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.

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 of Tamoxifen Loaded Lipid Nanoparticle by Taguchi (L12 (2 11)) Orthogonal Array Design

2020 ◽  
Vol 16 ◽  
Author(s):  
Poovi Ganesan ◽  
N Damodharan
Keyword(s):  
Orthogonal Array ◽  
Drug Loading ◽  
Optimization Technique ◽  
Pharmaceutical Products ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
Orthogonal Array Design ◽  
Formulation Development ◽  
Array Design ◽  
Lipid Nanoparticle

Background: A better understanding of the biopharmaceutical and physicochemical properties of drugs and the pharmaco-technical factors would be of great help for developing pharmaceutical products. But, it is extremely difficult to study the effect of each variable and interaction among them through the conventional approach Objective: To screen the most influential factors affecting the particle size (PS) of lipid nanoparticle (LNPs) (solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC)) for poorly water-soluble BCS class-II drug like tamoxifen (TMX) to improve its oral bioavailability and to reduce its toxicity to tolerable limits using Taguchi (L12 (2 11)) orthogonal array design by applying computer optimization technique. Results: The size of all LNPs formulations prepared as per the experimental design varied between 172 nm and 3880 μm, polydispersity index between 0.033 and 1.00, encapsulation efficiency between 70.8% and 75.7%, and drug loading between 5.84% and 9.68%. The study showed spherical and non-spherical as well as aggregated and non-aggregated LNPs. Besides, it showed no interaction and amorphous form of the drug in LNPs formulation. The Blank NLCs exhibited no cytotoxicity on MCF-7 cells as compared to TMX solution, SLNs (F5) and NLCs (F12) suggests that the cause of cell death is primarily from the effect of TMX present in NLCs. Conclusions: The screening study clearly showed the importance of different individual factors significant effect for the LNPs formulation development and its overall performance in an in-vitro study with minimum experimentation thus saving considerable time, efforts, and resources for further in-depth study.

scholarly journals Formulation, Development, and Optimization of Anti- Hypertensive Nisoldipine Extended-Release Tablet Formulation

2020 ◽  
Vol 5 (03) ◽  
pp. 37-44
Author(s):  
Kukkadapu Pavan Kumar ◽  
Katta Sunand ◽  
Nerella Mounika ◽  
Mohammed Abdul Samad ◽  
A. Madhu Babu ◽  
...  
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Aqueous Solubility ◽  
Cellular Membrane ◽  
Tablet Formulation ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Formulation Development ◽  
Release Tablet

A drug molecule has to be water-soluble to be readily delivered to the cellular membrane. Many drugs are waterinsoluble, which creates numerous problems in the development of dosage forms. Controlled drug delivery formulation releases the drug with controlled kinetics for days and months, reducing the frequency of dosing, minimizing side effects, and improving patient compliance. Nisoldipine is a calcium channel antagonist that is indicated for the treatment of hypertension with very poor aqueous solubility. Thus, there is a need to improve the rate of drug release. Hence, the study was carried out to design, formulate and evaluate sustained-release tablet formulation of nisoldipine. Nisoldipine controlled release matrix tablets were prepared by roll compaction method. Preformulation studies have confirmed the purity and compatibility of drug with excipients used in the formulation. Pre-compression studies have confirmed the stability of formulation blends for compression. All the prepared formulations were evaluated for various physical and compression parameters such as bulk and tapped density, hardness, friability, and in vitro drug release studies. The results of drug release from prepared compressed nisoldipine extended-release tablets were found to be within the desired range.

scholarly journals CHARACTERIZATION OF DRUGS ENCAPSULATED INTO MESOPOROUS SILICA

2019 ◽  
pp. 7-11
Author(s):  
ARIF BUDIMAN
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Molecular State ◽  
Water Soluble ◽  
Crystal Nucleation ◽  
Formulation Development ◽  
Scanning Calorimetry

Solubility of the drug has a strong influence to achieve higher bioavailability of the drug in systemic circulation. More than 70% NCEs (new chemical entities) are hydrophobic, and practically difficult into solid formulation due to their poor water solubility. Mesoporous silicas (MSP) have been used for drug delivery system, especially for poorly water-soluble drugs. Encapsulation and interaction of drugs in MSP can enhance the delivery and maintain the stability of the drug. However, the characterization of the drug in MSP is necessary to confirm its molecular state. In this review, we present an overview of reports related to the characterization of drug encapsulated into MSP. Encapsulation of drugs in MSP can prevent recrystallization of drugs due to its inhibition of crystal nucleation. A porous material in MSP can maintain the drug in a physically stable amorphous state. The preventing of drug crystallization in MSP can enhance the solubility and the dissolution rate of drug. Therefore, in this work, attempts have been made to understand the molecular state of the drug in MSP. The physicochemical characterization of drug by transmission electron microscopy (TEM), scanning electron microscope (SEM), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), powder x-ray diffraction (PXRD) and thermogravimetric analysis (TGA) were discussed. The effect of solvent and methods of drug loading and the effect of the shape of MSP on release profiles are also presented. Overall, this review provides information about the characterization of drug encapsulated into MSP which will be useful in pharmaceutical formulation development.

scholarly journals Formulation Development and Optimization of Oral Thin Films of Zolpidem Tartarate

2017 ◽  
Vol 1 (1) ◽  
pp. 26
Author(s):  
T. Neelima Rani
Keyword(s):  
Thin Films ◽  
Guar Gum ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Solvent Casting ◽  
Formulation Development ◽  
Water Soluble Polymer ◽  
Aqueous Solvent ◽  
Viscous Solution

<em>The aim of the present study was to formulate and evaluate oral thin films of zolpidem tartarate. Zolpidem tartarateis used to treat insomnia. It affects chemicals in your brain that may become unbalanced and cause sleep problems (insomnia). Zolpidem tartarate oral thin films were prepared by using solvent casting method. In this method, water soluble polymer is completely dissolved in to form uniform clear viscous solution other ingredients including API are dissolved in a small portion of aqueous solvent by using a high shear processor. This viscous solution is degassed under the vacuum to remove the air bubbles. This bubble free solution is poured into a glass mold and kept in oven at 40 º-50ºC. Oral disintegrating films are prepared using three grades of polymers HPMC E5, GUAR GUM and SODIUM ALGINATE Compatibility of Zolpidem tartarate with polymers was confirmed by FT-IR studies. All the formulations were evaluated for their physical appearance, average weight and thickness, folding endurance, disintegration time, tensile strength, percentage elongation, drug content, content uniformity and in vitro drug dissolution studies. From the result, it was concluded that the fast dissolving films of Zolpidem tartarate can be made by solvent casting technique with enhanced dissolution rate and taste masking by using suitable combination of sweeteners, flavors and citric acid. The final composition optimized was drug to Guar Gum ratio of 1:1, plasticizer concentration of 15% w/w of polymer. The film had acceptable physical properties, assay and uniformity values and in vitro dissolution within 2 minutes.</em>

scholarly journals FORMULATION DEVELOPMENT AND CHARACTERIZATION OF GELUCIRE BEADS OF ANTIHYPERTENSIVE DRUG FOR FLOATING DRUG DELIVERY SYSTEM USING 32 FACTORIAL DESIGNS

2021 ◽  
pp. 150-156
Author(s):  
KHUSHBOO RANKA ◽  
KAMAL S RATHORE
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Drug Loading ◽  
Linear Regression Analysis ◽  
Extended Period ◽  
Multiple Linear Regression Analysis ◽  
Water Soluble ◽  
Tween 20 ◽  
Formulation Development ◽  
Floating Drug Delivery

Objective: The aim of this study was to design and to optimize lipid based beads for multiunit floating drug delivery of ramipril. Methods: The beads prepared by melt-solidification method. In the investigation 32 full factorial design was used to investigate the joint influence of two formulation variable amount of Gelucire (X1) and Tween 20 (X2) as independent variable and the percentage drug release in 1 (Y1), 6 (Y2), and 12 h (Y3) as dependent variable. Gelucire 43/01 has chosen for release retardant and Tween 20 for solubility enhancement and drug loading agent. Results: The results of multiple linear regression analysis indicated that for obtain a floating drug delivery, the optimum concentrations of both the lipid and drug loading agent should be used. The factorial models were used to prepare optimized floating beads and optimized formulations showed controlled release profiles for the extended period of more than 12 h. Conclusion: From the study, it was concluded that beads of Gelucire for sparingly water-soluble drug ramipril can provide controlled release for extended period.

scholarly journals Nanocrystalization: An Emerging Technology to Enhance the Bioavailability of Poorly Soluble Drugs

2019 ◽  
Vol 7 (4) ◽  
pp. 259-278 ◽  
Author(s):  
Kavita Joshi ◽  
Akhilesh Chandra ◽  
Keerti Jain ◽  
Sushama Talegaonkar
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Chemical Properties ◽  
Active Pharmaceutical Ingredient ◽  
Pharmaceutical Product ◽  
Drug Formulation ◽  
Water Soluble ◽  
Drug Candidate ◽  
Formulation Development ◽  
New Formulation

Most of the active pharmaceutical ingredient used in the management of disease have poor water solubility and offer grueling problems in drug formulation development since low solubility is generally associated with poor dissolution characteristics which leads to poor oral bioavailability. The great challenge for the development of a pharmaceutical product is to create its new formulation and drug delivery system to limit solubility problems of existing drug candidate. Limited drug-loading capacity requires a large amount of carrier material to get appropriate encapsulation of the drug, which is another major challenge in the development of pharmaceutical product which could be resolved by developing nanocrystals (NCs). A significant research in the past few years has been done to develop NCs which helps in the delivery of poorly water soluble drugs via different routes. The technology could continue to thrive as a useful tool in pharmaceutical sciences for the improvement of drug solubility, absorption and bioavailability. Many crystalline compounds have pulled in incredible consideration much of the time, due to their ability to show good physical and chemical properties when contrasted with their amorphous counterparts. Nanocrystals have been proven to show atypical properties compared to the bulk. This review article explores the principles of the important nanocrystallization techniques including NCs characterization and its application.

Neurotoxicity and Neuroprotective Effects of Polyimides (PI) and Polyphenylenevinylene (PPV) against Hydrogen Peroxide (H2O2)

2011 ◽  
Vol 8 (2) ◽  
pp. 33
Author(s):  
Norfaezah Mazalan ◽  
Mazatulikhma Mat Zain ◽  
Nor Saliyana Jumali ◽  
Norhanim Mohalid ◽  
Zurina Shaameri ◽  
...  
Keyword(s):  
Hydrogen Peroxide ◽  
Drug Delivery Systems ◽  
Neuronal Cells ◽  
Water Soluble ◽  
Brain Delivery ◽  
Specific Therapy ◽  
Neuroprotective Effects ◽  
Water Soluble Polymer ◽  
Site Specific ◽  
Novel Drugs

Recently, research and development in the field of drug delivery systems (DDS) facilitating site-specific therapy has reached significant progression. DDS based on polymer micelles, coated micro- and nanoparticles, and various prodrug systems including water-soluble polymer have been prepared and extensively studied as novel drugs designed for cancer chemotherapy and brain delivery. Since polymers are going to be used in human, this study has the interest of testing two types of polymer, polyimides (PI) and polyphenylenevinylene (PPV) on neuronal cells. The objective of this study was to determine the possible neurotoxicity and potential neuroprotective effects of PI and PPV towards SH-SY5Y neuronal cells challenged by hydrogen peroxide (H2O2) as an oxidant. Cells were pretreated with either PI or PPV for 1 hour followed by incubation for 24 hour with 100 µM of H2O2. MTS assay was used to assess cell viability. Results show that PI and PPV are not harmful within the concentration up to 10 µM and 100 µM, respectively. However, PI and PPV do not protect neuronal cells against toxicity induced by H2O2 or further up the cell death.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Molecular Sieves ◽  
Release Kinetics ◽  
Drug Loading ◽  
Scale Up ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drugs ◽  
Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

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