PREPARATION AND EVALUATION OF METOLAZONE SOLID DISPERSIONS AND FAST DISSOLVING TABLETS USING STERCULIA FOETIDA SEED STARCH AND PLASDONE K-29/32 AS SUPERDISINTEGRANTS

Objective: The objective of the current study is to improve the solubility of the Biopharmaceutical Classification System (BCS) Class-II drug, Metolazone, using various superdisintegrants. Methods: Starches were extracted from Sterculia foetida seed powder by water and alkali techniques i.e., sodium hydroxide at 0.1%, 0.25% and 0.5% concentrations. Several phytochemical and physicochemical parameters were evaluated on the extracted starches. Solid dispersions of Metolazone were prepared by the solvent evaporation technique using plasdone K-29/32 alone and by mixing plasdone K-29/32 with Sterculia foetida seed starch. Various physical parameters were evaluated for the prepared solid dispersions. Tablets were prepared using Metolazone solid dispersions and varying concentrations of Sterculia foetida seed starch by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization using Scanning Electron Microscopy (SEM) and stability studies. Results: Phytochemical tests showed the presence of starch in all extracts. Starch prepared from 0.1% sodium hydroxide (SFS2) showed best physicochemical properties. In vitro dissolution studies revealed that solid dispersion MS4 containing Metolazone and plasdone K-29/32 in 1:3 ratios showed better drug release. Formulation MPT6 containing MS5 solid dispersion with 15% w/w of SFS2 showed enhanced drug release. SEM studies revealed no major interactions between drugs and excipients. Accelerated stability studies showed that all tablets were stable. Conclusion: Sterculia foetida seed starch and plasdone K-29/32 have enhanced the solubility of Metolazone

HUBUNGAN ANTARA REGULASI DIRI DENGAN ACADEMIC SELF-HANDICAPPING PADA MAHASISWA FAKULTAS TEKNIK UNIVERSITAS DIPONEGORO YANG SEDANG MENGERJAKAN TUGAS AKHIR

Kewajiban mahasiswa untuk menyelesaikan tugas akhir sebagai syarat kelulusan, telah menyebabkan munculnya indikasi strategi pertahanan harga diri yang justru merugikan mahasiswa. Academic self-handicapping adalah salah satu bentuk strategi perlindungan harga diri yang dapat menurunkan kualitas hidup dan prestasi akademik. Pada sisi lain, regulasi diri terbukti memiliki hubungan positif dengan pencapaian akademik yang dibutuhkan mahasiswa, terutama mahasiswa yang sedang mengerjakan tugas akhir. Penelitian ini dilakukan untuk mengetahui hubungan antara regulasi diri dan academic self-handicapping. Populasi penelitian ini adalah 1914 mahasiswa Fakultas Teknik Undip yang sedang mengerjakan tugas akhir dan 144 orang diambil sebagai sampel menggunakan convenience sampling. Pengukuran dalam penelitian ini dilakukan menggunakan Skala Regulasi Diri (41 aitem; α = 0,914) dan Skala Academic Self-Handicapping (27 aitem; α = 0,858). Uji korelasi Spearman Brown menunjukkan hubungan negatif yang signifikan antara regulasi diri dengan academic self-handicapping yang ditunjukkan dengan rxy = -0,229 dan p = 0,006 (p < 0,01). Semakin tinggi regulasi diri, maka semakin rendah academic self-handicapping. Mahasiswa yang sedang mengerjakan tugas akhir diharapkan dapat meminimalisir academic self-handicapping dengan menerapkan regulasi diri selama mengerjakan tugas akhir. Kata kunci: regulasi diri, academic self-handicapping, mahasiswa, tugas akhi

In-Vivo Evaluation of Some Novel Chromen- 2 One Based on Pharmacological Activity of Antipsychotic Drug

Most neuroleptics block the emesis hyper activity and aggression induced by apomorphine and other dopaminergic agonists. In higher doses, most neoroleptics induce characteristic cataleptic immobility that allows the animal to be placed in abnormal postures that persists, the aim of this project work was to carry out preliminary pharmacological screening of 2-[(4-methyl-2-oxo-2H-chromen-7-yl) oxy-(aryl)] acetamide. preliminary pharmacological screening of the synthesized compounds for the antipsychotic activity. The screening was limited to in vivo models only. The synthesized compounds were converted to their hydrochloride salts in order to make them water-soluble. These hydrochloride salts were used for the pharmacological testing purpose. The experiments were performed on Swiss albino mice (male) and the route of administration was intra peritoneal

FORMULATION AND EVALUATION OF FEBUXOSTAT FAST DISSOLVING TABLETS USING ENTADA SCANDENS SEED STARCH AND POLOXAMER-188 AS SUPERDISINTEGRANTS

Objective: The present study focused on solubility enhancement of the Biopharmaceutical Classification System (BCS) Class-II drug, Febuxostat using various super disintegrants. Methods: Starches were extracted from Entada scandens seed powder by alkali method i.e., sodium hydroxide at 0.1%, 0.25% and 0.5% concentrations and water. Starches were evaluated for various phytochemical and physicochemical tests. Solid dispersions of Febuxostat were prepared by fusion method using poloxamer-188 alone and by mixing poloxamer-188 with Entada scandens seed starch. Various physical parameters were evaluated for these solid dispersions. Tablets were prepared using Febuxostat solid dispersions and varying concentrations of Entada scandens seed starch by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) and stability studies. Results: Phytochemical tests revealed the presence of starch in all extracts. Starch prepared from 0.5% sodium hydroxide (ESS4) showed best physicochemical properties. In vitro dissolution studies revealed that solid dispersion F4 containing Febuxostat and poloxamer-188 in 1:3 ratios showed better drug release. Formulation FE5 containing F4 solid dispersion with 12.5% w/w of ESS4 showed enhanced drug release. FT2 tablets having 12.5% w/w of ESS4 showed better drug release when compared to others. FTIR and DSC studies revealed no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Accelerated stability studies showed that all tablets were stable. Conclusion: The super disintegrant property of Entada scandens seed starch was evaluated

PREPARATION AND EVALUATION OF DOLUTEGRAVIR SOLID DISPERSIONS

Objective: The current work mainly focuses on solubility enhancement of dolutegravir which is a BCS (Biopharmaceutical Classification System) class-II drug using various excipients. Methods: Solid dispersions of dolutegravir were prepared by solvent evaporation and fusion methods using carriers like poloxamer-188 and plasdone K-29/32 in different ratios (1:0.5 to 1:3.0). The amount of dolutegravir used was kept constant and the polymer concentrations were increased. Various physical parameters like angle of repose, carr’s index, Hausner’s ratio were calculated for the prepared solid dispersions. They were also evaluated for particle size and drug content uniformity along with in vitro drug release. Characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD) were also done. Results: Dolutegravir solid dispersions showed good to excellent flow properties. From in vitro dissolution studies, it was observed that the solid dispersion formulation DF3 containing dolutegravir and poloxamer-188 in 1:1.5 ratios prepared by fusion method showed better dissolution rate when compared with other formulations. The dissolution parameters were also evaluated. DF3 showed a higher drug release of 86.33% in 60 min. FTIR and DSC studies revealed that there were no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Conclusion: The solid dispersions prepared using poloxamer-188 by fusion method has enhanced the solubility of dolutegravir

A COMPARATIVE STUDY BETWEEN THE CUSTOMARY INHERITANCE LEGAL SYSTEM OF THE COMMUNITY AND THE ISLAMIC INHERITANCE LEGAL SYSTEM ON INHERITANCE DISTRIBUTION IN MUKOMUKO CITY DISTRICT OF MUKOMUKO REGENCY

The writing of this research aims to: (1) understand and explain the inheritance distribution system according to the customary inheritance law of the Mukomuko community; (2) understand and explain the inheritance distribution system according to the Islamic inheritance law; (3) understand, study, and compare between the customary inheritance system of the community and the Islamic inheritance legal system on the inheritance distribution. This research used a normative research method with a comparative approach. A comparative approach is an approach to investigate the similarities and differences in things, people, work procedures, ideas, and critics towards other people, groups, and people’s perspectives on a group, a country, or an event. This research revealed that: (1) the inheritance distribution system according to the clan customary inheritance law, either high heirloom property (known as Harta Pusaka Tinggi) or matrimonial property, is subjected to matrilineal principles (the inheritance right of daughters are greater than the sons); (2) the inheritance distribution system according to the Islamic inheritance system is subjected to Qur’an with patrilineal principles (the inheritance right of sons are greater than the daughters); (3) the comparison of inheritance distribution according to the customary legal system of the community and the Islamic inheritance legal system have some similarities and differences. Both systems have tangent points in which the customary law of the community is individual-collective which is under the matrilineal principles while the Islamic inheritance law is individual-bilateral which is under the patrilineal principles. Keywords: A comparative study, the customary inheritance law of the community, the Islamic inheritance law

STUDY OF INFLUENCE OF FORMULATION AND PROCESS VARIABLES ON ENTRAPMENT EFFICIENCY AND PARTICLE SIZE OF FLOATING MICRO BALLOONS OF DIPYRIDAMOLE BY DOE

Objective: In the current research work, dipyridamole, a BCS class–II drug, was aimed to be formulated as floating controlled release microballoons using ethyl cellulose as polymer and span 80 as surfactant to improve the gastric retention of drug as the multi-particulate dosage forms have tremendous advantages over single unit dosage forms. Methods: Microballoons were prepared by the emulsion solvent evaporation method. Prepared microballoons were characterized for entrapment efficiency, particle size, floating behavior and drug release studies. The study of effect of various formulation and process parameters like surfactant concentration, solvent volume, the volume of internal phase, polymer concentration, rotation speed on the drug entrapment efficiency and particle size of the microballoons were carried by using Box–Benhken to optimize the formulated microballoons. Results: The smallest particle size of the microballoons was found to be 205.9 µm in the F32 formulation. The highest drug entrapment efficiency was found to be 93.4% in the F34 formulation. Buoyancy studies showed all the formulations have good floating characteristics that lasted for a minimum of 24 h. The maximum yield of microballoons was found in the F7 formulation with 91.8% yield. The final results were statistically treated using ANOVA and were found to be significant (p value&lt;0.05). Conclusion: Thus, the obtained results and their statistical interpretations indicated floating microballoons of dipyridamole were formulated effectively

PHYTOCHEMICAL AND PHARMACOLOGICAL EVALUATION OF COMMIPHORA MUKUL FOR ANTIDEPRESSANT ACTIVITY IN ALBINO MICE

Objective: The main aim and objective of the present study is to investigate the effect of Commiphora mukul (Family: Burseraceae), on depression in mice using tail suspension test (TST) and forced swim test (FST).Methods: The oleo-gum resin of guggul was extracted with alcohol and fractionated with ethyl acetate and petroleum ether. All the fractions were subjected for preliminary phytochemical screening, using various qualitative tests. Till date, no scientific data were available on the antidepressant activity of this plant. So, in the present investigation, TST and FST are selected as animal models for evaluation of antidepressant activity in albino mice.Results: The preliminary phytochemical screening of guggul has revealed the presence of carbohydrates, proteins, tannins, and flavonoids in hydroalcoholic fraction. Ethyl acetate fraction showed positive results toward flavonoids, alkaloids, proteins, and steroids. Hydroalcoholic, ethyl acetate, and petroleum ether fractions (50 and 100 mg/kg p.o.) of guggul administered orally for 14 successive days had decreased the immobility periods significantly in a dose-dependent manner in both TST and FST, showing significant antidepressant-like activity. The activities of the fractions were found to be comparable to imipramine in both FST and TST.Conclusions: Although a number of synthetic drugs are being used as standard treatment for clinically depressed patient, they have adverse effects that can compromise the therapeutic treatment. In the traditional systems of medicine, many plants and formulations have been used to treat depression for thousands of years. The results of this study indicate the potential for the use of guggul as an adjuvant in the treatment of depression.Keywords: Guggul, Commiphora mukul, Antidepressant activity, Forced swim test, Tail suspension test, Depression

Formulation and Evaluation of Liquid Loaded Tablets Containing Docetaxel-Self Nano Emulsifying Drug Delivery Systems

Purpose: To prepare and characterize tablets loaded with self-nanoemulsifying drug delivery system (SNEDDS) containing docetaxel (DTL).Method: SNEDDS of docetaxel were prepared using various oils, surfactants, co-surfactant and solvents to improve the dissolution rate and bioavailability of the poorly water-soluble chemotherapeutic agent. The SNEDDS components were preliminarily screened for the solubility of the drug in various vehicles, miscibility of excipients, rate of emulsification and ternary phase diagrams. The tablets were prepared by direct compression process with a porous carrier, magnesium alumino-metasilicate, and subsequently loaded with SNEDDS by a simple absorption method. The tablets were then characterized for physical parameters, including tablet hardness, weight variation, disintegration, drug content and invitro drug release.Results: Cremophor-EL, polysorbate-80 and dehydrated alcohol mixture in the ratio 85:10:5 yielded docetaxel SNEDDS with droplet size of 12.16 nm and polydispersity (PDI) of 0.039. Tablets with high porosity suitable for loading with SNEDDS and containg the super-disintegrants, crosscarmellose sodium and sodium starch glycolate, in a concentration of 3, 4 and 5 %, achieved complete dissolution of docetaxel from the tablets. In vitro release of docetaxel from SNEDDS and the tablets was similar (p &lt; 0.05).Conclusion: SNEDDS of docetaxel is a promising approach to achieving a solid dosage form of the liquid-loaded drug delivery systems for enhancing the solubility and dissolution rate of the drug, and hence also its bioavailability.Keywords: Docetaxel, Drug carrier, SNEDDS, Self-nanoemulsifying, Solubility, Drug release, Anicancer, Surfactant, Co-surfactan

Eisenmenger syndrome in a patient with ventricular septal defect: a case report

Eisenmenger Syndrome (ES) represents Pulmonary Arterial Hypertension (PAH) associated with Congenital Heart Defects (CHD). Although patients survive until their third or fourth decades of life, the symptoms include dyspnea, cyanosis, fatigue, dizziness, and syncope. In addition, cardiac arrhythmias, a late complication are causing sudden death in patients with ES. Treatment options have been limited; however, recent successes have been achieved with the use of therapies targeted against the pathophysiological pathways that underlie PAH. The dual endothelin receptor antagonist and prostacyclins demonstrated to improve hemodynamics of the patients. This is the case of a 16 year old young female with ventricular septal defect that was admitted with increasing shortness of breath and cyanosis with clubbing which are clinical features of Eisenmenger syndrome. She was medicated with Furosemide, Sildenafil which improved her functional status