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.

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.

Formulation and Characterization of Eplerenone Mucoadhesive Buccal Tablets

2021 ◽  
pp. 3097-3103
Author(s):  
Harini Amballa ◽  
Navaneetha Kaluva ◽  
Sree Giri Prasad Beri ◽  
Krishna Mohan Chinnala ◽  
Mayuri Konda
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Release System ◽  
First Pass Metabolism ◽  
First Pass ◽  
Buccal Tablets ◽  
Pass Metabolism

Mucoadhesive drug release system is a preferably unidirectional release system where mucosal epithelial exterior is enclosed by the mucus deposit that interacts with the bio-adhesive drug delivery system and swelling time of the buccal dosage form which is amplified by mucin molecules at the location of administration. Eplerenone is an Anti-hypertensive drug that undergoes hepatic first pass metabolism and shows 69% of bioavailability. In order to bypass the hepatic first pass metabolism the drug is designed to be delivered through buccal cavity to avoid the first pass metabolism. Eplerenone buccal tablets were formulated by using direct compression method with different polymers like HPMC K 100M, Carbopol 934P, Carbopol 974P, Xantham Gum, Eudragit L100 and NaCMC in various concentrations and compositions. Incompatibility complications were not observed from the FTIR spectrums. The formulated and prepared buccal solid dosage forms were evaluated for pre-compressions and post- compression parameters such as hardness, weight variation, thickness, friability, surface pH, swelling index, in-vitro dissolution studies, drug content uniformity, mucoadhesion strength and mucoadhesion time. Evaluation results of formulation F12 are proven to be the optimal formulation showing highest mucoadhesion time, mucoadhesion strength and in-vitro drug release for prolonged period of time about 8 hours. Eplerenone is best delivered through buccal drug delivery system to enhance its oral bioavailability and bypass the hepatic first pass metabolism.

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 FORMULATION, IN VITRO AND EX VIVO CHARACTERIZATION OF MUCOADHESIVE BUCCAL TABLETS FOR ANTIHYPERTENSIVE DRUG

2018 ◽  
Vol 11 (8) ◽  
pp. 402 ◽  
Author(s):  
Himabindu Peddapalli ◽  
Vasudha Bakshi ◽  
Narender Boggula
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Surface Ph ◽  
Ex Vivo Permeation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Permeation Studies ◽  
Buccal Tablets ◽  
Pass Metabolism

Objective: Olmesartan belongs to a class of angiotensin II receptor blockers. It is used in the treatment of hypertension. However, it undergoes extensive hepatic first-pass metabolism, resulting in low oral bioavailability is about 26%. The aim of this study was to prepare and evaluate the mucoadhesive buccal tablets of olmesartan with a goal to increase the bioavailability and improve the patient compliance.Methods: Mucoadhesive buccal tablets were prepared by a direct compression technique using mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC K4M), sodium carboxymethylcellulose (SCMC), and Carbopol 934P. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, ex vivo mucoadhesive strength, ex vivo mucoadhesive time, and ex vivo permeation studies. The release kinetics was calculated to determine the drug release mechanism. Results: The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets F2, F7, and F11 showed satisfactory drug release rates with the diffusion controlled mechanism. Optimized buccal tablets developed for olmesartan possess reasonable mucoadhesive strength, mucoadhesive time, and surface pH was in an acceptable salivary pH 6.76±0.28–6.89±0.34. The ex vivo permeation studies for optimized tablets were shown satisfactory drug permeation and could meet the target flux 0.991 mg h−1cm−2.Conclusion: The obtained results could be used as a platform to develop the buccal delivery of this drug, which bypasses the first-pass metabolism and results in the improvement of bioavailability. Hence, the present study concludes that the olmesartan could be delivered through the buccal route.

Development and Optimization of Mirabegron of Solid Lipid Nanoparticles as an Oral Delivery for Overactive Bladder

2021 ◽  
Vol 09 ◽  
Author(s):  
Prajakta Raut ◽  
Makarand Gambhire ◽  
Dhruvi Panchal ◽  
Vaishali Gambhire
Keyword(s):  
Overactive Bladder ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Lipid Nanoparticles ◽  
Correlation Spectroscopy ◽  
Solid Lipid ◽  
Peg 400 ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Background: Mirabegron (MBN), a β-3 adrenergic agent, is used in the treatment of overactive bladder. MBN has alow water solubility, high first-pass metabolism, and low bioavailability, consequently, having poor absorption in the gastrointestinal tract. Objective: The present study is intended at formulating Mirabegron-loaded solid lipid nanoparticles (MBN-SLN) coated with PEG-400 to bypass hepatic first-pass metabolism and to improve its oral bioavailability. Methods: MBN-SLNs were developed using glyceryl monostearate by pre-emulsion- ultrasonication method which was then optimized applying Box-Behnken Design. The optimized batch of MBN-SLN was selected for surface-modification with PEG-400 (MBN-PEG-SLN) and characterized by photon correlation spectroscopy, DSC, and XRD. Bioavailability studies were conducted in Wistar rats after oral administration of plain MBN dispersion, MBN-SLN, and MBN-PEG-SLN. Results: Stable MBN-SLNs and MBN-PEG-SLN of the optimized batch having a mean particle size of 162.7 nm and 149.9 nm; Zeta potential of -39.1 mV and -30.9 mV; %entrapment of 89.90% and 90.12%, respectively, were developed. The results of the in-vitro drug release studies demonstrated a significant slow release of MBN from MBN-SLN (69.38%) and MBN-PEG-SLN (61.33%) as compared to the dispersion of pure drug (92.10%). The relative bioavailability, as a result of the invivostudies, of MBN from MBN-PEG-SLN increased by 2-fold, based on the Cmax values, in comparison with the plain MBN dispersion. Conclusion: Thus, the study established that the oral bioavailability of MBN could be improved by the administration of MBN-PEG-SLN. The obtained results indicate SLNs as a potential drug delivery system for improving the bioavailability of poorly bioavailable drugs such as MBN by abating the first-pass metabolism.

scholarly journals Preclinical Pharmacokinetic Evaluation of β-Lapachone: Characteristics of Oral Bioavailability and First-Pass Metabolism in Rats

2015 ◽  
Vol 23 (3) ◽  
pp. 296-300 ◽  
Author(s):  
Iksoo Kim ◽  
Hyeongmin Kim ◽  
Jieun Ro ◽  
Kanghee Jo ◽  
Sandeep Karki ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism ◽  
Pharmacokinetic Evaluation

scholarly journals Solid lipid nanocarriers as alternative drug delivery system for improved oral delivery of drugs

2020 ◽  
Vol 10 (6-s) ◽  
pp. 168-172
Author(s):  
Gorre Thirupathi ◽  
Samanthula Kumara Swamy ◽  
Alli Ramesh
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Lipid Nanoparticles ◽  
Delivery Systems ◽  
Chemical Degradation ◽  
Solid Lipid ◽  
First Pass Metabolism ◽  
First Pass ◽  
Lipid Nanocarriers ◽  
Pass Metabolism

Oral bioavailability of drugs is mainly limited due to the poor aqueous solubility, enhanced chemical degradation, reduced permeation and/or first pass metabolism. Various novel delivery systems are developed for improved oral bioavailability of these drugs such as modified orals, buccal, transdermal and osmotic delivery systems. Colloidal carrier systems such as nanoparticles, lipid nanoparticles, nanoemulsions, microspheres, liposomes, resealed erythrocytes and transfersomes were also developed to enhance the oral delivery. Among these, solid lipid nanocarriers (SLNs) also gain much attention on the enhancement of oral bioavailability. SLNs are submicron sized nanoparticles and composed of solid lipid, surfactants and cosurfactants. The enhanced oral bioavailability of poorly soluble drugs from SLNs might be due to the reduced particle size, bypassed presystemic metabolism, and enhanced gastric mucosa permeability. Vast literature is available for the advantages, limitations, preparation methods, evaluation parameters and application of SLNs in different routes. This review mainly focused on list of drugs developed as SLNs and considered as an alternative approach to enhance the oral bioavailability based on pharmacokinetic as well as pharmacodyanmic parameters was discussed. Keywords: Oral bioavailability, solubility, first-pass metabolism, solid lipid nanoparticles, pharmacokinetics, pharmacodynamics.

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.

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