particles of Boswellia serrata extract (SLBSP) to enhance the bioavailability of BAs. Methods The pharmacokinetic profile of BAs was studied in 10 healthy human volunteers following a single oral dose of 333 mg of SLBSP. Pharmacokinetic blood samples were collected at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, and 12 h post drug administration. Plasma KBA and AKBA levels were measured using a validated LC-MS/MS method. Pharmacokinetics parameters were estimated using Pheonix WinNonlin (Build 6.4.0.768) software. Results Ten healthy human volunteers were included and peak plasma concentration was achieved in 1.5 and 2.3 h for AKBA and KBA respectively. Maximum plasma concentration (C max) was 8.04 ± 1.67 ng/mL for AKBA and 23.83 ± 4.41 ng/mL for KBA whereas the corresponding area under the concentration-time curve (AUC) was 136.7 ± 56.77 ng/mL*h and 165.7 ± 24.5 ng/mL*h respectively. The elimination half-life (t 1/2) of AKBA and KBA was 6.8 ± 3.0 h and 2.45 ± 0.3 h respectively. Conclusions The SLBSP formulation of BSE showed enhanced oral bioavailability of BAs compared with historically reported data of unformulated BSE.

scholarly journals Enhanced Water Dispersibility of Curcumin Encapsulated in Alginate-Polysorbate 80 Nano Particles and Bioavailability in Healthy Human Volunteers

2019 ◽  
Vol 7 (1) ◽  
pp. 39-56 ◽  
Author(s):  
Roopa Govindaraju ◽  
Roopa Karki ◽  
Jayanthi Chandrashekarappa ◽  
Mukunthan Santhanam ◽  
Akshay K.K. Shankar ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Aqueous Solubility ◽  
Nano Particles ◽  
Simulated Gastric Fluid ◽  
Maximum Plasma ◽  
Polysorbate 80 ◽  
Healthy Human ◽  
Ionotropic Gelation ◽  
Quality Life ◽  
Human Volunteers

Background: The turmeric (Curcuma longa) plant, a perennial herb of the ginger family, is an agronomic crop in the south and southeast tropical Asia. Turmeric an Indian yellow gold and universal spice is described in Ayurveda, an ancient treatise on longevity and quality life for the treatment of various inflammatory disorders. The oral bioavailability of curcumin is low due to poor aqueous solubility, alkaline instability and speedy elimination. Objective: The present study is designed to prepare alginate polysorbate 80 nanoparticles to enhance aqueous solubility/dispersibility, hence bioavailability. Method: Curcumin-loaded alginate - polysorbate 80 nanoparticles were prepared by ionotropic gelation technique. Results: The optimized nano particles exhibited higher encapsulation efficiency (95%), particle size of 383 nm and Zeta potential of +200 mV. Formulations exhibited very low dissolution in Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF), but the major portion released in SCF which is attributed to the digestibility of alginate in Simulated Colonic Fluid (SCF) under the influence of colonic micro flora. FTIR and DSC observations revealed the successful entrapment of curcumin in alginate polysorbate-80 nanoparticles. The nanoparticles were more spherical, discrete and homogeneous. In healthy human volunteers, the oral bioavailability (AUC) of curcumin increased 5-fold after the consumption of curcumin nanosuspension compared to curcumin suspension. Maximum plasma concentration Cmax- 636 ± 122 ng/ml was observed at tmax- 2h for nanosuspension, whereas Cmax-87.7 ± 17.9ng/ml at tmax- 4h for suspension. Conclusion: Curcumin-loaded alginate - polysorbate 80 nanoparticles prepared by ionotropic gelation method, successfully entrapped curcumin. Both curcumin suspension and curcumin nanosuspension were safe and well tolerated and may thus be useful in the prevention or treatment of various inflammatory diseases of mankind.

scholarly journals DEVELOPMENT AND IN VIVO EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF ANTIPSYCHOTIC DRUG RISPERIDONE

2016 ◽  
Vol 8 (11) ◽  
pp. 43
Author(s):  
A. Kishore Babu ◽  
M. V. Ramana
Keyword(s):  
Drug Delivery ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Chemical Interaction ◽  
Research Work ◽  
In Vivo Evaluation ◽  
Healthy Human ◽  
Floating Tablets ◽  
Human Volunteers

Objective: The objective of this research work was to formulate and evaluate the floating drug delivery system containing Risperidone, to improve oral bioavailability by increasing gastric residence time.Methods: Total fifteen formulations of Risperidone floating tablets were prepared by direct compression method using different grades of HPMC polymers, Gelucire, Polyox and NaHCO3. In vivo radiographic studies were performed in human volunteers by incorporating barium sulphate.Results: The prepared tablets were characterized and found to exhibit satisfactory physicochemical characteristics. All the prepared batches showed good in vitro buoyancy with low floating lag time. It was observed that the tablets remained buoyant for more than 12h. Optimized formulation (F15) consisting of HPMC K100M, WSR 301, Gelucire 50/13 and NaHCO3, followed diffusion controlled zero-order kinetics and non-fickian transport of the drug. FTIR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. The in vivo radiographic studies revealed that the tablets remained in the stomach for 6h in fasting human volunteers. In vivo bioavailability studies performed in healthy human volunteers and Tmax, Cmax, AUC was calculated and confirmed significant improvement in bioavailability when compared with marketed formulation Respidon 2.Conclusion: The data obtained thus suggests that floating delivery system of Risperidone can be successfully designed to give controlled drug delivery and improved oral bioavailability.

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