DESIGN AND IN VITRO EVALUATION OF EXTENDED RELEASE TABLET OF NATEGLINIDE

The aim of present study is to formulate and evaluate extended release matrix tablet of Nateglinide by direct compression method using different polymer like HPMC K4 and HPMC K15. Matrix tablet of nateglidine were prepared in combination with the polymer HPMC K4, HPMC K15, along with the excipients and the formulations were evaluated for tablet properties and in vitro drug release studies. Nateglinide matrix tablet prepared by using polymer such as HPMC K4 and HPMC K15,  it was found that HPMC K15 having higher viscosity as compare to HPMC K4 therefore different concentration of polymer were studied to extend the drug release up to 12 h. The tablets of Nateglinide prepared by direct compression had acceptable physical characteristics and satisfactory drug release. The study demonstrated that as far as the formulations were concerned, the selected polymers proved to have an acceptable flexibility in terms of in-vitro release profile. In present the study the percent drug release for optimize batch was found to 94.62%.  Hence it can be conclude that Nateglinide extended release matrix tablet can prepared by using HPMC. The swollen tablet also maintains its physical integrity during the drug release study Keywords: Tablet, in-vitro drug release, Nateglinide, HPM

PREPARATION AND CHARACTERIZATION OF CO-CRYSTALS OF DIACEREIN

Diacerein, anti-inflammatory drug used in the treatment of osteoarthritis. Being a BCS class II drug, it has poor solubility, dissolution rate and other physicochemical properties. Thus the aim of present study was to prepare co-crystals of diacerein to improve solubility, dissolution rate. The diacerein co-crystals were prepared using urea and tartaric acid as conformer by Solvent drop grinding method. The diacerein co-crystals were characterized by scanning electron microscopy (SEM), FT-IR spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). The co-crystals were evaluated for solubility, dissolution rate and other physicochemical properties and compared with commercial diacern sample. The co-crystals exhibit the difference in the size and shape of crystals. The FT-IR spectra of diacerein co-crystals showed slightly different in the characteristic peaks compared to commercial diacerein sample. DSC data indicate the decrease in the melting endotherm of co-crystals compare to diacerein. The co-crystals with urea showed increase and intense peak and co-crystals with tartaric acid showed decreased number of peaks compared to commercial diacerein. The co-crystals of diacerein formulated in to the Tablet and evaluated for tablet properties. The tablet formulation showed improved tablet characteristics as well as dissolution rate compared to commercial diacerein

Formulation and Evaluation of Buccoadhesive Drug Delivery System for Lovastatin

Lovastatin, a hyperlipedemic agent used in the treatment of hypercholesterolemia, has poor bioavailability ( less than 5%) due to the first pass metabolism and thus the dosing frequency is more, as a result of which several side effects occurred with the current dosage form. The present study aimed to formulate and evaluate buccoadhesive tablets of Lovastatin using mucoadhesive polymer such as Carbopol 934P, Hydroxypropylmethyl cellulose (K4M, K100M) and sodium CMC. The different formulations of buccoadhesive tablet of Lovastatin were prepared by direct compression method and characterized for physicochemical parameters such as thickness, content uniformity, weight variation, hardness, and friability test. The swelling index, % matrix erosion, surface pH, bioadhesive strength, bioadhesive time and in-vitro drug release are also carried out which has been important aspect for success of buccoadhesive tablets. The FTIR study was carried out for drug and polymer compatibility.  All the formulation showed satisfactory tablet properties. Formulation (F5) containing Carbopol 934P and HPMC K4M in the ratio of (1:1) showed good bioadhesive strength and maximum drug release of 95.80% in 8 hours. The surface pH of all tablets was found to be satisfactory, close to buccal pH, hence no irritation would observe with these tablets. FTIR studies showed no evidence of interaction between drug and polymers. Keywords: Buccoadhesive tablets, Lovastatin, FTIR, Carbopol 934P, in-vitro drug releas

Modification of Physicochemical Properties of Active Pharmaceutical Ingredient by Pharmaceutical Co-Crystals

The oral drug delivery is widely used and accepted routes of administration, but it fails to provide the therapeutic effectiveness of drugs due to low solubility, poor compression and oral bioavailability. Crystal engineering is the branch where the modification of API is of great importance. Co-crystallization of API using a co-former is a hopeful and emerging approach to improve the performance of pharmaceuticals, such as micromeritic properties, solubility, dissolution profile, pharmacokinetics and stability. Pharmaceutical co-crystals are multicomponent systems in which one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients that are of GRAS category. In multidrug co-crystals one drug acts as API and other drug acts as coformer. This chapter illustrates the guidance for more efficient design and manufacture of pharmaceutical co-crystals with the desired physicochemical properties and applications

CO-CRYSTALS OF CARVEDILOL: PREPARATION, CHARACTERIZATION AND EVALUATION: CO-CRYSTALS OF CARVEDILOL

Carvedilol an antihypertensive drug, exhibit poor solubility and dissolution rate. Hence an attempt has been made to prepare the Co-crystals of Carvedilol to increase the solubility and dissolution rate by solvent evaporation method using coformer such as succinic acid, fumaric acid and oxalic acid. The prepared Co-crystals were evaluated for  solubility, dissolution rate and micromeritic properties. The Co-crystals were characterized by scanning electronic Microscopy (SEM), FT-Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-ray Diffractometry (XRD). The CAR-SA Co-crystal, CAR-FA Co-crystals and CAR-OA Co-crystals showed increased in solubility and dissolution rate compared to pure Carvedilol. The Co-crystals formed with coformer have showed improved micromeritic properties. SEM clearly showed the formation of new solid phase with the coformer. The FT-IR spectra indicate the shifting of characteristic peak in the Co-crystals but does not showed any interaction between the coformer used. DSC data showed the change in the endotherm with the melting points of Co-crystals. XRD spectra indicate the notified difference in the 2θ and the intensity of the peaks. Hence the Co-crystal formation could be helpful to improve the solubility, dissolution and micromeritic properties of Carvedilol

CRYSTAL FORMS OF LOMEFLOXACIN: PREPARATION, CHARACTERIZATION AND DISSOLUTION PROFILE

The present work was undertaken with the synthesis of crystal forms of Lomefloxacin from solvents of varying polarity (polar, protic solvents). The purpose of the present investigation was to employ crystallization techniques in order to improve the solubility and dissolution studies of Lomefloxacin. The experimental methods involved the preparation of lomefloxacin crystals by crystallization from single solvent technique. Crystals were prepared from solvents like distilled water, ethanol and methanol. Prepared crystals were undergone various studies in terms of crystal yield, melting point, true density, solubility and in vitro drug release study as well as characterized by technique viz: FT-IR, differential scanning calorimetry (DSC) and Powder X-ray Diffractometry(PXRD). Photomicrographs of the crystals shows that the crystals obtained from different solvents existed in different shape. Among all the crystals, LOME-I belongs to Type-1 and LOME–II belongs to Type-2 based on instrumental techniques. Highest crystal yield (88%) and maximum density (1.2021g/mL) was observed with LOME-I. Maximum solubility and dissolution rate was observed in LOME-III followed by LOME-II and LOME-I. However all prepared crystal forms showed higher solubility and dissolution profile when compare with commercial Lomefloxacin. It is concluded that the study has indicated the existence of two polymorphic forms of Lomefloxacin which was having better solubility and in vitro release than that of commercial Lomefloxacin.Key words: Polymorphism, Solubility, Dissolution rate, DSC, FT-IR, PXR

CRYSTAL FORMS OF LOMEFLOXACIN: PREPARATION, CHARACTERIZATION AND DISSOLUTION PROFILE

The present work was undertaken with the synthesis of crystal forms of Lomefloxacin from solvents of varying polarity (polar, protic solvents). The purpose of the present investigation was to employ crystallization techniques in order to improve the solubility and dissolution studies of Lomefloxacin. The experimental methods involved the preparation of lomefloxacin crystals by crystallization from single solvent technique. Crystals were prepared from solvents like distilled water, ethanol and methanol. Prepared crystals were undergone various studies in terms of crystal yield, melting point, true density, solubility and in vitro drug release study as well as characterized by technique viz: FT-IR, differential scanning calorimetry (DSC) and Powder X-ray Diffractometry(PXRD). Photomicrographs of the crystals shows that the crystals obtained from different solvents existed in different shape. Among all the crystals, LOME-I belongs to Type-1 and LOME–II belongs to Type-2 based on instrumental techniques. Highest crystal yield (88%) and maximum density (1.2021g/mL) was observed with LOME-I. Maximum solubility and dissolution rate was observed in LOME-III followed by LOME-II and LOME-I. However all prepared crystal forms showed higher solubility and dissolution profile when compare with commercial Lomefloxacin. It is concluded that the study has indicated the existence of two polymorphic forms of Lomefloxacin which was having better solubility and in vitro release than that of commercial Lomefloxacin

A study on Formulation and Evaluation of Gastroretentive tablet incorporating Ciprofloxacin Hydrochloride

Ciprofloxacin is a broad spectrum fluoroquinolone antibiotic effective in a broad range of infections including some difficult to treat ones. Because of wide-spectrum bactericidal activity, oral efficacy and good tolerability, it is used in Urinary tract infection, Gonorrhea, Bacterial gastroenteritis, Typhoid, Bone, soft tissue and gynecological infection, Respiratory infection and tuberculosis. The main objective of formulating the floating system was to reduce the frequency of administration, to improve patient compliance and improve bioavailability of drug by preparing a gastroretentive drug delivery system. Floating tablets of Ciprofloxacin hydrochloride were prepared by employing two different grades of control releasing polymers HPMC K4M and HPMC K100M in different concentration. Sodium bicarbonate was incorporated as a gas-generating agent. The tablets were evaluated for uniformity of weight, hardness, friability, drug content, floating behavior, swelling studies and dissolution studies. Among tablet formulations, formulation F3 showed maximum drug release i.e. 92.25% at the end of 12 h compared with other formulations and was concluded as optimized one. Keywords: Ciprofloxacin HCl, floating tablets, HPMC K4M, HPMC K 100M, FTIR