Wet Granulation Method Research Articles

Implementation and comparison of different taste masking techniques to design and assess dispersible tablet formulations

The objective of this study was to assess the efficacy of several taste-masking techniques and to study the impact of different formulation variables on the physicochemical properties of dispersible tablets containing Ranitidine as a model drug. Ranitidine powder was taste masked using various techniques. Factorial design (24) was applied to design the set of tablet formulations. The four factors implemented were the manufacturing method, filler type, superdisintegrant type and superdisintegrant concentration. Levels selected were direct compression and wet granulation for the manufacturing method, microcrystalline cellulose and mannitol for the diluent type, sodium starch glycolate and croscarmellose sodium for superdisintegrant type, and 2% and 10% for superdisintegrant concentration. Granulation with calcium carbonate (ratio of 1:8) was the taste-masking method of choice to be implemented. The formulated tablets results revealed that the manufacturing method has a significant influence on all the tested physicochemical properties (p-values < 0.05) such as tablet’s weight variation, hardness, friability, and disintegration time. Croscarmellose sodium obtained better results than sodium starch glycolate. Both fillers obtained good properties when implementing direct compression method with croscarmellose sodium concentration of 2%, or wet granulation method with croscarmellose sodium concentration of 10%. Drug release was also increased by increasing concentration of croscarmellose sodium. These findings represent an easy manufacturing procedure with relatively low-cost materials that can be implemented to formulate dispersible tablets of bitter tasting drugs that will enhance patient compliance and lead to faster onset of action.

Formulation of Pectin-Based Double Layer-Coated Tablets Containing Dexamethasone and Probiotics for Inflammatory Bowel Disease

Inflammatory Bowel Disease (IBD) is a chronic inflammatory condition in the colon that includes ulcerative colitis and Crohn’s disease. Dexamethasone is a steroid anti-inflammatory drug that can be used in IBD therapy. This study aims to obtain an optimum formulation of a dexamethasone drug delivery system for IBD treatment and to investigate its release profile based on an in vitro dissolution test. Dexamethasone was formulated as a double-coated tablet in combination with a probiotic L. acidophilus and B. longum mixture (1:1). The core tablets were produced using the wet granulation method, after which they were coated with pectin 4% b/v on the inner coat and a mixture of Eudragit L100 and S100 (1:4) on the outer coat. Three different core tablet formulas were prepared by varying the concentration of probiotics at 0%, 16% and 40% (F1, F2, and F3, respectively). The cumulative drug release of F1, F2 and F3 in HCl 0.1 N pH 1.2 for 2 hours were 42.92 ± 1.55%, 39.41 ± 4.10%, and 39.39 ± 1.63%, respectively, while in the phosphate buffer pH 6.8 they were 102.83 ± 1.56%, 105.08 ± 1.70%, and 98.81 ± 3.37% respectively, after 12 hours. From the results, we conclude that all formulas could be promising candidates for developing colon-targeted drug delivery.

Evaluation of modified Cenchrus americanus starch as disintegrant in formulation of chlorpheniramine maleate tablets

The aim of this research was to investigate the disintegrant properties of modified Cenchrus americanus starch (MCS) in chlorpheniramine maleate tablets formulation. The matured seeds of C. americanus were steeped in 4 L of 0.25 % w/v sodium hydroxide at 5 °C for 24h, washed, soaked in distilled water (30 ± 2 °C) for 24 h, and wet milled. The slurry was washed with distilled water through a 200 mesh screen, and the filtrate left undisturbed for 18 h. The top layer sediment was scrapped off, and the starch re-suspended with water. Further washing and sedimentation was done until the top layer of the starch became white. The starch was dried at 40 °C, defatted using Petroleum-Ether, air dried, sized (125µm) and characterized using standard methods. The MCS was used at 5, 10 and 15 % w/w as disintegrant in the formulation of chlorpheniramine maleate granules using the wet granulation method. Primogel at similar concentrations was used as comparing standard. Characterization of the granules for densities and flowability were done. Chlorpheniramine maleate tablets compressed from these granules were evaluated for uniformity of weight, hardness, disintegration time, assay and dissolution. Results showed poor flow properties for the MCS powder while the chlorpheniramine granules exhibited good flow. The tablets showed minimal variation in weight, good hardness (6.06±0.10 - 8.07±1.31 kgF), disintegration time (< 7 min), friability (< 1 %), and dissolution of more than 80 % within 30 min. The MCS compared favourably with primogel as disintegrant in chlorpheniramine tablets formulation and met with British Pharmacopoeia set limits.

Formulation and Evaluation of Controlled Release Tablet of Irbesartan

The main aim of present work was to formulate and evaluate controlled release matrix tablets of Irbesartan. It releases drugs at fixed and expected rate in a controlled manner either by dissolution and diffusion control mechanism. The matrix tablet was prepared by wet granulation method using by various concentration of HPMC and ethyl cellulose with combination of various release retardant polymer. The powder mixtures were subjected to various pre- compression parameters such as angle of repose, bulk density, tapped density and Carr’s index shows satisfactory result and the compressed tablets are evaluated for post- compression parameters such as weight variation, thickness, hardness, friability, drug content and in- vitro dissolution studies. In- vitro dissolution studies were carried out for 24 hours using 0.1N HCL for first 2 hours and ph 6.8 phosphate buffers for 24 hours and the result showed that formulations F3 and F4 show good dissolution profile to control the drug release respectively. The drug content of the formulation was determined by using 0.1 N HCL at 262nm. The drug content was maximum with formulation F5 and minimum with formulation F3.

Formulation and Evaluation of Oro-dispersible Bromhexine Hydrochloride Granules Using Sachelac-80

Background: Patients with sudden episodes of allergic or epileptic attacks and those who are mentally ill are less non-compliant and there is a lack of effective therapy. The need for delivering therapy at a very fast pace is the primary objective. Though oral medications exist for such patients these have their own disadvantages. Methods: Wet granulation method was used for preparation of Orodispersible (ORD) granules using Pearlitol 200 SD and Sachelac 80. Water soluble Bromhexine HCl granules were prepared by incorporating suitable surfactants, binder, to some extent co-surfactant and oils as well, so as to increase its bioavailability. The prepared granules were characterized by standard methods. Results: FTIR studies show drug- excipient compatibility. Formulation F1 shows superior results than other batches. Drug content of 97.5 %, with excellent flow properties and drug release of 102.3 % was observed for F1. A temperature of 40 ± 2°C and relative humidity of 75 ± 5% RH, was found to be most stable for F1 formulation as it indicated there were no significant changes in any of the parameters mainly in drug content. Similarly, FTIR study suggests compatibility as there are no interaction between any of the excipients as well active ingredient. Conclusion: This study showed that the method used for preparation resulted in pharmaceutical preparation that had fast onset of action, enhanced bioavailability, compliance in patients, enhanced stability and was cost effective.

Role of Aminated Derivatives of Natural Gum in Release Modulating Matrix System of Losartan Potassium

Objective: The investigation aimed to synthesize amino derivatives of various natural gums like Xanthan gum and Tamarind gum for using them as a release modulating polymer in the formulation of the hydrophilic matrix system of losartan potassium and to find the best amongst them. Developing oral sustained release matrix tablets for a drug with a constant release rate has always been a challenge to the pharmaceutical technologist. 
 Materials and Methods: Release modulating hydrophilic matrix tablets of losartan potassium were prepared by wet granulation method. A total number of 6 formulations of release modulating hydrophilic matrix tablets of losartan potassium were prepared using different polymeric ratios of Carbopol 934, aminated Tamarind gum and aminated Xanthan gum based on preliminary trial bathes. The formulated tablets were evaluated for both pre-compression and post-compression evaluation studies. 
 Results: Based on in vitro drug release study the effective formulations AXG 3 are shows a maximum similar release profile to other remains formulations with a theoretical drug release profile of losartan potassium for sustained release. Finally optimized formulation AXG 3 containing carbopol 934 (60 mg), aminated xanthan gum (40 mg), MCC (190 mg) and magnesium stearate (10 mg) showed 100±0.024 % drug release in 12 hr which is acceptable with theoretical drug release of losartan potassium for sustain release dose. Conclusion: Aminated derivatives of xanthan gum and Tamarind gum extend the drug release for 12 hr. Based on in vitro drug release studies of formulations, we concluded that the alteration in the concentration of carbopol 934 with an aminated derivative of xanthan gum in sustain release formulation development was more effective and economical.

Isolation, Characterization of Banana Starch and its Evaluation as a Disintegrating Agent in Dispersible Lornoxicam Tablet

Objective: The present study was designed to isolate, characterize, formulate, and evaluate the disintegration properties of banana starch in dispersible Lornoxicam tablet formulation. Methods: The alkaline extraction method used sodium hydroxide as a lye solution to isolate starch from unripe banana fruit. Starch was subjected to characterization for physicochemical properties, viscosity and flow properties, Fourier-transform infrared spectroscopy (FTIR) scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray crystallography (XRD) study. Flow properties of starch were determined as per the standard procedure. Tablets were formulated by a wet granulation method using starch as a disintegrant, and the in-vitro release characteristic of the prepared tablets was analyzed. Different concentrations of isolated starch were studied for disintegrating properties compared to corn starch. Results: Studies indicate that starch obtained is qualitatively and quantitatively comparable to corn starch. SEM, FTIR, DSC and XRD data confirmed the polysaccharide nature of the starch. The physicochemical properties of starch passed the prescribed evaluation tests for tablets. These tablets also confirmed the disintegration and dissolution specifications as per Indian Pharmacopoeia. Conclusion: From the above study, it can be concluded that starch obtained from banana shows qualitatively and quantitatively good disintegration characteristics compared to corn starch. These tablets also confirmed a significant degree of dissolution as per the standards. Evaluations also specified that banana starch possesses acceptable disintegrating characteristics compared to corn starch and can be used as a disintegrant in tablet formulation.

Formula optimization and physical stability evaluation of effervescent tablet preparations of aqueous extract of Moringa leaves (Moringa oleifera L.)

Moringa leaves (Moringa oleifera L.) are a plant that is widely consumed by Indonesian people and has high nutrition and antioxidants. Utilization of Moringa leaves as a health supplement requires an innovative dosage form to make it practical to use, one of which is by making it in the form of effervescent tablets. The purpose of this study was to obtain an optimal formula for effervescent tablets of aqueous extract of Moringa leaves (Moringa oleifera L.). This study was an experimental study, by preparing effervescent tablets of aqueous extract of Moringa leaves using 3 different formulas using the wet granulation method. The physical stability of the effervescent tablets obtained was then evaluated. The evaluation results were analyzed to obtain the optimal formula from the 3 formulas. The research results obtained showed that F3 was a formula that had good physical stability of granules and tablets. Granules from F3 have an angle of repose of 22.45°, and a compressibility percentage of 12.67%. F3 effervescent tablets have a weight uniformity that does not exceed 5% or 10%, size uniformity that is not more than 3 times the thickness of the tablet, and a faster dissolving time compared to other formulas, namely 1 minute 22 seconds. Based on these results, it can be concluded that the optimal formula of the 3 formulas is F3 with an acid and base concentration of 20% each.

"Formulation and Evaluation of Effervescent Granul from African Leaf Extract (Vernonia amygdalina Del.) "

African leaf plants (Vernonia amygdalina Del.) contain many secondary metabolites, one of which is flavonoids. African leaves are commonly used in traditional medicine. This study aims to determine the extract of African leaf plants can be formulated in the preparation of effervescent granules and is suitable for the criteria for good granules. African leaves were macerated using 96% ethanol as solvent and evaporated to obtain a thick extract. Then, the African leaf extract obtained was formulated into effervescent granules with a concentration of 10%. The production of effervescent granules is based on the principle of the wet granulation method. The results showed that the evaluation of the effervescent granules of African leaf extract was only suitable for the requirements of the haussner factor, porosity, particle size distribution, moisture content, angle of repose, dispersion, and pH but did not suitable for the requirements of compressibility and flowability. The flavonoid content in the African leaf extract is 96,2276% while the effervescent granule is 94,634%.94,634%.

ANTIOXIDANT ACTIVITY OF EFFERVESCENT GRANULES FROM KIRINYUH LEAVES (CHROMOLAENA ODORATA (L.) R. M. KING and H. ROB) AND LEAF OF MAREME (GLOCHIDION ARBORESCENS BLUME)

Objective: The objective of the study was to prepare and evaluate the formulation of the granules effervescent from kirinyuh and mareme leaves as an antioxidant. Methods: The method of making granules with the wet granulation method. The granulation method was used for making granules, meanwhile, the evaluations of the granules was included organoleptic tests, water content, solubility time, pH of the preparation, compressibility, flow time angle of repose and antioxidant activity. Results: The results showed that combination of kirinyuh and mareme as effervescent showed fulfilled all the test criteria, however, demonstrated weak antioxidant activity. Conclusion: The three formulations of effervescent granule preparations from kirinyuh leaves and mareme leaves have very weak antioxidant activity

THE ANTI-INFLAMMATORY TABLET FORMULATION OF COLEUS (PLECTRANTHUS SCUTELLARIODES) LEAVES EXTRACT USING KOLLICOAT®PROTECT COATING

Objective: The purpose of this study was to find the concentration of weight gain on the use of Kollicoat®Protect to produce coleus leaf extract film-coated tablets with good physical properties.
 Methods: Coleus extract was obtained by maceration using 70% ethanol. Tablet cores were prepared using the wet granulation method, then evaluated (uniformity of weight, size, hardness, friability, and disintegration time). Coated tablets were made in four variations of polymer weight gain, i.e. 5, 6, 7, and 8%. To determine the effect of the weight gain concentration of Kollicoat®Protect an evaluation of the coated tablets was carried out, i.e. the uniformity of weight, size, hardness, disintegration time, and physical appearance of the film-coated tablets.
 Results: The four variations (Film Coated Tablet, FCT 5, 6, 7, and 8%) in weight gain of film-coated tablets showed the physical appearance results per the applicable requirements. However, the physical observation test at room temperature showed the instability of the film-coated tablet. The qualitative analysis of thin-layer chromatography showed that the productive substances in the extracts, tablet cores, and film-coated tablets were still contained even though they had undergone several formulation stages.
 Conclusion: Film-coated tablets met the standards of the Indonesian Pharmacopoeia and the United States Pharmacopeia. After two weeks, there was slight instability in film-coated tablets at room temperature storage. The extract, tablet core, and film-coated tablet contain flavonoids.

The effect of partially pregelatinized cassava starch as disintegrant for paracetamol tablet

The use of partially pregelatinized starch in tablet formulations is entirely various; one of them is disintegrant. Present pregelatinized starch is imported from another country, which is relatively expensive. In contrast, many plants can be used as starch sources, including cassava which is relatively abundant in Indonesia. This study aimed to determine the effect of using partially pregelatinized starch from cassava as a disintegrant in paracetamol tablets. In this study, seven formulas were used with different disintegrants, three formulas using partially pregelatinized starch from cassava with concentrations of F1 5%, F2 10%, and F3 15%, three formulas using Starch 1500 with the same concentration as partially pregelatinized starch from cassava and one control formula without disintegrant. The tablet was made using the wet granulation method. The tablets produced were tested for physical properties (hardness, disintegration, and dissolution). In addition, compact ability of partially pregelatinized starch from cassava was compared with Avicel, Starch 1500, and cassava starch. Based on the results of the study showed that partially pregelatinized starch from cassava produced tablets that tended to be capping with less hardness than tablets with Starch 1500 and control tablets. The compact ability test results showed that the compact ability of partially pregelatinized starch from cassava was better than Starch 1500 and cassava starch. The disintegration test results showed that tablets with partially pregelatinized starch from cassava had faster disintegration than tablets with Starch 1500 and control tablets. The dissolution profile of tablets with partially pregelatinized starch from cassava is also better than other formulas.

Preparation and Evaluation of Sustained Release Tablet of Rifaximin by using Cross linked Sodium Alginate

Rifaximin treats traveler's diarrhea and irritable bowel syndrome by stopping the growth of the bacteria that cause diarrhea. Rifaximin treats hepatic encephalopathy by stopping the growth of bacteria that produce toxins and that may worsen liver disease. The short half life and high frequency of administration of drug makes it a suitable candidate for designing sustained drug delivery system. The aim of the present investigation was to develop a sustained release matrix tablet of Rifaximin using sodium alginate and cross linked sodium alginate and to evaluate the drug release kinetics. In order to achieve the required sustained release profile, the tablets were prepared by a wet granulation method. The formulated tablets were characterized for pre-compression and post-compression parameters and they were in the acceptable limits. The drug release data obtained after an in vitro dissolution study was fitted to various release kinetic models in order to evaluate the release mechanism and kinetics. The criterion for selecting the best fit model was linearity (coefficient of correlation). Drug release mechanism was found to follow a complex mixture of diffusion, swelling and erosion. The dosage form holds the potential to control the release rate of drug and extend the duration of action of a drug.

The Use of Ambon Banana Starch (Musa paradisiaca var. sapientum L.) as a New Binder in Tablet Formulation

Background: Synthetic materials are commonly used as binders in tablet formulations, this causes the price of tablets to be more expensive. For this reason, new discoveries are sought that can replace synthetic materials by utilizing materials from nature. One of the binders that comes from natural ingredients and is easily obtained is the Ambon Banana Starch (Musa paradisiaca var. sapientum (L.)). Objectives: This study was conducted to determine the physical characteristics of paracetamol tablets from Ambon banana starch (Musa paradisiaca var. sapientum L.) as a binder. Materials and Methods: Paracetamol tablets were compressed using the wet granulation method by adding a binder in the form of Ambon banana starch mucilago. The consentration of Ambon banana starch used was Formula I (15%), Formula II (17.5%) and Formula III (20%). Evaluation of the physical characteristics of the preparation is determined through the parameters of granule testing and tablet testing. Results: Formulation I, II, and III have met the requirements for the granule test. Meanwhile, in tablet testing, the results of size uniformity test, weight uniformity test, hardness test, and disintegration time test met the requirements for all formulations. However, in the friability test, Formula I (15%) did not meet the requirements with a value of 2.07% (requirement <1%), while formulas II and III had met the requirements. Conclusions: This study showed that Ambon banana starch can be used as a binder in tablet formulation.

EFFECT OF ZEIN ON CIPROFLOXACIN FLOATING TABLETS

Objective: This work was aimed to formulate and evaluate the effect of zein on Ciprofloxacin HCl floating tablets. According to previous studies, it was set up to be useful against bacteria i.e. Helicobacter pylori which leads to peptic ulcers. Thus, it is quite necessary to enhance the Gastric Retention Time for similar medicines. Methods: 12 different floating tablets of Ciprofloxacin HCl were formulated with wet granulation method with a rise in the concentration of zein. Further, all different formulations prepared were evaluated for different parameters i.e. pre-compression considerations, along with post-compression factors like weight variation, content uniformity, thickness, visual assessment, hardness, friability, buoyancy studies i.e. total floating time as well as floating lag time, swelling index, dissolution and drug release kinetics. Results: The F6 formulation was considered to be among finest formulation with appropriate hardness. It was found that with the increasing concentration of zein, the hardness of tablets was also increased. It showed TFT of more than 7 h, FLT of 310 sec, a swelling index time of 99.5 % in 4 hr, while drug release kinetics was found to follow Higuchi Model. Conclusion: Overall it was also found that HPMCK-100M is more effective as compared to HPMC-K15M and Zein has a major role in increasing the hardness of tablets. In the future, the investigation will be continued with the following studies: An in vivo study and a long-term stability study.

Diluent performance of a three component co-processed excipient for formulating ibuprofen tablets by wet granulation

Pharmaceutical tablets ingested orally remain the most popular dosage form in drug delivery, while the most frequently used route for administration of therapeutic agents remains the oral route. Recently, excipient development comprising a mixture of two or more materials assembled in a single frame by means of particle engineering, known as co-processed excipients, has gained enormous popularity. To prepare ibuprofen tablets by co-processing and wet granulation method and evaluate its diluent property. From the design of experiment (DOE), the optimized composition was obtained and ibuprofen granules were prepared for the newly developed co-processed excipient (lactose, mucin and corn starch BP) and starlac®, cellactose® and lactose as standards. The granules were evaluated for their micromeritic properties and compressed into tablets. Evaluation of the ibuprofen tablets for their physical properties and dissolution studies were done using British Pharmacopoeia methods. The results obtained showed that ibuprofen granules were flowable and compressible. The compressed ibuprofen tablets had good physical properties: minimal weight variation (495±9.46 – 501mg ±23.15), hardness (5.50 ±0.55 – 6.50±1.05 KgF), disintegration “time” < 15 min±0.37 and “friability” < 1.0 % ±0.00 - >1.0±0.07. The dissolution of ibuprofen tablets complied with British Pharmacopoeia criteria. The data obtained from the different evaluation parameters containing the co-processed excipient compared well with starlac, cellactose and lactose used as comparing standard. The co-processed excipient which performed better than starlac in terms of friability and lactose in terms of disintegration can serve as a good diluent in ibuprofen tablets.

Formulasi Granul Effervescent Ekstrak Aseton Rimpang Kencur (Kaempferia Galanga L.) dengan Variasi Konsentrasi Polivinilpirolidon

Kencur is one of the plants that is useful as an anthelmintic drug. This study aims to formulate effervescent granules of acetone extract of Kencur rhizome (Kaempferia galanga L.) with various concentrations of polyvinylpyrrolidone. Kencur rhizome extraction was carried out by maceration method using acetone solvent for 3 days then filtered and concentrated with a rotary vacuum evaporator. The extract was granulated using the wet granulation method with a ratio of citric acid monohydrate and tartaric acid 1:2. Variations in PVP concentrations were 2%, 4%, and 6%. Physical evaluation of granules includes Density and Porosity, Compressibility Index (Carr Index), Flow Time, and Angle of Bed. The best porosity was in formula 3 with 30.47±1.471. The compressibility index (Carr Index) of the three formulas is in the range of 515%. The best dosage flow times were formulas 2 and 3 with 8.67±0.526 and 7.58±0.344. The Hausner Ratio of the three formulas is below 1.25. The angles of repose in formulas 1 and 2 are 24.94º and 29.74º with a recline angle <40. The foam stopping time is 23 seconds. From theresults abtained it can be concluded that the formula with good pharmaceutical properties is formula 3 with a variation of 6% pvp concentration.

Probiotic-Assisted Colon-Specific Delivery of Anti-Inflammatory Drug – 5 ASA

Background: Mesalamine, one derivative of 5-aminosalicylic acid (5-ASA), has been recommended as the first-line medicine to induce and maintain remission in patients with mild-to-moderately active ulcerative colitis on account of its efficacy and safety. Objective: To evaluate the efficacy and safety of mesalamine in conjunction with probiotics for ulcerative colitis an ideal colon targeting system aims to deliver a therapeutic agent, selectively and effectively, to the colon. This system should ideally retain the drug release in the upper GI tract (stomach and small intestine); while trigger the drug release in the colon. Several approaches have been used to fabricate formulations to achieve a colon specific delivery of mesalamine such as; time dependent, enzymatic/microbial responsive approaches. This overview outlines the recent advances in mesalamine-colon delivery approaches for the potential treatment of ulcerative colitis and Crohn’ disease. Method: The matrix tablets of guar gum were prepared by wet granulation method Lactose, guar gum, talc and magnesium stearate were sifted separately through sieve number 60 to obtain particles of uniform size. Weighed quantity of Mesalamine was sifted through sieve number 100. Result: Matrix tablets containing Mesalamine were prepared by wet granulation method using guar gum as the colon targeting polymer and varying concentrations of probiotics Sporlac and Vivaflora to assist in colon targeting.

Effect of binder type on physical and in vitro properties of high dose inosine acedoben dimepranol tablets

The present work was conducted with the aim to formulate and evaluate the immediate release of 1000 mg tablets containing Inosine Acedoben Dimepranol (IAD). All the samples of the tablets containing 1000 mg IAD were prepared by conventional wet granulation method. Various type of binders like povidone, wheat starch, pregelatinized starch (starch 1500TM , Colorcon), microcrystalline cellulose and macrogol 6000 were used to prepare some series of tablets. Granules were evaluated for pre-compression parameters and tablets were evaluated for post- compression parameters. The composition batch № IAD1000 L04 was found to be the best for producing IAD 1000 mg tablets. The optimal lubricant system is glycerol dibehenate at a concentration of 2.94% plus magnesium stearate at a concentration of 0.46%. Optimized formulation was evaluated for in-vitro dissolution test. Stability studies were performed for the selected composition.

Effect of Hydrophilic Polymers on the Release Rate and Pharmacokinetics of Acyclovir Tablets Obtained by Wet Granulation: In Vitro and In Vivo Assays.

This study aims to evaluate the feasibility of producing acyclovir-containing modified release matrix tablets by a wet granulation method based on the type and concentration of two pharmaceutical-grade hydrophilic matrix polymers (i.e., hydroxypropyl methylcellulose (HPMC), carbomers, and their combinations) commonly used in biomedical applications. The mechanical properties of the tablets and in vitro and in vivo performance were studied. The physicochemical properties of the raw materials and corresponding physical mixtures were characterized by differential scanning calorimetry, showing that the hydrophilic polymers did not influence the physicochemical properties of the drug. The wet granulation process improved the flow and compression properties of the obtained granules. This method enabled the preparation of the matrix tablets of acyclovir with appropriate mechanical properties concerning hardness and friability. The drug release kinetics was governed by the type and concentration of the hydrophilic polymers composing the matrices. The study has proven that HPMC-composed tablets were superior in modified drug release properties compared to carbomer- and HPMC/carbomer-based tablets. Mathematical analysis of the release profiles, determined in a medium adjusted to pH 1.2 followed by pH 7.4, revealed that the drug released from the hydrophilic tablets followed non-Fickian first-order kinetics. An optimal HPMC-based formulation submitted to accelerated stability studies (40 °C, 75% RH) was stable for three months. A complete cross-over bioavailability study of the selected acyclovir-loaded sustained release tablets and marketed immediate-release tablets were compared in six healthy male volunteers. The extent of drug absorption from the sustained release tablets was significantly greater than that from immediate-release pills, which may improve the drug’s antiviral properties attributed to the lower elimination rate and enhanced acyclovir half-life.