scholarly journals Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Ripunjoy Bordoloi ◽  
Abdul Baquee Ahmed ◽  
Kunal Bhattacharya
Keyword(s):  
Dosage Form ◽  
Gamma Scintigraphy ◽  
Pharmacokinetic Parameters ◽  
Scanning Electron Micrographs ◽  
Drug Bioavailability ◽  
Duration Of Action ◽  
Study Objective ◽  
Release Study ◽  
Gastro Retentive

Abstract Background The current study was carried out to evaluate the possible application of Musa balbisiana starch in formulation of mucoadhesive microsphere for oral delivery of gliclazide (GLZ). The study objective was to improve the oral bioavailability along with prolongation of its duration of action for a better glycaemic control. Ionic gelation technique was employed in formulating the dosage form. Optimization of the batches was carried out by response surface methodology using 32 full factorial designs. The microsphere prepared was characterized for several parameters along with its in vitro release study. The gastrointestinal transit of the optimized batch of prepared microspheres after oral administration was studied in rabbits by using the gamma scintigraphy technique utilizing 99mTc as the labelling agent in the presence of stannous chloride. Also, the optimized batch was studied for its pharmacokinetic parameters. Moreover, the antidiabetic efficacy of the prepared microsphere was evaluated in rats by using the streptozotocin (STZ)-induced diabetic model. Results The factorial design experiment resulted in an optimum formulation coded as F8. The compatible nature of the drug and excipient was revealed from FTIR, DSC and IST studies. The scanning electron micrographs also showed the occurrence of spherical microspheres having a smooth surface. The in vitro release study provided an evidence of an initial burst effect that was followed by a prolong release phase. The pharmacokinetic parameters justified the ability of the prepared dosage form in sustaining the drug release with a 2.7-fold enhancement in drug bioavailability. The images obtained during the gamma scintigraphy study suggested the gastro-retentive nature of the dosage form with the gastro-retentive ability for more than 4 h. Also, the pharmacodynamics study carried out in diabetic rat model confirmed about the better efficacy of the dosage form in lowering the elevated blood glucose level. Conclusion The overall study data provide valuable information about the potential of this banana starch in formulation of a mucoadhesive dosage form that can be used for enhancement of bioavailability of drug-like gliclazide which in turn can provide a beneficial effect in the management of diabetes.

FORMULATION, OPTIMIZATION AND EVALUATION OF MOXIFLOXACIN HYDROCHLORIDE GASTRO RETENTIVE TABLETS

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (01) ◽  
pp. 79-84
Author(s):  
Raghavendra K. Gunda ◽  
◽  
A. Vijayalakshmi ◽  
K. Masilamani ◽  
◽  
...  
Keyword(s):  
Fickian Diffusion ◽  
In Vivo Studies ◽  
Pharmacokinetic Parameters ◽  
Wet Granulation ◽  
Statistical Parameters ◽  
Compression Technique ◽  
Ich Guidelines ◽  
Gastro Retentive

The objective of the current study was to develop gastro retentive formulation of moxifloxacin. HCl using various drug release modifiers and performing in vitro and in in vivo evaluations. Moxifloxacin is a novel synthetic fluoro quinolone antibacterial agent. Floating, muco adhesive tablets of moxifloxacin. HCl were prepared using variable amounts of HPMCK100M, Lannea coromandelica gum by direct compression technique and wet granulation technique, respectively. Formulations were developed, optimized and checked for pharmacopoeial tests. Results show that all the batches lie within the standard limits. Dissolution parameters of all formulations were sy=ubjected to kinetic fitting and various statistical parameters were determined. Formulation (FS5 ) containing 50 mg of HPMCK100M and 50 mg of LCG, is the best formulation showing similarity f2 =71.734, f1 = 4.271 with the marketed product (Avelox). It follows Higuchi's kinetics, non-fickian diffusion first order kinetics(n=0.717). In vivo studies were performed for the FS5 with 6 healthy rabbits and pharmacokinetic parameters were determined, compared with Avelox and it was found that FS5 produced similar results. Stability studies were performed for FS5 as per ICH guidelines. Results were found to be satisfactory. FS5 is expected to improve patient compliance by means of providing good clinical outcome

scholarly journals Gastro-retentive floating beads of curcumin β-cyclodextrin complex to treat stomach tumors

2011 ◽  
Vol 1 (1) ◽  
pp. 12 ◽  
Author(s):  
Shishu Goindi ◽  
Kamalpreet Mann ◽  
Nidhi Aggarwal
Keyword(s):  
Sustained Release ◽  
Dosage Form ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Solubility ◽  
Pharmacokinetic Studies ◽  
Cyclodextrin Complex ◽  
Enhanced Solubility ◽  
Tumor Studies ◽  
Gastro Retentive

The aim of present study was to develop a multi-unit gastro-retentive floating dosage form of curcumin with targeted and sustained release characteristics. Although, protective effect of curcumin against inflammation and cancer is well documented, the clinical potential is underutilized owing to the physicochemical properties of the molecule which lead to poor oral bioavailability. Aqueous solubility of curcumin was enhanced by complex formation with β-cyclodextrin (β-CD). This complex with enhanced solubility profile was further used to prepare multiple unit floating beads. Floating beads of curcumin β-cyclodextrin complex (FBCC) were prepared by dripping a mixture of sodium alginate and hydroxypropyl methylcellulose solution into calcium chloride solution acidified with acetic acid. FBCC were evaluated for percent drug entrapment, diameter, surface topography, buoyancy,<em> in vitro</em> release and pharmacodynamic activity against Benzo(a) pyrene [B(a)P] induced forestomach papillomas in albino female mice (Balb/C strain). The investigation revealed that floating beads possessed optimum formulation characteristics. The drug release from FBCC was fickian and sufficiently sustained for 12 h. Results of antitumor studies against B(a)P induced neoplasia of forestomach suggests that the tumor incidence significantly reduced (50%) using FBCC where as pure curcumin resulted in only 25% reduction. A multi-unit floating dosage form of curcumin β-CD complex possessing sustained release characteristics was developed for targeting gastric tumors. Results of i<em>n vitro</em> studies and anti-tumor studies in animals suggest that FBCC can be safely and effectively used to treat neoplasia of stomach. However, these preliminary investigations warrant further pharmacokinetic studies and clinical evaluation in humans

scholarly journals Comparative analysis of pharmacokinetic parameters of transdermal and intramuscular administration of Galavit®

2021 ◽  
Vol 23 (2) ◽  
pp. 114-121
Author(s):  
E. G. Kuznetsova ◽  
O. M. Kuryleva ◽  
L. A. Salomatina ◽  
S. V. Kursakov ◽  
Z. Z. Gonikova ◽  
...  
Keyword(s):  
Dosage Form ◽  
Animal Experiments ◽  
The Body ◽  
Intramuscular Administration ◽  
Pharmacokinetic Parameters ◽  
Therapeutic System ◽  
Transdermal Administration ◽  
Maximum Serum ◽  
Transdermal Therapeutic System

Introduction. Immunomodulator Galavit® is a promising domestic drug for the prevention and treatment of various infectious diseases. Earlier, the authors have developed and investigated in vitro its new dosage form – transdermal therapeutic system (TTS). Positive results from experiments made it possible to proceed to the study of the pharmacokinetic parameters of Galavit® TTS in animals.Objective: to compare the pharmacokinetic parameters of intramuscular and transdermal administration of immunomodulator Galavit® in animal experiments.Materials and methods. Sodium aminodihydrophthalazinedione was used as a substance in the form of a powder to prepare a solution for intramuscular administration of 100 mg (trade name Galavit®, manufacturer SELVIM LLC). The pharmacokinetics of transdermal and intramuscular injections were studied in male Chinchilla rabbits weighing 4.5–5.0 kg. Serum sodium aminodihydrophthalazinedione concentrations in animals were determined by highperformance liquid chromatography using a specially developed technique.Results. In contrast to the injection method, a prolonged and uniform inflow of the drug substance (MP) into the body is observed for percutaneous administration of sodium aminodihydrophthalazinedione. The maximum serum Galavit® concentration for a 40 mg dose (0.172 ± 0.054 μg/mL) and for a 80 mg dose (1.16 ± 0.22 μg/mL) remained at a constant level for 9 and 8 hours, respectively. The relative bioavailability of the Galavit® transdermal therapeutic system was 0.65 and 1.06 for the same doses.Conclusion. Application of Galavit® 80 mg transdermal therapeutic system provides bioavailability that is similar to the intramuscular administration of this drug at the same dose. At the same time, its maximum serum concentration significantly decreases and the retention time of Galavit® in the body increases by more than 10 times, which can contribute to prolongation of the drug effect. Due to the current growing interest in the use of immunomodulator Galavit® for coronavirus infection COVID-19, the development and study of a new dosage form is a promising task

scholarly journals FORMULATION DEVELOPMENT OF COLON TARGETED MESALAMINE PELLETS: IN VITRO-IN VIVO RELEASE STUDY

2019 ◽  
pp. 125-132 ◽  
Author(s):  
JAGAN BAHEKAR ◽  
SHAILESH WADHER
Keyword(s):  
In Vitro Release ◽  
Pharmacokinetic Parameters ◽  
High Dose ◽  
Aminosalicylic Acid ◽  
Formulation Development ◽  
In Vivo Release ◽  
Release Study ◽  
Vitro Release

Objective: This study was intended to investigate the potential of the colon specificity approach comprising of use of pH-sensitive and time-dependent polymers in combination for precise colonic release of Mesalamine or 5-Aminosalicylic acid (5-ASA). Methods: The extrusion and spheronization method, preferably employed in industry for allowing high dose capacity to formulate, was used to prepare drug pellets. The Wurster coating technique used for aqueous coatings of Eudragit NE 40D as an inner coat and Eudragit FS30D as outer coat. The changing pH media used for in vitro release study of optimization batches for both the coating levels. A scanning electron microscope (SEM) was used to evaluate coating thickness and surface morphology. Results: The pharmacokinetic parameters of formulation evaluated by in vivo study in rabbits revealed that the uncoated formulation released the drug too early in the gastrointestinal tract (GIT) with a mean Cmax of 1205.28±0.37 µg/ml at 2 h after administration, whereas desired lag time was achieved in case of coated pellets exhibiting mean Cmax 465.94±0.21 µg/ml and tmax of 8 h. Conclusion: The in vitro and in vivo release study divulge the reliability of approach involving the use of pH sensitivity and time dependency of polymer for drug release in a single formulation for the treatment of colonic diseases. Hence, the present study provides constructive results for colon targeting of 5-ASA pellets with industrially feasible processes.

scholarly journals Preparation and characterization of simvastatin/DMβCD complex and its pharmacokinetics in rats

2018 ◽  
Vol 68 (2) ◽  
pp. 145-157
Author(s):  
Fugen Gu ◽  
Jia Ning ◽  
Huimin Fan ◽  
Chunzhi Wu ◽  
Yi Wang
Keyword(s):  
Dissolution Rate ◽  
Free Drug ◽  
Pharmacokinetic Parameters ◽  
Complexing Agent ◽  
Phase Solubility ◽  
Pharmacokinetic Studies ◽  
Maximum Plasma ◽  
Drug Bioavailability ◽  
Scanning Calorimetry

Abstract Simvastatin is poorly bioavailable because it is practically insoluble in water and shows dissolution rate-limited absorption. Solubilizing effects of several β-cyclodextrin (βCD) derivatives such as HPβCD, SBEβCD and DMβCD on simvastatin in aqueous solution were investigated using the phase solubility technique. The solubility diagram of simvastatin with each βCD derivative could be classified as AL-type, indicating soluble complex formation of 1:1 stoichiometry. Among the above βCD derivatives DMβCD was found to be the ideal complexing agent for improving drug solubility. The simvastatin complex with DMβCD was prepared using the co-evaporation method and was then characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR) and in vitro dissolution. Dissolution and pharmacokinetic studies indicated that the simvastatin/DMβCD complex exhibited an increased dissolution rate, rapid absorption, and improved bioavailability in rats compared to free drug. Maximum plasma concentration (cmax) and the time to reach it (tmax) were 21.86 μg mL−1 and 1.4 h for the drug complex, 8.25 μg mL−1 and 3.0 h for free drug, respectively. Main pharmacokinetic parameters such as tmax, cmax were significantly different (p < 0.01) between the simvastatin complex and free drug. Bioavailability of the simvastatin complex relative to free drug was up to 167.0 %.

Erythrocytes as Carriers of Indinavir: Preparation, Characterization, In vitro and In vivo Pharmacokinetic Evaluation in Rats

2017 ◽  
Vol 10 (1) ◽  
pp. 3573-3581
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Shiva Krishna A ◽  
Ramesh M ◽  
Suresh G ◽  
Jyothi Sri S
Keyword(s):  
Sustained Release ◽  
Dosage Form ◽  
Antiretroviral Drugs ◽  
Pharmacokinetic Parameters ◽  
Intravenous Route ◽  
Rat Erythrocytes ◽  
Human Immuno Deficiency Virus ◽  
Equal Dose

Indinavir is a protease inhibitor of the human immuno-deficiency virus. Indinavir is commercially available as capsule of 200 mg and 400 mg. Adult dose is 800 mg every 8 h. i.e., 2400 mg per day is equivalent to 6 capsules per day. No other dosage form is available in the market. Sustained release dosage form of indinavir can produce maximum therapeutic effect with minimum side effects and achieve better patient compliance. Various carriers have  been used for the drug targeting among which cellular carriers such as erythrocytes offer greater potential advantages than other system.  The drug is never free in circulation thus reducing toxicity and the drug half-life in circulation increases thus kinetic patterns. Antiretroviral-loaded erythrocytes offer a promising therapy against HIV owing to their potential to deliver this kind of drugs to macrophages and reticulo-endothelial (RES) tissues. The aim of the present investigation was to develop and optimize antiretroviral indinavir encapsulated in rat erythrocytes. In this study, the encapsulation of indinavir by rat erythrocytes prepared and compared with indinavir dissolved in normal saline. The prepared formulations were administered to rats by intravenous route and plasma samples was analysed by LC-MS/MS technique. The pharmacokinetic parameters were calculated using Win-nonlin software. The prepared indinavir loaded erythrocytes showed enhanced bioavailability in equal dose due to higher extent of absorption owing to its retention in erythrocytes and releasing the drug slowly. Indinavir demonstrated a sustained release from loaded erythrocytes over a period of 36 h, which suggests a potential use of the erythrocyte as a slow systemic release system for antiretroviral drugs.

scholarly journals Effect of physicochemical properties on the pharmacokinetic parameters of the new representative of benzothiazinones antituberculosis drug macozinonе

2020 ◽  
Vol 92 (12) ◽  
pp. 165-171
Author(s):  
A. L. Khokhlov ◽  
A. O. Mariandyshev ◽  
V. S. Shcherbakova ◽  
I. V. Ozerova ◽  
Yu. G. Kazaishvili ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Dosage Form ◽  
Empty Stomach ◽  
Acetate Buffer Solution ◽  
Reverse Direction ◽  
Pharmacokinetic Parameters ◽  
Biorelevant Media ◽  
Treatment Regimens

Introduction.Tuberculosis (TB) is one of the top ten causes of death worldwide. Improvement of the treatment options via development of new drugs and treatment regimens that would be more convenient for patients is one of key options of improving the effecacy of the TB prevention and careis. Since the creation of new treatment regimens by minimizing the number of the drugs used and reducing the duration of treatment is the most promising and correct direction, macozinone, a new candidate of the benzothiazinone series, can become the basis for development of new chemotherapy regimens for drug-resistant forms of TB including the combination of macozinone with the most effective modern anti-TB drugs. Aim.Comparative evaluation of the pharmacokinetic properties of macozinone capsules 80 mg and the new dosage form a dispersible tablet for preparation of oral solution. Materials and methods.Solubility of the substance macozinone in biorelevant media in vitro, permeability of macozinone in the test Caco-2 in vitro, as well as pharmacokinetics of macozinone in dogs in vivo were evaluated. Results.The solubility assessment in biorelevant media showed that the average limit of macozinone substance dissolution in the pH 5.0 acetate buffer solution was from 6 to 9 mg/l, in FaSSIF medium (fasted) from 2.5 to 4 mg/l, and in FeSSIF medium (after meals) from 16.8 to 29 mg/l. It is established that the cell permeability of the pharmaceutical substance macozinone in the CACO-2 test system is on average 2.510-6cm/s in the forward direction from the apical to basolateral cell membrane, and 1.510-6cm/s in the reverse direction, which corresponds to low permeability. The main pharmacokinetic parameters of macozinone dispersable tablets 160 mg, after dosing with food and on an empty stomach, as well as capsules 80 mg, when administered on an empty stomach in vivo studies in dogs are presented. Discussion.The specific physicochemical properties of macozinone, the problems of developing the new dosage form, as well as ways of solving some of them are presented. Conclusion.In the process of new dosage forms development, the existing chemical properties of the macozinone substance should be considered. One of the promising ways of increasing bioavailability and, consiquently, efficacy is development a fundamentally new drug form with modified release within the absorption window.

Gastroretentive Microspheres: An Innovative Approach for Prolonging Gastric Residence

2019 ◽  
Vol 9 (01) ◽  
pp. 01-09
Author(s):  
Satyajit Panda ◽  
K Priyanka ◽  
R Varaprasad ◽  
Snigdha Pattnaik
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Dosage Form ◽  
Oral Drug Delivery ◽  
Extended Period ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Gastro Retentive

Gastro-retentive drug delivery systems (GRDDS) like gastro-retentive microspheres have gained immense popularity in the field of oral drug delivery. It is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. Different innovative approaches like magnetic field assisted gastro-retention, swelling systems, mucoadhesion techniques, floating systems with or without effervescence are being applied to fabricate gastroretentive microspheres. Apart from in-vitro characterization, successful gastro-retentive microspheres development demands well designed in-vivo study to establish enhanced gastro-retention and prolonged drug release. Gama scintigraphy and MRI are popular techniques to evaluate in-vivo gastric residence time. However, checking of their overall in-vivo efficacy still remains a major challenge for this kind of dosage form, especially in small animals like mice or rat. Reported in-vivo studies with beagle dogs, rabbits, and human subjects are only a handful in spite of a large number of encouraging in-vitro results. In spite of the many advantages, high subject variations in gastrointestinal physiological condition, effect of food, and variable rate of gastric emptying time are the challenges that limit the availability of gastro-retentive microspheres in the market.

scholarly journals Development, Characterization and bioavailability enhancement of oral floating sustained release beads containing Indomethacin

2018 ◽  
Vol 6 (04) ◽  
pp. 48-54
Author(s):  
Rajesh Kumar Sharma ◽  
Naresh Kalra ◽  
Jayesh Dwivedi ◽  
G. Jeyabalan ◽  
Gurpreet Singh
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Drug Bioavailability ◽  
Bioavailability Enhancement ◽  
In Vitro Drug Release ◽  
Inflammatory Agent ◽  
Drug Entrapment Efficiency ◽  
Uv Visible ◽  
Release Study

The purpose of this research was to prepare and evaluate floating gastroretentive beads of Indomethacin an Non-steroidal anti-inflammatory agent for increased drug bioavailability. Floating beads were prepared by dripping Method using different polymers in varying ratios. The formulations were optimized on the basis of floating ability and in-vitro drug release. The floating beads were evaluated for micromeritic properties, entrapment efficiency, as well as in-vitro buoyancy study and drug release. Indomethacin was estimated in the formulation by using UV/Visible spectrophotometer (Shimazdu UV-1800) at 321 nm. The floating beads shows drug entrapment efficiency, buoyancy and yield the 72.55%, 60.2 and 74.3%respectively. In vitro drug release study confirms formulation I4 was the best formulation as it releases 99.28 % of Indomethacin at the end of 24 hrs in controlled manner.

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