scholarly journals Extended Release Micro-pellets of Chiral Molecule of Metoprolol Succinate by Fluid Bed Technology

2017 ◽  
Vol 9 (01) ◽  
Author(s):  
Dipesh Patel ◽  
Bhupendra Prajapati
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Racemic Mixture ◽  
Drug Release Profile ◽  
Pore Former ◽  
Metoprolol Succinate ◽  
Fluid Bed ◽  
Beta Blocking ◽  
Blocking Activity ◽  
Inert Core

The objective is to prepare extended release micro-pellets of the s-Metoprolol Succinate which is chirally pure molecules. Commercially Metoprolol Succinate is available the racemic mixture of the s and r isomers. Out of both the isomers s-isomer is predominantly responsible for the cardiac beta blocking activity. So to use the more desirable beta blocking activity of s-Metoprolol Succinate, extended release micro-pellets of the s-Metoprolol Succinate was prepared. Due to pure chiral molecules the dose was also reduced to half to that of the racemic mixture. Extended release micro-pellets of the s-Metoprolol Succinate was prepared by the fluid bed technology, in which s-Metoprolol Succinate along with binder and anti-adherent material was sprayed on the inert core. These drug loaded pellets of the s-Metoprolol Succinate was than coated with ethyl cellulose as extended release polymer, hypromellose as pore former and acetyl tri butyl as novel plasticizer and talc as an anti-adherent. The formulation was further optimized for drug release, as per USP recommended dissolution condition, using central composite design (CC). Results shows that at level of 58-66% w/w extended release coating with any studied concentration of acetyl tri butyl citrate and hypromellose gives desired drug release profile.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

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    

scholarly journals MULTIPLE UNIT PELLET SYSTEM (MUPS) BASED FAST DISINTEGRATING DELAYED-RELEASE TABLETS FOR PANTOPRAZOLE DELIVERY

2018 ◽  
Vol 10 (1) ◽  
pp. 77
Author(s):  
Sandipkumar A. Patel ◽  
Nrupa G. Patel ◽  
Abhijeet B. Joshi
Keyword(s):  
Drug Release ◽  
Physical Properties ◽  
Microcrystalline Cellulose ◽  
Release Profile ◽  
Drug Release Profile ◽  
Delayed Release ◽  
Fluid Bed ◽  
Enteric Polymer ◽  
Multiple Unit ◽  
Extrusion Spheronization

Objective: The rationale for the study was to develop multiple unit pellet system (MUPS) of delayed release pantoprazole with desired physical properties and unaltered drug release profile from pellets even after compression into a fast disintegrating tablet.Methods: In the presented study, delayed release pellets of pantoprazole were developed by two methods, i.e. extrusion-spheronization and drug layering techniques, coated using enteric polymer and subsequently compressed in to tablet. In drug layering technique, pantoprazole was loaded on Celphere®102 (microcrystalline cellulose spheres) as well as on Suglet® (sugar spheres) in fluid bed processor. Acid resistant polymer Eudragit ND 30D was subsequently coated on each type of drug loaded pellets. Suitable tableting excipients were prepared such as soft pellets, Ceolus® (fibrous grade of microcrystalline cellulose) granules, Ludipress® (compressible lactose composition), Avicel® PH 200 and different combination of them. Various factors like property of pellets to be compressed, coating level, the composition of tableting excipient and ratio of drug-loaded pellets to tableting excipients were identified and optimized.Results: MUPS with delayed releasing pellets of pantoprazole proved to provide sufficient hardness, rapid disintegration property, and unaltered release profile after compression. Delayed release pantoprazole pellets prepared by drug layering on celphere® 102 followed by coating with Eudragit® NE 30D showed better compressibility to withstand the drug release properties. The combination of Ceolus® granules and Ludipress (in 1:1 ratio) was found to be suitable tableting excipient that helped compression of pellets without rupturing polymeric coat. Pellets to excipients ratio at 1:3 was found optimum.Conclusion: Compaction behaviour of pantoprazole delayed-release pellets without loss of original delayed release profile was achieved by formulating as MUPS based tablet of pantoprazole delayed release pellets using celephere® 102 was developed which was found suitable for desired release profile and physical properties.

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).

Formulation and Evaluation of Levetiracetam Extended Release Tablets

2013 ◽  
Vol 6 (1) ◽  
pp. 1958-1965
Author(s):  
Sudarshan Singh ◽  
Shankar Bhavesh ◽  
Sanjaykumar Nayak ◽  
Sunil Bothara
Keyword(s):  
Data Analysis ◽  
Drug Release ◽  
Extended Release ◽  
Zero Order ◽  
Release Profile ◽  
Matrix Tablet ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Mechanism

Extended release formulation of levetiracetam is approved by the food and drug administration as an add-on to other antiepileptic drugs for adults with partial onset seizures. The main objective of present study was to developed and evaluate matrix tablet of levetiracetam by using various grade of hydroxypropylmethylcellulose (HPMC) polymer. Various trials were taken by using HPMC K4M, K15M, and K100M.  Different parameters like Physical properties, FTIR, DSC, in vitro drug release profile and swelling index were determined. In vitro drug release was performed in phosphate buffer pH 6.8. The in vitro release profile was compared with model independent method. Stability studies were performed as per ICH guidelines for 1 month at (40 °C ± 2 °C/75 % ± 5 % RH).Data analysis was performed for determination of drug mechanism and order of drug release. The in vitro drug release profile of optimized formulation was compared with marketed formulation LEVERAXR. The regression value for zero order, first order, Higuchi and Korsmeyer Peppas was found to be 0.9604, 0.9245, 0.9889 and 0.9729, respectively. Similarity factor (f2) and dissimilarity factor (f1) was found to be 88.61 and 1.82, respectively. The FTIR and DSC study shows that there is no chemical interaction between levetiracetam and excipients. From the data analysis, it was concluded that optimized formulation follow Higuchi model having diffusion mechanism. The order of drug release was considered zero  order release. Stability study shows that there was no remarkable change in drug release after 1 month. It is concluded that the formulation is stable at accelerated conditions.

scholarly journals FORMULATION AND IN VITRO IN VIVO EVALUATION OF BOSENTAN PELLETS FOR PROLONGED DRUG RELEASE

2018 ◽  
Vol 11 (8) ◽  
pp. 498
Author(s):  
Narender Karra ◽  
Narayana Raju P ◽  
Sivakumar R
Keyword(s):  
Drug Release ◽  
Half Life ◽  
Elimination Rate ◽  
Pulmonary Artery Hypertension ◽  
Maximum Plasma ◽  
In Vivo Evaluation ◽  
Pore Former ◽  
Fluid Bed

Objective: The objective of this study was to develop extended release (ER) pellets of Bosentan, an endothelin receptor antagonist using fluid bed processor (coating).Method: The ER drug pellets of Bosentan were prepared using fluid bed coating. These drug-loaded pellets were further coated with ethyl cellulose of two viscosity grades and Eudragit as rate controlling polymers individual and in combination, hypromellose as pore former and binder, acetyl tributyl citrate as plasticizer, and magnesium stearate as anti-adhering agent.Results: The drug release was extended up to 24 h, and the drug release was mainly depends on the polymer type and polymer proportion. In vivo study of Bosentan, ER pellets were performed in healthy rabbits (New Zealand, White) of either sex weighing (3.0–3.3 kg) and were divided into two separate groups, each group consisting of 6 animals. Maximum plasma concentration (Cmax), maximum time (Tmax), area under the curve (AUC0-t), elimination rate constant (Kel), and half-life (T1/2) were studied for optimized formulation. Formulation was releasing the drug for a prolonged period of time.Conclusion: By the above results, it was observed that the prepared pellets could release the drug for an extended period when compared with the conventional dosage form of Bosentan, optimized formulation was shown longer half-life and Cmax indicates its acceptability. Finally, ER pellets of Bosentan were prepared for the treatment of pulmonary artery hypertension by fluid bed processor.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

Anticancer Nano Formulation of Imatinib with Chitosan Polymer

2019 ◽  
Vol 9 (01) ◽  
pp. 58-64
Author(s):  
Senthilnathan B ◽  
Billy Graham R ◽  
Chaarmila Sherin C ◽  
Vivekanandan K ◽  
Bhavya E
Keyword(s):  
Drug Release ◽  
Drug Targeting ◽  
Bone Marrow Failure ◽  
Lymphoblastic Leukemia ◽  
Release Profile ◽  
Nano Particles ◽  
Drug Release Profile ◽  
Study Results ◽  
Mast Cell Disease ◽  
Nano Formulation

Objective: Drug targeting is the capacity of the dosage form. In which the therapeutic agent acts specifically to desired site of action in the non-targeted tissue with the help of Nano particles is called as the drug targeting. IMATINIB is a used to treat cancer by chemo therapy. Cancers like chronic myeloid leukemia cancer (CML) and acute lymphoblastic leukemia cancer (ALL) and other specific types of gastrointestinal stromal cell tumor (GIST) systemic mast cell disease and Bone marrow failure disorder. It is administered by oral root. For ATP, Tyrosine kinase is act as a binding site. Methodology: The drug IMATINIB is loaded in the polymer chitosan, poly-(D) glucosamine is a bio compactible, bio degradable, nontoxic, antimicrobial and soluble in solvents. This preparation is done by emulsion-droplet coalescence method. Content of the Drug, Size of the particle and Zeta potential, Encapsulation efficiency and Drug release testing are described for this formulation in this study. Results: The Imatinib Nano particles were formulated and evaluated for its invitro drug release profile. Based on the invitro drug release profile of Imatinib nano particles formulation (INP1 – INP5) formulation INP3 was selected as the best formulation in which the particle size was 285.9nm. The invitro % drug release of INP3 formulation was 99.76 ± 0.82 and it was found to be the suitable formulation to manage the cancer. Conclusion: Hence it is concluded that the newly formulated controlled release nanoparticle drug delivery system of Imatinib may be idol and effective by allowing the drug to release continuously for 24 hrs.

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