scholarly journals Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug

2016 ◽  
Vol 3 (2) ◽  
pp. 4-12
Author(s):  
RK Yadav ◽  
Satyam Prakash ◽  
K Yadav ◽  
NK Yadav ◽  
M Mostafa
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Lag Time ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Drug Content ◽  
Drug Entrapment Efficiency ◽  
Gastro Retentive

Background  and  Objectives:  The  prevention  and  treatment  of  peptic  ulcers  has  become  an important challenge in the current medicine  world.   Modern progress in novel drug delivery system aims to improve the efficacy of the drug molecule by formulating a dosage form of RHCL. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in GI tract is to control the gastric residence time.  Therefore, a multi-unit gastro retentive dosage form of RHCL capable of floating on simulated gastric fluid for more than 12 hours was formulated and evaluated.Materials  and  Methods:  Nine  batches  of  the  light  liquid  paraffin  entrapped  emulsion  gel  beads were  prepared  by  a  new  emulsion  gelation  technique  using  sodium  alginate  and  xanthan  gum  as polymers.  The  polymeric  solution  was  extruded  into  Calcium  chloride  solution  by  the  use  of  21G needles.  Morphology  of  beads,  drug  content,  drug  entrapment  efficiency,  floating  lag  time  and buoyancy were studied. Compatibility study of Ranitidine HCl with polymers used in the formulation was performed using DSC and FT-IR.Results:  Mean  surface  diameter  were  between  1.220  ±  2.259%  (F1)  to  1.230  ±  2.316%  (F9)  and floating lag time were between 6 minute (F9) to 11 minute (F1). All formulations were buoyant for more than 12 hours in simulated gastric  fluid  at  37ºC.  The  drug  content  and  drug  entrapment efficiency  among  the  formulations  were  between  17.48%~19.68%  and  71.06%  ~84.32% respectively. Formulation F1 showed lowest drug content and drug entrapment efficiency while F9 showed highest drug content and drug entrapment efficiency. F4 showed most acceptable sustained drug release profile.Conclusion:  The gastro retentive drug delivery system designed as floating beads was found to be satisfactory drug delivery system for Ranitidine HCl to improve the bioavailability of the drug. Janaki Medical College Journal of Medical Sciences (2015) Vol. 3 (2): 4-12

scholarly journals Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

2021 ◽  
Author(s):  
Cheran K ◽  
Udaykumar B Bolmal ◽  
Archana S Patil ◽  
Umashri A Kokatanur ◽  
Rajashree S Masareddy
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Drug Entrapment Efficiency ◽  
Gastro Retentive

Abstract Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.

scholarly journals Microballoons: A Gastro Retentive Drug Delivery System

2019 ◽  
Vol 9 (4-s) ◽  
pp. 625-630
Author(s):  
Ankita Srivastava ◽  
Ruchi Shukla ◽  
Kusum Sharma ◽  
Hitesh Jain ◽  
D. B. Meshram
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Gastric Fluid ◽  
Oral Route ◽  
Gastric Retention ◽  
Preparation Temperature ◽  
Novel Technology ◽  
Floating Drug Delivery ◽  
Gastro Retentive

Oral route is most preferable and widely used route for the administration of drug. Microballoons becomes novel technology in pharmaceutical field in the floating drug delivery for achieving the gastric retention. Microballoons are also called as hollowspheres which are porous smooth in nature and thus show good floating properties in gastric fluid. Microballoons release the drug in controlled manner at the targeted site. Microballoons are spherical empty vesicles without core and that can remain buoyant in gastric region for prolong period of time without irritation in gastrointestinal tract. Multiparticulate particles having a low density system that can efficiently prolong the gastric retention time of the drugs, thus enhanced bioavailability and thus improve the dosing frequency. These are less soluble at higher pH environment. As microballoons delivery systems provide longer retention in gastric pH and enhance the solubility of drugs that are less soluble in high pH environment. The formation of cavity inside the microballoons depend on the preparation, temperature and the surface smoothness determine the floatability and the release rate of microballoons. Keywords: Microballoons, Gastro retentive drug delivery system, Hollowspheres, Controlled release

DEVELOPMENT AND IN VITRO EVALUATION OF FLOATING DRUG DELIVERY SYSTEM OF ACECLOFENAC

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (09) ◽  
pp. 63-66
Author(s):  
J. C Rathi ◽  
◽  
V. Rathi ◽  
S. Tamizharasi
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Gastric Residence Time ◽  
Floating Drug Delivery ◽  
Drug Entrapment Efficiency ◽  
Floating Drug Delivery System ◽  
Central Composite

The objective of the present investigation is to attain optimized floating drug delivery system for aceclofenac by determining the effects of some important factors for the prolongation of gastric residence time. Floating microspheres were prepared by solvent diffusion–evaporation method using ethyl cellulose and hydroxypropylmethylcellulose. A central composite design was applied to optimize the formulation. An appropriate balance between the levels of the polymer and stirring speed was imperative to acquire maximum drug entrapment efficiency, sustained release of the drug, floating ability and adequate particle size.

scholarly journals Formulation and Development of Gastroretentive Drug Delivery System of Efavirenz

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
Monica RP Rao ◽  
Pooja B. Karanjkar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Solid Dispersion ◽  
In Vitro Release ◽  
Lag Time ◽  
Intrinsic Dissolution ◽  
Drug Content

Efavirenz, a non-nucleotide reverse transcriptase inhibitor is an important drug for treating patients with Human Immunodeficiency Virus infections. It belongs to BCS class II have low solubility and poor intrinsic dissolution rate. It is highly basic (pKa 10.2) which makes it suitable candidate for floating dosage form for continuous delivery in stomach.The study was aimed to improve the solubility by solid dispersion technique.Saturation solubility study and drug content were evaluated for solid dispersion preparation. Saturation solubility shows 8 fold increases in 0.1 N HCL compared to plain drug and drug content was found to be between 95%-102%. Further effervescent floating gastroretentive drug delivery system was prepared by 32 full factorial design with independent variables i.e., concentration of HPMC K100 as matrix forming agent and citric acid as gas generating agent. Lag time, floating time, percent drug release were studied as responses. The optimized batch exhibited floating lag time of 40 sec and the in vitro release studies showed 89.5% drug release in 9 h and tablet remained floating for greater than 8 h. The study thus demonstrated that solubility is increased by solid dispersion technique and floating delivery systems may increase solubility and bioavailability of Efavirenz.

scholarly journals Formulation and in-vitro evaluation of niosomal drug delivery system for aceclofenac.

2019 ◽  
Vol 1 (3) ◽  
pp. 84-88
Author(s):  
Samreen ◽  
M. Aruna ◽  
Shaik Harun Rasheed
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Size Distribution ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Dosage Forms ◽  
Prolonged Release ◽  
Vesicle Size ◽  
Drug Content

In the past few decades, considerable attention has been focused on the development of new drug delivery system (NDDS). The NDDS should ideally fulfill two prerequisites. Firstly, it should deliver the drug at a rate directed by the needs of the body, over the period of treatment. Secondly, it should channel the active entity to the site of action. Conventional dosage forms including prolonged release dosage forms are unable to meet none of these. At present, no available drug delivery system behaves ideally, but sincere attempts have been made to achieve them through various novel approaches in drug delivery. The aim of present work is to develop a niosomal drug delivery system of aceclofenac. To perform drug-polymer compatibility FT-IR studies were carried out and observed that there was no interaction between the APl and excipients. 8 niosomal formulations are prepared by the thin film hydration method using the cholesterol as the phospholipid. Prepared niosomal formulations were characterized by vesicle size, shape, surface charge, entrapment efficiency, drug content and invitro drug release studies. The vesicle size, size distribution and zeta potential of the optimized formulation (F5) was found to be 65.6 nm and zeta potential was found to be -1.5mV. Size distribution curve confirms the normal size distribution of the vesicles. The % entrapment efficiency of niosomal vesicles formulations were found to be in the range of 54.18±0.59 to 92.71±0.56 and optimized formulation was found to be 92.71±0.56 and drug content of niosomes formulations (F1to F8) were determined to be in the range of 94.6 -97.8%. The pH of all topical niosomal gels were found to be in the range of 7.4±0.02 to 7.4±0.08.The best fit with higher correlation (r2> 0.99) was found with the Zero Order Release and follows Korsemeyer peppas equation for all the formulations, which means that release of Aceclofenac from the lipid bilayer vesicles were due to diffusion. The stability studies were carried out and there was no significant change found in the formulations.

Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Oral Dosage ◽  
Lag Phase ◽  
Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

Validation of A Simple HPLC-UV Method For the Quantification of Andrographolide in Self-Nano Emulsifying Drug Delivery System (Snedds) For Dissolution Study

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
Syukri Y ◽  
Afetma D. W. ◽  
Sirin M. ◽  
Fajri R. ◽  
Ningrum A. D. K. ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Gastric Fluid ◽  
Hplc Method ◽  
Good Precision ◽  
Intestinal Fluid ◽  
Dissolution Medium ◽  
Relative Standard ◽  
Sufficient Precision

This research aim to validation of a simple, rapid and accurate HPLC-UV method for the quantification of andrographolide isolated from Andrographis paniculata Ness in Self Nano Emulsifying Drug Delivery System (SNEDDS) formulation during the dissolution test. The assay was performed using a XTerra® MS C18 column (150 mm X 4.6 mm, five μm) with a mobile phase of methanol and water (70: 30), at 0.8 mL/min flow rate and UV detection of 229 nm. Simulation gastric fluid (SGF) and intestinal fluid (SIF) were prepared as dissolution medium. The validation parameter was conducted including the test on linearity, precision, accuracy, LOD, and LOQ. The result showed an excellent linearity with r = 0.999 and good selectivity for both medium dissolution. The method showed sufficient precision, with a relative standard deviation (RSD) smaller than % Horwitz. The accuracy reported as % recovery was found to be 102.61 and 101.17 % in each SGF and SIF dissolution medium. LOD and LOQ were found 0.46 and 1.40 in SGF medium, 0.87 and 2.64 in SIF medium. In conclusion, the HPLC method developed showed specificity and selectivity with linearity in the working range, good precision and accuracy and suitable for quantification andrographolide in SNEDDS formulation.

A Review on Emerging Floating Drug Delivery System

2016 ◽  
Vol 6 (4) ◽  
Author(s):  
Christe Mary M ◽  
Sasikumar Swamiappan
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Stomach Contents ◽  
Gastric Fluid ◽  
Dosage Forms ◽  
Gastric Residence Time ◽  
Advantages And Disadvantages ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System

Presently, various approaches have been exploited in the prolongation of gastric residence time which includes floating drug delivery system (FDDS), swelling and expanding systems, bio-adhesive systems, modified shape systems and high density systems. Among various methods, floating drug delivery system is considered to be a predominant method. Gastric emptying of dosage forms is an extremely varying process and ability to extend and control the emptying time is a valuable resource for the dosage forms. This FDDS is having the ability to provides a solution for this purpose. The FDDS is a bulk density system lower than the gastric fluid, so that the rest will float on the stomach contents for a prolonged period of time and allowing the drug to release slowly at a desired rate from the system and intensifies the bio-availability of the drug having narrow absorption window. The main intension of writing this review on floating drug delivery system is to study the mechanism of flotation to acheive the gastric retention and to discuss briefly about the background of FDDS, advantages and disadvantages, application of FDDS and factors affecting the gastric retension time.

scholarly journals Applicability of Gum Karaya in the Preparation and in Vitro Evaluation of Losartan Potassium as Chronotherapeutic Drug Delivery System

2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Tensile Strength ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
Gum Karaya

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 

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