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Formulation, in vitro, and in vivo evaluation of ebastine Solusome nanovesicle-based oral lyophilized tablets
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Background : Ebastine (EBS) is an antihistamine medication commonly used to alleviate symptoms associated with allergic rhinitis and pruritic skin conditions, such as urticaria and other pruritic dermatoses. The main advantage of oral lyophilisates is their high porosity, which facilitates rapid salivary penetration, short disintegration times, and improved bioavailability.

Method : EBS-loaded Solusome nanovesicles were formulated via the thin-film hydration technique using Soluplus® as a stabilizing agent within the nanovesicle system. The Solusome nanovesicles were concentrated using a rotary evaporator before the other excipients were added. The excipients used were gelatin, polyvinylpyrrolidone K90, glycine, and mannitol. They were dissolved in the concentrated Solusome nanovesicles, poured into tablet blister molds, and lyophilized to create EBS-loaded Solusome nanovesicle-based oral lyophilisates.

Results : The selected formula, F7, had the highest desirability value of 1, and its disintegration time and friability were 31.9 s and 0.991%, respectively. The dissolution profile showed a significant enhancement; more than 98% of the drug was released within only 40 min, whereas pure EBS achieved only 42% release during the same period. Compatibility studies showed that there was no chemical interaction between the tablet components. An in vivo bioavailability study of EBS showed that Solusome nanovesicles enhanced bioavailability compared with pure EBS.

Discussion : A notable improvement was observed in both the disintegration time and friability tests. The highly porous structure of oral lyophilisates allows rapid salivary penetration, resulting in very short disintegration times and enhanced bioavailability. Soluplus® can spontaneously form spherical micelles. Furthermore, the polyethylene glycol (PEG) segment of Soluplus® promotes the formation of stable, tightly packed bilayers, thereby reducing particle aggregation and preventing the formation of large vesicular structures.

Conclusion : This study aimed to develop EBS Solusome nanovesicles as oral lyophilisates. The primary goal was to improve tablet disintegration in the mouth, facilitate easier swallowing, and potentially enhance patient compliance. Additionally, the researchers aimed to achieve faster disintegration times for oral lyophilisates, thereby accelerating the onset of EBS therapeutic action.

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Publication Date
Wed Jul 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Fast Dissolving Tablets of Taste-Masked Ondansetron Hydrochloride by Solid Dispersion
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Ondansetron hydrochloride (ONH) is a very bitter, potent antiemetic drug used for the treatment and/or prophylaxis of chemotherapy or radiotherapy or postoperative induced emesis. The objective of this study is to formulate and evaluate of taste masked fast dissolving tablet (FDTs) of ONH to increase patient compliance.

 ONH taste masked granules were prepared by solid dispersion technique using Eudragit E100 polymer as an inert carrier. Solvent evaporation and fusion melting methods were used for such preparation.

Completely taste masking with zero release of drug in phosphate buffer pH 6.8was obtained from granules prepared by solvent evaporation method using drug: polymer ratio of 1:2, from which four formulas pas

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Publication Date
Sat Dec 30 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation, In-vitro, and Ex-vivo Evaluation of Ondansetron Loaded Invasomes for Transdermal Delivery
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Invasomes are newly developed types of nanovesicles. A vesicular drug delivery system is considered one of the approaches for transdermal delivery to enhance permeation and improve drug bioavailability. Ondansetron is a serotonin receptor antagonist used for treating vomiting associated with different clinical cases. The study aimed to prepare invasomal dispersions for improving permeation of ondansetron across the skin with a controlled release pattern. Twenty-seven formulas of ondansetron-loaded invasomes were prepared by a modified mechanical dispersion method. These formulas were optimized by studying the effect of variables on entrapment efficiency. Vesicle size, polydispersity, zeta potential, in-vitro release and ex-vivo perm

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Publication Date
Tue Jun 11 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and In-Vitro Evaluation as an Oral Microsponge Tablet of Baclofen
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The aim of the present study is to formulate floating effervescent microsponge tablet of the narrow absorption window drug, Baclofen (BFN) for controlling drug release and thereby decrease the side effect of the drug. The microsponges of BFN were prepared by non-aqueous emulsion solvent diffusion method (oil in oil emulsion method). The effects of drug: polymer ratio, stirring time and type of Eudragit polymer  on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selected microsponge formula was incorporated into the floating effervescent gastro-retentive tablet. The prepared fl

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Publication Date
Sat Aug 01 2020
Journal Name
Research Journal Of Pharmacy And Technology
Evaluation of in vivo and in vitro protective effects of quercetin on lipopolysaccharide-induced inflammation and cytotoxicology
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Quercetin, one of the flavonoids family member, can be found in many vegetables, fruits, and beverages with a noticeable nutritional pharmacological properties. This study was aimed to evaluate the ability of quercetin to inhibit lipopolysaccharide (LPS) that induced lethal toxicity in vivo, and to elucidate the importance of the quercetin as an antitumor agent in breast cancer cell line MCF-7.In vivo experiments included the effect of hesperidin and LPS on the liver and spleen of male mice. In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH), and catalase (CAT), while in the spleen, the concentration of cytokines was measured including IL-33 and TNF-α. In vitro experiments included MTT

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Publication Date
Fri Oct 01 2021
Journal Name
International Journal Of Drug Delivery Technology
Formulation and In-vitro Evaluation of Thermosensitive Ciprofloxacin HCL In-situ Gel for Local Nasal Infection
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Publication Date
Wed Jan 22 2020
Journal Name
Molecules
In Vivo and In Vitro Evaluation of the Protective Effects of Hesperidin in Lipopolysaccharide-Induced Inflammation and Cytotoxicity of Cell
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(1) Background: Plant flavonoids are efficient in preventing and treating various diseases. This study aimed to evaluate the ability of hesperidin, a flavonoid found in citrus fruits, in inhibiting lipopolysaccharide (LPS) induced inflammation, which induced lethal toxicity in vivo, and to evaluate its importance as an antitumor agent in breast cancer. The in vivo experiments revealed the protective effects of hesperidin against the negative LPS effects on the liver and spleen of male mice. (2) Methods: In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH) and catalase (CAT), whereas in spleen, the concentration of cytokines including IL-33 and TNF-α was measured. The in vitro expe

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Publication Date
Sat Feb 18 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences
Preparation and In-Vitro Evaluation of Floating Oral In- Situ Gel of Montelukast Sodium (Conference Paper) #
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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn: 1683 - 3597 , E-issn : 2521 - 3512)
Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation
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Nebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formulas wit

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation
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Nebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formul

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Publication Date
Tue Nov 22 2016
Journal Name
Der Pharma Chemica
Evaluation of Commercial Antacid Tablets in Iraq
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Antacids are commonly used drugs which are considered inert and free of pharmacological effect by many patients and physicians. They are weak bases that neutralize the gastric acid and relief pain. These weak bases dissociate to neutralize gastric acid and form neutral salts. The ultimate goal of antacid therapy is to reduce the concentration and a total load of acid in gastric juice to a pH 4 - 5. This in vitro study was promised to study the acid neutralizing capacity (ANC) of six commonly available antacids tablets in the Iraqi market by using back titration method. The highest ANC values were for Rennie (17.131± 0.083 and 16.926± 0.052 mEq) in two different hydrochloric acid (HCl) concentrations 1N and 0.5 N, respectively. The static

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