Hydroxypropyl Methylcellulose K4M Research Articles

Optimization In-vitro Evaluation and Scratch Wound Healing Assay of Hexacosane Topical Gel for Wound Healing.

The compounds hexocosane, a sterol hydrocarbon identified in the dichloromethane extract and isolated from marine sponges of the genus Agelas. Hexocosane possesses anti-inflammatory and antioxidant activities that reduce inflammation and oxidative stress, they promote cell proliferation and angiogenesis, facilitating tissue regeneration and repair. This multifaceted approach makes this secondary metabolite a promising candidate for developing advanced wound care therapies that effectively address both infection control and wound healing. On the basis of viscosity, in-vitro release, and skin retention, optimal gel formulations were developed with hexocosane (1%) to achieve the best results. A response surface methodology Box-Behnken design was applied on three factors and three levels [carbopol 940 (1, 1.25 and 1.5%), hydroxypropyl methylcellulose (HPMC) (1,1.5 and 1.2%), and propylene glycol (0–1–1.5% and 1–2%, respectively] using three factors and three levels. In order to assess the spreadability and viscosity, a glass slide and a Brookfield viscometer were used. An assay was conducted to determine how topical gel affects wound healing. The optimization study of the gel formulation, involving variations in adhesive polymer (Carbopol 940), release retarding polymer (HPMC K4M), and penetration enhancer (Surfactant), has identified three noteworthy formulations (F4, F8 & F14). Each formulation is characterized by specific attributes such as viscosity, in-vitro drug release, and skin retention. All samples were found to elicit significant wound healing efficacy as evidenced from the representative photomicrographs. The maximum efficacy was elicited by formulation (F4) with 100 mg drug at the time duration of 36 hours.

Development of Glycerosomal pH Triggered In Situ Gelling System to Ameliorate the Nasal Delivery of Sulpiride for Pediatric Psychosis.

Sulpiride (Sul) is a medication that blocks dopamine D2 receptors. It is used to treat gastrointestinal disturbances and has antipsychotic effects depending on the dose given. Sulpiride is subject to P-glycoprotein efflux, resulting in limited bioavailability and erratic absorption. Hence, the aim of this study was to generate a glycerosomal in situ gel of sulpiride for intranasal administration, specifically targeting children with schizophrenia who may have difficulty swallowing traditional solid medications, for enhancing its bioavailability. This study aimed to demonstrate the efficacy of intranasal administration of glycerin-encapsulated lipid-nanovesicles (glycerosomes) mixed with in situ gels for prolonged release of anti-psychotic medication. A Box-Behnken design was utilized to create sulpiride-loaded glycerosomes (Sul-GMs), with the lipid amount (A), glycerin concentration (B), and sonication time (C) acting as independent variables. Their impact on the entrapment efficiency, EE% (Y1), and in vitro drug release (Y2) were evaluated. The sulpiride EE% showed an increase when the glycerin concentration was raised to 25% v/v. Nevertheless, when the glycerin concentration was raised to 40% v/v, there was a notable decrease in the EE%. The optimized glycerosome was added to pH triggered carbopol 974P in situ gel formulations including HPMC K15M with different concentrations. The in situ gel formulation (G3) comprising 0.6% carbopol 974P and 0.6% hydroxypropyl methyl cellulose-K15M (HPMC K15M) demonstrated suitable pH, viscosity, desired gel strength, spreadability, and mucoadhesive strength. Consequently, it was selected for in vitro study, ex vivo permeation investigation, and in vivo evaluations. The glycerosomal in situ gel exhibited favorable ex vivo permeability of SU when applied to the nasal mucosa. The pharmacokinetic investigation revealed that the optimized Sul-loaded glycerosomal in situ gel exhibited a significant fourfold and twofold enhancement in systemic bioavailability compared to both the control gel and the commercially available formulation. Finally, the intranasal administration of Sul-loaded glycerosomal in situ gel is a promising alternative to oral treatment for pediatric patients with psychosis.

Design of berberine hydrochloride sustained-release cold sol using hydroxypropyl methyl cellulose K100M to achieve superior drug dissolution and transdermal absorption

In this study, berberine hydrochloride (Ber) was used as model drug to prepare a sustained-release cold sol using hydroxypropyl methyl cellulose (HPMC) to achieve superior drug dissolution and transdermal absorption effects. For comparison, a Ber cold sol without HPMC was also prepared using the same method. The preparation process was optimized based on the in vitro release and transdermal permeability of the drug. The results indicated that 1.67 wt% Carbomer 940 and 1.33 wt% HPMC K100M were selected as matrix components with the best sustained-release effect, and drug dissolution of cold sol prepared by combination of these two matrices was significantly slower than the cold sol without HPMC. In addition, transdermal absorption result demonstrated that 0.67 wt% glycerin and 1.33 wt% peppermint oil were the best osmotic enhancers for the optimization of Ber sustained-release cold sol. Herein, HPMC K100M performed important functions in the external application of Ber.

Diltiazem Hydrochloride Floating Matrix Tablet: Formulation and in vitro-in vivo Evaluation.

Diltiazem hydrochloride is a calcium channel-blocker with a plasma elimination half-life of 4.4 ± 1.3 h and has a narrow absorption window. So, this work aimed to prepare a gastro-retentive floating matrix tablet. The direct compression method was used to manufacture tablets. 32 factorial design was applied for optimization, taking Hydroxypropyl Methylcellulose K100M (HPMC K 100M) and the amount of sodium bicarbonate as independent factors and cumulative percentage release at 1 h, at 6 h, and at 12 h and floating lag time as dependent variables. The high amount of HPMC K100M and sodium bicarbonate shows good results. The optimized preparation was evaluated for differential scanning calorimetry, in-vivo gastric retention in male albino rabbits, kinetic modeling, and stability study. An in vivo study revealed gastric retention of tablets up to 6 h in healthy male Albino rabbits. The stability study indicated no significant change in the buoyancy and release profiles of the drug. From this study, it can be concluded that the gastro-retentive diltiazem hydrochloride floating matrix tablet was successfully prepared and retained inside the rabbit stomach for up to 6 h and was stable under accelerated stability study.

Formulation Development and Evaluation of Floating Beads of Propranolol Hydrochloride

Purpose: The purpose of present research work was to prepare sodium alginate and pectin antihypertensive floating beads of propranolol hydrochloride. Methods: Floating beads were prepared by using Ionotropic gelation technique using various natural and synthetic polymers in different proportion like sodium alginate, pectin, hydroxy propyl methyl cellulose k4m and calcium carbonate. Result: The floating beads were formulated and evaluated to physiochemical studies, Entrapment efficiency, swelling index, Invitro drug release, drug content, buoyancy studies (Floating time, floating lag time, total floating time) on the basis of evaluation of all floating beads were show good results. Conclusion: It Concluded that floating drug delivery system are float immediately upon contact with gastric fluid for increasing the bioavailability of drug and patient compliance.

3D printing of multi-unit gastro-retentive tablets for the pulsatile release of artesunate

Pulsatile drug delivery is hardly achieved by conventional gastro-retentive dosage forms. Artesunate as a typical anti-malaria medicine needs oral pulsatile release. Here, artesunate-loaded pulsatile-release multi-unit gastro-retentive tablets (APGTs) were prepared with a semi-solid extrusion three-dimensional (3D) printing method. An APGT was composed of three units: artesunate-loaded immediate and delayed release units and a block unit. The matrix of the immediate/delayed release units consisted of polyvinylpyrrolidone (PVP) K30 and croscarmellose sodium, which improved the rapid release of artesunate when contacting water. The block unit consisted of octadecanol, hydroxypropyl methyl cellulose K15M, PVP K30, and poloxamer F68. APGTs showed multi-phase release in simulated gastric liquids (SGLs). The first immediate release phase continued for 1 h followed by a long block phase for 7 h. The second rapid release phase was initiated when the eroded holes in the block unit extended to the inner delayed release unit, and this phase continued for about 14 h. Low-density APGTs could ensure their long-term floating in the stomach. Oral APGTs remained in the rabbit stomach for about 20 h. 3D printing provides a new strategy for the preparation of oral pulsatile-release tablets.

Development and Optimization of Polymeric Nanoparticles and their In vitro Deposition Studies Using Modified TSI

Background: To deliver the drug through the pulmonary route, polymers like oleoylcarboxymethyl chitosan (O-CMC), chitosan, and HPMC (hydroxypropyl methylcellulose) K4M are well known for their effective mucoadhesive properties. Drug-loaded polymeric nanoparticles have the potential for a therapeutic response for the targeted site is a beneficial approach. background: To deliver the drug through the pulmonary route, polymers like oleoyl-carboxymethyl chitosan (O-CMC), chitosan, and HPMC (hydroxypropyl methyl cellulose) K4M are well known for their effective mucoadhesive properties. Drug-loaded polymeric nanoparticles have potential for therapeutic response for the targeted site is a beneficial approach. Objective: The present study is to develop polymeric nanoparticles (PNPs) utilizing mucoadhesive polymers with varying concentrations as well as to develop the PNPs for pulmonary delivery. objective: The present study is to develop polymeric nanoparticles (PNPs) utilizing mucoadhesive polymers with varying concentrations as well as to developed the PNPs for pulmonary delivery. Methods: Polymeric nanoparticles are developed by homogenization and solvent evaporation methods and characterized by modified twin-stage impinger to study in vitro deposition. Results: The characterization of pirfenidone-loaded polymeric nanoparticles (PFD-PNPs) reveals that the mean particle size of O-CMC-PNPs is 140.8 nm ± 20, found to be less than CS-PNPs and HPMC-PNPs. The polydispersibility index reveals that the particles of all prepared formulations are homogenous. At the same time, the zeta potential of O-CMC-PNPs is 40.8 mV ± 5.64, and the entrapment efficiency is 91% ± 1.2, which is better as compared to Chitosan and HPMC K4M PNPs and makes them efficient for pulmonary delivery. Findings from the in vitro deposition study using modified TSI show that 88.5% of the drug delivered through nebulization from both the stage of right and left sides of the TSI suggests effective deposition in the lungs of O-CMC PNPs, and it may move to the deeper regions because of the lowest diameter of the particles. Sustaining release of the drug was found in the O-CMC PNPs for 8 hours, compared with 5 and 7 hours for HPMC PNPs and Chitosan PNPs, respectively. Conclusions: Overall, the results of the O-CMC-PNPs highlight that the prepared nanoparticles with O-CMC would be effective for pulmonary delivery instead of chitosan and HPMC K4M.

Establishment and Validation of a Transdermal Drug Delivery System for the Anti-Depressant Drug Citalopram Hydrobromide.

To enhance the bioavailability and antihypertensive effect of the anti-depressant drug citalopram hydrobromide (CTH) we developed a sustained-release transdermal delivery system containing CTH. A transdermal diffusion meter was first used to determine the optimal formulation of the CTH transdermal drug delivery system (TDDS). Then, based on the determined formulation, a sustained-release patch was prepared; its physical characteristics, including quality, stickiness, and appearance, were evaluated, and its pharmacokinetics and irritation to the skin were evaluated by applying it to rabbits and rats. The optimal formulation of the CTH TDDS was 49.2% hydroxypropyl methyl cellulose K100M, 32.8% polyvinylpyrrolidone K30, 16% oleic acid-azone, and 2% polyacrylic acid resin II. The system continuously released an effective dose of CTH for 24 h and significantly enhanced its bioavailability, with a higher area under the curve, good stability, and no skin irritation. The developed CTH TDDS possessed a sustained-release effect and good characteristics and pharmacokinetics; therefore, it has the potential for clinical application as an antidepressant.

Formulation Development of Mucoadhesive Tablets for Treatment of Hypertension using Losartan Potassium

Controlled-release losartan potassium incorporated bucccoadhesive tablets were prepared using guar gum and hydroxy propyl methylcellulose K4M (HPMC K4M). The polymers had demonstrated considerable influence for all reactions. Ethylcellulose, a naturally impermeable material, was employed as a backing layer. The direct compression approach was used to create nine distinct losartan potassium formulations. Drug and polymer compatibility was determined through preformulation research utilizing fourier transform infrared (FTIR) spectroscopy. Buccoadhesive tablets were evaluated by swelling, bioadhesive characteristics, pH and in-vitro drug dissolution. The bioadhesive strength of guar gum was found to be greater than that of HPMC K4M. The swelling effect provided by both polymers was adequate. All formulations were judged to have an adequate surface pH, with values falling between 7 and 5, suggesting no discomfort to the buccal cavity. Ex-vivo residence times ranging from 7.2 to >10 hours for all tablets tested demonstrated a high degree of adhesion. The improved formulation follows Fickian diffusion release process. The optimized formulation underwent a stability investigation in accordance with International Council for Harmonisation (ICH) criteria, and no significant changes were found.

Multivariate Analysis and Computational Predictability of Modified Release Formulation of Chirally Pure Metoprolol Succinate

This study employs computational techniques to predict the performance of a modified-release matrix formulation of chirally pure S (-) Metoprolol Succinate, using a Quality by Design (QbD) approach. The research defines the Quality Target Product Profile (QTPP) and Critical Quality Attributes (CQAs) of the S (-) Metoprolol Succinate matrix formulation. To assess risks, an Ishikawa diagram and Failure Mode Effect Analysis (FMEA) following ICH Q8 guidelines were conducted. The formulation screening process utilized Plackett–Burman design, followed by optimization through Box–Behnken design. The modified-release formulation was developed using high shear granulation, incorporating a combination of high and low viscosity Hydroxypropyl Methylcellulose (HPMC) polymers along with other excipients. The impact of polymer composition and stearic acid on the release profile of S (-) Metoprolol Succinate was investigated, revealing their significant influence on the drug delivery system's desired effect. Specifically, the variables X1: HPMC K4M and X2: HPMC K100M were identified as key factors affecting drug release (Y1). Statistical analysis (ANOVA) confirmed the significance of the selected model, with predicted outcomes aligning well with observed results, comparable to the reference product Seleken® XL range. Both drug content and release performance were found to be similar to the innovator formulation. In summary, this investigation underscores the potential of employing a QbD approach with a combination of low and high viscosity HPMC polymers to achieve precise single-dose delivery of S (-) Metoprolol Succinate.

Design, Development and Evaluation of Tetracycline Controlled Release Microspheres

Microsphere drug delivery methods have been used to boost efficacy, reduce toxicity, and improve patient compliance. Additional benefits of using microspheres to deliver medications include controlled drug release, improved bioavailability, and targeted drug delivery to the desired location. In order to achieve the required therapeutic effect, hydroxypropyl methyl cellulose K4M and sodium alginate are used as a polymer in microsphere delivery system and different concentration of aluminium chloride is used as cross linking agent. The advantage of microsphere formulations over traditional tablet or capsule formulations is that they increase the surface area exposed to the absorption site, boosting medication absorption and reducing drug dose frequency. Tetracycline is a broad-spectrum antibiotic that is frequently used to treat illnesses like pneumonia and respiratory tract infections. The encapsulation effectiveness, particle size, in -vitro release analysis and release kinetics of the microsphere formulations was assessed.

Formulation development and evaluation of nasal in situ gel of promethazine hydrochloride

Objective The present work aims to develop mucoadhesive thermosensitive nasal in situ gel for Promethazine hydrochloride using quality by design (QbD) approach. It can reduce nasal mucociliary clearance (MCC) and increase residence of the drug on nasal mucosa. This might increase drug absorption to improve bioavailability of the drug as compared to oral dosage form. Significance Promethazine hydrochloride is an antiemetic drug administered by oral, parenteral and rectal routes. These routes have poor patient compliance or low bioavailability. Nasal route is a better alternative as it has large surface area, high drug absorption rate and no first pass effect. Its only limitation is short drug retention time due to MCC. By formulating a mucoadhesive in situ gel, the MCC can be reduced, and drug absorption will be prolonged. Thus, improving bioavailability. Method In-situ gel was prepared by cold method having material attributes as concentration of Poloxamer 407 (X1) as gelling agent and hydroxypropyl methyl cellulose K4M (X2) as mucoadhesive agent. Critical Quality Attributes (CQA) were gelation temperature, mucoadhesive force and ex-vivo diffusion. Central composite design (CCD) was adopted for optimization. Result Optimized formulation satisfied all the CQA significant for nasal administration. Moreover, the formulation was found to be stable in accelerated stability studies for 3 months. Conclusion It can be concluded that since the drug can easily permeate through nasal mucosa and can gain access directly in the brain without undergoing first pass metabolism along with increased residence due to mucoadhesion, mucoadhesive in situ gel has potential to increase drug bioavailability.

Tailoring Risperidone-Loaded Glycethosomal In Situ Gels Using Box-Behnken Design for Treatment of Schizophrenia-Induced Rats via Intranasal Route.

Schizophrenic patients often face challenges with adherence to oral regimens. The study aimed to highlight the potentiality of intranasal ethanol/glycerin-containing lipid-nanovesicles (glycethosomes) incorporated into in situ gels for sustaining anti-psychotic risperidone (RS) release. The Box-Behnken Design (BBD) was followed for in vitro characterization. Glycethosomal-based in situ gels were examined by physical, ex vivo, and in vivo investigations. The ethanol impact on minimizing the vesicle size (VS) and enhancing the zeta potential (ZP) and entrapment efficiency (EE%) of nanovesicles was observed. Glycerin displayed positive action on increasing VS and ZP of nanovesicles, but reduced their EE%. After incorporation into various mucoadhesive agent-enriched poloxamer 407 (P407) in situ gels, the optimized gel containing 20% P407 and 1% hydroxypropyl methyl cellulose-K4M (HPMC-K4M) at a 4:1 gel/glycethosomes ratio showed low viscosity and high spreadability with acceptable pH, gel strength, and mucoadhesive strength ranges. The ethanol/glycerin mixture demonstrated a desirable ex vivo skin permeability of RS through the nasal mucosa. By pharmacokinetic analysis, the optimized gel showed eight-fold and three-fold greater increases in RS bioavailability than the control gel and marketed tablet, respectively. Following biochemical assessments of schizophrenia-induced rats, the optimized gel boosted the neuroprotective, anti-oxidant, and anti-inflammatory action of RS in comparison to other tested preparations. Collectively, the intranasal RS-loaded glycethosomal gel offered a potential substitute to oral therapy for schizophrenic patients.

Formulation and Evaluation of Gastroretentive In Situ Gelling System of Ketoprofen

Abstract A revolutionary concept for achieving long-term medication release is the gastroretentive in situ gelling system. The goal of this research was to formulate and test a gastroretentive in situ gel for ketoprofen delivery to targeted site to increase the residence and delivery time. Ketoprofen gastroretentive in situ gels were synthesized using a cation-driven gelation approach using various combinations and concentrations of polymers such as gellan gum, sodium alginate, and hydroxypropyl methylcellulose (HPMC) K100M. Visual appearance, pH, viscosity, in vitro gelation, in vitro buoyancy, drug content, density measurement, gel strength measurement, water uptake, and in vitro drug release were all evaluated. The total floating time was more than 12 h, with a floating lag time of less than 2 min. The formulations showed pH ranging from 6.89 to 7.61 and drug content ranging from 82.01% to 95.53%. For 11 h, the percent cumulative drug release of formulations F5 and F14, which contained a greater concentration of polymer sodium alginate (1.5%) and a combination of gellan gum and HPMC K100M (0.175% and 0.2%), was 84.10% and 85.49%, respectively. In vitro dissolution experiments and stability investigations both revealed no significant changes in drug content. The findings revealed that the formulated in situ gels aided in extending gastric residence duration, allowing the drug to be released in the stomach.

Optimised neem oil-bilayer tablets: A safe, effective and stable tool for the prevention of vector-borne disease outbreaks by Aedes albopictus

The control of mosquito breeding is an essential step towards the reduction of vector-borne disease outbreaks. Synthetic larvicidal agents produce resistance in vectors and cause safety concerns in humans, animals and aquatic species. The drawback of synthetic larvicides opened a new avenue for natural larvicidal agents, but poor dosage accuracy, need for frequent applications, low stability and sustainability are the major challenges with them. Hence, this investigation aimed to overcome those drawbacks by developing bilayer tablets loaded with neem oil to prevent mosquito breeding in stagnant water. The optimised batch of neem oil-bilayer tablets (ONBT) had 65%w/w hydroxypropyl methylcellulose K100M and 80%w/w ethylcellulose in its composition. After the completion of 4th week, 91.98 ± 0.871% azadirachtin was released from the ONBT, which was followed by a subsequent drop in the in vitro release. ONBT reported long-term larvicidal efficacy (>75%) and a good deterrent effect which was better than neem oil-based marketed products. The acute toxicity study on a non-target fish model (Poecilia reticulata), OECD Test No.203 confirmed the safety of the ONBT on non-target aquatic species. The accelerated stability studies predicted a good stability profile for the ONBT. The neem oil-based bilayer tablets can be used as an effective tool for the control of vector-borne diseases in society. The product may be a safe, effective and eco-friendly replacement for the existing synthetic as well as natural products in the market.

Enhancing Oral Absorption of Orlistat through Gastroretentive Mucoadhesive Pellets: Formulation and Evaluation

Aim: The aim of this study was to develop gastroretentive mucoadhesive pellets of Orlistat to improve its oral bioavailability and enhance its absorption.
 Methods: Orlistat pellets were prepared using Hydroxy Propyl Methyl Cellulose (HPMC) K100M, Sodium Carboxy Methyl Cellulose (NaCMC), Carbopol 934P, and Polyvinyl Pyrrollidone (PVP) K30 in varying ratios. Physical characteristics of the tablets were evaluated, and compatibility studies were performed between Orlistat and the excipients. Swelling index, mucoadhesion strength and drug release were measured for each formulation. Drug release kinetics and stability studies were carried out.
 Results: The combination of HPMC K100M, NaCMC, Carbopol 934P and PVP K30 provided balanced release and mucoadhesion with F13 showing sustained release up to 16 hours. The calibration curve demonstrated a good linear relationship between Orlistat concentration and absorbance over the range of 10 to 50 ?g/ml. Swelling index increased with time and polymer concentration and mucoadhesion strength increased with polymer viscosity and concentration. Drug release from formulations containing HPMC K100M, NaCMC and Carbopol 934P were 12-14 hours, 10-12 hours and 8-11 hours, respectively. Combination polymers in F10-F13 provided balanced release and mucoadhesion, with F13 showing sustained release up to 16 hours. The drug release followed zero order kinetics with non-Fickian diffusion. Stability studies on the optimized F13 formulation showed no significant changes in appearance, hardness, mucoadhesion or drug release over 3 months.
 Conclusion: The combination of HPMC K100M, NaCMC, Carbopol 934P and PVP K30 improved the oral bioavailability and absorption of Orlistat. The study demonstrated the importance of compatibility studies and the use of calibration curves for quantitative analysis. The findings provide valuable insights into the development of drug delivery systems for poorly bioavailable drugs.

DUAL RELEASE CHRONOTHERAPEUTIC SYSTEM OF POORLY WATER SOLUBLE ANTIHYPERTENSIVE DRUG CARVEDILOL: DESIGN, DEVELOPMENT AND IN VITRO CHARACTERIZATION

The current research investigation’s goal was to design a core-in-cup type pulsatile system of an antihypertensive drug (carvedilol phosphate) to reduce the evening and early-morning symptoms of hypertension. An inclusion complex of this drug was prepared with hydroxyl propyl beta cyclodextrin to increase carvedilol solubility. Using direct compression method, various batches of core tablets were formulated using Croscarmellose sodium as a superdisintegrant. Core tablets of the optimized formulation were press coated with backing layer and release-retarding plug layer. An in vitro release research was performed after evaluating the physicochemical characteristics of the core in cup design tablets. Based on the lag time of 8 h between the first and second pulse releases, a batch containing sodium alginate (100 mg) and hydroxypropyl methylcellulose K4M (100 mg) was chosen as the optimum batch. Thus, the dual-release core-in-cup pulsatile tablets may be utilized for managing the hypertension symptoms appearing in chronological order.

Impact of starch-hydrocolloid interaction on pasting properties and enzymatic hydrolysis

Hydrocolloids are extensively used for food processing because their techno functional properties (emulsifier, stabilizer, and structural agent). But there is increasing interest in their role connected with nutritional improvements, particularly related to starch hydrolysis rates, which might involve the viscosity resulting from starch-hydrocolloid interaction. The objective of this research was to investigate the impact of gels viscosity on the enzymatic hydrolysis of a range of starch gels made with different starches and hydrocolloids. Heterogeneous systems (starch-hydrocolloid) were prepared with several starches (corn, wheat, rice, potato, cassava, pea) and hydrocolloids (locust bean gum, guar gum, xanthan gum, hydroxypropylmethylcellulose K4M, psyllium) at different concentrations (0%–0.5% - 2.5%). The starch-hydrocolloid pasting behavior and their susceptibility to amylase hydrolysis was recorded with the Rapid Viscoanalyzer following a rapid method (Santamaria, Montes, Garzon, Moreira, & Rosell, 2022a). The viscosity decay due to alpha-amylase activity was modeled to obtain starch gels hydrolysis rate (k). A negative correlation was found among kinetic constant (k) and viscosity at 37 °C (r = −0.55), setback (r = −0.50), and area under the pasting curve (r = −0.42). For instance, xanthan gum and psyllium addition showed strong negative correlation between kinetic constant and viscosity at 37 °C (r = −0.75) and setback (r = −0.79), respectively, particularly when blended with potato starch. These correlations indicate that pasting properties of the starch-hydrocolloid systems might be predictors of the enzymatic digestion rate of the gels, allowing the design of foods with controlled postprandial glucose response.

Design, preparation, and in vitro evaluation of gastroretentive floating matrix tablet of mitiglinide.

The present research is focused on developing floating matrix tablets of mitiglinide to prolong its gastric residence time for better absorption. Gastroretentive tablets were prepared using a direct compression technique with hydroxypropyl methylcellulose K15M (HPMC K15M) and sodium alginate as matrix-forming polymers and sodium bicarbonate as the gas-forming agent. A 32 full factorial design was adopted to optimize the flotation and release profile of the drug. The concentration of HPMC K15M and sodium alginate were taken as the independent variables, and the floating lag time, time required for 50% drug release, and time required for 90% drug release were taken as dependent variables. The compatibility between drug and excipients was assessed by Fourier transform infrared (FTIR) spectroscopy. The prepared tablets were evaluated for different parameters such as hardness, friability, drug content, floating time, in vitro dissolution, and stability. Dissolution data were analyzed using various kinetic models to ascertain the mechanism of drug release. Finally, a radiographic study was conducted to estimate the retention time of the optimized floating matrix tablets of mitiglinide inside the body. The results revealed that all the physical properties of the developed formulations were within standard limits. The formulation M3, with the maximum amount of both independent variables, was considered to be the optimized formulation based on the desirability value. In addition, the optimized M3 formulation showed stability for over 6months, as evidenced by insignificant changes in lag time, drug release pattern, and other physical properties. Furthermore, radiographic examination indicated that the tablets remained afloat in gastric fluid for up to 12h in the rabbit's stomach. In conclusion, the developed floating matrix tablet of mitiglinide could be regarded as a promising formulation that could release the drug in the stomach at a controlled rate and, hence, offer better management of type II diabetes.

Preparation and Characterization of Hydroxypropyl methylcellulose Gastroretentive Film using Metoclopramide HCl

This study aimed to formulate a gastro retentive slow release dosage form based on oral film for metoclopramide hydrochloric acid (HCl), a medication with a narrow absorption window. The gastroretentive film was made using a solvent casting method with varying ratios of primary polymers (HPMC 15000 cps and HPMC K4M), secondary polymer (carbopol 934), and PEG-400 as a plasticizer. The film of hydroxypropyl methylcellulose (HPMC) K4M-3 (50:50) (HPMC K4M: carbopol) was buoyant for 20 minutes. The 52 wt % of metoclopramide HCl (metclo) was released from the HPMC K4M-3 film after 24 hours, and its swelling index was (46.5%). The mucoadhesive strength of the HPMC K4M-3 was 18 gm, and the film showed no effect on the rat’s stomach tissue compared to normal rat tissue histologically. The HPMC K4M-3 produced modest values of percent elongation of 77.6%. To conclude, the optimized film appeared to be a promising mucoadhesive gastro retentive oral film with the ease of administration and controlled release.