scholarly journals DEVELOPMENT AND EVALUATION OF NANOSPONGES LOADED EXTENDED RELEASE TABLETS OF LANSOPRAZOLE

2019 ◽  
Author(s):  
Dingwoke John Emeka Francis ◽  
Felix Sunday Yusuf
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Average Diameter ◽  
Powder Flow ◽  
Solvent Evaporation Method ◽  
Flow Properties ◽  
In Vitro Drug Release ◽  
Drug Molecules ◽  
Optimum Formulation

Nanosponges are tiny sponges with an average diameter below 1µm and consist of cavities filled with drug molecules. Lansoprazole is one of the classes of proton pump inhibitors, it reduces gastric acidity, and used in disorders such as gastric ulcer, duodenal ulcer and reflux oesophagitis.   In present study for extended delivery of lansoprazole at optimal concentration and to reduce the frequency of dosing and thus to increase patient convenience nanosponges loaded extended release tablets were prepared. Initially four different nanosponges formulations were prepared by solvent evaporation method and evaluated on various parameters. Ethyl cellulose was used as entrapping agent and dichloromethane as cross linking agent in various proportions and evaluated for powder flow properties, % yield, zeta potential, and in-vitro drug release characteristics. Based on the evaluation results, formulation NS1 was selected to prepare five extended release tablets formulations by using HPMC K30 and chitosan as extended release polymers. All five formulations were evaluated for thickness, hardness, friability, % drug content and in-vitro drug release. From the results, it was found that all the evaluation results are within pharmacopoeial limits. From this study, we concluded feasibility of extended release of Lansoprazole through nanosponge loaded extended release tablets. Formulation of batch NT1, containing HPMC K30 was found to be optimum formulation.

scholarly journals DESIGN AND IN VITRO EVALUATION OF EXTENDED RELEASE TABLET OF NATEGLINIDE

2018 ◽  
Vol 8 (5-s) ◽  
pp. 235-239
Author(s):  
NILESH M MAHAJAN ◽  
Kalyanee Wanaskar ◽  
Yogesh Bhutada ◽  
Raju Thenge ◽  
Vaibhav Adhao
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Tablet Properties ◽  
Vitro Release

The aim of present study is to formulate and evaluate extended release matrix tablet of Nateglinide by direct compression method using different polymer like HPMC K4 and HPMC K15. Matrix tablet of nateglidine were prepared in combination with the polymer HPMC K4, HPMC K15, along with the excipients and the formulations were evaluated for tablet properties and in vitro drug release studies. Nateglinide matrix tablet prepared by using polymer such as HPMC K4 and HPMC K15,  it was found that HPMC K15 having higher viscosity as compare to HPMC K4 therefore different concentration of polymer were studied to extend the drug release up to 12 h. The tablets of Nateglinide prepared by direct compression had acceptable physical characteristics and satisfactory drug release. The study demonstrated that as far as the formulations were concerned, the selected polymers proved to have an acceptable flexibility in terms of in-vitro release profile. In present the study the percent drug release for optimize batch was found to 94.62%.  Hence it can be conclude that Nateglinide extended release matrix tablet can prepared by using HPMC. The swollen tablet also maintains its physical integrity during the drug release study Keywords: Tablet, in-vitro drug release, Nateglinide, HPMC

scholarly journals Synthesis Characterization of Platinum (IV) Complex Curcumin Backboned Polyprodrugs: In Vitro Drug Release Anticancer Activity

Polymers ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 67
Author(s):  
Honglei Zhang ◽  
Yanjuan Wu ◽  
Xiao Xu ◽  
Chen Chen ◽  
Xiukun Xue ◽  
...  
Keyword(s):  
Drug Release ◽  
Combination Chemotherapy ◽  
In Situ Polymerization ◽  
Average Diameter ◽  
Monomethyl Ether ◽  
Resistant Cell ◽  
Burst Release ◽  
Tumor Resistance ◽  
In Vitro Drug Release

The conventional mono-chemotherapy still suffers from unsatisfied potency for cancer therapy due to tumor heterogeneity and the occurrence of drug resistance. Combination chemotherapy based on the nanosized drug delivery systems (nDDSs) has been developed as a promising platform to circumvent the limitations of mono-chemotherapy. In this work, starting from cisplatin and curcumin (Cur), we prepared a dual drug backboned shattering polymeric nDDS for synergistic chemotherapy. By in situ polymerization of the Cur, platinum (IV) complex-based prodrug monomer (DHP), L-lysine diisocyanate (LDI), and then conjugation with a hydrophilic poly (ethylene glycol) monomethyl ether (mPEG) derivative, a backbone-type platinum (IV) and Cur linkage containing mPEG-poly(platinum-co-Cur)-mPEG (PCPt) copolymer was synthesized. Notably, the platinum (IV) (Pt (IV)) and Cur were incorporated into the hydrophobic segment of PCPt with the fixed drugs loading ratio and high drugs loading content. The batch-to-batch variability could be decreased. The resulting prodrug copolymer then self-assembled into nanoparticles (PCPt NPs) with an average diameter around 100 nm, to formulate a synergetic nDDS. Importantly, PCPt NPs could greatly improve the solubility and stability of Cur. In vitro drug release profiles have demonstrated that PCPt NPs were stable in PBS 7.4, rapid burst release was greatly decreased, and the Pt and Cur release could be largely enhanced under reductive conditions due to the complete dissociation of the hydrophobic main chain of PCPt. In vitro cell viability test indicated that PCPt NPs were efficient synergistic chemotherapy units. Moreover, PCPt NPs were synergistic for cisplatin-resistant cell lines A549/DDP cells, and they exhibited excellent reversal ability of tumor resistance to cisplatin. This work provides a promising strategy for the design and synthesis of nDDS for combination chemotherapy.

scholarly journals Formulation and evaluation of floating microspheres of losartan potassium using sodium alginate and HPMC by solvent evaporation method

2019 ◽  
Vol 9 (1-s) ◽  
pp. 60-66 ◽  
Author(s):  
Kapil Purohit ◽  
Navneet Garud
Keyword(s):  
Drug Release ◽  
Solvent Evaporation ◽  
Losartan Potassium ◽  
Solvent Evaporation Method ◽  
In Vitro Drug Release ◽  
Evaporation Method ◽  
Sustained Action ◽  
Improve Patient

Hollow multі-unіt mіcrospheres were prepared by a solvent dіffusіon technіque іn emulsіon wіth a drug and an acrylіc polymer. These were dіssolved іn a mіxture of ethanol-dіchloromethane and poured іnto an aqueous solutіon of PVA wіth stіrrіng to form emulsіon droplets. The rate of drug release іn mіcro balloons was controlled by changіng the ratіo of polymer to drug. The mіcroballoons were floatіng іn vіtro for 12-24 hours when submerged іn aqueous medіa. Radіographіc studіes showed that mіcroballons admіnіstered orally to humans were dіspersed іn the upper part of the stomach and were held there for 3 hours agaіnst perіstaltіc movement. Floating Microspheres of Losartan potassium were formed by Solvent Evaporation method .The formulas LP7 of Losartan Potassium Floating Microspheres shows a very good drug release profiles and shown better sustained action till the end of last hour (24th hrs). It will improve patient compliance and increase in bioavailability which give better approach to treat hypertensive condition and the angiotensin receptor blocking action of Losartan lower the long term complications of Hypertension and reduce the risk of heart failure, CHF, Myocardial Infarction and also vascular damage in blood vessels and kidney. Keywords: Losartan Potassium, Floating microspheres, Drug Entrapment, In-vitro drug release.

scholarly journals Formulation design and characterization of osmotically controlled tablet of Ramipril

2017 ◽  
Vol 4 (1) ◽  
pp. 1 ◽  
Author(s):  
Bhabani Shankar Nayak ◽  
P. Ellaiah ◽  
Suprava Sethy ◽  
Monalisha Nayak ◽  
Subham Sourajit
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Enzyme Inhibitor ◽  
Release Kinetic ◽  
Flow Properties ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Weight Variation ◽  
Ft Ir

Objective: Ramipril is a long-acting angiotensin-converting enzyme inhibitor. The study aimed to design, formulate and evaluate the oral osmotic drug delivery dosage form of an anti-hypertensive drug, ramipril.Methods: The tablet was formulated using ramipril and different polymers like PVP- K30 and Ethyl cellulose. The microcrystalline cellulose (MCC - diluent), Potassium chloride, Mannitol (osmogen) and Magnesium stearate (lubricant) were used in all the formulations. All the tablets were manufactured by wet granulation method followed by film coating. Compatibility of the drug with excipients was determined by FT-IR spectral analysis. The granules were evaluated for bulk density, Carr’s index and Hausner’s ration to determine flow properties. The prepared compressed and coated tablets were evaluated for weight variation, thickness, hardness, friability, and drug content and in vitro drug release and release kinetic studies.Results: The FT-IR study revealed that drug was compatible with excipients.  The flow properties of granules of most formulation were excellent. All osmotic tablet formulations had good tablet physiochemical properties as per Pharmacopeia. The drug content of all tablet batches was satisfactory. The in vitro drug release study revealed that the formulation F7 containing 100 mg of ethyl cellulose release 100% of drug in 24 h with zero order release kinetics.Conclusions: Ramipril osmotic tablet could be used for safe management of hypertension with greater novelty.

IONOTROPIC TRAPPING LECITHIN BASED CILOSTAZOL NANOCOCHLEATES FOR DRUG DELIVERY APPLICATIONS

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (09) ◽  
pp. 24-32
Author(s):  
V. S Katoriya ◽  
◽  
G. S. Deokar ◽  
S. J. Kshirsagar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Controlled Drug Release ◽  
In Vitro Drug Release ◽  
Drug Molecules ◽  
Study Results ◽  
Phosphodiesterase Iii Inhibitor ◽  
Zero Order Release ◽  
Trapping Method

The nanocochleate drug delivery is based on encapsulating drugs in multilayered lipid crystal matrix (a cochleate) to potentially deliver the drug safely and effectively through the lipoidal membrane. Cilostazol is approved for the treatment of intermittent claudication and used as fibrinolytic agent, platelet aggregation inhibitor, bronchodilator agent, phosphodiesterase III Inhibitor and vasodilator agent. therefore, this drug delivery is suitable to deliver drug molecules into blood vessels. Formulations with lecithin showed good in vitro drug release, drug entrapment study results and the drug in formulations was found to be intact and compatible with lipids used. Two optimized formulations containing cilostazol lecithin-cholesterol showed Korsemayer peppas model perfect zero order release and showed better sustained and controlled drug release. Lecithin-cholesterol nanocochleates prepared by external ionotropic trapping method was found to be better ionic cross linking of drug-lipids particles. Therefore, ionotropic cross-linked particles are promising carriers for oral controlled release dosage forms.

Formulation and Evaluation of Levetiracetam Extended Release Tablets

2013 ◽  
Vol 6 (1) ◽  
pp. 1958-1965
Author(s):  
Sudarshan Singh ◽  
Shankar Bhavesh ◽  
Sanjaykumar Nayak ◽  
Sunil Bothara
Keyword(s):  
Data Analysis ◽  
Drug Release ◽  
Extended Release ◽  
Zero Order ◽  
Release Profile ◽  
Matrix Tablet ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Mechanism

Extended release formulation of levetiracetam is approved by the food and drug administration as an add-on to other antiepileptic drugs for adults with partial onset seizures. The main objective of present study was to developed and evaluate matrix tablet of levetiracetam by using various grade of hydroxypropylmethylcellulose (HPMC) polymer. Various trials were taken by using HPMC K4M, K15M, and K100M.  Different parameters like Physical properties, FTIR, DSC, in vitro drug release profile and swelling index were determined. In vitro drug release was performed in phosphate buffer pH 6.8. The in vitro release profile was compared with model independent method. Stability studies were performed as per ICH guidelines for 1 month at (40 °C ± 2 °C/75 % ± 5 % RH).Data analysis was performed for determination of drug mechanism and order of drug release. The in vitro drug release profile of optimized formulation was compared with marketed formulation LEVERAXR. The regression value for zero order, first order, Higuchi and Korsmeyer Peppas was found to be 0.9604, 0.9245, 0.9889 and 0.9729, respectively. Similarity factor (f2) and dissimilarity factor (f1) was found to be 88.61 and 1.82, respectively. The FTIR and DSC study shows that there is no chemical interaction between levetiracetam and excipients. From the data analysis, it was concluded that optimized formulation follow Higuchi model having diffusion mechanism. The order of drug release was considered zero  order release. Stability study shows that there was no remarkable change in drug release after 1 month. It is concluded that the formulation is stable at accelerated conditions.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

Sign in / Sign up

Export Citation Format

Share Document