scholarly journals Guar gum and hydroxy propyl methylcellulose compressed coated tablets for colonic drug delivery: in vitro and in vivo evaluation in healthy human volunteers

2011 ◽  
Vol 5 (2) ◽  
pp. 90-95 ◽  
Author(s):  
Fahima M. Hashem ◽  
Dalia S. Shaker ◽  
Mohamed Nasr ◽  
Ibrahim E. Saad ◽  
Reem Ragaey
Keyword(s):  
Drug Delivery ◽  
Guar Gum ◽  
Healthy Human ◽  
Colonic Drug Delivery ◽  
Human Volunteers

Gamma scintigraphic studies on guar gum matrix tablets for colonic drug delivery in healthy human volunteers

1998 ◽  
Vol 55 (2-3) ◽  
pp. 245-252 ◽  
Author(s):  
Y.S.R Krishnaiah ◽  
S Satyanarayana ◽  
Y.V Rama Prasad ◽  
S Narasimha Rao
Keyword(s):  
Drug Delivery ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Healthy Human ◽  
Colonic Drug Delivery ◽  
Human Volunteers

In Vitro and In Vivo Evaluation of Guar Gum-Based Matrix Tablets of Rofecoxib for Colonic Drug Delivery

2005 ◽  
Vol 2 (2) ◽  
pp. 155-163 ◽  
Author(s):  
S. Al-Saidan ◽  
Y. Krishnaiah ◽  
V. Satyanarayana ◽  
G. Rao
Keyword(s):  
Drug Delivery ◽  
Guar Gum ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
Colonic Drug Delivery

scholarly journals Development of Buccoadhesive Systems of Pentarocine for Systemic Drug Delivery

2003 ◽  
Vol 71 (4) ◽  
pp. 281-301
Author(s):  
D. Sampathkumar ◽  
M. Thilek Kumar ◽  
J. Balasubrarnaniam ◽  
J. Pandit
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Propylene Glycol ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Zero Order ◽  
Healthy Human ◽  
Human Volunteers

Bucoadhesive patches of Pentazocine (PZ) for unidirectional drug delivery were prepared by casting carboxy methyl cellulose (CMC) with glycerol or propylene glycol and CMC-hydroxy ethyl cellulose (HEC) with glycerol. In vitro mucoadhesivity of the prepared patches were determined using a modified mucoadhesive bond strength apparatus using rabbit small intestine mucosa (SIM). Drug release kinetics was evaluated from composite patches, prepared by covering all but one side of the PZ patches with 3M backing material. Biocompatability / buccoadhesion time and in vivo permeation of placebo and PZ loaded patches were determined using a double blind cross over study in healthy human volunteers. Drug release from CMC-glycerol patches and pure HEC patches showed zero order kinetics with diffusional exponent (n) ranging between 0.79 to 1.046, while that from CMC-HEC and CMC-propylene glycol patches showed an apparent zero order release kinetics. The prepared patches were well tolerated by the human volunteers as they did not produce any side effects at the contact surface. The in vitro mucoadhesivity of CMC-propylene glycol patches were significantly lower than CMC- glycerol based patches. The in vivo permeation of selected PZ patches delivered the drug well above the minimum buccal permeation rate, so as to attain effective blood concentration

A Study of Mucoadhesive Bond Strength of Buccoadhesive Compacts for Systemic Drug Delivery: In-vitro/ In-vivo correlation

2001 ◽  
Vol 69 (2) ◽  
pp. 123-141
Author(s):  
D. Kumar ◽  
J. Balasubramaniam ◽  
J. Pandit
Keyword(s):  
Drug Delivery ◽  
Bond Strength ◽  
Buccal Mucosa ◽  
Healthy Human ◽  
Human Volunteers ◽  
Intestine Mucosa ◽  
Systemic Drug Delivery ◽  
Systemic Drug

Compacts prepared from binary combinations of Carbopol® 934 P (CP), Polycarbophil (Noveon® AA1, PC) and Hydroxy propyl cellulose (Klucel®, HPC) and coated on all but one flat surface with Poly Methyl Methacrylate - PMMA (chloroformic solution) were evaluated for mucoadhesive bond strength on a modified mucoadhesive bond strength apparatus using rabbit stomach mucosa (SM) and small intestine mucosa (SIM). In -vitro mucoadhesion tests indicated that the detachment force increased linearly with concentration of CP/PC in the compacts. Mucoadhesion of the compacts with SIM were higher when compared to SM. The compacts with higher proportions of CPIPC showed longer buccoadhesion time (time the compact remained in contact with the buccal mucosa) than HPC alone in humans. In-vivo buccoadhesevity of the coated compacts was studied in healthy human volunteers. An index was used to study the redness and ulceration of the contact buccal mucosa. Compacts with higher proportions of CP/PC showed longer buccoadhesion time than HPC alone. Significant correlation coefficient (r) values (P<0.01) were obtained between in-vitro fracture strength of the compacts and in-vivo buccoadhesion time. Hence, the in-vitro mucoadhesive model developed by us provides useful information on the residence time of the compact for systemic drug delivery in the oral cavity, and compacts containing less than 50% of CP/PC were safer to use in humans.

scholarly journals ABT-378, a Highly Potent Inhibitor of the Human Immunodeficiency Virus Protease

1998 ◽  
Vol 42 (12) ◽  
pp. 3218-3224 ◽  
Author(s):  
Hing L. Sham ◽  
Dale J. Kempf ◽  
Akhteruzammen Molla ◽  
Kennan C. Marsh ◽  
Gondi N. Kumar ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitor ◽  
Response To Therapy ◽  
Hiv Protease ◽  
Healthy Human ◽  
Human Volunteers ◽  
Immunodeficiency Virus ◽  
Potent Protease Inhibitor

ABSTRACT The valine at position 82 (Val 82) in the active site of the human immunodeficiency virus (HIV) protease mutates in response to therapy with the protease inhibitor ritonavir. By using the X-ray crystal structure of the complex of HIV protease and ritonavir, the potent protease inhibitor ABT-378, which has a diminished interaction with Val 82, was designed. ABT-378 potently inhibited wild-type and mutant HIV protease (Ki = 1.3 to 3.6 pM), blocked the replication of laboratory and clinical strains of HIV type 1 (50% effective concentration [EC50], 0.006 to 0.017 μM), and maintained high potency against mutant HIV selected by ritonavir in vivo (EC50, ≤0.06 μM). The metabolism of ABT-378 was strongly inhibited by ritonavir in vitro. Consequently, following concomitant oral administration of ABT-378 and ritonavir, the concentrations of ABT-378 in rat, dog, and monkey plasma exceeded the in vitro antiviral EC50 in the presence of human serum by >50-fold after 8 h. In healthy human volunteers, coadministration of a single 400-mg dose of ABT-378 with 50 mg of ritonavir enhanced the area under the concentration curve of ABT-378 in plasma by 77-fold over that observed after dosing with ABT-378 alone, and mean concentrations of ABT-378 exceeded the EC50 for >24 h. These results demonstrate the potential utility of ABT-378 as a therapeutic intervention against AIDS.

scholarly journals Comparative Bioavailabilitv Studv of Two Brands of Terbutaline Sulphate Tablets in Healthy Human Volunteers

2004 ◽  
Vol 72 (3) ◽  
pp. 227-237
Author(s):  
Nahla S. Barakat ◽  
Nawal M. Khalafallah ◽  
Said A. Khalil
Keyword(s):  
Single Dose ◽  
Reference Product ◽  
Hplc Method ◽  
Fasting State ◽  
Unchanged Drug ◽  
Healthy Human ◽  
Terbutaline Sulphate ◽  
Human Volunteers

The purpose of this study was to evaluate the bioavailability of locally produced 2.5 mg terbutaline sulphate tablets (brand A ) relative to a reference product, Bricanyl 2.5 mg tablets (brand 6). The study was a single dose 5 mg randomized crossover one in 15 healthy volunteers in the fasting state. Urine was collected at intervals of 24 h. Total terbutaline excreted in urine as unchanged drug and as conjugates (sulphate and glucuronide) was determined by a developed and validated HPLC method. In-vitro characteristics of both brands were similar. Based on percent of the dose excreted in urine, the oral bioavailability ranged from 33.5% to 75.8% for both brands. Statistics were applied to judge bioequivalence according to USP 24 in-vivo bioequivalence guidance. Results indicated that brand A and B were bioequivalent and hence interchangeable in medical practice.

In vivo generation of human dendritic cell subsets by Flt3 ligand

Blood ◽  
2000 ◽  
Vol 96 (3) ◽  
pp. 878-884 ◽  
Author(s):  
Eugene Maraskovsky ◽  
Elizabeth Daro ◽  
Eileen Roux ◽  
Mark Teepe ◽  
Charlie R. Maliszewski ◽  
...  
Keyword(s):  
T Cell Immunity ◽  
Human Dendritic Cell ◽  
Flt3 Ligand ◽  
Healthy Human ◽  
Cell Immunity ◽  
Human Volunteers ◽  
Immune Response Regulation ◽  
Dendritic Cell Subsets

Abstract Dendritic cells (DCs) represent a family of ontogenically distinct leukocytes involved in immune response regulation. The ability of DCs to stimulate T-cell immunity has led to their use as vectors for immunotherapy vaccines. However, it is unclear whether and to what degree in vitro–generated DCs are representative of DCs that develop in vivo. Treatment of mice with human Flt3 ligand (FL) dramatically increases the number of DCs. We report here that administration of FL to healthy human volunteers increased the number of circulating CD11c+ IL-3Rlow DC (mean 44-fold) and CD11c− IL-3Rhigh DC precursors (mean 12-fold). Moreover, the CD11c+ DCs were efficient stimulators of T cells in vitro. Thus, FL can expand the number of circulating, functionally competent human DCs in vivo.

scholarly journals Assessment of Drug Delivery Kinetics to Epidermal Targets In Vivo

2021 ◽  
Vol 23 (3) ◽  
Author(s):  
M. Hoppel ◽  
M. A. M. Tabosa ◽  
A. L. Bunge ◽  
M. B. Delgado-Charro ◽  
R. H. Guy
Keyword(s):  
Experimental Approach ◽  
Input Function ◽  
Drug Uptake ◽  
Tape Stripping ◽  
Healthy Human ◽  
Topical Product ◽  
Human Volunteers ◽  
Dermal Pharmacokinetics

AbstractIt has proven challenging to quantify ‘drug input’ from a formulation to the viable skin because the epidermal and dermal targets of topically applied drugs are difficult, if not impossible, to access in vivo. Defining the drug input function to the viable skin with a straightforward and practical experimental approach would enable a key component of dermal pharmacokinetics to be characterised. It has been hypothesised that measuring drug uptake into and clearance from the stratum corneum (SC) by tape-stripping allows estimation of a topical drug’s input function into the viable tissue. This study aimed to test this idea by determining the input of nicotine and lidocaine into the viable skin, following the application of commercialised transdermal patches to healthy human volunteers. The known input rates of these delivery systems were used to validate and assess the results from the tape-stripping protocol. The drug input rates from in vivo tape-stripping agreed well with the claimed delivery rates of the patches. The experimental approach was then used to determine the input of lidocaine from a marketed cream, a typical topical product for which the amount of drug absorbed has not been well-characterised. A significantly higher delivery of lidocaine from the cream than from the patch was found. The different input rates between drugs and formulations in vivo were confirmed qualitatively and quantitatively in vitro in conventional diffusion cells using dermatomed abdominal pig skin.

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