FIXED-DOSE COMBINATION DRUGS AS TABLET IN TABLET: A REVIEW

2021 ◽  
Vol 1 (9) ◽  
pp. 169-177
Author(s):  
Pavazhaviji P ◽  
Rajalakshmi A. N
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Product Life Cycle ◽  
Pharmacokinetic Profile ◽  
Oral Dosage ◽  
Fixed Dose ◽  
Pharmaceutical Ingredients ◽  
Delayed Release ◽  
Dose Combination ◽  
Compression Coating

The Pharmaceutical industry has become more interested in developing fixed-dose combinations (FDCs) in recent years. FDCs have been used successfully in a variety of clinical areas, including diabetes, HIV/AIDS,and cardiovascular diseases etc. FDCs are intended to extend the product life cycle and enhance patient compliance by decreasing cost. Active Pharmaceutical ingredients are chosen for FDC development based on variety of purposes such as Pharmacokinetic profile, drug-drug interactions, mechanism of action, and manufacturability for successful development. Tablet in tablet technology has gained popularity in recent years for creating modified release products. The compression coating or solvent-free-coating technology is also known as Tablet in Tablet technology. Tablet in Tablet technology is presently the finest alternative technology for the formulation of bilayer tablets for physical separation of active medicines and used to avoid chemical incompatibilities and to produce different drug release patterns such as rapid release, sustained release, controlled release, delayed release, and pulsatile release. This review mainly focuses on combining the techniques of both FDC and Tablet in Tablet formulations which offer a wide variety of benefits such as increased patient compliance, convenience, separation of incompatible ingredients, avoiding close interaction of two drugs, achieving various drug release patterns and maximizing the potency of both drugs over conventional oral dosage forms Keywords: Fixed dose combinations, Tablet in tablet technology, Compression coated tablet, Bilayer tablet, delayed release

scholarly journals PHARMACOTECHNICAL DEVELOPMENT AND OPTIMIZATION OF MULTILAYERED TABLETS: AN UPDATED INDUSTRIAL REVIEW WITH EMPHASIS ON BILAYER TABLETS

2021 ◽  
pp. 55-64
Author(s):  
AHMED M. AGIBA ◽  
SOHA SAYED ABUL-ELLA ◽  
REHAB A. ABD EL-MONEM
Keyword(s):  
Process Parameters ◽  
Geriatric Patients ◽  
Review Article ◽  
Fixed Dose ◽  
Active Pharmaceutical Ingredients ◽  
Drug Release Profile ◽  
Influence Of Process Parameters ◽  
Pharmaceutical Ingredients ◽  
Dose Combination ◽  
Materials Used

Fixed-dose combination formulations are multilayered platforms designed for solving complex medication regimens and overcoming polypharmacy problems especially in chronic diseases with geriatric patients. Multilayered tablets are considered promising avenues to combine different active pharmaceutical ingredients (APIs) for a synergic therapeutic effect, or different formulations of the same API in order to achieve a specific drug release profile. Besides, multilayered tablets can extensively help in avoiding possible interactions between different drugs, as well as optimizing each formulation individually in terms of pharmacokinetics and manufacturability. This review article discusses the most suitable materials used in the manufacturing of multilayered tablets, describes novel approaches to manufacturing improvement and process parameters, the influence of process parameters on layer adhesion, and the characterization tests of multilayered tablets.

scholarly journals Fixed Dose Oral Dispersible Tablet of Bitter Drug Using Okra Mucilage: Formulation and Evaluation

2020 ◽  
Vol 10 (5) ◽  
pp. 149-158
Author(s):  
Pintu Dhar ◽  
Himangshu Sarma ◽  
Hemanta Kumar Sharma
Keyword(s):  
Drug Release ◽  
Bitter Taste ◽  
Oral Dosage ◽  
Taste Masking ◽  
Fixed Dose ◽  
Wet Granulation ◽  
Formulation Development ◽  
Dispersible Tablet ◽  
Promethazine Hydrochloride

Background: The solid oral dosage forms containing bitter drugs need improved palatability for administration. Formulation scientists have given attention to the improvement of taste masking technologies and utilised various strategies. Objective: The present work aimed to mask the bitter taste of Promethazine Hydrochloride by formulating Oral Dispersible Tablets using Okra mucilage as a taste-masking agent.  Methods: The Okra mucilage was extracted from Okra by the aqueous extraction process. An emulsion solvent diffusion technique was used for masking the bitter taste of Promethazine Hydrochloride by using Okra mucilage. The Oral Dispersible Tablet was prepared by the wet granulation method. The mucilage and the formulation were characterized and evaluated by standard methods and protocols. Results: Taste masking of the bitter drug was successfully achieved by Okra mucilage. The DSC and FTIR study revealed that the drug molecule was compatible with okra mucilage and drug entrapment efficacy was found to be 94.76%. The palatability test asserted that masking of the bitter taste of the drug.  The In vitro drug release study showed that the F7 tablet batch has a better drug release rate and followed non- fickian mechanism of drug release. Conclusion: Thus, taste masking with Okra mucilage was successful and this opens opportunities for application of common edible substances in formulation development. Keywords: Fast disintegrating tablet; Natural polymer; Mouth dissolving tablet; Promethazine Hydrochloride; Taste masking

scholarly journals Formulation and Evaluation of Fixed Dose Combination Suppositories Containing Stavudine, Lamivudine and Nevirapine for Pediatric Applications

2015 ◽  
Vol 7 (3) ◽  
pp. 87-96 ◽  
Author(s):  
Y. Padmavathi ◽  
B. M. Reddy ◽  
M. Renuka ◽  
K. Sumedha ◽  
N. P. Reddy
Keyword(s):  
Drug Release ◽  
Pediatric Hiv ◽  
Fixed Dose Combination ◽  
Fixed Dose ◽  
Physical Parameters ◽  
New Era ◽  
Weight Variation ◽  
Suppository Base ◽  
Dose Combination ◽  
Living With Hiv

Suppositories are the convenient way of administering drugs in infants. In view of the lack of suitable pediatric antiretroviral formulations in the market, suppositories containing fixed dose combination (FDC) of stavudine, lamivudine and nevirapine (SLN) were developed to allow administration of the correct weight-related dose in pediatric HIV patients as recommended by WHO. Suppositories containing 10 mg of stavudine, 40 mg of lamivudine and 70 mg of nevirapine were prepared by the fusion method using Witepsol H15 semi-synthetic suppository base. All the prepared suppositories were evaluated for various physical parameters like weight variation, melting point, drug content and hardness. The rate and extent of drug release was evaluated using USP apparatus I and samples were analyzed by a validated UV-multicomponent method. The use of surfactants significantly increased the drug release from formulations manufactured with Witepsol H 15 fatty base. The development of pediatric fixed-dose combination formulations represent a new era and mark an important milestone for children living with HIV/AIDS.

scholarly journals Investigating In Vitro and Ex Vivo Properties of Artemether/Lumefantrine Double-Fixed Dose Combination Lipid Matrix Tablets Prepared by Hot Fusion

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 922
Author(s):  
Christi A. Wilkins ◽  
Lissinda H. du Plessis ◽  
Joe M. Viljoen
Keyword(s):  
Drug Release ◽  
Stearic Acid ◽  
Ex Vivo ◽  
Matrix Tablets ◽  
Fixed Dose Combination ◽  
Fixed Dose ◽  
Lipid Matrix ◽  
Lipophilic Drugs ◽  
Dose Combination

Highly lipophilic antimalarial drugs, artemether and lumefantrine, whilst an effective fixed-dose combination treatment to lower the malarial disease burden, are therapeutically hindered by low aqueous solubility and varied bioavailability. This work investigates the plausibility of directly compressed lipid matrix tablets, their role as lipid-based formulations and their future standing as drug delivery systems. Lipid matrix tablets were manufactured from solid lipid dispersions in various lipid:drug ratios employing hot fusion—the melt mixing of highly lipophilic drugs with polymer(s). Sequential biorelevant dissolution media, multiple mathematical models and ex vivo analysis utilizing porcine tissue samples were employed to assess drug release kinetics and more accurately predict in vitro performance. Directly compressed stearic acid tablets in a 0.5:1 lipid:drug ratio were deemed optimal within investigated parameters. Biorelevant media was of immense value for artemether release analysis, with formulation SA0.5C1 (Stearic Acid:double fixed dose in a 0.5:1 ratio (i.e., Stearic acid 70 mg + Lumefantrine 120 mg + Artemether 20 mg); CombiLac® as filler (q.s.); and 1% w/w magnesium stearate) yielding a higher percentage of artemether release (97.21%) than the commercially available product, Coartem® (86.12%). However, dissolution media lacked the specificity to detect lumefantrine. Nonetheless, stearic acid lipid:drug ratios governed drug release mechanisms. This work demonstrates the successful utilization of lipids as pharmaceutical excipients, particularly in the formulation of lipid matrix tablets to augment the dissolution of highly lipophilic drugs, and could thus potentially improve current malarial treatment regimens.

scholarly journals DESIGN AND STATISTICAL OPTIMIZATION OF MOUTH DISSOLVING SUBLINGUAL FILM OF FIXED DOSE COMBINATION OF DOXYLAMINE SUCCINATE AND PYRIDOXINE HYDROCHLORIDE USING DESIGN OF EXPERIMENT IN THE TREATMENT OF NAUSEA AND VOMITING IN PREGNANCY

2018 ◽  
Vol 11 (12) ◽  
pp. 202
Author(s):  
Bobde Suwarna Suresh ◽  
Tank Hemraj M
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Nausea And Vomiting ◽  
Fixed Dose Combination ◽  
Fixed Dose ◽  
Pyridoxine Hydrochloride ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Folding Endurance ◽  
Dose Combination

Objective: The present research aims at formulating a mouth dissolving sublingual film of fixed dose combination of doxylamine succinate (DS) and pyridoxine hydrochloride (PH) that would provide faster onset of action and hence relief from the condition of nausea and vomiting in pregnancy.Methods: Mouth dissolving films were prepared using a solvent casting technique. A 23 full-factorial design of eight formulations was set up with three independent variables: X1 - polymer 1 HPMC E15 concentration, X2 - polymer 2 HPMC E5 concentration, and X3 - plasticizer PEG 400 concentration. The responses, i.e., dependent variables measured for the study were Y1 disintegration time in seconds, Y2 tensile strength in kg/cm2, Y3 drug release in the percentage of DS, and Y4 drug release in the percentage of PH. All the formulations were evaluated for physicochemical parameters such as clarity, weight, thickness, folding endurance, surface pH, and content. The design expert software 11.0 trial version was used for statistical analysis of the responses.Results and Conclusion: All the film formulations were found to be transparent, non-tacky, and easily peelable having the satisfactory tensile strength and folding endurance. The concentration of polymer 1 and 2 was found to have a significant effect on disintegration time and drug release of mouth dissolving films. The best film formulation DP1 was found to have a disintegration time of 77.66 s and found to release 96.22% of DS and 95.43% of pyridoxine HCl in 21 min.

scholarly journals 3D Printed Pellets (Miniprintlets): A Novel, Multi-Drug, Controlled Release Platform Technology

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 148 ◽  
Author(s):  
Atheer Awad ◽  
Fabrizio Fina ◽  
Sarah Trenfield ◽  
Pavanesh Patel ◽  
Alvaro Goyanes ◽  
...  
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Selective Laser Sintering ◽  
Three Dimensional ◽  
Single Step ◽  
Oral Dosage ◽  
Three Dimensional Printing ◽  
Pharmaceutical Ingredients ◽  
3D Printed ◽  
Oral Dosage Forms

Selective laser sintering (SLS) is a single-step three-dimensional printing (3DP) process that can be leveraged to engineer a wide array of drug delivery systems. The aim of this work was to utilise SLS 3DP, for the first time, to produce small oral dosage forms with modified release properties. As such, paracetamol-loaded 3D printed multiparticulates, termed miniprintlets, were fabricated in 1 mm and 2 mm diameters. Despite their large surface area compared with a conventional monolithic tablet, the ethyl cellulose-based miniprintlets exhibited prolonged drug release patterns. The possibility of producing miniprintlets combining two drugs, namely paracetamol and ibuprofen, was also investigated. By varying the polymer, the dual miniprintlets were programmed to achieve customised drug release patterns, whereby one drug was released immediately from a Kollicoat Instant Release matrix, whilst the effect of the second drug was sustained over an extended time span using ethyl cellulose. Herein, this work has highlighted the versatility of SLS 3DP to fabricate small and intricate formulations containing multiple active pharmaceutical ingredients with distinct release properties.

scholarly journals A Survey of the Regulatory Requirements for BCS-Based Biowaivers for Solid Oral Dosage Forms by Participating Regulators and Organisations of the International Generic Drug Regulators Programme

2018 ◽  
Vol 21 (1) ◽  
pp. 27 ◽  
Author(s):  
Joy Elizabeth Van Oudtshoorn ◽  
Alfredo García-Arieta ◽  
Gustavo Mendes Lima Santos ◽  
Christopher Crane ◽  
Clare Rodrigues ◽  
...  
Keyword(s):  
Generic Drug ◽  
Oral Dosage ◽  
Fixed Dose ◽  
Scientific Model ◽  
Regulatory Requirements ◽  
Regulatory Guidance ◽  
Dose Combination ◽  
Oral Dosage Forms

Purpose:  The Biopharmaceutics Classification System (BCS) based biowaiver is a scientific model which enables the substitution of in vivo bioequivalence studies with in vitro data as evidence of therapeutic equivalence subject to certain conditions. Despite being based on the same principles, BCS-based biowaivers are interpreted and regulated differently among international regulatory agencies. In this survey, the Bioequivalence Working Group (BEWG) of the International Generic Drug Regulators Programme (IGDRP) compared the criteria for BCS-based biowaivers applied by the participating regulators and organisations. Methods:  Differences and similarities regarding solubility, permeability, dissolution, excipients and fixed-dose combination products, were identified and compared in a detailed survey of each participant’s criteria for BCS-based biowaivers. These criteria were determined based upon the participants’ respective regulatory guidance documents, policies and practices. Results: This review has, with the exception of two participants who do not accept BCS-based biowaivers, revealed that most IGDRP participants interpret the BCS principles and conditions similarly but notable differences exist in the application of these principles.  Conclusion: Although many similarities exist, this review identifies several opportunities for greater convergence of regulatory requirements amongst the surveyed jurisdictions. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page

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