scholarly journals Applicability of Gum Karaya in the Preparation and in Vitro Evaluation of Losartan Potassium as Chronotherapeutic Drug Delivery System

2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Tensile Strength ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
Gum Karaya

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 

scholarly journals FORMULATION AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF LAFUTIDINE

2018 ◽  
Vol 8 (5) ◽  
pp. 393-399
Author(s):  
Ramdas T. Dolas ◽  
Shalindra Sharma ◽  
Madhuraj Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Active Agent ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Floating Tablets

The purpose of this research was to develop a novel gastroretentive drug delivery system based on wet granulation technique for sustained delivery of active agent. Quick GI transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to decreased efficacy of the administered dose and thus less patient compliance. Gastroretentive floating tablets, which was designed to provide the desired sustained and complete release of drug for prolonged period of time. Gastroretentive floating tablets of lafutidine were prepared by wet granulation technique using different concentrations of Gum Kondagagu, Gum olibanum and Locust bean Gum. The optimized formulation (LF14) exhibited 99.54% drug release in 12 hrs, while the buoyancy lag time was 33 sec. In-vitro drug release kinetics was found to follow both the Zero order and the possible mechanism of lafutidine release from the optimized formulation might be attributed to super case II transport mechanism. The Optimized formulation (LF14) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months. Keyword: Wet granulation, Floating lag Time, Gastroretentive, Lafutidine

scholarly journals Formulation and In Vitro Evaluation of Compressed Coated Tablets of Simvastatin for Pulsatile Drug Delivery

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Kumari P.V. Kamala ◽  
Mounica V. ◽  
Rao Y. Srinivasa
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Guar Gum ◽  
Lag Time ◽  
Blood Cholesterol ◽  
In Vitro Dissolution ◽  
Pulsatile Drug Delivery

Pulsatile drug delivery system is one type of drug delivery system, where the delivery device is capable of releasing drugs after a predetermined time-delay (i.e. lag time). This system has a peculiar mechanism of delivering the drug rapidly and completely after a "lag time," i.e., a period of "no drug release." These systems are beneficial for drugs having high first-pass effect drugs administered for diseases that follow chrono pharmacological behavior such as drugs having specific absorption sites in GIT, targeting to colon; and cases where nighttime dosing is required. The objective of the present study was to formulate and evaluate a press coated pulsatile drug delivery system of simvastatin in order to attain a time controlled release to lower the blood cholesterol level by releasing the drug with a distinct predetermined lag time of five hrs. Simvastatin is a water insoluble drug and its absorption is dissolution rate limited. The core formulations were composed of simvastatin and disintegrants like lycoat, SSG, ludiflash in different ratios and was coated with xanthan gum, guar gum, HPMC K4M, HPMC K15M as a release modifier. Press coated tablets were evaluated for hardness, friability, drug content, and in vitro drug release. Result of in vitro dissolution study of the prepared tablet suggested that, the release of drug from press coated tablets match with chrono-biological requirement of disease.

SELF-EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ACECLOFENAC: DESIGN & DEVELOPMENT USING QUALITY BY DESIGN (QBD) CONCEPT

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (06) ◽  
pp. 16-26
Author(s):  
V Suthar ◽  
◽  
M Gokel ◽  
S Butani ◽  
A Solanki
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Dosage Form ◽  
Quality By Design ◽  
Tween 80 ◽  
Current Approach ◽  
In Vitro Dissolution ◽  
Design Development

The aim of the present study was to develop self-emulsifying drug delivery system (SEDDS) of aceclofenac for potential improvement in the in vitro dissolution. The Food and Drug Control Agency (FDCA) has put more stress on the quality, safety and efficacy of the dosage form. The use of design of experiments and quality by Design (QbD) in the development of self emulsifying drug delivery system (SEDDS) containing aceclofenac is demonstrated. The optimum formulation contained Labrafil M 1944 CS, Tween 80 and Transcutol P. The systematic approach enabled us in identifying the design space. The results revealed that while devising the control strategies during manufacturing, more attention should be focused on the ratios of oil to surfactant and surfactant to co-surfactant. The drug was released at a faster rate due to a large surface area. The current approach enabled us to develop a dosage form which is economic, patient-friendly and does not require assistance of a doctor or nurse, especially at remote places at odd hours.

DEVELOPMENT AND EVALUATION OF ZIPRASIDONE LOADED SOLID SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEM

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (08) ◽  
pp. 53-60
Author(s):  
Purushottam Patil ◽  
Malik Shaikh ◽  
Paresh Mahaparale
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Physical Adsorption ◽  
Gastrointestinal Transit ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Poorly Water Soluble

Solid self-micro emulsification technique is the new approach for poorly water-soluble and poorly bioavailable drugs by allowing the drug substance to be incorporated into the oil phase and thus having the ability to permeate the GI membrane to a faster extent. Oleic acid, Tween 80, methanol and colloidal silicon dioxide were used as penetrant, surfactant, co-surfactant and adsorbent, respectively. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The results of DSC and FTIR studies did not reveal any possible drug-excipient interactions. The conversion of liquid self-microemulsifying drug delivery system (SMEDDS) into the solid SMEDDS increases the stability of the emulsion formulation achieved by physical adsorption of an adsorbent material. The release of drug from SMEDDS formulation is justified by in-vitro dissolution studies. SMEDDS increases the solubility of the drug and improves the bioavailability, without disturbing gastrointestinal transit. SMEDDS has the potential to provide a useful oral solid dosage form for the poorly water-soluble drug ziprasidone.

scholarly journals SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM OF EFAVIRENZ: FORMULATION, IN VITRO EVALUATION AND CHARACTERIZATION

2019 ◽  
pp. 217-226
Author(s):  
PAMU SANDHYA
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Visual Observation ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Tween 20

Objective: The main objective of this study was to preparation and evaluation of efavirenz (EFV) to enhance its solubility and dissolution rate by self-emulsifying drug delivery system. Methods: EFV self-emulsifying drug delivery systems (SNEDDS) were formulated using different oils, surfactant, and co-surfactant. Peceol, Tween 20, and Capmul MCM were used as oil, surfactant, and co-surfactant, respectively, followed by the evaluation by the performance of different tests such as visual observation, solubility studies, thermodynamic stability study, transmittance studies, drug content, and in-vitro release study. Results: Fourier-transform infrared studies revealed negligible drug and polymer interaction. From the phase diagram, it was observed that self-emulsifying region was enhanced with increasing surfactant and co-surfactant concentrations with oil. F13 was selected as optimized formulation on the basis of physicochemical parameters, particle size, and in-vitro dissolution studies with the release of 98.39±5.10% drug in 1 hour. The optimized formulation size was found to be 156.7 nm as mean droplet size and Z-Average of 808.6 nm with -18.3 mV as zeta potential. Conclusion: The study demonstrated that SNEDDS was a promising strategy to enhance the dissolution rate of EFV by improving solubility.

Formulation and Optimization of Self Emulsifying Drug Delivery System For Effective Anthelmintic Therapy

2021 ◽  
pp. 5831-5837
Author(s):  
Kiran C. Mahajan ◽  
Smita S. Pimple ◽  
Hemant A. Deokule
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase ◽  
In Vitro Dissolution ◽  
Ternary Phase Diagrams ◽  
Globule Size ◽  
Capmul Mcm ◽  
Negative Zeta Potential

The present study aims to develop and optimize a self-emulsifying drug delivery system for paediatric patients to improve the oral bioavailability of the anthelmintic drug, Praziquantel (PZQ) and to perform it’s in-vitro dissolution study. The solubility of PZQ was estimated in various vehicles to select proper component combination. Capmul MCM (oil), Cremophore RH40 (surfactant) and PEG400 (co-surfactant) were employed to construct pseudo-ternary phase diagrams. Eight formulations composed of Capmul MCM, at Smix ratios (1:1, 2:1 & 3:1) were selected. The optimized formulation F7 has a mean globule size 14.73 nm with a negative zeta potential -44.43 mV. The results indicated that PZQ loaded SEDDS, showed enhanced solubilization and nanosizing potential to improve the absorption of the drug.

scholarly journals Development of a self-microemulsifying drug delivery system of domperidone: In vitro and in vivo characterization

2013 ◽  
Vol 63 (2) ◽  
pp. 241-251 ◽  
Author(s):  
Ramesh Jakki ◽  
Muzammil Afzal Syed ◽  
Prabhakar Kandadi ◽  
Kishan Veerabrahma
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Ternary Phase Diagram ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Size Analysis

The main objective of this work was to prepare a self-micro emulsifying drug delivery system (SMEDDS) for enhancement of oral bioavailability of domperidone, a poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. The in vitro self-micro emulsification properties and droplet size analysis of SMEDDS were studied following their addition to water under mild agitation. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions (1:100, 1:500, 1:1000) and freeze-thaw stability. The optimized formulation, SMEDDS-B used for in vitro dissolution and bioavailability assessment, contained oil (Labrafac CC, 25 %, m/m), surfactant (Tween 80, 55 %, m/m), and co-surfactant (Transcutol®, 20 %, m/m). The preliminary oral bioavailability of domperidone from SMEDDS was 1.92-fold higher compared to that of domperidone suspension in rats. The AUC0-24 and cmax values were 3.38 ± 0.81 μg h mL-1 and 0.44 ± 0.03 μg mL-1 for SMEDDS-B formulation in comparison with 1.74 ± 0.18 μg h mL-1 and 0.24 ± 0.02 μg mL-1 for domperidone suspension, suggesting a significant increase (p < 0.05) in oral bioavailability of domperidone from SMEDDSS.

scholarly journals Quality-By-Design-Based Development of a Voxelotor Self-Nanoemulsifying Drug-Delivery System with Improved Biopharmaceutical Attributes

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1388
Author(s):  
Aristote B. Buya ◽  
Romano Terrasi ◽  
Jérémie K. Mbinze ◽  
Giulio G. Muccioli ◽  
Ana Beloqui ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Ternary Phase Diagram ◽  
Desirability Function ◽  
Limiting Factors ◽  
In Vitro Dissolution

Low aqueous solubility and poor oral bioavailability are limiting factors in the oral delivery of voxelotor, an antisickling agent. To overcome these limitations, a voxelotor self-nanoemulsifying drug delivery system was developed. Various oils, surfactants, and cosurfactants were screened for their solubilization potential for the drug. The area of nanoemulsification was identified using a ternary phase diagram. An experimental mixture design and a desirability function were applied to select SNEDDSs that contain a maximum amount of lipids and a minimum amount of surfactant, and that possess optimal emulsification properties (i.e., droplet sizes, polydispersity index (PDI), emulsification time, and transmittance percentage). The optimized SNEDDS formulation was evaluated for the self-emulsifying time (32 s), droplet size (35 nm), and zeta potential (−8 mV). In vitro dissolution studies indicated a 3.1-fold improvement in drug solubility from the optimized SNEDDS over pure drug powder. After 60 min of in vitro lipolysis, 88% of the voxelotor loaded in the SNEDDS remained in the aqueous phase. Cytotoxicity evaluation, using Caco-2 cells, indicated the safety of the formulation at 0.9 mg/mL. The transport of the voxelotor SNEDDS across Caco-2 monolayers was significantly enhanced compared to that of the free drug. Compared to the drug suspension, the developed SNEDDS enhanced the oral bioavailability (1.7-fold) of voxelotor in rats. The results suggest that further development of SNEDDSs for the oral delivery of voxelotor is needed.

Chronomodulated Delivery of Pantoprazole for Nocturnal Hyperacidity

2015 ◽  
Vol 8 (4) ◽  
pp. 3038-3044
Author(s):  
Mahalakshmi P ◽  
Suriyaprakash T N K ◽  
S. Lakshmana Prabu
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Lag Time ◽  
Delivery Systems ◽  
Burst Release ◽  
Dependent Manner ◽  
Compression Technique ◽  
Pulsatile Drug Delivery

The objective of this work was to design and evaluate an oral site-specific, pulsatile drug delivery system containing Pantoprazole sodium which can be targeted to colon in a pH and time dependent manner, to modulate the drug level in synchrony with the circadian rhythm of nocturnal hyperacidity. Five different composition of Core tablets were prepared by direct compression technique. Based on the release studies of core tablets, nine different compositions of press coated tablets were prepared and analyzed. The press coated tablet further coated by using five different proportions of Eudragit RS PO for providing consistent, reproducible chronomodulated release profile. Formulation FPC3 is more suitable among the formulations to design pulsatile release formulations of pantoprazole sodium for 6 hours lag time. After this lag time burst release was observed which exhibited sigmodial release pattern and that was considered to be an ideal for the pulsatile drug delivery system. The chronomodulated drug delivery systems for pantoprazole sodium for the treatment of hyperacidity was successfully developed and the release of the drug was sharp and complete after the lag time which is necessary for any pulsatile drug delivery systems.   

scholarly journals FORMULATION DEVELOPMENT AND IN VITRO EVALUATION OF CURCUMIN-LOADED SOLID SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM FOR COLON CARCINOMA

2019 ◽  
pp. 243-247
Author(s):  
CHENMALA KARTHIKA ◽  
RAMAN SURESHKUMAR ◽  
AMEER SUHAIL
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Delivery System ◽  
Delivery System ◽  
Dosage Form ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
The World ◽  
Tablet Dosage

Objective: Cancer is the deadliest disease affecting the life of the people all around the world. Colon cancer is the cancer which is affecting the colon region it is the last part of the gastrointestinal tract which is mainly responsible for the absorption of water and minerals from the food debris. Colon cancer is the second most cancer creating death in the world. It affects both male and female equally. Curcumin is a flavonoid used from decades for the treatment of various ailments including cancer. This present work is to formulate Self-nanoemulsifying drug delivery (SNEDDS) system with the help of curcumin for colon delivery. Materials and Methods: Nanoemulsion was prepared using the curcumin pre-concentrated self-nanoemulsifying drug delivery system, with which tablets were prepared and coated with pectin followed by the evaluation test such as in vitro dissolution and cell line studies. Results: Solubility profile of curcumin was found with a greater impact using Capmul MCM and Labrafac PG which is then added with the surfactants and co-surfactants and were converted into Nano-droplets. F1 formulation was selected after carrying out the characterisation studies and converted into a tablet dosage form and then coated with pectin, in vitro studies depicted a release of 80% in pH 6.8. Conclusions: Formulation of a solid self-Nano emulsifying drug delivery system using curcumin was successfully carried out. From the results obtained, the formulation (F1) was selected for the formation of the tablets and the further experimental part is carried out. The tablet dosage form is then coated with pectin and used for targeting the colon cancer cells for its treatment.

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