JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA

A Case Report of Lurasidone-Induced Tardive Dyskinesia: Therapeutic Role of Valbenazine

2024-12-06T07:50:34+07:00

Background: Tardive dyskinesia (TD) is a complex, potentially irreversible movement disorder primarily associated with the long-term use of antipsychotic medications, particularly typical neuroleptic drugs. TD can develop during treatment and persist long after the discontinuation of the culprit medication. The etiology of this condition involves dysregulation of dopaminergic signalling, especially within the striatum, leading to activation of D2 dopamine receptors. This imbalance affects the homeostasis of neurotransmitters, including GABA and Glu. Chronic dopamine receptor antagonism incites neuroadaptive alterations that may linger post-therapy, resulting in abnormal involuntary movements affecting the orofacial regions, limbs, and trunk, which profoundly diminish patient quality of life. Case: A 29-year-old female with a known history of schizophrenia presented with sudden-onset neurological symptoms, notably persistent orofacial dyskinesias such as lip smacking and grimacing, which had developed over a 24-hour period. A thorough review of her medications indicated that lurasidone, classified as an atypical antipsychotic, was likely responsible for the onset of these dyskinetic movement features. Consequently, the physician opted to discontinue lurasidone and initiate valbenazine at 40 mg once daily with the intent of managing the dyskinetic symptoms while considering the overall psychiatric and medical treatment plan for the patient. Conclusion: The emergence of orofacial dyskinesias in this patient suggests a possible adverse reaction to lurasidone, necessitating re-evaluation of her psychopharmacological regimen. Valbenazine, a selective vesicular monoamine transporter 2 inhibitor, may provide a tailored approach to mitigate dyskinetic movements, while maintaining therapeutic efficacy in psychiatric care.

The Effect of Quercetin on Coenzyme HMG-CoAR, ABCA1 Transporter, Dyslipidemia Profile and Hepatic Function in Rats Dyslipidemia Model

2024-11-25T08:53:59+07:00

Background: Dyslipidemia is a lipid metabolic disorder that increases the risk of cardiovascular disease, typically marked by abnormalities in triglycerides (TG), low-density lipoprotein (LDL), and total cholesterol (TC), along with decreased high-density lipoprotein (HDL) levels. This study explored the potential of quercetin, a natural substance, as a preventive agent against dyslipidemia induced by high-fat diet (HFD) in a rat model. Simvastatin, a standard cholesterol-lowering drug, was used for the comparison. Objective: The main objective of this research was to evaluate the potential of quercetin in lipid metabolism for dyslipidemia caused by HFD and compare its effects with the first-line drug therapy simvastatin, which has a similar mechanism. Methods: Rats fed a HFD were treated with quercetin and simvastatin, and their lipid profiles, liver enzyme activities, and molecular markers related to cholesterol metabolism were analyzed. Results: Quercetin markedly decreased cholesterol levels by inhibiting the enzyme 3-Hydroxy-3-Methylglutaryl-CoA Reductase (HMG CoAR). Cellular observation revealed that it also prevented liver damage and showed a protective effect on liver enzyme activity. Quercetin enhanced the expression of the Adenosine Triphosphate Binding Cassette subfamily A member 1 (ABCA1) protein, showing a protective effect against dyslipidemia akin to simvastatin, yet with a reduced likelihood of liver toxicity. Conclusion: Quercetin may serve as an effective and safer alternative to simvastatin for treating dyslipidemia, offering cholesterol-lowering benefits without hepatotoxic risks associated with long-term statin therapy.

Antidiarrhea Activity of Ethanol Extract of Rambutan Leaves (Nephelium lappaceum L.) in Capsule Form on Male Mice

2024-12-10T12:10:01+07:00

Background: Diarrhea is characterized by changes in stool form to soft or liquid, with an intensity of bowel movements more than three times a day. One of the plants used as an alternative treatment for diarrhea is rambutan, particularly its leaves. Previous studies have shown that rambutan leaf extract can treat diarrhea. Objective: The purpose of this study was to determine the antidiarrhea activity of ethanol extracts of rambutan leaves containing tannins and flavonoids that inhibit intestinal motility. Methods: This study was conducted experimentally using the intestinal transit method, which measures the length of the intestine passed through a marker. The smaller the ratio between the length of the intestine and the marker, the greater the decrease in intestinal motility in the mice. Group 1: loperamide HCl at a dose of 4 mg/kg BW; Group 2: placebo; Group 3: FI, FII, and FIII capsules at doses of 50 mg, 100 mg, and 150 mg. Results: The test results showed that Formulations 1, 2, and 3 had activities of 23.3%, 26.8%, and 32.3%, respectively. The capsule with the best results was formulation 3, at a dose of 150 mg. Compared with the positive control, the effectiveness of this capsule was 22% higher than that of loperamide. Conclusion: The results of this study showed that rambutan leaves extracted in capsule form effectively treats diarrhea. The one-way ANOVA test showed a significant difference between the FI, FII, and FIII groups (p <0.05).

A Comprehensive Evaluation of Antibiotic Usage: Establishing a Foundation for Effective Antimicrobial Stewardship

2024-12-09T22:44:50+07:00

Background: The intensive care unit (ICU) is a significant area of antibiotic use, accounting for a substantial proportion of the overall antibiotic consumption. The inappropriate use of antibiotics in such settings has a notable impact on the emergence of antimicrobial resistance. Objective: This study evaluated the rationality of antibiotic use in the ICU of RSUD Abdul Moeloek Hospital in Lampung Province. Methods: This study was conducted between December 2022 and February 2023 using a prospective method and purposive sampling. An evaluation was conducted using the Anatomical Therapeutic Chemical/Defined Daily Dose (ATC/DDD) system for quantitative analysis and Gyssens criteria for qualitative assessment. The research subjects comprised 55 individuals, the majority of whom were male (58.2%), aged > 65 years (29.1%), remained in the ICU for less than seven days (78.2%), and subsequently continued their treatment in a non-ICU (69.1%). Results: Quantitative analysis demonstrated that the total number of antibiotics administered in this study was 394.83 DDD, with a DDD/100 patient-day value of 113.78. Ceftriaxone was the most frequently prescribed antibiotic (219 DDD), whereas gentamicin was the least frequently prescribed (1 DDD). Qualitative analysis revealed that 17.6% of the patients exhibited irrational antibiotic use. Conclusion: Irrational use of antibiotics was observed in the following categories: IV A (1.1%); IV D (2.2%); III A (2.2%); III B (2.2%) IIA, (3.3%); IIB (5.5%); and I (1.1%). The study concluded that there was still a considerable degree of irrational antibiotic use.

In Silico Analgesic and Toxicity Analysis of Modified Paracetamol on COX-2 Receptor (PDB ID: 3LN1)

2024-11-08T17:59:23+07:00

Background: Paracetamol is often used as the main analgesic in Indonesia. The use of more than 4 g/day or a single dose above 10 g can cause hepatotoxicity. This can be overcome by modifying the structure through a computer-aided drug design (CADD) approach, particularly molecular docking, which aims to produce compounds with greater potency and fewer side effects. Objective: This study aimed to determine the analgesic activity and toxicity of paracetamol derivatives modified using the Topliss method. Methods: Analgesic activity was tested by molecular docking of the COX-2 receptor (PDB ID 3LN1) using AutoDock Tool 4.2 and toxicity testing using pkCSM and Protox Online Tool. Results: The results of docking showed that the free binding energy values for test compounds 1 to 5 are -10.59 kcal/mol, -10.17 kcal/mol, -8.79 kcal/mol, -10.01 kcal/mol, and -9.32 kcal/mol, respectively, with corresponding inhibition constants of 17.29 nM, 35.21 nM, 360.88 nM, 46.36 nM, and 146.65 nM. These values are lower than paracetamol, which has a free binding energy of -6.21 kcal/mol and an inhibition constant of 28,043 nM. The results showed that the test compound was more stable in ligand-receptor binding. Toxicity tests showed that all the test compounds and paracetamol belonged to toxicity class IV. The test compound had an LD₅₀ value of 1551 mg/kg, which was higher than that of paracetamol (338 mg/kg), indicating better effectiveness. Conclusions: Compound 2 was predicted to have the best biological activity and potential as an alternative to paracetamol.

Solubilization Inclusion Bodies from Synthetic Recombinant PGA Gene Expressed in E. coli BL21(DE3) by Denaturing and Non-denaturing Agents

2024-11-19T10:56:22+07:00

Background: With the rise in green chemistry, the synthesis of antibiotic compounds through enzymatic processes is a preferred option. Penicillin-G acylase (PGA) is an important enzyme for producing important antibiotics, such as penicillin and its derivatives. Therefore, studies on PGA have been conducted worldwide. In the penicillin biosynthetic pathway, PGA catalyzes the conversion of penicillin G into 6-amino penicillanic acid (6-APA), a precursor for the enzymatic synthesis of penicillin derivatives. Unfortunately, bacteria naturally produce PGA in small quantities. Objective: One strategy for producing this enzyme in large quantities is DNA recombination, which is expressed in Escherichia coli. The formation of inclusion bodies (IBs) is a common obstacle to protein overexpression in Escherichia coli. In this study, we discuss IBs solubilization methods for recombinant PGA derived from E. coli (rPGAEc) expressed in E. coli BL21 (DE3). Recombinant E. coli BL21 (DE3) cells harboring rPGAEc were induced with IPTG for enzyme expression. Induction was performed at 16 °C for 4 h and 24 h. The PGA enzyme expressed in the IBs form was then incubated in two solutions containing 8 M urea and 0.2% sarcosine to obtain a soluble enzyme. Results: Based on protein analysis by SDS-PAGE, a solution containing 8 M urea solubilized PGA more abundantly than 0,2% sarcosine. Conclusion: The solubilization technique of PGA expressed by E. coli proposed in this study is an alternative solution that can be considered for this purpose.

Formulation And Physical Evaluation of Body Scrub Cream From 95% Ethanol Extract of Breadfruit Peel (Artocarpus altilis) as Antioxidants

2024-12-11T13:04:04+07:00

Background: Breadfruit (Artocarpus altilis) peel contains many chemical compounds including alkaloids, flavonoids, saponins, polyphenols, and steroids/terpenoids. Breadfruit peel has potential as an antioxidant because it contains phenolic compounds, especially flavonoids and polyphenols. Objective: The aim of this study was to formulate and physically evaluate the preparation of a scrub cream from a 95% ethanol extract of breadfruit peel (Artocarpus altilis) and test its antioxidant activity. Methods: Body scrub cream formulations were prepared using different extract concentrations, such as F1 (no extract), F2 1%, F3 3%, F4 5%, and F5 (Vit C as an equalizer for the antioxidant activity test). Body scrub cream was formulated as an oil-in-water type cream preparation using breadfruit starch as a scrub. Physical evaluation of this preparation consisted of organoleptic, homogeneity, viscosity, pH, spreadability, adhesiveness, and room-temperature storage tests. The antioxidant activity was evaluated using the DPPH method. Results: The results of the physical evaluation test showed that the body scrub cream produced good results and complied with the requirements of cream products. Antioxidant activity test results show the IC₅₀ value of each formula is F1 (without extract) 107.8 µg/mL, F2 (1%) 72.48 µg/mL, F3 (3%) 56.54 µg/mL, F4 (5%) 43.40 µg/mL and F5 (vitamin C K+) 38.94 µg/mL. Conclusion: Based on these observations, the best formula is Formula 3 because the antioxidant test results are classified as strong, and the physical evaluation tests are considered stable.

Phytochemical Screening and Anti-hyperglycemic Effect Test of Ethanol Extract of Waru Leaf (Hibiscus tiliaceus) on Glucose-loaded Mice

2024-12-03T21:44:13+07:00

Background: The treatment of diabetes mellitus relies on synthetic drugs with various side effects. Therefore, it is necessary to explore alternative treatments with herbal therapies, such as Hibiscus tiliaceus leaves. Objectives: The aim of this study was to determine the anti-hyperglycemic effect of an ethanol extract from Hibiscus tiliaceus leaves in glucose-loaded mice. Methods: The initial stage of dried leaf characterization was to ensure the identity, quality, purity, and safety to be used, and then extracted using the maceration method with 70% ethanol solvent. The next step was phytochemical screening to identify secondary metabolite content. The anti-hyperglycemic effect was evaluated using the oral glucose tolerance test (OGTT) on 25 male mice divided into five treatment groups. The negative control group was given Na CMC 0.5% w/v Na CMC, and the positive control group was administered glibenclamide. The ethanol extract of Hibiscus tiliaceus leaves was administered at doses of 200, 400, and 800 mg/kg. Approximately 200 µL of blood was collected and analyzed for glucose levels. The data were statistically analyzed using one-way analysis of variance (ANOVA) with SPSS ver. 25 program. Results: Hibiscus tiliaceus leaves contain alkaloids, flavonoids, saponins, and tannins. The highest decrease in blood glucose levels was observed in the ethanol extract group at a dose of 400 mg/kg BW, with a decrease of 78.52%, followed by a dose of 200 mg/kg BW of 76.63%, a dose group of 800 mg/kg BW of 73.48%, and a positive control group (glibenclamide) of 34.68%, which was significantly different from the negative control group (Na CMC 0.5%) (p < 0.05). Conclusion: The ethanol extract of H. tiliaceus has anti-hyperglycemic effects.

An Effectiveness Test Combination of Ethanol Extracts of Buas-buas Leaves (Premna serratifolia L.) and Sappan Wood (Caesalpinia sappan L.) as Topical Antiinflammatory Agent in Male White Rats (Rattus novergicus)

2024-12-03T08:33:18+07:00

Background: Inflammation is the reaction of the immune system to tissue damage resulting from physical injury, harmful chemicals, or microbial agents. Steroid and non-steroid drugs are commonly used to treat inflammation, but long-term use can result in side effects, such as hormonal disorders and gastric ulcers. Buas-buas leaves and sappan wood has potential as traditional medicines, and based on empirical evidence, they utilize both plants as anti-inflammatory, antibacterial, antioxidant, antiallergic, and antiarthritic agents, as well as for the treatment of cardiovascular disorders, cough, and leprosy. Objective: This study aimed to evaluate the effect of combining 96% ethanol extracts from buas-buas leaves and sappan wood to deliver topical anti-inflammatory benefits. Methods: This research was experimental, using thirty male rats divided into six treatment groups: a negative control group with 2% carrageenan, Biocream® control group, a positive control group with Hydrocortisone Acetate, and three treatment groups receiving a combination of ethanol extracts from buas-buas leaves and sappan wood at concentrations of 1.67%, 2.5%, and 3.75%. The test compounds were administered after carrageenan injection. Measurement of skinfold thickness on the backs of the rats was conducted every hour for 6 h using digital calipers, and the difference in skinfold thickness of each rat, AUC value, and percentage of inflammation inhibition was calculated. Data analysis involved the Kolmogorov-Smirnov test and Levene's test to assess normality and homogeneity, respectively, and was subsequently followed by One-way ANOVA and a post-hoc test. Conclusion: The combination of ethanol extracts of Buas-Buas leaves and sappan wood can provide a topical anti-inflammatory effect, with the most effective concentration being 3.75% and an inflammation inhibition percentage of 32.77%.

Development of an Ocular Film Containing Ofloxacin in a Chitosan Matrix

2024-12-18T17:25:57+07:00

Background: Chitosan is a natural polymer that is widely used in pharmaceutical applications owing to its biodegradability and biocompatibility. High molecular weight chitosan, which is commonly found in the market (Sigma Aldrich), is acid soluble and thus limits its application for ocular purposes. Objective: This study aimed to improve the characteristics of high-MW chitosan ocular films by utilizing a water-soluble, low-MW chitosan modifier for the delivery of ofloxacin post-surgery. Methods: Various film formulas were prepared using high-MW chitosan as the main polymer matrix, glycerin and polyethylene glycol 400 as plasticizers, and low-MW chitosan as film modifiers. Glycerine was the best plasticizer that produced a good film appearance when added at an appropriate ratio, 8.33 times the weight of the high MW chitosan (TGc) and 6.25 times the weight of low- and high-MW chitosan blends at (1:1) ratio (MGb). The films were further developed as TGcs and MGbs were cross-linked using sodium tripolyphosphate to control the release of ofloxacin and improve its mechanical characteristics. Water absorption capability, mechanical characteristics, in vitro drug release, and antimicrobial activity were evaluated to determine the film formula. Results: The MGb formula showed the highest water absorption (approximately 230 %), while the lowest was shown by the TGcs formula (approximately 145 %). In contrast, the TGcs formula had the highest film elasticity (141.33±8.81%), and the MGb formula had the lowest (42.55±6.11%). Surprisingly, the best controlled release of ofloxacin for up to 24 h was produced by the MGbs film, which also showed the highest antimicrobial activity. MGbs also showed moderate film characteristics, which are suitable for ocular applications. Conclusion: The research concluded that The addition of water-soluble low-MW chitosan and a cross-linker agent can improve the controlled release and characteristics of chitosan-based ocular films.

Formulation and Evaluation of Transdermal Dissolving Microneedle Loaded with Ethanol Extract of Cocor Bebek Leaves (Kalanchoe pinnata)

2024-12-11T14:36:25+07:00

Background: Acne is a chronic skin inflammation caused by blockage of the sebaceous glands in the skin and hypercolonization of the acne-causing bacteria Propionibacterium acnes. Cocor bebek leaves (Kalanchoe pinnata) are known to contain various secondary metabolites, including flavonoids, with antibacterial activity. Objective: In an effort to prevent side effects from using oral and topical antibiotics to treat acne, an alternative acne treatment that is safer and more effective with a strong drug delivery system is needed: microneedle patch technology containing natural ingredients. Methods: A microneedle patch formulation of Cocor bebek leaf extract was developed using a combination of HPMC and PVP polymers. The evaluation of microneedle patches included irritation tests with rat test animals and antibacterial activity tests against Propionibacterium acnes. The results showed the formation of yellow microneedle patches with uniform needles. The evaluation results showed that the microneedle patch has an irritation index value classified as non-irritant and has antibacterial activity against Propionibacterium acnes, with the highest inhibitory diameter at an extract concentration of 30% with a moderate inhibition category. Conclusion: The microneedle patch cocor bebek leaf extract shows potential as an effective drug delivery system for the treatment of acne that is safe for use on the skin.

Formulation and Characterization of Analog Rice Using Arrowroot (Maranta arundinacea L.) and Hibiscus Flower (Hibiscus rosa sinensis L.)

2024-12-10T17:21:10+07:00

Background: Efforts to reduce high-carbohydrate consumption from rice include the development of analog rice from alternative sources such as arrowroot tubers (Maranta arundinacea L.). Proper formulation is crucial for producing analog rice with optimal quality, taste, and characteristics resembling conventional rice, while maintaining functional properties to meet carbohydrate and nutritional needs. Hibiscus (Hibiscus rosa-sinensis L.), which is rich in flavonoids, saponins, and anthocyanins, can enhance these formulations. Objective: The objective of this study was to evaluate the composition of a blend of arrowroot tubers (M. arundinacea L.) and hibiscus (H. rosa-sinensis L.) as a rice substitute. Methods: This study used 50 untrained panelists to conduct organoleptic tests on the shape, color, aroma, taste, and texture of rice and analog rice using five formulas (F1, F2, F3, F4, and F5). Furthermore, physical characteristics were tested, including the color index, 1000-grain weight, bulk density, and starch digestibility. Results: The characteristics test proved that all analog rice formulas had an average hedonic score in the range of 3.73-3.90; lower bulk Density than rice with a bulk density of 0.83 ± 0.02 g/mL; starch digestibility in the range of 0.62-0.67 g/mL; and has a yellow-red color range. Conclusion: The best and most preferred rice analog is Formula 5 (F5), with a composition of arrowroot tubers 57.8%, hibiscus 5.1%, mocaf 12.6%, GMS 0.6%, and water 23.9%.

Application of the Simplex Lattice Design Methode to Determine the Optimal Formula Nanoemulsion with Virgin Coconut Oil and Palm Oil

2025-01-12T11:26:58+07:00

Background: The success of nanoemulsion preparation is characterized by characteristics such as small droplet size, polydispersity index (PDI), and % transmittance, which are close to 100%. One of these factors is the type of oil component used. The Simplex Lattice Design (SLD) method can be used to determine the ratio of oil combinations to obtain an optimal nanoemulsion formula. Objective: The application of the Simplex Lattice Design (SLD) method can help researchers speed up the acquisition of optimal formulas without trial and error so that nanoemulsion formulas that meet specifications can be obtained. Methods: This research uses the Simplex Lattice Design (SLD) method with Design of Expert Version 13 software, with an upper limit value for oil (VCO and Palm Oil) of 2.66% and a lower limit value for oil (VCO and Palm Oil) of 0, which then The results of several formulas come out and characterization testing is carried out to get the best formula from the recommendations produced by the software. Results: The results of the Simplex Lattice Design (SLD) showed that oil affected the droplet size and PDI (p <0.05). Six optimal formulas were obtained, and after testing in the laboratory, there was no significant difference between the results of the SLD program and those of the laboratory (Sig. <0.05). Conclusion: This study shows that the Simplex Lattice Design (SLD) method is very effective.