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1.
Curr Pharm Teach Learn ; 9(6): 1170-1179, 2017 Nov.
Article in English | MEDLINE | ID: mdl-29233388

ABSTRACT

BACKGROUND: In the past decade, various health care programs have implemented diverse types of peer-assisted learning (PAL) programs, in particularly peer teaching (PT), due to their reported benefits for students (both those undertaking teaching and those being taught), teachers, and educational institutes. Unfortunately, peer teaching is still under-recognized in pharmacy programs worldwide when compared to other health care programs. The aim of this review is to provide an overview of the published literature centered on formal PT programs that are implemented in pharmacy schools. In addition, this review focuses on the methodologies adopted for peer teacher recruitment and training as well as the benefits gained by students (both those undertaking teaching and those being taught). The rationales behind PT implementation are recapitulated as well. Finally, a simple scheme for successful implementation of PT activity is provided to serve as a groundwork for educators. METHODS: Pre-defined key terms were used to search for experimental peer teaching activities in pharmacy schools between January 2000 and June 2016. Titles were selected based on pre-set eligibility criteria. Only complete research articles with clear design and evaluation sections were included in this review. Studies about inter-professional peer teaching activities between pharmacy students and other healthcare professions were also included. RESULTS: Six relevant educational research articles containing peer teaching activities were included. A lot of variety exists between different pharmacy courses implementing PT, the format/setting of PT, how peer teachers are selected, and how training and evaluation are implemented. The studies reviewed confirmed that PT was well received by most of the students and had a positive impact on their learning outcome. These findings cannot be generalized due to the insufficient number of studies published beside their methodological limitations and inadequate descriptions of the PT format. IMPLICATIONS: Though PT may be regarded as a feasible teaching strategy, care must be taken during implementation to ensure the fulfillment of the educational objectives. Proper validation of any PT initiative is required before incorporation into the pharmacy curriculum. More research using proper design and suitable sample sizes are recommended to determine the effect of PT activity on students' learning, skills development and confidence.


Subject(s)
Education, Pharmacy/methods , Peer Group , Teaching/standards , Curriculum/trends , Humans , Schools, Pharmacy/trends , Students, Pharmacy , Teaching/trends
2.
Drug Deliv ; 23(7): 2205-2219, 2016 Sep.
Article in English | MEDLINE | ID: mdl-25188303

ABSTRACT

Most of the newly designed drug molecules are lipophilic in nature and often encounter erratic absorption and low bioavailability after oral administration. Finding ways to enhance the absorption and bioavailability of these lipophilic drugs is one of the major challenges that face pharmaceutical industry nowadays. In view of that, the purpose of this review is to shed some light on a novel particulate self-assembling system named "beads" than can act as a safe carrier for delivering lipophilic drugs. The beads are prepared simply by mixing oils with cyclodextrin (CD) aqueous solution in mild conditions. A unique interaction between oil components and CD molecules occurs to form in situ surface-active complexes which are prerequisites for beads formation. This review mainly focuses on the fundamentals of beads preparation through reviewing present, yet scarce, literature. The key methods used for beads characterization are discussed in details. Also, the potential mechanisms by which beads increase the bioavailability of lipophilic drugs are illustrated. Finally, the related research areas that needs to be addressed in future for optimizing this promising delivery system are briefly outlined.


Subject(s)
Cyclodextrins/chemistry , Cyclodextrins/metabolism , Triglycerides/chemistry , Triglycerides/metabolism , Administration, Oral , Animals , Biological Availability , Drug Carriers/chemistry , Drug Delivery Systems/methods , Humans
3.
Drug Deliv ; 23(6): 1847-67, 2016 Jul.
Article in English | MEDLINE | ID: mdl-25390191

ABSTRACT

Most of the new drugs, biological therapeutics (proteins/peptides) and vaccines have poor performance after oral administration due to poor solubility or degradation in the gastrointestinal tract (GIT). Though, vesicular carriers exemplified by liposomes or niosomes can protect the entrapped agent to a certain extent from degradation. Nevertheless, the harsh GIT environment exemplified by low pH, presence of bile salts and enzymes limits their capabilities by destabilizing them. In response to that, more resistant bile salts-containing vesicles (BS-vesicles) were developed by inclusion of bile salts into lipid bilayers constructs. The effectiveness of orally administrated BS-vesicles in improving the performance of vesicles has been demonstrated in researches. Yet, these attempts did not gain considerable attention. This is the first review that provides a comprehensive overview of utilizing BS-vesicles as a promising pharmaceutical carrier with a special focus on their successful applications in oral delivery of therapeutic macromolecules and vaccines. Insights on the possible mechanisms by which BS-vesicles improve the oral bioavailability of the encapsulated drug or immunological response of entrapped vaccine are explained. In addition, methods adopted to prepare and characterize BS-vesicles are described. Finally, the gap in the scientific researches tackling BS-vesicles that needs to be addressed is highlighted.


Subject(s)
Bile Acids and Salts/metabolism , Drug Carriers/chemistry , Peptides/metabolism , Vaccines/chemistry , Vaccines/therapeutic use , Water/chemistry , Administration, Oral , Bile Acids and Salts/chemistry , Biological Availability , Chemistry, Pharmaceutical , Lipid Bilayers/chemistry , Liposomes , Peptides/chemistry , Solubility , Vaccines/immunology
4.
Pharm Dev Technol ; 21(6): 706-15, 2016 Sep.
Article in English | MEDLINE | ID: mdl-25996631

ABSTRACT

To circumvent the low and erratic absorption of orally administrated cinnarizine (CN), intranasal lyophilized gels containing unsaturated fatty acid liposomes (ufasomes) and encapsulating CN were prepared from oleic acid using a simple assembling strategy. The effects of varying drug concentration and cholesterol percentage on ufasomes size, polydispersity index and entrapment efficiency were investigated using 3(1)4(1) full factorial design. The optimized ufasomes that contained 14% cholesterol relative to oleic acid displayed spherical morphology with average size of 788 nm and entrapment efficiency of 80.49%. To overcome the colloidal instability of CN-loaded ufasomes dispersions and their short residence time in the nasal cavity, the ufasomes were incorporated into mucoadhesive hydrogels that were lyophilized into unit dosage forms for accurate dosing. Scanning electron micrographs of the lyophilized gel revealed that the included ufasomes were intact, non-aggregating and maintained their spherical morphology. Rheological characterization of reconstituted ufasomal lyophilized gel ensured ease of application. Furthermore, the gel induced minor histopathological alterations in sheeps' nasal mucosa. Ex-vivo confocal laser imaging confirmed the ability of ufasomes to penetrate deep through nasal mucosa layers. The results highlighted in the current work confirm the feasibility of using CN-loaded ufasomal gels for intranasal drug delivery.


Subject(s)
Cinnarizine/pharmacokinetics , Drug Delivery Systems/methods , Nanoparticles/metabolism , Nasal Mucosa/drug effects , Administration, Intranasal , Animals , Cinnarizine/administration & dosage , Cinnarizine/chemistry , Drug Liberation/drug effects , Drug Liberation/physiology , Freeze Drying/methods , Histamine H1 Antagonists/administration & dosage , Histamine H1 Antagonists/chemistry , Histamine H1 Antagonists/pharmacokinetics , Liposomes , Microscopy, Confocal/methods , Nanoparticles/administration & dosage , Nanoparticles/chemistry , Nasal Mucosa/metabolism , Nasal Mucosa/pathology , Sheep
5.
Am J Pharm Educ ; 79(4): 59, 2015 May 25.
Article in English | MEDLINE | ID: mdl-26089568

ABSTRACT

The shift in the pharmacist's role from simply dispensing medications to effective delivery of pharmaceutical care interventions and drug therapy management has influenced pharmacy education.(1-3) The educational focus has shifted from basic sciences to clinical and integrated courses that require incorporating active-learning strategies to provide pharmacy graduates with higher levels of competencies and specialized skills. As opposed to passive didactic lectures, active-learning strategies address the educational content in an interactive learning environment to develop interpersonal, communication, and problem-solving skills needed by pharmacists to function effectively in their new roles.(4-6) One such strategy is using educational games. The aim of this paper is to review educational games adopted in different pharmacy schools and to aid educators in replicating the successfully implemented games and overcoming deficiencies in educational games. This review also highlights the main pitfalls within this research area.


Subject(s)
Education, Pharmacy/methods , Games, Experimental , Teaching , Audiovisual Aids , Curriculum , Humans , Learning , Pharmacists , Problem-Based Learning , Students, Pharmacy
6.
Pharmacy (Basel) ; 3(3): 89-100, 2015 Jul 27.
Article in English | MEDLINE | ID: mdl-28975906

ABSTRACT

Like most of the pharmacy colleges in developing countries with high population growth, public pharmacy colleges in Egypt are experiencing a significant increase in students' enrollment annually due to the large youth population, accompanied with the keenness of students to join pharmacy colleges as a step to a better future career. In this context, large lectures represent a popular approach for teaching the students as economic and logistic constraints prevent splitting them into smaller groups. Nevertheless, the impact of large lectures in relation to student learning has been widely questioned due to their educational limitations, which are related to the passive role the students maintain in lectures. Despite the reported feebleness underlying large lectures and lecturing in general, large lectures will likely continue to be taught in the same format in these countries. Accordingly, to soften the negative impacts of large lectures, this article describes a simple and feasible 5-step paper-based model to transform lectures from a passive information delivery space into an active learning environment. This model mainly suits educational establishments with financial constraints, nevertheless, it can be applied in lectures presented in any educational environment to improve active participation of students. The components and the expected advantages of employing the 5-step paper-based model in large lectures as well as its limitations and ways to overcome them are presented briefly. The impact of applying this model on students' engagement and learning is currently being investigated.

7.
J Liposome Res ; 25(2): 107-21, 2015.
Article in English | MEDLINE | ID: mdl-25058447

ABSTRACT

Oro-dental diseases are generally associated with pain that is controlled using oral tablets containing NSAIDs. Lornoxicam, a relatively new NSAID, is effective in relieving pain accompanying different oro-dental problems. The aim of the current research is to prepare oro-dental analgesic and anti-inflammatory gel using provesicular approach to deliver lornoxicam directly to the site of action in the oral cavity. Local administration of lornoxicam is expected to be superior to systemic delivery in pain relieving and poses less GIT adverse effects. Different surfactants were utilized to prepare the proniosomal gels that rapidly transform into nano-sized niosomes after hydration with the oral saliva. The effect of the surfactant structure on vesicles size distribution and entrapment efficiency percentage (EE%) was investigated. The proniosomal formulations were incorporated into carbopol hydrogels that were characterized regarding rheological and mucoadhesion properties. Moreover, ex-vivo mucosal membrane permeation studies were conducted for selected proniosomal gels to quantify the permeation parameters and assess the amount of drug deposited within the oral mucosa. Results revealed that mucoadhesive proniosomes formulation prepared using Span 60 was optimal as it was nano-sized and also showed the highest EE%. The transmucosal flux of lornoxicam, from these proniosomal formulations, across the oral mucosa was significantly higher (p < 0.05) than lornoxicam containing carbopol gel and the percent drug diffused increased more than twofolds. The results collectively suggest that the mucoadhesive proniosomal gels can be assertively considered as a promising carrier for transmucosal delivery of lornoxicam into the oral cavity.


Subject(s)
Liposomes/chemistry , Pain/drug therapy , Piroxicam/analogs & derivatives , Analgesics/administration & dosage , Analgesics/chemistry , Analgesics/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Candidiasis, Oral/complications , Gels , Humans , Molecular Structure , Pain/complications , Piroxicam/administration & dosage , Piroxicam/chemistry , Piroxicam/therapeutic use , Surface-Active Agents/chemistry
8.
Int J Nanomedicine ; 9: 5449-60, 2014.
Article in English | MEDLINE | ID: mdl-25473283

ABSTRACT

Spironolactone (SL) is a US Food and Drug Administration-approved drug for the treatment of hypertension and various edematous conditions. SL has gained a lot of attention for treating androgenic alopecia due to its potent antiandrogenic properties. Recently, there has been growing interest for follicular targeting of drug molecules for treatment of hair and scalp disorders using nanocolloidal lipid-based delivery systems to minimize unnecessary systemic side effects associated with oral drug administration. Accordingly, the objective of this study is to improve SL efficiency and safety in treating alopecia through the preparation of colloidal nanostructured lipid carriers (NLCs) for follicular drug delivery. SL-loaded NLCs were prepared by an emulsion solvent diffusion and evaporation method using 23 full factorial design. All of the prepared formulations were spherical in shape with nanometric size range (215.6-834.3 nm) and entrapment efficiency >74%. Differential scanning calorimetry thermograms and X-ray diffractograms revealed that SL exists in amorphous form within the NLC matrices. The drug release behavior from the NLCs displayed an initial burst release phase followed by sustained release of SL. Confocal laser scanning microscopy confirmed the potential of delivering the fluorolabeled NLCs within the follicles, suggesting the possibility of using SL-loaded NLCs for localized delivery of SL into the scalp hair follicles.


Subject(s)
Drug Carriers/chemistry , Hair Follicle/metabolism , Lipids/chemistry , Nanostructures/chemistry , Spironolactone/chemistry , Spironolactone/pharmacokinetics , Alopecia , Animals , Hair Follicle/chemistry , Mice , Models, Chemical , Rhodamines/chemistry , Rhodamines/pharmacokinetics , Skin/chemistry , Skin/metabolism
9.
Int J Pharm ; 422(1-2): 139-50, 2012 Jan 17.
Article in English | MEDLINE | ID: mdl-22079716

ABSTRACT

Diphenyl dimethyl bicarboxylate (DDB) is a hepatocurative agent used for treatment of various liver diseases. However, DDB therapeutic effectiveness is restricted by its low oral bioavailability that arises from its poor solubility and dissolution. Aiming at surmounting the aforementioned restrictions, DDB provesicular dry powders exemplified by proniosomes and proliposomes were prepared using film-deposition technique employing sorbitol as a carrier. Upon dilution with water, the provesicular powders rapidly transformed into vesicular dispersions, either liposomes or niosomes, which were characterized regarding their percent encapsulation efficiency (EE%), vesicle size and distribution, morphology and in vitro drug release. The revealed optimal provesicular powder was exposed to solid state characterization, stability testing and in vivo performance evaluation. Results showed that provesicular powders with acceptable flowability can be prepared using a weight ratio of lipids mixture to sorbitol of 1:20. Proniosomal powder composed of Tween 80:cholesterol:stearylamine in molar ratio 7:3:0.5 loaded on sorbitol was selected as the optimal formulation as it showed the highest EE% and dissolution enhancement for DDB. The elevated levels of liver enzymes in hepatically injured Albino Wister rats were significantly reduced (P<0.05) after oral administration of the optimal proniosomal powder in comparison to free DDB. This improvement was confirmed histopathologically by minimizing the associated hepatic injury. Accordingly, proniosomes can be assertively considered as a promising stable precursor for immediate preparation of niosomal carrier for DDB with enhanced dissolution and hepatocurative activity.


Subject(s)
Chemical and Drug Induced Liver Injury/drug therapy , Dioxoles/pharmacology , Liver/drug effects , Administration, Oral , Alanine Transaminase/blood , Animals , Aspartate Aminotransferases/blood , Biomarkers/blood , Calorimetry, Differential Scanning , Carbon Tetrachloride , Chemical and Drug Induced Liver Injury/enzymology , Chemical and Drug Induced Liver Injury/pathology , Chemistry, Pharmaceutical , Dioxoles/administration & dosage , Dioxoles/chemistry , Disease Models, Animal , Drug Compounding , Liposomes , Liver/enzymology , Liver/pathology , Male , Microscopy, Electron, Transmission , Particle Size , Polysorbates/chemistry , Powder Diffraction , Powders , Rats , Rats, Wistar , Rheology , Solubility , Sorbitol/chemistry , Spectroscopy, Fourier Transform Infrared , Technology, Pharmaceutical/methods , Time Factors , Water/chemistry , X-Ray Diffraction
10.
AAPS PharmSciTech ; 12(4): 1335-47, 2011 Dec.
Article in English | MEDLINE | ID: mdl-21979886

ABSTRACT

The bioavailability of therapeutic agents from eye drops is usually limited due to corneal barrier functions and effective eye protective mechanisms. Therefore, the current study aims to enhance ocular bioavailability of brimonidine, a potent antiglaucoma drug, through the preparation of ocular inserts. Solvent casting technique was employed to prepare the inserts using polyvinylpyrrolidone K-90 (PVP K-90) as film-forming polymer blended with different viscosity grades of bioadhesive polymers namely hydroxypropyl methycellulose, carbopol, sodium alginate, and chitosan. The prepared ocular inserts were evaluated for various physicochemical parameters, swelling behavior, and in vitro release patterns. Sodium alginate-based ocular inserts revealed the most sustainment in drug release (99% at 6 h), so it was selected for further modifications via coating it, on one side or dual sides, using hydrophobic film composed of either ethylcellulose or Eudragit RSPO. The obtained in vitro release results for the modified ocular inserts revealed that ethylcellulose is superior to Eudragit RSPO in terms of brimonidine release sustainment effect. Ocular inserts composed of 7% PVP K-90, 1.5% low molecular weight sodium alginate with or without ethylcellulose coat were able to sustain the in vitro release of brimonidine. Their therapeutic efficacy regarding intraocular pressure (IOP) lowering effect when inserted in albino rabbits eyes showed superior sustainment effect compared with that of brimonidine solution. Furthermore, due to both the mucoadhesive property and the drug sustainment effect, the one-side-coated ocular insert showed more IOP lowering effect compared with that of its non-coated or dual-side-coated counterpart.


Subject(s)
Absorbable Implants , Adrenergic alpha-2 Receptor Agonists/administration & dosage , Drug Carriers , Polymers/chemistry , Quinoxalines/administration & dosage , Acrylic Resins , Administration, Ophthalmic , Adrenergic alpha-2 Receptor Agonists/chemistry , Alginates/chemistry , Animals , Brimonidine Tartrate , Calorimetry, Differential Scanning , Cellulose/analogs & derivatives , Cellulose/chemistry , Chemistry, Pharmaceutical , Chitosan/chemistry , Delayed-Action Preparations , Disease Models, Animal , Drug Compounding , Glaucoma/drug therapy , Glaucoma/physiopathology , Glucuronic Acid/chemistry , Hexuronic Acids/chemistry , Hydrophobic and Hydrophilic Interactions , Hypromellose Derivatives , Intraocular Pressure/drug effects , Kinetics , Methylcellulose/analogs & derivatives , Methylcellulose/chemistry , Ophthalmic Solutions , Polymethacrylic Acids/chemistry , Polyvinyls/chemistry , Povidone/chemistry , Quinoxalines/chemistry , Rabbits , Solubility , Spectroscopy, Fourier Transform Infrared , Technology, Pharmaceutical/methods , X-Ray Diffraction
11.
Pharm Dev Technol ; 16(4): 316-30, 2011 Aug.
Article in English | MEDLINE | ID: mdl-20307250

ABSTRACT

Novel fast-disintegrating multi-unit tablets (FDMUTs) were prepared to modify the release of lornoxicam (a potent non-steroidal anti-inflammatory drug with a short half-life) as well as to combine the advantages of multi-unit systems with the cost-effectiveness of compressed tablets. The proposed FDMUTs consisted of sustained-release lornoxicam beads directly compressed with fast-disintegrating component, containing amorphous solid dispersion of lornoxicam, anticipating rapid drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain extended analgesic effect. Initially, calcium-alginate and chitosan-alginate beads containing lornoxicam were prepared. Then, the erosion of selected beads formulation was suppressed by treatment with Eudragit RS either through polymer-reinforcement or beads coating. The beads, which elicited appropriate sustainment of lornoxicam release, were directly compressed with fast-disintegrating components to form FDMUTs. The release characteristics of the original beads were maintained after compression which indicates that the adopted compression process did not induce mechanical damage to the beads or coating. All of the prepared FDMUTs demonstrated acceptable physical properties that complied with compendial requirements. Release studies, performed in simulated gastric and intestinal fluids used in sequence to mimic the gastrointestinal transit, illustrate that the FDMUTs containing 8?mg lornoxicam equally distributed between the sustained-release beads and the fast-release component, showed the desired release profile.


Subject(s)
Acrylic Resins/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Delayed-Action Preparations/chemistry , Piroxicam/analogs & derivatives , Alginates/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Chemical Phenomena , Chitosan/administration & dosage , Drug Carriers/chemistry , Drug Compounding/methods , Drug Stability , Excipients/administration & dosage , Excipients/chemistry , Gastric Juice/metabolism , Gastrointestinal Transit , Glucuronic Acid/administration & dosage , Hexuronic Acids/administration & dosage , Humans , Hydrogen-Ion Concentration , Intestinal Secretions/metabolism , Piroxicam/administration & dosage , Piroxicam/pharmacokinetics , Solubility , Tablets
12.
Drug Dev Ind Pharm ; 36(3): 337-49, 2010 Mar.
Article in English | MEDLINE | ID: mdl-19722915

ABSTRACT

OBJECTIVE: The objective of this study was to modify the release characteristics of lornoxicam, a highly potent nonsteroidal anti-inflammatory drug, by preparing compression-coated tablets (CCTs) that provide complete drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain prolonged analgesic effect as well as meets the reported sustained release specifications. METHODS: Each of the prepared CCTs was composed of a sustained release tablet core and an immediate release coat layer. Amorphous, well-characterized, freeze-dried solid dispersion of lornoxicam with polyvinylpyrrolidone K-30 was employed in the coat layer to attain an initial rapid dissolution of lornoxicam in the stomach, assuring rapid onset of analgesic effect. Compritol ATO 888, a lipophilic matrix-forming material, was included in the core tablets to sustain lornoxicam release. Lactose was also incorporated into these core tablets to ensure complete release of lornoxicam in a time period comparable to the gastrointestinal residence time. RESULTS: All the prepared CCTs showed acceptable physical properties that complied with compendial requirements. On the basis of in vitro drug release studies, performed in simulated gastric and intestinal fluids in sequence to mimic the gastrointestinal transit, CCTs belonging to formulations F3 CCTs and F4 CCTs were able to show the desired release profile. CONCLUSION: This study demonstrated the possibility of modulating lornoxicam release using CCTs to meet the reported sustained release specifications.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Excipients/chemistry , Piroxicam/analogs & derivatives , Calorimetry, Differential Scanning , Chemical Phenomena , Chemistry, Pharmaceutical , Delayed-Action Preparations/chemistry , Drug Compounding/methods , Fatty Acids/chemistry , Gastrointestinal Transit , Humans , Hydrogen-Ion Concentration , Lactose/chemistry , Piroxicam/administration & dosage , Piroxicam/chemistry , Povidone/chemistry , Solubility , Spectroscopy, Fourier Transform Infrared , Surface Properties , Suspensions , Tablets , Time Factors , X-Ray Diffraction
13.
Pharm Dev Technol ; 15(2): 139-53, 2010.
Article in English | MEDLINE | ID: mdl-19895367

ABSTRACT

The short half-life of lornoxicam, a potent non-steroidal anti-inflammatory drug, makes the development of sustained-release (SR) forms extremely advantageous. However, due to its weak acidic nature, its release from SR delivery systems is limited to the lower gastrointestinal tract which consequently leads to a delayed onset of its analgesic action. Accordingly, the aim of this study was to develop lornoxicam SR matrix tablets that provide complete drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain protracted analgesic effect as well as meets the reported SR specifications. The proposed strategy was based on preparing directly compressed hydroxypropylmethylcellulose matrix tablets to sustain lornoxicam release. Basic pH-modifiers, either sodium bicarbonate or magnesium oxide, were incorporated into these matrix tablets to create basic micro-environmental pH inside the tablets favorable to drug release in acidic conditions. All the prepared matrix tablets containing basic pH-modifiers showed acceptable physical properties before and after storage. Release studies, performed in simulated gastric and intestinal fluids used in sequence to mimic the GI transit, demonstrate the possibility of sustaining lornoxicam release by combining hydrophilic matrix formers and basic pH-Modifiers to prepare tablets that meet the reported sustained-release specifications.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Excipients/chemistry , Piroxicam/analogs & derivatives , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Delayed-Action Preparations , Drug Carriers/chemistry , Drug Stability , Drug Storage , Gastric Juice/metabolism , Half-Life , Humans , Hydrogen-Ion Concentration , Hypromellose Derivatives , Intestinal Secretions/metabolism , Magnesium Oxide/chemistry , Methylcellulose/analogs & derivatives , Methylcellulose/chemistry , Piroxicam/administration & dosage , Piroxicam/pharmacokinetics , Sodium Bicarbonate/chemistry , Tablets
14.
AAPS PharmSciTech ; 10(4): 1357-67, 2009.
Article in English | MEDLINE | ID: mdl-19921543

ABSTRACT

The objective of the present study was to develop new directly compressed, double-layer tablets (DLTs) of lornoxicam, a highly potent nonsteroidal anti-inflammatory drug with short half-life, that are characterized by initial burst drug release in the stomach and comply with the release requirements of sustained-release products. Each of the proposed DLTs is composed of a fast-release layer and a sustained-release layer, anticipating rapid drug release that starts in the stomach to rapidly alleviate the symptoms and continues in the intestine to maintain protracted analgesic effect. An amorphous, freeze-dried inclusion complex of lornoxicam with hydroxypropyl-beta-cyclodextrin, present in 1:2 (drug/cyclodextrin) molar ratio, was employed in the fast-release layer to enhance the dissolution of lornoxicam in the stomach and assure rapid onset of its analgesic effect. Xanthan gum (XG), a hydrophilic matrix-forming agent, was integrated in the sustained-release layer to provide appropriate sustainment of drug release. The weight ratios between the sustained-release layer and fast-release layer present in DLTs were adjusted to reach optimal formulations. DLTs composed of sustained-release layer (40% XG) to fast-release layer in 2:1 weight ratio and those composed of sustained-release layer (50% XG) to fast-release layer in 1:1 weight ratio showed the desired release profile. The drug contained in the fast-release layer showed an initial burst drug release of more than 30% of its drug content during the first 30 min of the release study followed by gradual release of the drug for a period of 8 h.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Piroxicam/analogs & derivatives , Polysaccharides, Bacterial/administration & dosage , beta-Cyclodextrins/administration & dosage , 2-Hydroxypropyl-beta-cyclodextrin , Calorimetry, Differential Scanning , Delayed-Action Preparations , Drug Design , Piroxicam/administration & dosage , Piroxicam/chemistry , Solubility , Spectroscopy, Fourier Transform Infrared , Tablets , X-Ray Diffraction
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