Film Dosage Form Research Articles

Optimization of Mucoadhesive Buccal Film Dosage Form of Sodium Valproate using a Simplex Lattice Design Approach

The primary choice as an anticonvulsant for partial epilepsy, bipolar disorders (psychotic illnesses), and migraine medication is sodium valproate. Many dosage forms designed for the modified release of sodium valproic in tablets have disadvantages, including frequent use and increased toxicity. Therefore, it is necessary to design other dosage forms for the patient and maintain the therapeutic dose. The mucoadhesive buccal film was selected to overcome these problems. In the preparation of these films, this study used variations of chitosan and sodium carboxymethylcellulose (SCMC) as a carrier by solvent casting technique using the simplex lattice design approach. Several parameters characteristic, such as weight, film thickness, surface pH, swelling index, measurement of fold resistance, mucoadhesive residence time, uniformity of drug content and percentage of drug release, were selected as dependent variables. These results showed that the selected polymers influence the thickness, swelling index, and mucoadhesive residence time. The simplex lattice design analysis by the software design expert 10.0 showed the recommendation of optimum parameters desirability ratio of 0.64:0.36 for chitosan and SCMC in a film. The dissolution test was performed to determine the recommended release profile of mucoadhesive buccal film. According to Michaelis-Menten kinetics, the Kinet DS 3.0 software obtained a fitting model for the release profile.

Fabrication and Characterization of Orodispersible Composite Film from Hydroxypropylmethyl Cellulose-Crosslinked Carboxymethyl Rice Starch.

Crosslinked carboxymethyl rice starch (CLCMRS), prepared via dual modifications of native rice starch (NRS) with chloroacetic acid and sodium trimetaphosphate, was employed to facilitate the disintegration of hydroxypropylmethylcellulose (HPMC) orodispersible films (ODFs), with or without the addition of glycerol. Fabricated by using the solvent casting method, the composite films, with the HPMC--LCMRS ratios of 9:1, 7:1, 5:1 and 4:1, were then subjected to physicochemical and mechanical evaluations, including weight, thickness, moisture content and moisture absorption, swelling index, transparency, folding endurance, scanning electron microscopy, Fourier transform infrared spectroscopy, tensile strength, elongation at break, and Young’s modulus, as well as the determination of disintegration time by using the Petri dish method (PDM) and slide frame and bead method (SFM). The results showed that HPMC-CLCMRS composite films exhibited good film integrity, uniformity, and transparency with up to 20% CLCMRS incorporation (4:1 ratio). Non-plasticized composite films showed no significant changes in the average weight, thickness, density, folding endurance (96–122), tensile strength (2.01–2.13 MPa) and Young’s modulus (10.28–11.59 MPa) compared to HPMC film (135, 2.24 MPa, 10.67 MPa, respectively). On the other hand, the moisture content and moisture absorption were slightly higher, whereas the elongation at break (EAB; 4.31–5.09%) and the transparency (4.73–6.18) were slightly lowered from that of the HPMC film (6.03% and 7.03%, respectively). With the addition of glycerol as a plasticizer, the average weight and film thickness increased, and the density decreased. The folding endurance was improved (to >300), while the transparency remained in the acceptable range. Although the tensile strength of most composite films decreased (0.66–1.75 MPa), they all exhibited improved flexibility (EAB 7.27–11.07%) while retaining structural integrity. The disintegration times of most composite films (PDM 109–331, SFM 70–214 s) were lower than those of HPMC film (PDM 345, SFM 229 s). In conclusion, the incorporation of CLCMRS significantly improved the disintegration time of the composite films whereas it did not affect or only slightly affected the physicochemical and mechanical characteristics of the films. The 5:1 and 4:1 HPMC:CLCMRS composite films, in particular, showed promising potential application as a film base for the manufacturing of orodispersible film dosage forms.

Dr. Preparation of Metoclopramide-loaded Film Dosage Forms using Natural Polysaccharides

Natural polysaccharides are used as pharmaceutical or food ingredients. In this study, film dosage forms (FDs) containing the model drug metoclopramide (MCP) were prepared using sodium alginate or pectin as the film base, and the preparations were modified using additives such as chitin. The dissolution profiles of MCP from the FDs in a small volume of physiological saline were investigated. All the forms immediately swelled, disintegrated in physiological saline, and were transformed into a gelatinous substance. When the FD was prepared using sodium alginate, MCP incorporated in the form gradually dissolved into the test solution. In contrast, the drug immediately dissolved if the FD was prepared with pectin. The MCP dissolution rate can be controlled by modification of the film base with suitable additives. These results suggest that FDs prepared using these water-soluble polysaccharides can be useful for administering medicines to persons that have difficulty swallowing.

A Review on Current COVID-19 Vaccines and Evaluation of Particulate Vaccine Delivery Systems.

First detected in Wuhan, China, a highly contagious coronavirus, severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), also known as COVID-19, spread globally in December of 2019. As of 19 September 2021, approximately 4.5 million people have died globally, and 215 million active cases have been reported. To date, six vaccines have been developed and approved for human use. However, current production and supply capabilities are unable to meet global demands to immunize the entire world population. Only a few countries have been able to successfully vaccinate many of their residents. Therefore, an alternative vaccine that can be prepared in an easy and cost-effective manner is urgently needed. A vaccine that could be prepared in this manner, as well as can be preserved and transported at room temperature, would be of great benefit to public health. It is possible to develop such an alternative vaccine by using nano- or microparticle platforms. These platforms address most of the existing vaccine limitations as they are stable at room temperature, are inexpensive to produce and distribute, can be administered orally, and do not require cold chain storage for transportation or preservation. Particulate vaccines can be administered as either oral solutions or in sublingual or buccal film dosage forms. Besides improved patient compliance, the major advantage of oral, sublingual, and buccal routes of administration is that they can elicit mucosal immunity. Mucosal immunity, along with systemic immunity, can be a strong defense against SARS-CoV-2 as the virus enters the system through inhalation or saliva. This review discusses the possibility to produce a particulate COVID vaccine by using nano- or microparticles as platforms for oral administration or in sublingual or buccal film dosage forms in order to accelerate global vaccination.

Formulation, Optimization and Evaluation of Nanoparticulate Oral Fast Dissolving Film Dosage Form of Nitrendipine

The primary objective of the present research work was to develop nanoparticles incorporating (nanoparticulate) fast dissolving (orodispersible) film evincing enhanced solubility and bioavailability of nitrendipine (NIT). An antisolvent sonoprecipitation method was employed to produce the NIT nanosuspension (NS), which was optimized using the 32 optimal response surface design and then the optimized one was evaluated for various parameters (Gandhi et al., AAPS PharmSciTech 22 (1):1-15, 2021). The NIT nanoparticulate orodispersible film (N-ODF) was prepared utilizing the nanosuspension by the solvent casting method using the Vijay film-forming instrument. The N-ODF was optimized by the 23 full factorial design and was evaluated for several parameters. The optimized NS depicted a particle size of 505.74 ± 15.48 nm with a polydispersity index (PDI) of 0.083 ± 0.006 (Fig. 1b). The NIT nanoparticles showed a striking increment in saturation solubility (26.14 times), when compared with plain NIT (2). The developed NIT N-ODF exhibited thickness (0.148 ± 0.008 mm), folding endurance (280.33 ± 5.51 times), surface pH (6.86 ± 0.05), tensile strength (8.25 ± 0.13 kg/cm2), % elongation (63.5 ± 1.97%), and disintegration time (24.60 ± 1.31 s) to be within the standard intended limit. The in vitro dissolution study unveiled 100.28 ± 2.64% and 100.68 ± 2.50% of NIT release from lyophilized nanocrystals (in 8 min) and N-ODF (in 3.5 min), respectively, whereas the conventional NIT tablet took 30 min to release 99.94 ± 1.57% of NIT (Gandhi et al., AAPS PharmSciTech 22 (1):1-15, 2021). The in vivo pharmacokinetic study in rabbits inferred the achievement of significantly (p < 0.05) higher bioavailability of NIT on release from N-ODF in comparison to the conventional NIT tablet. Thus, the generation of N-ODF can be considered as a propitious move toward improving the efficacy of NIT to treat hypertension and angina pectoris.

Effect of Eudragit® NE 40D on The Properties of Pectin Film-Based Polymer Blends

In this work, pectin was used as the primary polymer component while Eudragit® NE 40D was used as polymer blending for the preparation of the thin films. Glycerin was used as a plasticizer. The samples were prepared by a solvent casting method, and their thickness, physicomechanical properties, and moisture ability were characterized. The ratio of Eudragit® NE 40D to pectin was varied to obtain films with tunable mechanical properties and moisture ability. The appearance of the pectin-based blended films was yellowish and transparent by visual observation, and the thicknesses of the pectin-based blended films were in the range of 102–138 µm. The mechanical property of softness of the pectin-based blended films was measured after blending with Eudragit® NE 40D. Thermal stability of pectin-based blended film was also dependent on the amount of Eudragit® NE 40D added; a broadly endothermic and exothermic transition peak were observed. The amorphous state was found in the pectin-based blended films. The cross-sectional morphology of the pectin-based blended films showed a homogeneous film without pores, cracks, or cavities. The moisture content and moisture uptake of the pectin-based blended films were in the range of 18.89–27.52% and 3.38–6.00%, respectively. Overall, the pectin-based blended films showed good properties and these results indicate that pectin-based blended films can potentially be used to prepare thin films for medical and pharmaceutical applications, including drug delivery film dosage forms.

Development, Evaluation, and Pharmacokinetic Assessment of Polymeric Microarray Patches for Transdermal Delivery of Vancomycin Hydrochloride.

Methicillin-resistant Staphylococcus aureus (MRSA) can cause harmful and potentially deadly infections. Vancomycin remains the first-line antibiotic treatment for MRSA-derived infections. Nevertheless, as a peptide drug, it is poorly absorbed when administered orally because of its high molecular weight and low permeability in the gastrointestinal tract and is therefore administered intravenously for the treatment of systemic diseases. In order to circumvent some of the many drawbacks associated with intravenous injection, other routes of drug delivery should be investigated. One of the strategies which has been employed to enhance transdermal drug delivery is based on microarray patches (MAPs). This work, for the first time, describes successful transdermal delivery of vancomycin hydrochloride (VCL) using dissolving MAPs (DMAPs) and hydrogel-forming MAPs (HFMAPs). VCL was formulated into DMAPs and reservoirs [film dosage forms, lyophilized wafers, and compressed tablets (CSTs)] using excipients such as poly(vinyl pyrrolidone), poly(vinyl alcohol), sodium hyaluronate, d-sorbitol, and glycerol. In this study, HFMAPs were manufactured using aqueous blends containing poly(methylvinyl ether-co-maleic acid) cross-linked by esterification with poly(ethylene glycol). The VCL-loaded CSTs (60% w/w VCL) were the most promising reservoirs to be integrated with HFMAPs based on the physicochemical evaluations performed. Both HFMAPs and DMAPs successfully delivered VCL in ex vivo studies with the percentage of drug that permeated across the neonatal porcine skin recorded at 46.39 ± 8.04 and 7.99 ± 0.98%, respectively. In in vivo studies, the area under the plasma concentration time curve from time zero to infinity (AUC0-∞) values of 162.04 ± 61.84 and 61.01 ± 28.50 μg h/mL were achieved following the application of HFMAPs and DMAPs, respectively. In comparison, the AUC0-∞ of HFMAPs was significantly greater than that of the oral administration control group, which showed an AUC0-∞ of 30.50 ± 9.18 μg h/mL (p < 0.05). This work demonstrates that transdermal delivery of VCL is feasible using DMAPs and HFMAPs and could prove effective in the treatment of infectious diseases caused by MRSA, such as skin and soft tissue infections, lymphatic-related infections, and neonatal sepsis.

Simultaneous Spectrophotometric Determination of Trigonelline, Diosgenin and Nicotinic Acid in Dosage Forms Prepared from Fenugreek Seed Extract.

Mathematical algorithms offer a useful method for quantitative analysis of compounds in multi-component mixtures to overcome the overlapping problems occurred in UV spectrophotometry. The aim of this study is to develop a method for simultaneous determination of bioactive compounds in herbal dosage forms produced from fenugreek extract. A UV- spectrophotometric method based on mathematical algorithm was used to simultaneous determination of trigonelline (TRG), diosgenin (DI), and nicotinic acid (NA). The maximum absorbance (λmax) was determined to be 232.65 nm, 296.23 nm, and 262.60 nm for TRG, DI, and NA, respectively. The calibration curves showed good linearity for all analytes in the concentration range of 1–20 μg/mL (R2=0.9995, 0.9997, 0.9994 for TRG, DI and NA, respectively). The Intra- and inter-day precisions were in the range of 1.1-10.7% and 1.2-8.2%, respectively. The accuracy of the method was 96.0% for TRG, 92.9% for DI, and 104.2% for NA. The limits of detection (LOD) and quantification (LOQ) were found to be 0.91 and 3.06 µg/mL for TRG, 0.99, and 3.30 µg/mL for DI and 0.33 and 1.10 µg/mL for NA. The validated method was applied for determination of the analytes in the tablet, capsule and thin film dosage forms prepared from the fenugreek seed extract. The mean recovery percentages of the analytes were in the range of 90.0-97.4%, 85.6-105.4%, and 90.0-99.0% for tablet, capsule, and film dosage forms, respectively. Generally, the validated method could be a good candidate for routine spectrophotometric determination of the analytes without any necessity for pre-analysis extraction.

In-Vivo evaluation of implantable film containing Microencapsulated Sustained Releas Dexamethasone Sodium Phosphate

Objective: This work involved in vivo evaluation of the previously prepared implantable film dosage form containing microencapsulated dexamethasone sodium phosphate (which is equivalent to 16 mg dexamethasone) and 4.4 mg pure dexamethasone sodium phosphate (which is equivalent to 4 mg dexamethasone) to be inserted at the inflamed areas to get suitable precise controlled release. Methods: the animals used were 33 rates divided into 8 groups and the inflammation was induced by using 2.0% carrageenan solution to be injected intra-dorsally then the film was inserted locally and then sacrifying the animals on different time tables to take sample from the site of inflammation for 5 months and examined under electron microscope. Results: the results showed that the prepared implantable film had immediate anti-inflammatory effect upon insertion at the inflamed tissue and its action continued effectively for five months. Conclusion: this work proved that implantable film containing dexamethasone should be used after surgery of joint replacement or any other surgery site as alternative to the applied regimen of giving IM injection of the commercially available 10mg dexamethasone intraoperatively and a second 10 mg within 24-hour postoperatively to reduce edema and pain followed by oral dexamethasone 0.5 mg on daily based till complete recovery which may last for 5 months or more and subject the patients to the serious systemic effects. The application of the implanted film therapy may reduce the rejection of the body to the replaced joint or other replacement surgery and improves patient compliance.

In-Vivo evaluation of implantable film containing Microencapsulated Sustained Releas Dexamethasone Sodium Phosphate

Objective: This work involved in vivo evaluation of the previously prepared implantable film dosage form containing microencapsulated dexamethasone sodium phosphate (which is equivalent to 16 mg dexamethasone) and 4.4 mg pure dexamethasone sodium phosphate (which is equivalent to 4 mg dexamethasone) to be inserted at the inflamed areas to get suitable precise controlled release. Methods: the animals used were 33 rates divided into 8 groups and the inflammation was induced by using 2.0% carrageenan solution to be injected intra-dorsally then the film was inserted locally and then sacrifying the animals on different time tables to take sample from the site of inflammation for 5 months and examined under electron microscope. Results: the results showed that the prepared implantable film had immediate anti-inflammatory effect upon insertion at the inflamed tissue and its action continued effectively for five months. Conclusion: this work proved that implantable film containing dexamethasone should be used after surgery of joint replacement or any other surgery site as alternative to the applied regimen of giving IM injection of the commercially available 10mg dexamethasone intraoperatively and a second 10 mg within 24-hour postoperatively to reduce edema and pain followed by oral dexamethasone 0.5 mg on daily based till complete recovery which may last for 5 months or more and subject the patients to the serious systemic effects. The application of the implanted film therapy may reduce the rejection of the body to the replaced joint or other replacement surgery and improves patient compliance.

3D printing of multilayered orodispersible films with in-process drying

The aim of this study was to prepare benzydamine hydrochloride loaded orodispersible films using modified semisolid extrusion 3D printing method. An innovative approach was developed where thin layer of drug loaded dispersion is printed and dried before printing of subsequent layers. Layer-by-layer drying as the in process step improves mechanical properties of films, uniformity of drug content and allows faster preparation of films in compounding settings due to shortening of drying time. Orodispersible films consisted of film forming maltodextrin, sorbitol as a plasticizer and hydroxyethylcellulose as a thickening agent. The height of the digital model showed excellent correlation with the disintegration time, weight, thickness and mechanical properties of prepared films. Drug content, predefined by volume of digital model and concentration of drug in print dispersion, showed excellent uniformity. The modified printing method shows great promise in a compounding production of personalized film dosage forms, and brings in possibilities such as one step preparation of films with compartmented drugs and incorporation of taste masking or release control layers.

A Novel Formulation Strategy to Deliver Combined DNA and VLP Based HPV Vaccine.

Human papillomaviruses (HPV) are small, double-stranded DNA viruses that cause cervical cancer, the second most lethal cancer among women in the world. Currently, two vaccines are on the market for preventing HPV-caused cervical cancers and warts. Both are virus-like particle (VLP)-based vaccines. However, these vaccines have limitations; they are costly, have an invasive route of administration, require trained personnel to administer, need cold chain storage to preserve them, and most of all, they are preventive vaccines that do not have curative effects. Therefore, it is necessary to develop therapeutic HPV vaccines to facilitate the control of HPV-associated malignancies and to address all these issues. Recently there are DNA vaccines under investigation to prevent HPV. In general, DNA-based vaccines are better than or an excellent alternative to traditional vaccines since they can closely mimic live infections and can induce both antibody and cell-mediated immune responses. DNA vaccines involve the delivery of plasmid DNA (pDNA) which encodes the specific antigens. DNA vaccines have potential to be effective therapeutic tools against HPV infections. Combining the VLP-based and DNA-based vaccines can be highly effective as they can complement each other. VLP vaccines are more prone to mucosal immunity whereas DNA vaccines are more towards systemic immunity. In this article, we discuss an optimal formulation that will contain both type of vaccines, preventive and therapeutic. A film dosage form can be a good option which can be administered in buccal or sublingual routes for systemic action or in the vaginal area for local action to treat cervical cancer and to protect from future infection. Multiple vaccines in native form or in particulate form can be incorporated in film dosage forms. The film dosage form of vaccines can elicit both antibody-mediated (preventative) and cell-mediated (therapeutic) mechanisms. Film dosage forms are feasible to prepare for vaccine administration in the mouth cavity, GI tract, and vagina.

Preparation, Characterization and Prevention of Auto-oxidation of Amorphous Sirolimus by Encapsulation in Polymeric Films Using Hot Melt Extrusion.

Sirolimus (SIR) is a macrocyclic lactone antibiotic and used therapeutically as a potent immunosuppressant for prophylaxis of kidney transplant rejection. The development of an oral dosage form is challenging because of very poor aqueous solubility (2.6µg/ml). The oral bioavailability of SIR is only 15-20 % and is affected by food and other drugs. The main reasons for low bioavailability are intestinal degradation by enzymes especially by cytochrome P4503A4, efflux by P-glycoprotein and hepatic first-pass metabolism. The main objective was to prepare a mouth dissolving film dosage form of amorphous SIR to improve dissolution. Crystalline SIR was transformed to its form amorphous by milling for 2 h at room temperature. Thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) were used for characterisation. The stability of amorphous SIR was studied at 4°C and 40°C/75% RH. Amorphous SIR was formulated as oral films by melt extrusion with polyvinylpyrrolidone- vinyl acetate (PVP-VA), Soluplus® and hydroxypropyl cellulose (HPC) as carriers. The films were characterized for drug content, physical state, dissolution profile and stability at 4°C and 40°C/75% RH. The PRXD and DSC confirmed the conversion of crystalline SIR to amorphous form by milling. The solubility of amorphous SIR was several folds higher than its crystalline form, but amorphous SIR was highly unstable at all tested temperatures (4° and 40°C). The extruded films exhibited higher dissolution and stability compared to milled SIR powder alone, but the process of extrusion had some detrimental effect on the chemical stability of amorphous SIR. The film formulations showed a significant improvement in the storage stability of the amorphous form of SIR and the solubility advantage of the amorphous form was evident in the dissolution testing. The oral films can potentially improve the bioavailability of SIR by absorption through the buccal mucosa.

Overview and Future Potential of Fast Dissolving Buccal Films as Drug Delivery System for Vaccines.

Vaccination is considered one of the most successful public health interventions of the modern era. Vaccines are categorized based on the antigen used, delivery system and the route of administration. Traditional vaccines are produced from the dead, attenuated or inactivated pathogens that cause disease. However, newly developed vaccines are DNA based, liposome based, and virus like particle (VLP) based which are more effective and specific to some malignant diseases. The delivery system of vaccines has been advanced along with time as well. New delivery systems such as nanoparticles, liposomes, or cells (for DNA) has been proven to develop a more efficient vaccine. Most vaccines are administered via intramuscular (IM), subcutaneous (SQ) or oral (PO) route. However, these routes of administration have limitations and side effects. An alternative route could be oral cavity administration such as buccal or sublingual administration using film dosage form as delivery vehicle. In this article, we thoroughly reviewed the possibility of developing a quickly soluble film-based delivery system for vaccine administration. We reviewed the different types of new vaccines and vaccine formulations such as VLP based, liposome, bilosome, particulate, and summarized their suitability for use in a film dosage form. Quickly soluble film dosage form is the most optimized form of buccal administration. A film dosage form applied in the buccal cavity has several advantages: they can avoid first pass effect, they are easy to administer and prepare, and they are more cost effective. Since there is no first pass effect, only a small quantity of the vaccine is needed. Vaccines in their original form or in a nano or microparticulate form can be used in a film. The film can also be developed in multilayers to protect the vaccine from degradation by saliva or swallowing. Films are easy to prepare, administer, and can be used for systemic and local action. In addition, most of the current vaccines use mostly the parenteral route of administration, which has some major drawbacks such as poor induction of mucosal immunity, less patient compliant, less potent, high cost and cumbersome production process. Sublingual and buccal vaccine delivery can be good alternatives as they are easier to prepare and safer than parenteral administration routes. The buccal and sublingual administration have the advantage to produce both systemic and mucosal immunity.

STUDIES ON EFFECT OF FORMULATION AND PROCESSING PARAMETERS ON STABILITY OF KETOROLAC TROMETHAMINE ORALLY DISSOLVING FILMS

Objective: The objective of the proposed work was to study the effect of various formulation and process parameters of solvent casting method on the physical and chemical stability of Ketorolac Tromethamine (KT) in the orally dissolving film dosage form.&#x0D; Methods: KT-excipient interaction study was carried out both in solid state and by processing samples through the solvent casting technique. The samples were evaluated using IR spectroscopy (IR) and X-ray diffractometry (XRD). Solvent casting method was used to prepare KT films using different film-forming polymers, and solvents. The drying temperature and pH of the dispersion were also varied to study the effect of these parameters on the stability of KT. All the formulations were analysed chemically initially and after one month of storage at 40 °C/75% RH.&#x0D; Results: During KT-excipient interaction study in solid state KT was found to be stable. No significant changes were observed in its impurity profile. Interaction between different polymers and KT was observed after the solvent casting process as revealed by IR and XRD analysis. The interaction was further confirmed in the film formulations upon chemical analysis. The polymers showing interaction with KT in XRD and IR were making it unstable chemically and were responsible for its chemical degradation as revealed by chemical analysis. It was also revealed that KT is most stable when processed using water as the solvent. KT was found to be stable when processed at a higher temperature and at acidic pH during film formation. It was found that chemical stability is more when Polyethylene oxide (PEO) and water under acidic pH are used and films are dried at a higher temperature.&#x0D; Conclusion: Both formulation parameters and processing conditions of the solvent casting technique affects the stability of drugs and hence should be studied as part of pre-formulation studies while developing orally dissolving films of drugs.

FORMULATION AND EVALUATION OF SUBLINGUAL FILMS OF APIXABAN

The concept of sublingual film dosage form has become popular as new delivery system. This system will provide maximum therapeutic efficacy, increased bioavailability and maximum stability by reducing the frequency of dosage. It will also avoid first pass metabolism of the drugs. This system provides more rapid drug absorption from the pre gastric area which may provide quick onset of action. The present research aimed to prepare sublingual films of apixaban reduces the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. The film was prepared using solvent casting method and optimized employing 32 factorial design considering two independent variables film forming polymer (HPMC E5) and PEG 400. Disintegration time, drug release and folding endurance were taken as dependent variables. The prepared optimized formulation showed minimum disintegration time (35 s), highest dissolution rate (99 %) and satisfactory physicochemical properties. It is evident from the above results that the developed formulation can be an innovative dosage form to improve the drug delivery, onset of action as well as improve patient compliance.&#x0D; Key Words: Apixaban, Sublingual films, HPMC

Drug Release Profiles and Disintegration Properties of Pectin Films.

We assessed the disintegration profiles of the film dosage forms (FDs) prepared using pectin by measuring the amount of pectin dissolved from the films in a limited amount of aqueous medium. Furthermore, we used miconazole and dexamethasone as standard drugs and investigated the relationship between the disintegration rate of the FDs and the rate of drug release. We used two types of pectin in this study to develop thin films with a thickness of approximately 25–35 μm. The FDs gradually disintegrated in the aqueous medium, and the disintegration profile of the FDs differed depending on the types of pectin. In addition, the rate of disintegration of the film matrix affected the dissolution rate of the drug incorporated into the FD. Thus, our results show that FDs prepared using pectin are beneficial because of their high solubility in a limited amount of medium, and the rate of drug release from the FDs can be regulated by selecting a specific type of pectin or by altering the concentration of the film base.

Formulation and development of vaginal films of poorly water soluble drug, metronidazole, using mixed solvency concept and their evaluations

Aim: To deliver antibacterial therapy in an efficacious way, film dosage form has been proposed for drug delivery in vagina which can overcome bioavailability issues of poorly water soluble drugs. The present research work is aimed to explore the application of mixed solvency concept to increase solubility of poorly water soluble drug, metronidazole. Materials and Methods: Metronidazole, a slightly soluble drug in water was tried to be solubilized by employing the combination of solubilizers like niacinamide, sodium benzoate, sodium caprylate, caffeine and urea to endeavour its fast dissolving film formulations. The procured sample of drug was characterized by UV, IR and DSC studies. The formulations were evaluated for various properties of film such as thickness, folding endurance, surface pH, disintegration time and thin layer chromatography. Stability studies of vaginal films of metronidazole were performed for ten weeks at room temperature, and refrigerated conditions. Results and Discussion: It was found that 97.54% and 97.58% of drug was remaining after stability study at respective temperatures in batch F1 and 98.53% and 96.57% in batch F4.Conclusion: It was concluded that the approach of mixed solvency concept is novel, safe, cost-effective and user friendly. It also eliminates the problem of toxicity associated with high concentration of water-soluble solubilizers. So, it may be employed in dosage form development of drugs with poor solubility to overcome bioavailability issues.&#x0D; Keywords: Solubility, metronidazole, vaginal films, mixed solvency concept.

HPLC Method Development for Estimation of Dissolution of Antipsychotic Drug as Sublingual Film Dosage Form

HPLC Method Development for Estimation of Dissolution of Antipsychotic Drug as Sublingual Film Dosage Form

ATR-FTIR spectroscopic imaging to study the drying and dissolution of pharmaceutical polymer-based films

Pharmaceutical film dosage forms have recently become of interest to pharmaceutical formulation development, particularly for patients who experience difficulty in swallowing tablets or capsules. Furthermore, formulation scientists require a reliable analytical approach to reveal vital insight and investigate the drying process of these films to consolidate suitable quality control.Since most of the polymer-based films containing a drug are produced via solution or dispersion states, an estimation of the physicochemical properties of drugs during drying and dissolution is critical to design novel formulations with the consideration to control drug release, i.e. safety and efficacy to patients. This work presents the novel application of attenuated total reflection–Fourier transform infrared (ATR–FTIR) spectroscopic imaging to study the drying process and dissolution behaviour of polymer-based films. Two types of the ibuprofen containing films, hydroxypropyl methylcellusose (HPMC) based films for immediate release and polyvinylpyrrolidone (PVP) based films for extended release, were studied in modified pH environments and changing hydrophobicity. ATR-FTIR imaging has revealed important information on water ingress into the films and the presence, distribution, and physicochemical state of the drug. ATR-FTIR imaging is a powerful technique to investigate and to deeply understand physicochemical processes for pharmaceutical polymer-based films.