• Advances in Traditional Medicine
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• v.7 no.1
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• pp.51-64
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• 2007

Mucus is an aqueous gel complex with a constitution of about 95% water, high molecular weight glycoprotein (mucin), lipid, salts etc. Mucus appears to represent a significant barrier to the absorption of some compounds. Natural mucoadhesive agent was isolated and purified from the aqueous extract of the seeds of prosopis pallida (PP). Formulated tablet with the isolated material by wet granulation method. Some natural edible substances are in consideration for candidates as mucoadhesive agents to claim more effective controlled drug delivery as an alternative to the currently used synthetic mucoadhesive polymers. Subjected the materials obtained from natural source i.e. PP and standard synthetic substance, sodium carboxymethyl cellulose for evaluation of mucoadhesive property by various in vitro and in vivo methods. Through standard dissolution test and a model developed with rabbit, evaluated in vitro controlled release and bioadhesive property of theophylline formulation. Mucoadhesive agent obtained from PP showed good mucoadhesive potential in the demonstrated in vitro and in viνo models. The results suggest that the mucoadhesive agent showed controlled release properties by their application, substantially. In order to assess the gastrointestinal transit time in vivo, a radio opaque X-ray study performed in healthy rabbit testing the same controlled release formulation with and without bioadhesive polymer. Plasma levels of theophylline determined by the HPLC method and those allowed correlations to the in vitro mucoadhesive study results. Better correlation found between the results in different models. PP may acts as a better natural mucoadhesive agent in the extended drug delivery system.

• Journal of Pharmaceutical Investigation
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• v.38 no.6
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• pp.387-392
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• 2008

Alfuzosin, an Alphal-adrenoceptor antagonist is used for the treatment of patients with voiding and in a lesser extent storage lower urinary tract symptoms (LUTS) associated to benign prostatic hyperplasia (BPH). The objective of this study was to formulate sustained release alfuzosin HCl granules and assess their formulation variables. The $Eudragit^{(R)}$ as a polymer, sustained release membrane, and dibutyl sebacate (DBS) as a plasticizer were used. Multi-coated alfuzosin HCl delivery systems composed of sugar sphere, various excipients, $Eudragit^{(R)}$ and HPMC (hydroxy propyl methyl cellulose), Cellulose Acetate were prepared by fluid-bed coater. Membrane layer were used $Eudragit^{(R)}$ RS PO and NE 30D. And the alfuzosin HCl coated beads were coated immediate release drug layer for initial burst. Its dissolution test was carried out compared to conventional products ($XATRAL^{(R)}$ XL). The release rate of drug from coated beads was higher than that from $XATRAL^{(R)}$ XL in pH 6.8.

• CELLMED
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• v.11 no.1
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• pp.6.1-6.7
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• 2021

In situ gelling devices, as they enter the body, are dosage forms in the shape of the sol but turn into gel types under physiological circumstances. Transition from sol to gel is contingent on one or a mixture of diverse stimuli, such as transition of pH control of temperature, irradiation by UV, by the occurrence of certain ions or molecules. Such characteristic features may be commonly employed in drug delivery systems for the production of bioactive molecules for continuous delivery vehicles. The technique of in situ gelling has been shown to be impactful in enhancing the potency of local or systemic drugs supplied by non-parenteral pathways, increasing their period of residence at the absorption site. Formulation efficacy is further improved with the use of mucoadhesive agents or the use of polymers with both in situ gelling properties and the ability to bind with the mucosa/mucus. The most popular and common approach in recent years has provided by the use of polymers with different in situ gelation mechanisms for synergistic action between polymers in the same formulation. In situ gelling medicine systems in recent decades have received considerable interest. Until administration, it is in a sol-zone and is able to form gels in response to various endogenous factors, for e.g elevated temperature, pH changes and ions. Such systems can be used in various ways for local or systemic supply of drugs and successfully also as vehicles for drug-induced nano- and micro-particles. In this review we will discuss about various aspects about use of these in situ gels as novel drug delivery systems.

• Journal of Pharmaceutical Investigation
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• v.40 no.spc
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• pp.9-17
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• 2010

Polymorphism has been recognized to be a critical issue throughout the drug product development process. Most of solid phase drugs have polymorphism, which has generated a great deal of interest and the field has been evolving rapidly. Preferably, thermodynamically most stable form of a drug substance is selected to obtain consistent bioavailability over its shelf life and various storage conditions. Moreover, it has the lowest potential for conversion from one polymorphic form to another. However, metastable or amorphous forms may be used intentionally to induce faster dissolution rate for rapid drug absorption and higher efficacy. For pharmaceutical industry, polymorphism is one of the key activities in form selection process together with salt selection. This article introduces the main features in the investigation of solid form selection especially polymorphic behavior with thermodynamic backgrounds, physicochemical properties with solubility, dissolution, and mechanical properties, and characterization techniques for proper analysis. The final form can be recommended based on the physicochemical and biopharmaceutical properties and by the processability, scalability and safety considerations. Pharmaceutical scientists especially in charge of formulation need to be well aware of the above issues to assure product quality.

• Journal of Pharmaceutical Investigation
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• v.29 no.2
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• pp.127-136
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• 1999

In order to eliminate demerits of conventional dosage forms, dipotassium glycyrrhizate was formulated as a slim mucoadhesive film type dosage form. The mucoadhesive drug layer gel containing dipotassium glycyrrhizate was prepared using $Noveon^{\circledR}$ AA-1, hydroxypropylcellulose-M, ethylcellulose N 100 and citric acid, and the protective layer gel by using ethylcellulose N 100, $Eudragit^{\circledR}$ RS and castor oil. The viscosity of drug layer gel of mucoadhesive film was enhanced as the increased amount of $Noveon^{\circledR}$ AA-1 or hydroxypropyl cellulose-M. The drug content was unifonnly $1160{\pm}14.6\;{\mu}g$, and was varied within 3.5%. The optimum film dosage form showed a good fluidity and malleability of drug layer, with 179 g of thickness, pH 5.7, 411 min of in vitro adhesion time and 172 g in gravity adhesive strength. The release time of drug from the mucoadhesive film was significantly shorter but was delayed when polymers such as ethylcellulose was added. From these results, the new mucoadhesive film may be effective for the treatment of aphthous stomatitis.

• Journal of Pharmaceutical Investigation
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• v.39 no.2
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• pp.111-115
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• 2009

The pharmacokinetics of cyclosporin A (CsA) after single and multiple oral dosing of new CsA self-micro-emulsifying drug delivery system (SMEDDS) in dogs were estimated. A single dose study was performed following a two-way crossover design against six dogs with reference SMEDDS. For a multiple dose study, three dogs were allocated for each drug, and 100 mg of drug was administered daily for 6 days. Whole blood concentration of CsA was analyzed by radio-immunoassay. Both drug showed identical blood concentration profiles in both studies, and no statistical difference was detected in pharmacokinetic parameters. The relative bioavailabilities of test SMEDDS were 91.4% and 89.1%, respectively, in the single dose study and the last day of multiple dose study. Especially, multiple dose study proved the good relationship between C-0/C-2 and AUC for reference SMEDDS, which is an indispensable part of therapeutic drug monitoring. These results suggest newly formulated CsA SMEDDS possibly shows identical pharmacokinetics and pharmacodynamic behaviors in clinical trials.

• Journal of Life Science
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• v.24 no.4
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• pp.437-446
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• 2014

Problems appear when triptans are taken orally. For example, the bioavailability of triptan is reduced by the digestive system, and the drug level in the blood reduces rapidly over time; there is also a possibility of gastrointestinal disorder. To improve side effects, a transdermal patch has been prepared in hydrogel form. The polymer matrix that makes up the hydrogel uses PVA; PEG is used as an additive to induce inter/intra hydrogen bonding of the PVA and almotriptan drug is added. In addition, to accelerate micro-phase separation between PVA chains, liquid nitrogen is used. In FT-IR analysis, the absorption bands of PVA, PEG, and almotriptan were found. The degree of crystallinity, the water uptake ability and tensile strength were increased with increasing PEG content. In drug release tests, the amount of drug released increased depending on the PEG content. In this study, hydrogels with 10 wt% PEG showed better performance in drug release. Approximately 60% of the total drug amount was released in 2 hr, and the drug continued to release for 1 day. Thus, the prepared hydrogel patch is suitable as a transdermal formulation for the second dose administration of triptans to patients who require recurrent migraine treatment within 24 hr after the first administration.

• CELLMED
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• v.10 no.3
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• pp.22.1-22.7
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• 2020

Introduction: Qūbā (Tinea Corporis) is a very common disease widely prevalent worldwide. 20 - 25 % individuals suffer for this stubborn disease. Unani System of Medicine offers its treatment. There are many pharmacopoeial formulations indicated for various types of dermatophytic infections. In this study clinical efficacy and safety of the topical Unani formulation Marham Kharish Jadeed (a compound drug in the dosage form of an ointment) was assessed and compared with a standard conventional medicine. Materials and methods: A clinical study was conducted on 60 participants of qūbā randomized into test and control groups (n=30 in each group). The participants were clinically diagnosed and confirmed by microscopy of skin scrapings. The efficacy of the Unani formulation was assessed in terms of TSS score and elimination of fungal elements from the skin lesions. The data collected were analyzed statistically. Results and discussion: The study showed that the Unani formulation had comparatively better efficacy clinically than conventional medicine Terbinafine hydrochloride 1% cream in terms of reduction of itching, erythema, scaling, peripheral raised margins of the lesion comparing to baseline. In this study, 27 participants in test group and 18 participants in control group were completely cured (≥75% reduction in TSS Score with Mycological Cure) after 4 weeks of treatment. The efficacy of the Unani formulation was found significant statistically. The individual drugs of the formulations having analgesic (Musakkin), blood purifier (Muṣaffi-i-Dam), demulcent (Mulaṭṭif), antifungal (Qātil-i-fafūndῑ), detergent (Jālῑ), refrigerant (Mubarrid) and antiseptic (Dāfi'-i-'Ufūnat) properties might be responsible for the efficacy of Unani formulation. Conclusion: The findings of the study suggested that the Unani formulation was found effective and safe in the management of qūbā. No local and systemic adverse effect was reported during the study.

• Biomolecules & Therapeutics
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• v.26 no.2
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• pp.218-223
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• 2018

The liver is an essential organ for the detoxification of exogenous xenobiotics, drugs and toxic substances. The incidence rate of non-alcoholic liver injury increases due to dietary habit change and drug use increase. Our previous study demonstrated that Ecklonia stolonifera (ES) formulation has hepatoprotective effect against alcohol-induced liver injury in rat and tacrine-induced hepatotoxicity in HepG2 cells. This present study was designated to elucidate hepatoprotective effects of ES formulation against carbon tetrachloride ($CCl_4$)-induced liver injury in Sprague Dawley rat. Sixty rats were randomly divided into six groups. The rats were treated orally with ES formulation and silymarin (served as positive control, only 100 mg/kg/day) at a dose of 50, 100, or 200 mg/kg/day for 21 days. Seven days after treatment, liver injury was induced by intraperitoneal injection of $CCl_4$ (1.5 ml/kg, twice a week for 14 days). The administration of $CCl_4$ exhibited significant elevation of hepatic enzymes (like AST and ALT), and decrease of antioxidant related enzymes (superoxide dismutase, glutathione peroxidase and catalase) and glutathione. Then, it leaded to DNA damages (8-oxo-2'-deoxyguanosine) and lipid peroxidation (malondialdehyde). Administration of ES formulation inhibited imbalance of above factors compared to $CCl_4$ induced rat in a dose dependent manner. Real time PCR analysis indicates that CYP2E1 was upregulated in $CCl_4$ induced rat. However, increased gene expression was compromised by ES formulation treatment. These findings suggests that ES formulation could protect hepatotoxicity caused by $CCl_4$ via two pathways: elevation of antioxidant enzymes and normalization of CYP2E1 enzyme.

• Archives of Pharmacal Research
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• v.29 no.12
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• pp.1187-1192
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• 2006

The aims of this study were to encapsulate arbutin (AR) in liposome to enhance the skin-whitening activity, and to investigate the effect of liposome formulation on the entrapment efficiency (EE%), skin permeation rate and skin deposition. The liposomes were prepared by a film dispersion method with several different formulations and were separated from the solution by using the gel-filtration method. The physical (size distribution, morphology) and chemical (drug entrapment efficiency, hairless mouse skin permeation and deposition) properties of liposomes were characterized. The entrapment efficiency in all liposome formulations varied between 4.35% and 17.63%, and was dependent on the lipid content. The particle sizes of liposomes were in the range of $179.9{\sim}212.8\;nm$ in all liposome formulations. Although the permeation rate of AR in the liposome formulations decreased compared with AR solution, the deposition amount of AR in the epidermis/dermis layers increased in AR liposomal formulation. These results suggest that liposomal formulation could enhance the skin deposition of hydrophilic skin-whitening agents, thereby enhancing their activities.