In vitro Controlled Release of two new Tuberculocidal Adamantane Aminoethers from Solid Pharmaceutical Formulations (II)

Drug Research ◽  
2017 ◽  
Vol 67 (11) ◽  
pp. 653-660 ◽  
Author(s):  
Marilena Vlachou ◽  
Angeliki Siamidi ◽  
Dimitrios Spaneas ◽  
Dimitrios Lentzos ◽  
Polixeni Ladia ◽  
...  
Keyword(s):  
Controlled Release ◽  
In Vitro Release ◽  
Pharmaceutical Formulations ◽  
Adamantane Derivative ◽  
In Vivo Studies ◽  
Matrix Tablet ◽  
The Us ◽  
Vitro Release

AbstractThe aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of two new tuberculocidal adamantane aminoethers (compounds III and IV), congeneric to the adamantane derivative SQ109, which is in final clinical trials, and aminoethers (I) and (II), using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids. The results suggest that both analogues, albeit more lipophilic than SQ109, and aminoethers (I) and (II), have the requisite in vitro release characteristics for oral administration. In conclusion, these formulations merit further assessment by conducting in vivo studies, at a later stage.

In vitro Controlled Release from Solid Pharmaceutical Formulations of two new Adamantane Aminoethers with Antitubercular Activity (I).

Drug Research ◽  
2017 ◽  
Vol 67 (08) ◽  
pp. 447-450 ◽  
Author(s):  
Marilena Vlachou ◽  
Angeliki Siamidi ◽  
Evanthia Diamantidi ◽  
Alexandra Iliopoulou ◽  
Ioannis Papanastasiou ◽  
...  
Keyword(s):  
Controlled Release ◽  
In Vitro Release ◽  
Antitubercular Activity ◽  
Pharmaceutical Formulations ◽  
Adamantane Derivative ◽  
In Vivo Studies ◽  
Matrix Tablet ◽  
The Us

AbstractThe aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of 2 new tuberculocidal adamantane aminoethers (compounds I and II), congeneric to the adamantane derivative SQ109, which is in final clinical trials, using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids. The results confirm that both analogues, albeit more lipophilic than SQ109, showed satisfactory in vitro release characteristics from solid pharmaceutical formulations. In conclusion, these formulations merit further assessment by conducting in the future bioavailability in vivo studies.

Bosentan Monohydrate Vesicles Loaded Transdermal Drug Delivery System: In Vitro In Vivo Evaluation

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Revathi M. ◽  
Indira Y.
Keyword(s):  
Controlled Release ◽  
Delivery System ◽  
Ex Vivo ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
In Vivo Evaluation ◽  
Vitro Release ◽  
Transdermal Route

This study elucidates the enhancement of the permeation of bosentan monohydrate through skin by encapsulating it in vesicles loaded transdermal delivery system. Niosomal vesicles were formulated by ether injection method. Formulation FN7 (span 60: cholesterol: poloxamer 401, 1.25:1:0.25) showed maximum entrapment efficiency of 96.7±0.037% and was optimized for loading in to transdermal system. Transdermal systems were formulated using both hydrophilic and hydrophobic polymers like HPMC, HEC and EC. Formulation F1 with HPMC was optimized based on in vitro release (99.21±1.45 %) and was further evaluated for ex-vivo permeation. The results indicate that the ex vivo release (98.13±1.65%) was as par with in vitro release and followed zero order super case- II transport mechanism. The in vivo studies were done on New Zealand male rabbits for oral and transdermal route. The results inferred no significant change in half-life of drug but a substantial difference in Tmax, AUC and MRT was observed in transdermal systems. A two fold increase in AUC was observed in transdermal route (18.609±7.251µg/ml/h) when compared to oral route (9.644±5.621µg/ml/h). A controlled release was attained up to 35h and reservoir effect was observed and this may be due to the barrier properties of skin. Drug encapsulated niosomes were released in to the skin by loosening the lipid layers and the surfactant acted as penetration enhancer. The study infers that niosomes loaded transdermal patches of bosentan monohydrate can enhance the bioavailability and provided controlled release for better therapeutic efficacy and safety of drug.

Development of Polymeric Nanocarriers for Brain Targeted Delivery of Atorvastatin: A Quality-By-Design Approach

2020 ◽  
Vol 10 (2) ◽  
pp. 149-158
Author(s):  
Guilherme A.G. Martins ◽  
Fabio S. Murakami ◽  
Mauro S. Oliveira ◽  
Ana F. Furian ◽  
Helen Treichel ◽  
...  
Keyword(s):  
Quality By Design ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Physicochemical Characteristics ◽  
In Vivo Studies ◽  
Mean Size ◽  
Release Study ◽  
Vitro Release

Objective: Atorvastatin (ATV) is effective in reducing total cholesterol and low-density lipoprotein levels. Furthermore, it produces pleiotropic effects in neurodegenerative conditions such as Parkinson's, Alzheimer's, and epilepsy. However, due to the effective defense system of the central nervous system (CNS), the development of new medicines for clinical conditions has proven difficult. In this context, nanotechnology was applied as a promising solution to promote drug vectorization to the brain. Methods: The solvent emulsification-diffusion method was used to develop nanoparticles (NPs) based on polylactic acid and coated with polysorbate 80 containing ATV. Quality-by-Design (QbD) was used in the optimization of nanoparticles production through the application of the experimental design Box-Behnken Design. Results: After optimizing the independent factors including sonication time, surfactant concentration and surfactant volume, the NPs presented physicochemical characteristics such as entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. Conclusion: The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies. The physicochemical characteristics included entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies.

Formulation and Evaluation of Pimozide Buccal Mucoadhesive Patches

1970 ◽  
Vol 2 (4) ◽  
pp. 739-747
Author(s):  
Biswajit Basu ◽  
Kevin Garala ◽  
Thimmasetty J
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
Poly Vinyl Alcohol ◽  
Content Uniformity ◽  
In Vivo Absorption ◽  
Systemic Drug Delivery ◽  
Vitro Release

Within the oral mucosal cavity, the buccal region offers an attractive route of administration for systemic drug delivery. Pimozide patches were prepared using HPMC (15 & 47 cPs), carbopol 934, poly vinyl alcohol, and poly vinyl pyrolidone. FTIR and UV spectroscopic methods revealed that there is no interaction between pimozide and polymers. The patches were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behaviour, tensile strength, and surface pH. In vitro release studies of pimozide-loaded patches in phosphate buffer (pH, 6.6) exhibited drug release in the range of 55.32 % to 97.49 % in 60 min. Data of in vitro release from patches were fit in to different equations and kinetic models to explain release kinetics. The models used were zero and first-order equations, Hixon-Crowell, Higuchi and Korsmeyer-Peppas models. In vivo absorption of pimozide from all the patches ranged from 47.96 % to 83.42 % in 60 min in human volunteers. In vivo studies in rabbits showed 85.97% of drug absorption from HPMC-15 cPs patch in 60 min. Good correlation among in vitro release and in vivo absorption of pimozide was observed

Evaluation of the correlation between in vivo and in vitro release of phenylpropanolamine HCl from controlled-release tablets

1992 ◽  
Vol 85 (1-3) ◽  
pp. 65-73 ◽  
Author(s):  
Shigeru Aoki ◽  
Keizo Uesugi ◽  
Kimio Tatsuishi ◽  
Hiroshi Ozawa ◽  
Masanori Kayano
Keyword(s):  
Controlled Release ◽  
In Vitro Release ◽  
Vitro Release ◽  
Controlled Release Tablets

scholarly journals IN VIVO EVALUATION OF QUINAPRIL TRILAYERED MATRIX TABLETS

2021 ◽  
pp. 117-125
Author(s):  
ASHWIN K ◽  
RAMA MOHAN REDDY T
Keyword(s):  
Drug Release ◽  
Drug Concentration ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Matrix Tablet ◽  
In Vivo Evaluation ◽  
Drug Content

Objective: The aim was to design, formulate, and evaluate the trilayer matrix tablets incorporated with quinapril for extend drug release. Methods: Quinapril trilayer matrix tablets were formulated using design of experiment software wherein initially 27 formulations (QF1-QF27) were designed for active layer from which one best formulation was chosen based on drug content, swelling index and in vitro release studies. The chosen formulation was formulated into extended release trilayed matrix tablet by varying proportions of polymers by direct compression and was evaluated for various physicochemical parameters, drug release. Best formulation was characterized for Fourier transform infrared (FTIR), stability, and pharmacokinetic study. Results: Out of 27 formulations highest drug release was exhibited by QF16 (98.85%) which was formulated into trilayer matrix tablets (AQF16- HQF16). Out of which EQF16 was found to exhibit highest values with 98.42% swelling index, 99.56% drug content, and 99.72% drug release in 24 h. All quinapril trilayer formulations showed zero-order and first-order for marketed product. The optimized formulation EQF16 was found to exhibit no interaction with excipients interpreted by FTIR and no significant changes were observed after loading for stability. In vivo studies conducted using optimized formulation EQF16 attained peak drug concentration (Tmax) of 4.0±0.06 and 1.0±0.03 h for the optimized and commercial formulations, respectively, while mean maximum drug concentration (Cmax) was 302.64±0.07 ng/mL and was significant (p<0.05) as compared to the quinapril marketed product formulation 358.78±0.75 ng/mL. Conclusion: Hence, quinapril was successfully formulated into trilayer matrix tablet and found to be stable.

scholarly journals FORMULATION AND EVALUATION OF TERBINAFINE HYDROCHLORIDE MICROSPONGE GEL

2019 ◽  
pp. 78-85
Author(s):  
VEDAVATHI THAVVA ◽  
SRINIVASA RAO BARATAM
Keyword(s):  
Antifungal Activity ◽  
Controlled Release ◽  
Side Effects ◽  
Research Work ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
Terbinafine Hydrochloride ◽  
Drug Content ◽  
Vitro Release

Objective: The purpose of the present research work was to formulate and evaluate Terbinafine hydrochloride microsponges using quasi emulsion solvent diffusion technique and microsponge gel by using carbopol for controlled release of the drug and consequently avoiding its side effects. Methods: Microsponges containing Terbinafine hydrochloride were obtained successfully with six different drugs: polymer ratios. The formulations were studied for particle size, physical characterization, and in vitro release. Results: A selected THCI microsponge (MS IV) due to its better results when compared to other microsponge formulations was incorporated in different concentrations of carbopol and formulated as gels and evaluated for its pH, viscosity, spreadability, drug content, in vitro release, antifungal activity and in vivo studies. Among the four microsponge gel formulations, THMG II showed better results like pH 6.2, viscosity 3960 cps, spreadability 18.1 g cm/s, drug content of 87.6% and drug release showed fickian release pattern. The antifungal studies showed a zone of inhibition with 15.8 mm when compared to the pure drug, 19.2 mm, marketed formulation 16.0 mm and also showed better antifungal activity on fungal induced guinea pig skin when compared with control. Conclusion: In this study, we found that the controlled release of terbinafine hydrochloride from the microsponge gel reduced side effects and remarkably decreased gel application for fungal treatment.

scholarly journals A 23 FACTORIAL DESIGN FOR FORMULATION AND DEVELOPMENT OF DOXYCYCLINE HYDROCHLORIDE IN SITU GEL FORMING SOLUTION FOR WOUND HEALING APPLICATION

2021 ◽  
pp. 221-232
Author(s):  
N. VISHAL GUPTA ◽  
S. SHANMUGANATHAN ◽  
SANDEEP KANNA ◽  
K. TRIDEVA SASTRI
Keyword(s):  
Wound Healing ◽  
Antimicrobial Agents ◽  
Gelation Time ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
Control Group ◽  
Gelation Temperature ◽  
Vitro Release

Objective: To develop and formulate doxycycline hydrochloride hydrogels employing various polymers for wound healing application. Methods: A thermo-reversible gel can transmute from a sol-gel in replication to environmental temperature vicissitudes made up of gallic acid (GA) and tamarind seed polysaccharide (TSP). An antimicrobial agent (doxycycline hydrochloride) integrated to provide the benefit and efficiently safeguard the wound from infection. A low temperature causes TSP to aggregate intermolecularly with GA to create a gel network. GA–TSP gel heat stability increased with increased concentration of GA. Prepared gel formulations were optimized by 23 factorial designs further evaluated for stability and compatibility, appearance, gelation temperature, gravitational flow simulation, in vitro release, in vivo excision wound model in rats. Results: A strong viscoelastic gel was formed at body temperature in the GA–TSP mixture containing 0.6% (w/v) GA. The prepared formulation exhibited absolute stability and compatibility. The formulations indicated a range of 23±1.47 to 50±1.40 °C. The viscosity values were in the range 6628 to 19146 cps. The optimized gel formulation (DT8) was prepared to analyze the checkpoints and further evaluated for gelation temperature ( °C), viscosity (cps), gelation time (s), and in vitro release of drugs (percent cumulative release of drugs) up to 12 h reflecting R1=36.5±0.61 °C, R2=12887±11 cps, R3=16.2±1.38 min and R4=94.65±0.59 percent. Formulation DT8 showed significant wound healing property and it is comparable to the control group. Formulation DT9 treated group showed faster epithelialization and greater rates of wound contraction in rats. Conclusion: The formulations comprising of TSP with antimicrobial agents demonstrated to be efficient in wound healing. Out of all formulations, DT8 showed better wound healing ability, which is evident from in vivo studies.

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