scholarly journals Formulation development and in-vitro evaluation of Molsidomine matrix tablets for colon specific release

2020 ◽  
Vol 10 (2) ◽  
pp. 59-68
Author(s):  
D. Hema Naga Durga ◽  
T. Lakshmi Sowjanya ◽  
T. Pavani ◽  
Lohithasu Duppala

Colon targeted tablets were prepared in two steps. Initially core tablets were prepared and then the tablets were coated by using different pH dependent polymers. Ethyl cellulose, Eudragit L100 and S100 were used as coating polymers. FT-IR studies were carried out to find out the possible interaction between the selected drugs and polymer. FT-IR studies revealed that there  was  no  interaction between the selected drug and excipients. The pre-compression blend of all formulations was subjected to various flow property tests and all the formulations passed the tests. The tablets were coated by using polymers and the coated tablets were subjected to various evaluation techniques. The tablets passed all the tests. Among all the formulations F3 formulation was found to be optimized as it was retarded the drug release up to 12 hours and showed maximum of 97.57% drug release. It followed zero order kinetics mechanism. The ideal formulation was subjected to stability studies at 40°C/75%RH. The stability studies indicated that the formulation was stable and retained its pharmaceutical properties at 40°C/75%RH over a period of 1 month. Keywords: Colon target, Ethyl cellulose, Eudragit L100 and S100, pH dependent polymers.

Author(s):  
B. Valli Manalan ◽  
Nadendla Swathi ◽  
Narra Nandini ◽  
N. Hari Sree ◽  
Nilla Tejaswi Sai Maha Lakshmi ◽  
...  

The aim of the present study was to design an oral sustained release matrix tablet of highly water soluble biguanide anti diabetic drug. The matrix tablets are prepared by melt granulation method using HPMC K 200M as hydrophilic drug release retarding polymer, and stearic acid as melt able binder as well as hydrophobic carrier. The drug and excipients compatibility was studied by FT – IR. The formulated matrix tablets were characterized for physical parameters and in vitro dissolution profile. FT – IR spectra revealed the absence of drug excipients interaction. The physical parameters of the tablets were found within the limits. The drug release kinetics demonstrated that by increasing the concentration of hydrophilic polymer and hydrophobic carrier the drug release rate was retarded proportionally. Kinetic modelling of in vitro release profile revealing that the drug release from the matrix tablets following first order kinetics, and the drug release mechanism of optimized (F7) formula following non fickian transport mechanism. Accelerated stability studies were performed according to ICH guide lines. Temperature 40±20 c and relative humidity 75±5% RH to study physical and chemical changes of formulation. No physical or chemical changes were observed after t accelerated stability studies.


Author(s):  
ZEESHAN SHAIKH

Objective: Irbesartan is an antihypertensive with limited bioavailability. The objective of the study was to develop controlled release matrix tablets of irbisartan drug. Methods: Tablets were prepared by wet granulation process. Result: In vitro drug release study revealed that HPMC causes initial burst release of drug hence combining HPMC sustained the action for 8 h (95.92±0.57% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism for drug release. Compared to conventional tablets, the release of model drug from these HPMC matrix tablets was prolonged, leading to achieve an effective therapy with a low dosage of the drug, to reduce the frequency of medication. The pharmacological and clinical properties of irbesartan, a noncompetitive angiotensin II receptor type 1 antagonist, successfully used for more than a decade in the treatment of essential hypertension. Results: Compatibility Studies In order to investigate the possible interactions between irbesartan and distinct polymers and/or diluents, FT-IR and DSC studies were carried out. FT-IR results proved that the drug was found to be compatible with excipients as wave numbers are almost similar for pure drug and also drug excipients mixture. In picture 1 and 2. DSC studies indicate that chosen excipients for the formulation were found to be compatible with the active ingredient as the melting endothermic peaks are in the range of 250-320 °C which is same as the melting point of irbisartan. Conclusion: Irbesartan exerts its antihypertensive effect through an inhibitory effect on the pressure response to angiotensin II. Irbesartan 150–300 mg once daily confers a lasting effect over 24 h, and its antihypertensive efficacy is further enhanced by the coadministration of hydrochlorothiazide.


Author(s):  
A. Bhavani ◽  
B. Hemalatha ◽  
K. Padmalatha

The present focus is on the development of sustained release formulations due to its inherent boons. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance, reduction in fluctuation and increased safety margin of potent drug. The present study was aimed to prepare a sustained drug delivery system to design a controlled release oral dosage form of Cefpodoxime proxetil. The sustained release matrix tablets of Cefpodoxime proxetil were prepared by wet granulation and evaluated for different parameters such as weight variation, drug content, thickness, hardness, friability and In vitro release studies. The in vitro dissolution study was carried out for 12 hours using USP (Type- II) paddle apparatus in hydrochloride (0.1N) as dissolution media for first 2 hours and phosphate buffer (pH 6.8) for next 10 hours. Based on the in vitro dissolution data, formulation F8 was selected as the best formulation from Cefpodoxime proxetil formulations (F1 – F9) as the drug release was retarded up to 12 hours with 96.29 % and followed zero order release kinetics & drug release mechanism was diffusion.


Author(s):  
Ruchi Tiwari ◽  
Akanksha Lahiri ◽  
Gaurav Tiwari ◽  
Ramachandran Vadivelan

The present study assessed the topical potential of nanofibers loaded with Mupirocin (MUP) for the treatment of burns. Nanofibers of MUP were composed of Polyvinyl Pyrrolidone (PVP), Gelatin Type-A, and Ethanol using two methods: Solvent casting and Electrospinning. Nanofibers were characterized for Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), Differential scanning calorimetry (DSC), Thermogravimetric analysis (TGA), Drug Content Studies, in-vitro drug permeation, antibacterial and stability studies. The FT-IR studies showed that the Electrospinning technique had a very good mixing of MUP with the polymer. SEM studies showed that the morphology of electrospinning nanofibers had diameters in the range of 70.41 nm- 406.83 nm. The thermal decomposition studies of optimized Nanofiber (E.S.1) were performed by DSC and TGA study and it was found that the formulation had high stability in high-temperature environments. Permeation studies showed that E.S.1 had the highest percentage amount and controlled release of the drug (90 %) up to 8 has compared to other formulations. Nanofibers prepared through the Electrospinning technique showed better antibacterial activity against Staphylococcus aureus as compared to the Solvent casting nanofibers. This research suggested that MUP loaded nanofibers can be potentially used as a topical drug delivery system for the treatment of burns. 


Author(s):  
Sundaramoorthy Kaliyan

Monolithic matrix tablets of metformin hydrochloride were formulated as extended release tablets by employing ethyl cellulose polymer and the extended release characterization of the formulated tablets was investigated.  Extended release matrix tablets containing 500 mg metformin hydrochloride were developed by changing concentration of drug :  polymer (EC) in the ratio of 5:1, 5:2, 5:3 and 5:4 by direct compression.  Formulations were optimized based on the acceptable tablet properties invitro and invivo drug release.  The resulting formulations produced robust tablets with optimum hardness, weight variation, drug content and low friability.  The result of invitro and invivo drug release studies indicated that formulation (drug:polymer =5:3), is the most successful of the study and exhibited constant and extended release of metformin hydrochloride 99-100.5% release at the end of 10 h compared with reference standard.  Further, the formulation F3 was subjected to exposure at room and accelerated condition to stability studies.  A decrease in release of the drug was observed on increasing polymer ratio at certain level.  Before tablet compression, the resulting formulation blends were evaluated for angle of repose, bulk density, % porosity, % compressibility index and drug polymer compatibility study of drug and excipients.  The t25, t50 and t90 drug release values was calculated from selected formulation F3 on every month of stability studies and comparision of both room and accelerated condition by statistical t-test, there is no difference between storage temperature. The formulation F3 was showed similar invitro and invivo drug release when compared to marketed sustained release tablet (F5M).


Author(s):  
Hir. R. Mehta ◽  
Vijay K. Patel

The present invention was aimed to formulate and evaluate Lafutidine gastro retentive films. The films were prepared by solvent casting technique using different film forming polymers like HPMC and Ethyl cellulose. PEG 400 used as a plastsizer. The prepared films were evaluated for number of parameters like Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, unfolding behavior, floating properties, drug content and In vitro drug release studies. From the trial batches the best release for gastroretentive film was shown by formulation T5 (Ethyl cellulose and PEG 400). Formulation T5 exhibited good appearance, better mechanical strength with acceptable flexibility. Also, formulation T5 was given more than 90 % drug released after 12 hr and 97.56 % Drug content.  For optimization of formulation, 32 factorial design was applied by taking Ethyl cellulose and PEG 400 as an independent variables. Drug release at 8 hour and folding endurance selected as dependent variables. Based on drug release study, L8 batch found most satisfactory in all formulation and the effect of Ethyl cellulose and PEG 400 found significant. L8 batch found stable during stability study. Key words: Lafutidine, Floating Films, Ethyl Cellulose.


2012 ◽  
Vol 1 (11) ◽  
pp. 376-383 ◽  
Author(s):  
M Mallikarjuna Gouda ◽  
A Ramakrishna Shabaraya ◽  
S M Shanta Kumar

Current study is to develop the colon targeted matrix tablet using the natural polysaccharide sterculia gum as carrier and model drug ciprofloxacin HCl. The matrix tablets were prepared by wet granulation technology using the various proportions of sterculia gum with carbopol 934 P, sterculia gum and ethyl cellulose polymer blends. Granules of all formulations were evaluated for rheological, post compressional properties and in vitro dissolution study in different pH buffers of pH 1.2 , pH 7.4 , pH 6.8 (saline phosphate buffer) without and with 4% rat cecal content in order to mimic GIT condition . Formulation SGC2 to SGC4 and SGE7 to SGE9 has released 13.6% to 38.9% in the initial 5h and released more amount of drug in stomach and small intestine than colon. Formulation SGC5 containing 45% of sterculia gum and 25% carbopol 934 p and Formulation SGE10 containing 45% of sterculia gum and 25% ethyl cellulose has released minimum 10.91 % to 13.04 % in the initial 5h and sustained the drug release up to 24 h and at the end of study released 75% to 79.99%. Formulations with 4% rat cecal content at the end of 24 h study drug released is 90.44% to 95.33% indicating higher amount of drug release is due to enzymatic break down of sterculia gum in the matrix tablet. Hence the above results conclude that the formulation SGC5 and SGE10 are potential in targeting the drug to colon to treat irritable bowel disease.DOI: http://dx.doi.org/10.3329/icpj.v1i11.12064 International Current Pharmaceutical Journal 2012, 1(11): 376-383


Author(s):  
Kukkadapu Pavan Kumar ◽  
Katta Sunand ◽  
Nerella Mounika ◽  
Mohammed Abdul Samad ◽  
A. Madhu Babu ◽  
...  

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.


Author(s):  
Gurram Lakshmana murthy ◽  
Vasia Tamreen ◽  
Chandrika C. ◽  
Shazia Iryn ◽  
Suchitra M ◽  
...  

The main of the research work to develop sustained release floating matrix tablets of ATZ, which were designed to extend the gastric residence time and prolong the drug release after oral administration. Different grades of polymers such as EC and HPMC K100M were used in order to get the desired floating and sustained release profile over prolonged period of time. All the formulations extended the drug release up to 24 hours and more and the formulations were optimized for the desired release profiles. The release and floating property was depends on the polymer type and polymer proportion. The formulation prepared with Ethyl cellulose and HPMC K100M has more floating time than the formulation prepared with the Ethyl cellulose alone. The FTIR study shows that there is no drug-polymer interaction. This study gives the preliminary idea about the development of the floating drug delivery systems of Atazanavir without the use of gas generating agent.


2019 ◽  
Vol 9 (4-s) ◽  
pp. 363-369
Author(s):  
SANJAY KUMAR GUPTA ◽  
Sradhanjali Patra ◽  
Syed Adnan Akber

The aim of this work was to develop a mucoadhesive buccal tablet for the buccal delivery of the alendronate via buccal mucosa. Buccal tablets of alendronate are designed to release drug at mucosal site for extended period of time without wash out of drug by saliva. Alendronate sodium is a bisphosphonates which has antiresorptive effect which is implicated in the prophylaxis and treatment of osteoporosis. Sodium alginate, ethyl cellulose and carbopol were selected as mucoadhesive polymers on the basis of their matrix forming properties. The objective of the study is to improve the bioavailability of alendronate buccal tablets. Extensive literature survey was done for the collection of theoretical and technical data. The methodology part includes the explanation of implemented methods in the present study. In present study, an attempt was made to design mucoadhesive buccal tablets containing alendronate, sodium alginate, ethyl cellulose and carbopol using as polymers. The tablets were prepared by direct compression method. The formulations were evaluated for hardness, thickness, friability, weight variation, drug content estimation, surface pH determination, swelling index, in vitro drug release. In vitro bioadhesive strength & in vitro release studies showed that formulation F11 showed optimum bioadhesive & exhibited optimum drug release 97.6% in 7hr. Kinetics results reveals that the F11 formulation follows zero order kinetics as correlation coefficient (r2) values are higher than that of first- order release kinetics.Optimized formula F11 show drug is released by non-Fickian diffusion mechanism. The stability studies of formulation F11 prepared mucoadhesive buccal tablets of alendronate were stable. Overall evaluations of the mucoadhesive of tablets show good mucoadhesive properties.


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