Relationship Between in Vitro Disintegration Time and in Vivo Release of Vitamins from a Triple-Dose Spaced-Release Preparation

The objective of the present investigation was to prepare oro dispersible tablets of ondansetron hydrochloride, because of its application in emesis condition, fast onset of action and avoidance of water is highly desirable. Tablets were prepared by direct compression using sodium starch glycolate and croscarmellose as superdisintegrants, as the combination of these two agents gives better disintegration of the tablet. Microcrystalline cellulose was used as diluent and mannitol, mint flavor, sodium saccharine to enhance the organoleptic properties of tablets. The tablets were evaluated for weight variation, mechanical strength, in vitro disintegration time, in vivo disintegration time, wetting time, and drug release characteristics. Hardness and friability data indicated good mechanical strength of tablets. The results of in vitro disintegration time and in vivo disintegration time indicated that the tablets dispersed rapidly in mouth within 3 to 5 seconds. Dissolution study revealed faster release rate of ondansetron hydrochloride from the tablets as compared to pure drug and marketed conventional tablet formulation of ondansetron hydrochloride. It was concluded that superdisintegrants addition technique is a useful method for preparing oro dispersible tablets by direct compression method

Download Full-text

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.6.9 ◽

2017 ◽

Vol 10 (6) ◽

pp. 3929-3936

Author(s):

Y. Srinivasa Rao ◽

K. Adinarayana Reddy

Keyword(s):

Drug Release ◽

Patient Compliance ◽

Onset Of Action ◽

In Vivo Evaluation ◽

Disintegration Time ◽

In Vitro Drug Release ◽

Surface Ph ◽

Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

Download Full-text

Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00824 ◽

2021 ◽

pp. 4736-4742

Author(s):

Sarika S. Malode ◽

Milind P. Wagh

Keyword(s):

Overactive Bladder ◽

Bitter Taste ◽

In Vitro Release ◽

In Vitro Dissolution ◽

Dissolution Time ◽

Disintegration Time ◽

Orodispersible Tablets ◽

Weight Variation

The objective of present work was to develop taste masked orodispersible tablets of mirabegron. Mirabegron is beta 3 adrenoceptor agonist used to treat overactive bladder. Overactive bladder (OAB) is defined as a symptom syndrome showing feeling of urgency to urinate, typically accompanied by frequent daytime and nocturnal urination, in the absence of proven infection or other obvious pathology. Over active bladders are generally common in geriatrics. Moreover, this drug has a very strong bitter taste. Frequent dosing requires frequent water intake, which further aggregates the condition of over active bladder and bitter taste of drug affects patient compliance. Hence a need arises to mask the bitter taste for development of an ODT which does not require consuming water with every dosage. In this work, the bitter taste of mirabegron was masked by forming a complex with an ion exchange resin tulsion 344. The drug resin complexation process was optimized for resin activation, drug: resin ratio, soaking time and stirring time. In –vitro release studies revealed complete drug elution from the complex within 10 minutes in pH 1.2 buffer. The taste-masked complex was then formulated into palatable orodispersible tablets using a direct compression approach by use of superdisintegrants to achieve a rapid disintegration. The tablets were evaluated for weight variation, hardness, friability, drug content, wetting time, In- vivo disintegration time and in-vitro dissolution time.

Download Full-text

In vitro and in vivo release of dinalbuphine sebacate extended release formulation: Effect of the oil ratio on drug release

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2017.08.083 ◽

2017 ◽

Vol 531 (1) ◽

pp. 306-312 ◽

Cited By ~ 3

Author(s):

Chan-Jung Li ◽

Mei-Yun Ku ◽

Chia-Yin Lu ◽

Yu-En Tien ◽

Wendy H. Chern ◽

...

Keyword(s):

Drug Release ◽

Extended Release ◽

Release Formulation ◽

Extended Release Formulation ◽

In Vivo Release

Download Full-text

In-vitro, ex-vivo, and in-vivo release evaluation of in situ forming buprenorphine implants using mixture of PLGA copolymers and additives

International Journal of Polymeric Materials ◽

10.1080/00914037.2018.1525541 ◽

2018 ◽

Vol 68 (16) ◽

pp. 965-977 ◽

Cited By ~ 1

Author(s):

Hossein Kamali ◽

Elham Khodaverdi ◽

Farzin Hadizadeh ◽

Seyed Ahmad Mohajeri ◽

Younes Kamali ◽

...

Keyword(s):

Ex Vivo ◽

In Situ Forming ◽

In Vivo Release

Download Full-text

QUALITY BY DESIGN (QBD) AS A TOOL FOR THE OPTIMIZATION OF INDOMETHACIN FREEZE-DRIED SUBLINGUAL TABLETS: IN VITRO AND IN VIVO EVALUATION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i5.42216 ◽

2021 ◽

pp. 160-171

Author(s):

MERVAT SHAFIK IBRAHIM ◽

NIHAL MOHAMED ELMAHDY ELSAYYAD ◽

ABEER SALAMA ◽

SHEREEN H. NOSHI

Keyword(s):

Response Surface ◽

Quality By Design ◽

Drug Dissolution ◽

Disintegration Time ◽

Optimization Study ◽

Freeze Dried ◽

Screening Study ◽

Wetting Time

Objective: This study aims to prepare and optimize indomethacin freeze-dried sublingual tablets (IND-FDST) by utilizing a quality by design (QbD) approach to achieve rapid drug dissolution and simultaneously bypassing the GIT for better patient tolerability. Methods: A screening study was utilized to determine the most significant factors which the quality attributes, namely disintegration time and % friability. Then an optimization study was conducted using a full response surface design to determine the optimized formula by varying the amount of the matrix-forming polymer (gelatin) and super disintegrant (croscarmellose sodium (CCS)). The variables' effect on the % friability, disintegration time, wetting time, and amount of drug release after 10 min (%Q10) was studied. The optimized formula was tested for compatibility, morphology as well as stability studies under accelerated conditions in addition to the in vivo pharmacodynamics in rats. QbD was adopted by utilizing a screening study to identify the significant formulation factors followed by a response surface optimization study to determine the optimized IND-FDST formulation. Results: Optimized IND-FDST comprised of gelatin/CCS combination in a ratio of 1:1 possessed adequate %friability (0.73±0.03%), disintegration time (25.40±1.21 seconds), wetting time (3.49±0.68 seconds), and % Q10 (100.99±5.29%) as well as good stability under accelerated conditions. IND-FDST also showed significant inhibition of edema, tumour necrosis factor-alpha, and interleukin-6 release in vivo compared to the oral market product by 70%, 42%, and 65%, respectively. Conclusion: QbD presents a successful approach in the optimization of a successful IND-FDST formula that showed superior in vivo and in vitro characteristics.

Download Full-text

Design Optimization and In Vitro-In Vivo Evaluation of Orally Dissolving Strips of Clobazam

Journal of Drug Delivery ◽

10.1155/2014/392783 ◽

2014 ◽

Vol 2014 ◽

pp. 1-15 ◽

Cited By ~ 8

Author(s):

Rajni Bala ◽

Sushil Khanna ◽

Pravin Pawar

Keyword(s):

Tensile Strength ◽

Drug Release ◽

Content Uniformity ◽

In Vivo Evaluation ◽

Disintegration Time ◽

Significant Difference ◽

Film Formulation ◽

Test Film

Clobazam orally dissolving strips were prepared by solvent casting method. A full 32 factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm2), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of Cmax (95.87%), tmax (71.42%), AUC0−t (98.125%), and AUC0−∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

Download Full-text

COMPARATIVE EVALUATION OF POLYMER COMBINATION IN THE DESIGN OF BRIMONIDINE TARTRATE OCULAR INSERTS

INDIAN DRUGS ◽

10.53879/id.49.07.p0030 ◽

2012 ◽

Vol 49 (07) ◽

pp. 30-35

Author(s):

P Goudanavar ◽

◽

N Ambhore ◽

D. Hiremath ◽

R Udupi

Keyword(s):

Polymer Concentration ◽

In Vitro Release ◽

Methyl Cellulose ◽

Carboxymethyl Chitosan ◽

Moisture Loss ◽

In Vivo Release ◽

Weight Variation ◽

Brimonidine Tartrate

Brimonidine is an anti-glaucoma agent useful in treatment of intraocular pressure. In the present study an attempt was made to formulate ophthalmic inserts of brimonidine tartrate (BT) in combination with polymers like methylcellulose, carboxymethyl chitosan and HPMC. Prepared ocular films were evaluated for uniformity in thickness, weight variation, % moisture absorption, % moisture loss, in vitro and in vivo release studies. The physical characteristics of the films were found to be within acceptable limits. The study confirmed that brimonidine tartrate can be delivered through films made of methyl cellulose, carboxymethyl chitosan and HPMC combination matrix cast with ethyl cellulose (EC). In vitro release study revealed that increasing the proportion of polymer concentration decreased the rate of release of brimonidine tartrate. In vivo release profile of ocular inserts revealed controlled release of drug over a period of 24 h. Optimized formulation CH3 was evaluated for in vivo release characteristics using rabbits as animal model. The optimized formulation CH3 was found to be stable at accelerated storage condition of 40/75 % RH.

Download Full-text

Formulation Development and Evaluation of Fast Dissolving Films of Oloptadine HCl

Asian Journal of Research in Pharmaceutical Science ◽

10.52711/2231-5659.2021-11-2-2 ◽

2021 ◽

Vol 11 (2) ◽

pp. 103-108

Author(s):

Ahirwar Varsha ◽

Khushwant S. Yadav ◽

Shailendra Bindaiya

Keyword(s):

Serotonin Receptor ◽

Formulation Development ◽

Onset Of Action ◽

Disintegration Time ◽

Percent Elongation ◽

Acid Hydrochloride ◽

H1 Receptor Antagonist ◽

In Vitro Disintegration

Our studies on the performance of formulation development and evaluation of fast dissolving films of Oloptadine HCL its anti-allergic drug. Prepare mouth dissolving film of Oloptadine HCl by solvent casting method. To characterize the prepared mouth dissolving film of Oloptadine HCL in terms of— Thickness, percent elongation, tack test, swelling index, in-vitro disintegration time and dissolution test. Oloptadine OLO), 11-[{z}-3-(Dimethlamino) propylidene]-6-11-dihydrobenz [b, e] oxepin-2-acetic acid hydrochloride, is widely used as an antihistaminic. Oloptadine HCL is a relatively selective histamine H1-receptor antagonist that inhibits the release of histamine from mast cells. Oloptadine does not affect alpha-adrenergic dopamine, muscarinic type 1 and 2 or serotonin receptor. They are hydrophobic in nature and non-polar, sparingly soluble in water and freely soluble methanol, ethanol. Olopatadine HCl is a mouth dissolving film. We is trying to sort out the problem of allergic. They are rapidly onset of action, when placed upon the tongue that it is disperse rapidly swallowing within 3-5 seconds without need of water or chewing.

Download Full-text