Formulation and evaluation of Buccal mucoadhesive tablets of diclofenac sodium using 23 factorial designs

Buccal tablets

Diclofenac sodium

Drug release

Mucoadhesion

Mucoadhesive tablets

Release kinetics

Structural Analysis and Characterization of 4-F-α-PVP Analog 4-F-3-Methyl-α- PVP Hydrochloride / 法医学杂志

OBJECTIVES@#To identify 1-(4-fluorophenyl)-2-(1-pyrrolidinyl) pentan-1-one (4-F-α-PVP) analog 1-(4-fluoro-3-methyl phenyl)-2-(1-pyrrolidinyl) pentan-1-one (4-F-3-Methyl-α-PVP) hydrochloride without reference substance.@*METHODS@#The direct-injection electron ionization-mass spectrometry (EI-MS), GC-MS, electrospray ionization-high resolution mass spectrometry (ESI-HRMS), ultra-high performance liquid chromatography-high resolution tandem mass spectrometry (UPLC-HRMS/MS), nuclear magnetic resonance (NMR), ion chromatography and Fourier transform infrared spectroscopy (FTIR) were integrated utilized to achieve the structural analysis and characterization of the unknown compound in the sample, and the cleavage mechanism of the fragment ions was deduced by EI-MS and UPLC-HRMS/MS.@*RESULTS@#By analyzing the direct-injection EI-MS, GC-MS, ESI-HRMS and UPLC-HRMS/MS of the compound in the samples, it was concluded that the unknown compound was a structural analog of 4-F-α-PVP, possibly with one more methyl group in the benzene ring. According to the analysis results of 1H-NMR and 13C-NMR, it was further proved that the methyl group is located at the 3-position of the benzene ring. Since the actual number of hydrogen in 1H-NMR analysis was one more than 4-F-3-Methyl-α-PVP neutral molecule, it was inferred that the compound existed in the form of salt. Ion chromatography analysis results showed that the compound contained chlorine anion (content 11.14%-11.16%), with the structural analysis of main functional group information by FTIR, the unknown compound was finally determined to be 4-F-3-Methyl-α-PVP hydrochloride.@*CONCLUSIONS@#A comprehensive method using EI-MS, GC-MS, ESI-HRMS, UPLC-HRMS/MS, NMR, ion chromatography and FTIR to identify 4-F-3-Methyl-α-PVP hydrochloride in samples is established, which will be helpful for the forensic science laboratory to identify this compound or other analog compounds.

Some technological studies on obtaining granular drug formulation from “Shimshin-6” traditional prescription / Монголын эм зүй, эм судлал

Introduction@#Amenorrhea has still been listed as one of common diseases among women in Mongolia. Some traditional prescription for amenorrhea, used commonly in Mongolian traditional medicine, needs more attention to dig out its scientific proof of therapeutic effect on pathogenesis of some diseases. Therefore, we aimed to research Shimshin-6 traditional prescription to develop a granule formulation for amenorrhea and other female reproductive diseases, and study its qualitative and quantitative characteristics.@*Material and method@#In this study, Shimshin-6 traditional prescription was randomly collected from 5 pharmaceutical manufacturers named as “Х-1, Х-2, Х-3, Х-4 and Х-5”. The collected prescriptions were granulated and optimized by a wet-granulation method. Then, granule spill weight and flow quality were detected in obtained granule formulation.@*Result@#20 types of granule formulation from Shimshin-6 were obtained by using 8% and 10% of gelatin, 6% and 8% of polyvinylpyrrolidone as a binder in these formulations. As a result, the suitable binder in this formulation was detected 6% of polyvinylpyrrolidone after researching the granule spill weight and flow rate. For the granule formulations of X-1, X-2 and X-5 prescriptions, the polyvinylpyrrolidone was chosen as the suitable binder due to the result from granule spill weight of the formulation. As for the X-3 and X-4 prescriptions, gelatin was the suitable binder in these formulations. After studying the flow quality of newly obtained granule formulations from “Х- 1, Х-2, Х-3, Х-4 and Х-5”, the most suitable binder was polyvinylpyrrolidone.@*Conclusion@#Altogether, these results showed that the most suitable binder for granulating Shimshin-6 traditional medicine was 6% of polyvinylpyrrolidone due to the results from granule spill weight and flow rate.

Radiosensitization effect of Ta 4C 3-PVP nanosheets on xenograft tumor in mice bearing 4T1 murine triple-negative breast cancer / 中华放射医学与防护杂志

Objective:To investigate the radiosensitizing effect of Ta 4C 3-PVP nanosheets on the tumor of 4T1 murine triple-negative breast cancer cells planted in mice. Methods:4T1 tumor-bearing mice model was established by subcutaneous injection of 4T1 cells into the right flank of the female BALB/c mice. The mice were divided into four groups uniformly according to their tumor size: blank control group, Ta 4C 3-PVP group, ionizing radiation (IR) group and Ta 4C 3-PVP plus IR group. A single dose of 8 Gy X-ray local irradiation was given to xenograft tumor at 24 h after tail intravenous injection of Ta 4C 3-PVP (20 mg/kg). The xenograft tumor volume and weight, the pathological changes of tumor tissue, the expression of tumor proliferative marker Ki-67 protein, and the formation of γ-H2AX foci [a DNA double-strand breaks (DSBs) molecular marker] were detected. Tumor growth curve was established, and enhancement factor (EF) and tumor inhibition rate were calculated. Results:Compared with the blank control group, tumor growth was significantly inhibited ( t=5.41, 9.59, P < 0.05) and tumor weight was markedly decreased ( t=2.67, 4.40, P < 0.05) in both IR group and Ta 4C 3-PVP plus IR group at day 16 after IR. The EF in Ta 4C 3-PVP plus IR group was 1.57, and tumor inhibition rate in Ta 4C 3-PVP plus IR group were about 64%, which was much higher than that of IR group alone(42%). Immunohistochemistry and immunofluorescence histochemistry assays showed that the expression of Ki-67 protein was obviously decreased and the amount of γ-H2AX foci was significantly increased in both IR group and Ta 4C 3-PVP plus IR group in comparison with the blank control group ( t=5.73, 8.02, 2.97, 9.86, P < 0.05). Moreover, the inhibition of Ki-67 protein expression and the increase of γ-H2AX foci were much higher in Ta 4C 3-PVP plus IR group than that in IR group ( t=4.75, 4.42, P < 0.05). Conclusions:Ta 4C 3-PVP nanosheets could enhance radiosensitivity of xenograft tumor in 4T1 tumor-bearing mice through increasing the IR-induced DNA DSBs.

Preparation of a co-amorphous form of bexarotene-PVP-K30 and evaluation in rats / 药学学报

Bexarotene is a synthetic analogue of retinoic acid and exerts protective effects on the nervous system. However, low bioavailability and poor solubility of the crystal type I form severely limits the application of bexarotene in the clinic. A co-amorphous sample of bexarotene-PVP-K30 was prepared and the structure was characterized by X-ray diffraction and infrared spectroscopy. To determine the pharmacokinetics and tissue distribution of bexarotene, an LC-MS method was established to profile and quantify bexarotene in plasma and tissues of SD rats. In vitro dissolution indicated that the co-amorphous form improved the dissolution of bexarotene in pure water 4.17-fold. After rats were orally administered bexarotene or bexarotene-PVP-K30 co-amorphous (equivalent to 30 mg·kg-1 bexarotene) the AUC of bexarotene was 7 034.89 and 10 174.03 μg·L-1·h respectively, the peak time was advanced from 7.33 h to 0.9 h with the amorphous form, and Cmax was enhanced from 627.76 to 3 011.88 μg·L-1. The co-amorphous form yielded higher concentrations of bexarotene in various tissues, especially brain, liver and kidney. Animal welfare and experimental procedures complied with the rules of the Animal Ethics Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences. The results indicate that bexarotene-PVP-K30 co-amorphous improves the pharmacokinetic characteristics of bexarotene and provides preclinical data in support of bexarotene-PVP-K30 for the treatment of brain diseases.

comparative study of dissolution profile of drug by enhancing aqueous solubility through Kneading method

Solid dispersions (SDs) are resulted by dispersion of drug in biologically inert matrix. They can be used to increase the solubility of a drug with low aqueous solubility, thereby improving its oral bioavailability. Higher drug dissolution rates from a SD can be facilitated by optimizing the wetting characteristics of the compound surface, as well as increasing the interfacial area available for drug dissolution. Although the latter can be easily accomplished by, for example: decreasing the particle size of the drug powder but micronized powders may result in further complications as they occasionally tend to agglomerate. A more preferable solution would be to introduce the drug in the form of a molecular dispersion. The aim of present study was to enhance the dissolution rate of diclofenac a practically less water-soluble drug. The same was done by preparation of solid dispersions of the drug employing different ratios of established polymers. This was done by using polymers namely; hydrophilic polymer β-cyclodextrins, PVP and PEG. The kneading method was used to prepare solid dispersions in various ratios with polymer. The dissolution data was studied for all the three formulations. The data obtained was compared with that of physical mixtures containing drug, polymer and lactose in the same ratio as that of solid dispersions. The dissolution data showed that best release was obtained in formulation f1 containing beta –cyclodextrins, PVP and PEG as polymer. The comparative data showed 98% release at approximately 4 hours with polymer β –cyclodextrins, whereas, 90% and 88% release were obtained using PEG and PVP respectively in the same time frame.

Superficial and Deep Skin Preparation with Povidone-Iodine for Ventriculoperitoneal Shunt Surgery : A Technical Note

OBJECTIVE: Ventriculoperitoneal (VP) shunt surgery is a common and effective treatment for hydrocephalus and cerebrospinal fluid disorders. Infection remains a major cause of morbidity and mortality after a VP shunt. There is evidence that a deep skin flora microbiome may have a role to play in post-operative infections. In this technical note, we present a skin preparation technique that addresses the issue of the skin flora beyond the initial incision. METHODS: The patient is initially prepped, as standard, with. a single layer of 2% CHG+70% isopropyl alcohol. The novel stage is the ‘double incision’ whereby an initial superficial incision receives a further application of povidone-iodine prior to completing the full depth incision. RESULTS: Of the 84 shunts inserted using the double-incision method (September 2015 to September 2016), only one developed a shunt infection. CONCLUSION: The double incision approach to skin preparation is a unique operative stage in VP shunt surgery that may have a role to play in reducing acute shunt infection.

Superficial and Deep Skin Preparation with Povidone-Iodine for Ventriculoperitoneal Shunt Surgery : A Technical Note

OBJECTIVE: Ventriculoperitoneal (VP) shunt surgery is a common and effective treatment for hydrocephalus and cerebrospinal fluid disorders. Infection remains a major cause of morbidity and mortality after a VP shunt. There is evidence that a deep skin flora microbiome may have a role to play in post-operative infections. In this technical note, we present a skin preparation technique that addresses the issue of the skin flora beyond the initial incision.METHODS: The patient is initially prepped, as standard, with. a single layer of 2% CHG+70% isopropyl alcohol. The novel stage is the ‘double incision’ whereby an initial superficial incision receives a further application of povidone-iodine prior to completing the full depth incision.RESULTS: Of the 84 shunts inserted using the double-incision method (September 2015 to September 2016), only one developed a shunt infection.CONCLUSION: The double incision approach to skin preparation is a unique operative stage in VP shunt surgery that may have a role to play in reducing acute shunt infection.

Silymarin-Laden PVP-Nanocontainers Prepared Via the Electrospraying Technique for Improved Aqueous Solubility and Dissolution Rate

Abstract The aim of the present research was to develop a silymarin-laden PVP-nanocontainer providing ameliorated aqueous solubility and dissolution of the drug. Several silymarin-laden formulations were formed with varying quantities of PVP and SDS via the solvent evaporation method using the electrospraying technique. The influence of the hydrophilic carriers on solubility and dissolution was explored. The solid-state characterization was carried out by particle-size analysis, PXRD, DSC, FTIR and SEM. All of the formulations demonstrated better solubility and dissolution than did silymarin plain powder. Both the SDS and PVP had positive effects on solubility and dissolution of silymarin in the aqueous media. An increased solubility was attained as the drug/PVP ratio was 1/4; however, further increase in PVP did not provide significant improvement. In particular, a nanocontainer formulation prepared with silymarin, PVP and SDS (1/4/0.5, w/w/w) exhibited the best solubility (26432.76 ± 1749.00 μg/mL) and an excellent dissolution (~92 % in 20 min) than did silymarin plain powder. Also, it demonstrated similar dissolution profiles compared to a commercial product; therefore, might be bioequivalent to the commercial product (f 1 = 3 and f 2 = 69). Moreover, cumulative undersize distribution values as represented by X10, X50 and X90 were 201 ± 21.01 nm, 488 ± 36.05 nm and 392 ± 48.10 nm, respectively. The drug existed in the amorphous state in the PVP-nanocontainers with no strong chemical bonding with other excipients. Thus, this formulation might be used for more effective administration of silymarin via the oral route.

A Case of Hydrophilic Polymer Embolism after TEVAR / 日本心臓血管外科学会雑誌

Hydrophilic polymer embolism (HPE) associated with endovascular therapy has steadily gained attention. We report a case of a 70-year-old man who had undergone one-debranched TEVAR. He had a history of distal arch replacement for dissecting aortic aneurysm 14 years earlier. Pseudoaneurysm at the proximal site of graft anastomosis was found on computed tomography (CT) angiogram during the follow-up. 1 debranching TEVAR was performed using the pull-through technique. Fourth days after the procedure, a skin rash appeared in the right lower extremity around the access site. Skin biopsy with pathological examination revealed HPE. We decided to observe a patient because there was no symptom of limb ischemia. Skin lesions improved and he was discharged on the 27th postoperative day. Hydrophilic polymers are widely used in the endovascular devices and there is an urgent need to better understand the complication of HPE.

Efeitos do banho prévio, da tricotomia e da antissepsia na redução da contaminação do sítio cirúrgico em cadelas submetidas à OSH eletiva / Effects of the previous bath, trichotomy and antisepsis in reducing contamination of the surgical site in bitches undergoing elective OSH

O objetivo deste estudo foi analisar a influencia do banho 24 horas antes do procedimento cirúrgico e da tricotomia pré-operatória na redução da contagem microbiana da pele do campo operatório, bem como a eficiência antisséptica do gluconato de clorexidina 0,5% e da polivinilpirrolidona iodada 10% para antissepsia do sítio cirúrgico, verificando sua ação 4 minutos e 2 horas após aplicação. Utilizaram-se 20 cadelas hígidas, alocadas ao acaso em 2 grupos de 10 animais: os animais do Grupo I foram submetidos ao banho 24 horas antes do procedimento cirúrgico, enquanto os do Grupo II não passaram por este procedimento. Foram isolados diversos gêneros bacterianos antes e após o uso dos antissépticos. Significância estatística foi verificada entre os grupos quanto ao efeito do banho prévio à cirurgia, apenas 2 horas após a aplicação de clorexidina. A tricotomia reduziu 26,48% da carga microbiana nos animais do Grupo I e elevou a carga microbiana em 41,19% nos animais do Grupo II, revelando diferença estatística. Após o uso dos antissépticos, não foi observada diferença estatística entre os grupos em nenhum momento. Do mesmo modo, a comparação da eficiência dos antissépticos com ou sem banho, não revelou significância estatística. A polivinilpirrolidona iodada causou reação alérgica em 15% dos animais e não foi observada irritação cutânea causada pela clorexidina. Conclui-se que o banho prévio tem efeito na redução da carga bacteriana apenas após 2 horas de antissepsia com clorexidina; a tricotomia é mais eficaz na redução microbiana quando o animal é submetido ao banho e os dois antissépticos são igualmente eficazes na antissepsia cirúrgica por até 2 horas quer o animal tome banho ou não previamente à cirurgia.(AU)

The objective of this study was to analyze the influence of bath 24 hours before surgery and preoperative shaving in reducing microbial count of the operating field skin and antiseptic efficiency of 0.5% chlorhexidine gluconate and 10% iodine polyvinylpyrrolidone for antisepsis of the surgical site, by checking its action 4 minutes and 2 hours after application. We used 20 healthy bitches, randomly allocated into 2 groups of 10 animals: Group I underwent bath 24 hours before surgery, whereas Group II did not undergo this procedure. Many bacterial genera have been isolated before and after use of antiseptics. Statistical significance was observed between the groups regarding the effect of bath prior to surgery, just two hours after application of chlorhexidine. Shaving reduced 26.48% of the microbial load in Group I and increased the microbial load in 41.19% in Group II, showing statistical difference. After the use of antiseptics, there was no statistical difference between the groups at any time. Similarly, comparison of the efficiency of the bath with or without antiseptic showed no statistical significance. The iodine polyvinylpyrrolidone caused allergic reaction in 15% of animals and was not observed skin irritation caused by chlorhexidine. We conclude that the prior bath is effective in reducing bacterial load just after 2 hours of antisepsis with chlorhexidine; shaving is more effective in reducing microbial when the animal is subjected to the bath and the two antiseptic agents are equally effective in surgical antisepsis or for up to 2 hours the animal did not take a bath or prior to surgery.(AU)

Acupuncture combined with local anesthesia for percutaneous vertebroplasty / 中国针灸

<p><b>OBJECTIVE</b>To observe the analgesic and sedative effects of acupuncture combined with local anesthesia for percutaneous vertebroplasty (PVP).</p><p><b>METHODS</b>Sixty patients of single segmental osteoporotic vertebral compression fractures who were prepared to receive PVP were randomly divided into an observation group, a control 1 group, a control 2 group, 20 cases in each group. The patients in the observation group were treated with electroacupuncture (EA) at Hegu (LI 4), Neiguan (PC 6) and Zusanli (ST 36) 20 min before operation; during operation, EA was given combined with regular anesthesia. The patients in the control 1 group were treated with intramuscular injection of parecoxib sodium (40 mg), combined with regular anesthesia. The patients in the control 2 group were treated with intravenous injection of dezocine (5 mg), combined with regular anesthesia. Visual analogue scale (VAS) and Ramesy sedation score were compared among the three groups.</p><p><b>RESULTS</b>In the observation group and control 2 group, the VAS during puncture and bone cement placement was higher than that before acupuncture (all <0.01); the VAS during bone cement placement was higher than that before puncture (<0.05, <0.01); the VAS after operation was lower than that during puncture and bone cement placement (<0.05, <0.01). In the control 1 group, the VAS during puncture and bone cement placement and after operation was higher than that before acupuncture (<0.01, <0.05), the VAS after operation was lower than that during puncture and bone cement placement (<0.05, <0.01). There was no significant difference in VAS and Ramesy score among three groups at all time points (all >0.05).</p><p><b>CONCLUSION</b>Compared with local anesthesia and analgesics, acupuncture combined with local anesthesia has similar analgesic and sedative effect for PVP, which could be considered a better method for PVP anesthesia.</p>

Finite Element Analysis and Clinical Application of Unilateral/Bilateral Percutaneous Vertebroplasty for Treating Osteoporotic Vertebral Compression Fractures in Elderly Patients / 医用生物力学

Objective To investigate the biomechanical properties and clinical effects of the unilateral/bilateral percutaneous vertebroplasty (PVP) on the treatment of osteoporotic vertebral compression fractures in elderly patients. Methods The finite element models of the unilateral/bilateral percutaneous vertebroplasty (PVP) in osteoporotic vertebral compression fractures were established to evaluate changes in strain and stress of the fractured vertebra after surgery. Eighty patients with osteoporotic vertebral compression fractures underwent unilateral or bilateral PVP were collected for retrospective analysis. The operation time,intraoperative fluoroscopy times,injected bone cement volume, bone cement leakage rate and visual analogue scales (VAS) score between the two groups were analyzed. Results The maximum strain and stress in unilateral PVP group were 1.18 times and 1.15 times of those in bilateral PVP group,respectively.The operation time and intraoperative fluoroscopy times in unilateral PVP group were obviously smaller than those in bilateral PVP group (P0.05).Conclusions The biomechanical effect of unilateral PVP was similar to that of bilateral PVP. The puncture needle localization of unilateral PVP for treating elderly patients with osteoporotic vertebral compression fractures had the advantage of less operation time and limited X-ray exposure.

Evident-Based Nursing Practice for a Ovarian cancer chemotherapy Patient with puncture piont infection of Peripherally Inserted Central catheter / 中国实用护理杂志

Objective To formulate a rational adjuvant therapeutic evidence-based nursing plan for a ovarian cancer chemotherapy patient with puncture piont infection of peripherally inserted central catheter(PICC).And practice in the clinic to solve the nursing problems in clinical nursing work. Methods According to the condition of the patient and using the PICO principle, we put forward clinical problems. We comprehensively searched the National Guideline Clearinghouse (NGC),Cochrane Library,Pub Med, EMbase,Medline,CNKI,VIP and Wanfang Data from 2007 to 2017. Relevant clinical guidelines, evidence summaries, systematic reviews/ Meta-analysis, randomized controlled trials (RCTs), and high quality reviews on nursing puncture piont infection of Peripherally Inserted Central catheter were collected and their authenticity, importance and applicability were evaluated. Results One Meta-analysis, fifteen RCTs, and one review were totally included. According to current evidence as well as the patient′s clinical conditions and preference, a comprehensive and effective adjuvant therapeutic and nursing programme was given to the patient. At the puncture point of PICC infection , PVP iodine was used to hydropathic compress for 15 minutes once a day.After naturally dried, cover with hydrocolloid dressing. After four-day treatment and nursing care, the patient with puncture piont infection had already recovered. Conclusion Evidence-based medicine approaches could help us develop comprehensive therapeutic plans for ovarian cancer chemotherapy patients with puncture piont infection of PICC, promote effectively the puncture point infection recovery,and ensure the normal safe use of PICC .Thereby alleviate pain, improve health, and increase patients′quality of life.

Preparation,Characterization and in vitro Dissolution Study of Total Flavonoids of Hippophae rhamnoi-des-PVP K30 Solid Dispersion / 中国药房

OBJECTIVE:To prepare total flavonoids of Hippophae rhamnoides(TFH)-PVP K30 solid dispersion,and to char-acterize and study its in vitro dissolution. METHODS:Solvent method was used to prepare TFH-PVP K30 solid dispersion with dif-ferent drug-loading ratio of 1:1,1:2,1:3,1:4,1:5;single factor test was designed to screen drug-loading ratio using dissolution parameter Td as index;orthogonal test was designed to optimize ultrasonic time,temperature of water bath and drying time for prep-aration technology using in vitro dissolution rate as index,and then validated. SEM,DSC and FT-IR were used to characterize sol-id dispersion. RESULTS:Td of TFH-PVP K30 solid dispersion was the lowest when drug-loading ratio was 1:3. Optimal technolo-gy was ultrasonic time 10 min,temperature of water bath 60 ℃ and drying time 12 h. 90 min accumulative dissolution rate of pre-pared TFH-PVP K30 solid dispersion was 90.22% in average(RSD=1.74%,n=3). The results of SEM,DSC and FT-IR showed that the drug as amorphous form dispersed in the PVP K30,the formation of hydrogen bond of the both. CONCLUSIONS:TFH-PVP K30 solid dispersion is prepared successfully,and in vitro dissolution rate of it is improved significantly.

Properties and in vitro dissolution of indomethacin Co-PVP amorphous preparation / 中国药学杂志

OBJECTIVE: To prepare indomethacin amorphous preparation with Co-PVP as carrier, characterize it for exploring the interaction between indomethacin and Co-PVP, and investigate the difference of dissolution between indomethacin crystalline and amorphous preparations. METHODS: The inhibitory effect of Co-PVP on the crystallization of indomethacin supersaturated solution was studied. The indomethacin amorphous preparation was prepared by solvent evaporation method and characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy (FT-IR). In addition, the dissolution behavior in vitro was investigated. RESULTS: Co-PVP had an inhibitory effect on the crystallization of indomethacin supersaturated solution evidently. Indomethacin existed in amorphous state in Co-PVP as hydrogen bonds formed between them. The amorphous preparation of indomethacin-Co-PVP improved the dissolution rate and extent obviously. CONCLUSION: The indomethacin amorphous preparation with Co-PVP as carrier can improve the dissolution in vitro significantly, which providing a reference for obtaining stable amorphous preparation.

Nursing care of patients with multiple metastatic vertebral tumors when treated by PVP / 中国实用护理杂志

Objective To investigate the nursing effect and experience of patients with multiple metastatic vertebral tumors when treated by PVP. Methods To analyze nursing care preoperative and postoperative opertion of 5 cases from January 2013 to December 2015. Results 5 cases were healed well with the pain relief, and no complications occurred. Conclusion It has good effect of multiple metastatic vertebral tumors treated by PVP. It is an effective means for patients have surgery and normal activities earlier by scientific and effective nursing measures before and after the operation.

Comparative Microbicidal Efficacy of Fractionated Extracts from In Vitro and In Vivo Raised Cells of Tinosporacordifolia Against MDR Pathogens

The present study was conducted to explore the hidden potential of natural products synthesized in the medicinal plant Tinosporacordifolia. This plantis prioritized by National Medicinal Plant Board, New Delhi. Leaf and inter nodal segments were inoculated on MS Medium fortified with IBA (1.0 mg/L) produced callus after four weeks. The calli were brown due to phenolic substance secreted by the explant. This problem was overcome by using adjuvant PVP (0.1%). Further, secondary metabolites were isolated from callus and field leaf through soxhlet extractor and fractionated by using column chromatography. The antibacterial activity of these fractioned extracts from Tinosporacordifolia callus and leaf were seen against multi drug resistance bacteria viz., Escherichia coli (ATCC 25922), Pseudomonas aeruginosa, (ATCC 27853) & Staphylococcus aureus (ATCC 29213) and against plant pathogenic fungus Fuseriumoxisporum(MTCC 8608) and Sclerotiniasclerotiorum (MTCC 8785). All fractionated extracts showed antimicrobial activity but callus extracts were proved to be best in compare to leaf extracts. Furthermore, we are trying to analyze different bio active compounds through GCMS.

A reliable crystallization process for the preparation of agomelatine form I / 中国药科大学学报

@#A reliable crystallization process was developed for the preparation of stable agomelatine form I. This antisolvent crystallization was explored in ethanol-n-heptane by adding PVP and ethanol-water system by adding HPMC, respectively. Factors such as solvent, polymer, concentration of polymer, and solvent ratio were subjected to detailed examination. Accelerated and long-term stability observations indicates that the presence of polymeric additives in the crystallization process enhances the stability of agomelatine form I.

Size Control of 99mTc-tin Colloid Using PVP and Buffer Solution for Sentinel Lymph Node Detection

Colloidal particle size is an important characteristic that allows mapping sentinel nodes in lymphoscintigraphy. This investigation aimed to introduce different ways of making a 99mTc-tin colloid with a size of tens of nanometers. All agents, tin fluoride, sodium fluoride, poloxamer-188, and polyvinylpyrrolidone (PVP), were mixed and labeled with 99mTc. Either phosphate or sodium bicarbonate buffers were used to adjust the pH levels. When the buffers were added, the size of the colloids increased. However, as the PVP continued to increase, the size of the colloids was controlled to within tens of nanometers. In all samples, phosphate buffer added PVP (30 mg) stabilized tin colloid (99mTc-PPTC-30) and sodium bicarbonate solution added PVP (50 mg) stabilized tin colloid (99mTc-BPTC-50) were chosen for in vitro and in vivo studies. 99mTc-BPTC-50 (100 nm) mainly accumulated in the liver. When a rabbit was given a toe injection, the node uptake of 99mTc-PPTC-30 decreased over time, while 99mTc-BPTC-50 increased. Therefore, 99mTc-BPTC-50 could be a good candidate radiopharmaceutical for sentinel node detection. The significance of this study is that nano-sized tin colloid can be made very easily and quickly by PVP.