scholarly journals Formulation and Characterization of Isradipine Nanoparticle for Dissolution Enhancement

2021 ◽  
Vol 30 (1) ◽  
pp. 218-225
Author(s):  
Rawaa M. Hussien ◽  
Mowafaq M. Ghareeb
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Drug Bioavailability ◽  
Particle Size Reduction ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Isradipine belong to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is  used in the treatment of hypertension, angina pectoris, in addition to Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, therefore, oral bio-availability will be approximately15 to 24 %.    The aim of this study was to formulate and optimize a stable  nanoparticles of a highly hydrophobic drug, isradipine by anti-solvent microprecipitation Method to achieve the higher in vitro dissolution rate, so that it will be absorbed by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism  and improve drug bioavailability.   Twenty one formulas of Isradipine nanoparticles were prepared by antisolvent precipitation method utilizing one of these polymers (Poloxamer 188, PVP-k30, HPMC E5, PVA, Poloxamer 407, and Soluplus) at different drugs: polymer ratios. The polymer type, the drug to polymer ratio, ultrasonication power and the effect of addition of co-stabilizer on the particle size, and polydispersity index (PDI)  were investigated.   Among all the prepared nanoparticles formulas, formula (F9) which contain Soluplus as a stabilizer at polymer: drug ratio of (1:0.75) and solvent: antisolvent ratio of (1:9) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 10 times than that of the pure drug. The investigations of the drug–excipients compatibility studies by FTIR and DSC, crystalline state by P-XRD, surface morphology by SEM were done. Moreover, the analysis by DSC and SEM of the nanoparticles of the selected formula (F12) indicate a reduction in the crystallinity and amorphization of the drug. It can be concluded that the dissolution rate of Isradipine was significantly increased through particle size reduction to nanosize.            

scholarly journals Optimization of ThermoreversibleIn SituNasal Gel of Timolol Maleate

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Swati Jagdale ◽  
Nirupama Shewale ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Ex Vivo ◽  
Nasal Delivery ◽  
Poloxamer 407 ◽  
Timolol Maleate ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Nasal route had shown better systemic bioavailability due to its large surface area, porous endothelial membrane, high total blood flow, and avoidance of first-pass metabolism. Timolol maleate is a beta blocker used primarily in the treatment of hypertension. Drug undergoes extensive hepatic first-pass metabolism (80%). The drug has half-life of 4 hrs. Oral bioavailability of timolol maleate is 61%. The aim of the present study was to optimize controlled releasein situnasal delivery for timolol maleate. HPMC and Poloxamer 407 were selected as polymer in formulation of thermoreversiblein situnasal gel. Optimization was carried out using 32factorial design. It was observed that formulations f1 and f4 revealed the highest % drug release, that is, 93.57% and 91.66%, respectively. Factorial design study indicated that the drug release and viscosity were most significant dependent factors.Ex vivodiffusion study through nasal mucosa indicated 67.26 ± 2.10% and 61.07 ± 2.49% drug release for f1 and f4 formulations. f1 was the optimized batch. This batch thus can act as a potential nasal delivery with enhanced bioavailability for the drug.

scholarly journals Gastroretentive drug delivery system of a lipid lowering agent

2013 ◽  
Vol 2 (9) ◽  
pp. 152-155
Author(s):  
D. Krishnarajan ◽  
N. Senthil Kumar ◽  
Rajesh Yadav
Keyword(s):  
Guar Gum ◽  
Lipid Lowering ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Natural Polymers ◽  
First Pass Metabolism ◽  
First Pass ◽  
Mucoadhesive Tablets ◽  
Pass Metabolism

The objective of this study was to develop mucoadhesive tablets of Simvastatin using natural polymers. Simvastatin has short biological half-life and high first pass metabolism hence which was designed to increase the gastric residence time which prolong the drug release. The tablets were prepared by wet granulation technique using Carbopol-934, guar gum, xanthine gum and chitosin as polymers. Formulations were evaluated for different parameters like hardness, friability, uniformity of weight, swelling characteristics, in vitro dissolution and kinetic studies. The dissolution was carried out for 12 hours in which the formulation with guar gum has shown highest dissolution release profile (F9). Thus the present study concludes that mucoadhesive tablets of simvastatin can be a good way to pass the extensive hepatic first pass metabolism and to improve the bioavailability of simvastatin.DOI: http://dx.doi.org/10.3329/icpj.v2i9.16077 International Current Pharmaceutical Journal, August 2013, 2(9): 152-155

Effect of various Polymers on Drug Release from Mucoadhesive Tablets of Cefixime Trihydrate

2021 ◽  
pp. 167-173
Author(s):  
Kumara Swamy Samanthula ◽  
Agaiah Goud Bairi ◽  
Shobha Rani Satla ◽  
Mahendra Kumar CB
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
First Pass Metabolism ◽  
First Pass ◽  
Mucoadhesive Tablets ◽  
Pass Metabolism

Cefixime trihydrate (CT) is a third-generation cephalosporin antibiotic and is used in the management of various infections caused by Gram +ve as well as Gram – ve bacteria. It has a plasma half-life of 3-4 h. It has poor oral bioavailability due to hepatic first pass metabolism. Hence, an attempt was made to develop CT mucoadhesive tablets for buccal delivery to avoid first-pass metabolism and improved oral delivery. CT mucoadhesive tablets developed using HPMC K4M, Na-CMC, guar gum and chitosan as rate controlling polymers and mucoadhesive agent, respectively and compressed by direct compression method. The prepared CT mucoadhesive tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, assay, mucoadhesive strength and in vitro release. From the results, all the evaluated parameters were within the pharmacopoeial limits. The in-vitro dissolution studies indicated that the CTmucoadhesive tablets formulation (F2) showed 99.7±1.4 % of drug release after 8 h and chose as the optimized formulation. The kinetic models suggest that the drug release follows Higuchi’s kinetics and tablets drug release was controlled by a diffusion mechanism.

scholarly journals Critical Review of Lipid-Based Nanoparticles as Carriers of Neuroprotective Drugs and Extracts

Nanomaterials ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 563
Author(s):  
Filipe Fernandes ◽  
Mónica Dias-Teixeira ◽  
Cristina Delerue-Matos ◽  
Clara Grosso
Keyword(s):  
Brain Parenchyma ◽  
Drug Bioavailability ◽  
Onset Of Action ◽  
Routes Of Administration ◽  
Neuroprotective Drugs ◽  
First Pass Metabolism ◽  
First Pass ◽  
The Central Nervous System ◽  
The Brain ◽  
Pass Metabolism

The biggest obstacle to the treatment of diseases that affect the central nervous system (CNS) is the passage of drugs across the blood-brain barrier (BBB), a physical barrier that regulates the entry of substances into the brain and ensures the homeostasis of the CNS. This review summarizes current research on lipid-based nanoparticles for the nanoencapsulation of neuroprotective compounds. A survey of studies on nanoemulsions (NEs), nanoliposomes/nanophytosomes and solid lipid nanoparticles (SLNs)/nanostructured lipid carriers (NLCs) was carried out and is discussed herein, with particular emphasis upon their unique characteristics, the most important parameters influencing the formulation of each one, and examples of neuroprotective compounds/extracts nanoencapsulated using these nanoparticles. Gastrointestinal absorption is also discussed, as it may pose some obstacles for the absorption of free and nanoencapsulated neuroprotective compounds into the bloodstream, consequently hampering drug concentration in the brain. The transport mechanisms through which compounds or nanoparticles may cross BBB into the brain parenchyma, and the potential to increase drug bioavailability, are also discussed. Additionally, factors contributing to BBB disruption and neurodegeneration are described. Finally, the advantages of, and obstacles to, conventional and unconventional routes of administration to deliver nanoencapsulated neuroprotective drugs to the brain are also discussed, taking into account the avoidance of first-pass metabolism, onset of action, ability to bypass the BBB and concentration of the drug in the brain.

scholarly journals In Vitro Evaluation of Different Approaches and Dissolution Enhancement Technique of Poorly Water-Soluble Drug Ibuprofen

2016 ◽  
Vol 64 (2) ◽  
pp. 169-175
Author(s):  
ASM Monjur Al Hossain ◽  
Konika Rani Dutta ◽  
Md Lokman Hossain
Keyword(s):  
Dissolution Rate ◽  
Methyl Cellulose ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Dissolution Profile ◽  
Physical Mixing ◽  
Pregelatinized Starch

Ibuprofen Solid Dispersion (SD) was prepared by simple Physical Mixing (PM) and Kneading Method (KM). In these two cases, four polymers named poloxamer 407, sodium carboxy methyl cellulose, croscarmellose sodium and pregelatinized starch were used to enhance the dissolution profile of Ibuprofen. In both methods, the ratio of drug and carrier were 1:1, 1:2, 1:3 of which the ratio of 1:3 in KM gave comparatively better result than PM method. In vitro dissolution study was performed in distilled water in 50 rpm and at 37 ± 0.5°C. In case of pure Ibuprofen, dissolution rate was only 26% after 60 minutes (mins) of dissolution. While in KM, Ibuprofen pregelatinized starch formulation at 1:3 ratio showed better dissolution rate. After 60 mins, dissolution rate of Ibuprofen was 72%. The SD formulations of Ibuprofen-pregelatinized starch and Ibuprofen-Na-CMC of physical mixing and kneading techniques (1:3 ratio) were characterized by Fourier Transform Infrared Spectroscopy (FTIR). Dhaka Univ. J. Sci. 64(2): 169-175, 2016 (July)

scholarly journals Design, Development and Characterization of Nifedipine Microspheres

2019 ◽  
Vol 9 (3) ◽  
pp. 138-146
Author(s):  
Arun Kumar Chalamalasetty ◽  
Boggula Narender ◽  
Bolledla Nirosha ◽  
Bakshi Vasudha ◽  
Peddapalli Himabindu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Oral Bioavailability ◽  
Ethyl Cellulose ◽  
Hydroxypropyl Methylcellulose ◽  
Prolonged Release ◽  
Design Development ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Back ground: Nifedipine is a calcium channel blocker and is used in treatment of angina of angina pectoris and hypertension. Nifedipine readily and almost completely absorbed from GIT, but undergoes first pass metabolism, resulting in low oral bioavailability is about 50%. Aim: The aim of the present study was to prepare and evaluate the microspheres of nifedipine with a goal of improving the bioavailability and giving a prolonged release of drug. Method: Emulsification (o/w) solvent evaporation method was employed in the preparation of nifedipine microparticles using ethyl cellulose and combination of ethyl cellulose and hydroxypropyl methylcellulose as the polymers. Results: FT-IR spectra of physical mixture showed no significant shifting of the peaks therefore it reveals that the drug is compatible with the polymer used. The percentage yield obtained in all the formulations was good and in the range of 59.25-94.44%. Among all the formulations, formulation with combination of ethyl cellulose and hydroxypropyl methylcellulose polymers M9 showed high amount of drug release i.e. (91.23%) in 12hrs. Drug release from microspheres with small mean particle size was faster than those with large mesh particle size and followed Higuchi model of kinetics. Conclusion: The obtained results could be used as essence to develop microspheres, which bypasses first-pass metabolism and results in the improvement of bioavailability. Hence, the present study has been a satisfactory attempt to formulate microspheres of nifedipine, with a view of improving its oral bioavailability and giving a prolonged release of drug. Keywords: Microspheres, nifedipine, hydroxypropyl methylcellulose E5, ethyl cellulose.

scholarly journals Formulation and evaluation of fast dissolving tablet of albendazole

2012 ◽  
Vol 1 (10) ◽  
pp. 311-316 ◽  
Author(s):  
Devendra Revanand Rane ◽  
Hemant Narhar Gulve ◽  
Vikas Vasant Patil ◽  
Vinod Madhaorao Thakare ◽  
Vijay Raghunath Patil
Keyword(s):  
Dissolution Rate ◽  
Microcrystalline Cellulose ◽  
Broad Spectrum ◽  
Pharmaceutical Journal ◽  
Direct Compression ◽  
Onset Of Action ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Albendazole is broad spectrum anthelmintic use against many helminths. It is used for treatment of Threadworm, Hookworm, and Tapeworm. It has low bioavailability due to its first pass metabolism.  In the present work, fast dissolving tablet of Albendazole was design with a view to and provide a quick onset of action. The main objective of the study was to formulate fast dissolving tablets of Albendazole to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablets prepared by direct compression and using super disintegrants in different concentration and evaluated for the pre-compression parameters. The prepared tablets were evaluated for post compressional evaluation. Among all, the formulation F3 containing 5%w/w superdisintegrant Crospovidone and 20%w/w Microcrystalline Cellulose was considered to be best formulation, which release up to 99.097% in 40 min.DOI: http://dx.doi.org/10.3329/icpj.v1i10.11848 International Current Pharmaceutical Journal 2012, 1(10): 311-316 

Identification of a Cranberry Juice Product Capable of Inhibiting Enteric CYP3A-Mediated First-Pass Metabolism in Humans

Planta Medica ◽  
2008 ◽  
Vol 74 (03) ◽  
Author(s):  
N Ngo ◽  
Z Yan ◽  
TN Graf ◽  
DR Carrizosa ◽  
EC Dees ◽  
...  
Keyword(s):  
Cranberry Juice ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Formulation and Evaluation of Nanosuspension of Simvastatin

2015 ◽  
Vol 8 (2) ◽  
pp. 2858-2873
Author(s):  
Rupali L. Shid ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L Shid
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Factorial Design ◽  
Dissolution Rate ◽  
In Vitro Dissolution ◽  
Total Drug ◽  
23 Factorial Design ◽  
Rate Of Dissolution

Poor water solubility and slow dissolution rate are issues for the majority of upcoming and existing biologically active compounds. Simvastatin is poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of this study wasto increase the solubility and dissolution rate of simvastatin by the  preparation of nanosuspension by emulsification solvent diffusion method at laboratory scale. Prepared nanosus-pension was evaluated for its particle size and in vitro dissolution study and characterized by zeta potential,differential scanning calorimetry (DSC) and X-Ray diffractometry (XRD), motic digital microscopy, entrapment efficiency, total drug content, saturated solubility study and in vivo study. A 23 factorial design was employed to study the effect of independent variables, amount of SLS (X1), amount of PVPK-30 (X2) and poloxamer-188 (X3) and dependent variables are total drug content and polydispersity Index. The obtained results showed that particle size (nm) and rate of dissolution has been improved when nanosuspension prepared with the higherconcentration of PVPK-30 with the higher concentration of PVP K-30 and Poloxamer-188 and lower concentration of SLS. The particle size and zeta potential of optimized formulation was found to be 258.3 nm and 23.43. The rate of dissolution of the optimized nanosuspension was enhanced (90% in 60min), relative to plain simvastatin  (21% in 60 min), mainly due to the formation of nanosized particles. These results indicate the suitability of 23 factorial  design for preparation of simvastatin loaded nano-suspension significantly improved in vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect. In vivo study shows increase in bioavailability in nanosuspension formulation than the plain simvastatin drug.

Development, Characterization and Optimization of Mucoadhesive Tablet for Buccal Delivery of Domperidone

2019 ◽  
Vol 9 (1) ◽  
pp. 37-49
Author(s):  
Jagdale Sachin ◽  
Panbude Aishwarya ◽  
Navasare Priya
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Research Work ◽  
Wet Granulation ◽  
Buccal Delivery ◽  
Scanning Calorimetry ◽  
Mucoadhesive Polymers ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Background and Objective: Upon oral administration domeperidone is rapidly absorbed, but subjected to the first pass effect which lowers systemic bioavailability to 15%. Mucoadhesive tablet can remain attached to buccal mucosa and becomes capable of bypassing hepatic first-pass metabolism to improve absorption directly into systemic circulation. The present research work was carried with an aim to develop, evaluate and optimize mucoadhesive tablet containing domperidone (DOME) for buccal delivery using different bio-adhesive polymeric combinations. </P><P> Methods: The buccal tablets were formulated by wet granulation method using isopropyl alcohol. The preliminary formulations were prepared using combinations of HPMC K4, HPMC K15, HPMC K100, HPMC E5 as mucoadhesive polymers. 32 full factorial design was applied to determine the effect of independent variables like concentration of mucoadhesive polymers (HPMC K15 and HPMC K100) over dependent variables like mucoadhesive properties (swelling index, bioadhesive strength and in vitro drug release). The prepared mucoadhesive tablets were evaluated for their tablet properties and mucoadhesive properties. The interactions between drug and polymers were studied by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). </P><P> Results: All formulations of factorial design showed satisfactory physicochemical, mechanical and bioadhesive characteristics. The formulation F9 exhibited maximum cumulative drug release, mucoadhesive strength and swelling index. Conclusion: The developed buccal tablet of domperidone might prove alternative to bypass the hepatic first pass metabolism and to avoid degradation which in turn may result in reducing the frequency of administration. Thus, mucoadhesive tablet of domeperidone may become viable alternative overcoming the side effects; achieving greater therapeutic effectiveness and improving the patient compliance.

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