Medicated Straws Based on Electrospun Solid Dispersions

Novel medicated straws were developed based on drug-loaded electrospun fibers prepared by direct current electrospinning (DCES) and high-speed electrospinning (HSES) of scaled-up productivity. Good quality micro- and nanofibers were electrospun using both techniques despite the multiple times higher throughput rate of HSES based on the scanning electron microscopic imaging (SEM). Solid state analyses revealed that the poorly soluble model drug carvedilol (CAR) was dispersed in an amorphous form in the electrospun polyvinylpyrrolidone (PVPK30) fibers. In vitro dissolution studies revealed ultrafast drug release from the prepared fibrous formulations inserted into plastic straws. Based on the results the developed drug delivery system is suitable for storing the formulation in a solid dosage form and in situ turning it into liquid form when administered.

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Electrosprayed Microparticulate Solid Dispersions Composed of Multiple Components

Applied Mechanics and Materials ◽

10.4028/www.scientific.net/amm.513-517.259 ◽

2014 ◽

Vol 513-517 ◽

pp. 259-264

Author(s):

Wei Qian ◽

Deng Guang Yu ◽

Lu Wang ◽

Shuo Lei Li ◽

Yi Fan Wang ◽

...

Keyword(s):

Solid Dispersions ◽

Sodium Dodecyl ◽

Active Pharmaceutical Ingredient ◽

Scanning Calorimetry ◽

Electron Microscopic ◽

Multiple Components ◽

Rapid Dissolution ◽

Poorly Soluble ◽

Average Size

An electrospraying process was developed for fabricating a new type of microparticulate third generation solid dispersions (SDs) composed of multiple components with ferulic acid (FA) as a model active pharmaceutical ingredient. The spraying fluids were the co-dissolving solutions of FA, polyvinylpyrrolidone K25 (PVP K25) and sodium dodecyl sulfate (SDS) in 95% ethanol aqueous solutions. Field emission scanning electron microscopic observations showed that the microparticles had an average size of 1.47 ± 0.75 μm. Results from the differential scanning calorimetry analyses suggested that FA and SDS were distributed in the polymer matrix in an amorphous status owing to the compatibility among components resulted from the second-order interactions, as verified by attenuated total reflectance Fourier transform infrared spectra.In vitrodissolution tests demonstrated that the microparticulate SDs could release all the contained FA within 1 minute, extremely faster than the raw FA particles. It can be concluded that electrospraying is a useful tool for creating new generation SDs composed of multiple components for enhancing the rapid dissolution of poorly soluble drugs.

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Bioavailability and Biological Disposition of Methaqualone*

Journal of International Medical Research ◽

10.1177/030006057400200201 ◽

1974 ◽

Vol 2 (2) ◽

pp. 85-99 ◽

Cited By ~ 8

Author(s):

Robert D Smyth ◽

Pramod B Chemburkar ◽

P P Mathur ◽

A F DeLong ◽

A Polk ◽

...

Keyword(s):

Intestinal Tract ◽

Chronic Administration ◽

Dosage Forms ◽

In Vitro Dissolution ◽

Elimination Kinetics ◽

Solid Dosage ◽

Liver And Kidney ◽

Gastro Intestinal Tract

The absorption of methaqualone from the gastro-intestinal tract is a dissolution—and not a permeability-rate limited process. Absorption from solution dosage forms can occur throughout the gastro-intestinal tract with maximum absorption from the intestine. Dissolution of solid dosage forms is favoured in the highly-acidic environment of the stomach and absorption of the in situ dissolved drug occurs in both stomach and upper small intestine. Methaqualone is found primarily in the plasma phase of whole blood and is highly bound to plasma proteins. The plasma elimination curve is biexponential with a rapid distributive phase and a slow elimination phase. The principle tissues of distribution are the metabolic and excretory tissues—liver and kidney — and lipid tissue. Metabolism occurs by hydroxylation of the methyl, tolyl and quinazolinone substituents via inducible hepatic microsomal oxidoreductases. Methaqualone is completely bio-transformed and excreted as O-glucuronide conjugates in urine and bile. Enterohepatic recirculation of metabolites occurs and is responsible for the prolonged urinary excretion profile. There is no change in absorption, distribution or elimination kinetics following chronic administration in man. Tablet and capsule formulations with good in vitro dissolution, stability and bioavailability characteristics were developed. Equivalent bioavailability of these tablet formulations was observed in the fasted and post-prandial state. Techniques were developed to correlate dissolution and absorption profiles of these formulations.

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An Overview: The Evaluation of Formation Mechanisms, Preparation Techniques and Chemical and Analytical Characterization Methods of the In Situ Forming Implants

Current Pharmaceutical Analysis ◽

10.2174/1573412916999200616125009 ◽

2020 ◽

Vol 16 ◽

Author(s):

Muge Kilicarslan ◽

Ayse Nur Buke

Keyword(s):

New Technologies ◽

In Vitro Dissolution ◽

Formation Mechanisms ◽

Liquid Form ◽

Characterization Methods ◽

Advantages And Disadvantages ◽

In Situ Forming

: One of the major developments of the last decade is the preparation of in situ forming implant formulations. Injectable, biocompatible and/or biodegradable polymer based in situ implants are classified differently due to implant formation based on in vivo solid depot or formation mechanisms inducing liquid form, gel or solid depot. In this review, published studies to date regarding in situ forming implant systems were compiled and their formation mechanisms, materials and methods used, routes of administration, chemical and analytical characterizations, quality control tests and in vitro dissolution tests were compared in Tables and they were evaluated. There are several advantages and disadvantages of these dosage forms due to the formation mechanism, polymer and solvent type and the ratio used in formulations and all of these parameters were discussed separately. In addition, new generation systems developed to overcome the difficulties encountered in in situ implants have been evaluated. There are, some approved products of in situ implant preparations that can be used for different indications are available on the market and the clinical phase studies nowadays. In vitro and in vivo data obtained by the analysis of the application of new technologies in many studies evaluated in this review showed that the number of approved drugs to be used for various indications with different drugs would increase in the future.

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Obtaining Cocrystals by Reaction Crystallization Method: Pharmaceutical Applications

Pharmaceutics ◽

10.3390/pharmaceutics13060898 ◽

2021 ◽

Vol 13 (6) ◽

pp. 898

Author(s):

Isabela Fanelli Barreto Biscaia ◽

Samantha Nascimento Gomes ◽

Larissa Sakis Bernardi ◽

Paulo Renato Oliveira

Keyword(s):

Large Scale ◽

In Vitro Dissolution ◽

Supersaturated Solution ◽

Scale Production ◽

In Situ Techniques ◽

Crystallization Method ◽

Large Scale Production ◽

Poorly Soluble

Cocrystals have gained attention in the pharmaceutical industry due to their ability to improve solubility, stability, in vitro dissolution rate, and bioavailability of poorly soluble drugs. Conceptually, cocrystals are multicomponent solids that contain two or more neutral molecules in stoichiometric amounts within the same crystal lattice. There are several techniques for obtaining cocrystals described in the literature; however, the focus of this article is the Reaction Crystallization Method (RCM). This method is based on the generation of a supersaturated solution with respect to the cocrystal, while this same solution is saturated or unsaturated with respect to the components of the cocrystal individually. The advantages of the RCM compared with other cocrystallization techniques include the ability to form cocrystals without crystallization of individual components, applicability to the development of in situ techniques for the screening of high quality cocrystals, possibility of large-scale production, and lower cost in both time and materials. An increasing number of scientific studies have demonstrated the use of RCM to synthesize cocrystals, mainly for drugs belonging to class II of the Biopharmaceutics Classification System. The promising results obtained by RCM have demonstrated the applicability of the method for obtaining pharmaceutical cocrystals that improve the biopharmaceutical characteristics of drugs.

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Mucilage of Coccinia grandis as an Efficient Natural Polymer-Based Pharmaceutical Excipient

Polymers ◽

10.3390/polym14010215 ◽

2022 ◽

Vol 14 (1) ◽

pp. 215

Author(s):

Kumbakonam Balachandran Ilango ◽

Senguttuvan Gowthaman ◽

Kumbakonam Ilango Seramaan ◽

Kumarappan Chidambaram ◽

Mohammad F. Bayan ◽

...

Keyword(s):

In Vitro Cytotoxicity ◽

In Vitro Dissolution ◽

Disintegration Time ◽

Solid Dosage ◽

Coccinia Grandis ◽

Synthetic Materials ◽

Cytotoxicity Studies ◽

Model Drug ◽

Instrumental Methods

Natural eco-friendly materials are recently employed in products to replace synthetic materials due to their superior benefits in preserving the environment. The herb Coccinia grandis is widely distributed in continents like Asia and Africa and used traditionally to treat fever, leprosy, asthma, jaundice, and bronchitis. Mucilage of Coccinia grandis was accordingly extracted, isolated by a maceration technique, and precipitated. The mucilage was evaluated for its physicochemical, binding, and disintegrant properties in tablets using paracetamol as a model drug. The crucial physicochemical properties such as flow properties, solubility, swelling index, loss on drying, viscosity, pH, microbial load, cytotoxicity was evaluated and the compatibility was analyzed using sophisticated instrumental methods (TGA, DTA, DSC, and FTIR). The binding properties of the mucilage was used at three different concentrations and compared with starch and PVP as examples of standard binders. The disintegrant properties of mucilage were used at two different concentrations and compared with standard disintegrants MCCP, SSG, and CCS. The tablets were punched and evaluated for their hardness, friability, assay, disintegration time, in vitro dissolution profiles. In vitro cytotoxicity studies of the mucilage were performed in a human embryonic kidney (HEK) cell line. The outcome of the study indicated that the mucilage had good performance compared with starch and PVP. Further, the mucilage acts as a better disintegrant than MCCP, SSG and CCS for paracetamol tablets. Use of a concentration of 3% or less demonstrated the ability of the mucilage to act as a super disintegrating agent and showed faster disintegration and dissolution, which makes it as an attractive, promising disintegrant in formulating solid dosage forms to improve the therapeutic efficacy and patient compliance. Moreover, the in vitro cytotoxicity evaluation results demonstrated that the mucilage is non-cytotoxic to human cells and is safe.

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Formulation and Evaluation of Microbially- triggered tablets of Valdecoxib

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v2i1.8841 ◽

2010 ◽

Vol 2 (1) ◽

Author(s):

Surender Verma ◽

S. Singh ◽

D. Mishra ◽

Atul Gupta ◽

Rakesh Sharma

Keyword(s):

Phosphate Buffer ◽

Guar Gum ◽

Oral Route ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Wet Granulation ◽

Dissolution Study ◽

Caecal Content ◽

Model Drug

The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher amount of drug which was also significantly higher than the dissolution media of same pH without caecal content (microflora) and it was concluded that guar gum can be used as a potential carrier for targeting drugs to colon.

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Influence of β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin on Enhancement of Solubility and Dissolution of Isradipine

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.3.8 ◽

2017 ◽

Vol 10 (3) ◽

pp. 3752-3757

Author(s):

Narendar D ◽

Ettireddy S

Keyword(s):

Inclusion Complex ◽

Dissolution Rate ◽

Solid Dispersions ◽

Physical Stability ◽

Molecular Complexes ◽

In Vitro Dissolution ◽

Molar Ratio ◽

Phase Solubility ◽

Cyclodextrin Complexation

The content of this investigation was to study the influence of β-cyclodextrin and hydroxy propyl-β-cyclodextrin complexation on enhancement of solubility and dissolution rate of isradipine. Based on preliminary phase solubility studies, solid complexes prepared by freeze drying method in 1:1 molar ratio were selected and characterized by DSC for confirmation of complex formation. Prepared solid dispersions were evaluated for drug content, solubility and in vitro dissolution. The physical stability of optimized formulation was studied at refrigerated and room temperature for 2 months. Solid state characterization of optimized complex performed by DSC and XRD studies. Dissolution rate of isradipine was increased compared with pure drug and more with HP-β-CD inclusion complex than β-CD. DSC and XRD analyzes that drug was in amorphous form, when the drug was incorporated as isradipine β-CD and HP-β-CD inclusion complex. Stability studies resulted in low or no variations in the percentage of complexation efficiency suggesting good stability of molecular complexes. The results conclusively demonstrated that the enhancement of solubility and dissolution rate of isradipine by drug-cyclodextrin complexation was achieved.

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In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

Medical Principles and Practice ◽

10.1159/000516299 ◽

2021 ◽

Author(s):

Mohsen Hedaya ◽

Farzana Bandarkar ◽

Aly Nada

Keyword(s):

Particle Size ◽

Tween 80 ◽

Aqueous Solubility ◽

In Vitro Dissolution ◽

In Vivo Evaluation ◽

Poorly Soluble ◽

Extent Of Absorption ◽

Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

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