Design and Characterization of Orlistat Bilayered controlled release Tablets

2021 ◽  
pp. 2976-2982
Author(s):  
P. V. Kamala Kumari ◽  
Y. Srinivasa Rao ◽  
S. Akhila ◽  
K. Bhavya Sindhu
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Half Life ◽  
Therapeutic Index ◽  
Immediate Release ◽  
Dosage Forms ◽  
Control Drug ◽  
Elimination Half ◽  
Biopharmaceutical Properties ◽  
Conventional Dosage

Drug delivery in conventional dosage forms often suffers from the drawbacks of repeated drug administration and large fluctuations in blood drug levels. Controlled drug delivery systems are a convenient way of controlling the dosing frequency responsible for rapid absorption and distribution of drug in conventional dosage forms, and are dependent upon two intrinsic properties of the drug, namely, elimination half-life (t1/2) and therapeutic index (TI). The goal is to give a drug at a sufficient rate, frequency and dose so that the ratio Cmax/Cmin in plasma at steady state is always maintained at effective concentrations during the course of therapy, reducing side effects or improving physicochemical and biopharmaceutical properties. The use of polymers provides the potential to control drug delivery both temporally and spatially. The objective of the present investigation was to develop bilayered tablets of orlistat to achieve controlled release and immediate release. The process is predetermined in such a way to release the drug at an IR and CR by using different polymers. Half life of orlistat is 1-2 hrs, as it has been released immediately. This paper mainly focuses on designing the process to release the drug in a controlled manner by using different polymers like sodium alginate, ethyl cellulose, HPMC.

scholarly journals TARGETING THE TARGET USING NANOPARTICLES - A REVIEW

2017 ◽  
Vol 10 (12) ◽  
pp. 6
Author(s):  
Aravinthrajkumar G ◽  
Gayathri R ◽  
Vishnupriya V
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Intravenous Injection ◽  
Immediate Release ◽  
Dosage Forms ◽  
The Body ◽  
Specific Location ◽  
The Right ◽  
Reproducible Manner

  The challenge of drug delivery is the liberation of drug agents at the right time in a safe and reproducible manner, usually to a specific target site. Conventional dosage forms, such as orally administered pills and subcutaneous or intravenous injection, are the predominant routes for drug administration. However, pills and injections offer limited control over the rate of drug release into the body; usually, they are involved in an immediate release of the drug. This article is about how nanoparticles can be used as an effective drug delivery system to target the drug to a specific location or organ.

scholarly journals PHARMACOKINETIC STUDIES OF A CHRONOTHERAPEUTIC DRUG DELIVERY SYSTEM OF LORNOXICAM BY LC-MS/MS METHOD

2018 ◽  
Vol 10 (6) ◽  
pp. 88
Author(s):  
Sindhu Abraham ◽  
Rajamanickam Deveswaran ◽  
Jayaraman Anbu ◽  
Sharon Furtado ◽  
Bharath Srinivasan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Maximum Concentration ◽  
Area Under The Curve ◽  
Immediate Release ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Elimination Half ◽  
Coated Tablet ◽  
Liquid Chromatography Tandem Mass

Objective: The objective of this study was to investigate differences in pharmacokinetic patterns of immediate release tablet (IR) and compression coated tablet (CCT) of lornoxicam, proposed for the chronotherapeutic treatment of rheumatoid arthritis.Methods: The dosage forms were administered to two groups of white New Zealand rabbits (n=3), and the plasma drug levels were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Pharmacokinetic parameters like maximum concentration (Cmax), time is taken to reach maximum concentration (Tmax), area under the curve (AUC), elimination half-life (t1/2) and Mean Residence Time (MRT) were determined.Results: In the case of IR tablets, the drug was detected within 15 min after oral administration and a Cmax of 1269.57±4.04 ng/ml were attained at 2±0.15 h. With CCT, the drug was detected only after 5 h and a Cmax of 1279.24±12.76 ng/ml were attained at 8±0.10 h. The CCT showed maximum drug release at the eighth hour in comparison to IR tablet which showed maximum release at the second hour of study.Conclusion: The predominant lag time prior to drug release from CCT is an indication that it is consistent with the requirements of chronopharmaceutical drug delivery. The results suggest that the compression coated tablet is a promising approach for chronotherapeutic management of rheumatoid arthritis.

scholarly journals Materials for Pharmaceutical Dosage Forms: Molecular Pharmaceutics and Controlled Release Drug Delivery Aspects

2010 ◽  
Vol 11 (9) ◽  
pp. 3298-3322 ◽  
Author(s):  
Heidi M. Mansour ◽  
MinJi Sohn ◽  
Abeer Al-Ghananeem ◽  
Patrick P. DeLuca
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Dosage Forms ◽  
Pharmaceutical Dosage Forms ◽  
Release Drug

scholarly journals FORMULATION OF POLY HERBAL NOVEL DRUG DELIVERY SYSTEM FOR ANTI RHEUMATOID ARTHRITIS

YMER Digital ◽  
2022 ◽  
Vol 21 (01) ◽  
pp. 41-55
Author(s):  
L Tamilselvi ◽  
◽  
R Senthamarai ◽  
A.M. Ismail ◽  
T Shri Vijaya Kirubha ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Interleukin 6 ◽  
Dosage Forms ◽  
Temporal Position ◽  
Transdermal Patch ◽  
Herbal Drug ◽  
Conventional Dosage

Novel herbal drug delivery system opens new vistas for delivery of herbal drugs at right place, at right concentration, for right period of time and also gives scientific angle to verify the standardization of herbal drug. Herbal Transdermal patches can develop valuable assessment and drug safety by additional site specific the way and temporal position in the body’s imperative to reduce the number and size of doses required to achieve the objective of systemic medication during topical application to the intact skin surface. Rheumatoid Arthritis (RA) is a chronic, progressive autoimmune disease of unknown cause. It is characterized by persistent inflammation that primarily affects the peripheral joints. In the present study, herbal transdermal patch was developed by using ethanolic extract of leaves of Cardiospermum halicacabum and rhizomes of Drynaria quercifolia that had already been widely used for the treatment of arthritis in conventional dosage forms. Evaluation of the developed patch for the effectiveness against RA was done by in vitro methods in terms of inhibition of albumin denaturation, measurement of Interleukin-6 cytokines by Enzyme-Linked Immuno Assay (ELISA). IC-50 value was determined from albumin denaturation inhibition assay. The herbal patch significantly and dosedependently inhibited Interleukin–6 cytokines. The present study revealed that the formulated polyherbal Transdermal patch will be the better drug of choice for the treatment of Rheumatoid Arthritis as compared to the conventional dosage forms.

Factors Influencing the Design and Performance of Oral Sustained/Controlled Release Dosage Forms

2009 ◽  
Vol 2 (3) ◽  
pp. 583-594
Author(s):  
Ranjith Kumar Mamidala ◽  
Vamshi Ramana ◽  
Sandeep G ◽  
Meka Lingam ◽  
Ramesh Gannu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Oral Drug Delivery ◽  
Dosage Forms ◽  
Oral Drug ◽  
Factors Influencing ◽  
Maximum Utility ◽  
Systemic Side Effects ◽  
And Performance ◽  
Dosing Intervals

Of all drug delivery systems, oral drug delivery remains the most preferred option for administration for various drugs. Availability of wide variety of polymers and frequent dosing intervals helps the formulation scientist to develop sustained/controlled release products. Oral Sustained release (S.R) / Controlled release (C.R) products provide an advantage over conventional dosage forms by optimizing bio-pharmaceutic, pharmacokinetic and pharmacodynamic properties of drugs in such a way that it reduces dosing frequency to an extent that once daily dose is  sufficient for therapeutic management through uniform plasma concentration providing maximum utility of drug  with reduction in local and systemic side effects and cure or control condition in shortest possible time by smallest quantity of drug to assure greater patient compliance. This review describes the various factors influencing the design and performance of sustained/controlled release products along with suitable illustrations.

Nano Sponges

2019 ◽  
Vol 12 (6) ◽  
pp. 4687-4693
Author(s):  
Amarjit Salunke Salunke ◽  
Neeraj Upamanyu ◽  
Alka Singh ◽  
Ashish Jaiswal
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Drug Release ◽  
Recent Work ◽  
Delivery System ◽  
Therapeutic Index ◽  
Free Carriers ◽  
The Us ◽  
Work Done ◽  
Drug Free

The convenient and recent drug delivery system always likely to have some ideal and unique characters, particularly for safety, desired actions, accurate delivery, enrich with a therapeutic index with minimal adverse occurrence. In this regard, Nano sponges serve as a recent advance new drug delivery. Many researchers are attracted and concerned on Nano sponges presently. The present twofold objective of the review clarifies why Nano sponges are recent and advanced delivery system along with challenges related to solubility, stability and controlled release of Nano sponge and proven techniques to overcome. Since the nano-sized drug free carriers are recently formulated and suggested for drug delivery, which can be loaded with the numerous drugs, hence dealing with an appropriate technique for drug release is the need of the present time. This article states the most convenient method for drug release, and at concluding part gives awareness on recent work done and result obtained on Nano sponge worldwide along with the unique summary on the US granted patents for Nano sponges. Thus, a complete scenario on recent work, methods for evaluations, unique and multiple characters of Nano sponge has been discussed and summarized.

Stiffness of targeted layer-by-layer nanoparticles impacts elimination half-life, tumor accumulation, and tumor penetration

2021 ◽  
Vol 118 (42) ◽  
pp. e2104826118
Author(s):  
Stephanie M. Kong ◽  
Daniel F. Costa ◽  
Anna Jagielska ◽  
Krystyn J. Van Vliet ◽  
Paula T. Hammond
Keyword(s):  
Drug Delivery ◽  
Half Life ◽  
Tumor Targeting ◽  
Layer By Layer ◽  
Elimination Half Life ◽  
Tumor Penetration ◽  
Anticancer Drug Delivery ◽  
Elimination Half ◽  
Tumor Accumulation

Nanoparticle (NP) stiffness has been shown to significantly impact circulation time and biodistribution in anticancer drug delivery. In particular, the relationship between particle stiffness and tumor accumulation and penetration in vivo is an important phenomenon to consider in optimizing NP-mediated tumor delivery. Layer-by-layer (LbL) NPs represent a promising class of multifunctional nanoscale drug delivery carriers. However, there has been no demonstration of the versatility of LbL systems in coating systems with different stiffnesses, and little is known about the potential role of LbL NP stiffness in modulating in vivo particle trafficking, although NP modulus has been recently studied for its impact on pharmacokinetics. LbL nanotechnology enables NPs to be functionalized with uniform coatings possessing molecular tumor-targeting properties, independent of the NP core stiffness. Here, we report that the stiffness of LbL NPs is directly influenced by the mechanical properties of its underlying liposomal core, enabling the modulation and optimization of LbL NP stiffness while preserving LbL NP outer layer tumor-targeting and stealth properties. We demonstrate that the stiffness of LbL NPs has a direct impact on NP pharmacokinetics, organ and tumor accumulation, and tumor penetration—with compliant LbL NPs having longer elimination half-life, higher tumor accumulation, and higher tumor penetration. Our findings underscore the importance of NP stiffness as a design parameter in enhancing the delivery of LbL NP formulations.

scholarly journals Bioavailability of immediate and controlled release formulations of lithium carbonate

2002 ◽  
Vol 24 (2) ◽  
pp. 74-79 ◽  
Author(s):  
Luciana Vismari ◽  
Maria Laura N Pires ◽  
Ana Amélia Benedito-Silva ◽  
Helena Maria Calil
Keyword(s):  
Single Dose ◽  
Controlled Release ◽  
Lithium Concentration ◽  
Area Under The Curve ◽  
Lithium Carbonate ◽  
Immediate Release ◽  
Dose Administration ◽  
Multiple Doses ◽  
Elimination Half ◽  
Controlled Release Formulations

INTRODUCTION/OBJECTIVES: Controlled-release lithium formulations were developed to minimize elevated blood peaks, related to side-effects and intoxications. However, there is little information about the bioavailability of the only controlled-release lithium formulation available in Brazil. The objective of this study was to compare the bioavailability of controlled-release and immediate-release lithium formulations, after single and multiple doses. METHODS: Twelve healthy volunteers received 900 mg of immediate-release or controlled-release lithium carbonate in single or multiple doses during 9 days. After single dose administration, the following parameters were analyzed for each formulation: maximum lithium concentration (Cmax); time to reach Cmax (t max); area under the curve of serum concentration versus time (AUC0-12 and AUC0-<FONT FACE=Symbol>¥</FONT>) and the elimination half-life (t1/2 elim.). After multiple doses, Cmax; t max; AUC0-12; mean (Cmean) and minimum drug concentration (Cmin) and degree of fluctuation (DF) were analyzed. A 90% confidence interval (90%CI) for the ratio between the AUCs for each formulation was constructed. RESULTS/DISCUSSION: Following single dose, the two formulations were bioequivalent; however, they were not after multiple doses. This fact could be a consequence of methodological limitations of lithium level's measurements since, following single dose, these levels could not be detected at time periods 24 and 48h in many volunteers, compromising the calculation of t1/2 elim ,and consequently of the AUC0<FONT FACE=Symbol>-¥</FONT> and the 90%CI to the ratio of these areas. Therefore, the bioequivalence found after single dose may be an unreliable result.

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