scholarly journals Evaluation of the Effect of Dissolution Conditions on the Release Profiles of Felodipine from the Extended Release Push-Pull Osmotic Tablets

2020 ◽  
Vol 36 (1) ◽  
Author(s):  
Vũ Thị Thanh Huyền ◽  
Nguyen Thanh Hai ◽  
Pham Thi Minh Hue
Keyword(s):  
Molecular Weight ◽  
Drug Release ◽  
Osmotic Pressure ◽  
Extended Release ◽  
Primary Component ◽  
Dissolution Medium ◽  
Drug Release Profile ◽  
Permeable Membrane ◽  
Release Profiles

The bilayered push–pull osmotic tablets of 5 mg felodipine were prepared by the double compression method, then the core tablets were coated with cellulose acetate as a semipermeable membrane. One releasing orifice was drilled by laser on the drug side of tablets. The osmotic tablets of felodipine containing low molecular weight PEO (200.000) as the primary component in the drug layer, high molecular weight PEO (5.000.000) as a swelling agent in the push layer and natri chloride as osmotic agent in both drug and push layers which were semi-permeable membrane coated with a weight gain of 8.5 % and the drilled release orifice of 0.8 mm. The influence of dissolution conditions on the release profiles of felodipine from the extended release push-pull osmotic tablets was studied. Dissolution studies of the osmotic tablets of felodipine were carried out in dissolution media with different media pH, stirring speeds or osmotic pressures. The results of the study showed that the drug release profile was similar in dissolution media containing surfactant mimics the in vivo state with varying pH and stirring speeds. However, felodipine released from the osmotic tablets was inversely proportional to the osmotic pressure of the dissolution medium. Therefore, the drug release rate from the osmotic tablets was independent of media pH and stirring speeds, but dependent on the osmotic pressure of the dissolution medium. Keywords Felodipine, push - pull osmotic pump, pH, stirring speeds, osmotic pressure. References    

Formulation and Evaluation of Extended Release Trihexyphenidyl Hydrochloride Hard Gelatin Capsules

2011 ◽  
Vol 4 (1) ◽  
pp. 1359-1367
Author(s):  
Madhusudan Rao Y ◽  
Vinay Kumar K ◽  
Jagan Mohan S ◽  
Kiran Kumar V
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Drug Release Profile ◽  
Coupled Diffusion ◽  
Weight Variation ◽  
Release Studies ◽  
Release Profiles

This work aims at investigating different types and levels of hydrophilic high molecular weight matrix agents, (including HPMC K15M, Metalose-60 SH, Metalose-65 SH and Metalose-90SH-SR), hydrophobic diluent (Talc) and formulation methods (Non-aqueous granulation and direct filling by simple mere mixture) in an attempt to formulate hard gelatin extended release matrix capsules containing Trihexyphenidyl HCl (Benzhexol). The drug release from all the extended release matrix capsules show polymer as well as talc concentration dependent retardation affect. The Metalose 90SH-SR concentration was optimized to approximately 27% w/w of total capsule net content weight. The hydrophobic diluent’s talc concentration was optimized and the useful concentration was approximately 17.45% w/w of the total net capsule content weight. The lactose concentration was also optimized and the effective concentration was found to be approximately 48.36% w/w. The prepared hard gelatin extended release capsules were evaluated for weight variation, Average net content, locked length, content uniformity, assay (drug content) and in-vitro drug release studies. From the in-vitro release studies of the prepared formulations, one formula was optimized from each method. All the formulations showed linear release profiles and extended the release of trihexyphenidyl HCl (Benzhexol) over 10 –12 h. The release profiles of extended release matrix capsules of trihexyphenidyl HCl (THP HCl) from the selected formulations were close to zero order and follow diffusion dependent release. The prepared extended release matrix capsules of trihexyphenidyl HCl (Benzhexol) produced from the optimized formulations ‘NAG-M90SH-SR-5 and DB M90SH-SR-4’ complied with the USP XXVII specifications. The difference factor (f1) and similarity factor (f2) was calculated for all these formulations and found to the below 15 and above 50. Irrespective of the formulation method type and its procedure, the prepared hydrophilic extended release matrix capsules showed non-Fickian anomalous transport (coupled diffusion in the hydrated matrix and polymer relaxation) as the values of release exponent (n) are in between 0.50 and 0.89. Finally it was clear that it is possible to design a formulation with any of the above two methods giving the desired drug release profile suggesting that nonaqueous granulation, Direct filling were good methods for preparing extended release matrix capsules of trihexyphenidyl HCl (Benzhexol).

scholarly journals Dissolution Test for Mianserin Hydrochloride in Tablets

2019 ◽  
Vol 3 (2) ◽  
pp. 18-22
Author(s):  
Letícia Lenz Sfair ◽  
Caren Gobetti ◽  
Martin Steppe ◽  
Elfrides Schapoval
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Dissolution Test ◽  
Dissolution Medium ◽  
Drug Release Profile ◽  
Dissolution Tests ◽  
Usp Apparatus ◽  
Usp Apparatus 2

A dissolution test for mianserin hydrochloride in coated tablets containing 30 mg was developed and validated using a fast ultraviolet spectrophotometric method. The appropriate conditions were determinate after testing sink conditions, agitation spped and dissolution medium. The sink conditions tested showed that mianserin hydrochloride was soluble in 0.01 and 0.1 M hydrochloric acid (HCl), acetate buffer pH 4.1 and 5.0 and phosphate buffer pH 6.8. Then, dissolution tests were performed to investigate the drug release in each medium. Optimal conditions to carry out the dissolution test were 900 mL 0.1 M HCl and USP apparatus 2 (paddle) at 50 rpm stirring speed. The quantification method was also adapted and validated. The UV method showed specificity, linearity, precision and accuracy. The in vitro dissolution test can be used to evaluate the drug release profile and the data was used as an aid to establish a possible correlation with in vivo data.

scholarly journals Development and biopharmaceutical evaluation of extended release formulation of tramadol hydrochloride based on osmotic technology

2009 ◽  
Vol 59 (1) ◽  
pp. 15-30 ◽  
Author(s):  
Pramod Kumar ◽  
Sanjay Singh ◽  
Brahmeshwar Mishra
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Relative Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Healthy Human ◽  
Tramadol Hydrochloride ◽  
Release Formulation ◽  
Extended Release Formulation

Development and biopharmaceutical evaluation of extended release formulation of tramadol hydrochloride based on osmotic technologyExtended release formulation of tramadol hydrochloride (TRH) based on osmotic technology was developed and evaluated. Target release profile was selected and different variables were optimized to achieve it. Formulation variables such as the level of swellable polymer, plasticizer and the coat thickness of semipermeable membrane (SPM) were found to markedly affect drug release. TRH release was directly proportional to the levels of plasticizer but inversely proportional to the levels of swellable polymer and coat thickness of SPM. Drug release from developed formulations was independent of pH and agitation intensity but dependent on osmotic pressure of the release media.In vivostudy was also performed on six healthy human volunteers and various pharmacokinetic parameters (cmax,tmax,AUC0-24,MRT) and relative bioavailability were calculated. Thein vitroandin vivoresults were compared with the performance of two commercial TRH tablets. The developed formulation provided more prolonged and controlled TRH release compared to the marketed formulation.In vitro-in vivocorrelation (IVIVC) was analyzed according to the Wagner-Nelson method. The optimized formulation (batch IVB) exhibited good IVIV correlation (R= 0.9750). The manufacturing procedure was found to be reproducible and formulations were stable over 6 months of accelerated stability testing.

In vitro and in vivo release of dinalbuphine sebacate extended release formulation: Effect of the oil ratio on drug release

2017 ◽  
Vol 531 (1) ◽  
pp. 306-312 ◽  
Author(s):  
Chan-Jung Li ◽  
Mei-Yun Ku ◽  
Chia-Yin Lu ◽  
Yu-En Tien ◽  
Wendy H. Chern ◽  
...  
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
In Vivo Release

scholarly journals Targeted and modular architectural polymers employing bioorthogonal chemistry for quantitative therapeutic delivery

2020 ◽  
Vol 11 (12) ◽  
pp. 3268-3280 ◽  
Author(s):  
Gayathri R. Ediriweera ◽  
Joshua D. Simpson ◽  
Adrian V. Fuchs ◽  
Taracad K. Venkatachalam ◽  
Matthias Van De Walle ◽  
...  
Keyword(s):  
Side Effects ◽  
Cancer Therapy ◽  
Drug Release ◽  
Standard Of Care ◽  
Release Profile ◽  
Specific Drug ◽  
Bioorthogonal Chemistry ◽  
Drug Release Profile ◽  
Therapeutic Delivery

There remain several key challenges to existing therapeutic systems for cancer therapy, such as quantitatively determining the true, tissue-specific drug release profile in vivo, as well as reducing side-effects for an increased standard of care.

scholarly journals IVIVC from Long Acting Olanzapine Microspheres

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Susan D'Souza ◽  
Jabar A. Faraj ◽  
Stefano Giovagnoli ◽  
Patrick P. DeLuca
Keyword(s):  
Drug Release ◽  
Rank Order ◽  
Plga Microsphere ◽  
Release Rates ◽  
Proper Selection ◽  
Long Acting ◽  
Selection Of ◽  
Release Profiles

In this study, four PLGA microsphere formulations of Olanzapine were characterized on the basis of theirin vitrobehavior at 37°C, using a dialysis based method, with the goal of obtaining an IVIVC.In vivoprofiles were determined by deconvolution (Nelson-Wagner method) and using fractional AUC. Thein vitroandin vivorelease profiles exhibited the same rank order of drug release. Further,in vivoprofiles obtained with both approaches were nearly superimposable, suggesting that fractional AUC could be used as an alternative to the Nelson-Wagner method. A comparison of drug release profiles for the four formulations revealed that thein vitroprofile lagged slightly behindin vivorelease, but the results were not statistically significant (P<0.0001). Using the four formulations that exhibited different release rates, a Level A IVIVC was established using the deconvolution and fractional AUC approaches. A nearly 1 : 1 correlation (R2>0.96) betweenin vitrorelease andin vivomeasurements confirmed the excellent relationship betweenin vitrodrug release and the amount of drug absorbedin vivo. The results of this study suggest that proper selection of anin vitromethod will greatly aid in establishing a Level A IVIVC for long acting injectables.

Metronidazole Loaded Polycaprolactone-Carbopol blends Based Biodegradable Intrapocket Dental Film for Local Treatment of Periodontitis

2020 ◽  
Vol 10 ◽  
Author(s):  
Nitin Dhedage ◽  
Gayasuddin Khan ◽  
Gufran Ajmal ◽  
Manish Kumar ◽  
Abhishek Jha ◽  
...  
Keyword(s):  
Drug Release ◽  
Gingival Crevicular Fluid ◽  
Local Treatment ◽  
Local Drug Delivery ◽  
Release Kinetic ◽  
Burst Release ◽  
Drug Release Profile ◽  
Initial Zone

: The goal of this research was to produce intrapocket dental film, composed of polycaprolactone and carbopol blends by a modified solvent casting method. Prepared films were consistent in thickness (2.10±0.56 to 2.50±0.39 mm) and weight (35.23±0.37 to 39.45±0.45 mg) with drug entrapment of up to 87.63±1.98 percent. The concentration of carbopol is observed to have a direct relationship with thickness, film weight, and swelling factor of the prepared dental film. The film has a surface pH close to gingival crevicular fluid pH and is therefore appropriate for the application. The developed film exhibited a biphasic drug release profile with an initial burst release followed by a continuous release for more than 11 days. Drug release kinetic study supports the release of the drug by a diffusion-based process, as best explained by the Korsmeyer Peppas kinetics (R2 = 0.9635). In-vitro antimicrobial activity was also in accordance with drug release, with a high initial zone of inhibition (ZOI) (49.32±0.156mm), followed by 14.28±0.080 mm ZOI on 11th day. The in-vivo study showed that the prepared film was able to prevent periodontal ligament degeneration as observed in the periodontitis experiment animal model. In conclusion, prepared intrapocket dental film based on caprolactone and carbopol can be used as a novel local drug delivery system for the management of periodontitis.

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