Drug Preparation Research Articles

Niosome preparation of atorvastatin drug with green preparation approach for in-vitro study of transdermal absorption with lavender essential oil

Introduction: Studies have pointef to anti-inflammatory properties of atorvastatin. In this research, noisome nanoparticles have been used to increase skin penetration and drug retention. Method: Atorvastatin niosomes were prepared using the sonication method. The effect of cholesterol: surfactant mixture ratio was investigated on physicochemical properties of nanoparticles. Studies have been performed on the morphological features, and characterization of nanoparticles. The toxicity of optimal formulation was investigated on a normal human fibroblast cell line. Different percentages of lavender essential oil were added to the optimal formulation gel, and skin drug delivery studies were performed. Results: The optimal formulation had the optimum particle size, PDI, zeta potential, and EE%, which leads to higher stability and dissolution of atorvastatin in the body. Morphological studies conducted on properties of nanoparticles illustrated a spherical shape and no interference with other formulation components. No cytotoxicity was detected for improved formulation of nanoparticles, including atorvastatin. In-vitro skin permeation results indicated that gel containing 0.5% lavender essential oil atorvastatin noisome (Atrosome) could enhance the dermal delivery of atorvastatin where a higher concentration of atorvastatin can be detected in skin layers. Conclusion: As evidenced by the results of this study, preparing nanoparticles from atorvastatin and adding essential oil to the final formulation exerts a positive effect on local drug delivery. Moreover, drug delivery with nanocarriers significantly increased the percentage of drug retention in the target site.

Manipulation of solid dosage forms for oral administration to paediatric patients for drug-resistant tuberculosis in South Africa: an observation study

BackgroundChildren represent a particularly vulnerable demographic in the context of drug-resistant (DR) tuberculosis (TB) due to their increased likelihood of close contact with adults diagnosed with the disease. Approximately 25 000–30 000 children develop DR-TB annually. While treatment success rates for DR-TB in children surpass those in adults, children and adolescents encounter distinct challenges throughout the diagnosis and treatment of DR-TB (including MDR-TB, Pre-XDR TB, and XDR-TB).AimTo identify current practices in drug administration to children diagnosed with DR-TB where appropriate dosage forms are not available in South Africa.MethodAn observational study was carried out at the study site to determine how medication prescribed was manipulated and administered by nursing staff to paediatric patients in the wards.ResultsThe observational study identified 8 drugs used in DR-TB at the study site, where some manipulation to the formulation was necessary to enable administration to paediatric patients. Linezolid and para-aminosalicylic acid are the only drugs available and registered in the South Africa in a formulation that is suitable for administration to paediatric patients. Activities carried out by nursing staff to enable the administration of DR-TB medication included cutting capsules and tablets and dissolving the tablet or capsule contents in distilled water to obtain the required suitable dose.DiscussionLack of availability of suitable dosage forms for paediatrics patients results in several challenges, such as additional time required for drug preparation, increased time duration of medication administration, and unpalatability of drugs. These challenges may subsequently affect compliance and therapeutic outcomes of the treatment of paediatric patients, especially as outpatients.ConclusionResearch needs to focus on the development of appropriate dosage forms for the paediatric population and focus on identifying cases of DR-TB in children. This will assist in building evidence to advocate for registration of child-friendly dosage forms thereby ensuring a sustainable supply of medication.

Factors Affecting Seaweed (Eucheuma cottoni) Production in Banten Province (Case in Lontar Village)

Seaweed is one of the plants that has a lot of potential as a functional food ingredient, active ingredient of drug preparation and even cosmetics that are quite natural in producing various pharmacological activities both as a source of antioxidants, antibacterials, antimicrobials and anticancer. Seaweed is currently a potential asset for areas that are able to produce it to meet the increasing market needs. Lontar Village, located in Banten Province, is one of the main seed producing areas. However, seed production factors are one of the main indicators that need to be used as a standard in this study, such as the length of the rope span, age characteristics, education characteristics, characteristics of the seed farmer's business experience. This type of research is quantitative and data is obtained primarily and secondarily. The data obtained were analyzed using the SPSS 26 program. The results of the study showed that the factors that influence seaweed production in Banten Province, especially Lontar Village, are influenced by the length of the rope span, age characteristics, education characteristics, characteristics of the seaweed farmer's business experience. The conclusion is that seaweed production is influenced by various characteristics, namely age, education, and seaweed farming experience.

Formulation and clinical evaluation of carbidopa/levodopa oral solution for the treatment of sepiapterin reductase deficiency

Backgroundsepiapterine reductase deficiency (SRD) is a rare levodopa (L-dopa)-responsive disorder treated with a combination therapy of controlled-release L-dopa and carbidopa. The currently available formulation of controlled-release carbidopa/L-dopa does not entirely meet the requirements for the long-term therapy in pediatric patients. In fact, administration of a manufactured tablet at a dose intended for adults necessitates its adjustment to the child’s needs, as the splitting of the tablet into smaller portions or its dilution in water. It’s essential to emphasize that tablets must not be crushed, as this can compromise the controlled-release mechanism and affect the efficacy of the medication. At the moment, commercial liquid formulations are not available. Given these limitations, in house drug preparation in hospitals and community pharmacies is a valid option to ensure the proper therapeutic management of these patients. Materials and methodswe described sample preparation, physical and microbiological analyses, taste testing, and tolerability of a 1:10 ratio carbidopa/L-dopa flavored (mint, raspberry, cacao, berries) and unflavored oral formulation (no sweetening agents were added). We also reported long-term follow-up of two pediatric patients with SRD. Resultswe documented the stability for 28 days at 25 °C of the liquid solution. All formulations were well-tolerated, and no adverse events were observed during or after assessing taste and tolerability. The long-term follow up of two patients was characterized by effective symptom control and optimal treatment adherence and compliance. Conclusionsin-house liquid drug formulations can be a valid option for pediatric patients with SRD. Given the significant impact of taste on medication adherence, the use of flavoring agents in the development of liquid formulations of L-dopa/carbidopa results a very useful strategy to obtain optimal adherence in the pediatric population.

A novel deep learning approach for optimizing preparation and usage of nonsteroidal anti-inflammatory drugs (NSAIDs) in spine care

Nonsteroidal anti-inflammatory drugs (NSAIDs) are essential for the management of pain and inflammation brought by illnesses of the spine. NSAIDs are essential in the treatment of inflammation and pain in a variety of spinal disorders. In order to relieve pain for patients and enhance their quality of life, NSAIDs should be used effectively. The effectiveness and safety of NSAIDs for spinal pain were assessed using a systematic review and meta-analysis. We gathered the patient data. The insufficient data is cleaned using tokenization and the data extraction employs Term Frequency-Inverse Document Frequency (TF-IDF). A Monarch Butterfly Optimization Dynamic Generative Adversarial Networks (MBO+DGAN) for the preparation and use of NSAIDs in spine care. Our studies show the possibility of the MBO+DGAN strategy to enhance the administration of NSAIDs in spine care, leading to improved clinical results, patient experiences and possibly lower healthcare costs. The MBO+DGAN assesses a method's effectiveness by evaluating its performance in terms of Accuracy (95%), Sensitivity (96%), Precision (97%) and Specificity (94%). The opportunity to use MBO+DGAN to improve how NSAIDs are created and utilized in the complex world of spine care. This technique offers an effective approach to enhance patient care and outcomes in the difficult field of spine healthcare by enabling customized treatment plans.

Efficacy of S-Flurbiprofen Plaster for Analgesia Following Total Hip Arthroplasty.

S-flurbiprofen (SFP) plaster, a non-steroidal anti-inflammatory drug preparation that penetrates effectively into deep tissue, is currently used as a conservative treatment for osteoarthritis. We investigated the analgesic and adverse effects of SFP plaster after total hip arthroplasty (THA). A retrospective comparative study identified 100 patients who underwent primary THA in our department. Group A consisted of 50 patients who received the selective cyclooxygenase-2 inhibitor celecoxib for 14 days after surgery, while Group B consisted of 50 patients who received SFP plaster for 14 days after surgery. We noted the numerical rating pain intensity scale (NRS) score, body temperature, and adverse effects of the analgesics. Groups A and B showed no significant difference in NRS scores (p > 0.05). The body temperature was significantly higher in Group B than in Group A on days one, two, three, and five (p < 0.01). In Group A, two patients (4%) showed drug-induced renal dysfunction, and one patient (2%) showed gastrointestinal disturbance. Patients in Group B showed no systemic or local adverse effects. The application of SFP plaster after THA provided an analgesic effect similar to that obtained with oral celecoxib without causing obvious side effects. Applying an SFP plaster may be an effective solution for postoperative analgesia.

Challenges in using DNA barcodes for authentication of Sida species

The Indian system of medicine’s “Ayurvedic pharmacopeia of India (API)” recommends the use of Sida cordifolia Linn (root), Sida cordata (Burm.f.) Borss.Waalk. (aerial part), Sida rhombifolia Linn. (root) and Abutilon indicum (Linn.) Sw. (root) in drug preparations of Bala, Nagabala, Mahabala and Atibala respectively. Moreover many Sida sp. are being used in China, South East Asia, Africa and South America in their traditional healthcare systems. It is a taxonomically complex genus often difficult to authenticate from dried/chopped herbal market samples. Many Sida sequences from the NCBI database, including published reports, were highly suspect and were redesignated into species groups during phylogenetic clustering. Among the four loci studied, ITS2 region was identified as the best for the Sida species identification followed by trnH-psbA. The trnH-psbA phylogeny however fails to differentiate between (1) S. beddomei and S. cordata, (2) S. alnifolia and S. scabrida, (3) S. cordifolia and S. fryxellii that formed monophyletic clusters. The average evolutionary divergence over Sequence Pairs within each species group for ITS2 locus ranged from 0.000 to 0.009 (Average=0.0021), while average Interspecific distance between species was 0.1175 making them ideal for authentication of Sida species. The matK and rbcL is recommended as a back-up loci for identifying intergeneric adulterants in case, the ITS2 or trnH-psbA amplification fails. The present study identified two market samples as adulterant species; (1) S. alnifolia and (2) a mixture of S. acuta and S. alnifolia/S.scabrida. The study provides a roadmap for Ayurvedic/herbal industry to utilize DNA barcoding for authentication of Sida species. At the same time the presence of “Unknown Sida group” highlights the need for further research to accurately classify and identify all Sida species at the phylogenetic level, utilizing the DNA barcode sequences to thoroughly understand the diversity and evolution of the Sida genus.

High accuracy discriminant analysis of preparation from 22 commercial antibodies based on UV spectroscopy combined with chemometrics

The demand for monoclonal antibodies (mAbs) in hospitals is continually rising due to the advancement of targeted therapy or immunotherapy. Typically, mAbs are produced in centralized chemotherapy production units and require rigorous control to ensure the right drug at the right dose before administration to patients.This study aimed to develop a robust discriminant analysis method using a large dataset comprising 22 mAbs used in cancer therapy. The discriminant analysis was based on UV spectroscopy coupled with chemometrics. A dataset consisting of 404 samples was prepared and analyzed using various preprocessing methods, wavelength selection and discriminant analysis algorithms to maximize overall accuracy. Validation of the newly developed discriminant analysis was conducted using samples collected from real manufactured preparations for patient (over 1,380 samples). The study achieved an overall accuracy of 99.6% and 99.8% on the 22 mAbs using partial least squares-discriminant analysis (PLS-DA) and k-nearest neighbors (kNN), respectively. The utilization of chemometrics for discriminating mAbs based on their UV spectra, following total area normalization, has been successfully demonstrated. This method has undergone validation, affirming its capability to swiftly and dependably distinguish different mAbs. Moreover, it effortlessly integrates within the workflow involved in the preparation of mAbs drugs within a cancer hospital setting. This advancement holds promise for streamlining processes and enhancing efficiency in the production and use of mAbs, thereby potentially benefiting patient care and treatment outcomes.

Syringin: a naturally occurring compound with medicinal properties.

Syringin, a phenylpropanoid glycoside, is widely distributed in various plants, such as Acanthopanax senticosus (Rupr. et Maxim.) Harms, Syringa reticulata (BL) Hara var. mandshurica (Maxim.) Hara, and Ilex rotunda Thumb. It serves as the main ingredient in numerous listed medicines, health products, and foods with immunomodulatory, anti-tumor, antihyperglycemic, and antihyperlipidemic effects. This review aims to systematically summarize syringin, including its physicochemical properties, plant sources, extraction and separation methods, total synthesis approaches, pharmacological activities, drug safety profiles, and preparations and applications. It will also cover the pharmacokinetics of syringin, followed by suggestions for future application prospects. The information on syringin was obtained from internationally recognized scientific databases through the Internet (PubMed, CNKI, Google Scholar, Baidu Scholar, Web of Science, Medline Plus, ACS Elsevier, and Flora of China) and libraries. Syringin, extraction and separation, pharmacological activities, preparations and applications, and pharmacokinetics were chosen as the keywords. According to statistics, syringin can be found in 23 families more than 60 genera, and over 100 species of plants. As a key component in many Chinese herbal medicines, syringin holds significant research value due to its unique sinapyl alcohol structure. Its diverse pharmacological effects include immunomodulatory activity, tumor suppression, hypoglycemic action, and hypolipidemic effects. Additionally, it has been shown to provide neuroprotection, liver protection, radiation protection, cardioprotection, and bone protection. Related preparations such as Aidi injection, compound cantharidin capsule, and Tanreqing injection have been widely used in clinical settings. Other studies on syringin such as extraction and isolation, total synthesis, safety profile assessment, and pharmacokinetics have also made progress. It is crucial for medical research to deeply explore its mechanism of action, especially regarding immunity and tumor therapy. Meanwhile, more robust support is needed to improve the utilization of plant resources and to develop extraction means adapted to the needs of industrial biochemistry to further promote economic development while protecting people's health.

The Early Access and the Potential Cost Savings by the Compassionate Use of Onco-haematological Drugs: Results from the Italian Study Compass-O.

Compassionate drug use (CDU) provides early access to not yet authorised medicines and is funded by pharmaceutical companies. The observational retrospective study Compass-O monitored the CDU of onco-haematological drugs, managed by seven Italian units for cytotoxic drug preparations (Unità Farmaci Antiblastici [UFA]), between 1 January, 2016 and 31 December, 2021. We aimed to evaluate the CDU of onco-haematological drugs managed by seven Italian UFA, between 2016 and 2021. The seven UFA provided anonymised data concerning CDU approved in the study period. The early access and potential cost savings for the National Health System (Servizio Sanitario Nazionale [SSN]) were analysed for CDU concerning drug-therapeutic indication combinations with complete data and reimbursed by SSN up to December 2023 (date of study execution), according to the executive decision of the Italian Medicines Agency (Agenzia Italiana del Farmaco [AIFA]). Both analyses distinguished solid/liquid tumours and categorised the combinations as innovative (fully/conditionally) or non-innovative based on AIFA assessments. Compass-O collected 783 CDU authorisations, with 572 (73.1%) analysable in terms of early access and cost savings. On average, early access amounted to 514 days and the total cost savings was €376,115,801. Compassionate drug use approvals involved mainly solid tumours (93.7% vs 6.3% for liquid tumours), and the combination of trastuzumab emtansine-breast cancer was the most dispensed (n = 73; early access = 426 days;potential cost savings: €610,388). Out of 572 CDU approvals, 200 (35%) were innovative drug-therapeutic indication combinations, with 598 days of early access and a total potential saving of €113,124,069. The study Compass-O showed a significant economic burden of CDU and a relevant need for early access, particularly for innovative drugs. However, there is currently no structured monitoring of CDU in Italy, suggesting the need for a national observatory, of which Compass-O can be the pilot phase.

Subcutaneous vs Intravenous Trastuzumab/Pertuzumab: A Time and Motion Substudy of a Phase II Trial of Adjuvant Trastuzumab/Pertuzumab for Stage I HER2+ Breast Cancer (ADEPT trial).

The time required for in-clinic drug administration can substantially affect breast cancer patients' quality of life. Subcutaneous (SC) drug administration, as opposed to intravenous (IV), may reduce this time commitment. This study sought to estimate the difference in time burden between IV and SC administration of trastuzumab and pertuzumab (HP). We prospectively enrolled a subcohort of patients participating in the ADEPT trial (ClinicalTrials.gov identifier: NCT04569747, investigating adjuvant HP plus endocrine therapy for stage I human epidermal growth factor receptor 2-positive breast cancer) to this single-arm crossover time and motion substudy. Patients received two cycles of IV HP followed by two cycles of SC HP. During each cycle, time points in drug preparation and administration were captured. The primary end point was total patient time in the treatment chair. Additional end points included total patient treatment experience time and total pharmacy workflow time. A sample size of 22 patients was estimated to provide 90.7% power with two-sided alpha .05 to detect a difference of 70 minutes in the primary end point by treatment arm (IV v SC). Twenty-two patients were enrolled. The mean total patient time in the treatment chair was 61.8 minutes shorter with SC versus IV HP (22.5 v 84.3 minutes; P < .0001). The mean total patient treatment experience time (incorporating time spent waiting for treatment initiation and time spent in the treatment chair) was 81.8 minutes shorter for SC administration (96 v 177.8 minutes; P < .0001). The pharmacy workflow time was 78.2 minutes shorter for SC versus IV formulation (41 v 119.2 minutes; P < .0001). SC administration of HP shortened patient time burden by approximately 1 hour. SC drug administration can facilitate faster workflows for health care professionals and improve patients' breast cancer treatment experience.

TRADITIONALLY USED MEDICINAL PLANTS FOR WOUND HEALING IN THIRUVALLUR DISTRICT, TAMIL NADU, INDIA

The present study aims to enumerate the ethno-medicinal uses of plants by the Irular communities residing around the Thiruvallur district. The medicinal use of (49) plants belonging to 39 families was identified and recorded by the tribes, along with their botanical identities and methods of drug preparation. The drugs administered locally to heal wounds, including antibiotics, antiseptics, etc., and the necessary information related to the traditional medicinal plants were highlighted in this paper. Wound healing activity is a cellular and biochemical process for restoring the original structure and functions of damaged tissue. The wound may occur from a physical, chemical, thermal, microbial, or immunological insult to the tissues. Various parts of the plants have been in use for several years in tribal communities, traditionally for treating many diseases like skin, colic, sores, cancer, etc. Due to their minimal side effects. The natural agents present in the plants induce wound healing and regeneration from tissue loss by multiple mechanisms. Plant extracts have immense potential for the treatment of wound healing activity. In this review, we focused on the wound healing activity with the pharmacological process of medicinal plants.

Ethnomedicinal Usage, Phytochemistry and Pharmacological Potential of Solanum surattense Burm. f.

Solanum surattense Burm. f. is a significant member of the Solanaceae family, and the Solanum genus is renowned for its traditional medicinal uses and bioactive potential. This systematic review adheres to PRISMA methodology, analyzing scientific publications between 1753 and 2023 from B-on, Google Scholar, PubMed, Science Direct, and Web of Science, aiming to provide comprehensive and updated information on the distribution, ethnomedicinal uses, chemical constituents, and pharmacological activities of S. surattense, highlighting its potential as a source of herbal drugs. Ethnomedicinally, this species is important to treat skin diseases, piles complications, and toothache. The fruit was found to be the most used part of this plant (25%), together with the whole plant (22%) used to treat different ailments, and its decoction was found to be the most preferable mode of herbal drug preparation. A total of 338 metabolites of various chemical classes were isolated from S. surattense, including 137 (40.53%) terpenoids, 56 (16.56%) phenol derivatives, and 52 (15.38%) lipids. Mixtures of different parts of this plant in water-ethanol have shown in vitro and/or in vivo antioxidant, anti-inflammatory, antimicrobial, anti-tumoral, hepatoprotective, and larvicidal activities. Among the metabolites, 51 were identified and biologically tested, presenting antioxidant, anti-inflammatory, and antitumoral as the most reported activities. Clinical trials in humans made with the whole plant extract showed its efficacy as an anti-asthmatic agent. Mostly steroidal alkaloids and triterpenoids, such as solamargine, solanidine, solasodine, solasonine, tomatidine, xanthosaponin A-B, dioscin, lupeol, and stigmasterol are biologically the most active metabolites with high potency that reflects the new and high potential of this species as a novel source of herbal medicines. More experimental studies and a deeper understanding of this plant must be conducted to ensure its use as a source of raw materials for pharmaceutical use.

Effects of Commonly used Surfactants, Poloxamer 188 and Tween 80, on the Drug Transport Capacity of Intestinal Glucose Transporters.

Some glycoside drugs can be transported through intestinal glucose transporters (IGTs). The surfactants used in oral drug preparations can affect the function of transporter proteins. This study aimed to investigate the effect of commonly used surfactants, Poloxamer 188 and Tween 80, on the drug transport capacity of IGTs. Previous studies have shown that gastrodin is the optimal drug substrate for IGTs. Gastrodin was used as a probe drug to evaluate the effect of these two surfactants on intestinal absorption in SD rats through pharmacokinetic and in situ single-pass intestinal perfusion. Then, the effects of the two surfactants on the expression of glucose transporters and tight-junction proteins were examined using RT-PCR and western blotting. Additionally, the effect of surfactants on intestinal permeability was evaluated through hematoxylin-eosin staining. The results found that all experimental for Poloxamer 188 (0.5%, 2.0% and 8.0%) and Tween 80 (0.1% and 2.0%) were not significantly different from those of the blank group. However, the AUC(0-∞) of gastrodin increased by approximately 32% when 0.5% Tween 80 was used. The changes in IGT expression correlated with the intestinal absorption of gastrodin. A significant increase in the expression of IGTs was observed at 0.5% Tween 80. In conclusion, Poloxamer 188 had minimal effect on the drug transport capacity of IGTs within the recommended limits of use. However, the expression of IGTs increased in response to 0.5% Tween 80, which significantly enhanced the drug transport capacity of IGTs. However, 0.1% and 2.0% Tween 80 had no significant effect.

Modelling the Potential Habitat of Taxus baccata Linn. in Shi-Yomi District of Arunachal Pradesh, India

Taxus baccata Linn., commonly known as Yew is a temperate conifer tree usually small to medium in size. The barks, leaves, and twigs have traditional medicinal uses. It is also processed to make taxol which is used in the preparation of anti-cancer drugs (breast and ovarian cancer). The plant is rare, endangered, and listed in Appendix II of CITES. In this study, we used the maximum entropy (MaxEnt) model to predict the potential distribution of the species. The results show an area of 2444.01 km2 (88.77%) as least suitable, followed by 237.06 km2 (8.61%%) as moderately suitable and only 72.01 km2 (2.62%) as highly suitable category. The model performance was reasonably good and reliable with a mean Area under curve (AUC) of 0.934 and a standard deviation of 0.018. Isothermality, precipitation seasonality, and mean diurnal range of temperature significantly contributed to predicting the suitable habitat of T. baccata. An examination of the model results shows the northern part of the district is the potential area of occurrence for T. baccata in the natural stand and suitable for regeneration. Thus, the model outcomes could be used to explore the natural population status of the plant.

Pharmacological properties and clinical development overview of pertuzumab (genetical recombination), trastuzumab (genetical recombination) and vorhyaluronidase alfa (genetical recombination) (PHESGO® combination for ‍subcutaneous injection MA, IN)

Pertuzumab and trastuzumab are anti-HER2 humanized monoclonal antibodies with different mechanisms of action. Their combination is expected to suppress intracellular HER2 signaling additively or synergistically. Their combination is widely recommended worldwide and has been established as a standard of care for HER2-positive breast cancer. However, improvement is required because of the prolonged time of intravenous infusion. Vorhyaluronidase alfa (rHuPH20) depolymerizes hyaluronan in the subcutaneous connective tissue. It's reported to increase the permeability and absorption levels of drugs. PHESGO® combination for subcutaneous injection MA/IN (PHESGO®) is a fixed-dose combination of pertuzumab, trastuzumab, and rHuPH20. A confirmatory phase III study (FeDeriCa) was conducted following a dose-finding phase I study (BO30185). Patients with HER2-positive early breast cancer were randomly assigned to receive either intravenous infusion of pertuzumab and trastuzumab or subcutaneous injection of PHESGO®, in combination with chemotherapy, to compare the pharmacokinetics (PK), efficacy and safety. A phase II study (PHranceSCa) was also conducted to assess patients' preference and satisfaction. Based on these results, population PK analysis, and other data, PHESGO® obtained marketing approval in Japan in September 2023 with indications for "HER2-positive breast cancer" and "advanced or recurrent HER2-positive colorectal cancer that has progressed following cancer chemotherapy and is not amenable to curative resection". By reducing the administration time, PHESGO® is expected to contribute to various needs of patients and improvement of their daily lives. Since drug preparation is not required, it can provide convenience to healthcare professionals, leading to stress reduction of medical resources as well.

Synthesis, optical properties, DNA, β-cyclodextrin interactions, and antioxidant evaluation of novel isoxazolidine derivative (ISoXD2): A multispectral and computational analysis

ISoXD2 are well explored among versatile and outstanding class of pharmacophores for the preparation and discovery of drugs. Herein, the electronic absorption and emission spectra of ISoXD2 were investigated in three different solvents. The observed transition was attributed to π-π* with charge transfer character. Changes in the excited state and shift of the absorption and emission peaks to longer wavelengths are observed as a result of increasing solvent polarity, due to the interactions between the ISoXD2 molecule and the solvent molecules surrounding it. Changing the solvent confirms its solvatochromic effect. UV–vis and fluorescence analysis revealed that ISoXD2 binds to deoxyribonucleic acid (DNA) by intercalation mode, with a stoichiometric ratio of 1:1.5. Moreover, the fluorescence intensity of DNA bound to ethidium bromide (EB) in the presence of ISoXD2 was investigated. From this analysis, the Stern-Volmer quenching constant (Ksv), quenching rate constant (kq), binding constant (Kb) and binding sites number (n) were found to be 5.654 × 103 M−1, 2.827 × 1011 M−1 s−1, 3.81 × 104 M−1 and 1.225, respectively. The interaction between ISoXD2 and β-CD was investigated through absorption spectra analysis. Kb for this interaction was determined to be 4.9 × 104 M−1. The free radical-scavenging ability of the prepared ISoXD2, examined by DPPH and ABTS assays have shown a good antioxidant activity. Furthermore, modeling study was conducted to explore their plausible binding mechanism with ISoXD2 and to support the experimental results.

Establishing an Intravesical Doublet Chemotherapy Clinic for Nonmuscle-Invasive Bladder Cancer Patients.

Intravesical sequential doublet chemotherapy (SDC) is being used increasingly as a rescue treatment for nonmuscle-invasive bladder cancer failing bacillus Calmette-Guérin (BCG), as single-agent chemotherapies are less effective, especially for carcinoma in situ. Considering the current BCG shortage, intravesical SDC also provides an efficacious alternative to BCG. Our aim is to detail the implementation to assist with establishing an efficient and practical intravesical SDC clinic for urologic practice. We searched PubMed for published studies with the Medical Subject Heading of "intravesical chemotherapy" and "non-muscle invasive bladder cancer." The search was limited to English-language journals and full papers only. The initial search resulted in 260 articles, of which 20 relevant studies were selected. Five important processes were identified in the successful and efficient administration of intravesical SDC: (1) patient preparation, (2) medication procurement, (3) medication administration, (4) medication immediate aftermath, and (5) patient instruction and education. Safety precautions should be taken when handling each chemotherapy drug. A clinical pharmacist may be required for drug preparation. An important step in providing intravesical SDC is to use a closed system for the instillation of the chemo-solution. A special protocol should be adopted for every drug with its proper dwell time. The induction course consists of weekly instillation for 6 weeks. If an initial response is noted, maintenance therapy is recommended, typically monthly for 24 months. Successful intravesical SDC clinics necessitate appropriate patient selection, standardized workflow procedures, patient education, and good communication between the urologist, clinical pharmacists, and oncology nurses.

Influence of Light Irradiation on the Degradation of Dezocine in Injections.

Dezocine, which is well-known as an analgesic, had about 45% share of the Chinese opioid analgesic market. Since drug products containing impurities could bring serious health consequences, it was important to control the generation of impurities and degradation products in the dezocine product. In this study, two kinds of photodegradation products (i.e., degradation product 1 and degradation product 2) in the dezocine injection were isolated using high-performance liquid chromatography. The possible structures of the photodegradation products were identified using both high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy. In addition, the possible generation mechanism showed that degradation product 1 was the oxidation product of dezocine, and degradation product 2 was the coupled dimer of dezocine. Finally, we found that the degradation rate of dezocine increased with the increase in light intensity. Moreover, the degradation of dezocine easily occurred under ultraviolet light in comparison with visible light. A deeper insight into the generation of the photodegradation products in the dezocine injection would directly contribute to the safety of drug therapy based on the dezocine injection by minimizing the degradant/impurity-related adverse effects of drug preparations.

Ethnobotanical Studies of Reputed Aphrodisiac Plants Used in Traditional Medicine in Haut-Katanga in DR of Congo

The goal of this study is to identify the plants used to treat sexual dysfunction in Haut-Katanga (DRC). Since most couples in sexual distress believe that resolving sexual dysfunction (SD) is the key to happiness, an ethnobotanical survey using a questionnaire guide was conducted among 36 traditional practitioners in four sites in Haut-Katanga province, including Lubumbashi, the provincial capital. The survey identified 52 species of aphrodisiac plants that are used to treat SD. Of these, 51 have been scientifically identified; they belong to 45 different genera and are contained in 28 families, with the Fabaceae having the highest representation (15.7%). These species are employed singly or in combination to prepare eighty recipes; the most common plant organ was the root bark (63%) in these recipes. Aqueous decoction (44%) and oral administration (75.3%) are the most commonly used routes of drug preparation and administration. Nearly 80 additional indications for the same plant species were discovered to be employed, such as sexually transmitted infections (7.17%), diabetes (3.69%), and hemorrhoids (4.07%). For every species, the Informant Consensus Factor (ICF) was determined. The plants with higher values (ICF≥0.17) included Bersama abyssinica Fres, Garcinia huillensis Welw, Cassia petersiana Bolle, Chenopodium album L, Clerodendrum capitatum (Willd) Schumach, Dialiopsis africana Radlk., Albizia adianthifolia (Schum.) W. Wight, and Crossopteryx febrifuga Mull.Arg.