FORMULATION AND EVALUATION OF MEDICATED TENOFOVIR ALAFENAMIDE FUMARATE CANDY FOR TREATMENT OF HUMAN IMMUNODEFICIENCY SYNDROME

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (10) ◽  
pp. 60-62
Author(s):  
Priya Mourya ◽  
Anindya Goswami ◽  
Neelesh Malviya ◽  
Keyword(s):  
Drug Delivery ◽  
Geriatric Patients ◽  
Oral Drug Delivery ◽  
Research Work ◽  
Oral Dosage ◽  
Drug Dissolution ◽  
Oral Drug ◽  
Weight Variation ◽  
Buccal Drug Delivery ◽  
Tenofovir Alafenamide

Medicated candies are solid oral dosage form containing medicaments in a flavored and sweetened base. The main advantages associated with buccal drug delivery are systemic absorption of drug, also increased bioavailability and avoidance of hepatic first pass metabolism. Tenofovir alafenamide fumarate is a drug of choice for the treatment of human immunodeficiency virus due to its potency and fewer side effects over tenofovir disoproxil fumarate. The aim of the present research work was to formulate and evaluate candy of tenofovir alafenamide fumarate for pediatric and geriatric patients for better patient acceptability. Medicated candies of tenofovir alafenamide fumarate were prepared by using heating and congealing method, and the prepared formulations were evaluated for various parameters such as organoleptic properties, weight variation, friability, hardness, drug content and in vitro drug dissolution time profile. On the basis of the above studies, it can be concluded that medicated candy can be utilized as alternative option for oral drug delivery for pediatric and geriatric patients.

scholarly journals The Development and Optimization of Hot-Melt Extruded Amorphous Solid Dispersions Containing Rivaroxaban in Combination with Polymers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 344
Author(s):  
Jong-Hwa Lee ◽  
Hyeong Sik Jeong ◽  
Jong-Woo Jeong ◽  
Tae-Sung Koo ◽  
Do-Kyun Kim ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Oral Drug Delivery ◽  
Amorphous Solid ◽  
Drug Dissolution ◽  
Oral Drug ◽  
Amorphous Solid Dispersion ◽  
Screw Speed ◽  
Hot Melt

Rivaroxaban (RXB), a novel oral anticoagulant that directly inhibits factor Xa, is a poorly soluble drug belonging to Biopharmaceutics Classification System (BCS) class II. In this study, a hot-melt extruded amorphous solid dispersion (HME-ASD) containing RXB is prepared by changing the drug:polymer ratio (Polyvinylpyrrolidione-vinyl acetate 64, 1:1–1:4) and barrel temperature (200–240 °C), fixed at 20% of Cremophor® RH 40 and 15 rpm of the screw speed, using the hot-melt extruding technique. This study evaluates the solubility, dissolution behavior, and bioavailability for application to oral drug delivery and optimizes the formulation of rivaroxaban amorphous solid dispersion (RXB-ASD). Based on a central composite design, optimized RXB-ASD (PVP VA 64 ratio 1:4.1, barrel temperature 216.1 °C, Cremophor® RH 40 20%, screw speed 15 rpm) showed satisfactory results for dependent variables. An in vitro drug dissolution study exhibited relatively high dissolution in four media and achieved around an 80% cumulative drug release in 120 min. Optimized RXB-ASD was stable under the accelerated condition for three months without a change in crystallinity and the dissolution rate. A pharmacokinetic study of RXB-ASD in rats showed that the absorption was markedly increased in terms of rate and amount, i.e., the systemic exposure values, compared to raw RXB powder. These results showed the application of quality by design (QbD) in the formulation development of hot-melt extruded RXB-ASD, which can be used as an oral drug delivery system by increasing the dissolution rate and bioavailability.

scholarly journals EFFECT OF NATURAL AND SYNTHETIC POLYMERS ON THE PROPERTIES OF CANDESARTAN CILEXETIL MATRIX TABLET PREPARED BY DRY GRANULATION

2016 ◽  
Vol 9 (9) ◽  
pp. 161
Author(s):  
Omar Saeb Salih ◽  
Roaa Abdalhameed Nief
Keyword(s):  
Drug Delivery ◽  
Candesartan Cilexetil ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Oral Drug ◽  
Matrix Tablet ◽  
Sustained Release Formulation ◽  
Weight Variation ◽  
Vitro Release

ABSTRACTObjective: The objective of this study is to develop a controlled release matrix tablet of candesartan cilexetil to reduce the frequency of administration,enhance bioavailability and improve patient compliance; a once daily sustained release formulation of candesartan cilexetil is desirable.Methods: The prepared tablets from F1 to F24 were evaluated with different evaluation parameters like weight variation, drug content, friability,hardness, thickness and swelling ability. In vitro release for all formulas were studied depends on the type and amount of each polymer, i.e. (16 mg,32 mg and 48 mg) respectively beside to the combination effect of polymers on the release of the drug from the tablet.Results: In vitro release showed that formula 13 had the faster release (100% after 4 h) which contained acacia (1:1) and the lowest sustain releasewas showed for F7 (73% after 8 h) which contained HPMC K100M (1:1). Formula 1 was an 89 % release after 8 h which contain eudragit RS100; F4was a 100 % release after 5 h which contain Na CMC, F10 was a 100% after 8 h which contain xanthan gum and F16 was a 100 % release after 5 hwhich contain tragacanth polymer. Formula 9 had a lower release than F7 and F8 respectively. Formula 7 can be used for sustain oral drug delivery ofcandesartan cilexetil while Formula 13 can be used in contrary as fast release tablets for faster response.Conclusion: Controlled drug delivery system is promising for less dosing and higher patient compliance.Keywords: Angiotensin II receptor antagonist, Hypertension, Matrix system, Control release.

scholarly journals FAST DISSOLVING DRUG DELIVERY SYSTEMS: FORMULATION, PREPARATION TECHNIQUES AND EVALUATION

2018 ◽  
Author(s):  
Satbir Singh ◽  
Tarun Virmani ◽  
Reshu Virmani ◽  
Geeta Mahlawat ◽  
Pankaj Kumar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Dosage Forms ◽  
Delivery Systems ◽  
Oral Dosage ◽  
Oral Drug ◽  
Self Medication ◽  
Onset Of Action ◽  
Fast Disintegrating Tablets

The Fast Dissolving Drug Delivery Systems sets a new benchmark was an expansion that came into existence in the early 1980’s and combat over the use of the different dosage form like tablets, suspension, syrups, capsules which are the other oral drug delivery systems. Fast Dissolving Drug Delivery System (FDTS)  has a major advantage over the conventional dosage forms since the drug gets rapidly disintegrated and dissolves in the saliva without the use of water .In spite of the downside lack of immediate onset of action; these oral dosage forms have valuable purposes such as self medication, increased patient compliance, ease of manufacturing and lack of pain. Hence Fast Disintegrating Tablets (FDTS) technology has been gaining importance now-a-days with wide variety of drugs serving many purposes. Fast Disintegrating Tablets (FDTS) has ever increased their demand in the last decade since they disintegrate in saliva in less than a minute that improved compliance in pediatrics and geriatric patients, who have difficulty in swallowing tablets or liquids. As fast dissolving tablet provide instantaneous disintegration after putting it on tongue, thereby rapid drug absorption and instantaneous bioavailability, whereas Fast dissolving oral films are used as practical alternative to FDTS. These films have a potential to deliver the drug systemically through intragastric, sublingual or buccal route of administration and also has been used for local action. In present review article different aspects of fast dissolving  tablets and films like method of preparations, latest technologies, evaluation parameters are discussed. This study will be useful for the researchers for their lab work.  

REVIEW ON GASTRORETENTIVE DRUG DELIVERY SYSTEM

2020 ◽  
pp. 38-45
Author(s):  
MANDAR J BHANDWALKAR ◽  
PRASAD S DUBAL ◽  
AKASH K.TUPE ◽  
SUPRIYA N MANDRUPKAR
Keyword(s):  
Drug Delivery ◽  
Small Intestine ◽  
Drug Delivery System ◽  
Residence Time ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Oral Drug ◽  
Low Solubility

In recent years, gastroretentive drug delivery system (GRDDS) has gained researcher’s interest in the field of oral drug delivery. Various GRDDS approaches can be utilized to retain the dosage forms in the stomach and to release the drug slowly for an extended period of time. GRDDS can be used to prolong the residence time of delivery system in the stomach. This results in targeting of drug release at a specific site for the systemic or local effects. GRDDS can be used to overcome challenges associated with conventional oral dosage forms and to release the drug at a specific absorption site to improve bioavailability of particular drug substance. The challenges include fast gastric emptying of the dosage form which results in the poor bioavailability of the drug. Prolongation of the retention of drugs in stomach those having low solubility at high intestinal pH improves the solubility of drugs. GRDDS has proved to be effective in systemic actions as well as in local actions to treat gastric or duodenal ulcers. Local activity in the upper part of the small intestine can be obtained by improving the residence time of delivery system in the stomach. The system is useful for drugs which are unstable in the intestine or having a low solubility/permeability in the small intestine. Various GRDDS approaches include high density (sinking) systems, low-density (floating systems), mucoadhesive, expandable, unfoldable, superporous hydrogel systems, and magnetic systems.

COLOCASIA ESCULENTA STARCH: NOVEL ALTERNATIVE DISINTEGRANT FOR PHARMACEUTICAL APPLICATION

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (02) ◽  
pp. 41-53
Author(s):  
Ujjwala Y. Kandekar ◽  
Mayuri H. Tapkir ◽  
Priyanka H. Bhalerao ◽  
Nikita B. Rukhe ◽  
Shubhada K. Kad ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Research Work ◽  
Colocasia Esculenta ◽  
Oral Drug ◽  
Wet Granulation ◽  
Disintegration Time ◽  
Pharmaceutical Application ◽  
Oral Drug Delivery System

Oral drug delivery system has always been the most prevalent route of administration and continuous efforts are made to improve the drug delivery by this route. Tablets are one of the most extensively used dosage forms and various excipients have been developed for their formulation. The purpose of the current research work was to isolate and study the physicochemical properties of the Colocasia esculenta starch and further compare its disintegration ability with maize starch. Starch was isolated from C. esculenta corms by aqueous extraction method and possesses characteristics that are typical of starches. It was further evaluated for the presence of other foreign matter and phytoconstituents. Results showed that the isolated sample was free from foreign organic matter and the total ash value was found to be 0.4%. Tablets were prepared by the wet granulation method by varying concentrations in the range of 2.5 to 10% w/w for both the starches. Pre and post-compression parameters were studied and were found to be within the pharmacopoeial limits. Disintegration tests showed that disintegration time decreases with increasing concentration of both the starches. At 10% w/w concentration, disintegration time was found to be lowest, hence it was selected as an optimized formulation Stability studies were performed on F4 batch and it was found to be stable. The determination of disintegration efficiency indicates that C. esculenta starch exhibits disintegrating potential.

scholarly journals A Review Extended Release Oral Drug Delivery System and Multiparticulate Drug Delivery Systems (MDDS)

2020 ◽  
pp. 84-92
Author(s):  
Swapnil B. Khambat ◽  
Shubham A. Kale.
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Extended Release ◽  
Oral Drug Delivery ◽  
Oral Dosage ◽  
Oral Drug ◽  
Solid Dosage ◽  
Oral Formulations ◽  
Oral Drug Delivery System ◽  
Oral Dosage Forms

The extended release product will optimize therapeutic effect and safety of a drug at the same time improving the patient convenience and compliance. By incorporating the dose for 24 hrs into one tablet/capsule from which the drug is released slowly. The concept of multiple unit dosage form was initially introduced in the early 1950’s.These forms play a major role in the design of solid dosage form processes because of their unique properties and the flexibility found in their manufacture. These forms can be defined as oral dosage forms consisting of a multiplicity of small discrete units, each exhibiting some desired characteristics. The release of drug from pellets depends on a variety of factors including the carrier used to form pellets and the amount of drug contained in them. Consequently, pellets provide tremendous opportunities for designing new controlled and extended release oral formulations, thus extending the frontier of future pharmaceutical development. The possible mechanism for drug release includes solution/diffusion through the continuous polymer phase or plasticizer channels, diffusion through aqueous pores and osmotically driven release through aqueous pores. To distinguish between these mechanisms, the release rate was studied as a function of coating thickness, plasticizer content and osmotic pressure in the dissolution medium.

scholarly journals Fast dissolving tablets: waterless patient compliance dosage forms

2019 ◽  
Vol 9 (1) ◽  
pp. 303-317
Author(s):  
SANTOSH KUMAR RADA ◽  
Annu Kumari
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Oral Route ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Oral Drug ◽  
Self Medication ◽  
Existing Problems ◽  
Solid Dosage ◽  
Oral Dosage Forms

Drug delivery by the oral route is the most prescribable and acceptable route in terms of patient’s compliance. Improvement of patient’s compliance has always a challenge towards the development of oral drug delivery system. In the market different types of oral dosage forms are available in which tablets, capsules, syrups, suspensions are preferred ones. Oral solid drug delivery faces drawback in case of swallowing especially with paediatrics and geriatric psychotic patients. Therefore scientists attracted towards fast mouth dissolving drug delivery systems to encounter existing problems with unique property of palatability and rapid disintegration. The concept of fast dissolving tablet came into existence in late 1970 and further improvements are still going on in connection with its preparation and methodology. Fast dissolving tablets have faster disintegration and dissolution rate and releases within 30 seconds as they come in contact with saliva. These systems also obviate the requirement of carry water during drug administration. This facilitate drug delivery to the patients of dysphasic, psychic, paediatrics, geriatric and bed-ridden, unconscious population. As fast dissolving tablets falls under desired expectation of safer, convenient and economical solid dosage forms, several techniques have been developed to improve disintegration quality in the recent past years. This article mainly focuses on formulation and evaluation technologies with recent advancement made so far in the field of fast dissolving tablets. Keywords: Fast disintegration; Dysphasia; Mouth dissolving; Self-medication.

scholarly journals Oral Strip Technology: A review

2014 ◽  
Vol 2 (02) ◽  
pp. 130-143 ◽  
Author(s):  
Hema Jaiswal
Keyword(s):  
Drug Delivery ◽  
Buccal Mucosa ◽  
Product Life Cycle ◽  
Oral Drug Delivery ◽  
Rapid Onset ◽  
Penetration Enhancers ◽  
Oral Dosage ◽  
Oral Drug ◽  
Drug Bioavailability ◽  
Good Tool

Over the recent past, many of the research groups are focusing their research on this technology. Amongst Oral drug delivery system Oral Strip Technology (OST) is gaining much attention. The advantages of OST are the administration to pediatric and geriatric patient population where the difficulty of swallowing larger oral dosage forms is eliminated. This technology has been used for local action, rapid release products and for buccoadhesive systems that are retained in the oral cavity to release drug in controlled fashion. OST offers an alternate platform for molecules that undergo first pass metabolism and for delivery of peptides. An ideal OST should have the following properties: high stability, transportability, ease of handling and administration, no special packaging material and/or processing requirements, no water necessary for application, and a pleasant taste. All these requirement are fulfilled by the oral films. The OST is a good tool for product life cycle management for increasing the patent life of existing molecules or products. Compared to some of the complicated and expensive process (like lyophilization) used to manufacture ODTs(Orally Disintegrating Tablets), the OST is relatively easy to fabricate,thus reducing the overall cost of the therapy. One of the reasons is that the buccal mucosa is less permeable and is thus not able to elicit a rapid onset of absorption and hence better suited for formulations that are intended for sustained release action. Further, the buccal mucosa being relatively immobile mucosa and readily accessible, it makes it more advantageous for retentive systems used for oral trans mucosal drug delivery. The primary disadvantage associated with buccal delivery route is the low flux that in turn results in low drug bioavailability. To overcome this hurdle, various buccal penetration enhancers have been studied which improve the absorption pattern of the molecules. The article shows OST encompassing materials used in OST, method of preparation, evaluation, applications, commercial technologies and future Business prospects of this technology.

Fast-dissolving Solid Dispersions for the Controlled Release of Poorly Water-soluble Drugs

2020 ◽  
Vol 26 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Beom-Jin Lee ◽  
Thao T.D. Tran
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Oral Drug Delivery ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Oral Drug ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

: Solid dispersions offer many advantages for oral drug delivery of poorly water-soluble drugs over other systems, including an increase in drug solubility and drug dissolution. The improvement of drug absorption and higher bioavailability of active pharmaceutical ingredients in the gastrointestinal tract have been reported in various studies. In certain circumstances, a rapid pharmacological effect is required for patients. Fast-dissolving solid dispersions provide an ideal formulation in such cases. This report will provide an overview of current studies on fast-dissolving solid dispersions, including not only solid dispersion powders with fast dissolution rates but also specific does forms for the controlled release of poorly water-soluble drugs. Specifically, the applications of fast-dissolving solid dispersions will be described in every specific case. Moreover, pharmaceutical approaches and the utilization of polymers will be summarized. The classification and analysis of fast-dissolving solid dispersions could provide insight into strategies and potential applications in future drug delivery developments.

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