Dissolution Testing:<i>In vitro</i>Characterization of Oral Controlled Release Dosage Forms

Guo, Michele Xuemei

doi:10.1002/9780470640487.ch15

Cited by 4 publications

(2 citation statements)

References 48 publications

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“…Third generation: The new technologies for drug delivery are delivery of poorly water-soluble drugs, long-term and non-invasive technology for delivering protein/nucleic acid/peptide, drug delivery to the targeted site using nanoparticles and the drug delivered through self-regulation [ 47 ]. Table 7 shows the evolution of controlled drug delivery systems [ 63 , 64 ].…”

Section: Controlled Release Dosage Form Design: Practical Considerationsmentioning

confidence: 99%

Controlled Drug Delivery Systems: Current Status and Future Directions

2021

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The drug delivery system enables the release of the active pharmaceutical ingredient to achieve a desired therapeutic response. Conventional drug delivery systems (tablets, capsules, syrups, ointments, etc.) suffer from poor bioavailability and fluctuations in plasma drug level and are unable to achieve sustained release. Without an efficient delivery mechanism, the whole therapeutic process can be rendered useless. Moreover, the drug has to be delivered at a specified controlled rate and at the target site as precisely as possible to achieve maximum efficacy and safety. Controlled drug delivery systems are developed to combat the problems associated with conventional drug delivery. There has been a tremendous evolution in controlled drug delivery systems from the past two decades ranging from macro scale and nano scale to intelligent targeted delivery. The initial part of this review provides a basic understanding of drug delivery systems with an emphasis on the pharmacokinetics of the drug. It also discusses the conventional drug delivery systems and their limitations. Further, controlled drug delivery systems are discussed in detail with the design considerations, classifications and drawings. In addition, nano-drug delivery, targeted and smart drug delivery using stimuli-responsive and intelligent biomaterials is discussed with recent key findings. The paper concludes with the challenges faced and future directions in controlled drug delivery.

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Section: Controlled Release Dosage Form Design: Practical Considerationsmentioning

confidence: 99%

Controlled Drug Delivery Systems: Current Status and Future Directions

2021

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“…For oral and transdermal systems, the relationships between in vitro drug release kinetics and in vivo bioavailability are fairly well understood. Once the in vitro-in vivo correlation (IVIVC) of a formulation is established, other formulations using different mechanisms can be easily produced with an expectation that the new systems will be as effective as the reference formulation [11, 12]. For most drug delivery systems developed in the 1G period, mainly for oral and transdermal delivery, understanding the physicochemical properties (e.g., in vitro drug release kinetics) was enough for developing clinically useful formulations.…”

Section: Differences Between 1g and 2g Drug Delivery Technologiesmentioning

confidence: 99%

Controlled Drug Delivery: Historical perspective for the next generation

Yun

Lee

Park

2015

Journal of Controlled Release

288

166

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The modern day drug delivery technology is only 60 years old. During this period numerous drug delivery systems have been developed. The first generation (1950–1980) has been very productive in developing many oral and transdermal controlled release formulations for clinical applications. On the other hand, the second generation (1980–2010) has not been as successful in generating clinical products. This is in large part due to the nature of the problems to overcome. The first generation of drug delivery technologies dealt with physicochemical problems, while the second struggled with biological barriers. Controlled drug delivery systems can be made with controllable physicochemical properties, but they cannot overcome the biological barriers. The third generation (from 2010) drug delivery systems need to overcome both physicochemical and biological barriers. The physicochemical problems stem from poor water solubility of drugs, large molecular weight of peptide and protein drugs, and difficulty of controlling drug release kinetics. The biological barriers to overcome include distribution of drug delivery systems by the body rather than by formulation properties, limiting delivery to a specific target in the body. In addition, the body's reaction to formulations limits their functions in vivo. The prosperous future of drug delivery systems depends on whether new delivery systems can overcome limits set by human physiology, and the development process can be accelerated with new ways of thinking.

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Recent advances in improving oral drug bioavailability by cocrystals

et al. 2018

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Introduction: Oral drug delivery is the most favored route of drug administration. However, poor oral bioavailability is one of the leading reasons for insufficient clinical efficacy. Improving oral absorption of drugs with low water solubility and/or low intestinal membrane permeability is an active field of research. Cocrystallization of drugs with appropriate coformers is a promising approach for enhancing oral bioavailability. Methods: In the present review, we have focused on recent advances that have been made in improving oral absorption through cocrystallization. The covered areas include supersaturation and its importance on oral absorption of cocrystals, permeability of cocrystals through membranes, drug-coformer pharmacokinetic (PK) interactions, conducting in vivo-in vitro correlations for cocrystals. Additionally, a discussion has been made on the integration of nanocrystal technology with supramolecular design. Marketed cocrystal products and PK studies in human subjects are also reported. Results: Considering supersaturation and consequent precipitation properties is necessary when evaluating dissolution and bioavailability of cocrystals. Appropriate excipients should be included to control precipitation kinetics and to capture solubility advantage of cocrystals. Beside to solubility, cocrystals may modify membrane permeability of drugs. Therefore, cocrystals can find applications in improving oral bioavailability of poorly permeable drugs. It has been shown that cocrystals may interrupt cellular integrity of cellular monolayers which can raise toxicity concerns. Some of coformers may interact with intestinal absorption of drugs through changing intestinal blood flow, metabolism and inhibiting efflux pumps. Therefore, caution should be taken into account when conducting bioavailability studies. Nanosized cocrystals have shown a high potential towards improving absorption of poorly soluble drugs. Conclusions: Cocrystals have found their way from the proof-of-principle stage to the clinic. Up to now, at least two cocrystal products have gained approval from regulatory bodies. However, there are remaining challenges on safety, predicting in vivo behavior and revealing real potential of cocrystals in the human.

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Dissolution Testing:In vitroCharacterization of Oral Controlled Release Dosage Forms

Cited by 4 publications

References 48 publications

Controlled Drug Delivery Systems: Current Status and Future Directions

Controlled Drug Delivery Systems: Current Status and Future Directions

Controlled Drug Delivery: Historical perspective for the next generation

Recent advances in improving oral drug bioavailability by cocrystals

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