DSpace Collection: PhD Thesis by Research Scholars of FoHS department

Evaluation of Anti-Diabetic Activity and Phytochemical Screening of Oroxylum Indicum Plant

2025-09-04T07:58:41Z

Title: Evaluation of Anti-Diabetic Activity and Phytochemical Screening of Oroxylum Indicum Plant Authors: Dhabaliya, Falgun Gunvantray; Dr. Mital, N. Manvar

Screening Of Indigenous Plants For Anticoagulant Activity And Isolation Of Active Constituent There From

2025-01-29T05:48:08Z

Title: Screening Of Indigenous Plants For Anticoagulant Activity And Isolation Of Active Constituent There From Authors: Katbamana, Rachanakumari V.; Manvar, Mital Abstract: Introduction: Blood coagulation is a vital, strictly controlled mechanism that creates clots quickly. On the other hand, blood coagulation abnormalities are frequently noted in several medical disorders. To find new uses for this plant, this study investigated the anticoagulant activity of methanolic extracts of Citrus medica fruit, Tecomella undulata bark, and Sesame indicum seed using in vitro techniques. Material and method: 70% methanol was used to extract the dried and powdered Citrus medica fruit, Tecomella undulata bark, and Sesame indicum seed. The concentrated dried crude extracts (CMME, TUME, and SIME) were then subjected to an analysis of their in-vitro anticoagulant activity on blood coagulation profile, including activated partial thromboplastin time (aPTT), prothrombin time (PT), and clotting time (CT). Petroleum ether, benzene, ethyl acetate, and butanol were used in a liquid partitioning process for the CMME and TUME extracts. The fractions were examined in vitro for their antioxidant potential, blood coagulation profile, clotting time (CT), prothrombin time (PT), and activated partial thromboplastin time (aPTT) at varying concentrations (2.5–10 mg/mL). The greatest anticoagulant fraction (the butanol fraction of TUME (TUBUF) and the ethyl acetate fraction of CMME (CMEAF)) was subjected to GCMS analysis. Using an animal model for seven days, the in-vivo anticoagulant activity of CMEAF (100, 200, and 400 mg/kg) was determined. The bioactive chemical constituents or constituents responsible for the anticoagulant activity were discovered by FTIR and HPTLC after being isolated by preparative TLC. Using the LCMS/MS technique, the bioactive molecule was quantified. Result: Prothrombin time (PT) (20.1, 18.83 seconds) activated partial thromboplastin times (APTT) (93.67, 63.67 seconds), and clotting time (18.29 ± 0.8, 15.37 ± 0.91 minutes) were all significantly (p<0.05) extended when administered with CMME and TUME 200 mg/kg. At a concentration of 7.5 mg/mL, the ethyl acetate fraction of Citrus medica (clotting time: 21.85 minutes; PT: 91.33 seconds; APTT: 114.67 seconds) and the butanol fraction of Tecomella undulata (17.95 minutes; PT: 48.33 seconds; APTT: 114.67 seconds) showed the highest prolongation significantly (P<0.001) prolonged effect. Ten compounds in Tecomella undulata's butanol fraction and fifteen compounds in Citrus medica's ethyl acetate fraction have antioxidant and anticoagulant activity, according to GCMS analytical data. Additionally, when compared to warfarin as standard, CMEAF prolongs clotting time, PT, and APTT in the in-vivo model at a dose of 200 mg/kg for five days. It was found that the amounts of gallic acid, quercetin, and rutin in CMEAF were 514.543 ng, 67.839 ng, and 53.691 ng, in that order. Ferulic acid, the isolated chemical, was verified using an FTIR chromatogram and an HPTLC fingerprint. Conclusion: The results of the study demonstrate the potential of Tecomella undulata, particularly its butanol fraction, as an antioxidant and anticoagulant, as well as a promising and unexplored source of bioactive compounds (pentanedioic acid, 2-oxo-dimethyl ester) with potential therapeutic applications. The ethyl acetate fraction of citrus medica, which is rich in flavonoids, may include bioactive substances such as gallic acid, quercetin, rutin, and ferulic acid that have anticoagulant qualities. This offers a possible route for the creation of brand-new anticoagulant medications. It can be investigated further to create novel treatments that address a range of medical issues.

Formulation And Development Of Solid Self Emulsifying Drug Delivery Systems Of Antihypertensive Drugs

2024-05-03T10:01:19Z

Title: Formulation And Development Of Solid Self Emulsifying Drug Delivery Systems Of Antihypertensive Drugs Authors: Buddhadev, Sheetal Sandip; Dr. Kevinkumar, C. Garala Abstract: Benidipine (BD), a dihydropyridine calcium channel blocker indicated in hypertension angina therapy, presents challenges with oral bioavailability owing to hepatic first-pass metabolism and high lipophilicity (log P of 4.28).In order to boost its bioavailability, numerous approaches, such as solid dispersions and nanosuspensions, have been investigated. Similarly, telmisartan (TEL), an angiotensin II receptor antagonist for hypertension, has problems with oral bioavailability owing to low solubility and high permeability. It is frequently administered together with other antihypertensive medicines, such as calcium channel blockers, for the treatment of hypertension with renal failure. Despite the excellent therapeutic use of both medications, BD and TEL experience different pharmacological issues due to their low solubility, as they both belong to BCS class II. Thus, in order to obtain the primary therapeutic advantages from the combination of BD and TEL in a single carrier, the smart drug delivery technique, i.e., the lipid-based drug delivery system, has been utilized in the present investigation in order to improve the bioavailability of both medications. The most advantageous lipidbased drug delivery methodology that may address the above-described challenges is SNEDDS. The goal of the present study is to evaluate the possibility of creating solid SNEDDSs as potential carriers for the oral administration of Benidipine and Benidipine (BD) with Telmisartan (TEL), applying the Quality by Design (QbD) approach. Based on pre-formulation and risk assessment studies, the maximal drug solubility in each oil, surfactant, and co-surfactant was selected. Ternary phase diagrams were generated for BD with Labrafil M 2125 CS (oil), Kolliphor EL (surfactants), and Transcutol P (co-surfactant) at 1:1, 2:1, and 3:1 ratios for determining the largest region for the creation of thermodynamically stable nanoemulsions. Similarly, utilizing Eucalyptus Oil, Kolliphor EL, and Transcutol P, the BD with TEL SNEDDS was created. The oil phase, the screened surfactant, and the co-surfactant have been employed for creating phase diagrams of BD with TEL in differing weight ratios of 1:1, 2:1, 3:1, 1:2, and 1:3. The central composite design has been selected for BD, and the Box-Behnken design (BBD) has been generated for BD with TEL to optimize various variables. Zeta potential, drug concentration, resistance to dilution, pH, refractive index, viscosity, thermodynamic stability, and cloud point were further examined in the most efficient formulation. Optimized formulation BD14 contained Benidipine (4mg), Labrafil M2125 Cs (30%), Kolliphor EL (45%), and Transcutol P (50%), which had a globule size of 156.20 ± 2.40 nm, PDI of 0.25, zeta potential of -17.36 ± 0.18 mV, selfemulsification time of 65.21 ± 1.95 sec, % transmittance of 99.80 ± 0.70%, and drug release of 92.65 ± 1.70% at 15 min. Similarly, BD with a TEL formulation was further investigated. The optimized formulation BT11 contained Benidipine (4mg), Telmisartan (40 mg), Eucalyptus oil (60%), Kolliphor EL (35%), and Transcutol P (10%), which had a globule size of 175.12±2.70 nm, a PDI of 0.226, a zeta potential of −24.98 ± 0.18 mV, a self-emulsification time of 53.00±2.10 sec, a % transmittance of 99.6±0.3%, and a drug release of 92.65±1.70 at 15 min. S-SNEDDS have been generated utilizing the adsorption process and investigated with FTIR, DSC, SEM, and PXRD. Neusilin US2, L-SNEDDS: Adsorbent (1:1.5), was selected as the carrier for pores in a mixture with excellent flow rate, flow ability, highest drug content, and drug release in order to facilitate further exploration of BD14 and BT11. In contrast to the percentages of 58.80% and 60.15% for the pure drug BD and a commercial specimen of BD, L-SNEDDS and S-SNEDDS of BD14 demonstrated that BD released more than 85% of its contents after 15 minutes and 100% after 60 minutes (f2< 50). Similarly, in contrast to the percentages of 50.1% and 58.1% for the pure drug BD, a commercial specimen of BD with TEL, L-SNEDDS, and S-SNEDDS of BT11 showed that BD released more than 85% of its contents after 15 minutes and 100% after 60 minutes (f2< 50). Similarly, when compared to the percentages of 48.7% and 59.8% for the pure drug TEL and a commercial specimen of BD with TEL, L-SNEDDS and S-SNEDDS of BT11 demonstrated that TEL released more than 85% of its contents after 15 minutes and 100% after 60 minutes (f2< 50). The release of drug kinetics of LSNEDDS of BD14, BT11, and S-SNEDDS of BD14, BT11, follow 1st-order kinetics, which shows the drug release from the porous matrix corresponds to the amount of drug remaining in its interior. The pharmacodynamics study results reveal that S-SNEDDS of BD and BD with TEL displayed greater bioavailability compared to both pure BD and BD with TEL medicines. After six months of storing at 40±2°C and 75±5% relative humidity, the BD-loaded S-SNEDDS of BD14 samples and the BD with TEL-loaded S-SNEDDS of BT11 exhibited no observable changes in emulsification efficacy, size of the globules, percentage of transmission, or release of the drug over a period of fifteen minutes. These results indicate that BD14 and BT11 in the boosted S-SNEDDS display chemical and structural stability. Consequently, research demonstrates that the production of oral S-SNEDDS of benidipine and benidipine with telmisartan may be advantageous for boosting BD and BD with TEL's water solubility, as well as the future delivery technique that may deliver both drugs to treat hypertension for enhanced treatment.

Spectroscopic and Chromatographic Method Development and Validation for the estimation of Antimicrobial Agents and their combinations in Synthetic Mixture and Assay Method for the Pharmaceutical Dosage Forms

2024-02-23T07:45:27Z

Title: Spectroscopic and Chromatographic Method Development and Validation for the estimation of Antimicrobial Agents and their combinations in Synthetic Mixture and Assay Method for the Pharmaceutical Dosage Forms Authors: Pandya, Yogi Umeshbhai; Dr. Samixa, R. Patel Abstract: Background: The present research work comprises of the Stability Indicating RP-HPLC newlineanalytical method development and validation for selected drugs andamp; pharmaceutical dosage newlineforms belonging to the Antimicrobial class. The antimicrobial drugs are frequently upgraded newlineand newly approved drugs by FDA and CDSCO are available in the markets in the form of newlinenew dosage forms as well as combined dosage forms with other drugs. For the newly newlineapproved drugs and their drug combinations, the Stability analytical methods are not newlineavailable in pharmacopoeia and even dissolution methods for the solid dosage forms are also newlinenot available for the combined dosage forms. Hence there is a need of newer analytical newlinemethods, as well as stability, indicating rapid- RP-HPLC technique and it is optimised for, newlineanalysis of drug during different stress conditions as well as in pure from and solid dosage newlineform along with the in-vitro dissolution studies carried out for solid dosage forms. Aim: The newlinemain aim of the present research work to develop and validate spectroscopic andamp; newlinechromatographic analytical methods for the estimation of antimicrobial agents and their newlinecombinations in synthetic mixture and assay method for the pharmaceutical dosage forms. newlineMaterials and Methods: Working Standard drugs- Doravirine, Lamivudine, Tenofovir, newlineCabotegravir, Rilpivirine, Dolutegravir, Fexinidazole, Maribavir, Molnupiravir, Amoxicillin, newlineClarithromycin, Vonoprazan, Combined formulations, Chromatographic HPLC system newlineShimadzu LC-20-AT, UV Spectrophotometer systronics andamp; shimadzu-1800, Hypersil- newlinecoloumn ODS-C18 ( 250 mm x 4.6 mm, 5 µm id), Analytical balance, sonicator, Dissolution newlineapparatus Veego Microprocessor. Results andamp; Discussions: The Stability Indicating RP-HPLC newlinemethods for selected antimicrobial drugs have been developed andamp; validated using ICH newlinerecommendations, which demonstrate its accuracy, precision andamp; robustness of the procedures. newlineThe ICH parameters Accuracy, Precision, LOD, LOQ, Linearity, Range, Selectivity were newlinesuccessfully performed