scholarly journals Poly-herbal tablet formulation by design expert tool and in vitro anti-lipase activity

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Amruta Balekundri ◽  
Amit Shahapuri ◽  
Mrityunjaya Patil
Keyword(s):  
Side Effects ◽  
Lipase Activity ◽  
Herbal Medicines ◽  
Active Role ◽  
Stability Study ◽  
Obese Patients ◽  
Design Expert ◽  
Study Results ◽  
Treatment Of Obesity

Abstract Background Traditional medicine being ethnic is preferred worldwide even in these modern days. Obesity is a lifestyle disorder. Many chemically synthesized medicines are available. Poly-herbal medicines can be one of the safest alternatives with less side effects in treating obese patients. Results The in vitro anti-lipase activity was carried out for a different concentration. The formulation of the poly-herbal tablets was designed using the Design Expert software. The pre-compression and post-compression studies show that the formulation F6 showed better results of all the formulations designed. Stability study results showed that the poly-herbal tablets were stable throughout the studies. Conclusion The results show that F6 is the better formulation based on the tablet evaluation, and all the extracts showed inhibitory activity against pancreatic lipase indicating its active role in the treatment of obesity.

Novel Swellable/Expandable Gastroretentive Floating Films of Gliclazide Folded in Capsule Shell for the Effective Management of Diabetes Mellitus: Formulation Development, Optimization and In vitro Evaluation

2020 ◽  
Vol 15 ◽  
Author(s):  
Diksha Sharma ◽  
Deepak Sharma
Keyword(s):  
Diabetes Mellitus ◽  
Drug Absorption ◽  
Gastric Fluid ◽  
Stability Study ◽  
Gastric Retention ◽  
Effective Management ◽  
In Vitro Evaluation ◽  
Capsule Shell ◽  
Study Results

Background: Gliclazide (GLZ) belongs to the second-generation of sulphonylureas, is a drug of choice for the management of type II DM. It belongs to BCS Class II. The major site of drug absorption for GLZ is the stomach; it displayed variation in the drug absorption rate and bioavailability due to the shorter gastric retention time. Floating mechanism performance gets affected when the gastric fluid level not sufficiently higher, which ultimately obstructs the floating behavior, which is the major limitation of reported formulations. This limitation can get over by folded the film into the capsule shell that dissolved in gastric fluid and film swell/expands to dimensions higher than pylorus sphincter (12mm), thus prevents its evacuation. Objective: To explore the floating mechanism in the designing of films along with a tendency to expand by swelling and unfolding by utilizing a mixture of hydrophilic and hydrophobic polymer to achieve the controlled drug delivery and prolonged gastric retention of drug. Methods: The gastroretentive floating films were formulated by the solvent casting technique using 32 full factorial design and subjected to in vitro evaluation parameters, drug-excipient compatibility, X-ray diffraction and accelerated stability study. Results: The pre-formulation study established the purity and identification of drug. FTIR study confirmed no drug excipient interaction. F3, F6, and F9 were optimized based on in vitro floating characteristics, swelling/expanding ability, and unfolding time study. All developed formulations were unfolded within 14-22 min after capsule disintegration. The F3 was selected as final formulation as its ability to control the release of drug for 24 hrs followed by Zero-order kinetics having super case 2 transport. XRD confirmed the amorphousness of drug within formulation. The stability study results revealed that formulation was quite stable at extreme storage condition. Conclusion: The developed novel formulation has a good potential for the effective management and treatment of Diabetes Mellitus.

scholarly journals In Vitro Evaluation of Eslicarbazepine Delivery via Enteral Feeding Tubes

2017 ◽  
Vol 52 (11) ◽  
pp. 752-760 ◽  
Author(s):  
Kristin Reindel ◽  
Fang Zhao ◽  
Susan Hughes ◽  
Vivek S. Dave
Keyword(s):  
Enteral Feeding ◽  
Hplc Method ◽  
Stability Study ◽  
Eslicarbazepine Acetate ◽  
Particle Size Reduction ◽  
Feeding Tubes ◽  
Stability Indicating ◽  
Acceptable Range ◽  
Study Results

Purpose: The feasibility of preparing an eslicarbazepine acetate suspension using Aptiom tablets for administration via enteral feeding tubes was evaluated. Methods: Eslicarbazepine acetate suspension (40 mg/mL) was prepared using Aptiom tablets after optimizing the tablet crushing methods and the vehicle composition. A stability-indicating high-performance liquid chromatography (HPLC) method was developed to monitor the eslicarbazepine stability in the prepared suspension. Three enteric feeding tubes of various composition and dimensions were evaluated for the delivery of the suspensions. The suspension was evaluated for the physical and chemical stability for 48 hours. Results: The reproducibility and consistency of particle size reduction was found to be best with standard mortar/pestle. The viscosity analysis and physical stability studies showed that ORA-Plus:water (50:50 v/v) was optimal for suspending ability and flowability of suspension through the tubes. The developed HPLC method was found to be stability indicating and suitable for the assay of eslicarbazepine acetate in the prepared suspension. The eslicarbazepine concentrations in separately prepared suspensions were within acceptable range (±3%), indicating accuracy and reproducibility of the procedure. The eslicarbazepine concentrations in suspensions before and after delivery through the enteric feeding tubes were within acceptable range (±4%), indicating absence of any physical/chemical interactions of eslicarbazepine with the tubes and a successful delivery of eslicarbazepine dosage via enteric feeding tubes. The stability study results showed that eslicarbazepine concentration in the suspension remained unchanged when stored at room temperature for 48 hours. Conclusion: The study presents a convenient procedure for the preparation of a stable suspension of eslicarbazepine acetate (40 mg/mL) using Aptiom tablets, for administration via enteral feeding tubes.

scholarly journals Effect of dexfenfluramine on gastric emptying of a mixed solid-liquid meal in obese subjects

1990 ◽  
Vol 63 (3) ◽  
pp. 447-455 ◽  
Author(s):  
Michael Horowitz ◽  
Anne Maddox ◽  
Judith Wishart ◽  
Jane Vernon-Roberts ◽  
Barry Chatterton ◽  
...  
Keyword(s):  
Gastric Emptying ◽  
Side Effects ◽  
Obese Patients ◽  
Solid Meal ◽  
Liquid Meal ◽  
Placebo Capsule ◽  
Obese Subjects ◽  
Treatment Of Obesity ◽  
Solid Liquid ◽  
Double Isotope

Recent studies suggest that dexfenfluramine (D-fenfluramine), because of its pure serotonergic effect, may be a more potent anti-obesity agent, associated with fewer side-effects than the racemate DL-fenfluramine. The effect of dexfenfluramine on gastric emptying of a mixed solid and liquid meal was assessed with a double-isotope scintigraphic technique in eleven obese patients. Each subject took a placebo capsule on the morning and evening of the day before, and on the morning of the first gastric emptying measurement. Dexfenfluramine was then taken at a dose of 15 mg twice daily and gastric emptying measurements were performed at 5 and at 29 d after the initiation of active treatment. Dexfenfluramine significantly slowed gastric emptying of the solid meal at both 5 and 29d when compared with the placebo (P < 0.05) and also delayed emptying of solid food from the proximal stomach (P < 0.01), but no significant effect on liquid emptying was observed. No significant side-effects were reported and there was a marginal weight loss (P< 0.005) during treatment. We conclude that inhibition of gastric emptying may contribute to the efficacy of dexfenfluramine in the treatment of obesity.

scholarly journals DESIGN EXPERT SUPPORTED FORMULATION DEVELOPMENT, MATHEMATICAL OPTIMIZATION AND PREDICTABILITY STUDY OF FLOATING TABLETS OF BISOPROLOL FUMARATE

2021 ◽  
pp. 242-248
Author(s):  
SHAIKH SHAOOR AHMAD ◽  
SHAIKH SIRAJ N. ◽  
PATEL M. SIDDIK ◽  
KHALIFA MAHMADASIF YUNUS ◽  
MAKRANI SHAHARUKH I. ◽  
...  
Keyword(s):  
Drug Release ◽  
Scale Up ◽  
Mathematical Optimization ◽  
Lag Time ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Floating Tablets ◽  
Design Expert

Objective: Focus of the study was to formulate Design expert Software assisted floating tablet of Bisoprolol Fumarate. Bisoprolol Fumarate is a Beta adrenergic blocking agent, used to treat cardiac diseases favorable characters to be formulated as sustained release Gastro retentive floating tablets. Methods: Floating Tablets of Bisoprolol Fumarate were prepared by using polymers such as Polyox N 12 K and Carbapol 940 P. Formulations were prepared by using direct compression method and evaluated for various parameters like Hradness, thickness, weight variations, Floating lag time Total floating time,% drug release and Stability Study etc. Results: FTIR spectroscopic study indicates no drug-excipients interaction in the prepared formulations. Hardness or crushing strength of the tablets of all the formulation was found between 5.8 and 6.5 kg/cm2. Floating lag time of all batches is in range of 1.18±2.0 to 2.43±1.6 (minutes). All other parameters of all batches are within an acceptable range. The polymer Carbopol 940 P had the significant negative effect of on the floating lag times. The In vitro dissolution profiles of optimized A3 Floating formulation of Bisoprolol Fumarate were found to sustain drug release 99.25 % up to 12 h with floating lag time of 1.45 min; Designed formulation was stable after Stability study. Optimization study was carried out by using 32 factorial designs to fabricate formulations. Conclusion: It can be conclude that reproducible results of various parameters in this developed formulation can easily scale up. Furthermore designed formulation will be very effective for controlling blood pressure.

scholarly journals Herbal Medicine and Acupuncture for Breast Cancer Palliative Care and Adjuvant Therapy

2013 ◽  
Vol 2013 ◽  
pp. 1-17 ◽  
Author(s):  
Guo-Shiou Liao ◽  
Maria Karmella Apaya ◽  
Lie-Fen Shyur
Keyword(s):  
Breast Cancer ◽  
Palliative Care ◽  
Side Effects ◽  
Herbal Medicine ◽  
Symptom Control ◽  
Herbal Medicines ◽  
Breast Cancer Patients ◽  
Effective Treatment Option

Breast cancer is a life-threatening disease among women worldwide with annual rates of reported incidence and death increasing alarmingly. Chemotherapy is a recommended and effective treatment option for breast cancer; however, the narrow therapeutic indices and varied side effects of currently approved drugs present major hurdles in increasing its effectiveness. An increasing number of literature evidence indicate that complementary and alternative medicine (CAM) used in treatment-related symptom control and alleviation of side effects plays an important role in increasing survival rate and quality of life in breast cancer patients. This review focuses on the use of herbal medicines and acupuncture in palliative care and as adjuvants in the treatment of breast cancer. Herbal medicinal treatments, the correlation of clinical use with demonstratedin vitroandin vivomechanisms of action, and the use of certain acupoints in acupuncture are summarized. The aim of this review is to facilitate an understanding of the current practice and usefulness of herbal medicine and acupuncture as adjuvants in breast cancer therapy.

scholarly journals Development of Epirubicin-Loaded Biocompatible Polymer PLA–PEG–PLA Nanoparticles: Synthesis, Characterization, Stability, and In Vitro Anticancerous Assessment

Polymers ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1212
Author(s):  
Salam Massadeh ◽  
Iman Almohammed ◽  
Eman Barhoush ◽  
Mustafa Omer ◽  
Nouf Aldhawi ◽  
...  
Keyword(s):  
Side Effects ◽  
Double Emulsion ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Synthesis Process ◽  
Free Form ◽  
Scanning Calorimetry ◽  
Biocompatible Polymer ◽  
Mcf 7

Epirubicin (EPI) is an anti-cancerous chemotherapeutic drug that is an effective epimer of doxorubicin with less cardiotoxicity. Although EPI has fewer side effects than its analog, doxorubicin, this study aims to develop EPI nanoparticles as an improved formula of the conventional treatment of EPI in its free form. Methods: In this study, EPI-loaded polymeric nanoparticles (EPI-NPs) were prepared by the double emulsion method using a biocompatible poly (lactide) poly (ethylene glycol) poly(lactide) (PLA–PEG–PLA) polymer. The physicochemical properties of the EPI-NPs were determined by dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), entrapment efficiency and stability studies. The effect of EPI-NPs on cancer cells was determined by high throughput imaging and flow cytometry. Results: The synthesis process resulted in monodisperse EPI-NPs with a size of 166.93 ± 1.40 nm and an elevated encapsulation efficiency (EE) of 88.3%. In addition, TEM images revealed the spherical uniformness of EPI-NPs with no aggregation, while the cellular studies presented the effect of EPI-NPs on MCF-7 cells’ viability; after 96 h of treatment, the MCF-7 cells presented considerable apoptotic activity. The stability study showed that the EPI-NPs remained stable at room temperature at physiological pH for over 30 days. Conclusion: EPI-NPs were successfully encapsulated within a highly stable biocompatible polymer with minimal loss of the drug. The used polymer has low cytotoxicity and EPI-NPs induced apoptosis in estrogen-positive cell line, making them a promising, safe treatment for cancer with less adverse side effects.

FORMULATION AND EVALUATION OF THYROID HORMONE(T3) IMMEDIATE RELEASE TABLETS

2021 ◽  
Vol 1 (10) ◽  
pp. 383-388
Author(s):  
Farghana Begam ◽  
Rajalakshmi A. N ◽  
Padmapriya S
Keyword(s):  
Thyroid Hormone ◽  
Chemical Characterization ◽  
Immediate Release ◽  
Magnesium Stearate ◽  
Stability Study ◽  
Direct Compression ◽  
Maize Starch ◽  
Disintegration Time ◽  
Study Results

The study was aimed to formulate and evaluate Thyroid hormone (T3) immediate release tablets of a model Reference Listed Drug (RLD). The objective was to develop a cost effective immediate release tablet formulation and to optimize the formula in product development same that of the reference product. The ingredients used were API (thyroid hormone), lactose monohydrate (diluent), acacia (binder), maize starch (disintegrant), sodium chloride (alkalinizing agent) and magnesium stearate (lubricant). The concentration of maize starch and magnesium stearate were altered to reach the objective. Totally five formulations (F1 - F5) were prepared by direct compression method. The plan of work involved involved in the study was1 Selection of drug and excipients, 2Physico–chemical characterization and drug identification, 3Preformulation parameters of the drug, 4Pre–compression parameters for the tablet blend, 5Formulation and development of the tablet dosage form, 6Post compression parameters of the tablet and 7Stability study. The stability studies were performed as per ICH guidelines. Among all the formulations F5 was found to be the best as it showed better results than the other formulations. In vitro disintegration time and percentage drug release results shown satisfactory results. Stability study results showed no significant changes in the formulation. Keywords: Thyroid hormone (T3), Immediate release tablets, Direct compression, Dissolution.

The Mechanistic Approach to Tackle Obesity Using Traditional Herbal Plants

2021 ◽  
pp. 104-123
Author(s):  
Saniyah Saleem Khan
Keyword(s):  
Side Effects ◽  
Herbal Medicines ◽  
World Health ◽  
Mechanistic Approach ◽  
Life Threatening ◽  
Herbal Plants ◽  
Treatment Of Obesity ◽  
Health Organization ◽  
Surgical Treatments ◽  
Global Health Problem

Obesity is a medical metabolic condition where a person accumulates excess body fat that might affect their health. Obesity is a prevalent global health problem linked with other life-threatening chronic diseases like cardiovascular, certain types of cancer, diabetes, renal, cerebrovascular, bone, and muscle-related diseases. According to the World Health Organization (WHO), obesity is the fifth foremost cause of global deaths. Many allopathic drugs and surgical treatments for managing obesity are available in the market. However, these conventional methods have adverse side effects and chances of recurrence. For more than 2,000 years, herbal medicines have been used for the treatment of many diseases efficiently. This chapter addresses the current progress in the effectiveness of several herbal medications used for the treatment of obesity without causing side effects. The possible effects and mechanisms of using these herbaceous plants in the treatment of obese and overweight humans and animals are covered extensively.

scholarly journals FORMULATION OPTIMIZATION AND EVALUATION OF FLURBIPROFEN EMULGEL

2020 ◽  
pp. 49-54
Author(s):  
DIKSHA S. CHODANKAR ◽  
SACHI S. KUDCHADKAR ◽  
RAJASHREE S. GUDE ◽  
PRERANA D. NAVTI ◽  
SANAM M. SAWANT
Keyword(s):  
Side Effects ◽  
Drug Release ◽  
Stability Study ◽  
Water Soluble ◽  
Gelling Agent ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Dermal Delivery

Objective: The objective of the present study was to formulate flurbiprofen (FLB) emulgel, evaluation of the formulations and the selection of an optimized formulation through in vitro drug release and drug content studies. Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) requiring frequent administration and its chronic intake can lead to systemic side effects like gastric irritation and GI bleeding. The development of a dermal drug delivery system can overcome these side effects. Methods: The emulgel formulations were produced using different combinations of oil and emulsifying agents. Carbopol 940 was used as a gelling agent. The prepared emulgels were evaluated for general appearance, pH, spreadability, extrudability, drug content, in vitro drug release, average globule size and viscosity. Results: Optimized formulation F7 showed a better in vitro drug release compared to the marketed gel preparation. The stability study for the optimized formulation was carried out at 25 °C/60 % RH for 3 mo and the emulgel was found to be stable concerning the physical appearance, pH and drug content. Conclusion: The study revolved around the formulation of emulgel containing Flurbiprofen for dermal delivery of the drug. Emulgel was formulated with the purpose to enhance the permeation of poorly water-soluble drug FLB. The study concluded that the optimized emulgel containing FLB exhibited better in vitro drug release profile compared to the marketed formulation.

scholarly journals Pharmaceutical Characterization and In Vivo Evaluation of Orlistat Formulations Prepared by the Supercritical Melt-Adsorption Method Using Carbon Dioxide: Effects of Mesoporous Silica Type

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 333 ◽  
Author(s):  
Heejun Park ◽  
Kwang-Ho Cha ◽  
Seung Hyeon Hong ◽  
Sharif Md Abuzar ◽  
Seungyeol Lee ◽  
...  
Keyword(s):  
Carbon Dioxide ◽  
Particle Size ◽  
Side Effects ◽  
Mesoporous Silica ◽  
Dissolution Rate ◽  
Lipase Activity ◽  
Pore Volume ◽  
In Vivo Studies

Orlistat, an anti-obesity drug, has two critical issues—the first is its low efficacy due to low water solubility and the second is side effects such as oily spotting due to its lipase inhibition. The present study was designed to propose a solution using a formulation with mesoporous silica to simultaneously overcome two issues. Orlistat was loaded onto mesoporous silica by the supercritical melt-adsorption (SCMA) method, using carbon dioxide (CO2). Various types of mesoporous silica were used as adsorbents, and the effects of the pore volume, diameter and particle size of mesoporous silica on the pharmaceutical characteristics were evaluated by various solid-state characterization methods and in vitro and in vivo studies in relation to pharmacological efficacy and the improvement of side effects. The results showed that the pore volume and diameter determine loadable drug amount inside pores and crystallinity. The dissolution was significantly influenced by crystallinity, pore diameter and particle size, and the inhibition of lipase activity was in proportion to the dissolution rate. In vivo studies revealed that the serum triglyceride (TG) concentration was significantly decreased in the group administered amorphous orlistat-loaded Neuisilin®UFL2 with the highest in vitro dissolution rate and lipase activity inhibition in comparison to the commercial product. Furthermore, oily spotting tests in rats revealed that undigested oil was adsorbed onto mesoporous silica after orlistat was released in the gastro-intestinal tract, and it correlated with in vitro result that oil adsorption capacity was dependent on the surface area of empty mesoporous silica. Therefore, it was concluded that mesoporous silica type plays a major role in determining the pharmaceutical characteristics of orlistat formulation prepared using SCMA with CO2 for improving the low solubility and overcoming the side effects.

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