HPMC K4M

Bilayer floating tablets of Dothiepin HCL were developed by direct compression method. Immediate release layer contains 30 mg of drug and super disintegrant sodium starch glycolate, serves the purpose of loading dose. Sustained release layer contained HPMC K4M, natural polymers like xanthan gum, guar gum, karaya gum release the drug for 12 hours’ time. Sodium bicarbonate and citric acid are used to produce effervescence. Floating lag time of optimized tablet is 92 sec, whereas floating duration is more than 12 hours. FTIR results revealed that there was no interaction between drug and HPMC K4M / xanthan gum. The post compression parameters of developed tablets were found to be satisfactory. In this study, it was confirmed that the formulations containing HPMC K4M, have shown better floating properties and finally the formulation containing a combination of HPMC K4M and xanthan gum in 3:1 ratio, has exhibited decent sustained drug release properties. The release kinetics of optimized formulation prepared with the combination of HPMC K4M and xanthan gum followed zero order kinetics.

The objective of the study was to develop an oral controlled release drug delivery system of Lamivudine using the sublimation method. Camphor was used as the sublimation material to prepare gastro retentive tablets that are low-density and easily floatable. Camphor was changed to pores in the tablet during the sublimation process. Floating properties of tablets and tablet density were affected by the sublimation of camphor. Release profiles of the drug from the gastro retentive tablets were affected by tablet density/porosity. The effects of different formulation variables HPMC and the effects of different concentrations were studied. The in vitro evaluation was carried out and it was found that the drug release was affected by different concentrations of polymers used. The highest percentage of drug release (96.89±0.83) was observed with xanthan polymer and followed diffusion with erosion mechanism (Non-Fickian transport).

The aim of the present study is to develop and evaluate floating microspheres containing candesartan cilexetil in order to achieve extended release of drug and thereby to enhance the patient compliance. Floating microspheres were prepared by using solvent evaporation method. The microspheres were formulated using different polymers like ethyl cellulose, HPMC K4M and eudragit RSPO 100 in different concentrations and combinations. The prepared floating microspheres were characterized for their percentage yield (95.44 - 98.52%), drug entrapment efficiencies (71.52 - 97.87 %) and percentage buoyancy (93.45 - 98.66%). The FTIR and DSC studies revealed absence of interactions between drug and selected polymers. In vitro release studies were performed in 0.1 N HCl which showed a drug release of 97.62 % at 24 hour in case of formulation (F7). Fitting the in vitro drug release data to Korsmeyer equation indicated that Fickian diffusion is the mechanism of drug release.

In the present work an attempt has been made to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance by formulating sustained release matrix tablets of tolterodine tartrate a bladder-selective anti muscarinic agent with proven efficacy and tolerability in the treatment of overactive bladder (OAB). Sustained release matrix tablets of tolterodine tartrate were prepared by direct compression method using two different polymers such as HPMC K4M and Xanthan gum as rate controlling polymer in different drug:polymer ratios such as 1:5, 1:10, 1:15, 1:20 with other tablet excipients such as microcrystalline cellulose as diluent, talc, magnesium stearate as glidant and lubricant, PVP K30 as binder, lactose as taste enhancer. The formulations were evaluated for pre-compression and post-compression parameters such as hardness, thickness, weight variation, friability, drug content uniformity, in vitro drug release profiles, short term stability studies and drug excipient interactions. Results revealed that among the 10 formulations the STH3 is considered as promising formulation, displayed almost first order release kinetics, releasing more than 75% drug release in 8.15 hours and remained sustained for more than 12 hours. Short term stability studies of promising formulation STH3 indicates that there are no significant changes in dissolution parameter values after 3 weeks storage at 45±1ËšC/75±5% RH.

Lisinopril dihydrate (LSP) primarily used in the treatment of hypertension, congestive heart failure and heart attack. Floating matrix tablets of LSP prepared with a view of prolonging gastric residence time with a controlled release mechanism to achieve improved patient compliance, least side effects, better drug therapy and all aspects of an ideal drug delivery system. Floating matrix tablets were prepared by  wet granulation technique using  varying concentrations of different grades of gel forming polymers like HPMC K100, HPMC K15, HPMC K4M with sodium bicarbonate as gas generating agent and evaluated for the physico-chemical parameters, floating lag time, total floating time, in vitro dissolution study and swelling studies. The physico-chemical properties of all the formulations were found to be within the prescribed official limits. FTIR study reveals that there was no interaction between drug and excipients. The amount of drug released from various FDDS formulations was found to be in the order of HPMC K100M > HPMC K15M > HPMC K4M. From among all the formulations, the formulation LF-9 with 30% HPMC K15M showed the best result in terms of the required lag time (82±5 sec) and floating duration of 12 h and releasing 99.5% of the drug in 12 h and is considered as the ideal formulation. The dosage form can control the release, avoid dose dumping and extend the duration of action of a drug with prolonged floating time.

Infestation of the head louse caused by Pediculus humanus capitis is an important public health problem worldwide. FDA has approved Ivermectin as an antilice drug in 2012. Commercially Ivermectin is available in the form of Sklice lotion in US market. Hence, in the present work an attempt was made to formulate hair gel of Ivermectin for better patient compliance and to avoid the side effects related with other formulations. The gels of 0.5% Ivermectin were prepared using different gelling agents such as carbopol 934, hydroxypropyl methylcellulose K4M, hydroxyethyl cellulose 250 HHX. Glycerin and propylene glycol were used as a humectants having plasticizer activity. The formulations were characterized for pH, viscosity, spreadability, extrudability, drug content, in vitro drug release, antilice activity, skin irritation study and stability studies. Among the selected formulations, formulation containing 2% HEC 250 HHX and 15% propylene glycol showed better viscosity, spreadability, extrudability and In vitro drug release as compared to other formulations. It showed excellent antilice activity and no skin irritation was observed. It was found to be stable at 25°C/60% and 40°C/75% RH over a period of 45 days. These results suggest the feasibility of the topical gel formulation of Ivermectin for the treatment of pediculosis.

The main objective of the present investigation was to formulate and evaluate chronomodulated pulsatile drug delivery system of Trimetazidine Hydrochloride which was aimed to release the drug after lag time (6 hrs) in order to mimic circardian rhythm of Angina Pectoris.Preformulation studies and compatibility studies were carried out for drug and excipients. Core tablet was prepared by direct compression using sodium starch glycolate as superdisintegrant and press coated with different polymer & varying its ratio. Further prepared tablets were optimized using 32 full factorial design. Nine batches were prepared varying the amount of polymer and ratio of polumer (HPMC K4M: EC) and they were evaluated for precompressional and postcompressional tests. Optimized batch was derived statistically using desirability function (Minitab 17).The Model was validated by formulating the check point batch. Accerelated stabilitiy study was carried out of optimized batch. Preformulation and compatibility studies was carried out using FTIR , DSC which shows satisfactory results, no interaction was found between drug and excipients. Press coating of core tablet with the combination of HPMC K4M and EC was found to be providing the desired release. Results of precompressional and postcompressional was found to be within the limits. Varying  the amount of coating and ratio of polymer have significant effect on lag time(Y1) as well as on time required for 90% drug release (Y2).Optimized batch shows lag time of 6 hrs followed by complete release within 1 hrs which is desiered in case of pulsatile delivery. No significant bias was found between predicted and observed value of check point batch.The data of stability study revealed that the optimized formulation is stable. Pulsatile drug delivery system of Trimetazidine Hydrochloride for chronomodulated therapy can be prepared by press coating technique using 200 mg of coating and HPMC K4M:EC(10:90) ratio of polymer which will provide lag time of 6hrs and complete release within 1 hrs.

In the present study, Flurbiprofen was used for preparing Floating dosage form that are designed to retain in stomach for a long time and have developed as a Floating drug delivery system by using various polymers like Carbopol 940 and HPMC K4M to enhance the bioavailability and therapeutic efficacy of Flurbiprofen. The mechanism of action of Flurbiprofen is Non selective COX inhibitor which inhibits the prostaglandin synthesis. Sodium bicarbonate and citric acid was incorporated as a gas generating agent. The direct compression method is used in present work. The formulation was optimized on basis of acceptable tablet properties like optimum hardness, uniform thickness, consistent weight uniformity and low friability. The prepared formulation shows better and significant result all the evaluated parameter. 

Ophthalmic drug delivery is one of the most interesting and challenging endeavors facing the pharmaceutical scientist. The anatomy, physiology and biochemistry of the eye render this organ highly impervious to foreign substances. The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid pre-corneal elimination of the drug may be overcome by the use of in situ gel forming systems that are instilled as drops into the eye and then undergo a sol-gel transition in the cul-de-sac. The purpose of the present work was to develop an ophthalmic drug delivery system of Pefloxacin mesylate for in situ gelling system byusing ion sensitive gelling agent (Gelrite) and viscofying agent (HPMCK4M). Optimization by 22 factorial design using Design expert software 8.0 version was applied to the formulations. Formulation with Gelrite (gellan gum) and HPMC K4M shows percent drug content of 99.83%, viscosity of 1864 cp at 20 rpm and in-vitro drug release of 88.32% which shows formulation is good. The developed formulation was found to be stable and provided sustained release of the drug over 8 hours.

Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation in a sustained manner; avoiding the first-pass metabolism. The goal of present investigation was to design and evaluate mucoadhesive buccal films of Repaglinide in order to avoid first-pass effect and release the drug for extended period of time. The Buccal films were formulated using polymers, Carbopol-971P and HPMC K4M, by solvent casting method; using PEG 400 as plasticizer. In this study, an attempt has been made to prepare Repaglinide inclusion complex; to enhance its solubility and was incorporated into the mucoadhesive buccal films in order to improve the bioavailability. A comparative study has been done between; uncomplexed Repaglinide loaded buccal films and inclusion complex loaded buccal films. The films prepared were evaluated for various physicochemical parameters and in vitro drug release. It was observed that inclusion complex loaded buccoadhesive films showed higher cumulative percentage of drug release at the end of 8 hours. The release data obtained was analyzed using various mathematical models. The Repaglinide loaded films followed zero order kinetics with principle mechanism of drug release being fickian diffusion. Whereas the inclusion complex loaded films followed zero order kinetics and exhibited non-fickian diffusion mechanism. HCC1 formulation having acceptable physicochemical parameters and with highest cumulative percentage of drug release (95.18%) at the end of 8 hours was chosen as optimum formulation and its short term stability studies revealed adequate stability of the formulation.