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A SYSTEMATIC REVIEW ON DEVELOPMENT AND EVALUATION OF CONTROLLED RELEASE AND FAST DISSOLVING FORMULATIONS FOR ANTI-DIABETIC DRUGS OVER PAST DECADE

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A SYSTEMATIC REVIEW ON DEVELOPMENT AND EVALUATION OF CONTROLLED RELEASE AND FAST DISSOLVING FORMULATIONS FOR ANTI-DIABETIC DRUGS OVER PAST DECADE

Manojkumar K. Munde * 1, 2, Nilesh S. Kulkarni 2 and Dhanya B. Sen 1

Department of Pharmacy 1, Sumandeep Vidyapeeth Deemed to be University, Piparia, Vadodara - 391760, Gujarat, India.

PES Modern College of Pharmacy (for Ladies) 2, Moshi, Pune - 412105, Maharashtra, India.

ABSTRACT: Diabetes mellitus is the heterogeneous metabolic disorder caused by the high blood sugar level. Untreated high blood sugar can damage kidneys, eyes, nerves and other organs. Type 1 diabetes mellitus disorder is caused by the lack of insulin hormone while type 2 diabetes mellitus is a disorder of insulin resistance by β cells of the pancreas. For the management of type 2 diabetes mellitus different drugs are available as single or combination forms like Pioglitazone, Repaglinide, Metformin, Voglibose, Glipizide. Several research activities were carried out for its development, formulation and evaluation by the development of controlled-release and fast-dissolving formulations. The extensive literature review revealed information related to the formulation of sustain/fast release dosage form for the antidiabetic drugs. Newer techniques were used by the researcher for the formulation of dosage forms as solvent diffusion-evaporation technique, Reverse phase evaporation technique, emulsion solvent evaporation technique and Hot melt extrusion granulation technique. The review represents the types of formulation, methods used, excipients used and evaluation parameters of developed dosage forms and their correlation with therapeutic success.

Keywords:

Diabetes mellitus, Formulations, Excipients, Evaluation

INTRODUCTION: Diabetes mellitus is the heterogeneous metabolic disorder caused by the high blood sugar level. Insulin moves sugar from the blood into cells and used as energy. Untreated high blood sugar can damage kidneys, eyes, nerves, and other organs 1. There are two important types of diabetes mellitus.

a) Type 1 Diabetes Mellitus: Type 1 diabetes mellitus is caused by the lack of insulin hormone. In type 1 diabetes mellitus use of insulin is required and which is given to the patient in injection form.

b) Type 2 Diabetes Mellitus: Type 2 diabetes mellitus is the common type of diabetes, and it is a disorder of insulin resistance by β-cells of the pancreas. In this condition, treatment includes the use of oral drugs, which increases the amount of insulin secreted by β-cells of pancreas 2.

There are different ways for the classification of antidiabetic drugs, which depend on nature, age, and lifestyle of the person as well as other factors 3.

FIG. 1: CLASSIFICATION OF ANTIDIABETIC DRUGS

Glibenclamide (GB): Glibenclamide is a sulfonylurea derivative and it is used for treatment of type 2 diabetes mellitus. Its route of administration is oral. It undergoes the hepatic first-pass effect and has a short half-life. The patient has to take the drug in several divided doses to maintain the desired therapeutic effect 4.

Gliclazide (GC): Gliclazide is a sulfonylurea derivative, and it is used for type 2 diabetes mellitus. The daily dose of gliclazide is 40 mg daily and increases upto the 320 mg daily. Gliclazide has high bioavailability (100%) from tablets, and absorption is not affected by food. The half-life of this drug is approximately 11 h 5, 6.

Glimepiride (GM): Glimepiride is the first drug under third-generation sulfonylurea; it is very potent and has a long duration of action. Glimepiride is used for the treatment of type 2 diabetes mellitus. It causes hypoglycemia by stimulating the release of the insulin from pancreatic β-cells and raising the sensitivity of peripheral tissue to the insulin. Glimepiride also has an ability to promote the movement of sugar from the blood to the β-cells 7.

FIG. 2: SITE OF ACTION OF ANTIDIABETIC DRUGS

Pioglitazone (PZ): Pioglitazone comes under the class of thiazolidinedione. It is used in the treatment of type 2 diabetes mellitus. Pioglitazone is BCS class II drug category and has poor aqueous solubility. Pioglitazone shows a delayed onset of action 8.

Repaglinide (RG): Repaglinide is an oral antihyperglycemic agent and also known as meglitinide. It also acts as binding to β cells of the pancreas and stimulates insulin release. Repaglinide comes under the BCS class II drug category. In the upper part of the intestinal tract, it is poorly absorbed. It is an extensive hepatic first-pass metabolism and bioavailability up to 56 % 9.

Metformin (MF): Metformin is a widely accepted, oral antihyperglycemic agent. It comes under the BCS class III drug category and it has the site-specific absorption in the gastrointestinal tract and bioavailability up to 60%. The half-life of the drug is 1.5 to 4.5 h and the recommended dose is 500 mg two or three times daily 10.

Voglibose (VB): Voglibose is an alpha-glucosidase inhibitor used in the treatment of lowering the blood glucose level in diabetic patients. It also has the ability to increase glucagon-like peptide (GLP)-1 secretion in humans 11.

TABLE 1: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2010

S. no. API Type of formulation and method used Excipient used Evaluation parameters Ref. no.
Parameter outputs
1 Glipizide Sustained-release Glipizide microspheres

emulsion (solvent diffusion-evaporation

technique)

 Eudragit® S100, Ethyl cellulose, ethanol, Dichloromethane, n-butanol Particle size range 71-289(mm) 12
% Recovery yield 96.26 ± 2.15%
Encapsulation efficiency 26.79±2.57 %
Drug release at 12 h 100.91± 2.86%
2 Acarbose Sustained release matrix tablets (Direct compression technique) Hydroxypropyl Methyl cellulose (HPMC),

Eudragit, Lactose

Microcrystalline Cellulose (MCC), Talc, Magnesium (Mg.) stearate

 Uniformity of weight 352±2.11(mg) 13
Friability 0.36±0.02 %
Crushing strength 5.4±0.71 (Kg/cm2)
% of polymer to the total tablet weight 42.9 %

TABLE 2: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2011

S. no. API Type of formulation and

method  used

 Excipient Used Evaluation parameters Ref. no.
Parameter outputs
3 Glimepiride and Parecoxib

combination

 Mucoadhesive tablet (Direct

compression technique)

 HPMC K4M, Carbopol-934P, Sodium Carboxy Methylcellulose-H, Poly vinyl Pyrrolidone-K30 (PVP), Saccharin sodium, Amaranth, Ethanol, Mg.

stearate

 Average weight 200±2.562 (mg) 14

 

 
Thickness 8.1±0.0469 (mm)
SurfacepH 6.68 ± 0.15
Water absorption 49.99 ±1.22%
Mucoadhesion

strength

 23.68 ±2.59

(g)
Drug content 99.97±8.54%
4 Metformin HCl and Pioglitazone HCl combination Floating bilayer tablets (Direct compression technique) HPMC K4M, HPMC E-15, Carbopol, Sodium, bicarbonate, Citric acid, Mg.  stearate, Lactose, PVP Hardness 3.5 ± 0.35 (Kg/cm2) 15
Thickness 0.35 ± 0.15 (mm)
Weight variation 5.1 ± 0.98%
Floating lag time 2 ± 0.28 min
Floating duration 12 ± 1.8 h
Drug content 97 ± 1.1%

TABLE 3: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2012

S. no. API Type of formulation and method used Excipient used Evaluation parameters Ref. no.
Parameter            Outputs        
5 Glimepiride Sustained release matrix tablets (Direct compression) HPMC (15cps), Hyderxypropyl cellulose (HPC), Ethylcellulose, MCC, Mg. stearate, Talc Thickness 3.80±1.20 (mm) 16
Hardness 3.20±0.40 (Kg/cm2)
Friability 0.24±0.12%
Drug content 99.42±1.46%
In-vitro release study (at the end of 12 h) 99.93%
6 Glimepiride Immediate-release tablets (Wet granulation Technique) Lactose Monohydrate, Croscarmellose

(CCS), Sodium starch glycolate (SSG), Povidone k 30, Avicel PH 102, Mg. stearate St-arch

 Weight

Variation

 399.9±0.74% 17
Hardness 3.5±0.35 (Kg/cm2)
Friability 0.12±0.00 %
Disintegration time 58.5±0.35 min
Assay

 

 98.3 %

 

TABLE 4: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2013

S. no. API Type of formulation and method used Excipient used Evaluation parameters Ref. no.
Parameter            Outputs        
7 Metformin HCl

 

 Niosomes (Reverse phase evaporation (REV) technique)

Matrix tablet

(Nonaqueous wet granulation technique)

 Span, Cholesterol,

Diabasic calcium phosphate (DCP), Dioleoyltrimethyl ammonium-propane (DOTAP)

 Mean particle size 223.5±2.7 µm 18
Polydispersity index 0.38±0.1
Zeta potential +8.7±1.2 mV
Entrapment efficiency 83.36%
8 Metformin HCl and Glipizide combination HPMC K 4M, HPMC K 15M, HPMC K 100M, Starch, PVP K-30, Lactose, Citric

acid, Sodium bicarbonate, MCC, Erythrosine lake, Talcum powder, Mg. stearate

 Weight

Variation

 0.43 ± 0.02% 19
Friability 0.21 ±0.06%
Hardness 8.00 ± 0.27 (Kg/cm2)
Thickness 7.48 ± 0.05(mm)
Drug content 99.01±0.12%
In-vitro release 94.83%

TABLE 5: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2014

S. no. API Type of formulation and method used Excipient used Evaluation parameters Ref. no.
Parameter Outputs
9 Gliclazide Modified release tablet

(Wet granulation technique)

 HPMC K15M, HPMC K100M, Ethyl Cellulose, Sodium bi-carbonate, Mg. sterate, Talc, Lactose Weight variation 507.2 ± 0.63 % 20
Hardness 4.35 ±0.24 (Kg/cm2)
Friability 0.025 %
Drug content 96.57 ± 0.039 %
First-order 0.973
10 Metformin HCl and Acarbose combination Bilayer tablets (Solid dispersions technique) Eudragit RS100 , Eudragit RLPO, Potassium permanganate, Caboxymethyl cellulose sodium,

MCC, Mg. stearate, Polyethylene glycol (PEG) 6000, PVP K30

 Weight 1530  ±20.20(mg) 21
Thickness 7.2±  0.057 (mm)
Hardness 12.5 ± 0.046 (Kg/cm2)
Friability 0.55±  0.011%
Drug content 98.4%
Disintegration

time

 48min
Swelling 30.7%
11 Metformin HCl Extended-release tablets (Wet granulation technique)

granulation technique

 MCC PH 102, HPMC (K4M, K200M, K15M, K100M), Aerosil, Povidone, Mg. stearate, Isopropyl alcohol(IPA) Thickness 5.9(mm) 22
Weight variation 799± 0.7%
Friability 0.30%
Hardness 7.1 (Kg/cm2)
% Drug

content

 100%
In-vitro drug release 53.7%

 TABLE 6: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2015

S. no. API Type of formulation and method  used Excipient used Evaluation parameters Ref. no.
Parameter Outputs
12 Glimepiride Sustained release tablet

(Direct compression technique)

 Carbopol , Ethylcellulose, Methocel K4 MCR, K15 MCR, K100 MCR, Xanthum gum, Lactose, Povidone K-30 Mg. stearate,

Talc

 Average weight 378 ±0.8 (mg) 23
Average diameter 13.24 ± 0.36 (mm)
Average thickness 2.26 ± 0.32 (mm)
Friability 0.352%
Hardness 20.91 ± 0.053 (Kg/cm2)
Radial tensile strength 0.445 (Kg/mm2)
Axial tensile

strength

 0.151 (Kg/mm2)
13 Metformin HCl Effervecent floating tablets (Wet granulation technique) HPMC K 100M,

HPMC K 200 CR ,

Corbopol 941 P,

MCC pH 101,

PVP-30K, HPMC K 100 L, Sodium bicarbonate, Colloidal silicon dioxide, Mg. stearate.

 Weight variation test 0.54 % 24
Thickness

Diameter

 5.12 (mm)
Hardness 13.9 (Kg/cm2)
Friability 0.782 %
Floating lag time 60 min
Duration of floating 12 h
14 Glimepiride Fast dissolving tablets (Direct compression technique) Avicel PH 101, Mannitol, Cross povidone, Sodium saccharin, Sodium lauryl sulfate (SLS), Mg. stearate, SSG, CCS Hardness 3.2 (Kg/cm2) 25
Friability 0.41%
Thickness 2.5 (mm)
Average weight of

tablet

 126 (mg)

 
Wetting time 144 (Sec)
Drug content 99.2%
Disintegration time 116 (sec)
15 Pioglitazone

HCl

 

 Control release tablet

(Solid dispersion by kneading technique)

 HPMC K4M ,

Ethylcellulose,

MCC, Mg. stearate

 

 Diameter 7.96±0.049 (mm) 26
Thickness 2.2±0.45 (mm)
Average weight 278.29±6.60 (mg)
Hardness 5.0±0.356 (Kg/cm2)
Friability 0.574±0.55 %
Drug content 98.83±2.053%
16 Repaglinide Mucoadhesive microspheres

(Double emulsion technique)

 Polycarbophil,

Dichloromethane, Span80, Liquid paraffin, N-hexane

 Mean particle size 24.30 +1.00 µm 27
Percentage of drug

entrapment

efficiency

 78.9%
Percentage mucoadhesion 84.11%
17 Repaglinide Nanoemulsion

(o/w nanoemulsion technique)

 Oleic acid, Isopropyl

myristate (IPM), Glycerol triacetate (Triacetin), Caproyl 90, Propylene glycol (PG), Monocaprylic ester (Sefsol 218), Propylene glycol laurate

 Droplet size 97.15±9.16 μL 28
Polydispersity

index

 0.198±0.017
Viscosity 23.857±0.541 cP
Refractive index 1.8502±0.008
Conductivity 501.18±5.76 S/m

TABLE 7: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2016

S. no. API Type of formulation and method used Excipient used Evaluation parameters Ref. no.
Parameter Outputs
18 Glimepiride

 

 Fast disintegrating tablets (Direct Compression technique) CP,SSG, CCP, MCC, Mg. stearate, Aerosil, Erythritol, Orange flavor Weight variation 99.75±0.89% 29
Thickness 2.2±0.18 (mm)
Hardness 2.8±0.08 (Kg/cm2)
Friability 0.72±0.11 %
Drug content 98±0.37 %
In-vitro dissolution studies 14.25 h
In-vivo disintegration time 26±0.39 min
Uniformity of weight 920.45±8.525 (mg)
19 Metformin HCl, Pioglitazone and Glimepiride combination Core-in-cup tablet (Direct compression technique) HPMCK100,

PVPK30, Microcrystalline cellulose powder

(MCCP), Mg. stearate, Talc, Aerosil, SSG, SLS

 Thickness 7.02±0.052 (mm) 30
Diameter 13.08±0.018(mm)
Hardness 6.92±0.582 (Kg/cm2)
Friability 0.42±0.055 %
Disintegration time 2.15±0.062 min
Drug content 101.42±0.548%
Floating lag time 5.2 min
20 Metformin and Sitagliptin combination Bilayer tablets

(Direct compression technique)

 HPMC K100M, Sodium carboxy methyl cellulose, Lactose, MCC, Pre gelatinized starch, CCS, SSG, Crosspovidone, Sodium bicarbonate, Mg. stearate, IPA, Ferric iron oxide red Total floating time 18- 24 h 31
Tablet density 0.846 g/ml
Swelling study 97.61%
Average weight 945.07 ±1.38 (mg)
Hardness 6.7 ± 0.5 (Kg/cm2)
Thickness 6.5 ± 0.63 (mm)
Friability 0.75%
Drug content 99.67 ±0.42 %
Disintegration time 52 ± 2.5 min
Cumulative % drug release 92.20%
In-vitro drug release 97.65%
Weight variation 449.25±1.82%
21 Acarbose Floating tablets

(Direct compression technique)

 HPMC K4M, Carbopol-934P, Sodium bicarbonate, Tartaric acid, Citric acid, Lactose, Talc, MCC, Mg. stearate Hardness 4.58±0.192 (Kg/cm2) 32
Friability 0.1592±0.0196 %
Thickness 5.60±0.0088 (mm)
Diameter 11.22±0.00095 (mm)
Percentage of drug

content

 96.83±6.18%
Lag time 38.33 ± 3.55 min
Swelling study 96%
Avg. Wt 319.2±0.8 (mg)
22 Nateglinide Sustained released tablet (Direct compression technique) HPMC K15M, Xanthum gum, Guar gum, Avicel PH 102, Mg.stearate, Talc Thickness 4.91±0.23 (mm) 33
Hardness 5.6±0.152 (Kg/cm2)
% Friability 0.68 %
% Drug content 100.21±0.20 %
In-vitro dissolution

study

 95%

 
Thickness 0.4 (mm)
23 Glibenclamide and  Metformin HCl combination Bilayer matrix Tablet (Direct compression technique) Lactose, MCC,

Mg. stearate, Aerosil,

Starch, HPMC K100M, HPMC 4KM

 Diameter 1.3 (mm) 34
Hardness 4 (Kg/cm2)
Weight variation 4.2%
Friability 0.7%
Assay 99.73%
% yield 80%
24 Nateglinide Floating microspheres

(Emulsion solvent evaporation technique)

 Ethylcellulose, Eudragit S-100, Ethanol, Dichloromethane, Tween-80 Average particle size 66 µm

 

 35
Percentage floating 78%
Floating time 15 min
Drug entrapment

efficiency

 85.95%

TABLE 8: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2017

S. no. API Type of formulation and method used Excipient used Evaluation parameters Ref. no.
Parameter Outputs
25 Glimepiride Sublingual tablet (Direct compression technique) Mg-stearate, Mais starch, Sucralose, Lemon flavor, Aerosil 200, Aerosil, Flulac, Dicalcium phosphate Assay 103% 36
Friability 0.40%
Weight variation 0.1141%
Hardness 4.5(Kg/cm2)
Disintegration time 21 sec
26 Glimepiride Sustained release matrix tablet

(Direct compression technique)

 HPMCK4, PVA, Carbopol, Mannitol, MCC, Talc,L actose Weight variation 351.66±0.47% 37
Hardness 7.25±0.014 (Kg/cm2)
Friability 0.67±0.014%
Thickness 6.46±0.094(mm)
Content uniformity 99.51±0.004 %
In-vitro drug release 94.864 %
27 Pioglitazone HCl Control

release tablets

 

 HPMC K4M, Ethyl cellulose, MCC, Mg. stearate Hardness 5.5±0.324(Kg/cm2) 38
Friability 0.553±0.34%
Drug Content 99.314±2.02%
In-vitro drug release 98.73±2.12%
28 Pioglitazone HCl Mouth dissolving tablets (Direct compression technique)

 

 Crospovidone , CCS, SSG, MCC, Lactose, Talc, Mg. stearate, Aspartame Hardness 3.7 (Kg/cm2) 39
Friability 0.68%
Thickness 4.23(mm)
Disintegration time 34 min
Wetting time 98.3 sec
Drug content 96.5%
29 Pioglitazone HCl Mouth dissolving tablets (Wet granulation technique) Crospovidone, CCS, SSG, MCC, Lactose, Talc, Mg. stearate, Aspartame Hardness 3.5(Kg/cm2)
Friability 0.74%
Thickness 4.25(mm)
Disintegration time 27 min
Wetting time 14 sec
Drug content 96.5%
30 Nateglinide Buccal films (solvent evaporation technique) Chitosan, Carbopol, PVP, HPMC, PG Thickness 0.48 ±0.02 (mm) 40
Weight 178.23 ±0.91 (mg)
Fold. end 320±5.0
Surface pH 6.73±0.005
Percentage moisture absorption (PMA) 5.21±0.07%
Percentage moisture loss (PML) 5.97±0.12%
Swelling percentage 120.9±0.9%
Drug content 49.50±0.22%

TABLE 9: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2018

S. no. API Type of formulation and method  used Excipient used Evaluation parameters Ref. no.
Parameter Outputs
31 Metformin  HCl Orodispersible tablets (Direct compression technique) Treated agar, Avicel-101,

Mg. stearate,

Talc, Manitol

 Hardness 4±0.23 (Kg/cm2) 41
Friability 0.4 %
Wetting time 26.66 sec
In-vitro dispersion time 15.60 sec
Disintegration time 11.4 min
Drug content 7.82 %
32 Glimepiride

 

 Sustained release tablet (Direct compression technique) Tamrind seeds, Ethylcellulose, MCC, Lactose, Talc, Mg. stearate Diameter 7.98±0.021 (mm) 42
Thickness 4.1±0.05 (mm)
Weight variation 323.79±0.59%
Hardness 6.2±0.08%
Friability 0.56±0.00%
Drug content 100.55±0.021%
33 Pioglitazone HCl

 

 Immediate release tablets (Direct Compression technique) CCS: CP, CP: SSG, SSG: CCS,

MCC, Lactose, Talc, Magnesium dioxide (MgO)

 Hardness 4.2 ±0.027 (Kg/cm2) 43
Friability 0.92±0.212 %
Thickness 3.2±0.40 (mm)
Disintegration time 19±1.63 min
Wetting time 40±0.21 min
Drug content 98.7±0.102 %
In-vitro drug Release 99.3±0.33 %
34 Pioglitazone HCl and Metformin HCl combination Dual release tablet (Hot melt Granulation technique) Avicel PH 102, Copovidone, SSG, Crospovidone, Red iron oxide,

Mg. stearate

 Average weight 1052±4.9 (mg) 44
Thickness 5.99±0.02 (mm)
Hardness 85 ± 4.18 (Kg/cm2)
Friability 0.21%
Disintegration time 68 min
Assay 99.82%
35 Nateglinide Floating tablets (Direct compression technique) Ethyl Cellulose, Carbopol 930,

Sodium bicarbonate,

citric acid,

PVP k-30, Talc,

Mg. stearate

 Weight variation 499 ± 0.236 % 45
Thickness 5.6 ± 0.03 (mm)
Hardness 5.5 ± 0.237 (Kg/cm2)
Friability 0.35 ± 0.078%
Drug content 100.99 ± 0.14%
Total floating time ˃24 min
In-vitro drug release studies 98.92%
36 Repaglinide Sustained release matrix (Wet granulation technique) HPMC K 100M, HPMC K4M, HPMC K 15M, Talc, PVP K30, Calcium Stearate, CCS, IPA Thickness 1.87±0.09 (mm) 46
Hardness 6.2±0.10

(Kg/cm2)
Friability 0.30±0.17%
Drug content 99.14%
In-vitro dissolution study 99.15%
37 Empagliflozin Spherical agglomerates (Direct compression technique) Caesalpinia spinosa, HPMCK100M,

Sodium alginate,

Mg. sterate, MCCPH112

 Diameter 7.03±0.03 (μm) 47
Thickness 2.49±0.04 (mm)
Hardness 8.31±0.05(Kg/cm2)
Friability 0.41±0.03%
Drug content 99.85±0.13%

TABLE 10: RESEARCH WORK CARRIED OUT BY RESEARCHERS FOR ANTIDIABETIC FORMULATION AND EVALUATION PUBLISHED IN 2019

S. no. API Type of formulation and method used Excipient used Evaluation parameters Ref. no.
parameter Outputs
38 Gliclazide Poorly water-soluble Gliclazide tablet (Direct compression technique) Starch-1500, Spray-dried Lactose, SSG, Mg. stearate, Cross povidone Weight variation 1.17 ± 0.05% 48
Friability 0.16 ± 0.04 %
Hardness 3.2 ± 0.45 (Kg/cm2)
Disintegration time 21 ± 3.0 min
Drug content 99.87 ± 0.51%
39 Canagliflozin Solid Dispersions (Solvent evaporation method) Eudragit® E PO, Methyl methacrylate, Solubility in distilled water 0.10 ± 0.005 (mg/ml) 49
Solubility in 0.75% SLS solution 10.08 ± 0.506

(mg/ml)
In-vitro dissolution 80%

CONCLUSION: Over the past decade, several research were carried out for the development and evaluation of fast dissolving and controlled release formulations for anti-diabetic drugs. For the drug which possesses limited or poor solubility were considered for solubility enhancement approaches. Various formulations were developed with improved solubility by using techniques as wet granulation, niosomal drug delivery, nanoemulsion, sublingual tablets, buccal films, mouth dissolving tablets, orodispersible tablets, spherical agglomerates and solid dispersion. This resulted in improvement of drugs bioavailability. Similarly, sustain or control release dosage forms were developed with the purpose of maintaining drug concentration within a therapeutic range over a period of time.

This is achieved through the development of floating tablets, effervescent floating tablets, floating or mucoadhesive tablets. Such dosage forms were useful for the chronic treatment of type 2 diabetes mellitus. This review emphasizes on the management of type 2 diabetes mellitus through the formulation of a dosage form to maintain blood sugar level, which resulted in patient compliance.

ACKNOWLEDGEMENT: The authors are very grateful to the Principal and Management of Department of Pharmacy, Sumandeep Vidyapeeth Deemed to be University for providing necessary facilities for the completion of this literature review.

CONFLICTS OF INTEREST: Nil

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    How to cite this article:

    Munde MK, Kulkarni NS and Sen DB: A systematic review on development and evaluation of controlled release and fast dissolving formulations for anti-diabetic drugs over past decade. Int J Pharm Sci & Res 2020; 11(10): 4874-83. doi: 10.13040/IJPSR.0975-8232. 11(10).4874-83.

    All © 2013 are reserved by the International Journal of Pharmaceutical Sciences and Research. This Journal licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 3.0 Unported License.

Article Information

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4874-4883

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English

IJPSR

M. K. Munde *, N. S. Kulkarni and D. B. Sen

Department of Pharmacy, Sumandeep Vidyapeeth Deemed to be University, Piparia, Vadodara, Gujarat, India.

manojpcist@gmail.com

18 October 2019

19 June 2020

25 August 2020

10.13040/IJPSR.0975-8232.11(10).4874-83

01 October 2020

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