Sustained Dosage Form Research Articles

Comparative in vivo evaluation of marketed sustained release and optimized pulsatile formulation of propranolol hydrochloride

Chrono pharmaceutical drug delivery system is devoted to the availability of active on a pace that idyllically matches biological requisite of disease treatment. It embodies time controlled and site-specific drug delivery systems, subsequently optimizing therapeutic action and lessening side-effect’s. In the present study optimized pulsatile formulation of Propranolol Hydrochloride ought to deliver drug at pre-set pattern at right time and site is evaluated for pharmacodynamic and pharmacokinetic performance after oral administration and compared with an existing marketed sustained formulation of Propranolol Hcl. The study was carried out in male New Zealand albino rabbits through cross over design pattern and levels of plasma measured by means of LC-MS/MS method. Pharmacokinetic parameters of designed pulsatile formulation was measured and observed to have statistical significance with existing marketed sustained formulation. The In-house pulsatile dosage form able to show lag phase and the mean residence time of pulsatile dosage form (23.20.14h.) was found to be beyond the marketed sustained dosage form (14.8 0.01h.). Pharmacokinetic data revealed a maximum guard against adrenaline levels at 6 h post oral intake and dropped to 50% after 12 h with Marketed formulation. Whereas in case of pulsatile formulation administration a maximum protection was obtained at 12 h. and continued over a period of 18 h. It is concluded that the designed pulsatile formulation offers a promising way of drug release for a programmed time period at desired site, once the administration time and pulse time are aligned with circadian pattern.

Brain targeting stealth lipomers of combined antiepileptic-anti-inflammatory drugs as alternative therapy for conventional anti-Parkinson’s

This study presents an alternative therapy to conventional anti-Parkinson’s treatment strategies; where motor and non-motor symptomatic complications are considered. Thus; providing sustainability, patient compliance, therapeutic safety and efficiency, based on triggering secretion of endogenous dopamine (DA). Exogenous DA has long been considered the best therapy, however, its poor blood brain barrier (BBB) permeability, fluctuated plasma levels, and non-motor complications negligence, decreased response to therapy with time. Consequently; brain targeting Tween®80-coated pegylated lipomers were tailored for intravenous administration (IV) of L-Dopa, and two drugs of reported neuroprotective effect: lamotrigine (LTG) and tenoxicam (TX). Single-step nanoprecipitation method was used; for its reproducibility and ease of scaling-up. Formulation targeting and anti-PD efficiency was evaluated against marketed standards and L-Dopa. In-vitro and in-vivo pharmacokinetic and dynamic studies were carried out for setting optimization standards upon varying inter-components ratio. Results revealed that lipomers are, generally, significantly efficient in brain targeting compared to oral tablets. LTG-lipomers (LF20) showed the maximum anti-PD compared to its TX and L-Dopa analogues. Combining LTG and TX had synergistic effect; highlighting a new prescription for both drugs. Thus; offering a safe, targeted, and therapeutically efficient sustained dosage form, capable of mitigating PD risk and treating it though weekly administration. Hence; presenting a novel promising anti-neurodegenerative strategy; on employing various mechanisms that were previously achieved through additional therapeutic supplements.

Formulation and evaluation of nanoparticulate ofloxacin ophthalmic gel using ionic gelation method

Oflaxacin is an ophthalmic and topical anti-bacterial agent used in the management of Allergic conjunctivitis, Trachoma, Blepharitis. The basic idea behind the development of such a system is to maintain a sustained drug release from the dosage form. Oflaxacin is suitable candidate for formulation into sustained dosage form in order to prolong the release of drug. The drug-excipient compatibility studies were carried out by using FTIR technique. Based on the results, excipients were found to be compatible with ofloxacin. In preformulation study, estimation of Ofloxacin was carried out by systronics UV spectrophotometer at λmax 284nm using distilled water, which had a good reproducibility and this method was used in entire study. Formulation was prepared by using ionic gelation method .The response drug content, entrapment efficiency, diffusion, spreadability, In vitro drug release was evaluated Drug content ranging from to 82.6 % to 91.24% entrapment efficiency values are ranged from 91.25% to 94.02% and in -vitro drug release studies are also studied. The In-vitro drug release study of Ofloxacin was carried out by using In-vitro diffusion apparatus.100ml of using tear fluid was taken in a beaker. The solution was stirred with 100rpm by maintaining the temperature of 37˚c ± 5˚c. The drug release data were explored for this type of release mechanism followed. The best fit with the highest determination R2 coefficients was shown by both the models (zero and peppas) followed by Higuchi model which indicate the drug release via diffusion mechanism. However as indicated by the values of R both of the models (zero and peppas) followed by Higuchi model were found to be efficient in describing the release of Ofloxacin.

Formulation and Evaluation of Floating Microspheres of 1,1-Dimethylbiguanide

1,1-Dimethylbiguanide is a hypoglycemic agent used in the treatment of non-insulin dependent Diabetes mellitus. It is a BCS Class –III drug having poor permeability. Plasma half life ranges from 1.5-3 hrs & oral bioavailability is 50-60%. Hence require frequent oral administration for adequate treatment of Diabetes in order to extend the gastric retention time oral sustained dosage form was developed in the form of microspheres using polymers (sodium CMC, HPMC K 100 M). The results presented that drug dissolution rate and drug entrapment increases while decreasing the polymer amount. All the formulations are evaluated for dissolution, entrapment efficiency, percentage buoyancy and 1,1-Dimethylbiguanide Microspheres of formulations, F-4 was found to be optimized formulation based on in-vitro release pattern and percentage buoyancy entrapment efficiency. Keywords: 1,1-Dimethylbiguanide, half-life formulations, efficiency.

Formulation and evaluation of floating tablet of H2-receptor antagonist

Context: Conventional sustained dosage form of ranitidine hydrochloride (HCl) does not prevent frequent administration due to its degradation in colonic media and limited absorption in the upper part of GIT.Objectives: Ranitidine HCl floating tablet was formulated with sublimation method to overcome the stated problem.Methods: Compatibility study for screening potential excipients was carried out using Fourier transform infrared spectroscopy (FT-IR) and differential scanning chromatography (DSC). Selected excipients were further evaluated for optimizing the formulation. Preliminary screening of binder, polymer and sublimating material was based on hardness and drug release, drug release with release kinetics and floating lag time with total floatation time, respectively. Selected excipients were subjected to 32 factorial design with polymer and sublimating material as independent factors. Matrix tablets were obtained by using 16/32” flat-faced beveled edges punches followed by sublimation.Results: FT-IR and DSC indicated no significant incompatibility with selected excipients. Klucel-LF, POLYOX WSR N 60 K and l-menthol were selected as binder, polymer and sublimating material, respectively, for factorial design batches after preliminary screening. From the factorial design batches, optimum concentration to release the drug within 12 h was found to be 420 mg of POLYOX and 40 mg of l-menthol. Stability studies indicated the formulation as stable.Conclusion: Ranitidine HCl matrix floating tablets were formulated to release 90% of drug in stomach within 12 h. Hence, release of the drug could be sustained within narrow absorption site. Moreover, the dosage form was found to be floating within a fraction of second independent of the pH of media ensuring a robust formulation.

Development and evaluation of sustained release tablet of betahistine hydrochloride using ion exchange resin tulsion t344.

An attempt was made to sustain the release of Betahistine hydrochloride by complexation technique using strong cation-exchange resin, Tulsion T344. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, swelling time, ratio of drug : resin, and temperature. The resinate was evaluated for micromeritic properties and characterized using XRPD and IR. For resinate sustained release tablets were formulated using hydoxypropyl methylcellulose K100M. The tablets were evaluated for hardness, thickness, friability, drug content, weight variation, and in vitro drug release. Tablets thus formulated (Batch T-3) provided sustained release of drug over a period of 12 h. The release of Betahistine HCl from resinate controls the diffusion of drug molecules through the polymeric material into aqueous medium. Results showed that Betahistine HCl was formulated into a sustained dosage form as an alternative to the conventional tablet.

Taste masked sustained release tablet of metformin hydrochloride

Sustained release formulation of metformin hydrochloride (MTHCL) presents significant challenges due to its poor inherent compressibility and high water solubility. Thus formulating MTHCL into sustained dosage form would provide slow release. But, it is bitter in taste and taste should be masked to formulate it in palatable form. So in the work undertaken, an attempt was made to sustained the release also to mask the bitter taste by complexation technique using strong cation-exchange resin, indion 244, 254 and 264 (Polyacrylic hydrogen with carboxylic functionality).The drug loading was optimized for mixing time, activation, pH, mode of mixing, drug:resin ratio and temperature.The resinate was evaluated for micromeritic properties, taste masking and characterized by X-Ray diffraction study and IR. Using resinate sustained release tablets were formulated using HPMC (K100M) and MCC (PH 102). The tablets were evaluated for hardness, thickness, friability, drug content, weight variation and in-vitro release. Tablets formulated (Batch B-9) provided sustained release over a period of time 10 hours with first order kinetics. The release of MTHCL from resinate controls the diffusion of drug molecules through the polymeric material into aqueous medium. The results showed that MTHCL was successfully taste masked and formulated into a sustained dosage form as an alternative to conventional tablet.

Formulation and in vitro evaluation of sustained release dosage form with taste masking of metformin hydrochloride

An attempt was made to sustain the release of metformin HCl as well as to mask the bitter taste by complexation technique using strong cation-exchange resins, indion 244 and indion 264. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, mode of mixing, ratio of drug:resin and temperature. The resinate was evaluated for micromeritic properties, taste masking and characterized using XRPD and IR. Using resinate sustained release tablets were formulated using hydoxypropylmethylcellulose K100M.The tablets were evaluated for hardness, thickness, friability, drug content, weight variation and in vitro drug release. Tablets thus formulated (Batch B-6) provided sustained release of drug over a period of 10 h with first order kinetics. The release of metformin HCl from resinate controls the diffusion of drug molecules through the polymeric material into aqueous medium. Results showed that metformin HCl was successfully taste masked and formulated into a sustained dosage form as an alternative to the conventional tablet.

The in vivo performance of theophylline microcapsules.

The possibility of using microcapsules as a sustained dosage form of theophylline has been investigated. The release characteristics of two formulae were compared with microcrystalline theophylline. Urine samples were assayed using H.P.L.C. to separate the unchanged theophylline which was detected by its U.V. spectrum. A single-compartment model for absorption and elimination could explain the results found. Both microencapsulated formulations showed a significantly extended absorption time over that of non-encapsulated theophylline.