Semisolid Dosage Forms Research Articles

Moisturizing Cream

A cream is a preparation usually for application to the skin. Creams are defines as "a semisolid dosage form containing one or more drug substances dissolved or dispersed in a suitable base

Synthetic membrane selection for in vitro release testing (IVRT): A case study of topical mometasone furoate semi-solid dosage forms

In vitro release testing (IVRT) is extensively used to develop the formulation of topical semi-solid products, to evaluate the quality and consistency of the product after scale-up and post-approval changes, and more recently to aid the evaluation of topical generic products’ equivalency. The selection of synthetic membrane is one of the most critical parameters of the method development part of IVRT. It is well known that the membrane features namely its polymer matrices, porosity, pore size, thickness can have a substantial effect on the IVRT data. However, there is no detailed information available in the literature regarding the membrane selection for different types of topical dosage forms. Therefore, we aimed to investigate whether difference topical semi-solid dosage forms of the same drug molecule would cause to variation in the membrane selection. Within this framework, rheological behaviour of commercially available three different types of topical semi-solid dosage forms (ointment, cream, and lotion) of mometasone furoate (0.1%) were primarily characterized. Then, the membrane inertness test was conducted using a series of synthetic hydrophilic membranes (regenerated cellulose, cellulose acetate, cellulose nitrate, mixed cellulose ester membranes) and hydrophobic membranes (polyether sulfone, polypropylene, polytetrafluoroethylene membranes) after identifying of an appropriate receptor medium that ensures sink condition for mometasone furoate. Lastly, IVRT studies from the topical semi-solid products were performed utilizing Franz-type diffusion cells. The membrane inertness and in vitro release data demonstrated that the cellulose acetate membrane showed superior diffusion properties in general while the other synthetic membranes exhibited varying outcomes for different semi-solid dosage forms of mometasone furoate. Overall, the results indicated that the release rate and the cumulative drug released amount of drug after 6 h through the different synthetic membranes might vary depending on the semi-solid dosage form. In order to select the synthetic membrane for IVRT, it should also be considered potential interactions between the polymer matrices and the chemical structure of drug molecule as well as formulation components prior to conducting membrane inertness test and IVRT studies.

Dual Chemotherapeutic Loading in Oxalate Transferrin-Conjugated Polymersomes Incorporated into Chitosan Hydrogels for Site-Specific Targeting of Melanoma Cells.

In this work, we developed a smart drug delivery system composed of poly (ethylene glycol)-block-poly (ε-caprolactone) (PEG-PCL)-based polymersomes (Ps) loaded with doxorubicin (DOX) and vemurafenib (VEM). To enhance targeted delivery to malignant melanoma cells, these drug-loaded nanovesicles were conjugated to the oxalate transferrin variant (oxalate Tf) and incorporated into three-dimensional chitosan hydrogels. This innovative approach represents the first application of oxalate Tf for the precision delivery of drug-loaded polymersomes within a semi-solid dosage form based on chitosan hydrogels. These resulting semi-solids exhibited a sustained release profile for both encapsulated drugs. To evaluate their potency, we compared the cytotoxicity of native Tf-Ps with oxalate Tf-Ps. Notably, the oxalate Tf-Ps demonstrated a 3-fold decrease in cell viability against melanoma cells compared to normal cells and were 1.6-fold more potent than native Tf-Ps, indicating the greater potency of this nanoformulation. These findings suggest that dual-drug delivery using an oxalate-Tf-targeting ligand significantly enhances the drug delivery efficiency of Tf-conjugated nanovesicles and offers a promising strategy to overcome the challenge of multidrug resistance in melanoma therapy.

Physical Test of Avocado Leaf Extract Cream Formula

Avocado (Perseaamericana Mill) is a plant that grows widely in subtropical and tropical areas, one of which is Indonesia. The leaves of the avocado plant, which we can use as traditional medicine, are reported to be anti-bacterial and can inhibit the growth of several bacteria, including Staphylococcus aurus. The active substances contained in avocado leaves are flavonoids, quercetin and tannin which are useful as anti-bacterials and as a source of natural antioxidants. This study aims to determine the results of the physical test of the avocado leaf extract cream formula. This type of research is quantitative with a descriptive research design. In testing the cream, an organoleptic test, homogeneity test, pH test, spreadability test, absorption test and adhesion test were carried out. The results obtained in the organoleptic test were seen from the yellowish brown color, the semi-solid dosage form, and the distinctive creamy smell of avocado leaves, the homogeneity test of the cream did not occur in phase separation, namely the water phase and the oil phase, the pH test of the cream had a pH of 7, the power test Spread the cream with a diameter of 6.1 cm, the cream's absorption test can absorb water optimally, and the cream's adhesion test obtains an adhesion time of 1.48 seconds. The physical test of the avocado leaf extract cream formula meets the requirements.

Preparation and Evaluation of Cream Containing Betel Leaf Extract for Removal of Cutaneous Warts

Abstract: Warts are common skin growths caused by the human papillomavirus (HPV). They can appear on any part of the body but are most commonly found on the hands, feet, and genitals. Warts are usually harmless but can be unsightly or cause discomfort, especially if they are frequent friction or pressure. There are several types of warts, including common warts, plantar warts (on the soles of the feet), genital warts, and flat warts (often found on the face). Creams are semisolid dosage form containing one or more drugs substances dissolved or dispersed in a suitable base. They are emulsion of either W/O, O/W creams are uses for various purposes. Wart removal cream contains some synthetic substances as well as herbal ingredients like betel steam which is having antiviral activity against the human papilloma virus (HPV). Then calcium carbonate and sodium hydroxide slowly absorbed into the skin causing rupturing of the skin cells that contains the wart virus. To prepare wart removal cream sodium hydroxide and calcium carbonate along with the aqueous extract of betel leaf by maceration with the excipients such as stearic acid, glycerin, methyl paraben, distilled water are used. Finally, the cream is evaluated with various parameters such as physical and chemical properties like pH, viscosity, spreadability, texture. As this cream has clove oil which is used as an analgesic to avoid the irritational pain. The pH of the cream is supposed to be basic and around 12-12.5. During the evaluation the pH of the cream was found out to be 12.1. Cream was easily spreadable and it had a pleasant appearance.

Research Progress on Taxus Extraction and Formulation Preparation Technologies.

Taxus, as a globally prevalent evergreen tree, contains a wealth of bioactive components that play a crucial role in the pharmaceutical field. Taxus extracts, defined as a collection of one or more bioactive compounds extracted from the genus Taxus spp., have become a significant focus of modern cancer treatment research. This review article aims to delve into the scientific background of Taxus extracts and their considerable value in pharmaceutical research. It meticulously sifts through and compares various advanced extraction techniques such as supercritical extraction, ultrasound extraction, microwave-assisted extraction, solid-phase extraction, high-pressure pulsed electric field extraction, and enzymatic extraction, assessing each technology's advantages and limitations across dimensions such as extraction efficiency, extraction purity, economic cost, operational time, and environmental impact, with comprehensive analysis results presented in table form. In the area of drug formulation design, this paper systematically discusses the development strategies for solid, liquid, and semi-solid dosage forms based on the unique physicochemical properties of Taxus extracts, their intended medical uses, and specific release characteristics, delving deeply into the selection of excipients and the critical technical issues in the drug preparation process. Moreover, the article looks forward to the potential directions of Taxus extracts in future research and medical applications, emphasizing the urgency and importance of continuously optimizing extraction methods and formulation design to enhance treatment efficacy, reduce production costs, and decrease environmental burdens. It provides a comprehensive set of preparation techniques and formulation optimization schemes for researchers in cancer treatment and other medical fields, promoting the application and development of Taxus extracts in pharmaceutical sciences.

Development of a film-forming oleogel with increased substantivity for the treatment of psoriasis

The aim of this work was the development of a film-forming formulation (FFF) for the topical treatment of psoriasis that shows an increased substantivity compared to conventional semi-solid dosage forms. The developed formulation is an oleogel. It is based on a combination of castor oil and medium chain triglycerides, and the oil-soluble film former MP-30 (Croda GmbH, Nettetal, Germany), a polyamide that upon mixing with a polar oil entraps the oil und thus substantially increases the viscosity of the formulation up to a semisolid state. Betamethasone dipropionate (BDP) and calcipotriole (CA) were used as active pharmaceutical ingredients (APIs). Oleogels of different compositions were evaluated regarding substantivity, rheological properties, ex-vivo penetration into the skin and ex-vivo permeation through the skin. Marketed products were used as controls. It was found that the amount of betamethasone dipropionate penetrating and permeating into and through the skin from the film-forming formulation is at an intermediate value compared to the marketed products. The substantivity of the developed formulation is described by an amount of 57.7 % formulation that remains on the skin surface and is thus significantly higher compared to the marketed products. In the film forming formulation, the proportion of API penetrating the skin remains the same when the skin repetitively brought in contact with a piece of textile during the penetration experiment. In contrast with the in-market formulations tested, this proportion was reduced by up to 97 %. As a result, the developed formulations can lead to an increased patient compliance.

A Validated IVRT Method to Evaluate Semisolid Dosage Form Containing Ximenynic Acid Using a Novel Approach

Purpose: Ximenynic acid (XMA) holds significant potential in the market, especially due to its widespread application in the cosmetics sector. As its various biological activities continue to be discovered, there is a sharp rise in demand for ximenynic acid. A novel analytical approach has been devised for an in-house product, comparable to the reference listed drug (Softalia, containing 30% ximenynic acid), utilized in gel formulations. This method is designed to conduct in-vitro release studies employing Franz vertical diffusion cell apparatus and analytical quantification via high-performance liquid chromatography (HPLC). Methods: The methodology has been assessed concerning specificity, linearity, the limit of quantitation (LoQ), limit of detection (LoD), inter-day precision, intermediate precision, accuracy, and solution stability. Following method development, the reference product containing 30% ximenynic acid underwent testing against the in-house XMA semisolid dosage form to accurately demonstrate “equivalence”, with results aligning with the applicable acceptance criteria falling within the range of 75 to 133.33%, as outlined in the FDA’s SUPAC-SS guidance. The in-vitro release assay has proven valuable for quality assurance, batch comparison, and monitoring the impacts of different formulations, scales, scaling up/down, methods, locations, and other variables. Results: This research fabricates specific IVRT techniques for performing assessments of semisolid dosage forms, which are required for many regulatory purposes.

Analytical Method Development and Validation of Beclomethasone Dipropionate and Fusidic Acid in pure and Pharmaceutical Dosage Form (Cream) by RP-HPLC

A simple, rapid, specific, cheap, eco-friendly, and accurate RP-HPLC method for simultaneous estimation of Beclomethasone Dipropionate and Fusidic Acid in pure and combination drugs has been developed and validated. A stationary phase of BDS Hypersil C18 ((250mm x 4.6m, 5m) and a mobile phase of Acetonitrile: Methanol: Orthophosphoric acid (60:20:20v/v) were used for the separation. The flow rate was continued at 1.0 ml/min and the effluent was observed at 230nm. The designated situations were appropriate for separating Beclomethasone Dipropionate and Fusidic acid eluted with a mean retention time of 7.2 and 5.1 minutes, respectively. The planned technique was validated as per the International Council for Harmonisation recommendation. Its linearity, specificity, system suitability, accuracy and precision, limit of detection, limit of quantitation, and robustness are some of the parameters that have been validated. The concentration range produced linear calibration curves of 1-6g/ml and 2-12g/ml for Beclomethasone Dipropionate and Fusidic Acid with R2 = 0.9961 and 0.9963. Percent RSD values for both intraday and interday were determined to be less than 2.0%. Demonstrating the accuracy of the approach. The technique was proven to be reliable. A successful application of the developed RP-HPLC method for the quantification of Beclomethasone Dipropionate and Fusidic Acid in marketed semi-solid dosage form (Cream).

Accelerated Stability Study of Kailas Jeevan – A Proprietary Ayurvedic formulation

Background: Stability studies are the test to assess the shelf life of the Ayurvedic proprietary medicines. Govt. of India made mandatary test for licencing and renewal of licencing of the proprietary medicine. Accelerated stability studies, testing interval of 0,3 and 6 months. Kailas Jeevan is a proprietary semisolid dosage form prepared in GMP approved Ayurveda Sumshodanalaya (P) Pvt. Ltd. Dhayri, Pune. It is indicated in Constipation, Cracked heels, Wounds, Pimples, Burns etc.
 Aims and Objectives: To evaluate the shelf life of Kailas Jeevan through accelerated stability study. Materials and Methods: The formulation was prepared in the GMP approved pharmacy. Shelf life of product was evaluated by assessing in changes in physicochemical, Microbial and quantification profiles, after keeping it in stability chamber at specific temperature (40±2°C) and relative humidity (75±5%). Analysis was carried out at the intervals of 0, 1, 3, 6, 9,12, 18 and 24 months. Average 25% degradation time was calculated to find the shelf life as per the Ayurvedic Pharmacopoea of India, Part I Vol ix guidelines. Results and Conclusion: The parameters assessed in accelerated study of Kailas Jeevan, was shown under limits till 24 months. Based on multiplication factor shelf life of Kailas Jeevan is 7.02 year.
 Key Words: Stability, Shelf life, Kailas Jeevan, Accelerated stability study

Использование метода многоволновой спектрофотометрии при контроле качества тизоля геля и метронидазола в новой мягкой лекарственной форме «Метронидазоль»

Introduction. For the introduction of new medicines into medical practice, a mandatory stage is quality control, which includes determining the quantitative content of active components using modern methods of pharmaceutical analysis. Tizol gel, included in soft dosage forms, is an independent pharmacologically active agent, therefore it is important to evaluate its content in complex medicinal preparations. Aim. To develop a method for quantitative determination of tizol gel and metronidazole in a new semisolid dosage form «Metronidazole» using multiple-wavelength spectrophotometry. Materials and methods. Pharmaceutical substance metronidazole, tizol gel, «Metronidazole» ointment containing 5% nitroimidazole in a tizol base was used for analysis. The studies were performed on spectrophotometer SF-2000 by multiple-wavelength spectrophotometry in the UV region. On the basis of experimental data, the metrological parameters of the developed analytical technique were calculated. Results and discussion. Experimental studies allowed us to justify the use of an acetate buffer solution with pH = 4 as the optimum solvent for the spectrophotometric analysis of tisol gel and metronidazole in the mixture. Analytical wavelengths (238 nm for tisol gel, 316 nm for metronidazole) were selected according to the UV spectra of the drugs obtained. According to the results of quantitative determination of the components of the Metronidazole ointment, the content of medicines is within the limits: metronidazole from 0.4900 to 0.5219 g, tizol gel (in terms of the mass fraction of titanium) – 2.32–2.46%, which are acceptable according to regulatory documentation (FSF 42-3157-06, OFS.1.8.0001). Conclusion. Quantitative analysis of tisol gel in complex pharmaceutical preparations was proposed for the first time. The method of quantitative determination by multiple-wavelength spectrophotometry has been developed which allows to determine the content of tizol gel and metronidazole in a new semisolid dosage form «Metronidazole» with relative errors of the average result not exceeding ± 3.00%.

A review of in vitro release test for method development and validation of semisolid dosage forms

A review of in vitro release test for method development and validation of semisolid dosage forms

Ecofriendly analytical quality by design-based method for determining Metronidazole, Lidocaine and Miconazole using RP-HPLC in semisolid dosage form

The article deals with the development of an analytical method based on AQbD and GAC for the simultaneous determination of Metronidazole (MET), Lidocaine (LID) and Miconazole (MIC) in oval dosage form using RP-HPLC. The separation was achieved on the stationary phase Zorbax C18 150 mm × 4.6 mm (i.d); 5 μm, using a gradient mobile phase containing Ethanol and Phosphate buffers. The linearity has been obtained for MET's 240-390 μg/mL, 32-52 μg/mL for LID and 64-104 μg/mL for MIC, with their LOD and LOQ as 31.25, 94.705 μg/mL (MIC) 1.463, 4.433 μg/mL (LID) and 7.981, 24.187 μg/mL for MIC, respectively. Finally, the method assessed for greenness using the three tools showed that the developed method was eco-friendly. The developed method is simple and reliable with a design space that helps for further improvement and is eco-friendly, making this method unique for adoption in regular quality control analysis.

Review–Formulation Development of Semi-Solid Dosage Form

Semi-solid dosage forms are generally found in medicines for all types of patients. Though, they have specific advantages, along with fast efficacy due to the devoid of dissolution time and quick absorption in the skin surface. Semi-solid formulations have been broadly used in pharmacy due to their high dosing adjustability, easy use off, and rapid onset of action. Keywords: Semi-solid dosage forms, Gels, Ointment, Cream

Application of Starch, Cellulose, and Their Derivatives in the Development of Microparticle Drug-Delivery Systems.

Micro- and nanotechnologies have been intensively studied in recent years as novel platforms for targeting and controlling the delivery of various pharmaceutical substances. Microparticulate drug delivery systems for oral, parenteral, or topical administration are multiple unit formulations, considered as powerful therapeutic tools for the treatment of various diseases, providing sustained drug release, enhanced drug stability, and precise dosing and directing the active substance to specific sites in the organism. The properties of these pharmaceutical formulations are highly dependent on the characteristics of the polymers used as drug carriers for their preparation. Starch and cellulose are among the most preferred biomaterials for biomedical applications due to their biocompatibility, biodegradability, and lack of toxicity. These polysaccharides and their derivatives, like dextrins (maltodextrin, cyclodextrins), ethylcellulose, methylcellulose, hydroxypropyl methylcellulose, carboxy methylcellulose, etc., have been widely used in pharmaceutical technology as excipients for the preparation of solid, semi-solid, and liquid dosage forms. Due to their accessibility and relatively easy particle-forming properties, starch and cellulose are promising materials for designing drug-loaded microparticles for various therapeutic applications. This study aims to summarize some of the basic characteristics of starch and cellulose derivatives related to their potential utilization as microparticulate drug carriers in the pharmaceutical field.

Lip Cream Formulation from Miana Leaf Extract (Coleus scutellarioides L.) As A Natural Dye


 
 
 
 Abstrack
 The miana leaves (Coleus scutellarioides L.) contain flavonoids that can provide specific dyes. The purpose of the study was to formulate miana leaf extract in lip cream preparations as natural dyes. The use of natural lip cream dyes is a solution to overcome the problem of synthetic lip cream dyes. One of the plants such as the miana leaves contains secondary metabolites, one of which is flavonoids which can provide dyes. The natural colors found in miana leaves can be used as natural dyes in cosmetics. The purpose of the study was to determine at what concentration the miana leaves produced the most optimal physical quality of color in the preparation of lip cream. The method of the research includes the manufacture of ethanol extract of miana leaves (Coleus scutellarioides L.) by maceration for 5 days with 96% ethanol solvent and followed by remeseration with the same solvent. The extract formulas used were 5%, 10%, and 15%. The evaluations included organoleptic, homogeneity test, physical test, pH test, irritation test and color preference test. The results of the lip cream preparation, the results of the organoleptic examination were declared to have a semi-solid dosage form, a distinctive odor and varied colors F1, cream color, F2 salmon red, F3 brick red, homogeneity examination results were declared homogeneous, the results of observation of the preparation did not state that there was no change on the shape, color and odor of the preparation, the average pH test results were 4.1, the test results were declared non-irritating, the result of the color preference of the three formulas that the panelists preferred was a concentration of 15% because the color was clear and very soft. Miana leaf ethanol extract can be made as a colorant in lip cream preparations.
 
 
 
 
 

Formulation and Evaluation of Herbal Facewash Preventing Dermatological Problem

Abstract: Facewash is one type of cosmeceuticals as well as semisolid dosage forms used for external purposes. It is applied on the skin surface to protect the skin from various microbial attacks. This type of cosmeceutical is also used to clean different types of skin problems like skin acne, skin pimples, skin rashes, dark circles, black spot, oily skin, skin discolored, etc. In this study, we have formulated one herbal face wash containing different extraction of herbal materials like fresh aloevera gel, leaves of neem, turmeric, lemon juice, Fresh leaves of Tulsi, fresh pudina leaves, Chandan, liquorice, Honey, Coffee, Multani mati, rose water as well as various types of excipients like sodium CMC, sodium lauryl sulphate, sodium benzoate, glycerol and distilled water. After formulation study we focused the evaluation cum validation of the formulated new herbal facewash like testing of pH ,Spreadability test, foam forming test, etc.

Block Copolymers of Ethylene Oxide and Propylene Oxide: Prospects for Medical and Pharmaceutical Application in Russia

Block copolymers of ethylene oxide and propylene oxide (EO/PO block copolymers) are polymeric non-ionic surfactants with a high hydrophilic–lipophilic balance also referred to as pluronics, poloxamers, or proxanols. These compounds are among the most demanded modern excipients for the production of medicines. EO/PO block copolymers are used both in the production of traditional (liquid, semi-solid, and solid) dosage forms and as part of targeted delivery systems. The extensive application of EO/PO block copolymers is due to the diverse array of their properties, including not only solubilising, emulsifying, gelling, and other effects but also thermoreversibility, which is essential for developing in situ delivery systems and 3D printing technologies.The aim of the study was to evaluate the potential of EO/PO block copolymers for medicinal use and to assess the range of medicinal products approved in the Russian Federation that contain EO/PO block copolymers.This review presents an analysis of the register of poloxamer-containing medicines approved in the Russian Federation, a list of the largest manufacturers of EO/PO block copolymers in the world, and a study of the possibility to use copolymers for medical purposes. Currently, there are more than 10 chemical manufacturers producing EO/PO block copolymers for the pharmaceutical, biotechnology, and other industries around the world. EO/PO block copolymers are included in more than 60 medicinal products present in the Russian pharmaceutical market; this observation indicates the need to phase out the import of poloxamers.

Rational Design of Topical Semi-Solid Dosage Forms-How Far Are We?

Specific aspects of semi-solid dosage forms for topical application include the nature of the barrier to be overcome, aspects of susceptibility to physical and chemical instability, and a greater influence of sensory perception. Advances in understanding the driving forces of skin penetration as well as the design principles and inner structure of formulations, provide a good basis for the more rational design of such dosage forms, which still often follow more traditional design approaches. This review analyses the opportunities and constraints of rational formulation design approaches in the industrial development of new topical drugs. As the selection of drug candidates with favorable physicochemical properties increases the speed and probability of success, models for drug selection based on theoretical and experimental approaches are discussed. This paper reviews how progress in the scientific understanding of mechanisms and vehicle-influence of skin penetration can be used for rational formulation design. The characterization of semi-solid formulations is discussed with a special focus on modern rheological approaches and analytical methods for investigating and optimizing the chemical stability of active ingredients in consideration of applicable guidelines. In conclusion, the combination of a good understanding of scientific principles combined with early consideration of regulatory requirements for product quality are enablers for the successful development of innovative and robust semi-solid formulations for topical application.

Application of Quality by Design Approach in the Optimization and Development of the UPLC Analytical Method for Determination of Fusidic Acid in Pharmaceutical Products

Background: Analytical techniques are a crucial method used in quality control procedures. Fusidic acid (FU), an antibacterial drug, is available on the market in a semisolid dosage form. This work aimed to develop a simple, sensitive, and robust UPLC assay for FU. Method: The effect of the formic acid concentration (X1 (1%, 0.55%, and 0.1%)), and column temperature (X2 (40, 32.5, and 25 °C)) on the retention time, peak area, and peak height were determined. Results: The results show that a long retention time of 1.18 min can be achieved with a low column temperature and a low to medium concentration of formic acid. A good peak height resolution was obtained with a low concentration of formic acid at different temperature settings. The optimized condition was suggested by the software program to analyze the drug in a mobile phase, consisting of 72% acetonitrile and 28% water containing 0.1% formic acid with a column temperature adjusted to 40 °C. Conclusion: The method was validated in terms of linearity, accuracy, precision, and robustness. In addition, the stability degradation study determined that the method can separate the drug from other degradation production. The method was applicable to determine the drug content in the marketed product.