New Approaches for Optimizing Oral Drug Delivery: Zero- Order Sustained Release to Pulsatile Immediate Release Using the Port System

2002 ◽  
pp. 273-280
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Oral Drug Delivery ◽  
Immediate Release ◽  
Zero Order ◽  
Oral Drug ◽  
New Approaches ◽  
Port System

scholarly journals FORMULATION AND EVALUATION OF NIFEDIPINE SUSTAINED RELEASE TABLETS BY USING DIFFERENT POLYMERS

2019 ◽  
Vol 8 (5) ◽  
Author(s):  
Shraddha Pawan Pareek ◽  
Sunil Kumawat ◽  
Vijay Sharma ◽  
Devender Sharma ◽  
Devendra Singh Rathore
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Pharmaceutical Products ◽  
Matrix Tablets ◽  
Oral Drug ◽  
Release Formulation ◽  
Therapeutic Benefits ◽  
Sustained Release Tablets

Oral drug delivery has been known for many years because the most generally utilized route of administration among all the routes that are explored for the general delivery of medication via various pharmaceutical products of different dosage forms.  The reason that the oral route achieved such quality could also be partly attributed to its simple administration moreover because the ancient belief that by oral administration the drug is well absorbed because the food stuffs that area unit eaten daily. In fact the event of a pharmaceutical product for oral delivery, no matter its physical kind involves variable extents of optimization of dose kind characteristics at intervals the inherent constraints of GI physiology.  The rationale for development of a extended release formulation of a drug is to enhance its therapeutic benefits, minimizing its side effects while improving the management of the diseased condition. The aim of the present investigation is to formulate and evaluate matrix tablets of Nifedipine using a mixture of polymers in view to sustain the drug release, reduce frequency of administration and improved patient compliance. In this research paper all evaluation parameter and stability studies also well discussed in well manner. Keyword: Matrix Tablets, Coating, Novel Drug Delivery System, Sustained Release Tablets

scholarly journals Formulation of Lipid-Based Tableted Spray-Congealed Microparticles for Sustained Release of Vildagliptin: In Vitro and In Vivo Studies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2158
Author(s):  
Khaled H. Al Zahabi ◽  
Hind Ben tkhayat ◽  
Ehab Abu-Basha ◽  
Al Sayed Sallam ◽  
Husam M. Younes
Keyword(s):  
Sustained Release ◽  
Oral Drug Delivery ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Once Daily ◽  
Significant Difference ◽  
In Vivo Pharmacokinetics

Spray-congealing (SPC) technology was utilized to prepare lipid-based microparticles (MP) capable of sustaining the release of Vildagliptin (VG) for use as a once-daily treatment for type 2 diabetes mellitus. VG microparticles were prepared using Compritol® and Gelucire®50/13 as lipid carriers in the presence of various amounts of Carbomer 934 NF. The lipid carriers were heated to 10 °C above their melting points, and VG was dispersed in the lipid melt and sprayed through the heated two-fluid nozzle of the spray congealer to prepare the VG-loaded MP (VGMP). The microparticles produced were then compressed into tablets and characterized for their morphological and physicochemical characteristics, content analysis, in vitro dissolution, and in vivo bioavailability studies in mixed-breed dogs. The VGMP were spherical with a yield of 76% of the total amount. VG was found to be in its semicrystalline form, with a drug content of 11.11% per tablet and a percentage drug recovery reaching 98.8%. The in vitro dissolution studies showed that VG was released from the tableted particles in a sustained-release fashion for up to 24 h compared with the immediate-release marketed tablets from which VG was completely released within 30 min. The in vivo pharmacokinetics studies reported a Cmax, Tmax, T1/2, and MRT of 118 ng/mL, 3.4 h, 5.27 h, and 9.8 h, respectively, for the SPC formulations, showing a significant difference (p < 0.05)) from the pk parameters of the immediate-release marketed drug (147 ng/mL, 1 h, 2.16 h, and 2.8 h, respectively). The area under the peak (AUC) of both the reference and tested formulations was comparable to indicate similar bioavailabilities. The in vitro–in vivo correlation (IVIVC) studies using multiple level C correlations showed a linear correlation between in vivo pharmacokinetics and dissolution parameters. In conclusion, SPC was successfully utilized to prepare a once-daily sustained-release VG oral drug delivery system.

Formulation and Evaluation of Tramadol Hydrochloride Sustained Release Matrix Tablets

2018 ◽  
Vol 8 (3) ◽  
Author(s):  
B Sai Adithya ◽  
Gulshan Mohammad ◽  
Rama Rao Nadendla
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Patient Compliance ◽  
Oral Drug Delivery ◽  
The Body ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Tramadol Hydrochloride

The ultimate goal of any oral drug delivery system is the successful delivery of the drug, in which almost 90% of the drugs are administered to the body for the treatment of various disorders and diseases as it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. The aim of the present study is to formulate sustained release matrix tablets of a model drug (Tramadol hydrochloride) using HPMC 100 MCR, HPC and EC 7cps as rate retarding polymers, microcrystalline cellulose as bulking agent, magnesium stearate as lubricant and aerosil as glidant. Drug and polymer interactions were evaluated by using FTIR and DSC. The FTIR spectrum and DSC thermograms stated that drug and polymer are compatible to each other. Tablets were prepared by direct compression technique. The micromeritic properties of formulation mixtures of all the formulations were carried out and they were found to be as angle of repose (31.150- 40.100), bulk density (0.310g/ml-0.337g/ml), tapped density (0.355g/ml-0.59g/ml), Carr’s index (8.11%-15.3%), Hausner’s ratio (1.08-1.18) which are within the limits. The formulated tablets were physically acceptable and exhibited acceptable weight variation, friability. In vitro dissolution studies were carried out using USP type-II dissolution apparatus and of all the formulations F6 (containing HPMC and HPC in equal proportions) exhibited prolonged drug release for about 8 hrsas per the objective of the work. The percent drug content varied between 88% to 99%. It can be concluded from the study that the sustained release tablets can be better alternative over immediate release tablets by improving patient compliance and reducing frequency.

scholarly journals Preparation and Evaluation of a Novel Oral Microemulsion Drug Delivery System for Enhancing the Bioavailability of Diltiazem

2021 ◽  
Vol 70 (2) ◽  
Author(s):  
Ranajit Nath ◽  
Ratul Bhowmik ◽  
Rajarshi Chakraborty ◽  
Sourav Datta ◽  
Apala Chakraborty
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Immediate Release ◽  
Oral Drug ◽  
Accelerated Stability ◽  
Oral Drug Delivery System

Diltiazem, a calcium ion cellular influx inhibitor is known for its limited and variable bioavailability. This study is intended to explore the benefits of microemulsion formulation as an oral drug delivery system for immediate release to improve the bioavailability and efficacy of Diltiazem. Methods: Oil in water microemulsion was prepared using the simple water titration method. The optimized formulation was evaluated for physicochemical parameters like viscosity, pH, conductivity, and accelerated stability studies. In vitro release, diltiazem microemulsion was investigated.

scholarly journals FORMULATION AND EVALUATION OF MODIFIED DISINTEGRATING SUSTAINED RELEASE TABLETS OF DICLOFENAC SODIUM

2021 ◽  
Vol 6 (4) ◽  
pp. 52-66
Author(s):  
Lukkad Harish R ◽  
Oswal Rajesh
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Concentration ◽  
Oral Drug Delivery ◽  
Diclofenac Sodium ◽  
Oral Drug ◽  
Total Drug ◽  
Sustained Release Tablets ◽  
Suitable Technique ◽  
Fast Disintegrating Tablets

Oral drug delivery is the largest and the oldest segment of the total drug delivery market. It is the fastest growing and most preferred route for drug administration. In oral drug delivery, the sustained release (SR) tablets maintains the desired drug concentration for prolong period of time, reduced 'see- saw' fluctuation, reduced total dose, improved efficiency in treatment. But many patients like paediatric, geriatric and also patients may have difficulty in swallowing (Dysphagia) find it difficult to swallow tablets and thus do not comply with prescription. This problem is overcome by formulating and developing modified disintegrating sustained release tablets. In this case, first microspheres of the drug are formulated by using any suitable technique. And then optimized microspheres formulation is further formulated in to the fast disintegrating tablets (FDT) by using superdisintegrants. So that after taking such a tablets, the tablet only disintegrates into the mouth then microspheres are separated and ingestion of such microspheres starts releasing drug for prolonged period of time. This concept fulfills both the advantages of sustained release and fast disintegrating tablets.

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