HPMC E5 Research Articles

Formulate and Evaluate, Fast Dissolving thin Film of Metoprolol Succinate

Objective: Metoprolol succinate, which is used to treat cardiovascular disorders, is a strong beta-1 adrenoreceptor blocker with cardio-selective effect but is heavily metabolised in the liver during the first pass. Our goal is to minimise hypertension by creating a film of metoprolol succinate that dissolves quickly.
 Methods: Metoprolol succinate films that dissolve in the mouth were made utilising a solvent casting technique. HPMC E5 was used as the film-forming agent, PEG400 was used as the plasticizer, and honey was included as the film-modifying agent in the final formulation. HPMC E15 (X1) and honey (X2) concentrations were used as independent variables, whereas disintegration time (DT), tensile strength (TS), and % cumulative drug release (CDR) were used as dependent variables in a 32-full factorial design. Thickness, folding endurance, tensile strength, disintegration time, and drug release were among the criteria used to assess the manufactured films. Results showed that HPMC E15 and honey both positively impacted DT and TS while negatively impacting CDR.
 Results: The optimum formulation was determined to be the one with a DT of 58.0 ±1.01 seconds, an in vitro drug release of 105.32± 1.55, and a tensile strength of 73.55 ± 1.37 g/cm2.
 Conclusion: Thus, employing a solvent casting method, a fast-dissolving thin film of Metoprolol succinate was created with effective taste masking and prompt in vitro drug release.
 Keywords: Metoprolol succinate, Fast dissolving oral film, HPMC E5, Honey, Solvent casting

Nano-suspension loaded mucoadhesive mouth dissolving film of meclizine hydrochloride

Meclizine Hydrochloride belongs to class H1 antagonist, antiemetic and anti-vertigo in nature, it is a Biopharmaceutical classification system (BCS) class II drug and is practically insoluble in water. The bottom-up approach was used in the formulation of nanosuspension in which methanol and millipore water was used as solvent and anti-solvent respectively, the stabilizers used for preparation were Polyvinylpyrrolidone K30 (PVP K30) and Hydroxypropyl Methylcellulose E15 (HPMC E15) which were found to be compatible with the formulation after Fourier Transform Infrared (FTIR) and Differential scanning calorimeter (DSC) studies. Mouth dissolving films were formulated by solvent casting method using glycerine lubricated petri dish and were kept for heating in a hot air oven at 45°C overnight. Characterization of nanosuspension-loaded mucoadhesive mouth dissolving films was done by evaluating various characteristics, the highest drug content was found to be 92.43±0.49% in Mouth dissolving film (MDF) 2. In-vitro drug release studies indicate that nanosuspension-loaded mucoadhesive mouth-dissolving film has a rapid drug release rate as compared to plain drug-loaded mouth-dissolving films and marketed tablet formulation.

IMPLEMENTING CENTRAL COMPOSITE DESIGN FOR THE DEVELOPMENT OF TACROLIMUS FILM FOR SUBLINGUAL ADMINISTRATION

Objective: The study aimed to develop fast-dissolving films (FDFs) of the immunosuppressant drug tacrolimus monohydrate for sublingual administration, employing central composite design (CCD), to improve its bioavailability. Methods: Tacrolimus: β-cyclodextrin inclusion complexes prepared earlier were formulated into FDFs. CCD was used for developing optimal film formulation with the desired characteristics. The solvent casting method was used for the preparation of films. For optimization, the independent variables selected were the concentration of hydroxy propyl methyl cellulose E5 (HPMC E5) (X1) and concentration of croscarmellose sodium (CCS) (X2) and the responses were disintegration time (Y1) and percentage drug release at 5 min (Y2). The suggested optimal films were subjected to further characterization. Results: All the formulations showed good mechanical properties. The composition of optimized FDF constituted 3.016% w/v of HPMC and 11.731%w/w of CCS and its average disintegration time was 27.28s and showed 83.13% mean drug release at 5 min. Differential Scanning calorimetry (DSC) analysis showed complete dispersion and partial conversion into the amorphous form of the drug, which was also confirmed by X-ray diffraction (XRD) studies. Scanning Electron Microscopy (SEM) revealed the smooth and porous nature of the film. Conclusion: The developed FDF may be used sublingually for delivering tacrolimus efficiently, avoiding its oral bioavailability problems.

Diosmin nanocrystal gel alleviates imiquimod-induced psoriasis in rats via modulating TLR7,8/NF-κB/micro RNA-31, AKT/mTOR/P70S6K milieu, and Tregs/Th17 balance

Diosmin is a flavonoid with promising anti-inflammatory and antioxidant properties. However, it has difficult physicochemical characteristics since its solubility demands a pH level of 12, which has an impact on the drug’s bioavailability. The aim of this work is the development and characterization of diosmin nanocrystals using anti-solvent precipitation technique to be used for topical treatment of psoriasis. Results revealed that diosmin nanocrystals stabilized with hydroxypropyl methylcellulose (HPMC E15) in ratio (diosmin:polymer; 1:1) reached the desired particle size (276.9 ± 16.49 nm); provided promising colloidal properties and possessed high drug release profile. Additionally, in-vivo assessment was carried out to evaluate and compare the activities of diosmin nanocrystal gel using three different doses and diosmin powder gel in alleviating imiquimod-induced psoriasis in rats and investigating their possible anti-inflammatory mechanisms. Herein, 125 mg of 5% imiquimod cream (IMQ) was applied topically for 5 consecutive days on the shaved backs of rats to induce psoriasis. Diosmin nanocrystal gel especially in the highest dose used offered the best anti-inflammatory effect. This was confirmed by causing the most statistically significant reduction in the psoriasis area severity index (PASI) score and the serum inflammatory cytokines levels. Furthermore, it was capable of maintaining the balance between T helper (Th17) and T regulatory (Treg) cells. Moreover, it tackled TLR7/8/NF-κB, miRNA-31, AKT/mTOR/P70S6K and elevated the TNFAIP3/A20 (a negative regulator of NF-κB) expression in psoriatic skin tissues. This highlights the role of diosmin nanocrystal gel in tackling imiquimod-induced psoriasis in rats, and thus it could be a novel promising therapy for psoriasis.Graphical abstract

Formulation and evaluation of Ketorolac tromethamine for transdermal drug delivery system

Nonsteroidal anti-inflammatory drugs (NSAIDs) such as Ketorolac Tromethamine are widely recommended to treat pain caused by osteoarthritis, ankylosing spondylitis, acute sciatica, rheumatoid arthritis and low back pain. Modern drug delivery technology, such as transdermal patches, is mostly used in the treatment of numerous diseases. As first-pass metabolism is avoided. Transdermal drug delivery systems (TDDS) can efficiently enhance bioavailability and help with the planned and controlled release of drug molecules into the systemic circulation. The purpose of this work was to produce matrix-type Ketorolac tromethamine transdermal patches by solvent evaporation using different polymer ratios, such as HPMC 15 cps, HPMC E5, and Eudragit S 100. Along with solvents like methanol and chloroform, plasticizers like glycerine, propylene glycol, and PEG 200 are used in this formulation. According to the FTIR study, Ketorolac Tromethamine had no significant interactions with other excipients. The following evaluations are carried out such as thickness, weight variation, folding durability, moisture content, drug content, surface pH, and In vitro diffusion are all evaluated for the prepared patches.

Oral Gastroretentive Film of Lacidipine for the Treatment of Gastroparesis

The research work was aimed to formulate and evaluate gastroretentive mucoadhesive film of calcium channel blocker, Lacidipine for treatment of gastroparesis. Box-Behnken design was used for preparation of optimized formulation using solvent casting method. In this design, different concentrations of mucoadhesive polymers HPMC E15, Eudragit RL100, and Eudragit RS100 were considered as independent variables and its effect on responses like percent drug release, swelling index at 12 h, and folding endurance of the film were examined. Drug and polymer compatibility studies were performed using Fourier transform infrared spectroscopy and differential scanning calorimetry. Optimized formulation was evaluated for organoleptic properties, weight variation, thickness, swelling index, folding endurance, drug content, tensile strength, percent elongation, drug release, and percent moisture loss. The results revealed that the film possessed considerable flexibility and smoothness, and in vitro drug release was found to be 95.22% ± 0.93% at the end of 12 h. Scanning electron microscopy imaging of film displayed smooth, uniform, and porous surface texture. The dissolution followed Higuchi's model and Hixson Crowell model displayed non-Fickian drug release mechanism. Furthermore, the film was incorporated in capsule and the presence of capsule showed no effect on the drug release profile. In addition, no change was observed in the appearance, drug content, swelling index, folding endurance, and drug release upon storage at 25°C ± 2°C and 60% ± 5% relative humidity for 3 months. Collectively, the study revealed that gastroretentive mucoadhesive film of Lacidipine could serve as an effective and alternate site-specific targeted delivery in the management of gastroparesis.

Articulation and Evaluation of Extended-Release Beads using a Sulfasalazine Drug

The present study was focused on optimization of the formulation for the extended-release capsule of mesalamine. Multi particulate system has long been employed to improve the bioavailability of drugs. Mesalamine pellets were prepared by Coating drug solution on sugar sphere followed by functional coating. The release pattern depends upon the pore formation on the outer surface of the unit particle or beads and then slowly and steadily releasing drugs from the inner core. Ethocel grade 7cps was used as a release controlling polymer with the aid of hydrophilic polymer HPMC E5 with pore former to work as a controlled drug delivery system. The functional coated Pellets were used for various parameters like assay and in-vitro dissolution profile. The study confirmed that mesalamine can deliver its effect into lower part of intestine. The finally prepared pellets were used for the treatment of IBD (Ulcerative colitis) Batch 2 had gave optimised result which follow the US specification. Kinetics was applied to the optimized Batch B-2 which was following Higuchi matrix and the mechanism of release was diffusion as the polymer used was HPMC E5 and Tri ethyl citrate –pore former and Ethocel- impenetrable barrier.

Formulation and Evaluation of Mucoadhesive Tablets of Acarbose for Type 2 Diabetes

The objective of the study was to develop mucoadhesive tablet of Acarbose (α-glycosidase inhibitor) to enhance the bioavailability and to further reduce the dosing frequency of administration. The Mucoadhesive tablets of Acarbose were prepared by using three different Mucoadhesive polymers such as HPMC E5 LV, Sodium alginate and Guar Gum in varying concentrations and by direct compression technique. The micromeritics evaluation such as angle of repose, bulk density, tapped density, compressibility index and Hausner's ratio showed good to satisfactory flow properties. Swelling index was calculated with respect to time. The swelling index profile of all formulations, prepared as per the experimental design showed an increase in the value of swelling index as the amount of polymer increased. Maximum swelling index was found seen with formulations containing Sodium alginate, the value increases with increasing the amount of sodium alginate. The highest adhesion force i.e. highest strength of mucoadhesive bond was observed with Formulation F9 containing Guar gum as 18.02±0.17 this followed by F6 containing Sodium alginate as 16.33±0.56 and formulation F8 containing Guar gum in the ratio 1:2 as 14.26±0.11. The Adhesion Force increases with increasing the concentration of Mucoadhesive polymers used. The Tablets containing HPMC E5 LV showed least adhesive force than tablets of other formulations. The formulation F6 containing Sodium alginate was taken as optimized formulation based on its mucoadhesive strength and in vitro release was found to be optimum. The optimized formulation was subjected to kinetic drug release studies. The formulation best fitted into zero order kinetics. The drug release was dominated by the erosion and swelling of the polymer. From the release exponent in the Korsmeyer-Peppas model it could be suggested that the mechanism that leads to the release of drug was non-Fickian diffusion. Keywords: mucoadhesive tablet, Acarbose, Gastroretentive

The preparation, characterization, and application of porous core–shell composite particles produced with laboratory-scale spray dryer

Objective To prepare porous core–shell composite particles (PCPs) in order to improve the flowability and compactibility of powder materials for direct compaction (DC), as well as the dissolution of tablets. Significance The results obtained are meaningful to boosting the development and further research of PCPs on DC. Methods: In this study, hydroxypropyl methylcellulose (HPMC E3) and polyvinylpyrrolidone (PVP K30) were selected as shell materials, the Xiao Er Xi Shi formulation powder (XEXS) was used as the core materials, ammonium bicarbonate (NH4HCO3), and sodium bicarbonate (NaHCO3) were employed as pore-forming agent. Using co-spray drying method to prepare composite particles (CPs). Then, the physical properties and comparison between different CPs were characterized comprehensively. Finally, the different CPs were directly compacted as tablets to explore the effect on the dissolution behavior of DC tablets, respectively. Results (i) The XEXS PCPs were prepared successfully by co-spray drying, and the yield of PCPs is almost 80%; (ii) The TS values of PCP-X-P-Na, PCP-X-P-NH4, PCP-X-H-Na and PCP-X-P-Na were 5.70, 7.56, 3.98, and 6.88 times higher than that of raw material (X); (iii) The disintegration time of PCPs tablets decreased 10–25% when compared with CPs tablets; (iv) The values of Carr’s index (CI), Hausner ratio (HR), Caking strength (CS), and Cohesion index (CoI) of PCP-X-H-NH4 were 19.16%, 19.29%, 40.14%, and 6.39% lower than that of X, respectively. Conclusions The PCPs prepared by co-spray drying did improve the flowability and compactibility of powder, as well as the dissolution of tablets.

Formulation and Evaluation of Nanosuspension of Ranolazine

Objectives The main objective of the study was to formulate and evaluate Ranolazine nanosuspension. Ranolazine is an oral anginal medication that belongs to Biopharmaceutics Classification System BCS Class II with low solubility and enters hepatic circulation.Methods Nanoedge technology was used to prepare the Ranolazine nanosuspension. Various characterization studies including drug content yield Fourier Transform Infrared Spectroscopy FT-IR Differential Scanning Calorimetry DSC Scanning electron microscopy SEM and in vitro drug release were carried out. HPMC E15 Eudragit L100 were used as stearic stabilizers lecithin as an electrostatic stabilizer Tween 80 as a surfactant ethanol as the solvent and water as the antisolvent.Result Based on the dissolution study the F3 formulation containing HPMC E15 as the stabilizer was considered the ideal formulation exhibiting a maximum drug release of 84.02 at 60 minutes.Conclusion FTIR and DSC studies indicated good compatibility within the dispersion.

FORMULATION AND EVALUATION OF BILAYER TABLET OF VALSARTAN & SPIRULINA

The objective of present study was to formulate and evaluate bilayer tablet of Valsartan (VS) and Spirulina (SP) for treatment of hypertension and diabetes. The combination of Valsartan and Spirulina is used, as Valsartan establishes the immediate release layer (initial dose) and Spirulina as sustained release layer (maintenance dose) respectively. The bilayer tablets of VS and SP was particularly designed to minimize the risk of hypertension, diabetes and improve the therapeutic efficacy and to prolong the drug release and patient compliance. The formulation variables for immediate release layer include sodium starch glycolate and crospovidone as super disintegrants and micro crystalline cellulose as filer. HPMC K100, HPMC E15, was used as polymers for sustained release. The result of in-vitro release data showed that HPMC K100 can sustain the drug release up to 12hrs. From these studies HPMC K100 has been selected for further studies of bilayer tablet. Valsartan and Spirulina bilayer tablets were prepared by direct compression method. The hardness of the bilayer tablets was found to be 6.30±0.02kg/cm2. The thickness of the bilayer tablets was found to be 3.15±0.02mm. The drug content of Valsartan and Spirulina was 98.10±0.90 (SR) and 98.84±0.09 (IR). The in-vitro drug release of bilayer tablets has Valsartan immediate release was within 45minutes and Spirulina from the tablets was found sustained over 12 hours with Zero order equation to analyze the release pattern of the drug from the polymeric system. The value of “n” was in the range of 0.1531, indicating the drug release followed fickian release. Fourier transform infrared spectroscopy (FT-IR) analysis indicated that the chemical interactions between the drugs and excipients were absent. The results of Accelerated stability studies showed that all parameters were within the expected specifications and there were no significant changes observed from initial to 3 month, indicating good stability.

Polymeric nanoparticle of Ebastine: Formulation, Characterization and in vitro Evaluation

The main aim of this research work was the development and evaluation of polymeric nanoparticle for the bioavailability improvement of Ebastine (EBT) to treat allergic condition. EBT is a piperidine derivative that binds preferentially to peripheral H1 receptors and is a long-acting, non-sedating second-generation histamine receptor antagonist. It is practically insoluble in water (class II, according to BCS). This work aims to formulate and adjust Ebastine polymeric nanoparticles to improve the EBT solubility as well as dissolution rate. For the synthesis of PNPs, the solvent evaporation technique was used, and three different types of stabilizer that used (HPMC E5, Soluplus, tween 80). The particle size analysis indicated that the optimized formula EBT 9 had a reduced nanoparticulate size of 42 nm, with a 90 percent increase in in-vitro dissolution profile compared to 17 percent for the comparison Ebastine powder in 0.1 N HCl media (pH 1.2). As a result, polymeric nanoparticles formulation of weakly water soluble EBS greatly improved the drug's dissolving rate and increased its solubility.

Factors affecting on in vitro release of miconazole from in situ ocular gel.

The reason for conducting this study is to prolong release of miconazole in the ocular site of action by ocular-based gels (OBGs) formulations. The formulation factors affecting on the release from OBG should be studied using various gelling agents in various concentrations to achieve the improvement in retention and residence time in response to prolonged release. In this study, the formulations were prepared using carbopol 940, pectin, sodium alginate, poloxamer 407, and poly(methacrylic acid) at 0.5%, 1%, and 1.5% w/v, respectively. Hydroxypropyl methylcellulose E5 (HPMC E5) 1% was added as thickening agent/viscosity builder. The formulation containing carbopol 940, pectin and sodium alginate at 1.5% w/v, displayed a noticable improvement in viscosity, gelling capacity, and extended release for 7 h in comparison with the reference drug. Overall, the release showed that the sodium alginate with HPMC E5 form in situ gel which had longer time of release reach to 12 h compared with other polymers. the release of miconazole from the OBGs affected significantly by two factors includes gelling capacity and viscosity builder. The novelty of this study is supporting the delivery of ocular drugs through a cornea as an important key of the eye instead of dependence on an internal blood supply using an oral or a parental administration.

Formulation and Evaluation of Captopril Loaded Niosomal Transdermal Films

Captopril was the first angiotensin-converting enzyme (ACE) inhibitor used for the management of hypertension. The aim of this study was to prepare and evaluate niosomal-loaded captopril transdermal films. Captopril has good solubility but has poor permeability and reduced bioavailability in the presence of food. The aim and objective are to improve bioavailability and permeability. The captopril-loaded niosomal formulations were prepared by thin film hydration technique, using materials like non-ionic surfactants such as Spans of different grades 20, 40, 60 and 80 and solvents like ethanol and chloroform. The FT-IR results revealed that there was no interaction between excipients and captopril. All the formulations showed better encapsulation efficiency. The dissolution studies showed prolonged drug release in comparison to pure captopril. On comprising all formulations, F3 showed sustained release of 98.44% up to 12hrs. The optimized niosomes of captopril were used to prepare transdermal films using methyl cellulose, HPMC E5, HPMC K4M and HPMC K15M as a film forming agents and dibutyl phthalate as a plasticizer. All the formulated captopril transdermal films were evaluated for drug content, folding endurance, weight variation and in-vitro drug permeation. The in-vitro drug permeation was found to be 99.58% over a period of 12 hrs. Based on the above results, administering niosomal-loaded captopril through the transdermal route is a better approach.

Formulation and Evaluation of Mouth Dissolving Films of Amlodipine Besylate by using Natural and Synthetic Polymers

The present study was undertaken with an objective of formulating the mouth dissolving films of Amlodipine Besylate to enhance convenience and compliance of the elderly and pediatric patients for better therapeutic efficacy. Various batches of Mouth dissolving Films of Amlodipine besylate were prepared by solvent casting method by using various concentration of gelatin and HPMC E5 with PEG- 400, Sodium starch glycolate, Sodium saccharine, Vanillin and Purified water and evaluated for appearance, weight variation, thickness, folding endurance, drug content, disintegration time and in-vitro drug release. The optimized formulation F4 (1:1 ratio of drug and HPMC E5) exhibited acceptable folding endurance (131±1.00), least disintegration time (26±1.00 seconds), highest drug content (100.01±0.89 %) and highest drug release (99.88±0.12%) in 10 minutes. It can be concluded from the study that the mouth dissolving films of amlodipine besylate, formulation F4 for sublingual administration can be an optimized formulation.

Development of the Amorphous Solid Dispersion of Curcumin: A Rational Selection of Polymers for Enhanced Solubility and Dissolution

The goal of this investigation was to determine the effectiveness of hydrophilic polymers in preparing a solid dispersion to enhance the solubility and dissolution of poorly water-soluble drugs, such as curcumin. In order to prepare the solid dispersion, curcumin was uniformly distributed in the polymeric matrix of polyethylene glycol (PEG 6000), hydroxypropyl methyl cellulose (HPMC E5), polyvinyl pyrrolidine (PVP K30), and bovine serum albumin (BSA) using the kneading and solvent evaporation methods. The developed dispersion formulations were characterized for solubility, dissolution, Fourier transform infrared (FTIR), X-ray diffractometry (XRD), scanning electron microscopy (SEM), and differential scanning calorimetry (DSC). Attaining enhanced physical stability with solubility is crucial in the selection of suitable polymer types and ratios. The optimized HPMC E5 and PVP based dispersion displayed 4.3 and 2.8 times greater solubility compared to the pure drug, respectively. The SEM also showed the optimized HPMC-based dispersion was smoother in comparison to the PVP-based dispersion. The XRD and DSC validated the successful modification of the crystal structure of curcumin resulting in the enhancement of its solubility and dissolution. In conclusion, the HPMC E5 formulation was the optimal candidate to create solid amorphous dispersions of curcumin, which might be employed as an effective delivery system.

Formulation of metoclopramide HCl gastroretentive film and in vitro- in silico prediction using Gastroplus® PBPK software

The new trends in pharmaceutical studies focus on targeting drug delivery and computer software that help in the body environment simulation, such as Gastroplus® software. The interest of this study is to prepare a gastroretentive film of metoclopramide HCl (MTC) that was followed by applying the in silico approach to estimate the in vivo prepared formulations. The films were prepared from HPMC E5 and sodium alginate polymers as primary polymers with the aid of secondary polymers. The sodium alginate high proportions films showed instant and long floating duration reaching 24 h but with variable folding endurance. Moreover, sodium alginate films with their secondary polymers carbopol and HPMC E5 slowed the release of MTC. The floating and slow-release patterns assessed the gastroretentive properties of sodium alginate films and were further examined by a mucoadhesive study that guaranteed mucosal adhesion, and the film’s FESEM images showed similar top morphology, but different side view structures. Last, the pharmacokinetic profile of selected films that approached the gastroretentive properties was in silico predicted depending on in vitro release study and floating duration employing the physiological-based pharmacokinetic model in Gastroplus® software. The model determines this prediction found successfully of intravenous and immediate oral release tablets (10 and 30 mg) of MTC. The simulation showed a high amount of MTC retained for long periods in the stomach to Sod.Alginate-3, Sod.Alginate-8, and Sod.Alginate-10 films (films of secondary polymers carbopol and HPMC E5) aid in reaching the optimum site of absorption jejunum 1 due to the slow MTC release.

Hot Melt Extrusion Assisted Felodipine Loaded Liquid Crystal Precursor with Enhanced Solubility and Sustained Drug Release Characteristics

Glyceryl monooleate (GMO) forms cubic mesophase upon hydration with sustained drug release characteristics. However its stickiness and stiffness often creates processing challenges for preparation of formulations. Felodipine (FLD), BCS class II molecule was used as model drug. Thus objective of the current work was to increase manufacturing feasibility of GMO using polymer and to enhance the release of felodipine by preparing LC precursors using HME. HPMC E5 polymer was selected for processing of FLD. Batch optimization was done using 23 Factorial design. The prepared batches were characterized for DSC, FTIR, hot stage microscopy (HSM), plane polarized light microscopy (PPL), PXRD and in vitro dissolution studies. The processing of FLD using HME process showed amorphization as revealed by PXRD studies. DSC and HSM studies showed solubilization of FLD in the molten mass of GMO and HPMC E5 confirming formation of solid dispersion. PPL demonstrated formation of cubic LC phase by GMO upon hydration of prepared formulations. The optimized batch of felodipine showed significant improvement in the dissolution profile of FLD with extended release profile. HME assisted liquid crystal precursors could act as promising formulations for BCS II drugs requiring extended drug release profile with improved processing feasibility of GMO.

Formulation and evaluation of doxepin hydrochloride by fast dissolving buccal film

Tricyclic antidepressants, as doxepin hydrochloride (DH), may also have analgesic neighborhood effect due to its biochemical mechanism of action. This is commonly performed via drug to be administers directly into the blood flow via the Buccal mucosa through using fast dissolving movie system. The main aim of the study was to formulate and evaluate Doxepin hydrochloride by fast dissolving buccal film. The Doxepin hydrochloride buccal film were prepared by the solvent casting method by using the different polymers (HPMC E15, PVA, and HEC). The FTIR test is conducted by this test there was no interaction between the drug and polymers. Then buccal film were evaluated for weight uniformity, thickness uniformity, folding endurance, disintegration study, drug content uniformity, and invitro drug release. The weight uniformity ranged from 47.00 to 55.33mg, thickness ranged from 0.17 to 0.25nm, folding endurance ranged from 344 to 355mm drug content ranged from 84 to 98% and disintegration study ranged from 42.0 to 54.3. The F9 formulation showed highest drug release i.e., 99.96% within 4 minutes. The IR spectra showed stable properties of doxepin hcl mixture of polymers used and revealed the absence of interaction between drug and selected polymer, stability studies were as per ich guideline and result indicated that the selected formulation was stable.

Design and Evaluation of Pulsincap System Containing Nanosuspension of Montelukast Sodium for Chronotherapy in Asthma

In the present study, an attempt was made to prepare a pulsincap chronomodulated drug delivery system for the treatment of asthma and associated early morning allergy. Pulsincap capsule was prepared by sealing the drug nanosuspension inside the formaldehyde treated insoluble capsule bodies with a swellable and erodible guar gum plug. The drug, Montelukast sodium (MLS) nanosuspension was prepared by emulsion-solvent evaporation method using HPMC E15 and sodium lauryl sulphate (SLS). Nanosuspension formulations were optimized by using statistical Central composite design (CCD) for the required size and stability. The entire capsules were enteric coated using Cellulose acetate phthalate (CAP). This enteric coat prevents the drug release in the stomach, further the swellable hydrogel plug protect the nanosuspension to maintain the lag phase (5h) and facilitate its burst release in the colon. The length of this lag phase depends upon the concentration and quantity of the hydro gel plug. In order to simulate the GIT environment, the dissolution studies were performed using a sequential pH change method. DSC studies confirmed the absence of drug-excipient interactions. From the design space provided by the CCD, F14 and F15 formulations were considered as optimized. SEM studies were conducted for F14 formulation and this was filled in the Chronomodulated pulsincap systems (CMPs). These CMPs showed the drug release after 5h lag phase. Hence, when CMPs containing MLS nanosuspension is administered during bed time, it starts releasing the drug at the early morning hours to reduce asthma and associated early morning allergies like rhinitis and sneezing. Further, extensive in vivo studies are needed to be conducted to confirm the efficiency of these CMPs.