Antidiabetic claims of Tinospora cordifolia (Willd.) Miers: critical appraisal and role in therapy

ABSTRACTCurrently, available conventional options for diabetes mellitus have certain limitations of their own, and options from medicinal plants with antihyperglycemic activities are being searched to meet the need. Antidiabetic properties of Tinospora cordifolia are highly appreciated in Ayurveda and even in recent modern researches. Several studies on its extracts (viz. immune- modulatory, anti-hyperglycemic, antioxidant, adaptogenic, hepatoprotective, hormone regulator etc.) and isolated phytoconstituents (like tinosporin, berberine, jatrorrhizine etc.) have reported that it is a preventive and curative antidiabetic herb, which are substantiated by clinical trials. Scattered information pertaining to antidiabetic potential of Tinospora is reported. Present review encompasses (i) in-depth information of reported antidiabetic activities of the plant in light of available experimental and clinical studies, and (ii) understanding on the possible mechanism of its action in combating the complex pathology of diabetes

“A Study to Assess the effectiveness of station-based skill training model through Objective Structured Clinical Examination (OSCE) on obstetrical assessment on Nursing students at selected Nursing colleges at Anand- Kheda district.”

Present paper based on pre-test post-test study to assess the effectiveness of Objective Structured Clinical Examination (OSCE) on obstetrical assessment on Nursing students at selected Nursing colleges at Anand- Kheda district, was carried out by the final year student of Dinsha Patel College of Nursing, Nadiad. The statement of the study was: “A Study to Assess the effectiveness of station-based skill training model through Objective Structured Clinical Examination (OSCE) on obstetrical assessment on Nursing students at selected Nursing colleges at Anand- Kheda district.” The objectives of the study were: (1) To assess the obstetrical assessment score by OSCE. (2) To evaluate the effectiveness of OSCE on obstetrical assessment among nursing students. Research design: Quasi experimental one  group pretest- post-test design research design with Quantitative research approach was used for research study. The researcher used convenient sampling technique for selecting the 40 samples. The tool used in the study were: Structure demographic questionnaires for Section-A & WHO standardized checklist for obstetrics assessment & management of obstetrical emergency. Validity of Tool was assessed by 7 experts. Assessment of the tool was ascertained by the chi-Square formula. Data analysis & Results: In Demographic variables- 16(40%) students were having age 21;  29(72.5%) were female students; 25(62.5 %) Hindu students  ; 14(35%) Final Year B.sc Nursing students, 13(32.5%) First year P.b.B.sc students & 13(32.5%) GNM Students; 21(52.5%) students were living in urban area ; All students-40(100%) having previous knowledge about obstetrical assessment;  34(85%) Students Having hands on experience during clinical training on obstetrical training ; 29(72.5%) Students agreed with having availability of advance models at their college/Institute; 34(85%) students agreed about teachers are doing bedside teaching for procedures on obstetrical assessment; OBG M.Sc. teachers during posting- 14(35%) agreed students; 22(55%) Teachers are doing demonstration of midwifery related  procedure in clinical  & 32(80%) in laboratory area; 15(37.5%) Students are doing redemonstration of midwifery related procedures by student in clinical area  & 21(52.5%) in laboratory area; 26(65%)  students knowing about OSCE & 13(32.5%) students having experience of been through OSCE examination. In Analysis and interpretation of collected data; In both Stations, In Post-OSCE Test, Average score & Average percentage was higher than Pre-OSCE Test score. There was any specific significant increase. This Reveals about effectiveness of OSCE. In Chi-Square (X²) Test, there was significant association between demographic variables-Nursing program, OBG M.Sc. teachers during posting, Demonstration of midwifery related  procedure by teachers in clinical area, Redemonstration of midwifery related procedures by student in clinical area, Experience of been through OSCE examination & Pre OSCE-Test.  Interpretation & Conclusion: In Paired t test analysis for the significance of Pre OSCE-Test and Post OSCE Test; In both Stations, Mean Post OSCE Test score was higher than the mean Pre OSCE-Test score and the paired t-test value greater than the tabulated ‘t’ . This was statistically proved. Hence the Investigator concluded that there was significant increase. So , this reveals that, OSCE is one of the best methods for Evaluation and  to improve clinical practice & decision-making skills in medical field

A Comparative Evaluation of Mono-, Di- and Triglyceride of Medium Chain Fatty Acids by Lipid/Surfactant/Water Phase Diagram, Solubility Determination and Dispersion Testing for Application in Pharmaceutical Dosage Form Development

Purpose To compare physiochemical properties of mono-, diand triglycerides of medium chain fatty acids for development of oral pharmaceutical dosage forms of poorly water-soluble drugs using phase diagrams, drug solubility, and drug dispersion experiments. Methods Phase diagrams were prepared using a monoglyceride (glycerol monocaprylocaprate: Capmul MCM ® EP), a diglyceride (glycerol dicaprylate) and two triglycerides (glycerol tricaprylate

In vitro dispersion test that could serve as a predictive method for assessing performance of lipid-based drug delivery systems

A relatively simple in vitro dispersion test using the USP Dissolution Apparatus II filled with 250 ml of dispersion fluid (0.01M HCl) at 37°C and a rotation speed of 50 RPM was used to assess the performance of lipid-based formulations. Solutions of probucol in mixtures with the surfactant Cremophor® EL with four different medium chain lipids (glyceryl monocaprylocaprate, Capmul® MCM EP; glyceryl dicaprylate; glyceryl tricaprylate, Captex® 8000 EP/NF; caprylic/capric triglyceride, Captex® 355 EP/NF) were formulated and filled into Size 00 hard gelatin capsules (~1 g/capsule) for dispersion testing. Drug concentration in the dispersion fluid and the particle size of the dispersed phase as a function of time were measured with, and without, filtration through 0.45 micron filters. All the lipid/surfactant mixtures dispersed in 80%), indicating suitability for their use in immediate-release formulations. The particle size of the unfiltered samples confirmed whether a microemulsion (1000 nm) was formed. The dispersion test developed here could be used to screen different lipid-based formulations for in vitro performance. Justification for using an in vitro dispersion test to predict in vivo performance of lipid-based drug delivery systems has been provided

Development of Solid SEDDS, II: application of Acconon® C-44 and Gelucire® 44/14 as solidifying agents for self-emulsifying drug delivery systems of medium chain triglyceride.

Self-emulsifying drug delivery systems (SEDDS) are usually isotropic liquids consisting of drugs, lipids, surfactants and/or co-surfactants that spontaneously form fine oil-in-water emulsions in contact with water. Since a solid dosage form has better patient acceptance than a liquid, it was investigated whether liquid SEDDS containing medium-chain lipids (mono- or tri-glycerides) may be converted to solids or semisolids using lauroyl polyoxyl glycerides (Acconon® C-44, ABITEC, and Gelucire® 44/14, Gattefosse) as solidifying agents. Acconon® C-44 and Gelucire® 44/14 were melted at 65EC. The liquid lipids or the liquid lipidsurfactant mixtures, with and without dissolved drug (probucol), were mixed with the melts, and the hot liquid solutions were filled into hard gelatin capsules. The solutions solidified inside the capsules when cooled to room temperature. Acconon® C-44 and Gelucire® 44/14 had a greater propensity for solidifying the triglyceride of medium chain fatty acids (Captex® 355, ABITEC) rather than the monoglyceride. Powder XRD, DSC and microscopic analyses indicated that the lauroyl polyoxyl glycerides crystallized at room temperature, while the lipid or the lipid-surfactant mixtures present in the formulations remained interspersed in between solids as a separate liquid phase. The drug remained dissolved in the liquid phase and there was no crystallization of the drug. Although Acconon® C-44 and Gelucire® 44/14 are themselves surface active, the dispersion testing using the USP apparatus II at 50 rpm and 37EC using 250 ml of 0.01N HCl as the dispersion medium showed that a second surfactant (Cremophor® EL®, BASF) was required in the solid formulation to maximize drug release and dispersion. Formulations containing 1:1 and 3:1 w/w ratios of Captex® 355 and Cremophor® EL produced lipid particles in the range of 200 to 450 nm. Thus, a novel approach of preparing solid SEDDS resulting in submicron emulsions with particle size <500nm is presented

Role of hypogastric artery ligation in obstetrics and gynaecology: a 20-year study at tertiary care center, Ahmedabad, western India

Background: Hypogastric artery ligation (HAL) was first introduced by the end of the 19th century to control intractable haemorrhage from the uterus of women with advanced cervical cancer. Bilateral HAL is a lifesaving procedure in massive pelvic haemorrhage.Methods: This is a retrospective study of 58 cases in which HAL was performed in the obstetrics and gynecology department at tertiary care center from January 2000 to December 2020. History, operative procedure findings, immediate and late postoperative complications, morbidity and mortality data were collected and reviewed from records.Results: In this study, total of 58 women who underwent HAL s; 53 bilateral and 5 unilateral. Fifty-three women required HAL for obstetric indications, in 5 cases it was required for gynaecological indications. 20 cases (34.5%) underwent bilateral HAL for atonic PPH, 16 cases (27.6%) during obstetric hysterectomy for morbidly adherent placenta, 5 (8.6%) for colporrhexis, 2 (3.4%) for broad ligament hematoma, 1 (1.7%) for colporrhexis and left sided broad ligament hematoma, 2 cases (3.4%) for secondary PPH and 7 cases (12.1%) for the ruptured uterus. In gynecological cases 4 cases (80%) underwent after vaginal hysterectomy to control pelvic haemorrhage and 1 case (20%) underwent HAL after myomectomy.Conclusions: HAL is an important surgical procedure and should be performed to reduce blood loss when conservation of the uterus is desired. It is also useful in controlling haemorrhage after major gynaecological surgeries and secondary hemorrhage following hysterectomy.

Development of Solid SEDDS, II: application of Acconon® C-44 and Gelucire® 44/14 as solidifying agents for self-emulsifying drug delivery systems of medium chain triglyceride.

Self-emulsifying drug delivery systems (SEDDS) are usually isotropic liquids consisting of drugs, lipids, surfactants and/or co-surfactants that spontaneously form fine oil-in-water emulsions in contact with water. Since a solid dosage form has better patient acceptance than a liquid, it was investigated whether liquid SEDDS containing medium-chain lipids (mono- or tri-glycerides) may be converted to solids or semisolids using lauroyl polyoxyl glycerides (Acconon® C-44, ABITEC, and Gelucire® 44/14, Gattefosse) as solidifying agents. Acconon® C-44 and Gelucire® 44/14 were melted at 65EC. The liquid lipids or the liquid lipidsurfactant mixtures, with and without dissolved drug (probucol), were mixed with the melts, and the hot liquid solutions were filled into hard gelatin capsules. The solutions solidified inside the capsules when cooled to room temperature. Acconon® C-44 and Gelucire® 44/14 had a greater propensity for solidifying the triglyceride of medium chain fatty acids (Captex® 355, ABITEC) rather than the monoglyceride. Powder XRD, DSC and microscopic analyses indicated that the lauroyl polyoxyl glycerides crystallized at room temperature, while the lipid or the lipid-surfactant mixtures present in the formulations remained interspersed in between solids as a separate liquid phase. The drug remained dissolved in the liquid phase and there was no crystallization of the drug. Although Acconon® C-44 and Gelucire® 44/14 are themselves surface active, the dispersion testing using the USP apparatus II at 50 rpm and 37EC using 250 ml of 0.01N HCl as the dispersion medium showed that a second surfactant (Cremophor® EL®, BASF) was required in the solid formulation to maximize drug release and dispersion. Formulations containing 1:1 and 3:1 w/w ratios of Captex® 355 and Cremophor® EL produced lipid particles in the range of 200 to 450 nm. Thus, a novel approach of preparing solid SEDDS resulting in submicron emulsions with particle size <500nm is presented

Effect of Difference in Fatty Acid Chain Lengths of Medium- Chain Lipids on Lipid/Surfactant/Water Phase Diagrams and Drug Solubility

Lipids consisting of medium chain fatty acids are commonly used in the development of lipid-based selfemulsifying and self-microemulsifying drug delivery systems. However, no systematic approach to selecting one lipid over another has been reported in the literature. In this study, propylene glycol (PG) monoester (PG monocaprylate, Capmul PG-8®) and PG diester (PG dicaprylocaprate, Captex 200P®) of C8-fatty acids were compared with PG monoester (PG monolaurate, Capmul PG-12®) and PG diester (PG dilaurate, Capmul PG-2L®) of C12-fatty acids with respect to their phase diagrams, and especially for their ability to form microemulsions in the presence of a common surfactant, Cremophor EL®, and water. The solubility of two model drugs, danazol and probucol, in the lipids and lipid/surfactant mixtures were also compared. The effect of the chain length of medium-chain fatty acids (C8 versus C12) on the phase diagrams of the lipids was minimal. Both shorter and longer chain lipids formed essentially similar microemulsion and emulsion regions in the presence of Cremophor EL® and water, although the C12-fatty acid esters formed larger gel regions in the phase diagrams than the C8-fatty acid esters. When monoesters were mixed with their respective diesters at 1:1 ratios, larger microemulsion regions with lower lipid particle sizes were observed compared to those obtained with individual lipids alone. While the solubility of both danazol and probucol increased greatly in all lipids studied, compared to their aqueous solubility, the solubility in C12-fatty acid esters was found to be lower than in C8-fatty acid esters when the lipids were used alone. This difference in solubility due to the difference in fatty acid chain length, practically disappeared when the lipids were combined with the surfactant

Istraživanja 3,4-diaril-1,2,5-oksadiazola i njihovih N-oksida: Potraga za boljim COX-2 inhibitorima

A series of 3,4-diaryl-1,2,5-oxadiazoles and 3,4-diaryl-1,2,5-oxadiazole N-oxides were prepared and evaluated for COX-2 and COX-1 binding affinity in vitro and for anti-inflammatory activity by the rat paw edema method. p-Methoxy (p-OMe) substituted compounds 9, 21, 34, 41, 42 showed COX-2 enzyme inhibition higher than that showed by compounds with other substituents. 3,4-Di(4-methoxyphenyl)-1,2,5-oxadiazole N-oxide (42) showed COX-2 enzyme inhibition of 54% at 22 µmol L-1 and COX-1 enzyme inhibition of 44% at 88 µmol L-1 concentrations, but showed very low in vivo anti-inflammatory activity. Its deoxygenated derivative (21) showed lower COX-2 enzyme inhibition (26% at 22 µmol L-1) and higher COX-1 enzyme inhibition (53% at 88 µmol L-1) but marked in vivo anti-inflammatory activity (71% at 25 mg kg-1) vs. celecoxib (48% at 12.5 mg kg-1). Molecular modeling (docking) studies showed that the methoxy group is positioned in the vicinity of the COX-2 secondary pocket and it also participates in hydrogen bonding interactions in the COX-2 active site. These preliminary studies suggest that the p-methoxy (p-OMe) group in one of benzene rings may give potentially active leads in this series of oxadiazole/N-oxides.Sintetizirana je serija 3,4-diaril-1,2,5-oksadiazola i 3,4-diaril-1,2,5-oksadiazol N-oksida i ocijenjena njihova sposobnost vezivanja na COX-2 i COX-1 in vitro i protuupalno djelovanje na edem šape štakora. Spojevi sa p-metoksi (p-OMe) supstituentom 9, 21, 34, 41, 42 bolje su inhibirali COX-2 nego ostali spojevi. 3,4-Di(4-metoksifenil)-1,2,5-oksadiazol N-oksid (42) inhibirao je COX-2 za 54% u koncentraciji od 22 µmol L-1, a COX-1 za 44% u koncentraciji 88 µmol L-1, ali je in vivo slabo djelovao protuupalno. Njegov deoksigenirani derivat 21 pokazao je slabiju inhibiciju COX-2 enzima (26% u koncentraciji 22 µmol L-1) i jaču inhibiciju COX-1 (71% u koncentraciji 25 mg kg-1) što je bolje od standarda celekoksiba (48% u koncentraciji 12,5 mg kg-1). Molekularno je modeliranje pokazalo da je metoksi skupina smještena u blizini sekundarnog džepa na enzimu COX-2 i da utječe na vodikove veze interakcija na aktivnom mjestu COX-2. Ova preliminarna istraživanja sugeriraju da bi se u seriji oksadiazol/N-oksida mogao naći predvodni spoj s p-metoksi skupinom na benzenskom prstenu