Drug-excipient Interactions Research Articles

Strategies for formulation of effervescent granules of an herbal product for the management of typhoid fever

Herbal medicines are currently being adopted as alternatives to orthodox medicines for the management of drug-resistant and emerging multidrug-resistant microbial strains of various diseases, including typhoid fever. A herbal decoction, MA 001, manufactured by the Centre for Plant Medicine Research (CPMR), has been used for the treatment of typhoid fever for at least two decades in Ghana with desirable outcomes. MA 001 is formulated from Citrus aurantifolia, Spondias mombin, Latana camara, Bidens pilosa, Trema occidentalis, Psidium guajava, Morinda lucida, Vernonia amygdalina, Persea americana, Paulina pinnatta, Momordia charantia and Cnestis ferruguinea medicinal plants. The low palatability and compliance to treatment due to the bulky nature of the decoction poses challenges in its optimum use. This study sought to design and formulate the therapeutic components of the aqueous herbal decoction of MA 001 into an optimal solid dosage form of effervescent granules to improve the delivery of MA 001 as well as increase patient compliance and convenience of product handling. The methods involved pre-formulation studies on the suitability of effervescent vehicles, formulation and evaluation of effervescent granules for drug excipient interactions using high performance liquid chromatography analysis. The findings indicate that the effervescent granules were suitable for use in the delivery of the therapeutic constituents for the treatment of typhoid fever as done with the decoction due to minimal herbal extract-excipient interaction.

Development and evaluation of Pharmacosome formulations of Mefenamic acid

Patience who suffered from menstrual pain disease is generally prescribed the non-steroidal anti-inflammatory drug (NSAIDs). Monorrhagia or another blood disorder & some gynecological disorder, which impairs body function and acts as an economic burden. Due to respective use of ACE by oral route, it may cause GI complication such as bleeding, pain, perforation, abdominal pain, and swelling. To decrease the side effect of ACE, it is given by topical route in promotes the safety & efficacy of the ACE. The Mefenamic Acid pharmacosomes were prepared by the hand shaking method technique and evaluated by various methods such as in-vitro release study, % yield, drug entrapment efficiency, pH of the prepared formulation. The prepared system was also characterized by FTIR spectrophotometer to identify the drug-excipients interaction. The maximum entrapment efficiency of pharmacosomes was found to be 90%. The main aim of this study was to develop and characterized a vesicular drug carrier system for topical delivery of Mefenamic Acid to overcome the problem related with oral route.

Inhaled Edoxaban dry powder inhaler formulations: Development, characterization and their effects on the coagulopathy associated with COVID-19 infection

Herein, we demonstrated the development and characterization of a dry powder inhaler (DPI) formulation of edoxaban (EDX); and investigated the in-vitro anticoagulation effect for the management of pulmonary or cerebral coagulopathy associated with COVID-19 infection. The formulations were prepared by mixing the inhalable micronized drug with a large carrier lactose and dispersibility enhancers, leucine, and magnesium stearate. The drug-excipient interaction was studied using X-Ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) methods. The drug and excipients showed no physical inter particulate interaction. The in-vitro drug aerosolization from the developed formulation was determined by a Twin Stage Impinger (TSI) at a flow rate of 60 ± 5 L /min. The amount of drug deposition was quantified by an established HPLC-UV method. The fine particle fraction (FPF) of EDX API from drug alone formulation was 7%, whereas the formulations with excipients increased dramatically to almost 7-folds up to 47%. The developed DPI formulation of EDX showed a promising in-vitro anticoagulation effect at a very low concentration. This novel DPI formulation of EDX could be a potential and effective inhalation therapy for managing pulmonary venous thromboembolism (VTE) associated with COVID-19 infection. Further studies are warranted to investigate the toxicity and clinical application of the inhaled EDX DPI formulation.

Design and Characterization of Buccal Films of Benzocaine for Mouth Ulcer

Mouth ulcer is very common in recent years, which occurs due to the damage of epithelial tissue and/or lamina propria that finally leads to tissue necrosis. Benzocaine has been used to treat the mouth ulcers due to its excellent local anaesthetic effect that relieves the pain associated with mouth ulcer. Hence an attempt was made to develop and characterize the buccal films of Benzocaine to treat mouth ulcers with an aim of prolonging the drug release and improving the patient convenience. The films were fabricated using the mucoadhesive polymer blend of chitosan and HPMC by solvent casting method and the physico-mechanical, in vitro drug release and ex vivo buccal mucosal permeation characteristics of the films were studied. All fabricated film formulations prepared were smooth and almost opaque, with good flexibility. The weight and thickness of all the formulations were found to be uniform. Drug content in the films ranged from 97–99%, indicating favorable drug loading and uniformity. The inclusion of HPMC, significantly reduced the bioadhesive strength and in vitro mucoadhesion time of chitosan films, although the degree of swelling increased. In vitro drug release and permeation studies in simulated saliva showed a prolonged release for a period of 6 h for all formulations. The formulation with Chitosan: HPMC ratio 1:1, 10% w/w polysorbate 80 and 10% w/w propylene glycol as plasticizers showed the best results which exhibited the cumulative percentage drug release of 87.9 % and the cumulative amount of drug permeation of 7.62mg/cm2 across goat buccal mucosa in 6 h. Drug-excipient interaction studies were carried out using DSC and FT-IR technique; films indicated no chemical interaction between drug and polymers used. Keywords: Benzocaine; mouth ulcer; mucoadhesion; buccal film

FORMULATION AND OPTIMIZATION OF NIFEDIPINE LOADED NANOCARRIERS

Objective: The main aim of this study to formulate a nifedipine-loaded nanocarrier for improving solubility and bioavailability. Methods: To improve the solubility of drug, nifedipine-loaded nanocarrier (lipotomes) were prepared by using the film lipid hydration technique. lipotomes were prepared by using tween 80, which is used for increasing solubility and cetyl alcohol for lipophilic environment. Drug excipients interaction determined by FTIR. lipotomes were characterized for particle size, Entrapment efficiency and zeta potential. lipotomes were optimized by using Design-Expert 12 software. Optimized formula further lyophilized by using different cyroproyectant to improve the stability and oral administration of the drug. Results: FTIR shows there was no interaction between formulation ingredients. Mean particle size, entrapment efficiency, zeta potential was determined and found to be 308.1 nm, 96.7%, 20.1mV, respectively. Surface morphology of lipotomes was observed by a scanning electron microscope (SEM). Optimized lipotomes was lyophilized with Mannitol (8% w/v) was the ideal cryoprotectant to retain the physicochemical characteristics of the OLT formulation after lyophilization. Conclusion: Nifedipine loaded nanocarrier was successfully prepared, using film hydration method. Which have good particle size, EE% and zeta potential. After lyophilization no significant changes was observed in particle size with good physical stability, so it could be a good choice for conventional drug delivery system by doing further investigation as in vitro and in vivo study

Impact of Solubility Enhancement Methods on the Dissolution Rate of Valsartan Sachet

The oral drug delivery is the most generally used route of administration that has been explored for the delivery of drugs through various pharmaceutical products. Solubility of drug plays critical role in achieving the optimum therapeutic levels of the drug in blood and thus bioavailability. There are many drugs of various therapeutic categories fall in Biopharmaceutics Classification System Classes II and IV as they lack solubility. For all these drugs, dissolution is the big issue for the absorption process. Valsartan is an effective antihypertensive agent and it can be used for the treatment of hypertension in most cases. The objective of this study is to prepare Valsartan as an oral sachet which can be used as an alternative dosage form after improvement of drug solubility using solubilizing agents such as sodium lauryl sulfate and tween 80. Three different formulas of Valsartan sachet were prepared by conventional technique of wet granulation method named conventional formula (Fc), sodium lauryl sulfate formula (Fs), and tween 80 formula (Ft) then compared with the available marketed product of Valsartan tablet (Fd) as a reference. The preformulations studies were conducted to exclude drug excipients interaction. Evaluation was performed in terms of weight variation, dose content uniformity, and drug release study using dissolution test apparatus. Fourier Transforms Infrared Spectroscopy reveals no drug excipient interaction and the drug release profile for Fs and Ft formulas within 30 min was 100.16% and 104.16%, respectively, while for Fc only 57.55% of the drug was released. This difference in the release profile was statistically significant (P < 0.05) between Fs and Ft with Fc, but a non- significant difference (P > 0.05) was observed between Fs and Ft with the marketed Valsartan tablet (Fd). The results support the possibility of using the prepared formulas Fs and Ft as a Valsartan sachet for the oral administration alternative to conventional Valsartan tablets Fd.

Development, Formulation and Evaluation of Sustain Release Dispersible Tablet of Ornidazole

This Present research with dispersible tablet can compromise the efficacy and safety of the treatment to children’s and geriatric patients with masking the bitter taste of drug and developing its dispersible tablet. The purpose of this research work was to develop Dispersible tablet of Ornidazole by masking the bitter taste. Tablet containing drug and excipients were prepared by direct compression method. Excipients in combinations were incorporated to achieve the aim. Effect of different combinations was studied to optimize the ideal formulation. Drug excipients interaction studies were carried out by FTIR spectral analysis. The tablets were evaluated for their hardness, wetting time, disintegrating time and dissolution parameters. It was concluded that the tablets having the combination of Dried Mucilage (obtained from dried seeds of ocimum bacilicum) and Sodium starch glycolate met all the evaluation parameters and thus selected as the optimized formulation. Optimized formulation was undergone for stability testing as a parameter to predict the shelf life as per ICH guidelines and proved for its adequate shelf life.

COMPATIBILITY STUDY BETWEEN PRAVASTATIN AND EZETIMIBE, AND PHARMACEUTICAL EXCIPIENTS USED IN FIXED-DOSE COMBINATION TABLET

Objective: The purpose of this study was to qualitatively predict drug-excipient binding interactions for stable drug formulation of a pravastatin and ezetimibe fixed-dose combination (FDC) tablet. Methods: Drug impurity-excipient interactions under accelerated conditions (40°C/75% relative humidity) for 4 weeks were confirmed by high-performance liquid chromatography, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and thermogravimetric (TG) analysis. Results: Pravastatin impurity was affected by four excipients under accelerated conditions for 4 weeks. Ezetimibe was affected by two excipients. Any other results were within the acceptance criteria. XRD analysis for physical stability revealed characteristic peaks of pravastatin and ezetimibe at a diffraction angle of 2θ (pravastatin: 4.1–24.4°, and ezetimibe: 13.62–29.59°) without a change in the crystalline form after 4 weeks. DSC and TG analysis showed evidence of stability in Alu-Alu foil. Conclusion: Thus, the tested excipients were confirmed to be compatible with pravastatin and ezetimibe and can be used in FDC bi-layer tablets.

Formulation and in vitro Evaluation of Matrix tablets containing Repaglinide

The aim of this project was to develop sustained release matrix tablets of Repaglinide. Sustained release matrix tablets of Repaglinide were prepared by the wet granulation method using polymers like Hydroxy propyl methyl cellulose, Microcrystalline cellulose, Eudragit RS-100 in different ratios. The matrix tablets of Repaglinide were evaluated for hardness, weight variation, friability, drug content uniformity, and in-vitro drug release. In order to determine the drug release mechanisms and kinetics, the data was subjected to zero order, first order, and higuchi and peppas diffusion model. Twelve batches of sustained release matrix tablets of Repaglinide were developed. Among these formulations F4, F8 and F12 formulation showed satisfactory physicochemical properties and drug content uniformity and sustained release of drug for 12 hours with maximum release of 86.95%, 84.91% and 84.91%. The optimized formulations were characterized for Differential scanning calorimetric analysis; Fourier transforms infrared spectroscopy and scanning electron microscopic studies. IR spectroscopic studies indicated that there were no drug-excipient interactions. The prepared sustained release matrix tablets of Repaglinide were successfully developed and evaluated.

Preparation of Cinnarizine Oral Lyophilizates

Background: Orally disintegrating tablets (ODTs) have gained an increasing interest in the pharmaceutical industry for the last years. Several technologies have been sophisticated for ODTs to improve patient compliance. In the present work, an attempt has been made to formulate and evaluate cinnarizine, a drug for motion sickness, in an easy to administer, rapid disintegrated dosage form (oral lyophilizates with enhanced disintegration and dissolution profile and consequent potential improvement in bioavailability.Materials and Methods: Cinnarizine oral lyophilizates were prepared by dispersing the drug in an aqueous solution of mannitol, hydroxypropyl methyl cellulose, and glycine. Different formulations were prepared by freeze-drying (lyophilisation) technique. The effect of concentration of mannitol, hydroxypropyl methyl cellulose, and freezing time on the lyophilizates characteristics was investigated. The drug-excipient interaction was investigated as well.Results: The resulting cinnarizine oral lyophilizates showed an enhanced disintegration (27.5±3.53 sec to 56±12.73 sec) and enhanced dissolution profile (25.09% to 44.7% after two minutes). The infrared spectroscopic studies showed no drug-excipient interactions. Furthermore, increasing the concentration of mannitol, increasing the concentration of hydroxypropyl methyl cellulose and duplication of the duration of freezing time had a negative influence on the disintegration and dissolution properties of the resulting lyophilizates.Conclusion: Cinnarizine oral lyophilizates were successfully prepared and resulted in a rapid disintegration, high dissolution profile, with stable characteristics and without noticeable drug-excipient interaction.

PharmDE: A new expert system for drug-excipient compatibility evaluation

Drug-excipient compatibility study is the essential basis for excipient selection at the pre-formulation stage. According to the pharmaceutical Quality by Design (QbD) principles, a comprehensive understanding of the ingredients' physicochemical properties and a theoretical evaluation of the interaction risk between the drugs and excipients are required for conducting rational compatibility experimental design. Currently, there is an urgent need to establish an artificial intelligence system for researchers to easily get through the problem because it is very inconvenient and hard to utilize those drug-excipient incompatibility data scattered in scientific literature. Here, we designed a knowledge-driven expert system named PharmDE for drug-excipient incompatibility risk evaluation. PharmDE firstly developed an information-rich database to store incompatibility data, covering 532 data items from 228 selected articles. Then, 60 drug-excipient interaction rules were created based on our knowledge and formulation research experiences. Finally, the expert system was developed by organically integrating the database searching and rule-based incompatibility risk prediction, which resulted in four main functionalities: basic search of incompatibility database, data matching by similarity search, drug incompatibility risk evaluation, and formulation incompatibility risk evaluation. PharmDE is expected to be a useful tool for drug-excipient compatibility study and accelerate drug formulation design. It is now freely available at https://pharmde.computpharm.org.

Comparative Evaluation of Amorphous Polymers in Solubility and Bioavailability Enhancement of Famotidine Through Solid Dispersion

The present study aimed to enhance the dissolution rate, therefore bioavailability, of famotidine (FMT) using its solid dispersions (SDs) with polyvinyl pyrrolidone (PVP)-K 30, milk powder, and inulin, both in-vitro and in-vivo. The study was also aimed to compare the effect of different amorphous polymers in enhancing the dissolution rate of FMT. The SDs were prepared with a 1:4 weight ratio by a solvent evaporation technique. Evaluation of the properties of the SDs was performed using dissolution, Fourier-transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD) studies. The SDs of FMT exhibited an enhanced dissolution rate. The FTIR spectroscopic studies showed the stability of FMT and the absence of well-defined drug excipient interaction. The XRD studies indicated the amorphous state of FMT in SDs. The drug release rate of all SDs formulation was found to be greater than the pure drug. Within one hour of dissolution studies, 99.43%, 92.5%, and 58.93% drug release were obtained, respectively, for PVP K-30, milk powder, and inulin. The first two were showing significantly higher release. SDs were also studied for bioavailability studies in-vivo in rats, which confirms that the SDs prepared by PVP K-30 and milk powder significantly enhancing the bioavailability of FMT. The maximum concentration of 15.05±2.45 μg/ml was achieved in 2 hours, and the area under the curve was found to be 33.78±7.3 μg. hour/ml. Therefore, the study results conclude that SDs of the FMT prepared by PVP K-30 successfully increases the dissolution and in-vivo bioavailability. Keywords – Solid dispersion, Second generation solid dispersions, Famotidine, In-vivo bioavailability, amorphous polymers, dissolution enhancement, solubility enhancement.

Strategies for Formulation of Effervescent Granules of an Herbal Product for the Management of Typhoid Fever

Herbal medicines are currently being adopted as alternatives to orthodox medicines for management of drug resistant and emerging multi drug resistant microbial strains of various diseases including typhoid fever. An herbal decoction, MA 001 manufactured by the Centre for Plant Medicine Research (CPMR) has been used for treatment of typhoid fever for at least two decades in Ghana with desirable outcomes. The low palatability and compliance to treatment due to the bulky nature of the decoction poses challenges in its optimum use. This study sought to design and formulate the therapeutic components of the aqueous herbal decoction of MA 001 into an optimal solid dosage form of effervescent granules to improve the delivery of MA 001 as well as increase patient compliance and convenience of product handling. Methods involved pre-formulation studies on suitability of effervescent vehicle, formulation and evaluation of effervescent granules for drug excipient interactions using high performance liquid chromatography analysis. The findings indicate that the effervescent granules were suitable for use in the delivery of the therapeutic constituents for the treatment of typhoid fever as done with the decoction due to minimal herbal extract-excipient interaction.

POTENTIATING MICONAZOLE ACTIVITY WITH CLOVE OIL AND CHITOSAN IN MICROEMULSION BASED GEL FOR TREATMENT OF FUNGAL INFECTION

The study aimed to investigate the in vitro antifungal activity of miconazole entrapped in microemulsion based gel with clove oil as permeation enhancer and chitosan as antifungal agent. SEM confirmed spherical droplets of microemulsion in the 2 micron size range. The viscosity of emugel was 2251 cP, excellent spreadability 31.27 ±0.219 g.cm/cc as compared to marketed formulation. pH was 5.528 ± 0.032, homogeneity was excellent and drug content was 98 % in optimized batch. No drug-excipients interaction was reported in FTIR spectroscopy. In vitro drug release showed 94.8 % in 6 h. Ex vivo skin permeation showed higher steady state flux than conventional cream. Antifungal activity on Candida albicans showed a zone of inhibition more than that of marketed preparation. Thus, it can be concluded that the formulation may hold some promise for the treatment of severe fungal infections.

Formulation and Evaluation of Effects of Superdisintegrants on Immediate Release Tablet of Linagliptin, a DPP-4 Inhibitor

The study aimed to develop and evaluate an immediate-release tablet dosage form of Linagliptin. Different concentrations (ranges 5-10%) of super-disintegrants, Croscarmellose sodium (CCS), and Sodium starch glycolate (SSG) were used to prepare nine tablet dosage forms (F1 to F9) through the direct compression method. The compatibility of the formulations was evaluated by FTIR to reveal any possible drug-excipient interactions and it was proved to be compatible with all formulations. Precompression (bulk density, tapped density, Carr’s index, Hausner’s ratio, and angle of repose) and post-compression parameters (weight variation, hardness, thickness, and friability) were analyzed for all tablets and the results were found satisfactory as well as within limits as per USP guidelines. All the formulated batches (F1 to F9) exhibited disintegration of tablets within 2 minutes, where formulation F9 represented the lowest disintegration time (51±3 sec) which was also found significantly better than the marketed product (310±5 sec). In terms of drug dissolution, 90% of drug release was observed for all nine formulations within 45 minutes and formulation F9 (5% CCS and 5% SSG) illustrated the rapid and highest dissolution rate compared to the marketed one’s, 100% drug release at 20 minutes and 91.77 % drug release at 30 minutes successively. The respective data sets of drug release were mathematically fitted to several kinetic models and for all formulations, drug release pattern obeyed first-order kinetics amongst those, formulation F2 (r2= 0.98), F4 (r2= 0.99), F5 (r2= 0.98), and F9 (r2= 0.97) were found to be best fitted in this kinetic norm. Based on disintegration time and dissolution data comparison to a brand leader market product, F9 was experienced as the best formulation. Furthermore, it was observed that if SSG and CCS were combined, then these two parameters were more improved compared to their separate uses. Thus, incorporation of the optimum amount of super-disintegrants in a formulation showed rapid swelling, faster disintegration as well as ease of dissolution of tablet dosage forms. Bangladesh Pharmaceutical Journal 24(2): 168-179, 2021

3D Printing of Dapagliflozin Containing Self-Nanoemulsifying Tablets: Formulation Design and In Vitro Characterization.

The 3D printing techniques have been explored extensively in recent years for pharmaceutical manufacturing and drug delivery applications. The current investigation aims to explore 3D printing for the design and development of a nanomedicine-based oral solid dosage form of a poorly water-soluble drug. A self-nanoemulsifying tablet formulation of dapagliflozin propanediol monohydrate was developed utilizing the semisolid pressure-assisted microsyringe (PAM) extrusion-based 3D printing technique. The developed formulation system consists of two major components (liquid and solid phase), which include oils (caproyl 90, octanoic acid) and co-surfactant (PEG 400) as liquid phase while surfactant (poloxamer 188) and solid matrix (PEG 6000) as solid-phase excipients that ultimately self-nanoemulsify as a drug encapsulated nanoemulsion system on contact with aqueous phase/gastrointestinal fluid. The droplet size distribution of the generated nanoemulsion from a self-nanoemulsifying 3D printed tablet was observed to be 104.7 ± 3.36 nm with polydispersity index 0.063 ± 0.024. The FT-IR analysis of the printed tablet revealed that no drug-excipients interactions were observed. The DSC and X-RD analysis of the printed tablet revealed that the loaded drug is molecularly dispersed in the crystal lattice of the tablet solid matrix and remains solubilized in the liquid phase of the printed tablet. SEM image of the drug-loaded self-nanoemulsifying tablets revealed that dapagliflozin propanediol monohydrate was completely encapsulated in the solid matrix of the printed tablet, which was further confirmed by SEM-EDS analysis. The in vitro dissolution profile of dapagliflozin-loaded self-nanoemulsifying tablet revealed an immediate-release drug profile for all three sizes (8 mm, 10 mm, and 12 mm) tablets, exhibiting >75.0% drug release within 20 min. Thus, this study has emphasized the capability of the PAM-based 3D printing technique to print a self-nanoemulsifying tablet dosage form with an immediate-release drug profile for poorly water-soluble drug.

Experimental investigation of ternary mixture of diclofenac sodium with pharmaceutical excipients

Abstract The goal of this work was the study of drug-excipient interactions of ternary mixtures between diclofenac sodium when introduced with excipients commonly explored in solid dosage formulas such as microcrystalline cellulose and stearic acid obtained by three methods. Differential scanning calorimetry (DSC) (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and the structural characterization technique of diffraction (XRPD) were used to investigate the characterization and potential physical and chemical interactions of solid products of diclofenac sodium with excipients prepared by different methods. This work revealed a possible interaction between diclofenac sodium, microcrystalline cellulose, and stearic acid in mixture prepared by microwave irradiation also; it was found compatibility for ternary mixtures prepared by physical mixture and co evaporation methods. Results of this study can be useful in the development of the method of preparation and select adequate excipients with suitable compatibility.

Formulation, In-Vitro Evaluation and Comparative Study Ofitopride Hydrochloride Loaded Sustained Release Matrix Tablet Using Okra Mucilage as a Natural Binder

Natural polymers are abundantly available in plants with their wider pharmaceutical applications and are preferred more than some synthetic polymers because of their biodegradable, biocompatible and non-toxic properties. The study aims to formulate Itopride Hydrochloride loaded Sustained Release (SR) matrix tablet from the mucilage extracted from okra plant (Abelmoschus esculantus) and carry out the comparative study on the release retardant effect of synthetic binders like HPMC K100M and sodium carboxymethyl cellulose and their combinations. The extraction of the mucilage was carried by the maceration process. The formulation of Itopride loaded SR matrix tablet was carried by moist granulation technique. The micrometric, physiochemical studies and purity tests confirms the suitability of mucilage as an excipient. Pre-compression study suggests good flow property of the powders. The minimum angle of repose was observed in F7 with 29.03±0.6º and F2 exhibited maximum angle of repose with 34.30±0.5º. Carr's index and Hausner's ratio was lower in F1 with 11.56±0.4 and 1.11±0.3 respectively. Drug-excipient interaction study performed using FTIR spectrophotometry suggested no interaction between the drug and excipients. The in-vitro drug release of Itopride Hydrochloride loaded SR tablet up to 12 hours in 0.1 N HCl was conducted and observed to be maximum in F3 with 87.34±5.33% and minimum in F6 with 77±5.65 %. Drug release from the formulations were significant compared to the marketed product of Itopride Hydrochloride (p<0.05). The data were analyzed by Tukey post hoc multiple comparison test.

Formulation, development and evaluation of novel oral soluble films of ziprasidone hydrochloride in the treatment of schizophrenia.

Objective: The Present investigation deals with the formulation development and evaluation of rapid dissolving oral films of ziprasidone HCl, an atypical antipsychotic agent, belongs to class-II of BCS classification. Methods: Ziprasidone is a poorly soluble bitter drug and hence inclusion complexes of drug with beta cyclodextrin in different compositions were prepared using kneading technique. Among the prepared compositions, the composition PM8 was chosen to incorporate the ziprasidone HCl into the films. Various film forming water soluble polymers were explored for the casting of oral soluble films. Based on their physical and mechanical properties HPMC E5 and HPMC E15 were selected for the casting of the ziprasidone HCl loaded films. The films were evaluated for various physicochemical, mechanical and thermal properties such as drug loading efficiency, disintegration time, in vitro drug release characters, folding endurance, tensile strength etc. X-Ray diffraction studies, Differential scanning calorimetry, Fourier transform infrared spectroscopy and stability studies were performed for the optimized formulation in order to determine the stability of the formulation and the presence of drug excipient interactions Scanning electron microscopic studies were carried out to find the morphology and the texture of the film. Results: All the physical and mechanical properties of the films were in acceptable limits. The film F4 formulated with 20% w/v HPMC E5 showed good drug loading efficiency and 100% drug release in less than 6 min. X-Ray diffraction studies, Differential scanning calorimetry, Fourier transform infrared spectroscopy and stability studies of formulation F4 revealed the stability of the formulation. Scanning electron microscopic studies showed the morphology of the films suggesting that the films have uniform surface. Conclusion: Overall findings suggested that ziprasidone HCl oral soluble films of HPMC E5 exhibited a desired disintegration time ≤ 50 seconds, good drug loading efficiency and stability.

Formulation and Evaluation of Dispersible tablets of a Model Anti-Parasitic Drug

The study was aimed to formulate and evaluate dispersible tablets of a model anti-parasitic drug (XXX) with an objective to produce fast dispersion of tablets by reducing the disintegration time using three superdisintegrants like Sodium Starch Glycolate (SSG), Crospovidone (PVP K30) and Croscarmellose sodium (CCS) and also diluents namely MCC and Lactose by changing their concentrations in each formulations. Totally six formulations (F1-F6) were prepared by direct compression method and evaluated for hardness, thickness, weight variation, friability, wetting volume, wetting time, water absorption ratio, uniformity of dispersion, in-vitro disintegration time, Drug content, in-vitro dissolution test and release kinetics study. FTIR studies was carried out to see possible drug excipients interaction. The stability studies were performed as per ICH guidelines. Among the formulations F6 formulation was found to be promising as it showed better results than other five formulations with In-vitro disintegration time, percentage drug release and dispersion time of 16 ± 0.93 seconds, 98.32±0.54% and 66±1.30 seconds respectively. Further the FTIR results revealed that there was no interactionF between drug and excipients. Stability study of formulation showed no significant changes in tablet properties and the drug follows Higuchi release kinetics with Fickian diffusion mechanism.