Formulation development and characterization of highly water-soluble drug-loaded extended-release pellets prepared by extrusion–spheronization technique

2019 ◽  
Vol 16 (5) ◽  
pp. 1351-1365
Author(s):  
Muhammad Iqbal Nasiri ◽  
Rabia Ismail Yousuf ◽  
Muhammad Harris Shoaib ◽  
Kamran Zaheer ◽  
Tariq Ali ◽  
...  
Keyword(s):  
Extended Release ◽  
Water Soluble ◽  
Formulation Development ◽  
Water Soluble Drug ◽  
Extrusion Spheronization

Formulation Development and Evaluation of Multiple Unit Pellet System of Tamsulosin Hydrochloride

2021 ◽  
pp. 5319-5324
Author(s):  
Gavaskar Basani ◽  
Madhusudan Rao Yamsani ◽  
Ramya Sri Sura
Keyword(s):  
Extended Release ◽  
Drug Loading ◽  
Prostate Gland ◽  
Water Soluble ◽  
Formulation Development ◽  
Water Soluble Polymer ◽  
Multiple Unit ◽  
Binder Concentration ◽  
Extrusion Spheronization ◽  
Drug Coating

The aim of current work was to grow extended release multiple unit pellets of Tamsulosin Hydrochloride, is an alpha-blocker, used for the healing of the symptoms of a prostate gland condition called BPH (benign prostatic hyperplasia) by extrusion- spheronization (E/S) and solution/suspension layering (S/S) method. In the Extrusion-Spheronization, A ratio of 75:25, 67:33, 64:36 Tamsulosin Hydrochloride and Microcrystalline cellulose were mixed for making drug pellets and extended release (ER) coating was performed in fluidized bed processor (FBP) by solution/suspension layering with Ethyl cellulose (aqueous. dispersion, 4 cps and 7 cps) and Hypromellose (5cps) with different ratios % weight buildups accordingly. In the Solution/suspension layering (S/S) method, Tamsulosin Hydrochloride drug pellets were prepared by layering onto MCC spheres in FBP. These drug pellets were further coated for extended release with HPMC, 5cps and EC, 7cps. In drug coating stage, drug and different binder (Hypromellose, 5 cps) concentrations 8, 10, 12, 14 mg/unit were coated onto the cores for optimization of binder concentration. The weight of MCC spheres were optimized for further formulations. For all the drug coated pellets, ER coating was given with EC, 7cps and HPMC, 5 cps at a coating level of 8% weight by weight. In the extrusion- spheronization (E/S) Optimization of Drug pellets: Among the trials TD3 (Tamsulosin HCl and MCC) showed good mechanical strength with better yield due to increased MCC concentration. Optimization of Extended Release Coating: Optimized TD3 drug pellets were coated with ER coating using water insoluble polymer (Aq.EC 25% dispersion/ EC, 4cps/ EC, 7cps) and water soluble polymer (HPMC, 5cps). Among these polymers, extended release coating was optimized (TD3E14) with the combination of EC, 7cps and HPMC, 5cps at 8% weight build up. In the Solution/Suspension layering: Optimization of binder concentration in drug coating stage: HPMC, 5cps with 12 mg/unit for TF7 was optimized based on %yield. Optimization of MCC spheres in drug coating stage in formulation of ER pellets with different weight drug pellets: The weight of MCC spheres (160, 170, 180, 190 mg/unit) used in the drug coating stage with binder HPMC, 5cps (12 mg/unit). These drug pellets were given with ER coating at 8% weight buildup by using EC, 7cps and HPMC, 5cps. Among these trials, TF7E7 was optimized. Based on the investigations of the present study, conclusions was. formulating low dose, high soluble, BCS class I drug- Tamsulosin Hydrochloride ER formulation by extrusion-spheronization showed flexibility for batch processing and cost effectiveness while solution/suspension layering was process feasible but time consuming due to high drug loading.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF HIGHLY WATER-SOLUBLE DRUG-LOADED CONTROLLED RELEASE MATRIX TABLETS

2021 ◽  
Vol 44 (1) ◽  
pp. 15-29
Author(s):  
Aqsa Siraj ◽  
Muhammad Nasiri ◽  
Syed Naqvi ◽  
Tariq Ali ◽  
Rabia Yousaf ◽  
...  
Keyword(s):  
Controlled Release ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Formulation Development ◽  
Water Soluble Drug

scholarly journals Preparation of pellets containing a standardized Artemisia annua L. extract by extrusion-spheronization

Revista Fitos ◽  
2021 ◽  
Vol 15 (1) ◽  
pp. 84-92
Author(s):  
Elviscley de Oliveira Silva ◽  
Ricardo Neves Marreto ◽  
Edemilson Cardoso da Conceição ◽  
Maria Teresa Bara
Keyword(s):  
Artemisia Annua ◽  
Antimalarial Activity ◽  
Hplc Method ◽  
Water Soluble ◽  
Solid Ratio ◽  
Solid Dosage ◽  
Artemisia Annua L ◽  
Water Soluble Drug ◽  
Average Size ◽  
Extrusion Spheronization

Artemisinin, the major substance with antimalarial activity of Artemisia annua L., is a poorly water-soluble drug. The development of pellets containing a standardized hydroethanolic extract of A. annua may overcome these drawbacks while offer an intermediate product with good technological properties for subsequent tablet manufacture. This work aimed to obtain and characterize A. annua pellets using the extrusion-spheronization technique. The extract was prepared by percolation and artemisinin content was determined using a validated HPLC method. The standardized extract was then used as a liquid binder in the preparation of pellets with different liquid: solid ratio. The formulation PF5 containing microcrystalline cellulose: A. annua extract (40:58) resulted in pellets with 1.49 ± 0.02 % (w/w) artemisinin, average size of approximately 500 µm and sphericity of 0.82 ± 0.08. These pellets were encapsulated in hard gelatin capsules and the percentage released was higher than 80% in 10 min using 0.1N HCl and phosphate buffer media. These data allow to suggest that the pelletizing strategy used made it possible to achieve the desired artemisinin dissolution and generates perspectives for the potential further use of the A. annua pellets as a solid dosage form for malaria treatment.

Fabrication and characterization of nanostructured lipid carrier system for effective delivery of poorly water-soluble drug quetiapine fumarate

2021 ◽  
pp. 6235-6244
Author(s):  
Deepak Patil ◽  
Seema Pattewar ◽  
Sarvesh Palival ◽  
Gargi Patil ◽  
Swapnil Sharma
Keyword(s):  
Entrapment Efficiency ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
Quetiapine Fumarate ◽  
Water Soluble Drug ◽  
Effective Delivery ◽  
Capmul Mcm ◽  
Central Composite ◽  
Poorly Water Soluble Drug

The aim of present study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of quetiapine fumarate, a second-generation antipsychotic drug. Quetiapine Fumarate (QF) loaded NLC were prepared by hot homogenization followed by an ultrasonication method. Response surface methodology - central composite design (CCD) was used to systemically examine the influence of concentration of capmul MCM EP, concentration of poloxamer 188 and concentration of egg lecithin on particle size (PS) and % entrapment efficiency (% EE) and to optimize the NLC formulation. The CCD consists of three factored design with five levels, plus and minus alpha (axial points), plus and minus 1 (factorial points) and the centre point. A mathematical relationship between variables was created by using Design Expert software Version 12. The statistical evaluations revealed that three independent variables were the important factors that affected the PS and % EE of QF loaded NLC. The best fitted mathematical model was linear and quadratic for PS and % EE respectively. The optimized formulations found with 218.1±0.14nm of PS and 93±0.16% of % EE. Results illustrated the superiority of developed QF loaded NLC formulation as a stable drug delivery system, providing better bioavailability with the possibility of better treatment for psychological disorders.

scholarly journals Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

2009 ◽  
Vol 59 (4) ◽  
pp. 453-461 ◽  
Author(s):  
Vikrant Vyas ◽  
Pankajkumar Sancheti ◽  
Poonam Karekar ◽  
Manali Shah ◽  
Yogesh Pore
Keyword(s):  
Solid Dispersion ◽  
Binary Systems ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Water Soluble Drug ◽  
Dispersion Systems ◽  
Rapid Dissolution

Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407 Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (DE30 70.9 ± 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug, indicating altered rheological characteristics of the polymer at its higher concentration, which might have retarded the release rate of tadalafil.

Investigation on release of highly water soluble drug from matrix-coated pellets prepared by extrusion–spheronization technique

2016 ◽  
Vol 13 (2) ◽  
pp. 333-344 ◽  
Author(s):  
Muhammad Iqbal Nasiri ◽  
Rabia Ismail Yousuf ◽  
Muhammad Harris Shoaib ◽  
Muhammad Fayyaz ◽  
Faaiza Qazi ◽  
...  
Keyword(s):  
Water Soluble ◽  
Water Soluble Drug ◽  
Extrusion Spheronization
Sign in / Sign up

Export Citation Format

Share Document