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1.
J Pharm Sci ; 2024 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-39374694

RESUMO

Amorphous solid dispersion (ASD) tablets based on hydrophilic polymer carriers may encounter disintegration challenges. In this work, the effect of different formulation composition variables on the ASD tablet disintegration performance was systematically studied. GDC-0334: copovidone (PVPVA) 60: 40 ASD prepared by spray drying was selected as the model ASD system. The effects of ASD loading, filler type and ratio, disintegrant type and level were then investigated using tablets made by direct compression process. Tablet disintegration time increased with the increase of ASD loading, especially when ASD loading exceeded 50%. At the same tablet solid fraction, when lactose was used as the soluble filler, faster tablet disintegration time was observed compared to the tablets with mannitol as the soluble filler. Among the three tested disintegrants, croscarmellose sodium performed the best in facilitating the ASD tablet disintegration, followed by sodium starch glycolate, and crospovidone was the poorest. When croscarmellose sodium was used as the disintegrant, 5% level was sufficient to enable ASD tablet disintegration at 60% ASD loading and further increase of croscarmellose sodium level to 8% did not provide additional benefit. Water uptake experiments were performed on selected tablets and the results demonstrated a positive correlation with tablet disintegration time, indicating water penetration is a major contributing step for the disintegration of our ASD tablets. Overall, this work provides a rationale for excipient selection and insights into building a platform formulation approach for developing immediate-release ASD tablets.

2.
Biomed Res Int ; 2024: 4875984, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39364267

RESUMO

Three-dimensional printing (3DP) has emerged as a game-changing technology in the pharmaceutical industry, providing novel formulation development in the pharmaceutical sector as a whole, which improved patients' individualized therapy. The pediatric population is among the key targets for individualized therapy. Children are a diverse group that includes neonates, infants, and toddlers, each with unique physiological characteristics. Treatment adherence has a significant impact on safe and effective pharmacotherapy in the pediatric population. Improvement of therapeutic dosage forms that provide for the special demands of the pediatric population is a significant challenge for the pharmaceutical industry. Scientists have actively explored 3DP, a quick prototype manufacturing method that has emerged in recent years from many occupations due to its benefits of modest operation, excellent reproducibility, and vast adaptability. This review illuminates the most widely used 3DP technology and its application in the development of pediatric-friendly drug formulations. This 3DP technology allows optimization of pediatric dosage regimens and cases that require individualized treatment, such as geriatrics, renal impairment, liver impairment, critically ill, pregnancy populations, and drugs with nonlinear pharmacokinetics. The fast evolution of 3DP expertise, in addition to the introduction of pharmaceutical inks, has enormous promise for patient dosage form customization.


Assuntos
Impressão Tridimensional , Humanos , Criança , Composição de Medicamentos/métodos , Lactente , Recém-Nascido , Pré-Escolar , Pediatria/métodos , Preparações Farmacêuticas/química , Preparações Farmacêuticas/administração & dosagem
3.
Curr Pharm Des ; 2024 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-39279110

RESUMO

Additive manufacturing, sometimes referred to as 3D printing or AM, has numerous applications in industries like manufacturing, aviation, aerospace, vehicles, and education. It has recently made considerable inroads into the healthcare industry, backed by technology breakthroughs such as fused deposition modeling, binder jetting, and inkjet printing. A variety of biomaterials, such as polycaprolactone, polycarbonate, polypropylene, and polylactic acid, have contributed to this increase. This essay delves into the revolutionary possibilities of 3D printing in healthcare, to shed light on the idea of customized medications via the improvement of efficiency and cost. Researchers are using polymers and additive manufacturing to make customized medical devices. However, obstacles including bureaucratic hurdles, technological developments, and the choice of appropriate materials and printers stand in the way of widespread implementation. To fully realize the promise of 3D printing in healthcare, these challenges must be overcome. The article highlights the revolutionary potential of 3D printing in healthcare by following its development from art and construction to customized drugs and patient-specific medical equipment. In addition to addressing issues like quality control and technological limitations, it emphasizes its wide range of applications in surgical planning, dentistry, and anatomical models. The necessity of adapting regulations and instructional programs is highlighted by discussing future trends like bioprinting and FDA-approved innovations. In order to properly utilize 3D printing in healthcare, this adaption is essential. Personalized prescriptions and increased efficacy from the incorporation of 3D printing could revolutionize the healthcare industry. But even with these advances, problems like choosing the right materials and getting over administrative roadblocks prevent widespread implementation. These challenges need to be successfully overcome for 3D printing in healthcare to reach its full potential.

4.
Molecules ; 29(17)2024 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-39275042

RESUMO

The emergence of natural products has provided extremely valuable references for the treatment of various diseases. Cucurbitacin B, a tetracyclic triterpenoid compound isolated from cucurbitaceae and other plants, is the most abundant member of the cucurbitin family and exhibits a wide range of biological activities, including anti-inflammatory, anti-cancer, and even agricultural applications. Due to its high toxicity and narrow therapeutic window, structural modification and dosage form development are necessary to address these issues with cucurbitacin B. This paper reviews recent research progress in the pharmacological action, structural modification, and application of cucurbitacin B. This review aims to enhance understanding of advancements in this field and provide constructive suggestions for further research on cucurbitacin B.


Assuntos
Triterpenos , Triterpenos/química , Triterpenos/farmacologia , Humanos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Animais , Cucurbitaceae/química , Estrutura Molecular , Relação Estrutura-Atividade , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia
5.
Front Pharmacol ; 15: 1429050, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39309003

RESUMO

Berberine (BBR) is a natural alkaloid, which has played an important role in the field of medicine since its discovery in the late 19th century. However, the low availability of BBR in vivo prevents its full effect. In recent years, a large number of studies confirmed that BBR has a protective effect on the nervous system through various functions, yet the issue of the inability to systematically understand the protection of BBR on the nervous system remains a gap that needs to be addressed. Many existing literature introductions about berberine in neurodegenerative diseases, but the role of berberine in the nervous system goes far beyond these. Different from these literatures, this review is divided into three parts: preparation method, mechanism, and therapeutic effect. Various dosage forms of BBR and their preparation methods are added, in order to provide a reasonable choice of BBR, and help to solve the problem of low bioavailability in treatment. More importantly, we more comprehensively summarize the mechanism of BBR to protect the nervous system, in addition to the treatment of neurodegenerative diseases (anti-oxidative stress, anti-neuroinflammation, regulation of apoptosis), two extra mechanisms of berberine for the protection of the nervous system were also introduced: bidirectional regulation of autophagy and promote angiogenesis. Also, we have clarified the precise mechanism by which BBR has a therapeutic effect not only on neurodegenerative illnesses but also on multiple sclerosis, gliomas, epilepsy, and other neurological conditions. To sum up, we hope that these can evoke more efforts to comprehensively utilize of BBR nervous system, and to promote the application of BBR in nervous system protection.

6.
Polymers (Basel) ; 16(18)2024 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-39339030

RESUMO

Additive manufacturing of pharmaceutical formulations offers advanced micro-structure control of oral solid dose (OSD) forms targeting not only customised dosing of an active pharmaceutical ingredient (API) but also custom-made drug release profiles. Traditionally, material extrusion 3D printing manufacturing was performed in a two-step manufacturing process via an intermediate feedstock filament. This process was often limited in the material space due to unsuitable (brittle) material properties, which required additional time to develop complex formulations to overcome. The objective of this study was to develop an additive manufacturing MicroFactory process to produce an immediate release (IR) OSD form containing 250 mg of mefenamic acid (MFA) with consistent drug release. In this study, we present a single-step additive manufacturing process employing a novel, filament-free melt extrusion 3D printer, the MicroFactory, to successfully print a previously 'non-printable' brittle Soluplus®-based formulation of MFA, resulting in targeted IR dissolution profiles. The physico-chemical properties of 3D printed MFA-Soluplus®-D-sorbitol formulation was characterised by thermal analysis, Fourier Transform Infrared spectroscopy (FTIR), and X-ray Diffraction Powder (XRPD) analysis, confirming the crystalline state of mefenamic acid as polymorphic form I. Oscillatory temperature and frequency rheology sweeps were related to the processability of the formulation in the MicroFactory. 3D printed, micro-structure controlled, OSDs showed good uniformity of mass and content and exhibited an IR profile with good consistency. Fitting a mathematical model to the dissolution data correlated rate parameters and release exponents with tablet porosity. This study illustrates how additive manufacturing via melt extrusion using this MicroFactory not only streamlines the manufacturing process (one-step vs. two-step) but also enables the processing of (brittle) pharmaceutical immediate-release polymers/polymer formulations, improving and facilitating targeted in vitro drug dissolution profiles.

7.
Int J Pharm ; 663: 124498, 2024 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-39187424

RESUMO

This work presents an indicator-based assessment of potential supply risks for pharmaceutical excipients. The assessment was conducted systematically through the steps of survey, data collection, and indicator value calculation. Japan was specified as the target, and all marketed products were analyzed. As the basis of the indicator, the Herfindahl-Hirschman index (HHI), a well-established method for measuring market concentration in economics, was adopted. Modifications were made to enable comparison of the risk levels of compounds, dosage forms, and diseases. Case studies were performed on each of these levels, and recommendations were obtained for risk mitigation. On the compound level, magnesium stearate, a commonly used lubricant, showed the highest risk, and a switch to alternative compounds was recommended. The dosage-form level evaluation showed that tablets and capsules could have higher risk levels than granules, indicating the importance of diversification. Finally, the disease-level evaluation showed that the supply of adult disease drugs might be risky because of the frequent use of tablets; less reliance on tablet forms was advised for adult diseases.


Assuntos
Excipientes , Excipientes/química , Japão , Medição de Risco , Preparações Farmacêuticas/química , Comprimidos , Humanos , Formas de Dosagem
8.
Front Pharmacol ; 15: 1404259, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39119615

RESUMO

Objective: With the modernization of traditional Chinese medicine (TCM) industry, the investment in research and development of new commercial Chinese polyherbal preparations (CCPPs) is increasing, and the varieties of CCPPs are growing. CCPPs play an increasingly important role in the TCM industry. This study has comprehensively summarized and analyzed the current situation of CCPPs that has been on the market in China, and provided suggestions for the research and promotion of CCPPs. Methods: This study took the CCPPs approved for marketing in domestic drug database of the National Medical Products Administration (NMPA) as the research object, and combined with the publication of related randomized controlled trials (RCTs) of CCPPs in 2020-2022 and the sales of CCPPs in domestic chain pharmacies, statistical analysis was carried out on the drug name, pharmaceutical companies, dosage form, number of flavors, CBDs, ICD-11 classification of diseases treated, etc. Results: Currently, 58,409 approvals for CCPPs have been issued in China, involving 9,986 varieties of CCPPs, 2,896 pharmaceutical companies and 39 dosage forms. The number of flavors of prescriptions of CCPPs varies from 1 to 90, among which Glycyrrhiza glabra L. [Fabaceae; Glycyrrhizae radix et rhizoma] and Angelica sinensis (Oliv.) Diels [Apiaceae; Angelicae sinensis radix] are the most widely used. The study found that the CCPPs with the most diverse variety is CCPPs for the treatment of respiratory diseases, some CCPPs can treat multiple system diseases. According to the survey, the sales of CCPPs for respiratory diseases in the chain pharmacies account for more than 1/3 of the total sales of the chain pharmacies, while the number of published randomized controlled trials (RCTs) on CCPPs for circulatory diseases was the largest. Conclusion: The approval process of CCPPs should be further standardized, and the transformation of TCM prescriptions into CCPPs should be promoted. In the approval process of CCPPs, it is suggested to strengthen the supervision of drug names to clarify the differences between the CCPPs of same name but different prescriptions. Improve the effectiveness and safety of CCPPs by improving the quality of CBDs. It is suggested to optimize the design of new drug research program of CCPPs to avoid waste of research resources.

9.
J AOAC Int ; 2024 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-39067039

RESUMO

BACKGROUND: The National Institute of Standards and Technology (NIST) has produced over 40 botanical dietary supplement Standard Reference Materials® (SRMs) and reference materials (RMs) with values assigned for chemical markers and/or active compounds. Although environmental accumulation or inadvertent introduction of toxic elements (arsenic, cadmium, lead, and mercury) is a potential source of exposure in botanical dietary supplement products, the majority of the dietary supplement SRMs/RMs do not have values assigned for the four major toxic elements. OBJECTIVE: To determine As, Cd, Pb, and Hg content in the current inventory of NIST botanical dietary supplement SRMs/RMs. METHODS: Fifteen SRMs/RMs suites of plant part, extract, and finished products [i.e., solid oral dosage form (SODF)] were analyzed for As, Cd, Pb, and Hg using nitric acid microwave-assisted digestion followed by quantification using inductively coupled plasma-mass spectrometry. RESULTS: Results for control samples were in good agreement with certified values indicating that the analyses of 38 individual botanical SRMs/RMs were in control. Characterization of linked plant/extract SRMs/RMs derived from the same source materials demonstrated that while extraction processes can often yield extracts with lower toxic element content for Hg or As, it is also possible for mass fraction levels to remain unchanged or even increase following extraction. CONCLUSION: The results fill significant knowledge gaps in toxic element content ranges for SRMs/RMs where no NIST assigned values existed, in particular for Hg content and for extract and SODF matrices. With comprehensive toxic element content now available, researchers can better select appropriate dietary supplement SRMs/RMs for use as controls in the analysis of dietary supplement ingredients and products. HIGHLIGHTS: Results for As, Cd, Pb, and Hg are reported for 38 dietary supplement SRMs/RMs including 6 suites of plant, extract, and SODF and 9 pairs of plant and extract from the same batch of plant material.

10.
Pharmaceutics ; 16(6)2024 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-38931818

RESUMO

Archaeosomes were manufactured from natural archaeal lipids by a microfluidics-assisted single-step production method utilizing a mixture of di- and tetraether lipids extracted from Sulfolobus acidocaldarius. The primary aim of this study was to investigate the exceptional stability of archaeosomes as potential carriers for oral drug delivery, with a focus on powdered formulations. The archaeosomes were negatively charged with a size of approximately 100 nm and a low polydispersity index. To assess their suitability for oral delivery, the archaeosomes were loaded with two model drugs: calcein, a fluorescent compound, and insulin, a peptide hormone. The archaeosomes demonstrated high stability in simulated intestinal fluids, with only 5% of the encapsulated compounds being released after 24 h, regardless of the presence of degrading enzymes or extremely acidic pH values such as those found in the stomach. In a co-culture cell model system mimicking the intestinal barrier, the archaeosomes showed strong adhesion to the cell membranes, facilitating a slow release of contents. The archaeosomes were loaded with insulin in a single-step procedure achieving an encapsulation efficiency of approximately 35%. These particles have been exposed to extreme manufacturing temperatures during freeze-drying and spray-drying processes, demonstrating remarkable resilience under these harsh conditions. The fabrication of stable dry powder formulations of archaeosomes represents a promising advancement toward the development of solid dosage forms for oral delivery of biological drugs.

11.
J Pharm Biomed Anal ; 247: 116258, 2024 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-38830272

RESUMO

Film-coated modified-release tablets are an important dosage form amenable to targeted, controlled, or delayed drug release in the specific region of the gastrointestinal (GI) tract. Depending on the film composition and interaction with the GI fluid, such coated products can modulate the local bioavailability, systemic absorption, protection as an enteric barrier, etc. Although the interaction of a dosage form with the surrounding dissolution medium is vital for the resulting release behavior, the underlying physicochemical phenomena at the film and core levels occurring during the drug release process have not yet been well described. In this work, we attempted to tackle this limitation by introducing a novel in vitro test based on optical coherence tomography (OCT) that allows an in-situ investigation of the sub-surface processes occurring during the drug release. Using a commercially available tablet based on osmotic-controlled release oral delivery systems (OROS), we demonstrated the performance of the presented prototype in terms of monitoring the membrane thickness and thickness variability, the surface roughness, the core swelling behavior, and the porosity of the core matrix throughout the in vitro drug release process from OROS. The superior spatial (micron scale) and temporal (less than 10 ms between the subsequent tomograms) resolution achieved in the proposed setup provides an improved understanding of the dynamics inside the microstructure at any given time during the dissolution procedure with the previously unattainable resolution, offering new opportunities for the design and testing of patient-centric dosage forms.


Assuntos
Preparações de Ação Retardada , Liberação Controlada de Fármacos , Comprimidos , Tomografia de Coerência Óptica , Tomografia de Coerência Óptica/métodos , Preparações de Ação Retardada/química , Sistemas de Liberação de Medicamentos/métodos , Solubilidade , Administração Oral , Porosidade , Comprimidos com Revestimento Entérico/química
12.
Ann Pharm Fr ; 2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-38945392

RESUMO

OBJECTIVE: The present work represents a reverse-phase high-performance liquid chromatography method in addition to stability studies for sequential estimation of remogliflozin etabonate, vildagliptin, and metformin HCl in tablet formulation. METHOD: The mentioned method utilizes a Phenomenex Luna C18 column (250×4.6mm, 5µm). It consists of a column oven's temperature of 35°C. Mobile phase includes a mixture of 50% phosphate buffer (pH - 6.8) and 50% acetonitrile along with a flow rate of 0.8mL/min and 20minutes of run time. The injection volume was 20µL; 217nm is a detection wavelength, and a PDA detector is used for detection. RESULTS: The suggested technique was proven and validated per the ICH Q2 (R1) guideline. The combination was put under stress conditions that included acid, base, thermal, photolytic, and oxidative degradation. The combination was considerably degraded under oxidative, acidic, and basic circumstances for deterioration, and the degradation results were accurately identified from the observed peaks, demonstrating the method's effectiveness in detecting stability. CONCLUSION: The technique was quick, precise, sensitive, and accurate; as a result, it may be used in quality control laboratories and the pharmaceutical industry for routine quality monitoring of tablets containing all three medications.

13.
Eur J Pharm Sci ; 200: 106814, 2024 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-38815699

RESUMO

Dosing conditions (type and amount of accompanying fluid, the type of food, the time of administration, and dosage form modifications such as crushing tablets) are critical and affect the performance of oral dosage forms in the gastrointestinal tract and thus bioavailability. Because older adults are the primary users of medications and are more susceptible to adverse effects, it is important to understand how they take their medications in order to reduce risks and increase benefits of the pharmacotherapy. The aim of the study was to investigate the real-life drug intake behaviour in geriatric patients and older adults and discuss their influence on drug absorption after oral administration. The data from two settings home vs. hospital and genders women vs. men were presented. A questionnaire study was performed among people aged at least 65 years from two settings (hospital vs. home), recruited mostly from community pharmacies and a regional hospital in Mecklenburg - Western Pomerania. The obtained data demonstrates that older adults and geriatric patients take their medications in the same way regardless of the setting and gender. There were no significant differences. Interviewed participants were mostly adherent to the doctor's recommendations and mostly took their medications in the same way every day. Medications are most commonly taken with a small (100 mL) or large (200 mL) glass of noncarbonated water, after food (during or after breakfast 64 % of intakes in the morning and during or after dinner 81 % of intakes in the evening). Meal usually consisted of bread, either with jam or honey (breakfast), or ham and cheese (dinner). All reported dosage form modifications were made to tablets. In almost all cases it was splitting the tablet, which was performed due to doctor's indication.


Assuntos
Comprimidos , Humanos , Masculino , Idoso , Feminino , Alemanha , Idoso de 80 Anos ou mais , Administração Oral , Inquéritos e Questionários , Adesão à Medicação
14.
Curr Drug Res Rev ; 2024 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-38706363

RESUMO

Pharmaceutical excipients play a crucial role in determining the outcome of delivered therapeutic cargo density. By far, polymers have captured the biggest share in the excipients market. This surge in demand motivated researchers to look for newer and novel polymeric platforms. Interpenetrating polymeric networks (IPN) are a class of polymer in the same polymer blend league, where two different polymer chains penetrate; and align with each other without any sustainable covalent bond. The novel agreement between the polymer chains equips the IPN with the characteristic features of each participating polymer unit, thus making IPN superior to its predecessors. IPN has crossed a long path, especially in the pharmaceutical medicine field, from the mere coinage of the term to widespread usage, especially in drug delivery, where they increased the bioavailability and efficacy of the co-delivered drugs. The current review will highlight the major studies that have led to the current face of the IPN in various pharmaceutical domains. The present review was conducted by comprehensively reviewing published reports within the recent period using multiple keywords related to IPN and its role in drug delivery. Moving forward, continued exploration and innovation in IPN technologies promise to further enhance their applications, offering novel solutions for the challenges in drug delivery and therapeutic cargo density.

15.
Int J Pharm ; 659: 124229, 2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-38762166

RESUMO

The swallowability of solid oral dosage forms (SODFs) is crucial for medication safety and adherence. Both regulatory agencies and sponsors are concerned with bringing swallowable SODFs to patients. However, no best practices are available for assessing swallowability. Therefore, we conducted a comparative analysis of clinical swallowability assessments (CSAs) for SODFs in regulatory submissions to identify current study design practices. CSAs were identified from a "swallowability" keyword search of a Food and Drug Administration database. Notable design trends among the 17 CSAs were not assessing swallowability as a primary endpoint (76 %); enrolling pediatric patients (76 %); administering assessments post-screening (76 %); and utilizing questionnaires (100 %). A design trend with near equal frequency (∼50 %) was single- or multiple-doses of product administration. Study subjects were the primary questionnaire respondents (82 %), usually using a Likert scale (92 %, 12/13). CSAs generally dichotomized the responses for analysis (65 %) without pre-specified threshold values (59 %). Overall, while study designs exhibited trends, methodology variations may impact swallowability measurements affecting the interpretation of results. Thus, developing robust and valid assessment tools for swallowability is imperative to produce clinically relevant data and inform regulatory decision-making. Collaboration between regulatory agencies and sponsors is warranted to create best practices and ensure high quality swallowability data.


Assuntos
Deglutição , Formas de Dosagem , Humanos , Administração Oral , Estados Unidos , United States Food and Drug Administration , Inquéritos e Questionários , Projetos de Pesquisa , Preparações Farmacêuticas/administração & dosagem
16.
Pharmaceutics ; 16(5)2024 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-38794246

RESUMO

The safe administration of solid oral dose forms in hospital inpatients with swallowing difficulties is challenging. The aim of this study was to establish the prevalence of difficulties in swallowing solid oral dose forms in acute hospital inpatients. A point prevalence study was completed at three time points. The following data were collected: the prevalence of swallowing difficulties, methods used to modify solid oral dose forms to facilitate administration, the appropriateness of the modification, and patient co-morbidities. The prevalence of acute hospital inpatients with swallowing difficulties was an average of 15.4% with a 95% CI [13.4, 17.6] across the three studies. On average, 9.6% of patients with swallowing difficulties had no enteral feeding tube in situ, with 6.0% of these patients receiving at least one modified medicine. The most common method of solid oral dose form modification was crushing, with an administration error rate of approximately 14.4%. The most common co-morbid condition in these patients was hypertension, with dysphagia appearing on the problem list of two (5.5%) acute hospital inpatients with swallowing difficulties. Inappropriate modifications to solid oral dose forms to facilitate administration can result in patient harm. A proactive approach, such as the use of a screening tool to identify acute hospital inpatients with swallowing difficulties, is required, to mitigate the risk of inappropriate modifications to medicines to overcome swallowing difficulties.

17.
Int J Pharm ; 659: 124278, 2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-38806095

RESUMO

The aim of this work was the development of a film-forming formulation (FFF) for the topical treatment of psoriasis that shows an increased substantivity compared to conventional semi-solid dosage forms. The developed formulation is an oleogel. It is based on a combination of castor oil and medium chain triglycerides, and the oil-soluble film former MP-30 (Croda GmbH, Nettetal, Germany), a polyamide that upon mixing with a polar oil entraps the oil und thus substantially increases the viscosity of the formulation up to a semisolid state. Betamethasone dipropionate (BDP) and calcipotriole (CA) were used as active pharmaceutical ingredients (APIs). Oleogels of different compositions were evaluated regarding substantivity, rheological properties, ex-vivo penetration into the skin and ex-vivo permeation through the skin. Marketed products were used as controls. It was found that the amount of betamethasone dipropionate penetrating and permeating into and through the skin from the film-forming formulation is at an intermediate value compared to the marketed products. The substantivity of the developed formulation is described by an amount of 57.7 % formulation that remains on the skin surface and is thus significantly higher compared to the marketed products. In the film forming formulation, the proportion of API penetrating the skin remains the same when the skin repetitively brought in contact with a piece of textile during the penetration experiment. In contrast with the in-market formulations tested, this proportion was reduced by up to 97 %. As a result, the developed formulations can lead to an increased patient compliance.


Assuntos
Betametasona , Compostos Orgânicos , Psoríase , Absorção Cutânea , Pele , Psoríase/tratamento farmacológico , Betametasona/administração & dosagem , Betametasona/análogos & derivados , Betametasona/química , Betametasona/farmacocinética , Animais , Compostos Orgânicos/química , Compostos Orgânicos/administração & dosagem , Absorção Cutânea/efeitos dos fármacos , Pele/metabolismo , Fármacos Dermatológicos/administração & dosagem , Fármacos Dermatológicos/química , Fármacos Dermatológicos/farmacocinética , Calcitriol/análogos & derivados , Calcitriol/administração & dosagem , Calcitriol/química , Triglicerídeos/química , Administração Cutânea , Óleo de Rícino/química , Suínos , Viscosidade , Química Farmacêutica/métodos , Reologia
18.
Pharmaceutics ; 16(4)2024 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-38675176

RESUMO

Since the acceptability of a medicine can significantly impact therapeutic outcomes, this study aimed to determine and compare the preferences of children, parents, and healthcare professionals for the most commonly used pediatric oral medicine formulations (syrup, mini-tablets, oblong tablets, round tablets) addressing all pediatric age groups, 0-<18 years (y). This survey study employed sex-, age-, and participant group-adapted questionnaires for eight cohorts of participants, i.e., children 6-<12 y, adolescents 12-<18 y, parents of children in four age groups (0-<2 y, 2-<6 y, 6-<12 y, and 12-<18 y), nurses, and pediatricians. Descriptive statistics were used for data analysis. In the age groups 0-<2 y and 2-<6 y, mini-tablets were preferred over syrup by all participants. In the age group 6-12 y, solid dosage forms were also preferred over syrup by all participants. In the age group 12-<18 y, healthcare professionals preferred solid dosage forms over syrup. Parents preferred higher amounts of mini-tablets and syrup compared to round and oblong tablets, while adolescents' preferences did not differentiate between these formulations. Based on the study results and in contrast to current practice, it is suggested to consider solid dosage forms for future age-appropriate medicinal products already for younger age groups.

19.
Patient Prefer Adherence ; 18: 753-766, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38558832

RESUMO

Background: Dosage forms (DF), which are primarily divided into solid, semisolid, liquid, and gaseous, are among the different factors that influence drug adherence. Thus, the purpose of this study was to evaluate how patients' preferences for pharmaceutical DF affected their adherence to medication in community pharmacies in Gondar town. Methods: A cross-sectional study on community pharmacies was carried out from June 25 to July 27, 2023. The statistical package for social sciences, version 26, was used for data analysis. Factors associated with patient medication discontinuation were found using both bivariate and multivariate logistic regressions. Results: According to our study, the majority of respondents (42.4%) preferred tablet DF. Most respondents (63.9%) DF preference was affected by the size of the medication, in which small-sized were most preferable (59.6%). The oral route of administration was the most preferable (71.2%). The majority of the respondents (59.9%) had a history of discontinuation of medicines. Being male (AOR=2.21, 95% CI: 1.29, 3.79), living in rural areas (AOR=1.98, 95% CI: 1.03, 3.83), types of DF (AOR=4.59, 95% CI: 1.28, 16.52), high frequency of administration (AOR=2.22, 95% CI: 1.08, 4.57), high cost of medication (AOR=3.09, 95% CI: 1.69, 5.68), getting some improvement from illness (AOR=3.29, 95% CI: 1.10, 9.87), and high number of drugs (AOR=3.29, 95% CI: 1.67, 13.85) were significantly associated with medication discontinuation. Conclusion: Our findings showed that tablet dosage forms, oral routes of administration, and once-daily taking of medicines were the most preferred by our respondents. Being male, living in rural areas, types of DF, high frequency of administration, high cost of medication, getting some improvement from illness, and high number of drugs were significantly associated with medication discontinuation. This provides an insight into what to consider when prescribing medicine to enhance patients' adherence and overall therapeutic outcomes.

20.
J Pharm Bioallied Sci ; 16(Suppl 1): S243-S246, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38595484

RESUMO

Background: Natural compounds rich in secondary metabolites have gained attention as alternative therapies for wound healing due to their potential advantages over conventional treatments. Pleurotus ostreatus mushrooms have been identified for their wound-healing properties, including promoting neovascularization, epithelialization, and collagen synthesis. Material and Methods: This study aimed to investigate the wound-healing properties of different doses of topical Extract of Pleurotus ostreatus in albino mice using an excisional wound model. The experimental design involved administering various concentrations of the extract to evaluate its effects on wound closure and histopathological and immunohistochemical parameters. Results: The results revealed significant wound closure and improvements in histopathological and immunohistochemical parameters in mice treated with Pleurotus ostreatus extract. These findings suggest the potential of Pleurotus ostreatus extract as a viable wound healing agent. Conclusion: Pleurotus ostreatus extract demonstrates promising wound-healing capabilities, including promoting wound closure and enhancing histopathological and immunohistochemical parameters in albino mice. Further research is warranted to explore its full therapeutic potential and mechanism of action in wound healing.

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