scholarly journals Preparation and Physicochemical Stability of Liquid Oral Dosage Forms Free of Potentially Harmful Excipient Designed for Pediatric Patients

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 190 ◽  
Author(s):  
Guillaume Binson ◽  
Karine Beuzit ◽  
Virginie Migeot ◽  
Léa Marco ◽  
Barbara Troussier ◽  
...  
Keyword(s):  
Water Solubility ◽  
Storage Condition ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Pharmaceutical Ingredients ◽  
Physicochemical Stability ◽  
Oral Liquid ◽  
Reliable Solution ◽  
Physical And Chemical ◽  
Harmful Excipients

Dexamethasone, hydrochlorothiazide, spironolactone, and phenytoin are commonly used in neonates, but no age-appropriate formulation containing these active pharmaceutical ingredients (APIs) is commercially available. Thus, pharmaceutical compounding of the liquid oral dosage form is required to enable newborn administration. A problem common to the compounded preparations described in the literature is that they include potentially harmful excipients (PHEs). Therefore, the aim of this study was to evaluate the feasibility of compounding oral liquid dosage forms free of PHE, containing dexamethasone, hydrochlorothiazide, phenytoin, or spironolactone and to assess their physicochemical stability. Due to the poor water solubility of the targeted APIs, oral suspensions were compounded using Syrspend® SF-PH4 Dry, a suspending vehicle free of PHE. Four HPLC coupled to UV spectrometry (HPLC-UV) stability-indicating methods were developed and validated according to international guidelines to assay the strength of the targeted APIs. Whatever storage condition was used (5 ± 3 °C or 22 ± 4 °C), no significant degradation of API occurred in compounded oral suspensions. Overall, the results attest to the physical and chemical stability of the four oral liquid dosage forms over 60 days under regular storage temperatures. Finally, the use of the proposed oral suspensions provides a reliable solution to reduce the exposure of children to potentially harmful excipients.

scholarly journals P47 Extent of paediatric exposure to pharmaceutical excipients: an exploratory study

2020 ◽  
Vol 105 (9) ◽  
pp. e31.1-e31
Author(s):  
Mohammed AbouDaya ◽  
Stephen Tomlin ◽  
Asia N Rashed
Keyword(s):  
Propylene Glycol ◽  
Dosage Forms ◽  
List Type ◽  
Liquid Formulation ◽  
Solid Dosage Forms ◽  
Patient Factors ◽  
Solid Dosage ◽  
Oral Liquid ◽  
Harmful Excipients

AimThe assumption that excipients are inactive therefore non-harmful to patients is a declining opinion due to raised safety concerns of excipient activity, particularly in children.1 There is limited data on the safety of excipients in children and a lack of standardisation of the risk-benefit use of excipients in the different paediatric populations.2 This study aimed to investigate the extent of excipient exposure in children taking long-term oral liquids, admitted to Hospital, and to identify whether patients could be switched to a solid alternative due to the harm posed from liquid formulations.MethodA prospective observational study conducted in a UK paediatric hospital. The electronic medication chart for hospitalised children aged 0–18 years on long-term (for ≥6 weeks) oral liquid medicines, were reviewed over a four-week period. A priority list of eight excipients (called harmful excipients) with known reported hazards was developed based on literature: propylene glycol, ethanol, parabens, benzyl alcohol, aspartame, sorbitol, polysorbate 80 and benzoic acid. The list was used to determine the extent of children exposure to the harmful excipients. Considering patient factors (age, swallowing ability, treated condition), prescribed dose and availability of solid dosage forms, the included long-term liquid medicines were assessed for a potential solid form alternative by a specialist paediatric clinical pharmacist.ResultsA total of 302 oral liquid medicine formulations prescribed for 60 patients (age range 10 days – 17 years) were included in the study, of which 68.9% (208/302) were long-term oral liquid formulations. The 208 oral liquid formulation contained a total of 1044 excipients resulted in 17.4 (± 9) excipients per patients. Majority of patients (98.3%, 59/60) were exposed to at least one harmful excipient in their medicines. Children aged 2–11 years and 6–11 years were exposed the most to harmful excipients (mean 8.2 ± 4.9 exposure per patient). Parabens (81.7%, 49/60) was the most common harmful excipient patients were exposed to, followed by sorbitol (76.7%, 46/60), ethanol (75.0%, 45/60) and propylene glycol (70.0%, 42/60). Considering patient factors, prescribed dose and availability of solid formulations, it was found that almost third of the prescribed long-term oral liquid medicines (33.0%, 68/208) could be switched to tablet or capsule forms by pharmacist without any change to the prescribed dose. While for another 3.4% (7/208) long-term liquid medicines could be switched to solid dosage forms with prescriber approval, as prescribed doses would need to be adjusted slightly.ConclusionThe study highlights the extent of excipients exposure in children on long-term oral liquid medicines, many of which could potentially be harmful. Healthcare professionals should aim to reduce the long-term risks of excipients by providing an oral solid substitute to replace oral liquid formulation, where possible, and ensuring excipients are within safe, acceptable limits.ReferencesFabiano V, Mameli C, Zuccotti GV. Paediatric pharmacology: remember the excipients. Pharmacol Res 2011;63:362–365.Buckley L, Salunke S, Thompson K, et al. Challenges and strategies to facilitate formulation development of pediatric drug products: Safety qualification of excipients. Int J Pharm 2018; 536:563–569.

scholarly journals Fast Dissolving Oral Films: A Novel Trend to Oral Drug Delivery System

2016 ◽  
Vol 2 (1) ◽  
pp. 58-68 ◽  
Author(s):  
Mukem Bhattarai ◽  
Amit Kumar Gupta
Keyword(s):  
Oral Drug Delivery ◽  
Oral Care ◽  
Prescription Medication ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Oral Drug ◽  
Early 19Th Century ◽  
Conventional Tablet ◽  
Pharmaceutical Ingredients ◽  
Oral Films

Oral routes are most commonly preferred route for delivering drug. Most common oral dosage forms are tablet and capsules. But many patients such as geriatric, pediatric and dysphasic patients find difficult to swallow conventional tablet and capsule. To overcome various problems related to swallowing, Fast dissolving Tablets (FDTs) were designed in early 19th century and hence further advancement has led to development of Fast Dissolving Oral Films (FDOFs). In the recent years, many of the pharmaceutical groups are focusing their research on rapid dissolving technology. Amongst the plethora of avenues explored for rapid drug releasing product, FDOFs technology is gaining much attention. These are solid dosage forms, which disintegrate or dissolve within 1 min when placed in the mouth without drinking water or mastication. This technology has been used for local action as well as rapid release products. The fast dissolving oral films are formulated using various Active pharmaceutical ingredients (API), film forming polymers, plasticizer, flavors, colors and sweeteners. Initially FDOFs are up to breath strips, confection and oral care markets. But now it became a novel and widely accepted technology for delivering OTC and prescription medication too.Sunsari Technical College Journal 2015, 2(1):58-68

scholarly journals Combining Surface Templating and Confinement for Controlling Pharmaceutical Crystallization

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 995
Author(s):  
Manali Banerjee ◽  
Blair Brettmann
Keyword(s):  
Crystal Size ◽  
Water Solubility ◽  
Pharmaceutical Research ◽  
Oral Dosage ◽  
Free Energies ◽  
Pharmaceutical Ingredients ◽  
Surface Functionality ◽  
Dissolution Properties ◽  
Combined Crystallization ◽  
Oral Dosage Forms

Poor water solubility is one of the major challenges to the development of oral dosage forms containing active pharmaceutical ingredients (APIs). Polymorphism in APIs leads to crystals with different surface wettabilities and free energies, which can lead to different dissolution properties. Crystal size and habit further contribute to this variability. An important focus in pharmaceutical research has been on controlling the drug form to improve the solubility and thus bioavailability of APIs. In this regard, heterogeneous crystallization on surfaces and crystallization under confinement have become prominent forms of controlling polymorphism and drug crystal size and habits; however there has not been a thorough review into the emerging field of combining these approaches to control crystallization. This tutorial-style review addresses the major advances that have been made in controlling API forms using combined crystallization methods. By designing templates that not only control the surface functionality but also enable confinement of particles within a porous structure, these combined systems have the potential to provide better control over drug polymorph formation and crystal size and habit. This review further provides a perspective on the future of using a combined crystallization approach and suggests that combining surface templating with confinement provides the advantage of both techniques to rationally design systems for API nucleation.

scholarly journals REVIEW: FAST DISSOLVING TABLET

2018 ◽  
Vol 10 (2) ◽  
pp. 5
Author(s):  
Aher Smita S. ◽  
Saudagar R. B. ◽  
Shinde Mayuri S.
Keyword(s):  
Dosage Form ◽  
Geriatric Patients ◽  
Oral Route ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Solid Dosage Forms ◽  
Solid Dosage ◽  
Tablet Disintegration ◽  
Physical And Chemical ◽  
Pass Metabolism

Fast dissolving tablets is one of the most widely accepted dosage forms and also most popular dosage form, especially for pediatric patients because of incomplete development of the muscular and nervous system and a case of geriatric patients suffering from Parkinson’s disorder or hand tremors. Some solid dosage forms like tablets and capsules are present days facing the problems like difficulty in swallowing (dysphagia), resulting in many incidences of non-compliance and making the therapy ineffective. Oral dosage form and oral route are the most preferred route of administration for various drugs have limitations like the first-pass metabolism. Fast dissolving tablets are one of them. FDT have benefits such as accurate dosing, easy portability and manufacturing, good physical and chemical stability and an ideal alternative for pediatric and geriatric patients. Some tablets are designed to dissolve fastly in saliva, within a few seconds, and are true fast-dissolving tablets. Others contain agents to enhance the rate of tablet disintegration in the oral cavity and are more appropriately termed fast-disintegrating tablets, as they may take up to a minute to completely disintegrate.

scholarly journals Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update

Pharmaceutics ◽  
2019 ◽  
Vol 11 (1) ◽  
pp. 41 ◽  
Author(s):  
Sam Maher ◽  
David Brayden ◽  
Luca Casettari ◽  
Lisbeth Illum
Keyword(s):  
Oral Delivery ◽  
State Of The Art ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Active Pharmaceutical Ingredients ◽  
Permeation Enhancers ◽  
Pharmaceutical Ingredients ◽  
Current State ◽  
Oral Formulations ◽  
Oral Dosage Forms

The application of permeation enhancers (PEs) to improve transport of poorly absorbed active pharmaceutical ingredients across the intestinal epithelium is a widely tested approach. Several hundred compounds have been shown to alter the epithelial barrier, and although the research emphasis has broadened to encompass a role for nanoparticle approaches, PEs represent a key constituent of conventional oral formulations that have progressed to clinical testing. In this review, we highlight promising PEs in early development, summarize the current state of the art, and highlight challenges to the translation of PE-based delivery systems into safe and effective oral dosage forms for patients.

Primordial science and pioneering approaches of guggul for chronic ailments – A modernized review

2020 ◽  
Vol 7 (2) ◽  
pp. 14-20
Author(s):  
Jamal Basha D ◽  
Kumar P R ◽  
Ranganayakulu D
Keyword(s):  
Water Solubility ◽  
Therapeutic Potential ◽  
Chemical Constituents ◽  
Signs And Symptoms ◽  
Dosage Forms ◽  
The Novel ◽  
Lipids Metabolism ◽  
Clinical Conditions ◽  
Novel Drug ◽  
Conventional Dosage

An oleo gum resin guggulu is a product which obtained as a result of gummosis from the bark of Commiphora wightii (Arnott) Bhandari [syn. Commiphoramukul (Hook. Ex Stocks) Family, Burseraceae]. It has been known for its immense applicability in the Ayurveda since time immemorial for the treatment of variety of disorders such as inflammation, gout, rheumatism, impotence, leprosy, obesity, and disorders of lipids metabolism. It is a mixture of phytoconstituents like terpenoids, steroids, flavonoids, guggultetrols, lignans, sugars, and amino acids. This review is an effort to compile all the information available on all of its chemical constituents which are responsible for its therapeutic potential, limitation of guggul extracts and the necessity of novel principles for gum guggul. Nowadays, Guggul is available as the marketed formulation for curing numerous clinical conditions and is accessible in combination with various other ingredients. Though conventional dosage form shows the dominance as patient compliance and easy availability, yet it has found to pose the problems like dose fluctuation, peak-valley effect, non-adjustment of the administered drug, invasiveness etc. Guggul lacks its desired effect due to its low bioavailability and water solubility. This makes it a partial or a deficient therapy for remedy of many signs and symptoms. Novel drug delivery system (NDDS), a new approach and has excluded many of drawbacks exhibited by conventional dosage forms. Some of the novel dosage forms of guggul has been formed like nanoparticles, nanovesicles, gugglusomes and proniosomal gel. But still, the novel formulations for guggul has its less outspread in the market. Guggul can be executed as a profitable drug using NDDS. There is a need to highlight the unidentified and unexplained facts about guggul so as to make it more efficacious and effective in terms of bioavailability and aqueous insolubility.

Application of Pregelatinized Meal of Rice and Sorghum in the Preparation of Instant Soups: Centesimal Characterization, Technological, Microbiological and Sensory Quality

2019 ◽  
Vol 15 ◽  
Author(s):  
Gomes Acg ◽  
Lima Mcpm ◽  
Caliari M ◽  
Alves Dg ◽  
Machado Alb ◽  
...  
Keyword(s):  
Fast Food ◽  
Water Solubility ◽  
Potato Starch ◽  
Rice Flour ◽  
Extrusion Process ◽  
Experimental Development ◽  
Sorghum Flour ◽  
Predicted Values ◽  
Experimental Values ◽  
Physical And Chemical

Due to the technological importance that the extrusion process represents in the application of fast food, the objective of this work was to apply pregelatinized rice and sorghum flours in the development of an instant preparation soup and to evaluate its centesimal, technological, and their sensorial analysis. Ten formulations of the instant soup were prepared from the mixtures experimental design. According to the experimental results, it can be stated that the predicted values corroborated with the experimental values, that is, a mixture was obtained for the instant soup with the characteristics of water absorption, water solubility, color, luminosity and viscosity close to the predicted by the models. After the physical and chemical analysis, the microbiological characterization of the best formulation defined by the desirability test was used, which demonstrated that the product is suitable to microbiological standards. The results obtained showed that the 80:10:10 instant soup formulation of pregelatinized rice flour, pregelatinized sorghum flour and potato starch allowed the experimental development of a new product with good nutritional characteristics benefits. It was obtained a food with good technological characteristics solubility and absorption in water, good viscosity, light color and with good sensory acceptance by the tasters.

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