Formulation of Bilayer Benzydamine HCl Patch Targeted For Gingivitis

Once daily sustained release tablets of venlafaxine, a novel antidepressant

Objective: The purpose of this study was to design and formulate mucoadhesive buccal patches of sodium cromoglycate (SCG) as an alternative way to overcome its poor oral absorption and short half-life.Methods: Mucoadhesive patches were prepared by solvent casting technique using cellulose acetate butyrate (CAB) alone or in combination with mucoadhesive polymers like SCMC (sodium carboxymethyl cellulose), HPMC 100M (hydroxyl propyl methyl cellulose) and Cbp934P (carbopol) in different concentrations. The successful patches were evaluated for thickness, weight variation, folding endurance, tensile strength, drug content, surface pH, moisture uptake, swelling percentage, mucoadhesion strength, residence time, in vitro release study, ex vivo permeation and in vivo pharmacokinetic studies.Results: The thickness of all prepared patches ranged from 0.210±0.006 to0.355±0.012, folding endurance was more than 300, weight variation did not exceed 0.179±0.015, tensile strength and % elongation ranged from 6.4±0.018 to 13.1±0.024, and from 30.4±0.88 to 53.4±0.78respectively. The swelling percentage after one hour was from 20.8±0.99 to 53.2±1.5. pH of all prepared patches did not exceed 6.8, the drug content was about 99 to 101%, moisture uptake did not exceed 10%. Mucoadhesion strength and residence time ranged from 17.2±0.14 to 51.2±0.26, and from 3.35±0.25 to 7.45±0.28 respectively. The cumulative release percentage of SCG was in the following descending order CAB>CAB with Cbp934P>CAB with HPMC>CAB with SCMC. The optimized patch (F9) decreased the Cmax and increased Tmax compared to the parenteral solution.Conclusion: It can be concluded that mucoadhesive buccal patch is a promising dosage form to prolong the release of SCG and enhance its poor oral bioavailability.

Objectives: The objective of this study is to extract Phytochemical constituent from Cinnamon Bark and to design and develop the transdermal patch of the herbal drug along with modern medicine Glibenclamide using solvent casting method to reduce the dose required to obtain same pharmacological the effect, also to reduce the toxicity of the drug. Methods: The Glibenclamide Transdermal patches were formulated by using the solvent casting method. The physical and chemical similarity of the medication and the base of patches were studied by Infrared Spectroscopy (FTIR). The outcomes recommended no physical and chemical properties incongruence between the medication and the patch base. The formulated transdermal patches were assessed for the weight difference, fatness, folding endurance, wetness, moisture captivation, ex vivo drug release, ex vivo drug absorption. Results: The diffusion examines were performed by utilizing the Franz diffusion cell and everted gut sac method. The best formulation F5 showed Thickness 0.230±0.009mm, Weight uniformity 0.170±0.021gm, % Moisture uptake 8.307±1.00 Moisture content 5.045±0.214, % Drug content 80.80±0.091, Folding endurance27±4.50. Formulation F5 exhibits the highest % cumulative drug release 67.90±1.01% in 8hrs and highest %Drug absorbed 4.263±0.41 in 120 min. Conclusion: It can be concluded the formulation no. F5 shows maximum bioenhancing action compared to all other patches which contains Glibenclamide along with the Ethanolic extract of the Cinnamon bark.

The topical route for local anaesthesia including ointments and creams can be easily washed off by wetting agents or with contact or movement. The goal and objective of the present study was to develop and formulate a transdermal patch for local anaesthesia. These patches were formulated by solvent casting method by the use of Hydroxypropyl Methylcellulose (HPMC) polymer, different enhancers, and vasoconstrictor which is the key ingredient for enhancing aesthetic activity. Formulated patches were evaluated for the physical and physicochemical parameters like moisture content, moisture uptake, folding endurance, water vapour permeability, drug content, and drug release, and in vivo study was done on rats. Amongst all the formulations, F7 was considered the ideal formulation which is the combination of HPMC polymer, polyoxyethylene 2-oleyl ether as an enhancer, and vasoconstrictor Tetrahydrozoline. For in vivo testing Tail flick method was applied and the effect of anaesthesia was maximum as compared to other formulations. In comparison to the control formulation, there was a 2.34-fold increase in aesthetic activity. When compared to the control formulation, the F7 formulation exhibited improved and longer efficacy. A transdermal bupivacaine patch incorporating a penetration enhancer and a vasoconstrictor could be created to improve the local cosmetic effects of bupivacaine.

INTRODUCTION Fast disintegrating/dissolving medicine delivery devices are oral films that swiftly disintegrate or adhere in the mouth. It includes the ability to administer systemic medications without having any first-pass effects. A first-generation antihistamine from the phenothiazine family is promethazine HCl. It is effective in treating motion sickness but it has a poor oral bioavailability. The study aims is to formulate promethazine fast dissolving oral film using natural and synthetic polymers and compare the formulations. MATERIAL AND METHODS This experimental study was conducted in the Pharmaceutic laboratory of Department of Pharmacy at Universal College of Medical Sciences, Bhairahawa, Nepal from February 2022 to July 2022. Fast dissolving oral films of promethazine were prepared by solvent casting method using polymers and plasticizers in varying concentrations. Weight variation, thickness variation, surface pH, folding endurance, swelling index, disintegration duration, dissolution study and medication content were among the several in vitro assessment criteria that were identified. RESULTS When examined for physical characteristics, thickness, weight uniformity, in vitro disintegration time, folding durability, drug content, and an in vitro drug release, films were determined to be adequate. The films of the F2 formulation demonstrated an increased rate of drug dissolution with a drug content of 99.17%, a disintegration time of 38 sec, and a drug release of more than 99% within 16 min. CONCLUSION Synthetic polymer (Hydroxypropyl methyl cellulose) showed better result in comparison to natural polymer (Sodium alginate).

In the present investigation, effort has been made to stabilize optimized nanosuspension of flurbiprofen through oral thin film formulation. To overcome the issue of stability of nanosuspension and poor bioavailability of flurbiprofen, nanosuspension loaded oral thin films were developed by solvent casting method. Oral thin films can be prepared by simple and scalable method easily. Nanosuspension loaded oral thin films were evaluated for thickness, % moisture absorption and loss, surface pH, weight variation, folding endurance, drug content, disintegration time, in vitro drug release and stability. The resultant oral thin films depicted that the particles size range was retained even after their stability study for three months. The dissolution rate of all flurbiprofen oral thin films were significantly increased compared with its marketed oral formulation. Thus it can be concluded that, oral thin films have potential for stabilization of nanosuspension with improved drug release.

The present study focuses on the formulation and evaluation of oxyphenbutazone-loaded transdermal patches intended to provide sustained drug delivery and enhance patient compliance. Oxyphenbutazone, a non-steroidal anti-inflammatory drug (NSAID), is associated with gastrointestinal side effects when administered orally; hence, transdermal delivery offers a promising alternative. The patches were prepared using the solvent casting technique with various polymers such as HPMC, PVA and SCMC in different ratios. The formulated patches were evaluated for physicochemical parameters including thickness, weight variation, folding endurance, surface pH, moisture content, moisture uptake, drug content, and in vitro drug release. Among the formulations, the optimized patch exhibited desirable properties and sustained drug release for up to 12 hours. The drug release kinetics followed controlled release behavior, indicating the potential of the developed patch as an effective transdermal drug delivery system for oxyphenbutazone. This approach may reduce the frequency of dosing and minimize systemic side effects, thereby improving overall therapeutic outcomes

Amoebiasis is an infection of the large intestine caused by Entamoeba histolytica. Tinidazole is the preferred drug used in the treatment of intestinal amoebiasis. The conventional tablet dosage form provides minimal amount of drug in the colon with undesirable adverse effect due to variation in the transit time. Hence, to target the drug directly to the site of action in the colon, there is need to develop colon targeted drug delivery systems that will enhance the therapeutic drug level, increases the bioavailability of active medicament and reduce the dose of drug. The fast disintegrating core tablet of Tinidazole was prepared by direct compression method. The core tablet was evaluated for hardness, thickness, Friability, weight variation, drug content, in vitro disintegration time and in vitro drug release studies. Using the optimized formulation (C3), different formulations (F1-F6) of coated tablet was prepared by using different polymers like chitosan and xanthan gum. The formulated coated tablet were evaluated for various parameters like for hardness, thickness, Friability, weight variation, drug content, swelling study and in vitro dissolution study. The optimized formulation F3 shows 6.24% drug release in Stomach and Small Intestine and maximum drug release up to 96.53% in the colon. The kinetic data analysis of formulations indicated that it fits to Korsmeyer -Peppas Model and follows zero order release kinetics. The mechanism of drug release from the tablet followed non-Fickian (super case-11) transport. The stability studies of the optimized formulation were investigated as per ICH guidelines. There were no significant changes in thickness, hardness, weight variation, friability, drug content and in vitro drug release. These findings suggest that compression coated tablet using polysaccharide carriers provide more site specific delivery, reduced degradation and release of drug in stomach and small intestine.

Metformin HCl microspheres were prepared with the aim of increasing its bioavailability and decreasing gastrointestinal side effects by means of sustained action. Eudragit RSPO and Eudragit RLPO, polymers of different permeability characteristics were used to prepare different microspheres. Emulsification solvent evaporation technique using acetone as the internal phase and liquid paraffin as the external phase was the method of choice. Six formulations were prepared using two polymers. The effect of drug loading and polymeric property on the surface morphology, entrapment efficiency, particle size and release characteristics of the microspheres were examined. FTIR and DSC studies established compatibility of the drug with the polymers. SEM studies clearly revealed the effect of drug loading and polymeric nature on the surface morphology of the microspheres. Entrapment efficiencies were within 77.09-97.11% and particle size of all the batches were in the acceptable range. Release data were treated with different mathematical kinetic models. The drug release profile showed that Eudragit RSPO and Eudragit RLPO have opposite effect on drug release. On the other hand, increase in drug loading results in increased drug release. Kinetic modeling of in vitro dissolution profiles revealed that the drug release mechanism varies from diffusion controlled to anomalous type. Dhaka Univ. J. Pharm. Sci. 12(2): 131-141, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17611

Ondansetron hydrochloride, a 5 HT3 antagonist is a powerful antiemetic drug which has oral bioavailability of 60% due to hepatic first pass metabolism and has a short half-life of 5 h. To overcome the above draw back, the present study was carried out to formulate and evaluate fast dissolving films of ondansetron hydrochloride for sublingual administration. The films were prepared from polymers such as polyvinylalcohol, polyvinyl pyrrolidone, Carbopol 934P in different ratios by solvent casting method. Propylene glycol or PEG 400 as plasticizers and mannitol or sodium saccharin as sweeteners were also included. The IR spectral studies showed no interaction between drug and polymer or with other additives. Satisfactory results were obtained when subjected to physico-chemical tests such as uniformity of weight, thickness, surface pH, folding endurance, uniformity of drug content, swelling index, bioadhesive strength, and tensile strength. Films were also subjected to in vitro drug release studies by using USP dissolution apparatus. Ex vivo drug permeation studies were carried out using porcine membrane model. In vitro release studies indicated 81–96% release within 7 min and 66–80% within 7 min during ex vivo studies. Drug permeation of 66–77% was observed through porcine mucosa within 40 min. Higher percentage of drug release was observed from films containing the sweeteners. The stability studies conducted for a period of 8 weeks showed no appreciable change in drug content, surface pH, and in vitro drug release.

–Betaxolol Hydrochloride is a cardio selective β1 adrenergic receptor blocking agent used in the treatment of chronic open angle glaucoma and ocular hypertension In the present study, an attempt was made to formulate Betaxolol HCl ocular inserts. In matrix type the formulations for Betaxolol containing 10%, 12%, and 14% w/v of Gelatin, 1%, 1.5%, 2%, 2.5% and 3% w/v for Chitosan were prepared by solvent casting method and plasticizer were used in different concentration for smoothing texture of the ocular inserts. The prepared batches of ocular inserts were evaluated for weight variation thickness, drug content uniformity, swelling index. An increase in average weight and thickness is due to increase in polymer concentration. IR spectral studies were performed to confirm the interaction of drug with excipients. All formulations were tested for in vitro drug release (Simulated tear fluid) by vial method. The formulations GH8 and C5 show a maximum cumulative percentage drug release of 98.76% and 97.72% at the end of 12 th hrs, respectively. The drug release in all formulations decreases as the polymer concentration increases. The dissolution data of formulation were subjected to first order, Higuchi’s, and peppas equations. Drug release from the ocuserts by diffusion controlled mechanism. No significant change in the drug content and physical features was observed during storage at 25 0 C/60% RH and 40 0 C/75% RH for the selected formulation for three months. Keywords––Betaxolol Hydrochloride, Chitosan, Gelatin, Ocular inserts.

Effect of hydrophilic polymer on solubility and taste masking of linezolid in multi-component cyclodextrin inclusion complex: Physicochemical characterization and molecular docking

Development and in vitro evaluation of a novel contraceptive vaginal mucoadhesive propranolol hydrochloride film

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers.
 Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin.
 Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability.
 Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

The present study aimed to improve solubility and prolong the release duration of a poorly soluble drug using a combination of two different types of formulations (solid dispersion and microspheres). The solid dispersions were prepared by fusion method using urea and mannitol as hydrophilic carriers. Microspheres were prepared by solvent evaporation method using Eudragit L-100 (EL100) and Eudragit RS PO (ERS) as rate-controlling polymers. Flurbiprofen (FBP)-urea (1:2) solid dispersion and microspheres of FBP-EL-100-ERS (1:0.25:0.75) were used for the development of controlled release formulation by mixing them in different proportions. The FBP-containing formulations were evaluated for percentage yield, drug content, morphology, in vitro release, and in vivo anti-inflammatory activity. The best selected formulation was further evaluated for the controlled and improved effects. SEM photomicrograph confirmed the spherical shape of microspheres and with particle size in the range of 73.5-85.4μm. In vitro release of FBP from controlled release formulations indicated that the formulation containing solid dispersion:microspheres (1:0.5) yielded prolonged effect up to 10h. The release kinetics followed zero-order, and the mechanism of drug release was found to be diffusion rate controlled. This formulation had shown better inhibition of edema of rat paw up to 16h and identified as a suitable product for controlled delivery of FBP. In conclusion, the concept of using a binary mixture of solid dispersion and microspheres can be used for other drugs that exhibit a poor solubility in stomach pH and a faster release in intestinal pH.