Semisolid Preparations Research Articles

A RECENT OVERVIEW OF LOCALLY ADMINISTERED TOPICAL OTIC DOSAGE FORMS

Ear diseases can significantly affect the life quality of patient, so the need for effective treatment encourages the development of new active substances and new dosage forms. Otic dosage forms may be solutions, suspensions, or emulsions of drops or spray for washing the ear or for administration to the ear canal. They may be ear-wash preparations in the form of solution or emulsion, or medicated semi-solid or solid preparations in the form of gel, cream, ointment, powders, sticks or buffers. These preparations can contain one or much more active ingredients in a suitable vehicle and additionally may contain different excipients for isotonisation, pH adjustment, viscosity or solubility enhancement, buffering, preservation, etc. These excipients should not alter the pharmacological effect of active substances and should not be toxic or irritating. Ear preparations can be packaged in single or multiple doses. It is anticipated that otic dosage forms will be improved and the importance of locally applied, safe and highly controlled drug delivery systems will increase in the future.

Measurement of the Water Content in Semi-solid Formulations Used to Treat Pressure Ulcers and Evaluation of Their Water Absorption Characteristics.

We investigated the water contents in commercial semi-solid preparations used for pressure ulcer (PU) treatment using near-IR spectroscopy (NIRS) and compared the results with those measured using the Karl Fischer (KF) method. The aim of this study was to determine a standard method and select the appropriate topical preparation with the optimal moisture for PU treatment. The water absorption properties of bases and formulations were evaluated with a time-dependent factor using Transwell as the model membrane. KF and NIRS were applicable as measurement methods of the water content in semi-solid formulations. NIRS was shown to be a useful, simple, nondestructive tool that is more advantageous than the KF method. The water absorption characteristics tested using Transwell revealed that the rate of and capacity for water absorption are determined not only by the absorption ability of the polymer base but also by other factors, such as the osmotic pressure exerted by additives. KF and NIR measurements can be used to choose external skin preparations to control the amount of water in PU treatment.

Microstructure and Simulation of Semisolid Aluminum Alloy Castings in the Process of Stirring Integrated Transfer-Heat (SIT) with Water Cooling

The continuing quest for aluminum castings with fewer defects has aroused the interest in rheological high-pressure die casting (RHPDC). A new machine, stirring integrated transfer-heat (SIT) device, based on the mechanical stirring and enhanced cooling for semisolid slurry preparation was proposed to produce the thin-walled communication shell part by RHPDC process. The influence of SIT process characteristics on the microstructure was studied. The microstructure of SIT-RHPDC shell part in different locations was investigated. Combined with simulation, the flow characteristics and the temperature field change in the melt under the stirring-only process and different stirring with internal water-cooling conditions were studied to get a better understanding of the nucleation, grain growth and solidification behavior. Under the dual action of agitation and heat dissipation in SIT device, the fluid convection has changed the temperature field of the melt significantly. The temperature field of the melt becomes relatively uniform from a great temperature gradient and the continuous cooling rate is increased to 5 °C/s. In the same time, the slurry has a greater supercooling degree, and flows more evenly in the filling process. The experimental results indicate that compared with microstructure of an HPDC component, the microstructure at different locations of SIT-RHPDC part is composed of refined rosiness and nearly spherical particles.

Avleha kalpna - A review

In Ayurveda Rasashastra and Bhaishajya Kalpna branch is more important. It deals with the preparation of medicine by using herbal, metal and animal origin substances. Herbal medicines are frequently used in Indian system of medicine since long time without any known side effect. Avaleha kalpana is a semi solid preparation of drugs, prepared with addition of jaggery, sugar or sugar candy and boiled with prescribed drug juice or decoction it is called as Avaleha. While preparing Avaleha Madhur dravya’s like Guda or Sharkara and honey are added to the juice or the Decoction. This article will review the concept of avaleha kalpana in the classics.

A Review on Topical Gels as Drug Delivery System

The clinical evidence indicates that topical gel is a safe and most effective treatment option for use in the management of skin related disease and used for local action to reduce the side effects associated with other conventional dosage form. Topical drug delivery systems include a large variety of pharmaceutical dosage form like semisolids, liquid preparation, sprays and solid powders. Most widely used semisolid preparation for topical drug delivery includes gels, creams and ointments. A gel is a cross-linked polymer network swollen in a liquid medium. Its properties depend strongly on the interaction between solid state polymer and the liquid component. Gels exhibit no steady-state flow. The interaction between polymer and the liquid dispersion medium form an interlacing three dimensional network of particles of dispersed phase. The increased viscosity caused by interlacing and consequential internal friction is responsible for the semisolid state. Topical gel formulation provides a suitable delivery system for drugs because they are less greasy and can be easily removed from the skin. Gel formulation provides better application property and stability in comparison to cream and ointments. Keywords: Topical, drug delivery, gels, review, skin. Percutaneous penetration, drug delivery, organogels, Hydrogel.

Formulation and evaluation of semisolid dosage forms of an anti-inflammatory drug.

Curcumin is one of the commonly used dietary supplements with wide pharmacological activities but the main hindrance in the commercial exploitation of curcumin is the issue with its solubility and stability. Hence, the aim of the present study was to formulate curcumin silver nanoparticles (CSNP) by chemical reduction method and to evaluate its solubility, stability as well as diffusion properties. The CSNP was combined with potent anti-inflammatory drug Diclofenac sodium (DS) to prepare gels (F1-F7), cream (F8) and ointment (F9). The DS-CSNP was subjected to in vitro and in vivo anti-inflammatory activity by albumin denaturation method and carrageenan-induced paw oedema method using albino rats, respectively. Results of the present study revealed that CSNP possess good solution stability in different pH solutions compared to pure curcumin, and the particle size as well as zeta potential were found to be 115nm and -5.69mV, respectively for CSNP. Based on the results of in vitro release study and in vitro anti-inflammatory activity, formulation F4, F5, F9 and marketed product were subjected for in vivo anti-inflammatory activity. Among the three formulations, formulation F9 showed the maximum inhibition of the oedema (82.25%) at the end of 90min followed by F5 and F4. In addition, formulations F4, F5, and F9 exhibited better in vivo anti-inflammatory activity in comparison with the marketed product which might be due to synergistic effect of the combination of curcumin silver nanoparticles and DS. In conclusion, CSNP-incorporated DS semisolid preparations were stable and can yield promising anti-inflammatory activity compared to marketed formulation; hence, these formulation can be exploited commercially in the preparation of anti-inflammatory dosage forms.

Sodium reduction in butter using microparticulated salt

PurposeExcessive sodium intake is associated with several diseases. Accordingly, several measures, including microparticulate salt, have been adopted to reduce the salt contents of food products. However, no studies have reported the effectiveness of microparticulate salt in semisolid and liquid products. Accordingly, the purpose of this paper is to evaluate the application of microparticulate salt to reduce sodium contents in semisolid products.Design/methodology/approachThe optimal salt content to be added in butter was defined by the just-about-right-scale test. Butter samples were prepared using microparticulate salt to achieve 25, 50 and 75 per cent reductions in conventional salt concentrations. Multiple comparison tests were performed to evaluate sample taste.FindingsThe ideal concentration of conventional salt to be added to butter was 2.16 per cent. Discriminative tests showed that samples with 25 and 75 per cent salt reduction showed significant differences (p ⩽ 0.05) compared with butter prepared at the ideal salt content, whereas the sample with 50 per cent salt reduction had no significant difference (p > 0.05). Thus, microparticulate salt showed higher salting power than conventional salt. These results indicated the effectiveness of microparticulate salt in the preparation of semisolid products with sodium reduction.Research limitations/implicationsMore detailed studies about the reduced-sodium butter shelf life are necessary to verify the microparticulate salt application in the product preparation. Moreover, microparticulate salt application in semisolid and liquid products elaboration must be more investigated to better elucidate its practicability of reducing sodium content in these kinds of products. Therefore, researchers are encouraged to test the proposed propositions further.Practical implicationsMicroparticulate salt has been successfully applied to reduce sodium in solid products, being added to the finished product surface. However, there are no studies that report its effectiveness in semisolid and liquid products, such as the butter, in which the salt is added during the product preparation. Thus, this research provides new scientific information to the food industry and research fields, to expand the knowledge of reduced-sodium products development using microparticulate salt with sensory quality.Originality/valueNo studies have evaluated the application of microparticulate salt for semisolid product preparation. Therefore, the findings will support the development of healthy products.

DEVELOPMENT OF SEMISOLID PREPARATIONS CONTAINING EXTRACT OF THAI POLYHERBAL RECIPE FOR ANTI-INFLAMMATORY EFFECT

Objective: The objective was to develop the semisolid preparations containing extract of Thai polyherbal recipe with anti-inflammatory effect.
 Methods: Polyherbal ethanolic extract was prepared by maceration and determined for phytochemicals and antioxidant activity. Effects of extract on the production of pro-inflammatory mediator-nitric oxide (NO)-were examined in RAW 264.7 cells. Semisolid preparations, balm, and gel, were prepared and evaluated. In vitro release profiles and mechanisms of phenolic compounds, phytochemical markers, from the preparations were investigated.
 Results: Polyherbal ethanolic extract was dark yellow-green, viscous liquid with the yields of 8.2%. Total phenolic and total flavonoid contents were 121.21±1.60 mg GAE/g and 26.55±1.38 mg QE/g, respectively. Antioxidant assay showed that polyherbal extract can scavenge the radical to a certain extent, with DPPH IC50 of 160.75±3.43 µg/ml and FRAP values of 91.94±4.17 mg FeSO4/g. In vitro anti-inflammatory test revealed that the extract inhibited NO production in a dose-dependent manner, with IC50 of 145.65±3.26 µg/ml. The yellowish-green color, homogenous and suitable for skin application polyherbal balm and gel was obtained. The higher release of phenolics from the gel was observed, with the cumulative release at 8 h of 119.0±4.3 mg GAE, whereas that from the balm was only 39.7±2.0 mg GAE. The phenolic release profile was found to be best fitted with the Higuchi model.
 Conclusion: The semisolid preparations containing Thai polyherbal recipe extract with anti-inflammatory effect were successfully prepared. The proper semisolid base and compositions are crucial for effective skin delivery as they influence the release rates of phytochemical markers.

Preparation and Evaluation of Hair Conditioner Using Mucus of Hibiscus Leaves (Hibiscus rosa-sinensis L.)

Many ornamental plant growing in tropical and subtropical regions one is Hibiscus which is a native plant from East Asia. Conditioner is one of semi solid preparation used to hair after using shampoo. The porpose of the research is getting formulation hair conditioner from Hibiscus with various concentration. This research is a descriptive analytic in the laboratory. Conditioner making with mix oil phase and melted water. The indrediens to be use are dimethicone, sethyl alcohol, stearic acid, TEA, glycerin, methyl paraben, propyl paraben and aquadest. Physical stability tests carried out were organoleptic test, homogeneity test, pH test and cream type test with various concentrations of hibiscus leaf mucus which were 15%, 20%, 25% and 30%, and as a comparison were the formulations of conditioner preparations without using hibiscus mucus . The results showed that the manufacture of conditioner with variations in the concentration of mucilage of hibiscus leaves (Hibiscus rosa-sinensis L.) and physical stability testing on formula 4 shows stable and softer textured results. The conclusion obtained is that formulas 1, 2, 3 and 4 have met the requirements of semi-solid preparations.

Study of the stability of organoleptic and structural-mechanical indicators of semi-solid preparations with metal nanoparticles

Aim. Research of the stability of organoleptic and rheological properties of semi-solid preparations with silver and gold nanoparticles.Methods. For the study of organoleptic parameters, a classic method for determining the stability with periodic control of dosage forms in two temperature regimens was used: 8-15 °C (cool place) and 15-25 °C (room temperature). To study the rheological characteristics of semi-solid preparations, a rotary viscometer with a system of coaxial cylinders was used.Results. We studied three medicinal forms based on silver nanoparticles - ointment, cream and gel, which can be promising for the use in dermatology, as well as two dosage forms based on nanoparticles of silver and gold for the use in dentistry and surgery for the treatment of infectious, purulent-inflammatory diseases of skin and mucous membranes of the oral cavity. Within 24 month of storage of dosage forms in a dark place in dark glass containers every 6 months the following parameters: homogeneity, odour, colour and pH were monitored. Rheological parameters were investigated after the preparation of dosage forms and after 24 months of storage. According to the rheological indicators rheograms of stream semi-solid preparations were constructed, and also indicators of mechanical stability were calculated. It was found that all samples are coagulation systems with a pseudoplastic flow type. The obtained rheograms contain loops of hysteresis, which characterize their certain degree of thixotropy.Conclusion. According to the results of studies the stability of organoleptic characteristics of semi-solid preparations at a storage temperature 8-15 0С in a place protected from light is established. According to the rheological properties, samples of studied semi-solid preparations have a good ability to apply on the skin and extrusion from tubes.

LABORATORY EQUIPMENT DURING PHARMACEUTICAL DEVELOPMENT OF SEMI-SOLID PREPARATIONS

Introduction. When developing drugs it is necessary to use laboratory equipment that simulates pilot and industrial equipment. For the production of semi-solid preparations the key equipment are rotor-stator dispersers and vacuum reactors-homogenizers. Aim. Investigation of the functional characteristics of laboratory equipment: Megatron® MT 1-50 dispersant SHS F/2 (Kinematica AG, Switzerland) and the RP-5 vacuum homogenizer reactor (Promvit, Ukraine). Materials and methods. During development a generic product Penciclovir cream 1% the initial particle size in suspension of penciclovir and particle size after grinding were studied by optical microscopy and laser diffraction methods. In a cream made in the reactor, the particle size of the dispersed phase of the o/w emulsion and suspension, as well as the absence of air bubbles, were determined by optical microscopy. The assay of penciclovir in 9 samples of the cream taken from the reactor-homogenizer was performed by liquid chromatography. By the of rotational viscometry method the rheological properties of the cream were studied. By the inductively coupled plasma atomic emission spectroscopy the getting of metal impurities from the disperser and the reactor-homogenizer into the suspension and cream were investigated. Results and discussion. With an increase in the rotor speed, the particle size of penciclovir in suspension decreases. The disperser effectively performs its function at a rotor speed of 25,000 rpm. In a cream made in the reactor, the deviations in the quantitative content of penciclovir from the average value in each sample are within the uncertainty of the analytical procedure, which indicates its uniform distribution. The reactor provides effective dispersion and uniform distribution of the oil phase, prevents the formation of a gas emulsion and allows getting a cream that, according to its rheological properties, corresponds to the reference preparation Fenistil® Pencivir cream 1%. In the production process metal impurities were not emitted into the suspension and the cream from the equipment. Conclusion. The disperser and the reactor during the production of cream with penciclovir are suitable for their intended use. It is rational to combine these two types of equipment at the sites for the production of semi-solid preparations. The disperser can also be used to produce emulsions with a very small particle size of the dispersed phase.

Development of oral foams for topical treatment of inflammatory bowel disease

The advantages of local therapy for the treatment of inflammatory bowel disease (IBD) are generally accepted. However, the effectiveness of such treatment is often limited due to insufficient targeting of the inflammatory lesions using classical modified release (MR) formulations. The exisiting MR products cannot always provide the therapeutically required high concentrations of the active pharmaceutical ingredient (API) at the inflammation site. This might be overcome by administration of semisolid preparations such as drug solutions or liquid foams. Foams can be used as suitable vehicles containing concentrated solutions of the API which can be easily spread and effectively cover the site of the inflammation. In the present work presented are foams that are suitable for oral administration as a solid dosage form. The novel systems are characterized by dynamic foaming, good smoothness and spreading capacity as well as reasonable stability under simulated intestinal conditions. The study results suggest that the orally applicable foams can be considered as an alternative medicine suitable for the topical treatment of IBD.

Avaleha Kalpana - A Review Dr. Abstract Key words:

In Ayurveda, Rasashastra and Bhaishajya Kalpana branch is more important. It deals with the preparation of medicine by using herbal, metal and animal origin substances. Herbal medicines are frequently used in Indian system of medicine since long time without any known side effect. Avaleha Kalpana is a semi solid preparation of drugs, prepared with addition of jaggery, sugar or sugar candy and boiled with prescribed drug juice or decoction it is called as Avaleha. While preparing Avaleha Madhura Dravya’s like Guda or Sharkara and honey are added to the juice or the decoction. This article will review the concept of Avaleha Kalpana in the classics.

Damaging of Ultrasonic Horn for Semisolid Feedstock Production

Ultrasound treatment is one of the known method to obtain the globular microstructure for semisolid processing of aluminum alloys. Notwithstanding the numerous advantages, the main industrial limit of this method is the low service life of the horn due to the combined hot corrosion and erosion phenomena. Various approaches are reported in literature to overcome this problem, but a real satisfactory option does not seem to be available yet. In this paper, the behavior of a H11 tool steel sonotrode coated with a thin layer of TiAlCN is investigated and compared with the performance of an uncoated steel one. The lifetime of the horn was evaluated in terms of effectiveness in semisolid feedstock material preparation. For this purpose, the microstructure of semisolid cast samples obtained after different working times was analyses by optical and scanning electron microscopy. Moreover, melt contaminations due to the probe dissolution were also evaluated. The applied coating exhibited a significant resistance to separate hot corrosion in liquid Al alloy and cavitation erosion phenomena in water. However, the combined effect of the two damaging mechanisms during ultrasound treatment of the molten alloy leaded to coating removal and to a horn consumption comparable to that of bare steel.

Pharmacognostical, physicochemical and microbiological standardisation of Tiryaq-e-arba (An Unani Polyherbal Formulation)

Background: Tiryaq-e-Arba is a famous semi-solid compound preparation of Unani medicine and useful in various medical conditions. Before this study, Standardization of this formulation has not been carried out. Aims: The present study was undertaken to standardise the Tiryaq-e-Arba. Material & Methods: Standardisation performed from the organoleptic evaluation, physico-chemical studies, estimation for organic and inorganic constituents, heavy metal toxicity, microbiological evaluation. Results & Discussion: Tiryaq-e-Arba was evaluated for organoleptic evaluation and found in confirmity. Physico-chemical parameters were evaluated on three samples and mean was determined. Bulk density, specific gravity, pH of 1% and 10% solution, moisture content, alcohol and water-soluble content were determined. Percentage of total ash, acid insoluble ash, water soluble ash were determined. Estimation for organic constituents viz. alkaloid, reducing sugars, phenols, volatile oils were done. In inorganic constituents, calcium, iron, copper were evaluated and the values were recorded. Heavy metal estimation revealed lead content but within limit set by WHO, while mercury, arsenic, cadmium were absent. Total bacterial count and total fungal count also within limits and absence of specific pathogens. Results were within limits set by WHO. Conclusions: By this study, we have developed standards for various parameters which can be used for reference for future studies. It provides information and controls, necessary to produce material of reasonable consistency. This study is not only helpful for the researchers, analysts, scientists but also strengthen the Unani System of Medicine.

Evaluation of the Physical Stability of Nanostructured Lipid Carrier (NLC) Meloxicam Before and After Strorage 40 Days

Objective: The aims this study was to determine the effect of lipid ratio Monostearin and Miglyol 808 roomates gives the physical stability after storage 40 days. Methods: The NLC making was done by using emulsification method in the formation of NLC meloxicam, 3 different lipid ratios were used, including ratios of 6: 4, 7: 3, 8: 2. Results: NLC meloxicam physical stability of the pH, viscosity, particle size, particle morphology and entrapment efficiency. NLC meloxicam belongs to semisolid preparations with pH value range of 5.72-5.87. Increasing viscosity of NLC system is caused by the increase of solid lipid. The measurement results of particle size of three different lipid formulas indicated that the lipid particle size was less than 1000 nm. Entrapment efficiency test of all NLC-lipid compositions revealed quite high result (> 80%). Conclusion: The system uses lipid monostearin NLC meloxicam and Miglyol 808 at a ratio of 8: 2 is the most optimal combination shows physical stability after storage 40 days.

Ketoconazole-conjugated ZnO nanoparticles based semi-solid formulation and study their impacts on skin disease.

In this study, the ketoconazole-conjugated zinc oxide (ZnO) nanoparticles were prepared in a single-step approach using dextrose as an intermediate compound. The physical parameters confirmed the drug conjugation with ZnO and their size was around 70-75 nm. The drug loading and in vivo drug release studies indicated that the -CHO group from the dextrose increase the drug loading up to 65% and their release kinetics were also studied. The anti-fungal studies indicated that the prepared nanoparticles exhibit strong anti-fungal activity and the minimum concentration needed is 10 mg/ml. The nanoparticles loaded semi-solid gel was prepared using carbopol, methylparaben, propyl paraben and propylene glycol. The in vitro penetration of the ketoconazole-conjugated nanoparticles was studied using the skin. The results indicated that the semi-solid gel preparations influenced the penetration and also favoured the accumulation into the skin membrane. The veterinary clinical studies indicated that the prepared gel is highly suitable for treatment of Malassezia.

A new design for the review and appraisal of semi-solid dosage forms: Semi-solid Control Diagram (SSCD).

The Semi-solid Control Diagram (SSCD) is a new tool designed for the study of different excipients and different semi-solid dosage forms. It can be used to review and evaluate different formulations and/or batches and facilitate the selection of one of them that will present the most suitable galenic characteristics for topical application. It is also useful to track stability studies by comparing the diagrams, which allows to measure the impact of subjecting the formulation to different conditions and times to be examined. In this study, the Semi-solid Control Diagram (SSCD) is used as an instrument for studying and evaluating semi-solid pharmaceutical dosage forms, by comparing several different semisolid preparations (lipogels). With these results, the tool is validated and the best formulation has been discriminated from the others.

Papaverine hydrochloride containing nanostructured lyotropic liquid crystal formulation as a potential drug delivery system for the treatment of erectile dysfunction.

PurposePapaverine hydrochloride (PaHCl) is an old, well-known drug with spasmolytic activity but it has therapeutic effect in erectile dysfunction, too. As an intracavernous injection, it is not used in urologic clinics today because the side effects of the injection are pain, scarring or priapism. Our aim was to develop and test a topical semi-solid preparation containing PaHCl that would provide an alternative administration option by eliminating the undesirable side effects of the injection.Materials and methodsLyotropic liquid crystal (LLC) systems were formulated as a semi-solid preparation with different concentrations of PaHCl. The characterization of the LLC structure was performed by polarization microscopy using a Leica image analyzer and rheological measurements. The drug diffusion and penetration tests were performed with in vitro synthetic membrane and an ex vivo human epidermis, using Franz diffusion cell to test the skin penetration of PaHCl. Human skin was investigated by Raman microscope to visualize the Active Pharmaceutical Ingredient (API) in different skin layers.ResultsThe results of diffusion and penetration showed reverse concentration dependency. The in vitro and ex vivo studies correlated with each other and the results of Raman microscopy. The LLC structure influenced the penetration results, the lower viscosity and lamellar structure increased penetration through the skin.ConclusionBased on our results, a PaHCl containing topically used LLC formulation may be a suitable and effective alternative to the injectable formulation.

Nanotechnology in Wound Healing; Semisolid Dosage Forms Containing Curcumin-Ampicillin Solid Lipid Nanoparticles, in-Vitro, Ex-Vivo and in-Vivo Characteristics.

Purpose: Wound healing is a natural biologic process, but the duration of it may take too long. Trying to shorten this process is one of the challenges for scientists. Many technologies were applied to achieve this goal as well as nanotechnology. In this study semi solid formulations containing curcumin and ampicillin solid lipid nanoparticles (SLNs) were prepared to evaluate as burn wound healing agent.Methods: Curcumin as an anti-inflammatory and anti-bacterial agent and ampicillin as an antibiotic were applied. In-vitro and in-vivo evaluations were carried out. Particle size, loading efficiency, release profile, morphology and anti-bacterial efficacy of desired nanoparticles were evaluated at first. Then the remaining of the antibacterial effect in semi solid preparations was studied. Animal studies for both toxicology using rabbits and skin burn model using rats were designed. Pathology studies after applying of formulations was done too.Results: Desired nanoparticles were spherical in shape and particle size in range of 112-121 nm, with low zeta potential. For increasing stability of particles they were freeze dried using cryoprotectant. Lyophilized particles show no significant size enlargement. Results showed that both ointment and gel preparations have reasonable anti-bacterial effects, both of them cause increasing in the rate of wound healing in comparison with placebos and control groups and none of the formulations showed acute toxicity.Conclusion: It seems that using nanotechnology could shorten wound healing process to reduce treatment costs and increase compliance of patients.